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Physicochemical characterization and in vivo evaluation of poloxamer-based solid suppository containing diclofenac sodium in rats

Title
Physicochemical characterization and in vivo evaluation of poloxamer-based solid suppository containing diclofenac sodium in rats
Author
최한곤
Keywords
diclofenac sodium; poloxamer 124; poloxamer 188; mucoadhesive; poloxamer-based solid suppository; pharmacokinetics
Issue Date
2005-09
Publisher
ELSEVIER SCIENCE BV
Citation
INTERNATIONAL JOURNAL OF PHARMACEUTICS, v. 301, No. 1-2, Page. 54-61
Abstract
To develop a poloxamer-based solid suppository with poloxamer mixtures, the melting point of various formulations composed of poloxamer 124 (P 124) and poloxamer 188 (P 188) were investigated. The dissolution and pharmacokinetic study of diclofenac sodium delivered by the poloxamer-based suppository were performed. Furthermore, the identification test in the rectum and morphology test of rectal tissues were carried out after its rectal administration in rats. The poloxamer mixtures composed of P 124 and P 188 were homogeneous phases. Very small amounts of P 188 affected the melting point of poloxamer mixtures. In particular, the poloxamer mixture [P 124[P 188 (97/3%)] with the melting point of about 32 degrees C was a solid form at room temperature and instantly melted at physiological temperature. Very small amounts of P 188 hardly affected the dissolution rates of diclofenac sodium from the suppository. Dissolution mechanism analysis showed the dissolution of diclofenac sodium was proportional to the time. The poloxamer-based suppository gave significantly higher initial plasma concentrations and faster T x of diclofenac sodium than did conventional PEG-based suppository, indicating that the drug from poloxamer-based suppository could be absorbed faster than that from PEG-based one in rats. It retained in the rectum for at least 4 h and could not irritate or damage the rectal tissues of rats. Thus, the poloxamer-based solid suppository with P 124 and P 188 was a mucoadhesive, safe and effective rectal dosage form for diclofenac sodium. (C) 2005 Elsevier B.V. All rights reserved.
URI
https://www.sciencedirect.com/science/article/pii/S0378517305003340http://repository.hanyang.ac.kr/handle/20.500.11754/111481
ISSN
0378-5173; 1873-3476
DOI
10.1016/j.ijpharm.2005.05.037
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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