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Enhanced rectal bioavailability of ibuprofen in rats by poloxamer 188 and menthol.
Int J Pharm. 2004 Jan 09; 269(1):169-76.IJ

Abstract

To improve the bioavailability of poorly water-soluble ibuprofen in the rectum 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 poloxamer gels 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 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, 1.2mg/ml. Menthol improved the dissolution rates of ibuprofen from poloxamer gels. Release mechanism showed that the release rate of ibuprofen from the poloxamer gels without menthol was independent of the time but the drug might be released from the poloxamer gels with menthol by Fickian diffusion. Furthermore, the poloxamer gel with menthol (poloxamer/menthol/ibuprofen (15%/0.25%/2.5%)) gave significantly higher initial plasma concentrations, C(max) 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 poloxamer gel with poloxamer 188 and menthol was a more effective rectal dosage form for 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 availableNo affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

14698588

Citation

Yong, Chul Soon, et al. "Enhanced Rectal Bioavailability of Ibuprofen in Rats By Poloxamer 188 and Menthol." International Journal of Pharmaceutics, vol. 269, no. 1, 2004, pp. 169-76.
Yong CS, Yang CH, Rhee JD, et al. Enhanced rectal bioavailability of ibuprofen in rats by poloxamer 188 and menthol. Int J Pharm. 2004;269(1):169-76.
Yong, C. S., Yang, C. H., Rhee, J. D., Lee, B. J., Kim, D. C., Kim, D. D., Kim, C. K., Choi, J. S., & Choi, H. G. (2004). Enhanced rectal bioavailability of ibuprofen in rats by poloxamer 188 and menthol. International Journal of Pharmaceutics, 269(1), 169-76.
Yong CS, et al. Enhanced Rectal Bioavailability of Ibuprofen in Rats By Poloxamer 188 and Menthol. Int J Pharm. 2004 Jan 9;269(1):169-76. PubMed PMID: 14698588.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Enhanced rectal bioavailability of ibuprofen in rats by poloxamer 188 and menthol. AU - Yong,Chul Soon, AU - Yang,Chae Ha, AU - Rhee,Jong-Dal, AU - Lee,Beom-Jin, AU - Kim,Dong-Chool, AU - Kim,Dae-Duk, AU - Kim,Chong-Kook, AU - Choi,Jun-Shik, AU - Choi,Han-Gon, PY - 2003/12/31/pubmed PY - 2004/5/18/medline PY - 2003/12/31/entrez SP - 169 EP - 76 JF - International journal of pharmaceutics JO - Int J Pharm VL - 269 IS - 1 N2 - To improve the bioavailability of poorly water-soluble ibuprofen in the rectum 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 poloxamer gels 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 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, 1.2mg/ml. Menthol improved the dissolution rates of ibuprofen from poloxamer gels. Release mechanism showed that the release rate of ibuprofen from the poloxamer gels without menthol was independent of the time but the drug might be released from the poloxamer gels with menthol by Fickian diffusion. Furthermore, the poloxamer gel with menthol (poloxamer/menthol/ibuprofen (15%/0.25%/2.5%)) gave significantly higher initial plasma concentrations, C(max) 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 poloxamer gel with poloxamer 188 and menthol was a more effective rectal dosage form for ibuprofen. SN - 0378-5173 UR - https://www.unboundmedicine.com/medline/citation/14698588/Enhanced_rectal_bioavailability_of_ibuprofen_in_rats_by_poloxamer_188_and_menthol_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378517303005143 DB - PRIME DP - Unbound Medicine ER -