The dissolution rate of a drug directly affects its absorption and utilization in vivo. The dissolution test is used to evaluate the quality of formulation and production process. Entecavir is approved by the United States FDA for the treatment of chronic hepatitis B. Entecavir monohydrate (ETV-H) is used in commercial ETV tablets. The anhydrous form of entecavir (ETV-A) often appears as an impurity polymorph during the preparation process. This study aims to investigate the dissolution behavior of ETV-H in four dissolution media (water, pH 1.2, pH 4.0, and pH 6.8) and compare with those of ETV-A. The dissolution rates of ETV-H at pH 6.8, pH 4.0, and ultrapure water were faster than those of ETV-A, resulting in faster complete dissolution of ETV-H. To save time in the dissolution testing, an analytical method based on the Noyes Whitney equation is proposed to obtain the fitted (predicted) dissolution curve. Differences (loss values) between the predicted and experimental dissolution curves for ETV-H at pH 6.8 and pH 1.2 were 0.0013 and 0.016, respectively. The proposed analytical method can save up to 75% of experimental time and can be used for dissolution testing of active pharmaceutical ingredients in the production of pharmaceutical crystals.
{"title":"Predicting Dissolution of Entecavir Using the Noyes Whitney Equation","authors":"Yanlei Kang, Jiahui Chen, Zhenyu Duan, Zhong Li","doi":"10.14227/dt300123p38","DOIUrl":"https://doi.org/10.14227/dt300123p38","url":null,"abstract":"The dissolution rate of a drug directly affects its absorption and utilization in vivo. The dissolution test is used to evaluate the quality of formulation and production process. Entecavir is approved by the United States FDA for the treatment of chronic hepatitis B. Entecavir monohydrate (ETV-H) is used in commercial ETV tablets. The anhydrous form of entecavir (ETV-A) often appears as an impurity polymorph during the preparation process. This study aims to investigate the dissolution behavior of ETV-H in four dissolution media (water, pH 1.2, pH 4.0, and pH 6.8) and compare with those of ETV-A. The dissolution rates of ETV-H at pH 6.8, pH 4.0, and ultrapure water were faster than those of ETV-A, resulting in faster complete dissolution of ETV-H. To save time in the dissolution testing, an analytical method based on the Noyes Whitney equation is proposed to obtain the fitted (predicted) dissolution curve. Differences (loss values) between the predicted and experimental dissolution curves for ETV-H at pH 6.8 and pH 1.2 were 0.0013 and 0.016, respectively. The proposed analytical method can save up to 75% of experimental time and can be used for dissolution testing of active pharmaceutical ingredients in the production of pharmaceutical crystals.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66814573","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}
B. Yaméogo, Wendpouiré Zoungrana-Somé, B. C. Sombié, Hermine Zimé-Diawara, Bertrand W. F. Goumbri, Aïssata Sanfo-Diasso, E. Kabré, R. Semdé
Amoxicillin is a penicillin antibiotic widely prescribed to treat many infections. Several brands of oral forms of amoxicillin are available on the local market. The aim of this study was to evaluate the physicochemical quality and in vitro bioequivalence of several brands of amoxicillin capsules (500 mg) marketed in Burkina Faso. Nine different brands of amoxicillin capsules (eight generic and the innovator brand) were purchased from local authorized distributors. Quality control tests (identification, uniformity of weight, disintegration, assay, and dissolution) were performed according to the United States Pharmacopoeia monograph. The comparison of in vitro dissolution profiles was performed in three different pH media (1.2, 4.5, 6.8) using statistical calculations of difference ( f 1 ) and similarity ( f 2 ) factors. All brands met USP specifications for physicochemical quality. Amoxicillin content was 104.60–116.04% of the label claim. Mean disintegration time was 6.12–13.44 minutes and dissolution exceeded 80% within 60 minutes. When comparing dissolution profiles, f 1 values > 15 and f 2 values < 50 were obtained for two brands at all three pH levels; these brands cannot be considered interchangeable with the innovator brand. Six out of eight tested generic brands can be considered interchangeable with the innovator product.
