Dissolution Technologies最新文献

{"title":"Comparison of Release Rates Derived from Cutaneous Versus Film-Forming Solution Containing Terbinafine: Approach Towards Qualification and Validation of In Vitro Parameters","authors":"Y. Upadhyay, Ashutosh Kumar Singh, Sanjeev Mishra, S. Gurule, A. Khuroo, Soumya Verma, Neeta Tiwari, S. Bedi","doi":"10.14227/dt290122p28","DOIUrl":"https://doi.org/10.14227/dt290122p28","url":null,"abstract":"Excipients play a very important role in the release pattern of an active pharmaceutical ingredient from topical semisolid dosages forms, and their physical and chemical properties can influence the release. The aim of this paper was to provide a validated, sensitive, and reproducible method to assess the in vitro release rate of an antifungal drug (Terbinafine) from controlled drug delivery systems (cutaneous and film-forming solution) and to prove product sameness. The samples obtained from in vitro testing were analyzed through a high performance liquid chromatographic (HPLC) system coupled with UV spectrometer at a wavelength of 283 nm. A Franz diffusion cell (FDC) system was used for the dissolution test. We recorded the drug release from the formulation for 6 hours. The release rate obtained from cutaneous and filmforming solutions were compared statistically to depict the sameness. The results met the relevant acceptance criteria (i.e., 90% confidence interval, falling within the limits of 75–133%) as defined in the scale-up and post-approval changes (SUPAC-SS) guidance. The obtained results confirm the competence of the IVRT method for the assessment of product sameness.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66813144","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":"Testing the In-Vitro Product Performance of Nanomaterial-Based Drug Products: View of the USP Expert Panel","authors":"M. Wacker, Xujin Lu, Matt Burke, lshai Nir, R. Fahmy","doi":"10.14227/dt290122p6","DOIUrl":"https://doi.org/10.14227/dt290122p6","url":null,"abstract":"Today, a wide variety of nanomaterial-based drug products enter the US market, creating the need for reliable standards and technologies to measure their performance in-vitro. A growing number of new performance assays are evaluated for testing the drug release from nanomaterials. On the one hand, they include real time separation methods such as dialysis, fiber optical systems, and flow-separation techniques. On the other hand, sample-and-separate methods such as centrifugation, filtration, and solid-phase extraction are commonly used. In our evaluation of the existing practices, we provide guidance in method development and validation of release assays. Also, we discuss requirements for standardization and documentation of release data. Furthermore, we highlight the knowledge gaps and challenges associated with drug release testing of nanomaterial-based drug products. dx.doi.org/10.14227/DT290122P6 Reprinted with permission. © 2021 The United States Pharmacopeial Convention. All rights reserved. Correspondence should be addressed to: Kahkashan Zaidi, Senior Principal Scientist, United States Pharmacopeia, 12601 Twinbrook Parkway, Rockville, MD 20852-1790; email: kxz@usp.org. INTRODUCTION Over the years, a wide variety of nanomaterialbased drug products have entered the global healthcare market (1, 2). A recent USP chapter, Drug Products Containing Nanomaterials <1153>, provides clarification on terminology including liposomes, nanoparticles, nanocrystals, micelles, nanobubbles, nanofibers, nanotubes, nanoemulsions, and dendrimers. These novel dosage forms are characterized by exceptionally small dimensions and specific properties that make them more difficult to evaluate using conventional methodologies. In the following article, recent trends and developments in the area of in-vitro performance testing of nanomaterialbased drug products will be discussed. For some of these dosage forms such as semisolids or inhalation products, the sample collection plays an important role. These issues will be discussed in more detail by other Stimuli articles and are beyond the scope of the present work. CURRENT USP FRAMEWORK Currently, <1153> summarizes dosage forms that exhibit specific features related to the use of nanotechnology and provides the terminology to be used in the context of the USP framework. To a certain extent, the versatility of drug delivery concepts is reflected by the performance parameters that have been discussed for 7 FEBRUARY 2022 www.dissolutiontech.com nanomaterials. These performance parameters include the drug release, the physical stability or \"dispersibility\" of colloids, the ability of the carrier to protect the drug from degradation, as well as the release of compounds into specific compartments known to influence the biodistribution, such as the plasma proteins (3) or lipids (4). This versatility is reflected in different sections of the USP as well. For example, Gene Therapy Products <1047> recognizes the use of liposomes","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66813205","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":"Study of Drug