Dissolution Technologies最新文献_第7页

In Vitro Solubility and Release Profile Correlation with pKa Value of Efavirenz Polymorphs 依非韦伦多晶型药物的体外溶解度和释放谱与pKa值的相关性

IF 0.6 4区医学

Dissolution Technologies Pub Date : 2021-01-01 DOI: 10.14227/dt280321p14

Yoga Windhu Wardhana, Eli Nur Aisyah, I. Sopyan, T. Rusdiana

{"title":"In Vitro Solubility and Release Profile Correlation with pKa Value of Efavirenz Polymorphs","authors":"Yoga Windhu Wardhana, Eli Nur Aisyah, I. Sopyan, T. Rusdiana","doi":"10.14227/dt280321p14","DOIUrl":"https://doi.org/10.14227/dt280321p14","url":null,"abstract":"Efavirenz (EFV) was approved by the United States Food and Drug Administration in 1998 with no polymorphic forms, but further research defined 23 different forms, including amorphous and solvated forms. This study aims to determine the ability of dissolved EFV polymorphs in in vitro media kinetic release models of pKa values. The polymorph types were obtained through various organic solvents such as acetonitrile, n-hexane, and methanol, i.e., form I, II, and III. The characteristics were distinguished by polarisation microscopy, differential scanning calorimetry (DSC), Fourier transform infrared (FTIR), and Raman spectroscopy. The solubility and dissolution of each polymorph were examined by adding 0.25% sodium lauryl sulphate (SLS) to the comparative dissolution media (water, HCl at pH 1.2, phosphate buffer at pH 4.6 and 6.8). The different microscopic shapes provided a unique fingerprint in the FTIR and the Raman spectra. The thermal behaviour examination provided a DSC thermogram with a specific melting point for each polymorph. The results of the solubility and dissolution tests reported that the highest peak was reached by form II, followed by forms III and I. These followed the pKa values of each polymorph, namely 10.12, 10.63, and 10.37 for form I, II, and III, respectively. The dissolution profile shows that pH conditions affect the release kinetics of form I compared to the metastable forms. The kinetic model of form I is pH-dependent; the acidic medium provided a slower release rate. Unlike the metastable forms, drug loading remained constant but still followed Higuchi’s kinetic release model, even in acidic medium.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66813128","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 2

Summary Report on Workshop on In Vitro Release Test (IVRT) and In Vitro Permeation Test (IVPT) Methods 体外释放试验(IVRT)和体外渗透试验(IVPT)方法研讨会总结报告

IF 0.6 4区医学

Dissolution Technologies Pub Date : 2021-01-01 DOI: 10.14227/dt280421p450

K. Thakker

引用次数: 1

A Data Set to Verify Volume and Sample Removal Correction Calculations for Dissolution Testing 一个数据集，以验证体积和样品去除校正计算溶解测试

IF 0.6 4区医学

Dissolution Technologies Pub Date : 2021-01-01 DOI: 10.14227/DT280221P16

Alger D. Salt

引用次数: 1

Questions and Answers August 2021 2021年8月

IF 0.6 4区医学

Dissolution Technologies Pub Date : 2021-01-01 DOI: 10.14227/dt280321p46

Margareth R. C. Marques, M. Liddell

引用次数: 0

A BCS-Based Biowaiver Approach Using Biphasic Dissolution Test 基于bcs的双相溶出试验生物去除方法

IF 0.6 4区医学

Dissolution Technologies Pub Date : 2021-01-01 DOI: 10.14227/dt280421p40

Daniela Amaral Silva, K. J. Curo Melo, N. Davies, N. Bou-Chacra, H. Ferraz, R. Löbenberg

{"title":"A BCS-Based Biowaiver Approach Using Biphasic Dissolution Test","authors":"Daniela Amaral Silva, K. J. Curo Melo, N. Davies, N. Bou-Chacra, H. Ferraz, R. Löbenberg","doi":"10.14227/dt280421p40","DOIUrl":"https://doi.org/10.14227/dt280421p40","url":null,"abstract":"Biowaivers based on the Biopharmaceutics Classification System (BCS) class can be used to establish therapeutic equivalence based on dissolution tests, which can be used as a surrogate to determine if two pharmaceutical equivalent products are interchangeable (i.e., bioequivalent). The objective of the present study was to use a biphasic dissolution system to replicate a study in which the authors followed compendial methods to examine the in vitro performance of widely used drug products. Furthermore, since biphasic dissolution studies are mainly applied to poorly soluble drugs, the present study was conducted to broaden its application to highly soluble drugs. The approach taken in this manuscript was to have scientific insight and mechanistic understanding rather than a strict regulatory application. In the initial study, none of the tested metronidazole products were (in vitro) equivalent to the comparator pharmaceutical product (CPP) or to other manufacturers. We hypothesized that whereas in vitro equivalence was not achieved in compendial methods, the partitioning profile to the organic phase in the biphasic system could signal in vitro equivalence between the tested drug products and CPP. In the aqueous phase of the biphasic system, the tested metronidazole products followed a similar pattern as obtained in the compendial buffer; however, this was not the case for the organic phase partition profiles. All the tested products had a good correlation to the CPP, which could indicate in vitro equivalence between these products. This could potentially allow for a biowaiver application. Hence, the application of biphasic dissolution to highly soluble drugs might be beneficial to estimate the product’s in vivo behavior. Further clinical studies would be needed to confirm these findings to guarantee their interchangeability.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66813321","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Questions and Answers May 2021 2021年5月

