Lack of dietary fiber contributes to many health issues, particularly chronic vascular diseases. Mixed linkage β-1.3 - 1.4 beta-glucan (beta-glucan, in this paper) is a confirmed beneficial ingredient for the human d...Lack of dietary fiber contributes to many health issues, particularly chronic vascular diseases. Mixed linkage β-1.3 - 1.4 beta-glucan (beta-glucan, in this paper) is a confirmed beneficial ingredient for the human diet through reduction of cholesterol and the glycemic index. Barley contains the highest beta-glucan content of all the grains, and in this study, a percentage of flour from two high beta glucan lines was, each, added to an array of wheat-based food products to measure how it impacted total dietary fiber. Results showed that beta-glucan content was higher in all the products containing the added high beta-glucan flour, along with increased total dietary fiber content. Protein content in the food products is also increased with the higher protein in the barley flours added. Beta-glucan content in the barley-added products increased to 1.2% - 4.0% versus 0.2% - 0.5% in the pure wheat products, while the dietary fibers increased to 3.5% - 24.4% versus 2.1% - 9.1% in pure wheat product controls. This research provided experimental evidence that using a high beta-glucan barley ingredient in food can increase dietary fiber to benefit health.展开更多
The active ingredients of Camellia japonica flowers(CJF)at high and low altitudes,as well as their skin care efficacy were compared.The dried red CJF at high and low altitudes were ultrasonically extracted with 70%eth...The active ingredients of Camellia japonica flowers(CJF)at high and low altitudes,as well as their skin care efficacy were compared.The dried red CJF at high and low altitudes were ultrasonically extracted with 70%ethanol,and these extracts were concentrated and then diluted to a constant volume.The content of total flavonoids,total polyphenols and total proteins was tested and analyzed.In addition,DPPH free radical scavenging,inhibition of the formation of advanced glycation end products,and inhibitory activity against elastase was measured to compare their skin care efficacy in anti-oxidation,anti-glycation,anti-wrinkling and firming.The results showed that,based on the dry weight of CJF,the content of total flavonoids and total proteins of the CJF at high altitude was approximately 1.5 times of the CJF at low altitude,while the content of total polyphenols was approximately 2.4 times that of the CJF at low altitude.The skin care efficacy of CJF at high altitude was significantly better than that of the CJF at low altitude.This work could provide theoretical basis for the selection and application of Camellia japonica flowers in the field of cosmetics.展开更多
This article explores China’s state-level knowledge production on medicinal ingredients in northwestern Sichuan in the 1950s.Drawing on county-level archives,published materials and interviews,this historical article...This article explores China’s state-level knowledge production on medicinal ingredients in northwestern Sichuan in the 1950s.Drawing on county-level archives,published materials and interviews,this historical article traces how different levels of governments and state-owned trading companies produced knowledge about medicinal ingredients and its production.It argues that on one hand the state’s procurement standards codified the knowledge about medicinal ingredients from the marketplace and the local producers.On the other hand,direct extraction of knowledge from the medicine gatherers and cultivators verbalized and collected the previously tacit local knowledge about the production of medicinal ingredients,which would help to alleviate the shortage in the supply of traditional Chinese medicines throughout the 1950s.展开更多
[Objectives]To analyze the effect of Mongolian pharmaceutical Betel Shisanwei Ingredient Pills in the clinical treatment of patients with depression.[Methods]From June 2020 to May 2021,64 patients with depression who ...[Objectives]To analyze the effect of Mongolian pharmaceutical Betel Shisanwei Ingredient Pills in the clinical treatment of patients with depression.[Methods]From June 2020 to May 2021,64 patients with depression who received treatment in Inner Mongolia Minzu University were selected to participate in this study.These patients were randomly numbered from 1 to 64,and then divided into two groups according to the principle of odd or even number.Patients with odd number were regarded as the reference group,and treated by western medicine fluoxetine;patients with even number were regarded as the study group,and treated by Mongolian pharmaceutical Betel Shisanwei Ingredient Pills.The therapeutic effects of the two groups of patients were compared.[Results]Before treatment,there was no significant difference in the scores of patients'depressive syndromes between the two groups(P>0.05).After treatment,there were two significant changes in comprehensive score of depressive symptoms in both groups.Compared with before treatment,the data of the same group after treatment decreased significantly.Comparison between the two groups showed that the score of patients'depressive syndromes in the study group(13.28±5.49)was significantly lower than that in the reference group(18.46±6.51),and the overall response rate of treatment in the study group(96.88%,31/32)was obviously higher than that in the reference group(75.00%,24/32),showing statistically significant differences(P<0.05).[Conclusions]In the treatment of depression,Mongolian medicine therapy can significantly improve the depressive syndromes in patients,with more prominent curative effects,and is worthy of promotion and application.展开更多
In the development of new drugs products,especially the development of traditional Chinese medicine active ingredients,solubility and oral bioavailability are the main factors which are restricting the development of ...In the development of new drugs products,especially the development of traditional Chinese medicine active ingredients,solubility and oral bioavailability are the main factors which are restricting the development of new drugs,whereas the physicochemical properties of active ingredients are the key element to affecting these factors.Pharmaceutical cocrystal provides an excellent opportunity to develop new drugs with excellent physical and chemical properties such as melting point,solubility,stability and bioavailability while retaining the pharmacological properties of individuals active pharmaceutical ingredients among pharmaceutical cocrystal compounds.Traditional Chinese herbal medicine has the characteristics of multiple pathways and multiple targets,mainly because it contains many active ingredients,like cocrystals thereof with many components.The active ingredients extracted from traditional Chinese herbal medicine have a wide range of pharmacological activities,but most of the active ingredients affect the development of traditional Chinese medicine active ingredients due to their physical and chemical properties such as solubility.Traditional Chinese medicine pharmaceutical cocrystals can not only improve the physical and chemical properties of drugs without changing the internal structure of drugs,so as to provide a new scheme for the development of traditional Chinese medicine active ingredients.This paper reviews the research progress of active ingredients of traditional Chinese medicine pharmaceutical cocrystal.The preparation methods of cocrystals are summarized and the advantages of cocrystals are illustrated with examples.展开更多
People continue to recognize the important role of Chinese medicine in the treatment of diseases,and there is an urgent need to clarify the mechanism of Chinese medicine.Because of the multi-target and multi-component...People continue to recognize the important role of Chinese medicine in the treatment of diseases,and there is an urgent need to clarify the mechanism of Chinese medicine.Because of the multi-target and multi-component characteristics of traditional Chinese medicine,it is difficult to elaborate from a single perspective.As a high-quality animal model,Caenorhabditis elegans with the characteristics of small size and fast reproduction,has been widely used in traditional Chinese medicine activity experiments.In this article,Caenorhabditis elegans,as model organisms used to screen the active components of traditional Chinese medicine were reviewed.展开更多
