“素”胶囊已在国内外生产

据来自多方面的报道，一种以取自植物的原料及其衍生物为原材料的“素”胶囊，不仅已在国外生产，并也已经在中国生产和上市。

RP-HPLC determination of lycopene in microcapsules

Aim A RP- HPLC method for determination of lycopene in microcapsules was established. Methods The HPLC assay was performed on an Alltima Cls （4.6 mm × 250 mm, 5μm） column with a mixture of methanol-THF-water （66：30：4, V/V/V） as mobile phase at a flow rate of 1.5 mL·min^-1 and the UV detection wavelength was 472 nm. Results The linear range of lycopene was 3.6-18 μg·mL^-1, r = 0.999 8, the average recovery was from 99.81% to 101.06% with RSD less than 1.83%. The RSD of intra-day and interday precision were less than 3.34%. Conclusion The method is simple, accurate and suitable for the determination of lycopene in microcapsules.

Preparation and Characterization of Chitosan/Ethylcellulose Complex Microcapsule

In this work a system which consists of chitosan microcores entrapped in ethylcellulose is presented. Vitamin D2 was efficiently entrapped in chitosan microcores with spray-drying method and was microencapsulated by coating of ethylcellulose. The average size of chitosan microspheres was 6.06 um. The morphology and release properties of microcapsules were tested. The results of release in vitro showed that the microcapsule could realize sustained release for 12 h in artificial intestinal juice.

Effect of oral erythromycin on gastric and small bowel transit time of capsule endoscopy

AIM： To determine the effect of oral erythromycin on gastric and small bowel transit time of capsule endoscopy. METHODS： Consecutive patients who underwent capsule endoscopy during the 16-mo study period were either given 250 mg oral erythromycin, 1 h prior to swallowing the capsule endoscope or nothing. The gastric and small bowel transit time, and the small bowel image quality were compared. RESULTS： Twenty-four patients received oral erythromycin whereas 14 patients were not given any prokinetic agent. Patients who received erythromycin had a significantly lower gastric transit time than control （16 min vs70 min, P= 0.005）, whereas the small bowel transit time was comparable between the two groups （227 rain vs 183 min, P= 0.18）. Incomplete small bowel examination was found in three patients of the control group and in one patient of the erythromycin group. There was no significant difference in the overall quality of small bowel images between the two groups. A marked reduction in gastric transit time was noted in two patients who had repeat capsule endoscopy after oral erythromycin. CONCLUSION： Use of oral erythromycin significantly reduces the gastric transit time of capsule endoscopy.

Sulfation Kinetics in the Preparation of Cellulose Sulfate

In the established apparatus, the conversion ratios of cellulose sulfation (X) under different sulfation conditions were measured. The range of temperature was from -5℃ to +5℃, and the H2SO4 concentration was from 3.1 mol·L-1 to 4.5mol·L-1. The experimental results were used for the establishment of the kinetic model for cellulose sulfation. With the model, X values and the yield of NaCS (Y) can be calculated, thus the reaction with respect to H2SO4 concentration is determined to be third order.

CALCITONIN GENE-RELATED PEPTIDE INDUCES FIBRO-BLASTS FROM HIP PSEUDOCAPSULE TO PRODUCE CYTOKINES

Objective To investigate calcitonin gene-related peptide (CGRP) involvement in the process of aseptic loosening. Methods We isolated fibroblasts from periprosthetic pseudocapsular tissue at the time of revision hip arthroplasty performed due to aseptic loosening. Fibroblasts were incubated for 24 h in the presence of CGRP, and the levels of interleukin (IL)-1β, IL-6, and tumor necrosis factor (TNF)-α in the media were determined using enzyme-linked immunosorbent assay kit. Results We found that the levels of IL-1β, IL-6, and TNF-α increased in a time-and concentration-dependent manner. ConclusionThese inflammatory cytokines play an important role in the development of periprosthetic osteolysis and implant loosening. Our results suggest that CGRP may be involved in the pathogenesis of aseptic loosening.

