Dissolution Technologies最新文献_第9页

The Case for Physiologically Based Biopharmaceutics Modelling (PBBM): What do Dissolution Scientists Need to Know? 基于生理学的生物制药模型(PBBM)的案例:溶解科学家需要知道什么?

IF 0.6 4区医学

Dissolution Technologies Pub Date : 2020-01-01 DOI: 10.14227/dt270320p6

V. Gray, J. Mann, Ric Barker, X. Pepin

{"title":"The Case for Physiologically Based Biopharmaceutics Modelling (PBBM): What do Dissolution Scientists Need to Know?","authors":"V. Gray, J. Mann, Ric Barker, X. Pepin","doi":"10.14227/dt270320p6","DOIUrl":"https://doi.org/10.14227/dt270320p6","url":null,"abstract":"The purpose of this article is to inform the dissolution scientist of a powerful emerging tool that provides in vivo linkage to dissolution methods. This tool is physiologically based biopharmaceutics modelling (PBBM). Dissolution scientists are mostly concerned with analytical sections of drug development, so exposure to modeling and other pharmacokinetics and biopharmaceutic concepts may be uncommon. PBBM is an in-silico model that focuses on the interactions between the in vivo physiology and the formulation and drug characteristics. The principles behind PBBM is that all mechanisms related to drug release, dissolution, and diffusion from the site of administration to the site of action can be described in a mechanistic way or semi-empirical way. The integration of in vitro dissolution data in PBBM is described, including examples of software and modeling applications. The expertise needed to use the software and appropriate training is discussed. The key inputs that are expected from the dissolution scientist include an understanding of the aqueous solubility across the physiological pH range, impact of in vivo relevant bile salts and phospholipids on solubilization, and the impact of surface pH on dissolution rate. An example of an advanced in vitro system, TNO intestinal model (TIM-1), will be discussed and its importance in establishing a biorelevant understanding of dissolution behavior. PBBM can evaluate the clinical relevance of a dissolution method and justify specifications and ultimately provide an approval advantage to the sponsor. A well-supported dissolution method that provides clinically relevant drug product specifications (CRDPS) will be viewed with favor by the regulators. Therefore, the partnering of a dissolution scientist and biopharmaceutics scientist to develop PBBM is clearly an important step forward in drug development.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"27 1","pages":"6-19"},"PeriodicalIF":0.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66812689","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: 11

Amorphous Solid Dispersions in Early Stage of Formulation Development: Predicting Excipient Influence on Dissolution Profiles Using DDDPlus 配方开发早期阶段的非晶固体分散体:使用DDDPlus预测辅料对溶解谱的影响

IF 0.6 4区医学

Dissolution Technologies Pub Date : 2020-01-01 DOI: 10.14227/dt270220p6

J. Njoku, Dwaipayan Mukherjee, G. K. Webster, R. Löbenberg

{"title":"Amorphous Solid Dispersions in Early Stage of Formulation Development: Predicting Excipient Influence on Dissolution Profiles Using DDDPlus","authors":"J. Njoku, Dwaipayan Mukherjee, G. K. Webster, R. Löbenberg","doi":"10.14227/dt270220p6","DOIUrl":"https://doi.org/10.14227/dt270220p6","url":null,"abstract":"Excipients play an important role in the formulation of dosage forms and can be used to improve the bioavailability of a drug through physical interactions that alter the rate of dissolution of a drug. The objective of this study was to predict the effect of formulation on the dissolution rate of a poorly soluble drug using computer simulations. Solid dispersion of ritonavir was prepared. Dissolution test results of direct compressed tablets with and without disintegrant in various media with physiologically relevant pH were compared with simulations. Solubilizer and disintegrant effect were evaluated on the Dose, Disintegration, and Dissolution Plus (DDDPlus) simulation software (version 5.0.0011, Simulations Plus, Inc., Lancaster, CA, USA) using previously published solubility data on ritonavir. Observed and predicted dissolution profiles similarity tests and drug release mechanisms were assessed. Optimization of the solubilizer effect coefficient (SEC) on the program gives good estimations of the effect of copovidone in the solid dispersion in the dissolution profiles of all tablets. The SEC is dependent on the solubility of the active pharmaceutical ingredient (API) at the local pH and the dissolved concentration of the solubilizer. Disintegrant concentration in the program has no effect on simulations, rather the disintegration time was the predictive factor. Drug release was formulation controlled in the tablets without disintegrant and in the tablets with disintegrant was via drug diffusion and polymer surface erosion. DDDPlus has the potential to estimate the effect of excipients in a formulation on in vitro dissolution at an early stage in the drug development process. This could be useful in decisions on formulation strategies to enhance bioavailability in poorly soluble drugs.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"27 1","pages":"6-13"},"PeriodicalIF":0.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66813007","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

