DoE-Based Solid Self-microemulsifying Drug Delivery System (S-SMEDDS) Approach for Improving the Dissolution Properties of Raltegravir Potassium.

Autor: Jain, Sourabhkumar, Dudhat, Kiran, Soniwala, M. M., Kotadiya, Nirav, Mori, Dhavalkumar
Zdroj: Journal of Pharmaceutical Innovation; Mar2023, Vol. 18 Issue 1, p29-42, 14p
Abstrakt: Objective: Raltegravir potassium (RP) exhibits very low water solubility over the range of physiological pH (1.2, 4.5, and 6.8), which leads to poor dissolution properties and ultimately high intra- and inter-patient variabilities. The present research work aimed to prepare RP-loaded solid self-microemulsifying drug delivery system (S-SMEDDS) of RP to improve its dissolution characteristics. Methods: Based on results of drug solubilization capacity and emulsification efficiency, labrasol, Tween-20, and PEG-400 were selected as oil, emulsifier, and co-emulsifier, respectively. A ternary phase diagram was generated to identify the proportion of compositions that, upon mixing, formed a clear and transparent microemulsion. In the present investigation, simplex lattice design was used to explore the effect of variations in the composition of excipients on significant formulation characteristics. Result: The regression analysis suggested a significant effect of the change in the proportion of composition on selected response variables. Optimized SMEDDS formulation was mixed with selected carriers in a mortar to prepare S-SMEDDS. The results of DSC and powder X-ray diffraction studies indicated the complete transformation of the crystalline drug into the amorphous or molecular level dispersed form when neusiline US2 was used as a carrier. Conclusion: The results of in vitro dissolution studies proved significant improvement in the dissolution properties from the S-SMEDDS formulation compared to the pure drug (f2 < 50). [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index