Release Kinetics of Rosuvastatin Calcium Immediate-Release Tablets Marketed in Saudi Arabia","authors":"W. Ahsan, Md. Shamsher Alam, S. Javed, H. Alhazmi, M. Albratty, A. Najmi, M. Sultan","doi":"10.14227/dt290222pgc1","DOIUrl":"https://doi.org/10.14227/dt290222pgc1","url":null,"abstract":"Rosuvastatin (RST), a BCS class II drug, is a poorly water-soluble antihyperlipidemic agent. The aim of the present work was to determine and compare the drug release kinetics from the RST calcium innovator (Crestor) and generic products (Ivarin and Resova) marketed in Saudi Arabia by employing various drug release kinetic mathematical models. A dissolution study was performed on all RST calcium immediate-release tablets. The in vitro drug release profiles were determined in three different dissolution media: 0.1 N HCl (pH 1.2), 0.05 M phosphate buffer (pH 6.8), and 0.05 M citrate buffer (pH 6.6). Drug release data were obtained, correlated quantitatively, and interpreted with the help of mathematical models, then the drug release kinetics were analyzed. The criterion for selecting the most suitable model was based on the highest coefficient of correlation ( R 2 ) with the dissolution profile in each respective media. The innovator product followed the Hixson-Crowell model ( R 2 = 0.955) only in 0.1 N HCl (pH 1.2), whereas in other media all the formulations followed first order release kinetics with non-swellable matrix Fickian diffusion, which is considered ideal for an immediate-release tablet formulation.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66813351","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":"Formulation and Evaluation of Bisoprolol Hemifumarate Emulgel for Transdermal Drug Delivery","authors":"R. Gul, Y. Khan, Tajala Aman","doi":"10.14227/dt290522p38","DOIUrl":"https://doi.org/10.14227/dt290522p38","url":null,"abstract":"The aim of this study was to formulate and evaluate bisoprolol hemifumarate emulgel using carbopol 934P with the enhancers, thymus oil and olive oil. Thymus oil and olive oil were used as permeation enhancers. The emulsion formulations were added to a base gel. The emulgel was characterized for physical characteristics, stability, skin irritation, and drug release. Formulations F1 and F5 indicated the best in-vitro drug release when compared with other preparations. Bisoprolol hemifumarate emulgel containing carbopol 934P and thymus oil or olive oil enhancers could be further developed for a topical drug delivery system.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"05 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66813919","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":"Update on Gastrointestinal Biorelevant Media and Physiologically Relevant Dissolution Conditions","authors":"Daniela Amaral Silva, N. Davies, N. Bou-Chacra, H. Ferraz, R. Löbenberg","doi":"10.14227/dt290222p62","DOIUrl":"https://doi.org/10.14227/dt290222p62","url":null,"abstract":"Dissolution testing constitutes one of the most widely used in vitro performance tests during drug development and routine quality control testing. It monitors the rate and extent of in vitro drug release (batch release test), and it is often used to ensure consistent in vivo performance. The purpose of this review is to summarize and update the many physiologically adapted media and buffers proposed over the years, focusing on the upper gastrointestinal tract because this is where most drug absorption occurs. Emphasis will be given on the application of bicarbonate-based media because this is the major buffering species in the human intestinal lumen. Due to the pragmatical difficulties of using bicarbonate-based dissolution media, surrogate media with simpler buffer systems are desirable. Herein we describe some of the proposed models and different approaches to develop such substitutes. Special consideration has to be taken when dealing with enteric coated (delayed release) formulations because the interaction of coating polymer with bicarbonate is very complex. All factors considered, using physiologically relevant conditions can ameliorate the risks and enable drug development with increased likelihood to select formulations with the desired in vivo performance.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66813252","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":"A Novel Application of an Effervescent Agent in Naproxen Liqui-Pellets for Enhanced Drug Release","authors":"Matthew Lam, A. Nokhodchi","doi":"10.14227/dt290222p94","DOIUrl":"https://doi.org/10.14227/dt290222p94","url":null,"abstract":"Liqui-Pellet formulations have been introduced as a technology to improve the dissolution rate of poorly water-soluble drugs. This study aimed to incorporate sodium bicarbonate (NaHCO 3 ) into the Liqui-Pellet formulation to explore the potential impact on the drug release rate. Naproxen Liqui-Pellet formulations containing 5%, 12%, 22%, 32%, and 42% w/w of NaHCO 3 were successfully produced and their physicochemical properties were investigated and compared with a physical mixture pellet formulation. Incorporation of such a large amount of functional