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Enhanced oral bioavailability of ibuprofen in rats by poloxamer gel using poloxamer 188 and menthol.
Drug Dev Ind Pharm. 2005 Aug; 31(7):615-22.DD

Abstract

To improve the oral bioavailability of poorly water-soluble ibuprofen with poloxamer and menthol, the effects of menthol and poloxamer 188 on the aqueous solubility of ibuprofen were investigated. The dissolution and pharmacokinetic study of ibuprofen delivered by the ibuprofen-loaded preparations composed of poloxamer 188 and menthol were then performed. In the absence of poloxamer, 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 menthol formed eutectic mixture with six parts ibuprofen. In the presence of poloxamer, the solutions with the same ratio of menthol to ibuprofen showed an abrupt increase in the solubility of ibuprofen. The poloxamer gel with menthol/ibuprofen ratio of 1:9 and higher than 15% poloxamer 188 showed the maximum solubility of ibuprofen, 1.2 mg/mL. The simultaneous addition of menthol and poloxamer 188 significantly improved the dissolution rates of ibuprofen from aqueous solution due to the ibuprofen solubility-improving effect of menthol in the presence of poloxamer. Furthermore, the ibuprofen-loaded preparation with menthol and poloxamer 188 gave significantly higher initial plasma concentrations, Cmax, and AUC of ibuprofen than did the preparation without menthol and poloxamer 188, indicating that the simultaneous addition of menthol and poloxamer 188 could improve the oral bioavailability of ibuprofen in rats. In modern pain management it is always desirable for the ibuprofen-loaded preparation with poloxamer 188 and menthol to show a rapid onset of action with a minimal phase of lag time to feel the decreased pain. From an industry point of view, it is more desirable for a formulation to be fast acting, easy to use, and cost effective. Thus, the ibuprofen-loaded preparation with poloxamer 188 and menthol was a more effective oral dosage form for poorly water-soluble ibuprofen.

Authors+Show Affiliations

College of Pharmacy, Yeungnam University, Gyongsan, South Korea.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

16207608

Citation

Yong, Chul Soon, et al. "Enhanced Oral Bioavailability of Ibuprofen in Rats By Poloxamer Gel Using Poloxamer 188 and Menthol." Drug Development and Industrial Pharmacy, vol. 31, no. 7, 2005, pp. 615-22.
Yong CS, Lee MK, Park YJ, et al. Enhanced oral bioavailability of ibuprofen in rats by poloxamer gel using poloxamer 188 and menthol. Drug Dev Ind Pharm. 2005;31(7):615-22.
Yong, C. S., Lee, M. K., Park, Y. J., Kong, K. H., Xuan, J. J., Kim, J. H., Kim, J. A., Lyoo, W. S., Han, S. S., Rhee, J. D., Kim, J. O., Yang, C. H., Kim, C. K., & Choi, H. G. (2005). Enhanced oral bioavailability of ibuprofen in rats by poloxamer gel using poloxamer 188 and menthol. Drug Development and Industrial Pharmacy, 31(7), 615-22.
Yong CS, et al. Enhanced Oral Bioavailability of Ibuprofen in Rats By Poloxamer Gel Using Poloxamer 188 and Menthol. Drug Dev Ind Pharm. 2005;31(7):615-22. PubMed PMID: 16207608.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Enhanced oral bioavailability of ibuprofen in rats by poloxamer gel using poloxamer 188 and menthol. AU - Yong,Chul Soon, AU - Lee,Mi-Kyung, AU - Park,Young-Joon, AU - Kong,Kyung-Hwan, AU - Xuan,Jing Ji, AU - Kim,Ji-Hyun, AU - Kim,Jung-Ae, AU - Lyoo,Won Seok, AU - Han,Sung Soo, AU - Rhee,Jong-Dal, AU - Kim,Jong Oh, AU - Yang,Chae Ha, AU - Kim,Chong-Kook, AU - Choi,Han-Gon, PY - 2005/10/7/pubmed PY - 2006/7/6/medline PY - 2005/10/7/entrez SP - 615 EP - 22 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 31 IS - 7 N2 - To improve the oral bioavailability of poorly water-soluble ibuprofen with poloxamer and menthol, the effects of menthol and poloxamer 188 on the aqueous solubility of ibuprofen were investigated. The dissolution and pharmacokinetic study of ibuprofen delivered by the ibuprofen-loaded preparations composed of poloxamer 188 and menthol were then performed. In the absence of poloxamer, 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 menthol formed eutectic mixture with six parts ibuprofen. In the presence of poloxamer, the solutions with the same ratio of menthol to ibuprofen showed an abrupt increase in the solubility of ibuprofen. The poloxamer gel with menthol/ibuprofen ratio of 1:9 and higher than 15% poloxamer 188 showed the maximum solubility of ibuprofen, 1.2 mg/mL. The simultaneous addition of menthol and poloxamer 188 significantly improved the dissolution rates of ibuprofen from aqueous solution due to the ibuprofen solubility-improving effect of menthol in the presence of poloxamer. Furthermore, the ibuprofen-loaded preparation with menthol and poloxamer 188 gave significantly higher initial plasma concentrations, Cmax, and AUC of ibuprofen than did the preparation without menthol and poloxamer 188, indicating that the simultaneous addition of menthol and poloxamer 188 could improve the oral bioavailability of ibuprofen in rats. In modern pain management it is always desirable for the ibuprofen-loaded preparation with poloxamer 188 and menthol to show a rapid onset of action with a minimal phase of lag time to feel the decreased pain. From an industry point of view, it is more desirable for a formulation to be fast acting, easy to use, and cost effective. Thus, the ibuprofen-loaded preparation with poloxamer 188 and menthol was a more effective oral dosage form for poorly water-soluble ibuprofen. SN - 0363-9045 UR - https://www.unboundmedicine.com/medline/citation/16207608/Enhanced_oral_bioavailability_of_ibuprofen_in_rats_by_poloxamer_gel_using_poloxamer_188_and_menthol_ L2 - https://www.tandfonline.com/doi/full/10.1080/03639040500216113 DB - PRIME DP - Unbound Medicine ER -