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Telmisartan Spongelike Particles as Oral Capsule: Effect of Polymer Type and Concentration on the Formulation Properties | ||
| karbala journal of pharmaceutical sciences | ||
| Article 1, Volume 6, Issue 10, 2015, Pages 0-0 PDF (0 K) | ||
| Authors | ||
| Hussam H. Tizkam; Alaa A. Abdul Rassol; Ahmed A. Hussain | ||
| Abstract | ||
| Telmisartan (TEL) is a selective angiotensin II receptor blocker used in the management of cardiovascular disorders. It is a class II drug according to Biopharmaceutics Classification System (BCS); with poor solubility and high permeability. Due to its hydrophobic nature, TEL shows low dissolution profile in gastrointestinal fluid resulting in poor absorption, and consequently poor bioavailability. The aim of current study is to prepare TEL spongelike particles (SP) system that enhances the dissolution rate and solubility of TEL. The TEL SP formulas were prepared by quasi-emulsion solvent diffusion method using different types of polymer, e.g., Eudragit E100, Eudragit RS100, Eudragit S100, Eudragit RL100 or Eudragit L100. The effect of polymer type and concentration on the formulation of TEL SP were investigated. Twenty TEL SP formulations were prepared. They were investigated and characterized for production yield, loading efficiency and in vitro drug release in 0.1N HCl pH 1.2). The results showed that the best TEL SP formula was F2 which was prepared using Eudragit E100 as the SP-forming polymer at drug:polymer ratio of (5:1). The TEL SP formula (F2) showed good production yield, loading efficiency, and fast dissolution rate in 0.1 N HCl (more than 80% in less than 30 min). The selected TEL SP formula (F2) was incorporated into hard gelatin capsules. Finally, one can conclude that the SP technology can be a promising alternative way for the formulation of poorly water soluble drugs, such as TEL, into immediate release formulation. Key wards: Telmisartan, spongelike, solubility, Eudragit. | ||
| Keywords | ||
| telmisartan; spongelike; solubility; Eudragit | ||
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