Studies on the development of colon targeted oral drug delivery systems for ornidazole in the treatment of amoebiasis.
The aim of the present study is to develop colon-targeted drug delivery systems for ornidazole using guar gum as a carrier. The core formulation containing ornidazole was directly compressed. Compression-coated tablets of ornidazole containing various proportions of guar gum in the coat were prepared. All the formulations were evaluated for hardness and drug content uniformity and were subjected to in vitro drug release studies. The amount of ornidazole released from tablets at different time intervals was estimated by the HPLC method. The compression-coated formulations released less than 8% of ornidazole in the physiological environment of stomach and small intestine. The compression-coated tablets with 85%, 75%, and 65% of guar gum coat released about 21%, 38%, and 73% of ornidazole, 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 ornidazole tablets with either 65% (OLV-65) or 75% (OLV-75) of guar gum coat are most likely to provide targeting of ornidazole for local action in the colon owing to its minimal release of the drug in the first 5 hr. The ornidazole compression-coated tablets showed no change in physical appearance, drug content, or in dissolution pattern after storage at 40 degrees C/75% relative humidity for 6 months.
Krishnaiah
Y S R
YS
Department of Pharmaceutical Sciences, Andhra University, Visakhapatnam, India. krishnaysr112@rediffmail.com
Muzib
Y Indira
YI
Rao
G Srinivasa
GS
Bhaskar
P
P
Satyanarayana
V
V
D000284:Administration, Oral; D000562:Amebiasis / Q000188:drug therapy*; D000818:Animals; D002432:Cecum / Q000187:drug effects / Q000378:metabolism; D003106:Colon / Q000187:drug effects* / Q000378:metabolism; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D016503:Drug Delivery Systems; D004355:Drug Stability; D005079:Excipients; D005685:Galactans / Q000008:administration & dosage / Q000191:economics / Q000493:pharmacokinetics; D006245:Hardness Tests; D008297:Male; D008351:Mannans / Q000008:administration & dosage / Q000191:economics / Q000493:pharmacokinetics; D009950:Ornidazole / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D053149:Plant Gums; D051381:Rats; D013608:Tablets, Enteric-Coated
D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005079:Excipients; D005685:Galactans; D008351:Mannans; D053149:Plant Gums; D013608:Tablets, Enteric-Coated; D009950:Ornidazole; C007894:guar gum