Biopharmaceutics classification system: importance and inclusion in biowaiver guidance

Abstract

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.

Pharmaceutical development of tablets containing a spray-dried optimized extract from Lippia origanoides H. B. K.: influence of excipients and toxicological assessment

“…After dissolution, the drug is released from this pharmaceutical form, and becomes available to be absorbed. Many factors can interfere in the process of tablet dissolution, such as the particle size, solubility, and chemical nature of the drug, as well as the composition in excipients of the formulation (Arrunátegui et al, 2015;Cristofoletti, Dressman, 2017). The FDA (Food and Drug Administration, USA) states that these formulations must release 85% of the active substance between the initial 15 and 60 minutes of the test, according to the biopharmaceutical characteristics of the drug (FDA-CDER, 1997).…”

Impact of Tablet Shape on Drug Dissolution Rate Through Immediate Released Tablets

“…Domperidone, a drug model for immediate release dosage form was selected according to its biopharmaceutical classification system that classified to class II, suggesting that the release of these type of drugs from dosage forms is easily controlled by formulation composition. 15 Therefore, we can easily study and evaluate dissolution manner related to various tablet shapes. The objective of the present study was to investigate the impact of different tablet shapes on dissolution rate.…”

Method Optimization for Determination of Drug Solubility Limit

“…Drugs can be classified into BCS Class I (highly soluble and permeable), Class II (highly permeable but poorly soluble), Class III (highly soluble but poorly permeable), and Class IV (poorly soluble and poorly permeable) according to Biopharmaceutics classification system [1]. Classes II and IV are poorly water-soluble and normally characterized as high molecular weights, large log P values, and poor water solubility, generally have problems with drug bioavailability.…”