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Studies on the development of oral colon targeted drug delivery systems for metronidazole in the treatment of amoebiasis.
Int J Pharm. 2002 Apr 02; 236(1-2):43-55.IJ

Abstract

The aim of the present study is to develop colon targeted drug delivery systems for metronidazole using guar gum as a carrier. Matrix, multilayer and compression coated tablets of metronidazole containing various proportions of guar gum were prepared. All the formulations were evaluated for the hardness, drug content uniformity, and were subjected to in vitro drug release studies. The amount of metronidazole released from tablets at different time intervals was estimated by high performance liquid chromatography method. Matrix tablets and multilayer tablets of metronidazole released 43-52% and 25-44% of the metronidazole, respectively, in the physiological environment of stomach and small intestine depending on the proportion of guar gum used in the formulation. Both the formulations failed to control the drug release within 5 h of the dissolution study in the physiological environment of stomach and small intestine. The compression coated formulations released less than 1% of metronidazole in the physiological environment of stomach and small intestine. When the dissolution study was continued in simulated colonic fluids, the compression coated tablet with 275 mg of guar gum coat released another 61% of metronidazole after degradation by colonic bacteria at the end of 24 h of the dissolution study. The compression coated tablets with 350 and 435 mg of guar gum coat released about 45 and 20% of metronidazole, respectively, in simulated colonic fluids indicating the susceptibility of the guar gum formulations to the rat caecal contents. The results of the study show that compression coated metronidazole tablets with either 275 or 350 mg of guar gum coat is most likely to provide targeting of metronidazole for local action in the colon owing to its minimal release of the drug in the first 5 h. The metronidazole compression coated tablets showed no change either in physical appearance, drug content or in dissolution pattern after storage at 40 degrees C/75% RH for 6 months.

Authors+Show Affiliations

Department of Pharmaceutical Sciences, Andhra University, 530 003, Visakhapatnam, 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

11891069

Citation

Krishnaiah, Y S R., et al. "Studies On the Development of Oral Colon Targeted Drug Delivery Systems for Metronidazole in the Treatment of Amoebiasis." International Journal of Pharmaceutics, vol. 236, no. 1-2, 2002, pp. 43-55.
Krishnaiah YS, Bhaskar Reddy PR, Satyanarayana V, et al. Studies on the development of oral colon targeted drug delivery systems for metronidazole in the treatment of amoebiasis. Int J Pharm. 2002;236(1-2):43-55.
Krishnaiah, Y. S., Bhaskar Reddy, P. R., Satyanarayana, V., & Karthikeyan, R. S. (2002). Studies on the development of oral colon targeted drug delivery systems for metronidazole in the treatment of amoebiasis. International Journal of Pharmaceutics, 236(1-2), 43-55.
Krishnaiah YS, et al. Studies On the Development of Oral Colon Targeted Drug Delivery Systems for Metronidazole in the Treatment of Amoebiasis. Int J Pharm. 2002 Apr 2;236(1-2):43-55. PubMed PMID: 11891069.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Studies on the development of oral colon targeted drug delivery systems for metronidazole in the treatment of amoebiasis. AU - Krishnaiah,Y S R, AU - Bhaskar Reddy,P R, AU - Satyanarayana,V, AU - Karthikeyan,R S, PY - 2002/3/14/pubmed PY - 2002/6/25/medline PY - 2002/3/14/entrez SP - 43 EP - 55 JF - International journal of pharmaceutics JO - Int J Pharm VL - 236 IS - 1-2 N2 - The aim of the present study is to develop colon targeted drug delivery systems for metronidazole using guar gum as a carrier. Matrix, multilayer and compression coated tablets of metronidazole containing various proportions of guar gum were prepared. All the formulations were evaluated for the hardness, drug content uniformity, and were subjected to in vitro drug release studies. The amount of metronidazole released from tablets at different time intervals was estimated by high performance liquid chromatography method. Matrix tablets and multilayer tablets of metronidazole released 43-52% and 25-44% of the metronidazole, respectively, in the physiological environment of stomach and small intestine depending on the proportion of guar gum used in the formulation. Both the formulations failed to control the drug release within 5 h of the dissolution study in the physiological environment of stomach and small intestine. The compression coated formulations released less than 1% of metronidazole in the physiological environment of stomach and small intestine. When the dissolution study was continued in simulated colonic fluids, the compression coated tablet with 275 mg of guar gum coat released another 61% of metronidazole after degradation by colonic bacteria at the end of 24 h of the dissolution study. The compression coated tablets with 350 and 435 mg of guar gum coat released about 45 and 20% of metronidazole, respectively, in simulated colonic fluids indicating the susceptibility of the guar gum formulations to the rat caecal contents. The results of the study show that compression coated metronidazole tablets with either 275 or 350 mg of guar gum coat is most likely to provide targeting of metronidazole for local action in the colon owing to its minimal release of the drug in the first 5 h. The metronidazole compression coated tablets showed no change either in physical appearance, drug content or in dissolution pattern after storage at 40 degrees C/75% RH for 6 months. SN - 0378-5173 UR - https://www.unboundmedicine.com/medline/citation/11891069/Studies_on_the_development_of_oral_colon_targeted_drug_delivery_systems_for_metronidazole_in_the_treatment_of_amoebiasis_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378517302000066 DB - PRIME DP - Unbound Medicine ER -