Design of a gastroretentive mucoadhesive dosage form of furosemide for controlled release

The aim of the present study was to develop and characterize a gastroretentive dosage form suitable for controlled drug release.It consists of a drug loaded polymeric film made up of a bilayer of immediate(IR)and controlled release(CR)layers folded into a hard gelatin capsule.Gast roretention results from unfolding and swelling of the film and its bioadhesion to the gastric.mucosa.Furosemide,a drug with a narrow absorption window,was selected as the model drug.Inclusion of hydroxypropyl β-cyclodextrin in both layers and Carbopol■ 971P NF in the CR layer of the bilayer film resulted in optimum drug release,bioadhesion and mechanical properties.The film with zig-zag folding in the capsule was shown to unfold and swell under acidic conditions and provide IR of drugover 1 hand CR for up to 12 h in acidic medium.X-ray diffraction,differential scanning calorimetry and scanning electron microscopy revealed uniform dispersion of furosemide in the polymeric matrices.The results indicate the dosage form is gastroretentive and can provide controlled release of drugs with narrow therapeutic wind ows.

Effects of probiotics and its fermented milk on constipation: a systematic review

This study reviewed clinical evidence of probiotics-mediated effects on constipation.Four databases were used in the literature searches,namely Cochrane Library,Embase,Pubmed,and Web of Science.The last retrieval time was March 2021.Collected data were analyzed by Review Manager(version 5.3)and Stata(version 14).The primary search retrieved 8418 articles after removing duplicates.Eventually,26 studies were included in the meta-analysis.Administration of probiotics signifi cantly increased stool frequency(MD:1.15 times/week;95%CI:0.59 to 1.70;P<0.0001),improved bloating(MD:-0.48;95%CI:-0.89 to-0.07;P=0.02),reduced abdominal pain(MD:-0.71;95%CI:-1.25 to-0.16;P=0.01),and improved quality of life(MD:-0.73;95%CI:-1.37 to-0.10;P=0.02).However,the clinical effect of intake of probiotics on stool consistency was non-signifi cant(MD:0.07;95%CI:-0.34 to 0.48;P=0.73).Based on our analysis,probiotic supplements were effective in relieving constipation through symptom improvement.The effectiveness of dosage forms of intervention ranked:capsules>others(tablets,powder)>fermented milk.

Voltammetric behavior of sedative drug midazolam at glassy carbon electrode in solubilized systems

Redox behavior of midazolam was studied at a glassy carbon electrode in various buffer systems,supporting electrolytes and pH using differential pulse,square-wave and cyclic voltam-metry.Based on its reduction behavior,a direct differential pulse voltammetric method has been developed and validated for the determination of midazolam in parenteral dosage.Three well-defined peaks were observed in 0.1% SLS,Britton-Robinson (BR) buffer of pH 2.5.The effect of surfactants like sodium lauryl sulfate (SLS),cetyl trimethyl ammonium bromide (CTAB) and Tween 20 was studied.Among these surfactants SLS showed significant enhancement in reduction peak.The cathodic peak currents were directly proportional to the concentration of midazolam with correlation coefficient of 0.99.

新型液相色谱-荧光检测法测定药物剂型和人血浆中的他达拉非和盐酸达泊西汀(英文)

Tadalafil(TAD)and dapoxetine HCl(DAP)are recently co-formulated and both show native fluorescence.Therefore,a novel,accurate,specific and sensitive reversed-phase high performance liquid chromatographic method with fluorescence detection was developed and validated for their separation and quantitation in dosage form and human plasma using avanafil as an internal standard(IS).Separation was achieved using isocratic elution within 7.0 min on C18column and acetonitrile-0.15%triethylamine(40∶60,v/v;pH 4)as a mobile phase.The flow rate was 1.0 mL/min and the detection was time-programmed at 330,410 and 370 nm for TAD,DAP and IS,respectively,after excitation at 236 nm.The linear ranges from 0.01 to 30.00μg/mL for each drug with the limits of detection of 4.20 and 7.20 ng/mL for TAD and DAP,respectively.The method was validated in accordance to the International Conference on Harmonization(ICH)guidelines and was successfully applied to spiked human plasma with mean recoveries of 98.17%and 98.83%for TAD and DAP respectively.

