FORMULATION DEVELOPMENT OF EFAVIRENZ TABLET AND EVALUATION OF ITS COMPARATIVE DISSOLUTION TEST AND BIOEQUIVALENCE STUDY

• Main Author: Diar Febryanto, Hery
• Format: Theses
• Language: Indonesia
• Online Access: https://digilib.itb.ac.id/gdl/view/70779
• Institution: Institut Teknologi Bandung

Efavirenz is an antiretroviral drug that used as first line theraphy for HIV because of its long-term safety benefits. The aim of this study was to develop an efavirenz tablet formulation and conduct an evaluation of the comparative dissolution test and bioequivalence test between efavirenz and Stocrin tablets. There are 3 factors that can affect to dissolution of efavirenz: crospovidone as a disintegrant, sodium lauryl sulfate as a solubility enhancer, and hydroxy propyl cellulose as a binder. Optimization has been done to improve flow properties, compressibility, disintegration time, and dissolution. Tests using XRD and SEM were carried out to see polymorphism and crystal form of efavirenz as well as the possibility changes in efavirenz during the granulation and tableting processes. The quality of tablets was evaluated. The efavirenz tablets was controlled with a weight of 500±25 mg and a hardness of 74,5±4,82 N. The result showed that the tablets had a friability of 0.11%, disintegration time of 6,13±1,06 minutes, assay of 97,44±0,83%, and the amount of efavirenz that dissolved after 30 minutes was 86,10±0,84%. The F2 values in the dissolution test compared between efavirenz and Stocrin at pH 1.2; 4.5; and 6.8 were 43.12; 42.52; and 71.25, respectively. The results of XRD test showed that efavirens used was form 1 and had a peak at 2? 8? which was different from efavirens used in Stocrin tablets. SEM test results showed that there were differences in particle shape between efavirenz powder, powder form of efavirenz tablets and powder form of Stocrin tablets. Bioequivalence testing of Cmax value between test drug and reference drug was bio-inequivalent with 90% confidence interval ratio 74,55-89,26%; while AUC0-72 between test drug and reference drug was bioequivalent with 90% confidence interval ratio 84,37-92,19%.