Absorption Enhancer and Polymer (Vitamin E TPGS and PVP K29) by Solid Dispersion Improve Dissolution and Bioavailability of Eprosartan Mesylate
- Authors
- Ahn, JS[Ahn, Jae Soon]; Kim, KM[Kim, Kang Min]; Ko, CY[Ko, Chan Young]; Kang, JS[Kang, Jae Seon]
- Issue Date
- 20-May-2011
- Keywords
- Bioavailability; Eprosartan mesylate; PVP K29; Solid dispersion; Vitamin E TPGS
- Citation
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.32, no.5, pp.1587 - 1592
- Indexed
- SCIE
SCOPUS
KCI
- Journal Title
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY
- Volume
- 32
- Number
- 5
- Start Page
- 1587
- End Page
- 1592
- URI
- https://scholarworks.bwise.kr/skku/handle/2021.sw.skku/70012
- DOI
- 10.5012/bkcs.2011.32.5.1587
- ISSN
- 0253-2964
- Abstract
- The aim of the present study was to improve the solubility and bioavailability of a poorly water-soluble drug in human body, using a solid dispersion technique (hot melt extrusion). The solid dispersion was prepared by cooling the hot melt of the drug in the carrier (Vitamin E TPGS and PVP). The dissolution rate of formulation 1 from a novel formulation prepared by solid dispersion technique was equal to release of formulation 6 (40% of eprosartan mesylate is in contrast to teveten (R)) within 60 min (Table 1). The oral bioavailability of new eprosartan mesylate tablet having vitamin E TPGS and PVP K29 was tested on rats and dogs. Of the absorption enhancer and polymer tested, vitamin E TPGS and PVP K29, resulted in the greatest increases of AUC in animals (about 2.5-fold increase in rat and dog). When eprosartan mesylate was mixed with the absorption enhancer and polymer in a ratio of 2.94:2:1, vitamin E TPGS and PVP K29 improved eprosartan mesylate bioavailability significantly compared with the conventional immediate release (IR) tablet Teveten (R) (formulation 7). These results show that solid dispersion using vitamin E TPGS and PVP K29 is a promising approach for developing eprosartan mesylate drug products.
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Collections - Pharmacy > Department of Pharmacy > 1. Journal Articles
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