IF 0.6 4区医学

Dissolution Technologies Pub Date : 2021-01-01 DOI: 10.14227/DT280221P43

Margareth R. C. Marques, M. Liddell

引用次数: 0

Questions and Answers November 2021 2021年11月

IF 0.6 4区医学

Dissolution Technologies Pub Date : 2021-01-01 DOI: 10.14227/dt280421p54

Margareth R. C. Marques, M. Liddell

引用次数: 0

Evaluation of In Vitro Equivalence of Commonly Available Generic Brands of Amlodipine Tablets in Saudi Arabia Under Biowaiver Conditions 沙特常用仿制药氨氯地平片在生物豁免条件下的体外等效性评价

IF 0.6 4区医学

Dissolution Technologies Pub Date : 2021-01-01 DOI: 10.14227/DT280221PGC1

A. Najmi, Mohammed Al Bratty, B. Al-Bassam, Rami Ali Aseri, Turki Suliman Wadani, Abdulrahman Ibrahim Al-Muntashiri, H. A. Alhazmi, M. Sultan, S. Javed

{"title":"Evaluation of In Vitro Equivalence of Commonly Available Generic Brands of Amlodipine Tablets in Saudi Arabia Under Biowaiver Conditions","authors":"A. Najmi, Mohammed Al Bratty, B. Al-Bassam, Rami Ali Aseri, Turki Suliman Wadani, Abdulrahman Ibrahim Al-Muntashiri, H. A. Alhazmi, M. Sultan, S. Javed","doi":"10.14227/DT280221PGC1","DOIUrl":"https://doi.org/10.14227/DT280221PGC1","url":null,"abstract":"When a medicine is not able to treat the disease for which it was intended, as in case of substandard and falsified drug products, it may prolong the disease and in worst scenario, the patient may die because of the untreated illness or the product itself. To ensure the quality and safety of medicine, WHO recommends timely evaluation of pharmaceutical quality. The present study is an attempt to evaluate the pharmaceutical properties and in vitro drug release of four generic brands and one innovator product (Norvasc) of amlodipine tablets (5 mg) according to USP and WHO guidelines. The products passed the compendial specifications of weight variation (˂ 5% deviation), friability (˂ 1% weight loss), and assay (90–110% of labeled amount). The tablets were fast-disintegrating, as complete disintegration observed in 1.20–1.64 min. The dissolution profiles of the generic products were equivalent to the innovator brand in pH 1.2 HCl and acetate buffer (pH 4.5) without statistical treatment (≥ 85% release in 15 min). In phosphate buffer (pH 6.8), ≥ 85% of drug dissolved in 30 min and in vitro equivalence was established by calculating the difference factor (f1 ˂ 15), similarity factor (f2 ˃ 50), and dissolution efficiency (± 10%). The tested brands met WHO BCS-based biowaiver criteria for in vitro dissolution testing, which ensured their pharmaceutical and therapeutic equivalence without in vivo screening and interchangeability with the innovator product.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"3 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66813461","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

Comparison of Efavirenz Release in Biorelevant Dissolution Media Using Manual Sampling and In Situ UV Fiber Optic System 人工取样与原位紫外光纤系统对依非韦伦在生物相关溶出介质中释放的比较

IF 0.6 4区医学

Dissolution Technologies Pub Date : 2021-01-01 DOI: 10.14227/dt280321p6

Thalita Martins da Silva, Marcelo Chaves, B. F. C. Patricio, H. Rocha

{"title":"Comparison of Efavirenz Release in Biorelevant Dissolution Media Using Manual Sampling and In Situ UV Fiber Optic System","authors":"Thalita Martins da Silva, Marcelo Chaves, B. F. C. Patricio, H. Rocha","doi":"10.14227/dt280321p6","DOIUrl":"https://doi.org/10.14227/dt280321p6","url":null,"abstract":"There has been a growing interest in the use of biorelevant dissolution media in drug formulations research and development. Biorelevant media mimic the physiological conditions of the human gastrointestinal tract, which allows for a more discriminating dissolution test. That is even more important for poorly soluble drugs, like efavirenz and other class II (Biopharmaceutical Classification System) drugs. Traditionally, these media were used in the compendial standard dissolution apparatus; however, reduced automation of the conventional tests could be, in general, costly, high-labor, and error-prone. Thus, the use of in situ ultraviolet (UV) fiber optic probes has been applied in research and development and in quality control routines for drug manufacturing. The present study aims to assess the suitability of an in situ UV dynamic monitoring system for characterization of dissolution behavior of 600-mg efavirenz immediate-release coated tablets in different biorelevant media by comparison with traditional manual sampling. The biorelevant media used were fasted and fed state simulated intestinal fluid (FaSSIF, FaSSIF-V2, FeSSIF, FeSSIF-V2) and SLS (0.5%). Both sampling methods were similar for FaSSIF, FaSSIF-V2, and SLS. For FeSSIF and FeSSIF-V2, the results were statistically different due to high concentration of oxidation phospholipids and degradation lipids in these media. These results support the use of dynamic monitoring of dissolution in FaSSIF, FaSSIF-V2, and SLS, and inform understanding of the rate-limiting steps, which may improve quality and accuracy in data acquisition for dissolution tests with biorelevant media.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66813272","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Quality Assessment of Brands of Prednisolone (5 Mg) Tablets Marketed in Abuja Metropolis of Nigeria 尼日利亚阿布贾市售品牌强的松龙(5mg)片质量评价

IF 0.6 4区医学

Dissolution Technologies Pub Date : 2021-01-01 DOI: 10.14227/DT280121P24

J. Isaac, Galadima I. Hayatu, J. E. John, K. Ekere, Aisha Daburi, Sunday O. Omachoko, Philip F. Buiders

引用次数: 2