Investigation on the Possibility of Biowaivers for Ibuprofen

Álvarez, C.; Núñez, Ignacio Medina; Torrado, J. J.; Gordon, John; Potthast, Henrike; García‐Arieta, Alfredo

doi:10.1002/jps.22472

Cited by 56 publications

(52 citation statements)

References 19 publications

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“…Those drugs can quickly dissolve at intestinal pH in the gastrointestinal (GI) tract and exhibit good oral absorption like BCS class I drugs even though they are almost insoluble at gastric pH (Davies, 1998;Davies and Anderson, 1997;Potthast et al, 2005). However, the risk of approving a biowaiver for BCS class IIa drugs has been reported (Alvarez et al, 2011). This study raised questions regarding the dissolution system used to predict in vivo performance and the likely discrepancy between in vitro and in vivo dissolution.…”

Section: Introductionmentioning

confidence: 90%

In vitro dissolution methodology, mini-Gastrointestinal Simulator (mGIS), predicts better in vivo dissolution of a weak base drug, dasatinib

Tsume

Takeuchi

Matsui

et al. 2015

European Journal of Pharmaceutical Sciences

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Section: Introductionmentioning

confidence: 90%

In vitro dissolution methodology, mini-Gastrointestinal Simulator (mGIS), predicts better in vivo dissolution of a weak base drug, dasatinib

Tsume

Takeuchi

Matsui

et al. 2015

European Journal of Pharmaceutical Sciences

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“…Therefore, formulation strategies for compounds of this class target a solubility improvement in an effort to optimize their biopharmaceutical profiles [1,16,17]. Consequently, we selected the BCS 2 APIs Diclofenac, Ibuprofen, Ketoprofen, Naproxen, Sulfadiazine, Sulfamethoxazole and Tolbutamide for this study [18][19][20][21][22]. Frequently, solubility improvement of ionizable APIs is subject to salt screening, with sodium being the most commonly used counterion for acidic APIs [1] and therefore, sodium salts were used as a control group.…”

Section: Discussionmentioning

confidence: 99%

Transformation of acidic poorly water soluble drugs into ionic liquids

Balk

Wiest

Widmer

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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“…For this class the limiting step of absorption is dissolution in vivo, thus the dissolution profile should be clearly defined and reproducible, emphasizing the importance of using methods that reflect or control the dissolution process in vivo (WHO, 2006;Alvarez et al, 2011). Cristofoletti and colleagues (2013) calculated the diagnostic indicators utilizing 22 results of in vitro dissolution profiles performed at neutral conditions (phosphate buffer under pH 6.8-7.5) for a set of eight non-BE (all of them because of Cmax) and 14 BE drug products containing five weak acidic drugs, with pKa of less than 5.5 and which have dose numbers lower than one at pH values ranging from 6.8 to 7.4.…”

Section: Discussionmentioning

confidence: 99%

Biopharmaceutics classification system: importance and inclusion in biowaiver guidance

Arrunátegui

Silva-Barcellos

Bellavinha

et al. 2015

Braz. J. Pharm. Sci.

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Pharmacological therapy is essential in many diseases treatment and it is important that the medicine policy is intended to offering safe and effective treatment with affordable price to the population. One way to achieve this is through biowaiver, defined as the replacement of in vivo bioequivalence studies by in vitro studies. For biowaiver of new immediate release solid oral dosage forms, data such as intestinal permeability and solubility of the drug are required, as well as the product dissolution. The Biopharmaceutics Classification System (BCS) is a scientific scheme that divides drugs according to their solubility and permeability and has been used by various guides as a criterion for biowaiver. This paper evaluates biowaiver application, addressing the general concepts and parameters used by BCS, making a historical account of its use, the requirements pertaining to the current legislation, the benefits and risks associated with this decision. The results revealed that the use of BCS as a biowaiver criterion greatly expands the therapeutics options, contributing to greater therapy access of the general population with drug efficacy and safety guaranteed associated to low cost.Uniterms: Medicines/biowaiver. Biopharmaceutics Classification System. Drugs/solubility. Drugs/ permeability. Drugs/dissolution. Drugs/legislation.O tratamento farmacológico é essencial frente a várias patologias e é fundamental que a política de medicamentos tenha por objetivo oferecer à população tratamento seguro, eficaz e de preço acessível. Uma forma de alcançar esse objetivo é por meio da bioisenção, definida como a substituição de estudos de bioequivalência in vivo por estudos in vitro. Para bioisentar novos medicamentos sob a forma farmacêutica sólida oral de liberação imediata são utilizados dados de permeabilidade intestinal e solubilidade do fármaco, bem como sua dissolução a partir da forma farmacêutica. O Sistema de Classificação Biofarmacêutica (SCG) é um esquema científico que divide os fármacos em classes de acordo com solubilidade e permeabilidade e vem sendo utilizado como critério para bioisenção em diversas legislações. O presente artigo faz uma avaliação desta utilização, abordando os conceitos gerais e parâmetros utilizados pelo SCB, fazendo um relato histórico da aplicação da bioisenção, das exigências pertinentes às legislações vigentes, dos benefícios e riscos inerentes a uma tomada de decisão sobre bioisenção baseada neste critério. Os resultados revelaram que a utilização do SCB como critério amplia enormemente as possibilidades de bioisenção, contribuindo para o maior acesso da população em geral a medicamentos com garantida eficácia, segurança e menor custo.Unitermos: Medicamentos/bioisenção. Sistema de Classificação Biofarmacêutica. Fármaco/solubilidade. Fármaco/permeabilidade. Fármaco/dissolução. Fármaco/legislação.

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Investigation on the Possibility of Biowaivers for Ibuprofen

Cited by 56 publications

References 19 publications

In vitro dissolution methodology, mini-Gastrointestinal Simulator (mGIS), predicts better in vivo dissolution of a weak base drug, dasatinib

In vitro dissolution methodology, mini-Gastrointestinal Simulator (mGIS), predicts better in vivo dissolution of a weak base drug, dasatinib

Transformation of acidic poorly water soluble drugs into ionic liquids

Biopharmaceutics classification system: importance and inclusion in biowaiver guidance

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