{"title":"Physicochemical Quality and In Vitro Bioequivalence of Amoxicillin Capsules Marketed in Burkina Faso, Africa","authors":"B. Yaméogo, Wendpouiré Zoungrana-Somé, B. C. Sombié, Hermine Zimé-Diawara, Bertrand W. F. Goumbri, Aïssata Sanfo-Diasso, E. Kabré, R. Semdé","doi":"10.14227/dt300123pgc1","DOIUrl":"https://doi.org/10.14227/dt300123pgc1","url":null,"abstract":"Amoxicillin is a penicillin antibiotic widely prescribed to treat many infections. Several brands of oral forms of amoxicillin are available on the local market. The aim of this study was to evaluate the physicochemical quality and in vitro bioequivalence of several brands of amoxicillin capsules (500 mg) marketed in Burkina Faso. Nine different brands of amoxicillin capsules (eight generic and the innovator brand) were purchased from local authorized distributors. Quality control tests (identification, uniformity of weight, disintegration, assay, and dissolution) were performed according to the United States Pharmacopoeia monograph. The comparison of in vitro dissolution profiles was performed in three different pH media (1.2, 4.5, 6.8) using statistical calculations of difference ( f 1 ) and similarity ( f 2 ) factors. All brands met USP specifications for physicochemical quality. Amoxicillin content was 104.60–116.04% of the label claim. Mean disintegration time was 6.12–13.44 minutes and dissolution exceeded 80% within 60 minutes. When comparing dissolution profiles, f 1 values > 15 and f 2 values < 50 were obtained for two brands at all three pH levels; these brands cannot be considered interchangeable with the innovator brand. Six out of eight tested generic brands can be considered interchangeable with the innovator product.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66814108","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}
R. P. da Silva, Michele George Issa, V. Bezzon, A. G. Rodrigues, H. Ferraz
{"title":"Dissolution Profile of Calcium Supplements in Brazil: A Critical Analysis and Formulation Proposal","authors":"R. P. da Silva, Michele George Issa, V. Bezzon, A. G. Rodrigues, H. Ferraz","doi":"10.14227/dt300323p154","DOIUrl":"https://doi.org/10.14227/dt300323p154","url":null,"abstract":"","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66814404","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}
J. Panić, N. Todorović, Kristina Jonas, Ana Stjepanović, Gordana Švonja-Parezanović, Milana Vuković, M. Lalic-Popovic
Generic formulations share the same active pharmaceutical ingredient (API), but differences in excipients can impact the quality and efficacy of formulations. In this study, four gastro-resistant pantoprazole tablet formulations were selected from the Serbian drug market to compare their dissolution profiles. The influence of high and low humidity on disintegration and dissolution was examined. The tablets were removed from the primary packaging and packed in plastic boxes, which were then placed in the desiccator with low (30%) and high (75%) humidity conditions for 1 week to simulate storing medicines in weekly pill organizers. Dissolution, disintegration, and uniformity of content were analyzed according to the 10 th European Pharmacopoeia . Pantoprazole content was determined using UV-Vis spectrophotometry. Dissolution profiles were compared with one-way analysis of variance and similarity factor analysis ( f 2 ). Although a difference was detected in the dissolution profiles of pantoprazole tablets, the overall dissolution rate was satisfactory for all formulations in all conditions tested. After being exposed to high humidity, two formulations failed to meet the requirements for disintegration due to the enteric coating being damaged during the acid stage of the test. This could lead to the absence of therapeutic effect. Therefore, patients should be advised to keep their pantoprazole tablets away from high humidity, preferably in the original packaging.