In the past two decades, a considerable amount of research has focused on the determination of the digestible(DE) and metabolizable energy(ME) contents of feed ingredients fed to swine. Compared with the DE and ME sys...In the past two decades, a considerable amount of research has focused on the determination of the digestible(DE) and metabolizable energy(ME) contents of feed ingredients fed to swine. Compared with the DE and ME systems, the net energy(NE) system is assumed to be the most accurate estimate of the energy actually available to the animal. However, published data pertaining to the measured NE content of ingredients fed to growing pigs are limited. Therefore, the Feed Data Group at the Ministry of Agricultural Feed Industry Centre(MAFIC) located at China Agricultural University has evaluated the NE content of many ingredients using indirect calorimetry. The present review summarizes the NE research works conducted at MAFIC and compares these results with those from other research groups on methodological aspect. These research projects mainly focus on estimating the energy requirements for maintenance and its impact on the determination, prediction, and validation of the NE content of several ingredients fed to swine. The estimation of maintenance energy is affected by methodology, growth stage,and previous feeding level. The fasting heat production method and the curvilinear regression method were used in MAFIC to estimate the NE requirement for maintenance. The NE contents of different feedstuffs were determined using indirect calorimetry through standard experimental procedure in MAFIC. Previously generated NE equations can also be used to predict NE in situations where calorimeters are not available. Although popular, the caloric efficiency is not a generally accepted method to validate the energy content of individual feedstuffs. In the future,more accurate and dynamic NE prediction equations aiming at specific ingredients should be established, and more practical validation approaches need to be developed.展开更多
In this study, the IL-2 mRNA levels of T lymphocytes in normal mice stimulated by nine Chinese herbal medicinal ingredients (CHMIs) were measured using semiquantification reverse transcription polymerase chain react...In this study, the IL-2 mRNA levels of T lymphocytes in normal mice stimulated by nine Chinese herbal medicinal ingredients (CHMIs) were measured using semiquantification reverse transcription polymerase chain reaction. The results showed that astragalus polysaccharide (APS), epimedium polysaccharide (EPS), Chinese angelica polysaccharide (CAPS), propolis flavone (PF), and astrogalosides (AS) promoted IL-2 mRNA levels in T lymphocytes in vitro and in vivo to differing degrees, and the level of IL-2 mRNA induced by propolis polysaccharide (PPS) in vitro was higher than that induced by the control, which differed from that of PPS in vivo.展开更多
The topical administration of the compound Chinese herbal medicine transdermal preparation has been widely used in treating the mastitis of cows. In order to understand the metabolic process, four cows suffering from ...The topical administration of the compound Chinese herbal medicine transdermal preparation has been widely used in treating the mastitis of cows. In order to understand the metabolic process, four cows suffering from clinical mastitis were selected for the pharmacokinetic study. The transdermal preparation was applied to the diseased part of breast. Then the plasma and milk samples were collected respectively at 0, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, and 36 h, The concentrations of baicalin and phillyrin in plasma and milk were determined by HPLC and the data of time-concentrations were analyzed by the pharmacokinetic software. The results showed that two ingredients in the plasma were not detectable, but they in the milk had linear relationship with the time. The peak concentration of baicalin [(2.84 ±0.15)μg mL^-1] appeared at (4.93 ± 0.35) h, AUC0.1OQ was (27.32 ± 7.91) mg L^-1 h^-1, and the mean retention time was (28.31 ±0.49) h. The peak concentration of phillyrin [(0.49 ± 0.41) μg mL^-1] achieved at (3.68 ± 3.14) h, AUC0-LOQ was (4.10± 0.31) mg L^-1 h^-1, and the mean retention time was (14.52 ± 0.02) h. These suggested that two ingredients had slow absorbing speed and high absorbing degree. They could not be eliminated in a short time, thus exerted the topical curative effect.展开更多
Background: Determination of the endogenous loss of fat(ELF) is used to adjust for the estimation of true total tract digestibility(TTTD) of fat in diets and ingredients.Any factor which affected ELF may further affec...Background: Determination of the endogenous loss of fat(ELF) is used to adjust for the estimation of true total tract digestibility(TTTD) of fat in diets and ingredients.Any factor which affected ELF may further affect the digestibility of fat,including sources and concentrations of fat and fiber in the diet.There are some reports of determining the ELF using regression methods based on different levels of fat intake,while reports on effects of dietary fiber content and different fiber-rich ingredients in pig diets on ELF are very limited.Therefore,the objective of this study was to determine the effects of dietary fiber content and different fiber-rich ingredients on endogenous losses of fat and fatty acids at the end of ileum and throughout the entire intestinal tract in growing pigs.Methods: In Exp.1,the effect of fiber content on endogenous loss of fat was determined using six growing pigs(Duroc × Landrace × Yorkshire;27.6 ± 2.4 kg),fitted with a T-cannula at the end of ileum.The experimental design was a 6 × 6 complete Latin square design with six periods of feeding and six diets.The six experimental fat-free diets were formulated to include graded levels of neutral detergent fiber(NDF)(0,40,80,120,160 and 200 g/kg) and soybean hull(SH) was the only fiber source,providing 0,75,150,225,300 and 375 g/kg,respectively.Chromic oxide was included at4 g/kg in all diets as an indigestible marker.In Exp.2,six crossbred growing barrows(27.6 ± 1.6 kg) were used and the experimental design was the same as for Exp.1.The six fat-free diets were formulated to include six common fiber-rich ingredients and the concentration of NDF was 100 g/kg.The six fiber-rich ingredients were defatted rice bran(DRB),sugar beet pulp(SBP),rice hull(RH),corn germ meal(CGM),SH and wheat bran(WB) and they were fed at represented250,270,145,250,170 and 280 g/kg in the diet,respectively.Results: In Exp.1,the endogenous loss of fatty acids profile did not change as dietary NDF increased in growing pigs.The endogenous losses of fat,C16:0,C18:0,C18:1,C18:2,total unsaturated fatty acids(UFA) and total saturated fatty acids(SFA) in growing pigs at the end of ileum and throughout the entire intestinal tract increased linearly as NDF content of diets increased.The endogenous losses of fat,as well as C16:0 and C18:0 throughout the entire intestinal tract also increased quadratically as NDF content of diets increased.The ELF increased from 0.71 to 3.14 g/kg of dry matter intake(DMI) and 0.56 to 8.21 g/kg DMI at the end of ileum and throughout the entire intestinal tract in growing pigs,respectively.The ELF occurred in the hindgut except for the growing pigs fed 0 and 4% NDF in their diets.The endogenous losses of C16:0 and UFA occurred primarily in the upper regions of the gut and the greatest endogenous losses of C18:0 occurred in the hindgut.The endogenous losses of fat,individual SFA and total SFA throughout the entire intestinal tract were much greater than that at the end of ileum.However,the endogenous losses of individual UFA and total UFA were less throughout the intestinal tract than