A Look at Cleaning Effectiveness in Automated Dissolution Systems 自动溶解系统的清洁效果研究

IF 0.6 4区医学

Dissolution Technologies Pub Date : 2020-01-01 DOI: 10.14227/dt270220p14

G. K. Webster, Xi Shao, K. Nelson, Matthew A. Gragg

引用次数: 0

Drug Release Pattern of Oral Dual-Release Pellets Through the Gastrointestinal Tract: Case Example of Diclofenac Sodium 口服双释放微丸经胃肠道的药物释放模式:以双氯芬酸钠为例

IF 0.6 4区医学

Dissolution Technologies Pub Date : 2020-01-01 DOI: 10.14227/dt270220p22

R. Hamed, S. Alnadi

{"title":"Drug Release Pattern of Oral Dual-Release Pellets Through the Gastrointestinal Tract: Case Example of Diclofenac Sodium","authors":"R. Hamed, S. Alnadi","doi":"10.14227/dt270220p22","DOIUrl":"https://doi.org/10.14227/dt270220p22","url":null,"abstract":"The purpose of this research was to evaluate the release pattern of the dual-release pellets of diclofenac sodium (DS), coated with entericand sustained-release layers, in dissolution media that resemble the physiological variables of the gastrointestinal (GI) fluid. Dissolution testing in three pH stages (acidic, intermediate, and basic) was conducted using USP apparatus I (basket) rotating at 100 rpm. The acidic pH stage resembles the gastric fluid during fasted and fed states, the intermediate pH stage resembles the fluid of the proximal small intestine (duodenal fluid), and the basic pH stage resembles the fluid of the small intestine during fasted and fed states and distal GI. DS pellets showed excellent gastric resistance in the acidic pH stage for 2 h. In the intermediate pH stage, DS pellets showed a gastric resistance for 2 h, followed by a low percent of DS release thereafter (15.2% after 10 h). DS release was accelerated in the basic pH stage, particularly in pH media 6.5–7.2. This is because the enteric-coated film starts to dissolve at pH > 5.5. In addition, DS release was influenced by the buffer capacity (β)/ionic strength (I) of the dissolution media, where DS release increased with increasing β/I of phosphate buffers (pH 6.8) up to a concentration of 50 mM and then decreased at 100 mM. These dissolution results corroborated with equilibrium solubility data and sink conditions (S values) of DS in the media of the three pH stages. This study provides an insight into the release pattern of the dual-release DS pellets throughout the GI tract to better correlate the in vitro release data of these pellets to those in vivo.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"27 1","pages":"22-30"},"PeriodicalIF":0.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66812190","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 August 2020 2020年8月

IF 0.6 4区医学

Dissolution Technologies Pub Date : 2020-01-01 DOI: 10.14227/dt270320p44

Margareth R. C. Marques, M. Liddell

引用次数: 1

In Vitro Comparative Quality Evaluation of Non-Expired and 10 Years-Expired Lamotrigine Immediate-Release Tablet Formulations - Pilot Study 未过期和过期10年拉莫三嗪速释片的体外质量比较研究

IF 0.6 4区医学

Dissolution Technologies Pub Date : 2020-01-01 DOI: 10.14227/dt270120p14

Gordana Švonja Parezanović, M. Lalic-Popovic, S. Goločorbin-Kon, N. Todorović, N. Pavlović, M. Mikov

