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Preparation of ibuprofen-loaded liquid suppository using eutectic mixture system with menthol.
Eur J Pharm Sci. 2004 Dec; 23(4-5):347-53.EJ

Abstract

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+Show Affiliations

College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, South Korea.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

15567287

Citation

Yong, Chul Soon, et al. "Preparation of Ibuprofen-loaded Liquid Suppository Using Eutectic Mixture System With Menthol." European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, vol. 23, no. 4-5, 2004, pp. 347-53.
Yong CS, Oh YK, Jung SH, et al. Preparation of ibuprofen-loaded liquid suppository using eutectic mixture system with menthol. Eur J Pharm Sci. 2004;23(4-5):347-53.
Yong, C. S., Oh, Y. K., Jung, S. H., Rhee, J. D., Kim, H. D., Kim, C. K., & Choi, H. G. (2004). Preparation of ibuprofen-loaded liquid suppository using eutectic mixture system with menthol. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, 23(4-5), 347-53.
Yong CS, et al. Preparation of Ibuprofen-loaded Liquid Suppository Using Eutectic Mixture System With Menthol. Eur J Pharm Sci. 2004;23(4-5):347-53. PubMed PMID: 15567287.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Preparation of ibuprofen-loaded liquid suppository using eutectic mixture system with menthol. AU - Yong,Chul Soon, AU - Oh,Yu-Kyoung, AU - Jung,Se Hyun, AU - Rhee,Jong-Dal, AU - Kim,Ho-Dong, AU - Kim,Chong-Kook, AU - Choi,Han-Gon, PY - 2004/03/11/received PY - 2004/08/05/revised PY - 2004/08/16/accepted PY - 2004/11/30/pubmed PY - 2005/5/20/medline PY - 2004/11/30/entrez SP - 347 EP - 53 JF - European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences JO - Eur J Pharm Sci VL - 23 IS - 4-5 N2 - 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. SN - 0928-0987 UR - https://www.unboundmedicine.com/medline/citation/15567287/Preparation_of_ibuprofen_loaded_liquid_suppository_using_eutectic_mixture_system_with_menthol_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0928-0987(04)00205-2 DB - PRIME DP - Unbound Medicine ER -