{"title":"Influence of Storage Conditions on the Pantoprazole Dissolution Profile for Gastro-Resistant Tablet Formulations","authors":"J. Panić, N. Todorović, Kristina Jonas, Ana Stjepanović, Gordana Švonja-Parezanović, Milana Vuković, M. Lalic-Popovic","doi":"10.14227/dt300223pgc1","DOIUrl":"https://doi.org/10.14227/dt300223pgc1","url":null,"abstract":"Generic formulations share the same active pharmaceutical ingredient (API), but differences in excipients can impact the quality and efficacy of formulations. In this study, four gastro-resistant pantoprazole tablet formulations were selected from the Serbian drug market to compare their dissolution profiles. The influence of high and low humidity on disintegration and dissolution was examined. The tablets were removed from the primary packaging and packed in plastic boxes, which were then placed in the desiccator with low (30%) and high (75%) humidity conditions for 1 week to simulate storing medicines in weekly pill organizers. Dissolution, disintegration, and uniformity of content were analyzed according to the 10 th European Pharmacopoeia . Pantoprazole content was determined using UV-Vis spectrophotometry. Dissolution profiles were compared with one-way analysis of variance and similarity factor analysis ( f 2 ). Although a difference was detected in the dissolution profiles of pantoprazole tablets, the overall dissolution rate was satisfactory for all formulations in all conditions tested. After being exposed to high humidity, two formulations failed to meet the requirements for disintegration due to the enteric coating being damaged during the acid stage of the test. This could lead to the absence of therapeutic effect. Therefore, patients should be advised to keep their pantoprazole tablets away from high humidity, preferably in the original packaging.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66814321","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}
Marilyn Martinez, D. Longstaff, V. Fellner, M. Coffey
{"title":"Factors Influencing the Selection of Medium for Evaluating Drug Solubility and Dissolution in Bovine Milk","authors":"Marilyn Martinez, D. Longstaff, V. Fellner, M. Coffey","doi":"10.14227/dt300323p134","DOIUrl":"https://doi.org/10.14227/dt300323p134","url":null,"abstract":"","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66814376","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}
R. Berthelsen, S. Larsen, A. Müllertz, K. Box, Jesper Østergaard
The objective of this study was to investigate the implications of changing dissolution parameters, including pH ramp time, absence and presence of simulated intestinal fluid (SIF)
本研究的目的是探讨改变溶解参数的影响，包括pH斜坡时间、模拟肠液(SIF)的缺失和存在。
{"title":"Biorelevant Dissolution of Dipyridamole and Piroxicam Using an Automated UV/Vis Spectrophotometric and Potentiometric Dissolution Testing Platform","authors":"R. Berthelsen, S. Larsen, A. Müllertz, K. Box, Jesper Østergaard","doi":"10.14227/dt300323p144","DOIUrl":"https://doi.org/10.14227/dt300323p144","url":null,"abstract":"The objective of this study was to investigate the implications of changing dissolution parameters, including pH ramp time, absence and presence of simulated intestinal fluid (SIF)","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66814391","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 August 2023","authors":"Margareth R. C. Marques, M. Liddell","doi":"10.14227/dt300323p176","DOIUrl":"https://doi.org/10.14227/dt300323p176","url":null,"abstract":"","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66814526","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}
Ebtesam W. Elsayed, Ahmed A. El-Ashmawy, N. Mursi, L. Emara
Gliclazide (GLZ) is an ampholyte with pH-dependent solubility in the gastrointestinal pH range. Although the effects of different pH values on GLZ release have been thoroughly investigated in compendial dissolution media, the effects of gastrointestinal fluid components and pH are not well known. Multiple response optimization was carried out employing two optimization criteria to obtain different release profiles (optimized alginate-gelatin beads, OP-1 and OP-2). Thermograms indicated polymorph formation (OP-1) and changes in GLZ crystallinity (OP-2). Fourier transform infrared (FT-IR)-spectra confirmed GLZ chemical stability. GLZ release in gradient compendial and biorelevant media was studied employing two dissolution methodologies using fed state simulated gastric and intestinal fluid (FeSSGF and FeSSIF, respectively). A validated HPLC/UV method for GLZ analysis in biorelevant media was developed. OP-1 and OP-2 showed low relative error between the actual and predicted values. In the gradient biorelevant media, OP-1 showed faster GLZ release than OP-2. In the gradient compendial media, OP-1 showed slower GLZ release in pH 1.2 and faster release in pH 7.4 than OP-2. Generally, both formulations showed slower GLZ release in biorelevant compared to compendial media. SEM images of OP-1 showed tiny pores on the bead surface after GLZ release in biorelevant media. Meanwhile, thin polymer layers were diffused around the beads (OP-1 and OP-2) after GLZ release in compendial media. In conclusion, GLZ release was mainly affected by pH rather than media components. A cost-effective biorelevant dissolution methodology was proposed.