{"title":"In Vitro Comparative Quality Evaluation of Non-Expired and 10 Years-Expired Lamotrigine Immediate-Release Tablet Formulations - Pilot Study","authors":"Gordana Švonja Parezanović, M. Lalic-Popovic, S. Goločorbin-Kon, N. Todorović, N. Pavlović, M. Mikov","doi":"10.14227/dt270120p14","DOIUrl":"https://doi.org/10.14227/dt270120p14","url":null,"abstract":"This study aimed to compare the different physical parameters and dissolution profiles of 10 years-expired with nonexpired lamotrigine (LTG) immediate-release tablet formulations. Dissolution tests were conducted using a validated high-performance liquid chromatography method. Dissolution characteristics of the tablet formulations were evaluated at three points spanning the physiological pH range (pH 1.2, pH 4.5, pH 6.8). Physical characteristics of LTG tablets were determined according to the European Pharmacopoeia. The dissolution profile comparison was carried out using model-independent (statistical) and model-dependent (kinetic) methods to provide detailed information about dissolution data. The t-test was applied to investigate differences between expired and non-expired tablets, and the differences were considered statistically significant if p ≤ 0.05. The results demonstrated no statistical differences in physical characteristics between expired and non-expired tablets; however, there were differences in the dissolution profiles, which could cause different pharmacokinetic profiles. The results of this investigation showed that the drug content did not change significantly. Therefore, the lower dissolution rate for expired LTG tablets is due to an interaction of LTG with one or more excipients in the tablet formulation during aging.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"27 1","pages":"14-20"},"PeriodicalIF":0.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66812437","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

Effect of Medium pH on In Vitro Dissolution of Marketed Tetracyclines (Tetracycline and Doxycycline) Solid Oral Dosage Forms in Bahia, Brazil 培养基pH对巴西巴伊亚市市售四环素(四环素和强力霉素)固体口服剂型体外溶出度的影响

IF 0.6 4区医学

Dissolution Technologies Pub Date : 2020-01-01 DOI: 10.14227/dt270220p32

João Luís Silva Oliveira, Gilmar Antônio de Carvalho Teles Júnior, Desirée A. Bonfim, Carlos Magno Ramos Carvalho Júnior, Jéssica A. Santos, M. S. Ferreira, A. Júnior

{"title":"Effect of Medium pH on In Vitro Dissolution of Marketed Tetracyclines (Tetracycline and Doxycycline) Solid Oral Dosage Forms in Bahia, Brazil","authors":"João Luís Silva Oliveira, Gilmar Antônio de Carvalho Teles Júnior, Desirée A. Bonfim, Carlos Magno Ramos Carvalho Júnior, Jéssica A. Santos, M. S. Ferreira, A. Júnior","doi":"10.14227/dt270220p32","DOIUrl":"https://doi.org/10.14227/dt270220p32","url":null,"abstract":"Tetracyclines are widely used for the treatment of infections of the lower respiratory tract and other systems. In Brazil, tetracyclines are available as generic and similar products. The aim of this study was to evaluate the in vitro release of tetracycline capsules (500 mg) and doxycycline tablets (100 mg) in different reaction media, from dissolution profiles, using sensitive and rapid ultraviolet spectrophotometric methods. The dissolution test was used to obtain and compare dissolution profiles and establish similarities of pharmaceutical formulations in compliance with the Brazilian (for tetracycline hydrochloride capsules) and United States (USP) (for doxycycline hydrochloride tablets) pharmacopoeia. For both drugs, the dissolution studies were conducted using an USP type 2 apparatus at 75 rpm with 1000 mL distilled water at 37.0 ± 0.5 oC for 90 minutes, to evaluate the influence of pH (1.0–8.0) on the release of drugs. The methods were validated, showing precision, linearity, and accuracy. All the products satisfactorily released tetracycline and doxycycline, with at least 80% of the drug dissolved within 30 minutes. Tetracycline and doxycycline are weak acids, which favors their dissolution in acid media (pH range 1.0–6.0). This research contributes to studies that guarantee the quality control of tetracyclines and to the expansion of the novel methodologies established by the Brazilian Pharmacopoeia for doxycycline.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"27 1","pages":"32-40"},"PeriodicalIF":0.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66812935","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

In Vitro Bioequivalence of Pregabalin Capsules (150 mg): An Alternative to In Vivo Bioequivalence Studies 普瑞巴林胶囊(150mg)的体外生物等效性:体内生物等效性研究的另一种选择

