Design and optimization of mefloquine hydrochloride microparticles for bitter taste masking.

AAPS PharmSciTech
Punit P ShahArti Thakkar

Abstract

The objective of the present investigation was to reduce the bitterness with improved dissolution, in acidic medium (pH 1.2), of mefloquine hydrochloride (MFL). Microparticles were prepared by coacervation method using Eudragit E (EE) as polymer and sodium hydroxide as precipitant. A 3(2) full factorial design was used for optimization wherein the drug concentration (A) and polymer concentration (B) were selected as independent variables and the bitterness score, particle size and dissolution at various pH were selected as the dependent variables. The desirability function approach has been employed in order to find the best compromise between the different experimental responses. The model is further cross validated for bias. The optimized microparticles were characterized by FT-IR, DSC, XRPD and SEM. Bitterness score was evaluated by human gustatory sensation test. Multiple linear regression analysis revealed that the reduced bitterness of MFL can be obtained by controlling the dissolution of microparticles at pH 6.8 and increasing the EE concentration. The increase in polymer concentration leads to reduction in dissolution of microparticles at pH > 5 due to its insolubility. However the dissolution studies at pH 1.2 demonstr...Continue Reading

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Citations

Aug 7, 2013·International Journal of Pharmaceutics·Chintan VoraRajashree Mashru
Dec 25, 2010·AAPS PharmSciTech·Dionysios Dennis DouroumisSilke Schminke
Nov 11, 2011·International Journal of Nanomedicine·Jingling TangLinhua Wu
Dec 24, 2008·Acta Pharmaceutica : a Quarterly Journal of Croatian Pharmaceutical Society and Slovenian Pharmaceutical Society, Dealing with All Branches of Pharmacy and Allied Sciences·Punit P ShahAtul C Badhan
Jun 15, 2013·Drug Development and Industrial Pharmacy·Mohammed ManiruzzamanDennis Douroumis
May 3, 2014·Drug Development and Industrial Pharmacy·Zhenzhong GeChunsheng Gao
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Jun 7, 2013·The Journal of Pharmacy and Pharmacology·Tamami HaraguchiTakahiro Uchida
Nov 5, 2013·The Journal of Pharmacy and Pharmacology·Mohammed ManiruzzamanDennis Douroumis
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