In Vivo Bioequivalence and In Vitro Similarity Factor (f2) for Dissolution Profile Comparisons of Extended Release Formulations: How and When Do They Match?

Duan, John; Riviere, Kareen; Marroum, Patrick

doi:10.1007/s11095-011-0377-x

Cited by 51 publications

(19 citation statements)

References 13 publications

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“…As faixas de teor das cápsulas de cada produto, e o resultado da avaliação individual dos mesmos quanto à uniformidade de conteúdo podem ser observados na Tabela 1. O perfil de dissolução representa uma técnica relativamente rápida e barata para avaliar formas farmacêuticas sólidas antes do teste clínico 17 , entretanto, é fundamental para uma melhor avaliação das formulações a aplicação de modelos de comparação específicos, como os fatores de semelhança (f1) e diferença (f2) propostos por Moore & Flanner 15 . A Tabela 2 mostra o f1 e f2 das formulações estudadas em relação ao medicamento de referência.…”

Section: Resultsunclassified

Avaliação Da Qualidade De Cápsulas De Omeprazol Produzidas Em Farmácias Magistrais

et al. 2016

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Objetivo: Avaliar a qualidade de seis formulações de cápsulas contendo Omeprazol. Metodologia: Foram realizadas análises de peso médio, uniformidade de conteúdo, teor de princípio ativo e cinética de dissolução. As formulações A, B, C e D, corresponderam às cápsulas de farmácias magistrais, E e F corresponderam ao medicamento de referência e ao produto similar, respectivamente. Resultados: Todas as amostras foram aprovadas na análise de peso médio. As formulações C e D foram reprovadas nos ensaios de teor e uniformidade de conteúdo, a formulação F foi reprovada quanto à uniformidade de princípio ativo. Quanto à cinética de dissolução, o medicamento de referência e a formulação B condizem com as especificações. O perfil de dissolução do Peprazol ® , comparado às formulações magistrais e ao similar é bastante diferenciado. Conclusões: Os resultados mostram que a maioria dos medicamentos manipulados e os produtos similares são inadequados quanto a qualidade de suas formulações. Descritores ABSTRACTObjective: It was intended to evaluate the quality of six formulations containing omeprazole. Methods: Analysis of average weight, uniformity of content, content of active ingredient and dissolution kinetics were performed. Formulations A, B, C and D correspond to capsules obtained from compounding pharmacies, E and F correspond to the reference product and the similar product. Results: All samples were adopted in the analysis of average weight. Formulations C and D were to fail the test and content uniformity of content, F was rejected for uniformity of active ingredient. With regard to the kinetics of dissolution, the reference product and formulation B are consistent. The dissolution profile of the Peprazol ® compared to similar formulations, and compounding is very different. Conclusions: The results show that most of the manipulated medicines and similar products are inadequate as the quality of his formulations.

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Section: Resultsunclassified

Avaliação Da Qualidade De Cápsulas De Omeprazol Produzidas Em Farmácias Magistrais

et al. 2016

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“…The f 2 value fitted the result between 0 and 100. The two dissolution profiles were believed to be similar when the f 2 value was larger than 50, with the mean deviation over all time points being less than 10% [31][32][33]. The calculated value was 77.8 indicating that the releases were synchronous.…”

Section: Resultsmentioning

confidence: 99%

Theranostic Nanoemulsions: Codelivery of Hydrophobic Drug and Hydrophilic Imaging Probe for Cancer Therapy and Imaging

Yang

Wang

et al. 2014

Nanomedicine (Lond.)

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“…A recent study by Duan et al (30) analyzed the correspondence between the f 2 and in vivo results obtained by simulations, and concluded that although the results were consistent in most cases, care should be taken when the completeness of the dissolution profiles differ more than 10% or when the shapes of the dissolution profiles are significantly different.…”

Section: Resultsmentioning

confidence: 99%

Biopharmaceutical Relevance of Dissolution Profile Comparison: Proposal of a Combined Approach

Ruiz¹,

Volonté²

2014

Dissolution Technol.

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The aims of the present study were to evaluate the performance of the main methods proposed for the comparison of percentage dissolved versus time curves and to recommend a more biorelevant combined approach for the comparison of dissolution profiles of multisource drug products. In vitro dissolution tests of four brands of oxcarbazepine (OxCBZ) tablets were performed, and the resulting profiles were compared by model-independent, model-dependent, and ANOVA-based statistical methods. After a careful analysis of the results, some methods were chosen and applied to the comparison of dissolution profiles of four brands of carbamazepine (CBZ) tablets and two brands of phenytoin (PHT) capsules. Finally, these in vitro results were qualitatively correlated with the corresponding in vivo results previously obtained with the same CBZ and PHT products assayed in healthy volunteers. The analysis of the dissolution data obtained with OxCBZ tablets allowed discarding the ANOVA-based statistical methods since in all cases they were over-discriminating from a biopharmaceutical point of view. The remaining comparison methods were applied to in vitro profiles of CBZ and PHT products and the results correlated with in vivo data. The most suitable methods for the biopharmaceutical comparison of in vitro dissolution profiles were the model-independent ones, and among them, the best correlations were the f 2 similarity factor along with a measure of the dissolution extent (e.g., area under the curve). This combined approach gives a robust and informative result with the most biopharmaceutical relevance.

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In Vivo Bioequivalence and In Vitro Similarity Factor (f2) for Dissolution Profile Comparisons of Extended Release Formulations: How and When Do They Match?

Abstract: When f2 is used for in vitro dissolution profile comparison, the completeness of the dissolution profiles should not differ more than 10%, and the shapes of the dissolution profiles should not be significantly different.

Cited by 51 publications

References 13 publications

Avaliação Da Qualidade De Cápsulas De Omeprazol Produzidas Em Farmácias Magistrais

Avaliação Da Qualidade De Cápsulas De Omeprazol Produzidas Em Farmácias Magistrais

Theranostic Nanoemulsions: Codelivery of Hydrophobic Drug and Hydrophilic Imaging Probe for Cancer Therapy and Imaging

Biopharmaceutical Relevance of Dissolution Profile Comparison: Proposal of a Combined Approach

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