| Preparation of ibuprofen-loaded liquid suppository using eutectic mixture system with menthol. | |
| | |
MedLine Citation:
|
PMID: 15567287 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
To prepare an ibuprofen-loaded liquid suppository using eutectic mixture with menthol, the effects of menthol and poloxamer 188 (P 188) on the aqueous solubility of ibuprofen were investigated. The physicochemical properties such as gelation temperature, gel strength and bioadhesive force of various formulations composed of ibuprofen, menthol and P 188 were investigated. Then, the pharmacokinetic study of ibuprofen delivered by the liquid suppositories composed of P 188 and menthol were then performed. In the absence of P 188, the solubility of ibuprofen increased until the ratio of menthol to ibuprofen increased from 0:10 to 4:6 followed by an abrupt decrease in solubility above the ratio of 4:6, indicating that four parts of ibuprofen formed eutectic mixture with six parts of menthol. In the presence of P 188, the solutions with the same ratio showed abrupt increase in the solubility of ibuprofen. Furthermore, the solution with ratio of 4:6 showed more than 2.5- and 6-fold increase in the solubility of ibuprofen compared with that without additives and that without menthol, respectively. The poloxamer gel with menthol/ibuprofen ratio of 1:9 and higher than 15% poloxamer 188 showed the maximum solubility of ibuprofen, 1.2mg/ml. Ibuprofen increased the gelation temperature and weakened the gel strength and bioadhesive force of liquid suppositories. However, menthol did the opposite due to forming the eutectic mixture with ibuprofen. The ibuprofen-loaded liquid suppository [P 188/menthol/ibuprofen (15/0.25/2.5%)] with the maximum ibuprofen solubility of 1.2mg/ml was administered easily to the anus and to remain at the administered site without leakage after the dose. Furthermore, it gave significantly higher initial plasma concentrations, Cmax and AUC of ibuprofen than did solid suppository, indicating that the drug from poloxamer gel could be more absorbed than that from solid one in rats. Thus, the liquid suppository system with P 188 and menthol, a more convenient and effective rectal dosage form for ibuprofen will be expected to enhance the rectal bioavailability of ibuprofen. |
| | |
Authors:
|
Chul Soon Yong; Yu-Kyoung Oh; Se Hyun Jung; Jong-Dal Rhee; Ho-Dong Kim; Chong-Kook Kim; Han-Gon Choi |
Related Documents
:
|
9248667 - Components of the blood acid-base disturbance that accompanies urethane anaesthesia in ... 3430867 - Suppression of brown adipose tissue metabolism following intraventricular bombesin in r... 165727 - Regulation of liver diphosphofructose phosphatase of the rat and hamster. 7246797 - Temperature dependence of rat circadian pacemaker. 8388707 - Evidence that endogenous arginine-vasopressin (avp) is involved in the maintenance of t... 20658207 - Evaluation of fluoride-induced oxidative stress in rat brain: a multigeneration study. |
Publication Detail:
|
Type: Comparative Study; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
|
Title: European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences Volume: 23 ISSN: 0928-0987 ISO Abbreviation: Eur J Pharm Sci Publication Date: 2004 Dec |
Date Detail:
|
Created Date: 2004-11-29 Completed Date: 2005-05-19 Revised Date: 2006-11-15 |
Medline Journal Info:
|
Nlm Unique ID: 9317982 Medline TA: Eur J Pharm Sci Country: Netherlands |
Other Details:
|
Languages: eng Pagination: 347-53 Citation Subset: IM |
Affiliation:
|
College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, South Korea. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Animals Ibuprofen / chemical synthesis*, pharmacokinetics Male Menthol / chemical synthesis*, pharmacokinetics Rats Rats, Sprague-Dawley Solubility Suppositories Technology, Pharmaceutical / instrumentation, methods* |
| Chemical | |
Reg. No./Substance:
|
0/Suppositories; 1490-04-6/Menthol; 15687-27-1/Ibuprofen |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: N4-alkyloxycarbonyl derivatives of cytosine: physicochemical characterisation, and cytosine regenera...
Next Document: Development and validation of a direct, non-destructive quantitative method for medroxyprogesterone ...