{"title":"Biorelevant Dissolution Testing of Numerically Optimized Multiparticulate Drug Delivery Systems of Gliclazide","authors":"Ebtesam W. Elsayed, Ahmed A. El-Ashmawy, N. Mursi, L. Emara","doi":"10.14227/dt300223p88","DOIUrl":"https://doi.org/10.14227/dt300223p88","url":null,"abstract":"Gliclazide (GLZ) is an ampholyte with pH-dependent solubility in the gastrointestinal pH range. Although the effects of different pH values on GLZ release have been thoroughly investigated in compendial dissolution media, the effects of gastrointestinal fluid components and pH are not well known. Multiple response optimization was carried out employing two optimization criteria to obtain different release profiles (optimized alginate-gelatin beads, OP-1 and OP-2). Thermograms indicated polymorph formation (OP-1) and changes in GLZ crystallinity (OP-2). Fourier transform infrared (FT-IR)-spectra confirmed GLZ chemical stability. GLZ release in gradient compendial and biorelevant media was studied employing two dissolution methodologies using fed state simulated gastric and intestinal fluid (FeSSGF and FeSSIF, respectively). A validated HPLC/UV method for GLZ analysis in biorelevant media was developed. OP-1 and OP-2 showed low relative error between the actual and predicted values. In the gradient biorelevant media, OP-1 showed faster GLZ release than OP-2. In the gradient compendial media, OP-1 showed slower GLZ release in pH 1.2 and faster release in pH 7.4 than OP-2. Generally, both formulations showed slower GLZ release in biorelevant compared to compendial media. SEM images of OP-1 showed tiny pores on the bead surface after GLZ release in biorelevant media. Meanwhile, thin polymer layers were diffused around the beads (OP-1 and OP-2) after GLZ release in compendial media. In conclusion, GLZ release was mainly affected by pH rather than media components. A cost-effective biorelevant dissolution methodology was proposed.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66814268","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 2023","authors":"Margareth R. C. Marques, M. Liddell","doi":"10.14227/dt300123p247","DOIUrl":"https://doi.org/10.14227/dt300123p247","url":null,"abstract":"","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"1 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66813997","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}
Hassan M. Alsulais, Ali K. Alqaisum, Ahmed A. Aldoulah, Ashfaq A Mohsin, Hassan M. Ghonaim
Introduction : Ciprofloxacin is a fluoroquinolone class of antibiotics with broad-spectrum antibacterial activity. Biowaiver studies of generic ciprofloxacin products can be used to establish bioequivalence with the reference product. Methods : The experiments are carried out using the reference product, Ciprobay (Bayer, Germany), and three generic products, Cipromax (Spimaco Addwaeih, Saudi Arabia), Ciproxen (Jamjoom Pharma, Saudi Arabia), and Quinox (Tabuk Pharmaceuticals, Saudi Arabia). In vitro tests were done according to the United States Pharmacopeia (USP) standards to evaluate the physicochemical characteristics including weight variation, hardness, thickness, disintegration, and dissolution. Results : All four products tested met the standard limits for physical and physicochemical parameters. In addition, the dissolution test indicated that the three generics are equivalent to the reference product in terms of quality, and all products released more than 80% of drug within 30 minutes. Conclusion: The four tested brands of ciprofloxacin can be used interchangeably.
{"title":"Comparative Study of Brand and Generics Ciprofloxacin Tablets Available in the Saudi Market","authors":"Hassan M. Alsulais, Ali K. Alqaisum, Ahmed A. Aldoulah, Ashfaq A Mohsin, Hassan M. Ghonaim","doi":"10.14227/dt300223pgc12","DOIUrl":"https://doi.org/10.14227/dt300223pgc12","url":null,"abstract":"Introduction : Ciprofloxacin is a fluoroquinolone class of antibiotics with broad-spectrum antibacterial activity. Biowaiver studies of generic ciprofloxacin products can be used to establish bioequivalence with the reference product. Methods : The experiments are carried out using the reference product, Ciprobay (Bayer, Germany), and three generic products, Cipromax (Spimaco Addwaeih, Saudi Arabia), Ciproxen (Jamjoom Pharma, Saudi Arabia), and Quinox (Tabuk Pharmaceuticals, Saudi Arabia). In vitro tests were done according to the United States Pharmacopeia (USP) standards to evaluate the physicochemical characteristics including weight variation, hardness, thickness, disintegration, and dissolution. Results : All four products tested met the standard limits for physical and physicochemical parameters. In addition, the dissolution test indicated that the three generics are equivalent to the reference product in terms of quality, and all products released more than 80% of drug within 30 minutes. Conclusion: The four tested brands of ciprofloxacin can be used interchangeably.","PeriodicalId":11380,"journal":{"name":"Dissolution Technologies","volume":"59 1","pages":""},"PeriodicalIF":0.6,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66814333","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}
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