at the end of ileum.In Exp.2,the endogenous losses of fat at the end of ileum were greater in growing pigs fed CGM or WB diets.The endogenous loss of fatty acids profile changed to a slight degree at the end of ileum that the endogenous loss of UFA(particularly C18:1 and C18:2) in growing pigs fed CGM or WB diets were greater(P < 0.01) than that for the other four diets.The greatest(P < 0.01) endogenous loss of SFA(particularly C18:0) was in growing pigs fed the RH diet.The endogenous losses of fat,C16:0,C18:0 and SFA over the entire intestinal tract were much greater in growing pigs fed CGM or WB diets,whereas the lowest values were in growing pigs fed DRB diet.The ELF at the end of ileum in growing pigs fed CGM or WB diets were 3.50 or 4.17 g/kg DMI,respectively,and the ELF over the entire intestinal tract was 7.23 or 7.38 g/kg DMI.The contribution in percentage of ELF in the upper gut was greater than that in the hindgut of growing pigs fed DRB and RH diets,while the ELF in the upper gut and hindgut were equal in growing pigs fed SBP,CGM and WB diets.On the whole,the endogenous losses of C18:1 and C18:2 throughout the entire intestinal tract in growing pigs fed the six fiber-rich ingredients diets were less than losses at the end of ileum,whereas the endogenous loss of fat,C16:0,C18:0 and SFA were greater throughout the intestinal tract than at the end of ileum.Conclusion: The profile of loss in endogenous fatty acids did not change as dietary NDF increased in growing pigs and the endogenous losses of fatty acids(C16:0,C18:0,C18:1 and C18:2) fat,UFA and SFA increased linearly as NDF content increased in the diets of pigs.The endogenous losses of fat or fatty acids at the end of ileum were greater in growing pigs fed RH,CGM or WB diets.The endogenous losses of fat,fatty acids(C16:0 and C18:0) and SFA were greater over the entire intestinal tract in pigs fed CGM or WB diet,while these values were the lowest in growing pigs fed the DRB diet.The contribution in percentage losses of fat in the upper gut were greater than in the hindgut of growing pigs fed DRB and RH diets,while the contribution of losses of fat in the upper gut and hindgut were equal in growing pigs fed SBP,CGM and WB diets.In addition,the endogenous loss of individual or total UFA was less over the entire intestinal tract of growing pigs fed fiber diets than that at the end of ileum,and the greatest endogenous losses of fat,individual or total SFA were over the entire intestinal tract.Therefore,differences in fiber content and the nature of fiber-rich ingredients in diets of pigs have different effects to the endogenous losses of fat or fatty acids.Considering the requirement of fat or fatty acids of pigs,careful attention must be paid that the endogenous losses of fat and fatty acids when fiber ingredients are used in diets of pigs.展开更多
Great differences between municipal solid wastes (MSW) produced at different places and different times in terms of such parameters as physical ingredient and heating value lead to difficulty in effective handling of ...Great differences between municipal solid wastes (MSW) produced at different places and different times in terms of such parameters as physical ingredient and heating value lead to difficulty in effective handling of MSW. In this paper, ingredient, heating value and their temporal varying trends of typical MSW in Beijing were continuously measured and analyzed. With consideration of the process in pyrolysis and incineration, correlation between physical ingredients and heating values was induced, favorable for evaluation of heating value needed in handling of MSW from simple analysis of physical ingredients of it.展开更多
Honeysuckle, the dry flower bud or with open flower of Lonicerajaponica in caprifoliaceae, has been touted as a cure-all for heat-clearing and detoxifying effect. Honeysuckle contains abundant components such as volat...Honeysuckle, the dry flower bud or with open flower of Lonicerajaponica in caprifoliaceae, has been touted as a cure-all for heat-clearing and detoxifying effect. Honeysuckle contains abundant components such as volatile oil, flavonoids and organic acids, playing the role of antibiosis, antivirus, antiphlogosis, immunopotenfiation and antioxidation. The active ingredients and pharmacological action of honeysuckle are reviewed in the paper, so as to lay the foundation for further application of honeysuckle in veterinary clinic.展开更多
Probiotical cell fragments (PCFs) are structural components of the probiotic cell lysate(s) and exhibit similar beneficial effects on the host as live probiotic bacteria. With cell fragment technology (CFT?), the stru...Probiotical cell fragments (PCFs) are structural components of the probiotic cell lysate(s) and exhibit similar beneficial effects on the host as live probiotic bacteria. With cell fragment technology (CFT?), the structural fragments are isolated and purified from live probiotic cells. While observed to be strain-dependent as in the case of live probiotics, orally administered PCFs demonstrated a broad spectrum of immune modulation functions;anti-allergy;anti-inflammation;anti-bacterial and anti-viral properties;anti-mutagenic;and radioprotective and detoxification abilities in humans and animals. The PCFs mechanisms of action include events of motifs of cell wall peptidoglycans, DNA motifs, nucleotide containing components, lipoteichoic acids (LPAs), surface layer (S-layer) proteins, and cytoplasmic proteins. Different immunological in vivo-in vitro tests have shown that PCFs, essentially, have the ability to stimulate the macrophages, and induce cytokines such as interleukins, tumor necrosis factors (TNFs), interferons (IFNs), and natural killer (NK) cells. PCFs may be used as ingredients for foods and beverages or as nutritional supplements with long term stability and shelf-life up to 5 years. PCFs may also be used as health restorative ingredients in cosmetic products. The outcome of probiotics CFT? stands as an advantage to the food and pharmaceutical industries, regarding the formulation of novel products with unadulterated sensory characteristics of origin. Hence, PCFs are being characterized here as “novel nutraceutical ingredients” for health maintenance in both humans and animals.展开更多
Background: The current study was carried out to provide a reference for monitory of aflatoxin B_1(AFB_1),zearalenone(ZEN) and deoxynivalenol(DON) contamination in feed ingredients and complete feeds were colle...Background: The current study was carried out to provide a reference for monitory of aflatoxin B_1(AFB_1),zearalenone(ZEN) and deoxynivalenol(DON) contamination in feed ingredients and complete feeds were collected from different Province in China from 2013 to 2015.Methods: A total of 443 feed ingredients, including 220 corn, 24 wheat, 24 domestic distillers dried grains with soluble(DDGS), 55 bran, 20 wheat shorts and red dog, 37 imported DDGS, 34 corn germ meal and 29 soybean meal as well as 127 complete feeds including 25 pig complete feed(powder), 90 pig complete feed(pellet), six duck complete feed and six cattle complete feed were randomly collected from different Province in China,respectively, by high-performance chromatography in combined with UV or fluorescence analysis.Results: The incidence rates of AFB_1, ZEN and DON contamination of feed ingredients and complete feeds were80.8, 92.3 and 93.9 %, respectively. The percentage of positive samples for DON ranged from 66.7 to 100 %.Domestic DDGS and imported DDGS presented the most serious contamination AFB_1, ZEN and DON contamination levels of feeds ranged from 61.5 to 100 %, indicated that serious contamination over the studied 3-year period.Conclusion: The current data provide clear evidence that AFB_1, ZEN and DON contamination of feed ingredients and complete feeds in different Province in China is serious and differs over past 3-year. The use of corn, domestic DDGS, imported DDGS and corn germ meal, which may be contaminated with these three mycotoxins, as animal feed may triggered a health risk for animal. Feeds are most contaminated with DON followed by ZEN and AFB_1.Mycotoxins contamination in feed ingredients and complete feeds should be monitored routinely in China.展开更多
