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Studies on the development of colon-targeted delivery systems for celecoxib in the prevention of colorectal cancer.
J Drug Target. 2002 May; 10(3):247-54.JD

Abstract

The nonsteroidal anti-inflammatory drugs (NSAIDs) are found to be potential chemopreventive agents of colorectal cancer. Celecoxib, an NSAID with selective cyclooxygenase-2 inhibition, was proved to be effective for the prevention of colon cancer in patients with familial adenomatous polyposis (FAP) and sporadic polyps. In the light of this information, the present study was carried out to develop oral colon-targeting drug delivery systems for celecoxib using guar gum as a carrier. Matrix tablets containing various proportions of guar gum were prepared by wet granulation technique using starch paste as a binder. The tablets were evaluated for hardness, drug content and were subjected to in vitro drug release studies. The amount of celecoxib released from the matrix tablets at different time intervals was estimated by a HPLC method. Guar gum matrix tablets released only 2-4% of celecoxib in the physiological environment of stomach and small intestine depending on the proportion of guar gum used in the formulation. When the dissolution study was continued in simulated colonic fluids (rat caecal content medium), the matrix tablets containing 20% of guar gum released another 37% of celecoxib after degradation by the colonic bacterial action. The matrix tablets containing 30% of guar gum released about 24% of celecoxib in simulated colonic fluids indicating the susceptibility of the guar gum formulations to the rat caecal contents. The results of the study show that the matrix tablets containing either 20 or 30% of guar gum are most likely to target celecoxib for local action in the colon. The guar gum matrix tablets of celecoxib showed no change either in physical appearance, drug content or in dissolution pattern after storage at 40 degrees C/RH 75% for 6 months. Differential scanning calorimetry (DSC) studies indicated no possibility of interaction between celecoxib and guar gum/other formulation excipients.

Authors+Show Affiliations

Department of Pharmaceutical Sciences, Andhra University, India. krishnaysr112@rediffmail.comNo 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

12075826

Citation

Krishnaiah, Y S R., et al. "Studies On the Development of Colon-targeted Delivery Systems for Celecoxib in the Prevention of Colorectal Cancer." Journal of Drug Targeting, vol. 10, no. 3, 2002, pp. 247-54.
Krishnaiah YS, Satyanarayana V, Kumar BD, et al. Studies on the development of colon-targeted delivery systems for celecoxib in the prevention of colorectal cancer. J Drug Target. 2002;10(3):247-54.
Krishnaiah, Y. S., Satyanarayana, V., Kumar, B. D., & Karthikeyan, R. S. (2002). Studies on the development of colon-targeted delivery systems for celecoxib in the prevention of colorectal cancer. Journal of Drug Targeting, 10(3), 247-54.
Krishnaiah YS, et al. Studies On the Development of Colon-targeted Delivery Systems for Celecoxib in the Prevention of Colorectal Cancer. J Drug Target. 2002;10(3):247-54. PubMed PMID: 12075826.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Studies on the development of colon-targeted delivery systems for celecoxib in the prevention of colorectal cancer. AU - Krishnaiah,Y S R, AU - Satyanarayana,V, AU - Kumar,B Dinesh, AU - Karthikeyan,R S, PY - 2002/6/22/pubmed PY - 2002/11/26/medline PY - 2002/6/22/entrez SP - 247 EP - 54 JF - Journal of drug targeting JO - J Drug Target VL - 10 IS - 3 N2 - The nonsteroidal anti-inflammatory drugs (NSAIDs) are found to be potential chemopreventive agents of colorectal cancer. Celecoxib, an NSAID with selective cyclooxygenase-2 inhibition, was proved to be effective for the prevention of colon cancer in patients with familial adenomatous polyposis (FAP) and sporadic polyps. In the light of this information, the present study was carried out to develop oral colon-targeting drug delivery systems for celecoxib using guar gum as a carrier. Matrix tablets containing various proportions of guar gum were prepared by wet granulation technique using starch paste as a binder. The tablets were evaluated for hardness, drug content and were subjected to in vitro drug release studies. The amount of celecoxib released from the matrix tablets at different time intervals was estimated by a HPLC method. Guar gum matrix tablets released only 2-4% of celecoxib in the physiological environment of stomach and small intestine depending on the proportion of guar gum used in the formulation. When the dissolution study was continued in simulated colonic fluids (rat caecal content medium), the matrix tablets containing 20% of guar gum released another 37% of celecoxib after degradation by the colonic bacterial action. The matrix tablets containing 30% of guar gum released about 24% of celecoxib in simulated colonic fluids indicating the susceptibility of the guar gum formulations to the rat caecal contents. The results of the study show that the matrix tablets containing either 20 or 30% of guar gum are most likely to target celecoxib for local action in the colon. The guar gum matrix tablets of celecoxib showed no change either in physical appearance, drug content or in dissolution pattern after storage at 40 degrees C/RH 75% for 6 months. Differential scanning calorimetry (DSC) studies indicated no possibility of interaction between celecoxib and guar gum/other formulation excipients. SN - 1061-186X UR - https://www.unboundmedicine.com/medline/citation/12075826/Studies_on_the_development_of_colon_targeted_delivery_systems_for_celecoxib_in_the_prevention_of_colorectal_cancer_ DB - PRIME DP - Unbound Medicine ER -