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In vivo evaluation of guargum-based colon-targeted oral drug delivery systems of celecoxib in human volunteers.
Eur J Drug Metab Pharmacokinet. 2002 Oct-Dec; 27(4):273-80.EJ

Abstract

The present study involved the in vivo evaluation of orally administered guar gum-based colon-targeted tablet formulations of celecoxib (colon-targeted tablet-20 or colon-targeted tablet-30) as compared with an immediate release capsule in 15 human volunteers. Blood samples were obtained at different time intervals and the plasma concentration of celecoxib was estimated by reversed phase HPLC. The immediate release capsules of celecoxib might have disintegrated very fast in GI tract and absorbed quickly from stomach and small intestine thereby producing peak plasma concentration (Cmax of 478 +/- 57 ng/ml) within 3.8 +/- 0.1 h (Tmax). Though celecoxib could be seen in plasma after oral administration of colon-targeted tablet-20 or colon-targeted tablet-30 between 1 and 2 h, low levels of drug were observed upto 8 h resulting in peak concentration (Cmax) of 78 +/- 6 ng/ml or 88 +/- 15 ng/ml at 10.5 +/- 1.9 h or 13.5 +/- 1.4 h (Tmax) respectively, whereas the immediate release capsules produced peak plasma concentration (Cmax) of 478 +/- 57 ng/ml at 3.8 +/- 0.1 h (Tmax). Colon-targeted tablets showed decreased AUC(0-infinity), Cmax and absorption rate constant, prolonged absorption time (ta), and increased t1/2 in comparison with the immediate release capsules. The results of the study indicated that the guar gum-based colon-targeted tablets of celecoxib did not release the drug significantly in stomach and small intestine, but delivered to the colon resulting in a slow absorption of the drug and making it available for local action in the colon.

Authors+Show Affiliations

Krishnaiah YS
Department of Pharmaceutical Sciences Andhra University, Visakhapatnam, India.
Satyanarayana V
No affiliation info available
Dinesh Kumar B
No affiliation info available
Karthikeyan RS
No affiliation info available
Bhaskar P
No affiliation info available

MeSH

Anti-Inflammatory Agents, Non-SteroidalArea Under CurveCapsulesCelecoxibColonDrug Delivery SystemsExcipientsGalactansHalf-LifeHumansMannansPlant GumsPyrazolesSolubilitySulfonamides

Pub Type(s)

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

Language

eng

PubMed ID

12587957

Citation

Krishnaiah, Y S R., et al. "In Vivo Evaluation of Guargum-based Colon-targeted Oral Drug Delivery Systems of Celecoxib in Human Volunteers." European Journal of Drug Metabolism and Pharmacokinetics, vol. 27, no. 4, 2002, pp. 273-80.
Krishnaiah YS, Satyanarayana V, Dinesh Kumar B, et al. In vivo evaluation of guargum-based colon-targeted oral drug delivery systems of celecoxib in human volunteers. Eur J Drug Metab Pharmacokinet. 2002;27(4):273-80.
Krishnaiah, Y. S., Satyanarayana, V., Dinesh Kumar, B., Karthikeyan, R. S., & Bhaskar, P. (2002). In vivo evaluation of guargum-based colon-targeted oral drug delivery systems of celecoxib in human volunteers. European Journal of Drug Metabolism and Pharmacokinetics, 27(4), 273-80.
Krishnaiah YS, et al. In Vivo Evaluation of Guargum-based Colon-targeted Oral Drug Delivery Systems of Celecoxib in Human Volunteers. Eur J Drug Metab Pharmacokinet. 2002 Oct-Dec;27(4):273-80. PubMed PMID: 12587957.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - In vivo evaluation of guargum-based colon-targeted oral drug delivery systems of celecoxib in human volunteers. AU - Krishnaiah,Y S R, AU - Satyanarayana,V, AU - Dinesh Kumar,B, AU - Karthikeyan,R S, AU - Bhaskar,P, PY - 2003/2/18/pubmed PY - 2003/7/23/medline PY - 2003/2/18/entrez SP - 273 EP - 80 JF - European journal of drug metabolism and pharmacokinetics JO - Eur J Drug Metab Pharmacokinet VL - 27 IS - 4 N2 - The present study involved the in vivo evaluation of orally administered guar gum-based colon-targeted tablet formulations of celecoxib (colon-targeted tablet-20 or colon-targeted tablet-30) as compared with an immediate release capsule in 15 human volunteers. Blood samples were obtained at different time intervals and the plasma concentration of celecoxib was estimated by reversed phase HPLC. The immediate release capsules of celecoxib might have disintegrated very fast in GI tract and absorbed quickly from stomach and small intestine thereby producing peak plasma concentration (Cmax of 478 +/- 57 ng/ml) within 3.8 +/- 0.1 h (Tmax). Though celecoxib could be seen in plasma after oral administration of colon-targeted tablet-20 or colon-targeted tablet-30 between 1 and 2 h, low levels of drug were observed upto 8 h resulting in peak concentration (Cmax) of 78 +/- 6 ng/ml or 88 +/- 15 ng/ml at 10.5 +/- 1.9 h or 13.5 +/- 1.4 h (Tmax) respectively, whereas the immediate release capsules produced peak plasma concentration (Cmax) of 478 +/- 57 ng/ml at 3.8 +/- 0.1 h (Tmax). Colon-targeted tablets showed decreased AUC(0-infinity), Cmax and absorption rate constant, prolonged absorption time (ta), and increased t1/2 in comparison with the immediate release capsules. The results of the study indicated that the guar gum-based colon-targeted tablets of celecoxib did not release the drug significantly in stomach and small intestine, but delivered to the colon resulting in a slow absorption of the drug and making it available for local action in the colon. SN - 0378-7966 UR - https://www.unboundmedicine.com/medline/citation/12587957/In_vivo_evaluation_of_guargum_based_colon_targeted_oral_drug_delivery_systems_of_celecoxib_in_human_volunteers_ DB - PRIME DP - Unbound Medicine ER -