Tripterygium Wilfordii Hooks. f (TW) also called yellow vine, yellow vine wood, yellow wax vine, breakgut herb etc., belongs to Galactia genus, its medicinal parts mostly belong to the wooden part of the double-layer ...Tripterygium Wilfordii Hooks. f (TW) also called yellow vine, yellow vine wood, yellow wax vine, breakgut herb etc., belongs to Galactia genus, its medicinal parts mostly belong to the wooden part of the double-layer decortical root. Traditional Chinese medicine (TCM) holds that it has the function of clearing Heat and removing toxin, dispelling Wind to fr- ee collateral, relaxing tendon to activate blood circulation, subsiding swelling and analgesia, insecticide and hemostasis. The studies on botanical resources, chemical ingredients and pharmacology of TW are briefly introduced as follows.展开更多
Objective:To predict the potential active ingredients (PAIs) and mechanism of action of traditional Chinese medicine formulations used to delay aging.Methods:We incorporated the use of quantum-chemistry calculations a...Objective:To predict the potential active ingredients (PAIs) and mechanism of action of traditional Chinese medicine formulations used to delay aging.Methods:We incorporated the use of quantum-chemistry calculations and machine learning to predict the active ingredients of some Chinese herbal medicines used to delay aging.Then,a network-pharmacology approach was used to uncover how these PAls delayed aging.Results:Twelve PAls with anti-aging effects were discovered:androsterone,MHP,cortisone,propyl methyl trisulfide,retinol,retinal,cortisol,11-cis-Retinol (2R,3R)-3-hydroxyproline,4,5alpha-Dihydrocortisone (2S)-2-ammonio-6-ureidohexanoate and17alpha,21-Dihydroxy-5beta-pregnane-3,11,20-trione.Enrichment analyses indicated that a putative compound target and aging target were significantly associated with:regulation of the immune system;insulin receptor signaling pathway;regulation of the mitotic cell cycle;response to nutrient levels;response to oxidative stress;release of cytochrome c from mitochondria;learning or memory;inflammatory response.Conclusions:A novel method was proposed to predict the PAls of anti-aging herbal medicines by incorporating quantum-chemistry calculations and machine learning.Then,a network-pharmacology approach was used to uncover how these PAls delay aging.The information provided by our study on PAls may aid the discovery of anti-aging drugs.展开更多
Using Mo, B-Fe alloy and Fe powders as raw materials, and adding C, Cr and Ni ingredients, respectively, or C, Cr and Ni mixed powders, ternary boride hard alloy clad materials was prepared on Q235 steel substrate by ...Using Mo, B-Fe alloy and Fe powders as raw materials, and adding C, Cr and Ni ingredients, respectively, or C, Cr and Ni mixed powders, ternary boride hard alloy clad materials was prepared on Q235 steel substrate by means of in-situ reaction and vacuum liquid phase sintering technology. The influence of alloy ingredients on the mechanical properties of ternary boride hard alloy clad materials was investigated. The results indicate that a mixture of 0.8% C, 5% Cr and 2% Ni ingredients gives a ternary boride hard alloy clad material with optimal mechanical properties, such as high transverse rupture strength, high hardness and good wear resistance.展开更多
Various effective ingredients extracted from traditional Chinese medicine have achieved more and more attention in the field of cancer therapy due to their high bioactivity and good safety.These traditional Chinese me...Various effective ingredients extracted from traditional Chinese medicine have achieved more and more attention in the field of cancer therapy due to their high bioactivity and good safety.These traditional Chinese medicine effective ingredients include paclitaxel,arsenical trioxide,camptothecin and so on.However,poor water solubility and low bioavailability of these traditional Chinese medicine ingredients severely hindered their clinical application.The rapid development of nanotechnology provided a new platform,new opportunities and new challenges for their effective delivery in vitro and in vivo.This minireview provides a concentrated summary of the most recent progresses made in this emerging field,highlighting the“combination ancient traditional Chinese medicine ingredients and advanced nanotechnology”strategy for favoring the construction of next generation cancer nanomedicines.展开更多
The assumptions and models for solubility modelling or prediction in systems using nonpolar solvents, or water and complex triterpene and other active pharmaceutical ingredients as solutes aren't well studied. Fur...The assumptions and models for solubility modelling or prediction in systems using nonpolar solvents, or water and complex triterpene and other active pharmaceutical ingredients as solutes aren't well studied. Furthermore, the assumptions concerning heat capacity effects(negligibility, experimental values or approximations) are explored, using non-polar solvents(benzene), or water as reference solvents, for systems with solute melting points in the range of 306–528 K and molecular weights in the range of 90–442 g/mol. New empirical estimation methods for the Δ_(fus)C_(pi) of APIs are presented which correlate the solute molecular masses and van der Waals surface areas with Δ_(fus)C_(pi). Separate empirical parameters were required for oxygenated and non-oxygenated solutes. Subsequently, the predictive capabilities of the various approaches to solubility modelling for complex pharmaceuticals,for which data is limited, are analysed. The solute selection is based on a principal component analysis, considering molecular weights, fusion temperatures, and solubilities in a non-polar solvent, alcohol, and water, where data was available. New NRTL-SAC parameters were determined for selected steroids, by regression. The original UNIFAC, modified UNIFAC(Dortmund), COSMO-RS(OL), and COSMO-SAC activity coefficient predictions are then conducted, based on the availability of group constants and sigma profiles. These are undertaken to assess the predictive capabilities of these models when each assumption concerning heat capacity is employed. The predictive qualities of the models are assessed, based on the mean square deviation and provide guidelines for model selection, and assumptions concerning phase equilibrium, when designing solid–liquid separators for the pharmaceutical industry on process simulation software. The most suitable assumption regarding Δ_(fus)C_(pi) was found to be system specific, with modified UNIFAC(Dortmund) performing well in benzene as a solvent system, while original UNIFAC performs better in aqueous systems.Original UNIFAC outperforms other predictive models tested in the triterpene/steroidal systems,with no significant influence from the assumptions regarding Δ_(fus)C_(pi).展开更多
文摘Lack of dietary fiber contributes to many health issues, particularly chronic vascular diseases. Mixed linkage β-1.3 - 1.4 beta-glucan (beta-glucan, in this paper) is a confirmed beneficial ingredient for the human diet through reduction of cholesterol and the glycemic index. Barley contains the highest beta-glucan content of all the grains, and in this study, a percentage of flour from two high beta glucan lines was, each, added to an array of wheat-based food products to measure how it impacted total dietary fiber. Results showed that beta-glucan content was higher in all the products containing the added high beta-glucan flour, along with increased total dietary fiber content. Protein content in the food products is also increased with the higher protein in the barley flours added. Beta-glucan content in the barley-added products increased to 1.2% - 4.0% versus 0.2% - 0.5% in the pure wheat products, while the dietary fibers increased to 3.5% - 24.4% versus 2.1% - 9.1% in pure wheat product controls. This research provided experimental evidence that using a high beta-glucan barley ingredient in food can increase dietary fiber to benefit health.
