Telmisartan Spongelike Particles as Oral Capsule: Effect of Polymer Type and Concentration on the Formulation Properties
karbala journal of pharmaceutical sciences,
2015, Volume 6, Issue 10, Pages 0-0
AbstractTelmisartan (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.
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