Solid formulation of a supersaturable self-microemulsifying drug delivery system for valsartan with improved dissolution and bioavailability
- 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
- Issue Date
- 7-Nov-2017
- Publisher
- IMPACT JOURNALS LLC
- Keywords
- valsartan; SMEDDS; solid carrier; tablet; optimization
- Citation
- ONCOTARGET, v.8, no.55, pp 94297 - 94316
- Pages
- 20
- Journal Title
- ONCOTARGET
- Volume
- 8
- Number
- 55
- Start Page
- 94297
- End Page
- 94316
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/3646
- DOI
- 10.18632/oncotarget.21691
- ISSN
- 1949-2553
1949-2553
- 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 (R) MCM (13.2 mg), Tween (R) 80 (59.2 mg), Transcutol (R) P (59.2 mg), and Poloxamer 407 (13.2 mg). In the present study, by using Florite (R) PS-10 (119.1 mg) and Vivapur (R) 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 (R) 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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