Development of pulsatile systems for targeted drug delivery of celecoxib for prophylaxis of colorectal cancer.
The aim of the present study was to formulate fast release enteric-coated tablets for drug delivery to the colon. Two different approaches were used for the preparation of these tablets. The first included making use of superdisintegrant (SD) in the tablet. The amount of super disintegrant (cross-linked PVP) in the tablet and the coat weight were varied to formulate a suitable time-controlled release system, that would provide colon-specific drug delivery. The second approach consisted of development of osmogen-based tablets for drug delivery into the tracts of the colon. Two different osmogens, sodium chloride and potassium chloride, were used. These also were coated at different coat levels. Celecoxib was used as a model drug. In vitro drug release studies showed that superdisintegrants were more effective in showing burst effect in the tablets and therefore showed a rapid drug release as compared with osmogens, which would show a sustained drug release all through the colon. Osmotic tablets were formulated making use of a high concentration of osmogen sodium chloride (OM-SC) and potassium chloride (OM-KC) were further enteric-coated. These also were found to be useful in providing a sustained delivery of nearly 80-90% of the drug into the colonic region. The coat weight required in these tablets for protection in the upper gastrointestinal conditions varied from 9.69% in OM-KC tablets to 4.65% in OM-SC tablets.
Sinha
V R
VR
University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India. vr_sinha@yahoo.com
Bhinge
J R
JR
Kumria
Rachna
R
Kumar
Manoj
M
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics; D001682:Biological Availability; D000068579:Celecoxib; D002482:Cellulose / Q000737:chemistry; D015179:Colorectal Neoplasms / Q000517:prevention & control*; D016503:Drug Delivery Systems / Q000379:methods*; D005079:Excipients / Q000737:chemistry; D006801:Humans; D011092:Polyethylene Glycols / Q000737:chemistry; D011109:Polymethacrylic Acids / Q000737:chemistry; D011145:Polyvinyls / Q000737:chemistry; D011189:Potassium Chloride / Q000737:chemistry; D011720:Pyrazoles / Q000008:administration & dosage* / Q000493:pharmacokinetics; D011759:Pyrrolidines / Q000737:chemistry; D012965:Sodium Chloride / Q000737:chemistry; D013449:Sulfonamides / Q000008:administration & dosage* / Q000493:pharmacokinetics; D013608:Tablets, Enteric-Coated / Q000737:chemistry; D013678:Technology, Pharmaceutical / Q000379:methods
D000894:Anti-Inflammatory Agents, Non-Steroidal; D005079:Excipients; D011109:Polymethacrylic Acids; D011145:Polyvinyls; D011720:Pyrazoles; D011759:Pyrrolidines; D013449:Sulfonamides; D013608:Tablets, Enteric-Coated; C505150:poly(N-vinylpyrrolidine); C038300:methylmethacrylate-methacrylic acid copolymer; D011092:Polyethylene Glycols; D012965:Sodium Chloride; D011189:Potassium Chloride; D002482:Cellulose; D000068579:Celecoxib; C109691:microcrystalline cellulose