文摘The active ingredients of Camellia japonica flowers(CJF)at high and low altitudes,as well as their skin care efficacy were compared.The dried red CJF at high and low altitudes were ultrasonically extracted with 70%ethanol,and these extracts were concentrated and then diluted to a constant volume.The content of total flavonoids,total polyphenols and total proteins was tested and analyzed.In addition,DPPH free radical scavenging,inhibition of the formation of advanced glycation end products,and inhibitory activity against elastase was measured to compare their skin care efficacy in anti-oxidation,anti-glycation,anti-wrinkling and firming.The results showed that,based on the dry weight of CJF,the content of total flavonoids and total proteins of the CJF at high altitude was approximately 1.5 times of the CJF at low altitude,while the content of total polyphenols was approximately 2.4 times that of the CJF at low altitude.The skin care efficacy of CJF at high altitude was significantly better than that of the CJF at low altitude.This work could provide theoretical basis for the selection and application of Camellia japonica flowers in the field of cosmetics.
基金Foundation for the History of Science and Technology in East AsiaPhD Support Scheme from The Faculty of Arts at the Chinese University of Hong Kong。
文摘This article explores China’s state-level knowledge production on medicinal ingredients in northwestern Sichuan in the 1950s.Drawing on county-level archives,published materials and interviews,this historical article traces how different levels of governments and state-owned trading companies produced knowledge about medicinal ingredients and its production.It argues that on one hand the state’s procurement standards codified the knowledge about medicinal ingredients from the marketplace and the local producers.On the other hand,direct extraction of knowledge from the medicine gatherers and cultivators verbalized and collected the previously tacit local knowledge about the production of medicinal ingredients,which would help to alleviate the shortage in the supply of traditional Chinese medicines throughout the 1950s.
文摘[Objectives]To analyze the effect of Mongolian pharmaceutical Betel Shisanwei Ingredient Pills in the clinical treatment of patients with depression.[Methods]From June 2020 to May 2021,64 patients with depression who received treatment in Inner Mongolia Minzu University were selected to participate in this study.These patients were randomly numbered from 1 to 64,and then divided into two groups according to the principle of odd or even number.Patients with odd number were regarded as the reference group,and treated by western medicine fluoxetine;patients with even number were regarded as the study group,and treated by Mongolian pharmaceutical Betel Shisanwei Ingredient Pills.The therapeutic effects of the two groups of patients were compared.[Results]Before treatment,there was no significant difference in the scores of patients'depressive syndromes between the two groups(P>0.05).After treatment,there were two significant changes in comprehensive score of depressive symptoms in both groups.Compared with before treatment,the data of the same group after treatment decreased significantly.Comparison between the two groups showed that the score of patients'depressive syndromes in the study group(13.28±5.49)was significantly lower than that in the reference group(18.46±6.51),and the overall response rate of treatment in the study group(96.88%,31/32)was obviously higher than that in the reference group(75.00%,24/32),showing statistically significant differences(P<0.05).[Conclusions]In the treatment of depression,Mongolian medicine therapy can significantly improve the depressive syndromes in patients,with more prominent curative effects,and is worthy of promotion and application.
基金The National Natural Science Foundation of China(No.81973977,No.81273872)the Fundamental Research Funds for the Central Universities(2021JCXK02)supported this study.
文摘In the development of new drugs products,especially the development of traditional Chinese medicine active ingredients,solubility and oral bioavailability are the main factors which are restricting the development of new drugs,whereas the physicochemical properties of active ingredients are the key element to affecting these factors.Pharmaceutical cocrystal provides an excellent opportunity to develop new drugs with excellent physical and chemical properties such as melting point,solubility,stability and bioavailability while retaining the pharmacological properties of individuals active pharmaceutical ingredients among pharmaceutical cocrystal compounds.Traditional Chinese herbal medicine has the characteristics of multiple pathways and multiple targets,mainly because it contains many active ingredients,like cocrystals thereof with many components.The active ingredients extracted from traditional Chinese herbal medicine have a wide range of pharmacological activities,but most of the active ingredients affect the development of traditional Chinese medicine active ingredients due to their physical and chemical properties such as solubility.Traditional Chinese medicine pharmaceutical cocrystals can not only improve the physical and chemical properties of drugs without changing the internal structure of drugs,so as to provide a new scheme for the development of traditional Chinese medicine active ingredients.This paper reviews the research progress of active ingredients of traditional Chinese medicine pharmaceutical cocrystal.The preparation methods of cocrystals are summarized and the advantages of cocrystals are illustrated with examples.
基金This work was financially supported by Scientific Research Fund Project of Education Department of Liaoning Province(LJKZ0960)Science Foundation of Shenyang Pharmaceutical University(GGJJ2021105).