Pharmaceutical cocrystals: A review of preparations, physicochemical properties and applications

Pharmaceutical cocrystals are multicomponent systems in which at least one component is an active pharmaceutical ingredient and the others are pharmaceutically acceptable ingredients.Cocrystallization of a drug substance with a coformer is a promising and emerging approach to improve the performance of pharmaceuticals,such as solubility,dissolution profile,pharmacokinetics and stability.This review article presents a comprehensive overview of pharmaceutical cocrystals,including preparation methods,physicochemical properties,and applications.Furthermore,some examples of drug cocrystals are highlighted to illustrate the effect of crystal structures on the various aspects of active pharmaceutical ingredients,such as physical stability,chemical stability,mechanical properties,optical properties,bioavailability,sustained release and therapeutic effect.This review will provide guidance for more efficient design and manufacture of pharmaceutical cocrystals with desired physicochemical properties and applications.

Randomized Clinical Trials of Traditional Chinese Medicines for Treating Ulcerative Colitis:A Scoping Review

Objective:Traditional Chinese medicines(TCMs)are efficacious against ulcerative colitis(UC).In recent years,the number of randomized clinical trials(RCTs)of TCM has increased.Thus,it is very important to summarize the basic characteristics,quality,and types of TCM interventions in published RCTs.This scoping review was performed to systematically identify and describe the current situations about RCTs of TCMs for treating UC.Hope to express the focus and specifics of nowadays research in TCM interventions in RCTs and evaluate their common disadvantages exposed to help advance in TCM researching.Materials and Methods:A scoping review was conducted according to the PRISMA extension for scoping reviews.We searched two English databases and four Chinese databases from the date of establishment of each database to January 2020.Data from RCTs focusing on any TCM treatment for patients with UC were extracted and evaluated.Selection and characterization were performed by two independent reviewers using predefined forms.All discrepancies were resolved by consensus discussion with a third reviewer.Microsoft Excel 2010 was used to extract the following data from the included studies:(1)basic information of the included studies including research ID,article title,publication language,journal,year of publication,and funding information;(2)patient information including gender,age,disease course,disease stage,severity,sample size;and(3)information on intervention measures,types of intervention measures,drug dosage forms,and treatment courses.Results:The search identified 2225 RCTs published between1987 and 2020.These studies covered 36 provinces in China.The time frame of the RCTs was<28 days in approximately one-third of the RCTs(647,29.08%).Only one RCT was published in English.Nearly three-quarters of RCTs(1665,74.83%)did not report the severity of the disease.Three types of interventions were included in the RCTs:pharmacotherapy(2028,91.15%),nonpharmacotherapy(57,2.56%),and a combination of the two(140,6.29%).The administration modes of the intervention groups were evaluated.Drug therapy involved 12types of TCM dosage forms,which were decoctions,troches,powders,capsules,granules,pills,suppositories,ointments,injections,gels,oral liquids,and substitute tea according to the frequency of use.Nondrug intervention measures involved 10 treatment options,namely,acupuncture,moxibustion,hemospasia,auricular point,acupoint catgut embedding,acupoint injection,scrapping,tuina,acupoint application,and five-tone therapy according to the frequency of use.Most studies included in this review were low in quality.This underscores the need for improvement in the quality of trial methodology in TCM RCTs.

Are the release characteristics of Erzhi pills in line with traditional Chinese medicine theory?A quantitative study

Objective:Traditional Chinese medicine(TCM)has been widely used throughout China to prevent and cure diseases for thousands of years,and now it is a part of the integrative medicine field that is available in Western societies.To ensure the safety and quality of the herbal medicines that are a major part of the TCM tradition,they must be held to modern pharmaceutical standards.Erzhi pill(EZP)is a Chinese Pharmacopeia-listed herbal preparation that is used in the long-term clinical management of postmenopausal symptoms,osteoporosis and menstrual disorders.Until now,whether the drug release mechanism of EZP is in line with its intended TCM usage has not been studied.Methods:The release of specnuezhenide from three EZPs(self-made,Leiyunshang and Renhe)in simulated gastric fluid(SGF),acetate buffer(p H 4.5 buffer)and simulated intestinal fluid(SIF)was investigated in a dissolution test.The water uptake capacity and erosion extent of the three EZPs were investigated using swelling and erosion studies.The drug release mechanism was further assessed through statistical model fitting,using DDSolver software.Results:The release of specnuezhenide from all three EZPs in SGF was less than 50%within a 4 h period.However,over 70%of the specnuezhenide was released from each EZP in both p H 4.5 buffer and SIF in the same time.Analysis of the swelling and erosion behaviors and the drug release mechanism of the three EZPs confirmed that the release rate from EZP followed a sustained release profile,which was an interactive combination of swelling and erosion.Conclusion:This study showed that the release pattern from the pills was in line with the intended TCM use of EZP.TCM had not only theoretically considered sustained release from the pills,but also formulated them to achieve this release pattern.When establishing quality control standards for pills,the theoretical TCM usage and the actual release patterns need to be considered.