Physical properties and in vivo bioavailability in human volunteers of isradipine using controlled release matrix tablet containing self-emulsifying solid dispersion
- Authors
- Phuong Ha-Lien Tran; Thao Truong-Dinh Tran; Piao, Zong Zhu; Toi Van Vo; Park, Jun Bom; Lim, Jisung; Oh, Kyung Teak; Rhee, Yun-Seok; Lee, Beom-Jin
- Issue Date
- Jun-2013
- Publisher
- ELSEVIER SCIENCE BV
- Keywords
- Self-emulsifying solid dispersion; Enhanced dissolution; Controlled release tablet; Physicochemical properties; In vivo bioavailability
- Citation
- INTERNATIONAL JOURNAL OF PHARMACEUTICS, v.450, no.1-2, pp 79 - 86
- Pages
- 8
- Journal Title
- INTERNATIONAL JOURNAL OF PHARMACEUTICS
- Volume
- 450
- Number
- 1-2
- Start Page
- 79
- End Page
- 86
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/14537
- DOI
- 10.1016/j.ijpharm.2013.04.022
- ISSN
- 0378-5173
1873-3476
- Abstract
- Poorly water-soluble drug with a short half-life such as isradipine (IDP) offer challenges in the controlled release formulation because of low dissolution rate and poor bioavailability. Self-emulsifying solid dispersions (SESD) of IDP consisted of surfactant and fatty acid in poloxamer 407 (POX 407) as a carrier and were manufactured by the melting method. Then, controlled release HPMC matrix tablet containing SESD were prepared via direct compression. The dissolution behaviors and in vivo bioavailability of controlled release matrix tablet in healthy human volunteers were investigated. The physical properties of solid dispersion were also examined using differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM). It was shown that structure of IDP was amorphous in the solid dispersion. The dissolution rate of IDP from SESD was markedly enhanced because of increased solubility and wetting effect. Controlled release HPMC matrix tablets containing SESD released drug in a controlled manner and were stable during storage over 3 months at 40 degrees C/75% RH. Furthermore, the tablet containing 5 mg IDP SESD showed significantly increased oral bioavailability and extended plasma concentration compared with the marketed 5 mg Dynacirc (R) capsule. A combined method of solid dispersion and controlled release technology could provide versatile dosage formulations containing IDP with poor water solubility and short half-life. (C) 2013 Elsevier B.V. All rights reserved.
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Collections - College of Pharmacy > School of Pharmacy > 1. Journal Articles
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