Liquisolid Technique Based Sustained Release Tablet of Trimetazidine Dihydrochloride

Abstract

Aim

It is suggested here that liquisolid technique has the potential to be optimized for the reduction of drug dissolution rate and thereby production of sustained release tablets matrices of Trimetazidine Di hydrochloride (TZH a water soluble drug).

Method

TZH was dispersed in polsorbate-80 a non-volatile liquid vehicle. Then a binary mixture of carrier–coating materials (Ethyl cellulose (F1, F2 and F3), Eudragit L-100 (E1, E2 and E3) and RS-100 (S1, S2 and S3) as the carrier and aerosil as the coating material) was added to the liquid medication under continuous stirring. Precompression studies, such as flow properties were also carried out. The formed mixture was compressed to get tablets matrices by using the tableting machine. The prepared liquisolid matrix tablets were evaluated by hardness, friability, and in vitro dissolution studies. The dissolution profile of the prepared SR matrix tablets were compared with a marketed formulation (MR). TZH tablets prepared by liquisolid technique showed greater retardation, when compared with marketed matrix tablets.

Conclusion

This investigation provided evidence that Polysorbate-80 (Tween 80) has important role in sustaining the release of drug from liquisolid matrices. The dissolution profile followed the Higuchi and Peppas model, shows near zero order release for prolonged period. The FT-IR spectra revealed that there is no interaction between drug-excipients used; there is no significant difference in the mean percentage of drug released from formulation E3 after storing for 6 months at 40 ± 2 °C/75 ± 25% RH, after 12 h. The amount of TZH released from marketed formulation (MR) and Liquisolid matrices (E3), showed a significant difference statistically (ANOVA P < 0.05).