叶黄素制品在大鼠体内药代动力学和生物利用度

目的:研究叶黄素微胶囊和叶黄素油悬浮液两种叶黄素制品在大鼠体内的药代动力学和相对生物利用度。方法:建立大鼠血浆中叶黄素的LC-MS/MS测定方法。考察大鼠分别灌胃给予100 mg/kg叶黄素微胶囊或叶黄素油悬浮液后血药浓度变化,应用DAS 2.0软件计算药动学参数,根据叶黄素微胶囊和叶黄素油悬浮液药-时曲线下面积AUC(0-t)计算相对生物利用度。结果:叶黄素浓度5 ng/ml^200 ng/ml的浓度范围内线性关系良好(r=0.997);定量下限为为5 ng/ml;10 ng/ml、50 ng/ml和160 ng/ml三个浓度剂量组的方法回收率分别为69.7%、94.9%和98.1%;提取回收率分别为75.3%、70.9%和73.4%。大鼠单剂量给予叶黄素微胶囊和叶黄素油悬浮液的主要药动学参数Cmax分别为(65.8±38.9)mg/L和(48.3±17.3)mg/L,Tmax分别为(4.7±3.0)h和(3.7±0.8)h,AUC(0-32)分别为(566.6±203.6)mg/L·h和(385.2±107.3)mg/L·h,叶黄素微胶囊的相对生物利用度为147.1%。结论:所建立LC-MS/MS方法简单、快速,可用于大鼠叶黄素血药浓度的测定和药动学研究。以叶黄素油悬浮液为参比制剂,叶黄素微胶囊在大鼠体内的生物利用度明显提高。

水飞蓟素对大鼠骨折愈合中FGF-2表达的影响

目的:探讨水飞蓟素在大鼠骨折早期愈合过程中对成纤维细胞生长因子2(FGF-2)表达的影响,为水飞蓟素促进骨折愈合提供实验参考。方法:选取雌性SD大鼠120只,随机分为正常对照组20只,骨折组100只。将骨折组100只大鼠用10%水合氯醛以3ml/kg腹腔麻醉,右侧胫骨常规备皮,络合碘消毒2次,自胫骨结节向下切开约1.5cm切口,向外分离胫前肌肉,切开骨膜自胫骨结节下0.5cm线锯截断胫骨,0.8mm克氏针髓内固定,逐层关闭切口。造模成功后将成模大鼠随机分5组:骨折模型组,金天格组(120mg/kg),以及水飞蓟素不同剂量组(40mg/kg、80mg/kg、120mg/kg)灌胃,2、4、6周各组分别随机选取8只大鼠行尾静脉采血,用ELISA法检测血清FGF-2的表达,骨组织采用免疫组织化学染色检测软骨中FGF-2的表达水平,通过X线对骨折愈合情况进行评分。结果:(1)血清FGF-2结果:在第2、4、6周,各组间有显著性差异,但在第4、6周骨折模型组、空白对照组与水飞蓟素40mg/kg、水飞蓟素80mg/kg、水飞蓟素120mg/kg、金天格80mg/kg组间无统计学差异;(2)免疫组化结果:术后第2周、第4周,除金天格组与水飞蓟素120mg/kg外,其余各组间均有统计学差异。第6周时,除金天格组、水飞蓟素120mg/kg与水飞蓟素80mg/kg外,其余各组间均有统计学差异。(3)X线对骨折愈合情况评分结果:术后2周时,水飞蓟素3组给药组大鼠骨折处均可见明显骨痂生长;术后4周时,3组大鼠骨折线均开始模糊,骨痂体积明显减少;6周时,三组均有部分大鼠已达到骨性愈合,髓腔部分再通。骨折愈合评分术后2、4周可见水飞蓟素80mg/kg/d、水飞蓟素120mg/kg组骨痂生成量均比骨折模型组明显增多,但水飞蓟素各剂量组间无明显差异。术后6周,3组间均无统计学差异。结论:水飞蓟素对大鼠骨折早期愈合具有积极的促进作用。其促进大鼠胫骨骨折早期愈合作用可能与FGF-2的表达有关。

Dangfei Liganning Capsules (当飞利肝宁胶囊) Attenuate the Susceptibility of Rat Nonalcoholic Fatty Liver to Carbon Tetrachloride Toxicity