IF 0.6 4区医学

Dissolution Technologies Pub Date : 2020-01-01 DOI: 10.14227/dt270420p24

Shahnaz Usman, A. Saeed, Sakina Fatima, V. Ramesh, F. Shah, Quamrul Islam

{"title":"In Vitro Bioequivalence of Pregabalin Capsules (150 mg): An Alternative to In Vivo Bioequivalence Studies","authors":"Shahnaz Usman, A. Saeed, Sakina Fatima, V. Ramesh, F. Shah, Quamrul Islam","doi":"10.14227/dt270420p24","DOIUrl":"https://doi.org/10.14227/dt270420p24","url":null,"abstract":"Introduction: We aimed to study the dissolution behavior of available brands of pregabalin in the United Arab Emirates (UAE) (Ras Al Khaimah) market and to report efficiency and fungibility data for generic brands under biowaiver conditions. Methods: The pharmaceutical parameters of five brands of pregabalin 150 mg capsules were analyzed, including the reference product and four generic products. Dissolution tests were performed as per WHO and FDA recommendations (pH 1.2, 4.5, and 6.8). United States Pharmacopeia (USP) apparatus 2 (paddle, 50 rpm) was used to assess drug release. Multiple time points were measured to estimate the drug release profile of the capsules. Pharmacokinetic models and similarity factor analysis were performed. Results: The percentage of drug release within 15 minutes was 95–102% at pH 1.2, 86–95% at pH 4.5, and 89–98% at pH 6.8. Different kinetic models were used to analyze the suitability level of drug release from the different capsules. In all the three buffers, first order kinetics and the Korsmeyer–Peppas model demonstrated the drug release with R2 ≥ 0.95, which helps to predict and evaluate the acceptability level of drug release. The similarity and difference factor results were within the acceptable range for all capsules. Conclusion: The dissolution profiles of all tested capsules of pregabalin in the UAE market are pharmaceutically and therapeutically equivalent. The results indicate that the post-market analysis is essential for determining interchangeability of different brands of the same drug.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"27 1","pages":"24-31"},"PeriodicalIF":0.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66812706","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

In Vitro Comparative Dissolution Assessment of Different Brands of Co-Amoxiclav Tablets in Pakistan 不同品牌复方阿莫昔拉夫片在巴基斯坦的体外比较溶出度评价

IF 0.6 4区医学

Dissolution Technologies Pub Date : 2020-01-01 DOI: 10.14227/dt270420pgc1

M. Waqas, R. Ali, M. Usman, Muhammad Shahid, A. Rasul, B. Khan, G. Murtaza

{"title":"In Vitro Comparative Dissolution Assessment of Different Brands of Co-Amoxiclav Tablets in Pakistan","authors":"M. Waqas, R. Ali, M. Usman, Muhammad Shahid, A. Rasul, B. Khan, G. Murtaza","doi":"10.14227/dt270420pgc1","DOIUrl":"https://doi.org/10.14227/dt270420pgc1","url":null,"abstract":"Dissolution test results are the principal indicator in estimating the in-vivo bioavailability of most oral solid dosage forms and are an important quality attribute to assess the generic formulation. This study was designed to assess the release of co-amoxiclav from finished pharmaceutical solid dosage formulations. Both innovator and generic tablets of co-amoxiclav were subjected to dissolution testing (USP method 2 and HPLC). The innovator’s product (product A) met compendial criteria regarding bioavailability of both amoxicillin and clavulanic acid. The two generic brands, product B and C, failed to meet the criteria for release of amoxicillin (i.e., 80–85%); however, they did achieve 100% release of clavulanic acid in the initial half hour. Moreover, analysis showed significant variance between the innovator’s and generic brands (p < 0.05 for both of amoxicillin products). Hence, the innovator’s and generic brands are not bioequivalent for amoxicillin release, despite both compliance with limits for clavulanic acid release. Failure to achieve dissolution standards argues that compliance with compendial guidelines is critical for generic manufacturing of co-amoxiclav.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66812793","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 November 2020 2020年11月

IF 0.6 4区医学

Dissolution Technologies Pub Date : 2020-01-01 DOI: 10.14227/dt270420p42

Margareth R. C. Marques, M. Liddell

引用次数: 0