Physicochemical characterization of diclofenac sodium-loaded poloxamer gel as a rectal delivery system with fast absorption
- Title
- Physicochemical characterization of diclofenac sodium-loaded poloxamer gel as a rectal delivery system with fast absorption
- Author
- 최한곤
- Keywords
- Diclofenac sodium; Sodium chloride; Poloxamer gel; Pharmacokinetics
- Issue Date
- 2003-05
- Publisher
- TAYLOR & FRANCIS INC
- Citation
- DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, v. 29, issue. 5, page. 545-553
- Abstract
- Rectal poloxamer gel systems composed of poloxamers and bioadhesive polymers were
easy to administer to the anus and were mucoadhesive to the rectal tissues without
leakage after the dose. However, a poloxamer gel containing diclofenac sodium could
not be developed using bioadhesive polymers, since the drug was precipitated in this
preparation. To develop a poloxamer gel using sodium chloride instead of bioadhesive
polymers, the physicochemical properties such as gelation temperature, gel strength, and
bioadhesive force of various formulations composed of diclofenac sodium, poloxamers,
and sodium chloride were investigated. Furthermore, the pharmacokinetic study of
diclofenac sodium delivered by the poloxamer gel was performed. Diclofenac sodium
significantly increased the gelation temperature and weakened the gel strength and
bioadhesive force, while sodium chloride did the opposite. The poloxamer gels with
less than 1.0% sodium chloride, in which the drug was not precipitated, were inserted
into the rectum without difficulty and leakage, and were retained in the rectum of rats
for at least 6 hr. Furthermore, poloxamer gel gave significantly higher initial plasma
concentrations and faster Tmax of diclofenac sodium than did solid suppository, indicating that drug from poloxamer gel could be absorbed faster than that from the solid one
in rats. Our results suggested that a rectal poloxamer gel system with sodium chloride
and poloxamers was a more physically stable, convenient, and effective rectal dosage
form for diclofenac sodium.
- URI
- https://www.tandfonline.com/doi/full/10.1081/DDC-120018643https://repository.hanyang.ac.kr/handle/20.500.11754/155765
- ISSN
- 0363-9045
- DOI
- 10.1081/DDC-120018643
- Appears in Collections:
- COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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