Solid formulation of a supersaturable self-microemulsifying drug delivery system for valsartan with improved dissolution and bioavailability.

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ID: 44791
2017
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Abstract
In order to improve the dissolution and oral bioavailability of valsartan (VST), and reduce the required volume for treatment, we previously formulated a supersaturable self-microemulsifying drug delivery system (SuSMEDDS) composed of VST (80 mg), Capmul MCM (13.2 mg), Tween 80 (59.2 mg), Transcutol P (59.2 mg), and Poloxamer 407 (13.2 mg). In the present study, by using Florite PS-10 (119.1 mg) and Vivapur 105 (105.6 mg) as solid carriers, VST-loaded solidified SuSMEDDS (S-SuSMEDDS) granules were successfully developed, which possessed good flow properties and rapid drug dissolution. By introducing croscarmellose sodium (31 mg) as a superdisintegrant, S-SuSMEDDS tablets were also successfully formulated, which showed fast disintegration and high dissolution efficiency. Preparation of granules and tablets was successfully optimized using D-optimal mixture design and 3-level factorial design, respectively, resulting in percentage prediction errors of <10%. In pharmacokinetic studies in rats, the relative bioavailability of the optimized granules was 107% and 222% of values obtained for SuSMEDDS and Diovan powder, respectively. Therefore, we conclude that novel S-SuSMEDDS formulations offer great potential for developing solid dosage forms of a liquefied formulation such as SuSMEDDS, while improving oral absorption of drugs with poor water solubility.
Reference Key
yeom2017solidoncotarget Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Yeom, Dong Woo;Chae, Bo Ram;Kim, Jin Han;Chae, Jun Soo;Shin, Dong Jun;Kim, Chang Hyun;Kim, Sung Rae;Choi, Ji Ho;Song, Seh Hyon;Oh, Dongho;Sohn, Se Il;Choi, Young Wook;
Journal oncotarget
Year 2017
DOI
10.18632/oncotarget.21691
URL
Keywords
optimization tablet smedds solid carrier valsartan

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