excipient is impossible or near impossible in the classical liquisolid formulation due to weight and size limitations, particularly for high-dose drugs. The results showed that NaHCO 3 is an effective functional excipient to enhance the drug dissolution rate. The Liqui-Pellet formulation with 42% w/w NaHCO 3 released 76.4% of drug after 2 hours at pH 1.2, which was 14 times faster than the physical mixture pellet (5.5% drug release in 2 h). In general, a faster dissolution rate was observed with increasing NaHCO 3 concentration; however, there was a limit to this effect. Above a certain limit, the influence of NaHCO 3 on the dissolution rate lessened. The flowability test showed that all formulations have good to excellent flowability. Overall, this study demonstrates the flexibility of Liqui-Pellets in terms of formulation design, which in turn further supports the potential of Liqui-Pellets as the next generation oral dosage form.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66813340","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":"Dissolution Method Troubleshooting: An Industry Perspective","authors":"J. Mann, Andre Hermans, Nathan D. Contrella, B. Nickerson, Carrie A. Coutant, Christian Jede, S. Kao, D. Kou, Emmanuel Scheubel, Fredrik Winge, Johanna Milsmann, M. Mueller-Zsigmondy, N. Zaborenko","doi":"10.14227/dt290422p190","DOIUrl":"https://doi.org/10.14227/dt290422p190","url":null,"abstract":"Quality control dissolution testing represents a key product performance test for solid oral dosage forms and is the most likely QC test to result in laboratory investigations because of the relatively complex relationship between the dissolution performance, the drug product properties, and the systems necessary to measure the quality attribute. The Dissolution Working Group of the International Consortium for Innovation and Quality in Pharmaceutical Development (IQ) has pooled our collective knowledge to outline some common ways that dissolution methods can fail. Examples and case studies are given to highlight errors related to equipment, method, materials, measurement, people, and the environment. Best practices for building method understanding and avoiding the exemplified issues are discussed. Case studies highlight the importance of buffer preparation, potential impact of contamination of the dissolution medium, additive-induced degradation, risks in the use of automation, differences between dissolution systems, and the effect of filter selection. Investing in analyst training programs, understanding the capabilities of your equipment portfolio, and using well-designed studies for robustness and ruggedness will reduce dissolution method investigations and improve compliance and productivity during the method lifecycle.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66813605","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 February 2022","authors":"Margareth R. C. Marques, M. Liddell","doi":"10.14227/dt290122p46","DOIUrl":"https://doi.org/10.14227/dt290122p46","url":null,"abstract":"","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66813160","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":"Dissolution Profile of Apixaban Tablets: Method Development and Validation Using HPLC Analysis","authors":"Natália Olegário dos Santos, Nathalie R. Wingert, M. Steppe","doi":"10.14227/dt290122p22","DOIUrl":"https://doi.org/10.14227/dt290122p22","url":null,"abstract":"Apixaban is an anticoagulant agent that inhibits factor Xa, commercially available as coated tablets at the dosages of 2.5 and 5.0 mg. There is no official monograph of the formulation in the current international pharmacopoeias. From research and development to finished product quality control, the dissolution test is an important tool to evaluate the quality of pharmaceutical formulations. This study aimed to develop and validate an in vitro method to assess the dissolution profile of apixaban immediate-release (5 mg) coated tablets. Several conditions were tested in this study until the most suitable one was reached. The selected method included the following parameters: 0.01 M hydrochloric acid (pH 2.3, 500 mL), USP paddle apparatus, 75 rpm, 37 °C, with seven sampling points and a total test time of 90 minutes. Quantitative analysis was performed by high performance liquid chromatography using a previously validated method. The dissolution method was validated following the official guidelines, demonstrating specificity, linearity, precision, accuracy, and robustness. This study enabled the development of an adequate, effective, and reliable method, which contributes to the evaluation of apixaban release in new products and the quality control of formulations containing this drug.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66813590","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 November 2022","authors":"Margareth R. C. Marques, M. Liddell","doi":"10.14227/dt290422p238","DOIUrl":"https://doi.org/10.14227/dt290422p238","url":null,"abstract":"","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66813787","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}