文摘People continue to recognize the important role of Chinese medicine in the treatment of diseases,and there is an urgent need to clarify the mechanism of Chinese medicine.Because of the multi-target and multi-component characteristics of traditional Chinese medicine,it is difficult to elaborate from a single perspective.As a high-quality animal model,Caenorhabditis elegans with the characteristics of small size and fast reproduction,has been widely used in traditional Chinese medicine activity experiments.In this article,Caenorhabditis elegans,as model organisms used to screen the active components of traditional Chinese medicine were reviewed.
基金financially supported by the Modern Agricultural Industry Technology System(CARS-36)Developing key equipment for digital management and monitoring environment in animal production(2013AA10230602)+2 种基金National Natural Science Foundation of China(31372317)the 111 Project(B16044)China Postdoctoral Science Foundation
文摘In the past two decades, a considerable amount of research has focused on the determination of the digestible(DE) and metabolizable energy(ME) contents of feed ingredients fed to swine. Compared with the DE and ME systems, the net energy(NE) system is assumed to be the most accurate estimate of the energy actually available to the animal. However, published data pertaining to the measured NE content of ingredients fed to growing pigs are limited. Therefore, the Feed Data Group at the Ministry of Agricultural Feed Industry Centre(MAFIC) located at China Agricultural University has evaluated the NE content of many ingredients using indirect calorimetry. The present review summarizes the NE research works conducted at MAFIC and compares these results with those from other research groups on methodological aspect. These research projects mainly focus on estimating the energy requirements for maintenance and its impact on the determination, prediction, and validation of the NE content of several ingredients fed to swine. The estimation of maintenance energy is affected by methodology, growth stage,and previous feeding level. The fasting heat production method and the curvilinear regression method were used in MAFIC to estimate the NE requirement for maintenance. The NE contents of different feedstuffs were determined using indirect calorimetry through standard experimental procedure in MAFIC. Previously generated NE equations can also be used to predict NE in situations where calorimeters are not available. Although popular, the caloric efficiency is not a generally accepted method to validate the energy content of individual feedstuffs. In the future,more accurate and dynamic NE prediction equations aiming at specific ingredients should be established, and more practical validation approaches need to be developed.
基金This work was supported by the National Natural Science Foundation of China(30070566).
文摘In this study, the IL-2 mRNA levels of T lymphocytes in normal mice stimulated by nine Chinese herbal medicinal ingredients (CHMIs) were measured using semiquantification reverse transcription polymerase chain reaction. The results showed that astragalus polysaccharide (APS), epimedium polysaccharide (EPS), Chinese angelica polysaccharide (CAPS), propolis flavone (PF), and astrogalosides (AS) promoted IL-2 mRNA levels in T lymphocytes in vitro and in vivo to differing degrees, and the level of IL-2 mRNA induced by propolis polysaccharide (PPS) in vitro was higher than that induced by the control, which differed from that of PPS in vivo.
基金supported by the Major Project of Re-vitalizing the Old Industrial Bases of Science and Edu-cation Commission of Heilongjiang Province, China(1151gzd04)the 11th Five-Year Plan Major Re-search Projects of Science and Technology Commis-sion of Heilongjiang Province (GA06B202-3)
文摘The topical administration of the compound Chinese herbal medicine transdermal preparation has been widely used in treating the mastitis of cows. In order to understand the metabolic process, four cows suffering from clinical mastitis were selected for the pharmacokinetic study. The transdermal preparation was applied to the diseased part of breast. Then the plasma and milk samples were collected respectively at 0, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, and 36 h, The concentrations of baicalin and phillyrin in plasma and milk were determined by HPLC and the data of time-concentrations were analyzed by the pharmacokinetic software. The results showed that two ingredients in the plasma were not detectable, but they in the milk had linear relationship with the time. The peak concentration of baicalin [(2.84 ±0.15)μg mL^-1] appeared at (4.93 ± 0.35) h, AUC0.1OQ was (27.32 ± 7.91) mg L^-1 h^-1, and the mean retention time was (28.31 ±0.49) h. The peak concentration of phillyrin [(0.49 ± 0.41) μg mL^-1] achieved at (3.68 ± 3.14) h, AUC0-LOQ was (4.10± 0.31) mg L^-1 h^-1, and the mean retention time was (14.52 ± 0.02) h. These suggested that two ingredients had slow absorbing speed and high absorbing degree. They could not be eliminated in a short time, thus exerted the topical curative effect.
基金supported by the Prevention and Control of Nutritional Metabolism and Toxic Diseases in Livestock and Poultry(2016YFD0501204)the 111 Project(B16044)
文摘Background: Determination of the endogenous loss of fat(ELF) is used to adjust for the estimation of true total tract digestibility(TTTD) of fat in diets and ingredients.Any factor which affected ELF may further affect the digestibility of fat,including sources and concentrations of fat and fiber in the diet.There are some reports of determining the ELF using regression methods based on different levels of fat intake,while reports on effects of dietary fiber content and different fiber-rich ingredients in pig diets on ELF are very limited.Therefore,the objective of this study was to determine the effects of dietary fiber content and different fiber-rich ingredients on endogenous losses of fat and fatty acids at the end of ileum and throughout the entire intestinal tract in growing pigs.Methods: In Exp.1,the effect of fiber content on endogenous loss of fat was determined using six growing pigs(Duroc × Landrace × Yorkshire;27.6 ± 2.4 kg),fitted with a T-cannula at the end of ileum.The experimental design was a 6 × 6 complete Latin square design with six periods of feeding and six diets.The six experimental fat-free diets were formulated to include graded levels of neutral detergent fiber(NDF)(0,40,80,120,160 and 200 g/kg) and soybean hull(SH) was the only fiber source,providing 0,75,150,225,300 and 375 g/kg,respectively.Chromic oxide was included at4 g/kg in all diets as an indigestible marker.In Exp.2,six crossbred growing barrows(27.6 ± 1.6 kg) were used and the experimental design was the same as for Exp.1.The six fat-free diets were formulated to include six common fiber-rich ingredients and the concentration of NDF was 100 g/kg.The six fiber-rich ingredients were defatted rice bran(DRB),sugar beet pulp(SBP),rice hull(RH),corn germ meal(CGM),SH