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

[1]  C. Leopold,et al.  Drug release from liquisolid systems: speed it up, slow it down , 2011, Expert opinion on drug delivery.

[2]  B. El-Houssieny,et al.  Bioavailability and biological activity of liquisolid compact formula of repaglinide and its effect on glucose tolerance in rabbits. , 2010, Bioscience trends.

[3]  A H Hosmani,et al.  Evaluation of in vitro dissolution profile comparison methods of sustained release tramadol hydrochloride liquisolid compact formulations with marketed sustained release tablets. , 2010, Drug discoveries & therapeutics.

[4]  B. Matthews Regulatory aspects of stability testing in Europe. , 1999, Drug development and industrial pharmacy.

[5]  Martindale : the extra pharmacopoeia , 1996 .

[6]  J. Passeron [Effectiveness of trimetazidine in stable effort angina due to chronic coronary insufficiency. A double-blind versus placebo study]. , 1986, Presse medicale.

[7]  Y. Asiri,et al.  In vivo evaluation of hydrochlorothiazide liquisolid tablets in beagle dogs. , 2001, International journal of pharmaceutics.

[8]  Yousef Javadzadeh,et al.  Liquisolid technique as a new approach to sustain propranolol hydrochloride release from tablet matrices. , 2008, International journal of pharmaceutics.

[9]  A. Nokhodchi,et al.  Enhancement of dissolution rate of piroxicam using liquisolid compacts. , 2005, Farmaco.

[10]  B. D. Rohera,et al.  Powdered Solution Technology: Principles and Mechanism , 1992, Pharmaceutical Research.

[11]  E. Gil,et al.  Development and optimization of a novel sustained-release dextran tablet formulation for propranolol hydrochloride. , 2006, International journal of pharmaceutics.

[12]  B. Sa,et al.  Development of Fast Dispersible Aceclofenac Tablets: Effect of Functionality of Superdisintegrants , 2008, Indian journal of pharmaceutical sciences.

[13]  A. Lloyd,et al.  Effects of plasma irradiation on the wettability and dissolution of compacts of griseofulvin. , 2004, International journal of pharmaceutics.

[14]  S. Rossi,et al.  Investigation on bonding and disintegration properties of pharmaceutical materials , 1996 .