ENHANCEMENT OF DISSOLUTION RATE OF EFAVIRENZ BY SOLID DISPERSION IN STARCH 1500 AND SOLUPLUS ALONE AND IN COMBINATION
| Main Author: | M.Priyadarsini, K. P. R. Chowdary* , and S.V.U.M.Prasad |
|---|---|
| Format: | Article Journal |
| Bahasa: | eng |
| Terbitan: |
, 2018
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| Subjects: | |
| Online Access: |
https://zenodo.org/record/1283400 |
Daftar Isi:
- Efavirenz, a widely prescribed antiretroviral drug belongs to class II under BCS and exhibit low and variable oral bioavailability due to its poor aqueous solubility. As such it needs enhancement in the dissolution rate and bioavailability to derive its maximum therapeutic efficacy. The objective of the present study is to prepare and evaluate solid dispersions of Efavirenz in Starch 1500 and Soluplus alone and in combination for enhancing the dissolution rate and dissolution efficiency of Efavirenz. The individual and combined effects of the two carriers, Starch 1500 and Soluplus in enhancing the dissolution rate and dissolution efficiency of Efavirenz were evaluated in a 22 factorial study. Solid dispersions of Efavirenz in Starch 1500 alone were prepared using four ratios of drug: carrier namely 2:1, 1:1, 1:2 and 1:3 by solvent evaporation method. Solid dispersions of Efavirenz in Soluplus alone were prepared at three concentrations namely 0.5, 1.0 and 2% by common solvent method. Solid dispersions of Efavirenz in combined carriers namely Starch 1500 and Soluplus were prepared as per 22 factorial design. All the solid dispersions prepared were evaluated for drug content uniformity, dissolution rate and dissolution efficiency in comparison to Efavirenz pure drug. The dissolution rate and dissolution efficiency of Efavirenz could be significantly enhanced by solid dispersion in Starch 1500 and Soluplus alone and in combination. The individual and combined effects of Starch 1500 and Soluplus in enhancing the dissolution rate and dissolution efficiency of Efavirenz are highly significant (P < 0.01). Soluplus gave significant enhancement in the dissolution rate of Efavirenz at very low concentrations where as a large proportion of Starch 1500 is required for a similar enhancement in the dissolution rate of Efavirenz. Combination of Starch 1500 and Soluplus resulted in a much higher enhancement in the dissolution rate and dissolution efficiency of Efavirenz than is possible with them individually. Combination of Starch 1500 and Soluplus is recommended for enhancing the dissolution rate and dissolution efficiency of Efavirenz. Key words: Efavirenz, Solid dispersion, Dissolution Rate, Starch 1500, Soluplus, Factorial study