Development of a solidified self-microemulsifying drug delivery system (S-SMEDDS) for atorvastatin calcium with improved dissolution and bioavailability
- Authors
- Yeom, Dong Woo; Son, Ho Yong; Kim, Jin Han; Kim, Sung Rae; Lee, Sang Gon; Song, She Hyon; Chae, Bo Ram; Choi, Young Wook
- Issue Date
- Jun-2016
- Publisher
- ELSEVIER SCIENCE BV
- Keywords
- Atorvastatin; SMEDDS; Solidified SMEDDS; Solid carrier; Sylysia (R) 350; Mannitol
- Citation
- INTERNATIONAL JOURNAL OF PHARMACEUTICS, v.506, no.1-2, pp 302 - 311
- Pages
- 10
- Journal Title
- INTERNATIONAL JOURNAL OF PHARMACEUTICS
- Volume
- 506
- Number
- 1-2
- Start Page
- 302
- End Page
- 311
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/6826
- DOI
- 10.1016/j.ijpharm.2016.04.059
- ISSN
- 0378-5173
1873-3476
- Abstract
- To improve the dissolution and oral bioavailability (BA) of atorvastatin calcium (ATV), we previously introduced an optimized self-microemulsifying drug delivery system (SMEDDS) using Capmul (R) MCM (oil), Tween (R) 20 (surfactant), and tetraglycol (cosurfactant). In this study, various solid carriers were employed to develop a solidified SMEDDS (S-SMEDDS): mannitol (M) and lactose (L) as water-soluble carriers, and Sylysia (R) 350 (S) and Aerosil (R) 200 (A) as water-insoluble carriers. Maximum solidifying capacities (SCmax) of water-insoluble carriers were significantly greater than those of water-soluble carriers were. The resultant powders were free flowing with an angle of repose <40 degrees and Carr's index 5-20%, regardless of the solid carrier types. S-SMEDDS with mannitol (S(M)-SMEDDS) or lactose (S(L)SMEDDS) had a smaller droplet size and greater dissolution than S-SMEDDS with Sylysia (R) 350 (S(S)SMEDDS) or Aerosil (R) 200 (S(A)-SMEDDS). Following oral administration of various formulations to rats at a dose equivalent to 25 mg/kg of ATV, plasma drug levels were measured by LC-MS/MS. The relative BAs (RBAs) of SMEDDS, S(M)-SMEDDS, and S(S)-SMEDDS were 345%, 216%, and 160%, respectively, compared to that of ATV suspension. Additionally, at a reduced dose of ATV equivalent to 5 mg/kg, the RBAs of S(M)-SMEDDS and S(S)-SMEDDS compared to that of SMEDDS were 101% and 65%, respectively. These results suggest that S(M)-SEMDDS offers great potential for the development of solid dosage forms with improved oral absorption of drugs with poor water solubility. (c) 2016 Elsevier B.V. All rights reserved.
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