Dissolution Technologies最新文献

{"title":"Dissolution Method Evaluation for Carvedilol Tablets","authors":"Josyane Márcia Vasconcelos Alves, Livia D. Prado, H. Rocha","doi":"10.14227/dt270120p30","DOIUrl":"https://doi.org/10.14227/dt270120p30","url":null,"abstract":"Carvedilol is an antihypertensive agent with blocking non-selective (selectivity for β1 and β2 adrenoceptors is moderate) with vasodilating properties conferred on the α-receptor blockade. The molecular structure has one chiral center, so the drug exists as two enantiomers. Furthermore, it presents different polymorphs depending on the synthetic route that is used to obtain the drug. Carvedilol is a weak base, practically insoluble in water, acidic solutions, and gastric and intestinal fluids, and is classified as Class II (Biopharmaceutical Classification System). It presents different solubilities in accordance with the pH of the solvent. In a previous report, it was demonstrated that batches provided by different manufacturers could have different physicochemical properties. The objective of the present study is to evaluate these properties in the formulation of the final tablets and evaluate the best dissolution method. Different media were used to evaluate the impact of raw material characteristics on in vitro release of drug from tablets containing 12.5 mg carvedilol. Pilot batches were obtained by direct compression and wet granulation. Dissolution profiles were compared with a reference drug. Formulations evaluated by wet granulation using carvedilol with a specific particle size (d10 ~ 10 μm and d90 ~ 95 μm) had similar dissolution profiles to the reference product according to United States Pharmacopeia test 2 and fasted-state simulated intestinal fluid (FaSSIF). The results showed the composition of dissolution medium has a direct impact on the dissolution profile of carvedilol.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"27 1","pages":"30-35"},"PeriodicalIF":0.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66812539","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}

{"title":"Assessment of Physicochemical Properties and Comparison of Dissolution Profiles of Metformin Hydrochloride Tablets in Saudi Arabia","authors":"Mohammed Al Bratty, H. Alhazmi, Shamsher Alam, Intakhab Alam, S. Javed, N. Alam","doi":"10.14227/dt270120p36","DOIUrl":"https://doi.org/10.14227/dt270120p36","url":null,"abstract":"Although prevalence of substandard or counterfeit drugs is a world-wide problem, poor and developing countries are affected the most. To be a quality product, drug formulation must comply with certain standards. Consequently, in this study, metformin hydrochloride (MH) tablets (500 mg) available in the Saudi Arabian market were assessed through various pharmacopeial quality control tests. Parameters including weight variation, hardness, friability, drug content, and disintegration time were evaluated. Results were within acceptable limits for all selected products (nine generic and an innovator). Fourier-transform infrared spectroscopy (FT-IR) spectra of MH for all tested products were completely superimposed with that of the pure drug, confirming the use of correct active ingredient in all tablet formulations. The products were also evaluated by comparing the dissolution profile of the generic products with the innovator brand in pH 6.8 phosphate buffer. The range of percent drug release in 30 min was 82.71–98.43%, in comparison to 91.86% for reference product, which complies with the USP-NF specification of at least 80% drug release in 30 min. The difference factor (f1), similarity factor (f2, except product H), and dissolution efficiency revealed that the dissolution profiles of the tested products were comparable to that of the reference product. These results show that the tested generic products were biopharmaceutically similar (except product H) to the innovator formulation. Therefore, the consumer can select any one of these equivalent products as a substitute for innovator product in case of cost concern or unavailability.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"42 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66812551","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}

{"title":"Questions and Answers","authors":"Margareth R. C. Marques, M. Liddell","doi":"10.14227/dt270120p46","DOIUrl":"https://doi.org/10.14227/dt270120p46","url":null,"abstract":"","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":"66812595","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}

{"title":"Meeting Report: Dissolution Testing, Biowaiver, and Bioequivalence","authors":"V. Gray, D. Diaz, Susan D’Souza","doi":"10.14227/dt270320p40","DOIUrl":"https://doi.org/10.14227/dt270320p40","url":null,"abstract":"","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"39 1","pages":"40-42"},"PeriodicalIF":0.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66813106","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}