Objective: To test whether nonalcoholic hepatic steatosis sensitizes carbon tetrachloride (CCl4)-induced liver injury, and to assess the therapeutic effect of Chinese medicine extracts of Dangfei Liganning capsules (当飞利肝宁胶囊) and their potential underlying mechanisms. Methods: Male Wistar rats were fed a high-fat diet to induce nonalcoholic fatty liver disease (NAFLD) or a normal diet (N). Eight weeks later, a nonlethal dose of CCl4 was applied intraperitoneally. From the start, HF-CCl4 rats were administered daily Dangyao extracts (D), Dangfei Liganning capsules (DF), or Diammonium Glycyrrhizinate (G) intragastrically. Rats were sacrificed 48 h after CCl4 administration. In addition to serum biochemistry, liver histopathology was observed using hematoxylin-eosin (HE) and oil red O staining, and hepatic levels of triglyceride (TG), malondialdehyde (MDA), glutathione (GSH), superoxide dismutase (SOD), caspase-3 activation and cytochrome P450 (CYP2E1) expression were assessed. Results: There was almost no response to the nonlethal dose of CCl4 in the N control group. However, the HF group demonstrated massive steatosis, and elevated levels of serum ALT and AST, liver MDA, CYP2E1, and caspase-3 activation, whereas the levels of GSH and SOD were significantly decreased. All indexes assessed were dramatically worse in the HF-CCl4 group compared to the HF group, in addition to the more severe steatosis, hepatocyte ballooning, and inflammatory infiltration apparent in the centrilobular area. The medicines we tested affected the pathological changes in HF-CCl4 rats to differing degrees: DF and G led to improvements in all of the above examined indexes, including an obvious improvement in histopathology, and DF improved serum ALT and MDA levels more markedly than G, whereas D extracts produced only mild liver injury attenuation. Conclusion: Liver with NAFLD is more sensitive to hepatotoxicity; furthermore, the disrupted balance of oxidative stress and anti-oxidant defense contributes to the underlying mechanisms. Dangfei Liganning capsules potentially decrease this toxic susceptibility and alleviate liver injury in non-alcoholic fatty liver.

Stability of β-carotene microcapsules with Maillard reaction products derived from whey protein isolate and galactose as coating materials

The stability of β-carotene microcapsules using Maillard reaction products（MRPs） derived from whey protein isolate（WPI） and galactose as coating materials, was studied under the varying environmental conditions of temperature, pH, air, incandescent light, and ultraviolet（UV） light.Scanning electron microscopy showed that microcapsules prepared by WPI-galactose MRPs displayed a smooth and less concave-convex surface and that the particle size（D_（50）） of the microcapsules made with WPI-galactose MRPs was smaller than those made with WPI-galactose mixture.The storage stability of β-carotene microencapsulated in WPI-galactose MRPs was remarkably better than that of β-carotene microencapsulated in the WPI-galactose mixture and that of β-carotene crystal, in respect of temperature, pH, air, incandescent light, and UV light measurements.When the storage temperature was increased from 5 to 105 ℃, the retention rate of β-carotene microcapsules significantly decreased（P〈0.05）.When p H values were increased from 1 to 12, the β-carotene retention rate of the microcapsules significantly increased and afterward decreased.Compared with the retention rate of β-carotene microencapsulated in a WPI-galactose mixture, the retention rate of β-carotene microencapsulated in WPI-galactose MRPs was at a maximum between pH 8 and 9.Under the actions of air, incandescent light, and UV light, the retention rates of β-carotene microcapsules in WPI-galactose MRPs and WPI-galactose mixture, as well as in β-carotene crystal, decreased significantly as the storage time increased（P〈0.05）.Therefore, the use of WPI-galactose MRPs as coating materials can aid in improving the storage stability of β-carotene microcapsules.

Microencapsulated β-carotene preparation using different drying treatments

β-Carotene is one of the most abundant natural pigments in foods;however,usage of β-carotene is limited because of its instability.Microencapsulation techniques are usually applied to protect microencapsulated p-carotene from oxidization.In this study,β-carotene was microencapsulated using different drying processes:spray-drying,spray freeze-dryi ng,coati ng,and spray granulation.The properties of morphology,particle size,water con tent,thermal characteristic,and chemical stability have been explored and compared.Scanning electron microscopy measure?ments showed that the coated powder had a dense surface surro un ded by starch and suggested that the coati ng process gave a microencapsulated powder with the smallest bulk density and the best compressibility among the prepared powders.The chemical stabilities of microcapsules were evaluated during six months of storage at different temperatures.The coated powder had the highest mass fraction of β-carotene,which indicated that the coating process was superior to the three other drying processes.

