Conceptuation, formulation and evaluation of sustained release floating tablets of captopril compression coated with gastric dispersible hydrochlorothiazide using 23factorial design

Autor: Puttagunta Srinivasa Babu, Govada Kishore Babu, Pathuri Lakshmi Sirisha
Rok vydání: 2014
Předmět:
Zdroj: International Journal of Pharmaceutical Investigation
ISSN: 2230-973X
Popis: Ambulatory blood pressure monitoring is regarded as the gold standard for hypertensive therapy in non-dipping hypertension patients. A novel compression coated formulation of captopril and hydrochlorothiazide (HCTZ) was developed in order to improve the efficacy of antihypertensive therapy considering the half-life of both drugs. The synergistic action using combination therapy can be effectively achieved by sustained release captopril (t 1/2 = 2.5 h) and fast releasing HCTZ (average t 1/2 = 9.5 h). The sustained release floating tablets of captopril were prepared by using 2 3 factorial design by employing three polymers i.e., ethyl cellulose (EC), carbopol and xanthan gum at two levels. The formulations (CF 1 -CF 8 ) were optimized using analysis of variance for two response variables, buoyancy and T 50% . Among the three polymers employed, the coefficients and P values for the response variable buoyancy and T 50% using EC were found to be 3.824, 0.028 and 0.0196, 0.046 respectively. From the coefficients and P values for the two response variables, formulation CF 2 was optimized, which contains EC polymer alone at a high level. The CF 2 formulation was further compression coated with optimized gastric dispersible HCTZ layer (HF 9 ). The compression coated tablet was further evaluated using drug release kinetics. The Q value of HCTZ layer is achieved within 20 min following first order release whereas the Q value of captopril was obtained at 6.5 h following Higuchi model, from which it is proved that rapid release HCTZ and slow release of captopril is achieved. The mechanism of drug release was analyzed using Peppas equation, which showed an n >0.90 confirming case II transportation mechanism for drug release.
Databáze: OpenAIRE