Avaliação biofarmacêutica in vitro de cápsulas de fluconazol

Porta, Valentina; Yamamichi, Érika; Storpirtis, Sílvia

doi:10.1590/s1516-93322002000300009

Cited by 7 publications

(9 citation statements)

References 17 publications

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“…Taking into consideration the dissolution results reported in the literature, and its high solubility (Tables and ), it seems safe to expect fluconazole tablets, capsules and powder for oral suspension to dissolve rapidly (≥85% in 30 min) at pH values within the physiological pH range. Moreover, comparative in vitro dissolution testing in different pH 1.2, 4.5, 6.8 media (500 mL for 50 and 100 mg and 900 mL for other strengths), as recommended by the various BCS guidance documents using the basket apparatus at 100 rpm can provide reasonable assurance for BE of the product.…”

Section: Discussionmentioning

confidence: 99%

“…Porta et al 110,111 reported more than 85% drug release from reference capsules (Zoltec 150 mg; Pfizer, Sao Paulo, Brazil) within 20 min in basket apparatus containing 900 mL 0.1 N HCl dissolution medium stirred at 100 rpm. The test product was found to release more than 85% drug in the above mentioned medium within 10 min 110,111 and was determined to be bioequivalent to the reference capsules. 84 Corrêa et al 99 proposed a basket assembly with 900 mL of 0.1 M HCl stirred at 75 rpm for 30 min for dissolution testing of fluconazole capsules.…”

Section: Surrogate Techniques For In Vivo Be Testingmentioning

confidence: 99%

See 1 more Smart Citation

Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Fluconazole

Charoo¹,

Cristofoletti²,

Graham³

et al. 2014

Journal of Pharmaceutical Sciences

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Section: Discussionmentioning

confidence: 99%

Section: Surrogate Techniques For In Vivo Be Testingmentioning

confidence: 99%

Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Fluconazole

Charoo¹,

Cristofoletti²,

Graham³

et al. 2014

Journal of Pharmaceutical Sciences

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“…A velocidade de dissolução influencia diretamente o início, a intensidade e a duração da resposta terapêutica, além de controlar a biodisponibilidade geral do medicamento a partir de sua forma farmacêutica 24 . No entanto, conclusões definitivas sobre biodisponibilidade e bioequivalência somente são possíveis após a realização de estudos in vivo 25 . O perfil de dissolução do medicamento de referência e da formulação B mostraram-se adequados as especificações preconizadas, estando de acordo com as exigências farmacopeicas [13][14] .…”

Section: Discussionunclassified

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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“…In the GastroPlus ™ fluconazole database, records were created for two batches of three different products, namely A1, A2, B1, B2, C1, and C2, as previously described by [29]; A1 and A2 were batches #1 and #2, respectively, of the reference product Zoltec ® 150 mg capsules, whereas B1, B2, C1, and C2 were batches #1 and #2 of two different products found in the Brazilian market. The dissolution tests were performed using the United States Pharmacopeia (USP) apparatus 1 (basket) with 900 mL of 0.1 M HCl at 37 ± 0.5 °C and 100 rpm for 30 min and yielded results ( n = 6 for each product) [29] that were used in the software to simulate the plasma concentration for each product (A1, A2, B1, B2, C1, and C2).…”

Section: Methodsmentioning

confidence: 99%

In Silico Prediction of Plasma Concentrations of Fluconazole Capsules with Different Dissolution Profiles and Bioequivalence Study Using Population Simulation

et al. 2019

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A biowaiver is accepted by the Brazilian Health Surveillance Agency (ANVISA) for immediate-release solid oral products containing Biopharmaceutics Classification System (BCS) class I drugs showing rapid drug dissolution. This study aimed to simulate plasma concentrations of fluconazole capsules with different dissolution profiles and run population simulation to evaluate their bioequivalence. The dissolution profiles of two batches of the reference product Zoltec® 150 mg capsules, A1 and A2, and two batches of other products (B1 and B2; C1 and C2), as well as plasma concentration–time data of the reference product from the literature, were used for the simulations. Although products C1 and C2 had drug dissolutions < 85% in 30 min at 0.1 M HCl, simulation results demonstrated that these products would show the same in vivo performance as products A1, A2, B1, and B2. Population simulation results of the ln-transformed 90% confidence interval for the ratio of Cmax and AUC0–t values for all products were within the 80–125% interval, showing to be bioequivalent. Thus, even though the in vitro dissolution behavior of products C1 and C2 was not equivalent to a rapid dissolution profile, the computer simulations proved to be an important tool to show the possibility of bioequivalence for these products.

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Avaliação biofarmacêutica in vitro de cápsulas de fluconazol

Cited by 7 publications

References 17 publications

Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Fluconazole

Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Fluconazole

Avaliação Da Qualidade De Cápsulas De Omeprazol Produzidas Em Farmácias Magistrais

In Silico Prediction of Plasma Concentrations of Fluconazole Capsules with Different Dissolution Profiles and Bioequivalence Study Using Population Simulation

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