Design and in vitro evaluation of a novel vaginal drug delivery system based on gelucire.
Carbamazepine indicated for the control of epilepsy, undergoes extensive hepatic first-pass metabolism after oral administration. A vaginal dosage form of carbamazepine is not commercially available. Conventional suppository having poor retention in the vaginal tract, as they are removed in a short time by the tract's self-cleansing action, having poor patient compliance. To overcome such problems, delivery system with mucoadhesive polymers polyox WSR N-60K and Ucarflock 302 that prolong drug permanence on the vaginal mucosa were developed. In the present study the suitability of gelucires to formulate vaginal pesseries was investigated. The possible modification of carbamazepine release kinetics by using gelucires blends and hydrophilic additives in the pesseries was evaluated. It was observed that among gelucire grades melting point higher than 37 degrees C, the release rate proved to be highly dependant on HLB value and matrix composition. In most of the formulations carbamazepine release occurred by disintegration and erosion of the matrices which is depending upon the vehicle employed. The aging study revealed that the formulations containing G50/13 and G50/13-G44/14 blends undergo some changes during one year of shelf aging. From the results obtained it can be concluded that different gelucire grades and their blends along with hydrophilic polymer could be successesively used to formulate prolong release carbamazepine pesseries.
Geeta
M Patel
MP
Department of Pharmaceutics & Pharmaceutical Technology, S.K. Patel College of Pharmaceutical Education and Research, Ganpat University, Kherva-382711. Gujarat, India. geekhappy2002@yahoo.co.in
Madhabhai
M Patel
MP
D000268:Adhesiveness; D000282:Administration, Intravaginal; D000818:Animals; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D002220:Carbamazepine / Q000008:administration & dosage* / Q000493:pharmacokinetics; D016503:Drug Delivery Systems / Q000379:methods*; D004355:Drug Stability; D005079:Excipients / Q000737:chemistry; D005223:Fats / Q000737:chemistry*; D005260:Female; D008855:Microscopy, Electron, Scanning; D009092:Mucous Membrane / Q000737:chemistry; D009821:Oils / Q000737:chemistry*; D010570:Pessaries; D011092:Polyethylene Glycols / Q000737:chemistry*; D011205:Povidone / Q000737:chemistry; D011817:Rabbits; D012822:Silicon Dioxide / Q000737:chemistry; D013499:Surface Properties; D014885:Waxes / Q000737:chemistry
D005079:Excipients; D005223:Fats; D009821:Oils; D014885:Waxes; C104509:gelucire 44-14; C071184:Gelucire 50-13; C061199:Polyox WSR-N 60; D002220:Carbamazepine; D011092:Polyethylene Glycols; D012822:Silicon Dioxide; D011205:Povidone