Modelos in vitro para determinação da absorção de fármacos e previsão da relação dissolução/absorção

Souza, Jacqueline de; Freitas, Zaida Maria Faria de; Storpirtis, Sílvia

doi:10.1590/s1516-93322007000400004

Cited by 32 publications

(29 citation statements)

References 68 publications

(28 reference statements)

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…The standardization of intrinsic dissolution test should be made carefully because this method is influenced by internal and external factors (properties of solid state, surface area, hydrodynamic condition, composition of dissolution media, vibration, rotation speed, presence of dissolved gases in dissolution media, sample sites) (Issa, Ferraz, 2011;Souza, Freitas, Storpirtis, 2007). Thus, all these conditions were controlled and standardized to minimize any interference.…”

Section: Intrinsic Dissolution Methodsmentioning

confidence: 99%

Equilibrium solubility versus intrinsic dissolution: characterization of lamivudine, stavudine and zidovudine for BCS classification

Dezani

Pereira

Caffaro

et al. 2013

Braz. J. Pharm. Sci.

View full text Add to dashboard Cite

Solubility and dissolution rate of drugs are of major importance in pre-formulation studies of pharmaceutical dosage forms. The solubility improvement allows the drugs to be potential biowaiver candidates and may be a good way to develop more dose-efficient formulations. Solubility behaviour of lamivudine, stavudine and zidovudine in individual solvents (under pH range of 1.2 to 7.5) was studied by equilibrium solubility and intrinsic dissolution methods. In solubility study by equilibrium method (shake-flask technique), known amounts of drug were added in each media until to reach saturation and the mixture was subjected to agitation of 150 rpm for 72 hours at 37 °C. In intrinsic dissolution test, known amount of each drug was compressed in the matrix of Wood's apparatus and subjected to dissolution in each media with agitation of 50 rpm at 37 °C. In solubility by equilibrium method, lamivudine and zidovudine can be considered as highly soluble drugs. Although stavudine present high solubility in pH 4.5, 6.8, 7.5 and water, the solubility determination in pH 1.2 was not possible due stability problems. Regarding to intrinsic dissolution, lamivudine and stavudine present high speed of dissolution. Considering a boundary value presented by Yu and colleagues (2004), all drugs studied present high solubility characteristics in intrinsic dissolution method. Based on the obtained results, intrinsic dissolution seems to be superior for solubility studies as an alternative method for biopharmaceutical classification purposes.Uniterms: Drugs/solubility. Drugs/dissolution rate. Intrinsic dissolution/method/biopharmaceutical classification. Biopharmaceutical Classification System.A solubilidade e a taxa de dissolução de fármacos são de grande importância em estudos de pré-formulação de formas farmacêuticas. A melhora na solubilidade permite que os fármacos sejam candidatos potenciais à bioisenção, podendo ser uma boa maneira para desenvolver formulações dose-eficientes. O comportamento de solubilidade da lamivudina, estavudina e zidovudina em solventes individuais (sob faixa de pH 1,2 a 7,5) foi estudado pelos métodos de solubilidade em equilíbrio e dissolução intrínseca. No estudo de solubilidade pelo método do equilíbrio (método de agitação de frascos), conhecidas quantidades do fármaco foram adicionadas em cada meio até atingirem a saturação e a mistura foi submetida à agitação de 150 rpm por 72 horas a 37 °C. No ensaio de dissolução intrínseca, conhecida quantidade de cada fármaco foi comprimida na matriz do aparato de Wood e submetida à dissolução em cada meio com agitação de 50 rpm a 37 °C. No método de solubilidade em equilíbrio, a lamivudina e a zidovudina podem ser consideradas como fármacos altamente solúveis. Embora a estavudina apresente alta solubilidade nos meios pH 4,5, 6,8, 7,5 e água, a determinação da solubilidade em pH 1,2 não foi possível devido a problemas de estabilidade. Com relação à dissolução intrínseca, a lamivudina e a estavudina apresentaram alta velocidade de dissolução. Considerando o valor ...

show abstract

Section: Intrinsic Dissolution Methodsmentioning

confidence: 99%

Equilibrium solubility versus intrinsic dissolution: characterization of lamivudine, stavudine and zidovudine for BCS classification

Dezani

Pereira

Caffaro

et al. 2013

Braz. J. Pharm. Sci.

View full text Add to dashboard Cite

show abstract

“…Although for the registration of new drugs is necessary to define the absolute bioavailability, this is not usually easily accessible. As regards the other applicable models difficulties of standardization of methodologies, reproducibility of results and inconsistency with in vivo data are observed (Souza, Freitas, Storpirtis, 2007).…”

Section: Discussionmentioning

confidence: 99%

“…The need to obtain data relating to intestinal permeability of drugs has raised the development of various models for the determination of permeability, which may be in vivo, in situ, in vitro and in silico (Souza, Freitas, Storpirtis, 2007). The methods continue to be improved and it is recommended that conclusions should be obtained by using more than one method (Balimane et al, 2000).…”

Section: Permeabilitymentioning

confidence: 99%

Biopharmaceutics classification system: importance and inclusion in biowaiver guidance

Arrunátegui

Silva-Barcellos

Bellavinha

et al. 2015

Braz. J. Pharm. Sci.

Self Cite

View full text Add to dashboard Cite

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.

show abstract

“…Dissolution studies represent an indispensable tool for pharmaceutical development, since they make it possible to check whether the formulation is suitable for the purpose for which it is intended (Sittichai et al, 2007). In the sector of pharmaceutical production and quality control, the dissolution test can be used to detect quality deviations in parameters such as content uniformityand ensure reproducibility between production batches (Marques, 2002;Souza et al, 2007).…”

Section: Introductionmentioning

confidence: 99%

Dissolution test of herbal medicines containing Passiflora sp.

Costa¹,

Alves²,

Conceição³

et al. 2011

Rev. bras. farmacogn.

View full text Add to dashboard Cite

Abstract:The dissolution test is an essential tool to assess the quality of herbal medicines in the solid dosage form for oral use. This work aimed to evaluate the dissolution behavior of three herbal medicines in the form of capsules and tablet containing Passiflora, produced with powder or dried extract. Assay of total flavonoids and dissolution methods were validated and obtained results allowed the quantification of flavonoids with precision, accuracy and selectivity. The percentage of total flavonoids found was 2% for capsule A (containing only powder), 0.97% for capsule B (containing only dried extract) and 5.5% for tablet. Although the content was lower, the release of flavonoids present in the capsule containing dried extract was 12% higher over 30 min, with dissolved percentage values of 87 and 75, for the capsules containing extract and powder, respectively. The tablet containing dried extract presented dissolution of 76%, despite the higher content of flavonoids, which may be due to pharmacotechnical problems. Obtained data demonstrated the need to implement these tests in the quality control of herbal medicines, confirming the release of the active ingredients that underlie the pharmacological action of these medicines.

show abstract

Modelos in vitro para determinação da absorção de fármacos e previsão da relação dissolução/absorção

Abstract: Fármacos contidos em formas farmacêuticas sólidas devem ter

Cited by 32 publications

References 68 publications

Equilibrium solubility versus intrinsic dissolution: characterization of lamivudine, stavudine and zidovudine for BCS classification

Equilibrium solubility versus intrinsic dissolution: characterization of lamivudine, stavudine and zidovudine for BCS classification

Biopharmaceutics classification system: importance and inclusion in biowaiver guidance

Dissolution test of herbal medicines containing Passiflora sp.

Contact Info

Product

Resources

About