Research Papers:

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

Dong Woo Yeom, Bo Ram Chae, Jin Han Kim, Jun Soo Chae, Dong Jun Shin, Chang Hyun Kim, Sung Rae Kim, Ji Ho Choi, Seh Hyon Song, Dongho Oh, Se Il Sohn and Young Wook Choi _

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Oncotarget. 2017; 8:94297-94316. https://doi.org/10.18632/oncotarget.21691

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Dong Woo Yeom1,*, Bo Ram Chae1,2,*, Jin Han Kim1, Jun Soo Chae1, Dong Jun Shin1, Chang Hyun Kim1, Sung Rae Kim1, Ji Ho Choi1, Seh Hyon Song2, Dongho Oh2, Se Il Sohn2 and Young Wook Choi1

1College of Pharmacy, Chung-Ang University, Seoul 06974, Republic of Korea

2Daewon Pharm. Co., Ltd, Seoul 04994, Republic of Korea

*These authors have contributed equally to this work

Correspondence to:

Young Wook Choi, email: [email protected]

Keywords: valsartan; SMEDDS; solid carrier; tablet; optimization

Received: June 27, 2017    Accepted: September 20, 2017    Published: October 09, 2017


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.

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