and wheat bran(WB) and they were fed at represented250,270,145,250,170 and 280 g/kg in the diet,respectively.Results: In Exp.1,the endogenous loss of fatty acids profile did not change as dietary NDF increased in growing pigs.The endogenous losses of fat,C16:0,C18:0,C18:1,C18:2,total unsaturated fatty acids(UFA) and total saturated fatty acids(SFA) in growing pigs at the end of ileum and throughout the entire intestinal tract increased linearly as NDF content of diets increased.The endogenous losses of fat,as well as C16:0 and C18:0 throughout the entire intestinal tract also increased quadratically as NDF content of diets increased.The ELF increased from 0.71 to 3.14 g/kg of dry matter intake(DMI) and 0.56 to 8.21 g/kg DMI at the end of ileum and throughout the entire intestinal tract in growing pigs,respectively.The ELF occurred in the hindgut except for the growing pigs fed 0 and 4% NDF in their diets.The endogenous losses of C16:0 and UFA occurred primarily in the upper regions of the gut and the greatest endogenous losses of C18:0 occurred in the hindgut.The endogenous losses of fat,individual SFA and total SFA throughout the entire intestinal tract were much greater than that at the end of ileum.However,the endogenous losses of individual UFA and total UFA were less throughout the intestinal tract than at the end of ileum.In Exp.2,the endogenous losses of fat at the end of ileum were greater in growing pigs fed CGM or WB diets.The endogenous loss of fatty acids profile changed to a slight degree at the end of ileum that the endogenous loss of UFA(particularly C18:1 and C18:2) in growing pigs fed CGM or WB diets were greater(P < 0.01) than that for the other four diets.The greatest(P < 0.01) endogenous loss of SFA(particularly C18:0) was in growing pigs fed the RH diet.The endogenous losses of fat,C16:0,C18:0 and SFA over the entire intestinal tract were much greater in growing pigs fed CGM or WB diets,whereas the lowest values were in growing pigs fed DRB diet.The ELF at the end of ileum in growing pigs fed CGM or WB diets were 3.50 or 4.17 g/kg DMI,respectively,and the ELF over the entire intestinal tract was 7.23 or 7.38 g/kg DMI.The contribution in percentage of ELF in the upper gut was greater than that in the hindgut of growing pigs fed DRB and RH diets,while the ELF in the upper gut and hindgut were equal in growing pigs fed SBP,CGM and WB diets.On the whole,the endogenous losses of C18:1 and C18:2 throughout the entire intestinal tract in growing pigs fed the six fiber-rich ingredients diets were less than losses at the end of ileum,whereas the endogenous loss of fat,C16:0,C18:0 and SFA were greater throughout the intestinal tract than at the end of ileum.Conclusion: The profile of loss in endogenous fatty acids did not change as dietary NDF increased in growing pigs and the endogenous losses of fatty acids(C16:0,C18:0,C18:1 and C18:2) fat,UFA and SFA increased linearly as NDF content increased in the diets of pigs.The endogenous losses of fat or fatty acids at the end of ileum were greater in growing pigs fed RH,CGM or WB diets.The endogenous losses of fat,fatty acids(C16:0 and C18:0) and SFA were greater over the entire intestinal tract in pigs fed CGM or WB diet,while these values were the lowest in growing pigs fed the DRB diet.The contribution in percentage losses of fat in the upper gut were greater than in the hindgut of growing pigs fed DRB and RH diets,while the contribution of losses of fat in the upper gut and hindgut were equal in growing pigs fed SBP,CGM and WB diets.In addition,the endogenous loss of individual or total UFA was less over the entire intestinal tract of growing pigs fed fiber diets than that at the end of ileum,and the greatest endogenous losses of fat,individual or total SFA were over the entire intestinal tract.Therefore,differences in fiber content and the nature of fiber-rich ingredients in diets of pigs have different effects to the endogenous losses of fat or fatty acids.Considering the requirement of fat or fatty acids of pigs,careful attention must be paid that the endogenous losses of fat and fatty acids when fiber ingredients are used in diets of pigs.
基金The Key Projects of Chinese Academy of Sciences(No.KY95T-03-02)the National Natural Science Foundation of China(No.59776023)
文摘Great differences between municipal solid wastes (MSW) produced at different places and different times in terms of such parameters as physical ingredient and heating value lead to difficulty in effective handling of MSW. In this paper, ingredient, heating value and their temporal varying trends of typical MSW in Beijing were continuously measured and analyzed. With consideration of the process in pyrolysis and incineration, correlation between physical ingredients and heating values was induced, favorable for evaluation of heating value needed in handling of MSW from simple analysis of physical ingredients of it.
文摘Honeysuckle, the dry flower bud or with open flower of Lonicerajaponica in caprifoliaceae, has been touted as a cure-all for heat-clearing and detoxifying effect. Honeysuckle contains abundant components such as volatile oil, flavonoids and organic acids, playing the role of antibiosis, antivirus, antiphlogosis, immunopotenfiation and antioxidation. The active ingredients and pharmacological action of honeysuckle are reviewed in the paper, so as to lay the foundation for further application of honeysuckle in veterinary clinic.
文摘Probiotical cell fragments (PCFs) are structural components of the probiotic cell lysate(s) and exhibit similar beneficial effects on the host as live probiotic bacteria. With cell fragment technology (CFT?), the structural fragments are isolated and purified from live probiotic cells. While observed to be strain-dependent as in the case of live probiotics, orally administered PCFs demonstrated a broad spectrum of immune modulation functions;anti-allergy;anti-inflammation;anti-bacterial and anti-viral properties;anti-mutagenic;and radioprotective and detoxification abilities in humans and animals. The PCFs mechanisms of action include events of motifs of cell wall peptidoglycans, DNA motifs, nucleotide containing components, lipoteichoic acids (LPAs), surface layer (S-layer) proteins, and cytoplasmic proteins. Different immunological in vivo-in vitro tests have shown that PCFs, essentially, have the ability to stimulate the macrophages, and induce cytokines such as interleukins, tumor necrosis factors (TNFs), interferons (IFNs), and natural killer (NK) cells. PCFs may be used as ingredients for foods and beverages or as nutritional supplements with long term stability and shelf-life up to 5 years. PCFs may also be used as health restorative ingredients in cosmetic products. The outcome of probiotics CFT? stands as an advantage to the food and pharmaceutical industries, regarding the formulation of novel products with unadulterated sensory characteristics of origin. Hence, PCFs are being characterized here as “novel nutraceutical ingredients” for health maintenance in both humans and animals.
