Taste masking of Promethazine Hydrochloride using Eudragit E100via solid dispersion technique to develop fast disintegrating tablets

[摘要] The purpose of present study was to mask the intensely bitter taste of promethazine HCl and toformulate fast disintegrating tablets (FDTs) of the taste masked drug. The taste masking wasdone via solid dispersion (SD) technique using Eudragit E100 (amino-alkyl methacrylatecopolymer) in different ratios. The drug-polymer compatibility and their compatibility withprocess condition were evaluated on the basis of FTIR spectroscopy and there was no sign ofany interaction between drug and polymer and within the prepared system. The SD preparedwith different ratio of drug and polymer was evaluated for drug release in phosphate buffer (pH6.2), and for in vivo taste. The SD with drug polymer ratio of 1:4 did not give any taste andshows minimum release in phosphate buffer (pH 6.2); therefore that ratio was selected as bestcandidate for development of FDTs. The nine batches were prepared using crospovidone andcroscarmellose to find out effect of both the polymers on in vitro and in vivo disintegration time.The prepared batches were also evaluated for different parameters such as hardness, friability,wetting time, in vitro dispersion time, and for in vivo taste. Crospovidone 20% w/w gave theminimum disintegration time. The tablets of the final formulation containing 38.16 % mannitoland 9.14 % of microcrystalline cellulose showed the minimum disintegration time of 23 sec. Thetaste evaluation of the tablets in comparison to quinine sulfate in human volunteers revealed aconsiderable taste masking. Thus results conclusively demonstrated successful masking of tasteand fast disintegration of the developed formulation in the oral cavity.

[学科分类] 药理学