Formulation and Evaluaton of Floating Tablet of Cefpodoxime Proxetil
Abstract
Ideal once daily floating drug delivery system should release the drug for 24 hours and float up to 24 hrs. Once daily floating matrix tablet of Cefpodoxime proxetil should be release the drug for 24 hours to maintain the effective plasma level. All the formulations were prepared by using two different grades of HPMC (K100 and K4), cross povidone and MCC pH 101. HPMC is a matrix forming agent. All the formulations showed buoyancy lag time of less than 5 seconds regardless of concentration of HPMC K100 M, K4 and cross povidone. It may be due to the low density of tablet. The swelling index of HPMC K100 M was found to be higher than that of HPMC K4 M. This may be due to high molecular weight and high viscosity of HPMC K100 M. The formulation F1 containing low level of HPMC K100 M (75 mg) and low level of cross povidone (75 mg) showed higher burst release and maintained drug release up to 24 hours. The tablet was remained floated for 24 hours. High level of HPMC K100 M (F2, F3, F5,F6,) results in greater amount of gel being formed. This gel increases diffusion path length of the drug and hence release rate decreases. On the same line it formulation F5 and F8 should show relatively less drug release as high level of HPMC K100 M(100 mg & 125 mg respectively) is used in these formulations. But both the formulations released more than 97% drug within 24 hours. the formulations F10,F13,F14,F16,F17 released the drug within 20 hours. The formulation F11 which contains high amount of HPMC K4 M than F10 (100mg) and low level of cross povidone (75 mg) shows drug release up to 24 hours with sufficient floating duration. The formulation F15 and F18 contains high level of HPMC K4 M (125mg) and high level of cross povidone (100mg and 125mg) respectively. Both the formulations showed sustained drug release up to 24 hrs.
References
2. Alvisi V, Gasparetto A, Dentale A, Heras H, Felletti-Spadazzi A, Ambrosi AD. Bioavailability of a controlled release formulation of ursodeoxycholic acid in man. Drugs Exp Clin Res 1996;22:29-33.
3. Ponchel G, Irache JM. Specific and non-specific bioadhesive particulate systems for oral delivery to the gastrointestinal tract. Adv Drug Del Rev 1998;34:191-19.
4. Fix JA, Cargill R, Engle K. Controlled gastric emptying. III. Gastric residence time of a non disintegrating geometric shape in human volunteers. Pharm Res 1993;10:1087-89.
5. Davis SS, Stockwell AF, Taylor MJ, Hardy JG, Whalley DR, Wilson CG, Bechgaard H, Christensen FN, et al. The effect of density on the gastric emptying of single- and multiple-unit dosage forms. Pharm Res 1986;3:208-13.
6. Kawashima Y, Niwa T, Takeuchi H, Hino T, lto Y. Preparation of multiple unit hollow microspheres (microballons) with acrylic resin containing tranilast and their drug release characteristics (in vitro) and floating behavior (in vivo). J Control Rel 1991;16:279-90.
7. Hilton AK, Deasy PB. In vitro and in vivo evaluation of an oral sustained-release floating dosage form of amoxycillin trihydrate Int J Pharm 1992;86:79-88.
8. Sheth PR, Tossounian J. The hydrodynamically balanced system (HBS™): a novel drug delivery system for oral use. Drug Dev Ind Pharm 1984;10:313-39.
9. Sheth PR, Tossounian JL. Novel sustained release tablet formulations. US Patent 4,167,558.1979.
10. Ritschei WA, Menon A, Sakr A. Biopharmaceutic evaluation of furosemide as a potential candidate for a modified release peroral dosage form Methods Find. Exp. Clin Pharmacol 1991;13:629-36.
11. Ingani HM, Timmermans J, Moes AJ. Conception and in vivo investigation of peroral sustained release floating dosage forms with enhanced gastrointestinal transit. Int J Pharm 1987;35:157-64.
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