基金supported by the Province Science and Technology Major Project of the Department of Science&Technology of Hunan Province(2015NK1002)Changsha City Science and Technology Program of China(k1508008-21)+1 种基金National Key R&D Program(2016YFD0501208)the National Natural Science Foundation of China(31402088,31501964 and31402091)
文摘Background: The current study was carried out to provide a reference for monitory of aflatoxin B_1(AFB_1),zearalenone(ZEN) and deoxynivalenol(DON) contamination in feed ingredients and complete feeds were collected from different Province in China from 2013 to 2015.Methods: A total of 443 feed ingredients, including 220 corn, 24 wheat, 24 domestic distillers dried grains with soluble(DDGS), 55 bran, 20 wheat shorts and red dog, 37 imported DDGS, 34 corn germ meal and 29 soybean meal as well as 127 complete feeds including 25 pig complete feed(powder), 90 pig complete feed(pellet), six duck complete feed and six cattle complete feed were randomly collected from different Province in China,respectively, by high-performance chromatography in combined with UV or fluorescence analysis.Results: The incidence rates of AFB_1, ZEN and DON contamination of feed ingredients and complete feeds were80.8, 92.3 and 93.9 %, respectively. The percentage of positive samples for DON ranged from 66.7 to 100 %.Domestic DDGS and imported DDGS presented the most serious contamination AFB_1, ZEN and DON contamination levels of feeds ranged from 61.5 to 100 %, indicated that serious contamination over the studied 3-year period.Conclusion: The current data provide clear evidence that AFB_1, ZEN and DON contamination of feed ingredients and complete feeds in different Province in China is serious and differs over past 3-year. The use of corn, domestic DDGS, imported DDGS and corn germ meal, which may be contaminated with these three mycotoxins, as animal feed may triggered a health risk for animal. Feeds are most contaminated with DON followed by ZEN and AFB_1.Mycotoxins contamination in feed ingredients and complete feeds should be monitored routinely in China.
文摘Tripterygium Wilfordii Hooks. f (TW) also called yellow vine, yellow vine wood, yellow wax vine, breakgut herb etc., belongs to Galactia genus, its medicinal parts mostly belong to the wooden part of the double-layer decortical root. Traditional Chinese medicine (TCM) holds that it has the function of clearing Heat and removing toxin, dispelling Wind to fr- ee collateral, relaxing tendon to activate blood circulation, subsiding swelling and analgesia, insecticide and hemostasis. The studies on botanical resources, chemical ingredients and pharmacology of TW are briefly introduced as follows.
基金the Natural Science Foundation of China(81373985).
文摘Objective:To predict the potential active ingredients (PAIs) and mechanism of action of traditional Chinese medicine formulations used to delay aging.Methods:We incorporated the use of quantum-chemistry calculations and machine learning to predict the active ingredients of some Chinese herbal medicines used to delay aging.Then,a network-pharmacology approach was used to uncover how these PAls delayed aging.Results:Twelve PAls with anti-aging effects were discovered:androsterone,MHP,cortisone,propyl methyl trisulfide,retinol,retinal,cortisol,11-cis-Retinol (2R,3R)-3-hydroxyproline,4,5alpha-Dihydrocortisone (2S)-2-ammonio-6-ureidohexanoate and17alpha,21-Dihydroxy-5beta-pregnane-3,11,20-trione.Enrichment analyses indicated that a putative compound target and aging target were significantly associated with:regulation of the immune system;insulin receptor signaling pathway;regulation of the mitotic cell cycle;response to nutrient levels;response to oxidative stress;release of cytochrome c from mitochondria;learning or memory;inflammatory response.Conclusions:A novel method was proposed to predict the PAls of anti-aging herbal medicines by incorporating quantum-chemistry calculations and machine learning.Then,a network-pharmacology approach was used to uncover how these PAls delay aging.The information provided by our study on PAls may aid the discovery of anti-aging drugs.
基金Project(59975054) supported by the National Natural Science Foundation of China
文摘Using Mo, B-Fe alloy and Fe powders as raw materials, and adding C, Cr and Ni ingredients, respectively, or C, Cr and Ni mixed powders, ternary boride hard alloy clad materials was prepared on Q235 steel substrate by means of in-situ reaction and vacuum liquid phase sintering technology. The influence of alloy ingredients on the mechanical properties of ternary boride hard alloy clad materials was investigated. The results indicate that a mixture of 0.8% C, 5% Cr and 2% Ni ingredients gives a ternary boride hard alloy clad material with optimal mechanical properties, such as high transverse rupture strength, high hardness and good wear resistance.
基金This research was funded by the Postdoctoral Research Grant in Henan Province(201901025)National Natural Science Foundation of China(82003298).
文摘Various effective ingredients extracted from traditional Chinese medicine have achieved more and more attention in the field of cancer therapy due to their high bioactivity and good safety.These traditional Chinese medicine effective ingredients include paclitaxel,arsenical trioxide,camptothecin and so on.However,poor water solubility and low bioavailability of these traditional Chinese medicine ingredients severely hindered their clinical application.The rapid development of nanotechnology provided a new platform,new opportunities and new challenges for their effective delivery in vitro and in vivo.This minireview provides a concentrated summary of the most recent progresses made in this emerging field,highlighting the“combination ancient traditional Chinese medicine ingredients and advanced nanotechnology”strategy for favoring the construction of next generation cancer nanomedicines.
基金supported by the National Research Foundation of South Africa under the South African Research Chair Initiative of the Department of Science and Technology and the National Research Foundation Research and Innovation Support and Advancement (RISA) program
文摘The assumptions and models for solubility modelling or prediction in systems using nonpolar solvents, or water and complex triterpene and other active pharmaceutical ingredients as solutes aren't well studied. Furthermore, the assumptions concerning heat capacity effects(negligibility, experimental values or approximations) are explored, using non-polar solvents(benzene), or water as reference solvents, for systems with solute melting points in the range of 306–528 K and molecular weights in the range of 90–442 g/mol. New empirical estimation methods for the Δ_(fus)C_(pi) of APIs are presented which correlate the solute molecular masses and van der Waals surface areas with Δ_(fus)C_(pi). Separate empirical parameters were required for oxygenated and non-oxygenated solutes. Subsequently, the predictive capabilities of the various approaches to solubility modelling for complex pharmaceuticals,for which data is limited, are analysed. The solute selection is based on a principal component analysis, considering molecular weights, fusion temperatures, and solubilities in a non-polar solvent, alcohol, and water, where data was available. New NRTL-SAC parameters were determined for selected steroids, by regression. The original UNIFAC, modified UNIFAC(Dortmund), COSMO-RS(OL), and COSMO-SAC activity coefficient predictions are then conducted, based on the availability of group constants and sigma profiles. These are undertaken to assess the predictive capabilities of these models when each assumption concerning heat capacity is employed. The predictive qualities of the models are assessed, based on the mean square deviation and provide guidelines for model selection, and assumptions concerning phase equilibrium, when designing solid–liquid separators for the pharmaceutical industry on process simulation software. The most suitable assumption regarding Δ_(fus)C_(pi) was found to be system specific, with modified UNIFAC(Dortmund) performing well in benzene as a solvent system, while original UNIFAC performs better in aqueous systems.Original UNIFAC outperforms other predictive models tested in the triterpene/steroidal systems,with no significant influence from the assumptions regarding Δ_(fus)C_(pi).