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- W2763080742 abstract "// Dong Woo Yeom 1, * , Bo Ram Chae 1, 2, * , Jin Han Kim 1 , Jun Soo Chae 1 , Dong Jun Shin 1 , Chang Hyun Kim 1 , Sung Rae Kim 1 , Ji Ho Choi 1 , Seh Hyon Song 2 , Dongho Oh 2 , Se Il Sohn 2 and Young Wook Choi 1 1 College of Pharmacy, Chung-Ang University, Seoul 06974, Republic of Korea 2 Daewon Pharm. Co., Ltd, Seoul 04994, Republic of Korea * These authors have contributed equally to this work Correspondence to: Young Wook Choi, email: ywchoi@cau.ac.kr Keywords: valsartan; SMEDDS; solid carrier; tablet; optimization Received: June 27, 2017 Accepted: September 20, 2017 Published: October 09, 2017 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." @default.
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- W2763080742 date "2017-10-09" @default.
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- W2763080742 title "Solid formulation of a supersaturable self-microemulsifying drug delivery system for valsartan with improved dissolution and bioavailability" @default.
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- W2763080742 doi "https://doi.org/10.18632/oncotarget.21691" @default.
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