{"title":"American Association of Pharmaceutical Scientists (AAPS) and Chinese National Institutes for Food and Drug Control (NIFDC) Joint Workshop on Dissolution, Bioequivalence, Product Performance, and Quality","authors":"Xujin Lu, Baoming Ning, N. Fotaki, Sandra Suarez Sharp, D. Burgess, S. Haddouchi","doi":"10.14227/dt270220p42","DOIUrl":"https://doi.org/10.14227/dt270220p42","url":null,"abstract":"","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"27 1","pages":"42-50"},"PeriodicalIF":0.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66812945","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}

{"title":"Questions and Answers May 2020","authors":"Margareth R. C. Marques, M. Liddell","doi":"10.14227/dt270220p71","DOIUrl":"https://doi.org/10.14227/dt270220p71","url":null,"abstract":"","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"27 1","pages":"71-72"},"PeriodicalIF":0.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66813019","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}

{"title":"In Vitro Release Testing (IVRT) of Topical Hydrocortisone Acetate Creams: A Novel Approach Using Positive and Negative Controls","authors":"Nyengeterai Amanda Mudyahoto, Seeprarani Rath, Ashmita Ramanah, I. Kanfer","doi":"10.14227/dt270120p6","DOIUrl":"https://doi.org/10.14227/dt270120p6","url":null,"abstract":"The objective was to develop and validate an in vitro release testing (IVRT) method to assess the release of hydrocortisone acetate (HCA) from five topical formulations. A marketed generic cream containing 1% HCA was used as the reference product. Vertical diffusion cells (VDCs) were used to assess and compare the release rates of HCA from cream formulations containing 0.5%, 1%, and 1.5% HCA. The study describes a novel approach to test the discriminatory power by including both positive and negative controls to declare pharmaceutical equivalence or inequivalence. The validated method was found to be sensitive, linear, precise, reproducible, robust, and selective for the analysis of HCA from topical cream products. Equivalence or inequivalence was established based on SUPAC-SS acceptance criteria using a 90% CI with limits of 75–133.33%. The IVRT method was shown to have discriminatory ability to appropriately measure significant differences in drug release from various cream formulations. This approach also provides useful information for the future development of acceptable IVRT methods to assess topical dosage forms for local action containing different drugs. INTRODUCTION Since an in vitro release rate can reflect numerous and combined effects of several physical and chemical parameters, including solubility, particle size of the active pharmaceutical ingredient (API) and rheological properties of the dosage form, in vitro release testing (IVRT) has been recommended by the United States Food and Drug Administration (US FDA) as a test to assess pharmaceutical equivalence/inequivalence between preand post-approval product changes (1, 2). The utility of IVRT was extended in 2012 when the US FDA published a draft guidance for assessing bioequivalence (BE) of acyclovir topical ointment, which was the first such publication recommending IVRT for use as a waiver of BE studies for a locally acting topical product (3). This particular guidance provided useful and promising information for the future application of IVRT as a method for assessment of the sameness of topical formulations intended for local action. Subsequently, the US FDA has published several draft guidances using in vitro methods for biowaivers for topical products (3– 8). In addition, a recent draft guideline published by the European Medicines Agency (EMA) also makes provision to use IVRT for the approval of generic products (9). However, a comprehensive validation of the IVRT method is imperative to ensure that the resulting method has the requisite attributes of sensitivity, precision, selectivity, and reproducibility necessary to detect differences relating to qualitative (Q1) and quantitative (Q2) properties and the microstructure and arrangement of matter (Q3) between products (10, 11). In light of the above, an IVRT method was developed and validated to assess creams containing 1% hydrocortisone acetate (HCA). Two marketed products containing 1% HCA and three additional creams ","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"27 1","pages":"6-12"},"PeriodicalIF":0.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66812605","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}