Comparison of the effect and safety of Kuntai capsule and hormone replacement therapy in patients with perimenopausal syndrome:a systematic review and Meta-analysis

OBJECTIVE: To assess the effectiveness and safety of Kuntai capsule and hormone replacement therapy in treatment of perimenopausal syndrome.METHODS: Articles were retrieved from the databases Cochrane Database of Systematic Reviews,Pub Med, Chinese National Knowledge Infrastructure, China Science and Technology Journal Database, and Wanfang Database. Only randomized controlled trials were included; 15 trials involving1243 patients were identified from January 2005 to April 2015. A systemic review and Meta-analysis of publications was performed. The review was limit-ed to randomized controlled trials that compared Kuntai capsule and hormone replacement therapy to treat perimenopausal syndrome for at least 3months. The primary outcome assessed was the treatment efficacy at 3 months, including effective rate of Kupperman menopausal scores, Kupperman menopausal scores, and blood estradiol(E2) or blood follicle stimulating hormone(FSH) levels.Other outcomes assessed were safety or adverse events, such as gastrointestinal complaints, breast distending pain, or vaginal bleeding.RESULTS: Kupperman menopausal scores showed no significant difference in effective rate [odds ratio(OR): 1.05, 95% confidence intervals(CI): 0.71 to1.55] and changes in FSH level [mean difference(MD): 2.14, 95% CI:-2.36 to 6.65]. There was a significant statistical difference in Kupperman menopausal scores(MD:-1.14, 95% CI:-2.03 to-0.25)and changes in E2level(MD:-16.41, 95% CI:-18.83to-13.69). There were fewer adverse events in the Kuntai capsule group than in the hormone replacement therapy group(OR: = 0.35, 95% CI: 0.25 to0.48, P < 0.01).CONCLUSION: Compared with hormone replacement therapy, Kuntai capsule can improve perimenopausal symptoms and blood E2 levels, and reduce the incidence of adverse events.

Effect of naringenin in Qianggu capsule on population pharmacokinetics in Chinese women with primary osteoporosis

OBJECTIVE:To characterize naringenin(NAR) population pharmacokinetics(PPK) in Chinese women with primary osteoporosis.METHODS:Ninety-eight female patients with primary osteoporosis from the Jingshan,Beixinqiao,Jiaodaokou,Chaoyangmen,and Donghuamen communities in Beijing,China,aged 40 to 80 years,received oral Qianggu capsules(250 mg).Blood samples were collected before and at 0.5,1,2,3,4,6,8,10,12,and 24 h after administration.The concentration of NAR in the blood samples was measured using high performance liquid chromatography-tandem mass spectrometry.PPK analyses were performed with nonlinear mixed-effect modeling software(version 7.1.2,PsN3.2.12).The clearance(C1),central distribution volume(V),absorption rate constant(Ka1),peripheral distribution volume(VII),and inter-compartmental clearance(CLII) were set as parameters and estimated by the base model,covariate model,and final model.Kidney-Yang deficiency[Shenyangxu(SYAX)]and liver-kidney-Yin deficiency(Ganshenyinxu) are patterns of symptoms in Traditional Chinese Medicine that were set as covariates,along with age,height,blood urea nitrogen,serum creatinine,alanine transaminase,aspartate transaminase,and hyperlipidemia.Both stepwise forward and backward procedures were accomplished to build models.The final model was evaluated by internal and external validation,visual predictive check,bootstrap,and leverage analysis.RESULTS:A one compartment open model with first order degradation was the best fitted to the concentration-time profiles following oral administration of NAR.The mean of population parameters of the final model,C1,SYAX on C1,V,Ka1,CLII,and VII,were measured to be 37.6 L/h,0.427 L,123 L/h,0.12/h,0.3056,and 1.446,respectively.Inter-individual variability was estimated and SYAX was identified as a significant covariate.CONCLUSION:The population pharmacokinetic model described in this study could effectively characterize the pharmacokinetic profile of NAR following administration of a single dose of oral Qianggu capsules in Chinese women with primary osteoporosis.Among the tested covariates,only SYAX was a significant factor.