Tags

Type your tag names separated by a space and hit enter

In vitro and in vivo evaluation of guar gum-based matrix tablets of rofecoxib for colonic drug delivery.
Curr Drug Deliv. 2005 Apr; 2(2):155-63.CD

Abstract

The present study was carried out to develop and evaluate guar gum-based matrix tablets of rofecoxib for their intended use in the chemoprevention of colorectal cancer. Matrix tablets containing 40% (RXL-40), 50% (RXL-50), 60% (RXL-60) or 70% (RXL-70) of guar gum were prepared by wet granulation technique, and were subjected to in vitro drug release studies. Guar gum matrix tablets released only 5 to 12% of rofecoxib in the physiological environment of stomach and small intestine. The matrix tablets RXL-40 disintegrated completely within 10 h in a dissolution medium without rat caecal contents (control study), and hence not studied further. When the dissolution study was continued in simulated colonic fluids (rat caecal content medium), the matrix tablets RXL-50 were acted upon by colonic bacterial enzymes releasing the entire quantity of drug wherein there was no appreciable difference when compared to that released in control study. The matrix tablets RXL-60 released another 88% of rofecoxib whereas matrix tablets RXL-70 released only 57% of rofecoxib in simulated colonic fluids indicating the susceptibility of the guar gum formulations to the rat caecal contents. The guar gum matrix tablets RXL-70 were subjected to in vivo evaluation in human volunteers to find their ability of targeting rofecoxib to colon. The delayed Tmax, prolonged absorption time (ta), decreased Cmax and decreased ka indicated that rofecoxib was not released significantly in stomach and small intestine, but was delivered to colon resulting in a slow absorption of the drug and making it available for local action in human colon.

Authors+Show Affiliations

Department of Pharmaceutics, Faculty of Pharmacy, Kuwait University, PO Box 24923, SAFAT 13110, Kuwait.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

16305416

Citation

Al-Saidan, S M., et al. "In Vitro and in Vivo Evaluation of Guar Gum-based Matrix Tablets of Rofecoxib for Colonic Drug Delivery." Current Drug Delivery, vol. 2, no. 2, 2005, pp. 155-63.
Al-Saidan SM, Krishnaiah YS, Satyanarayana V, et al. In vitro and in vivo evaluation of guar gum-based matrix tablets of rofecoxib for colonic drug delivery. Curr Drug Deliv. 2005;2(2):155-63.
Al-Saidan, S. M., Krishnaiah, Y. S., Satyanarayana, V., & Rao, G. S. (2005). In vitro and in vivo evaluation of guar gum-based matrix tablets of rofecoxib for colonic drug delivery. Current Drug Delivery, 2(2), 155-63.
Al-Saidan SM, et al. In Vitro and in Vivo Evaluation of Guar Gum-based Matrix Tablets of Rofecoxib for Colonic Drug Delivery. Curr Drug Deliv. 2005;2(2):155-63. PubMed PMID: 16305416.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - In vitro and in vivo evaluation of guar gum-based matrix tablets of rofecoxib for colonic drug delivery. AU - Al-Saidan,S M, AU - Krishnaiah,Y S R, AU - Satyanarayana,V, AU - Rao,G S, PY - 2005/11/25/pubmed PY - 2005/12/24/medline PY - 2005/11/25/entrez SP - 155 EP - 63 JF - Current drug delivery JO - Curr Drug Deliv VL - 2 IS - 2 N2 - The present study was carried out to develop and evaluate guar gum-based matrix tablets of rofecoxib for their intended use in the chemoprevention of colorectal cancer. Matrix tablets containing 40% (RXL-40), 50% (RXL-50), 60% (RXL-60) or 70% (RXL-70) of guar gum were prepared by wet granulation technique, and were subjected to in vitro drug release studies. Guar gum matrix tablets released only 5 to 12% of rofecoxib in the physiological environment of stomach and small intestine. The matrix tablets RXL-40 disintegrated completely within 10 h in a dissolution medium without rat caecal contents (control study), and hence not studied further. When the dissolution study was continued in simulated colonic fluids (rat caecal content medium), the matrix tablets RXL-50 were acted upon by colonic bacterial enzymes releasing the entire quantity of drug wherein there was no appreciable difference when compared to that released in control study. The matrix tablets RXL-60 released another 88% of rofecoxib whereas matrix tablets RXL-70 released only 57% of rofecoxib in simulated colonic fluids indicating the susceptibility of the guar gum formulations to the rat caecal contents. The guar gum matrix tablets RXL-70 were subjected to in vivo evaluation in human volunteers to find their ability of targeting rofecoxib to colon. The delayed Tmax, prolonged absorption time (ta), decreased Cmax and decreased ka indicated that rofecoxib was not released significantly in stomach and small intestine, but was delivered to colon resulting in a slow absorption of the drug and making it available for local action in human colon. SN - 1567-2018 UR - https://www.unboundmedicine.com/medline/citation/16305416/In_vitro_and_in_vivo_evaluation_of_guar_gum_based_matrix_tablets_of_rofecoxib_for_colonic_drug_delivery_ DB - PRIME DP - Unbound Medicine ER -