Department of Pharmaceutics, College of Pharmacy, Baghdad University, Iraq.

Department of Pharmaceutics, College of Pharmacy, Baghdad University, Iraq.
Telmisartan , Solid dispersion ,PEG6000 ,Poloxamer407 ,

Telmisartan (TEL) is an antihypertensive agent that inhibits the angiotensin. TEL is a BCS class II compound. Therefore, bioavailability of TEL can be improved by increasing its solubility. Recently solid dispersion technique gain high interest by pharmaceutical researcher as an approach for solubility enhancement for poorly soluble dugs. Sixteen formulas of solid dispersion of TEL were prepared using two polymers separately PEG6000 and poloxamer 407 at 4 drug to polymer ratios (1:1, 1:3, 1:5, and 1:7) following two method of preparations (melting and solvent evaporation). The prepared solid dispersions were evaluated for production yield percent, drug content, solubility, FTIR, and DSC study analysis. The results indicate that all prepared formulas of solid dispersion show solubility enhancement at different degree but the maximum solubility enhancement was observed with poloxamer 407 at ratio of 1:1 prepared in melt method. The solubility of telmisartan solid dispersion is increased 27 times the pure one. In addition, the results indicate that as polymer to drug ratio increased, the solubility was increased regarding PEG6000 while the best ratio for poloxamer was 1:1. Moreover, comparison of methods shows that the melting method produce higher enhancement in solubility than solvent evaporation method for both polymers.The FTIR study reveals that there is no chemical interaction while DSC analysis shows disappearance of endothermic peak of drug indicates reducing crystallinity of drug. It can be concluded from the results of this study that solid dispersion of Telmisartan with poloxamer 407 is promising approach for solubility enhancement by simple method.

5 , 11 , 2015