ENHANCEMENT OF THE SOLUBILITY AND THE DISSOLUTION RATE OF CANDESARTAN CILEXETIL USING MICROSPONGE TECHNOLOGY

Shaimaa Nazar Abd Alhammid

doi:10.22159/ajpcr.2018.v11i9.26816

Authors

Shaimaa Nazar Abd Alhammid Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Iraq.

DOI:

https://doi.org/10.22159/ajpcr.2018.v11i9.26816

Keywords:

Candesartan cilexetil, Eudragit, Microsponges, Polyvinyl alcohol, Quasi-emulsion solvent diffusion method

Abstract

Objective: The aim of the present study is to enhance the dissolution rate of candesartan cilexetil (CC) using microsponges. Candesartan is therapeutically a potent antihypertensive agent, but it suffers a major drawback of poor oral bioavailability, which is estimated to be 15% due to its low solubility in the gastrointestinal fluids and hepatic first-pass metabolism.

Methods: Eudragit-based microsponges were prepared by quasi-emulsion solvent diffusion method using different drugâ€“polymer ratios (1:1 to 1:6), stirring speeds (250â€“750 rpm), and emulsifier concentrations (polyvinyl alcohol) (0.05%â€“0.083% w/v). Differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) study for CC, physical mixtures of drugâ€“polymer, and selected formula were investigated to estimate compatibility of CC with other used ingredients. All formulations were evaluated for particle size, production yield, and loading efficiency. The in vitro drug release study of optimized formulation was performed in phosphate buffer pH 6.8.

Results: The obtained results indicated that formula F3 which contains eudragit RS100 at drug:polymer ratio (6:1) was showed the smallest particle size with higher production yield and loading efficiency. DSC and FTIR study of the physical mixtures of drug and polymer revealed no drugâ€“polymer interaction. The results clearly confirm that the percentage of CC released at 30 min from F3, CC powder, and self-made tablet was 54%, 20.325, and 38.9%, respectively.

Conclusion: Microsponges technique was considered as a promising system to enhance the solubility and dissolution rate of poor-water soluble CC.

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Author Biography

Shaimaa Nazar Abd Alhammid, Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Iraq.

Assistant Professor in Pharmaceutics department and Assistant Dean in the College of Pharmacy University of Baghdad for Scientific Affairs and Post Graduate Studies

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