Development and validation of dissolution method for carvedilol compression-coated tablets

Abstract

The present study describes the development and validation of a dissolution method for carvedilol compression-coated tablets. Dissolution test was performed using a TDT-06T dissolution apparatus. Based on the physiological conditions of the body, 0.1N hydrochloric acid was used as dissolution medium and release was monitored for 2 hours to verify the immediate release pattern of the drug in acidic pH, followed by pH 6.8 in citric-phosphate buffer for 22 hours, to simulate a sustained release pattern in the intestine. Influences of rotation speed and surfactant concentration in medium were evaluated. Samples were analysed by validated UV visible spectrophotometric method at 286 nm. 1% sodium lauryl sulphate (SLS) was found to be optimum for improving carvedilol solubility in pH 6.8 citric-phosphate buffer. Analysis of variance showed no significant difference between the results obtained at 50 and 100 rpm. The discriminating dissolution method was successfully developed for carvedilol compression-coated tablets. The conditions that allowed dissolution determination were USP type I apparatus at 100 rpm, containing 1000 ml of 0.1N HCl for 2 hours, followed by pH 6.8 citric-phosphate buffer with 1% SLS for 22 hours at 37.0 ± 0.5 ºC. Samples were analysed by UV spectrophotometric method and validated as per ICH guidelines.Uniterms: Carvedilol/coated tablets. Compression coated tablets/dissolution. pH 6.8 citric-phosphate buffer. Hydrochloric acid. Sodium lauryl sulphate.O presente estudo descreve o desenvolvimento e a validação de método de dissolução para comprimidos revestidos de carvedilol. O teste de dissolução foi efetuado utilizando-se o aparelho para dissolução TDT-06T. Com base nas condições fisiológicas do organismo, utilizou-se ácido clorídrico 0,1 N como meio de dissolução e a liberação foi monitorada por 2 horas para se verificar o padrão de liberação imediata do fármaco em condições de pH baixo, seguidas por pH 6,8 em tampão cítrico-fosfato por 22 horas, para simular o padrão de liberação controlada no intestino. Avaliou-se a influência da velocidade de rotação e a concentração de tensoativo no meio. As amostras foram analisadas por método espectrofotométrico UV-visível validado, em 286 nm. O laurilsulfato sódico a 1% (SLS) mostrou-se ótimo para aumentar a solubilidade do carvedilol em pH 6,8 em tampão cítrico-fosfato. A análise da variância não mostrou diferença significativa entre os resultados obtidos a 50 e a 100 rpm. O método da dissolução discriminante foi desenvolvido com sucesso para os comprimidos revestidos de carvedilol. As condições que permitiram a determinação da dissolução foram: aparelho USP tipo I a 100 rpm, contendo 1000 mL de HCL 0,1 N por 2 horas, seguido de pH 6,8 com tampão cítrico-fosfato, com 1% de SLS por 22 horas a 37,0 ± 0,5 o C. Amostras foram analisadas por método espectrofotométrico e validadas pelas normas ICH.Unitermos: Carvedilol/comprimidos revestidos. Comprimidos revestidos por compressão/dissolução. Tampão cítrico-fosfato pH 6.8. Ácido clorídrico. Laurilsulfato de sódio.

Fabrication and in vitro evaluation of novel pH‐sensitive poly (2‐methoxyethyl methacrylate‐co‐itaconic acid) microgels

“…In the thermograms of the formulation F2, no such peak was found, suggesting molecular dispersion of EMT throughout the p(MEMA‐co‐IA) network. Our results are according to the literature reported earlier …”

Development and Validation of <i>In Vitro</i> Discriminatory Dissolution Testing Method for Fast Dispersible Tablets of BCS Class II Drug

“…The maximum solubility shown by domperidone was observed in 0.1 N HCl and it increased as the pH decreases. 16,17 The solubility of domperidone in water is very low and is enhanced by the addition of surfactant (SLS). SLS caused an increase in the solubility with concentration 0.5% and a further increase in concentration had no significant effect on solubility as shown in Table 2.…”

In Vitro Cefixime Dissolution in Pharmacopeia-Recommended Medium and Simulated Gastrointestinal Fluids: A Comparative Study

“…Although it was reported that a dilute hydrochloric acid-based solution at pH 1-2 can simulate gastric fluid, and phosphate-buffered solution at pH 6.8 can mimic intestinal fluid, dissolution media that are more closely representing physiological conditions may provide more accurate results [11]. There are many types of simulated gastrointestinal fluids which have been reported for in vitro drug dissolution of many drugs [12][13][14][15].…”