{"title":"In Vitro Therapeutic Equivalence of Two Multisource (Generic) Formulations of Sodium Phenytoin (100 mg) Available in Peru","authors":"Angel T. Alvarado, A. M. Muñoz, Jessica Michiko Miyasato, E. Alvarado, Berta Loja, L. Villanueva, Mario Pineda, M. Bendezu, Juan J. Palomino-Jhong, Jorge A. García","doi":"10.14227/dt270420p33","DOIUrl":"https://doi.org/10.14227/dt270420p33","url":null,"abstract":"( 13 ). An f 2 value of exactly 100 means that the profile of the generic drug is identical to the reference; if the value is 50–99, then the profiles are similar ( 10, 12, ABSTRACT This in vitro study evaluated the therapeutic equivalence of two multisource (generic) formulations of 100-mg phenytoin as immediate-release tablets available in the Peruvian pharmaceutical market, compared with the reference medicine, to establish interchangeability. The mean weight, hardness, and content of active substance were evaluated, prior to analyzing the dissolution profile. USP dissolution apparatus 2 (paddle) was used at 75 rpm with 900 mL of dissolution medium at 37 ± 0.5 °C at pH levels of 1.2, 4.5, and 6.8. The generic and reference formulations had similar weight or drug content, but hardness values were significantly different ( p = 0.029). At pH 1.2, the generic products were considered therapeutically equivalent to the reference product based on similarity factor ( f 2 ) and dissolution efficiency values; however, at pH 4.5 and 6.8, there were differences in dissolution performance based on f 2 values below the acceptable range.","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":"66812745","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}

{"title":"Investigation of Dissolution Performance of Hard Gelatin Capsule Products Using Various Sinkers","authors":"Yaser Mansuroglu, J. Dressman","doi":"10.14227/dt270320p21","DOIUrl":"https://doi.org/10.14227/dt270320p21","url":null,"abstract":"Dissolution testing is a commonly used tool for the quality control of various dosage forms. For this purpose, consistent test conditions are necessary to obtain reproducible test results. Typical issues that can affect the dissolution performance of tested capsule formulations are floating and coning. Recently, the International Conference on Harmonisation (ICH) guideline recommended the use of sinkers to prevent coning, although no accompanying data to support the recommendation has been published in the open literature to date. Therefore, we initiated studies designed to address the following key questions. A) Do all sinkers prevent flotation of the dosage form? B) Does using sinkers consistently increase the dissolution rate? C) Do sinkers consistently decrease coning? Three commercially available hard capsule drug products were studied: acetaminophen, fluconazole, and ketoprofen. Dissolution was performed without a sinker and with four commercially available sinkers (CLIPS, CAPLOTH, CAPWAST, and JP). Analysis of the results revealed that, although three of the four sinkers were able to adequately address flotation problems, in many cases their use led to artifactual increases or decreases in the dissolution of the capsules. Further, sinkers do not seem to be generally useful for addressing coning issues. Instead, an increase in the stirring speed or use of peak vessels should be considered.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":"21-32"},"PeriodicalIF":0.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66813084","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}

{"title":"Comment on the Importance of Documenting Drug Solubility Measurement Methodology, Including Characterizing the Physical Form of the Solute, for Meaningful Understanding, Interpretation, and Reporting of Solubility Data","authors":"W. Brown, V. Gray, J. Krämer, J. Mauger, K. Warner","doi":"10.14227/dt260419p6","DOIUrl":"https://doi.org/10.14227/dt260419p6","url":null,"abstract":"T his commentary continues the discussion initiated in a previous article entitled “Comment on the Importance of Data Transparency, Openness, and Reproducibility in Dissolution Science and Technology” (1). As a follow-up, this commentary more specifically provides a scan of current practices in the literature that are applicable to solubility data reported in Dissolution Technologies, with the goal of enhancing reproducibility and meaningful interpretations of these data.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":" ","pages":""},"PeriodicalIF":0.6,"publicationDate":"2019-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45439362","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}