Background:The osmotic drug delivery systems suitable for oral administration typically consist of a compressed tablet core that is coated with a semipermeable membrane that has an orifice drilled on it by means of a laser beam or mechanical drill. Ketorolac is a nonsteroidal agent with powerful analgesic. Oral bioavailability of ketorolac was reported to be 90% with very low hepatic first-pass elimination; the biological half-life of 4-6 hours requires frequent administration to maintain the therapeutic effect.Aim:The aim of the current study was to design a controlled porosity osmotic pump (CPOP)based drug delivery system for controlled release of an NSAID agent, ketorolac tromethamine, which is expected to improve patient compliance due to reduced frequency; it also eliminates the need for complicated and expensive laser drilling and maintain continuous therapeutic concentration.Design:The CPOP was designed containing pore-forming water-soluble additives in the coating membrane, which after coming in contact with water, dissolve, resulting in an in situ formation of a micro porous structure.Materials and Methods:The effect of different formulation variables, namely level of pore former (PVP), plasticizer (dibutyl phthalate) in the membrane, and membrane weight gain were studied.Results and Conclusion:Drug release was inversely proportional to the membrane weight but directly related to the initial concentration of pore former (PVP) in the membrane. Drug release was independent of pH and agitational intensity, but dependent on the osmotic pressure of the release media. Based on the in vitro dissolution profile, formulation F3C1 (containing 0.5 g PVP and 1 g dibutyl phthalate in coating membrane) exhibited Peppas kinetic with Fickian diffusion-controlled release mechanism with a drug release of 93.67% in 12 hours and hence it was selected as optimized formulation. SEM studies showed the formation of pores in the membrane. The formulations were stable after 3 months of accelerated stability studies. CPOP was designed for effective administration of drugs for prolonged period of time.
The aim of this investigation was to develop gastroretentive mucoadhesive tablets of cephalexin, which will retain in the stomach for 10 h. Cephalexin, a first-generation cephalosporin, becomes ionized in intestinal pH because pKa is 4.5 and thus reducing its bioavailability. The various batches were prepared by wet granulation method using variety of mucoadhesive polymers such as hydroxyl propyl methyl cellulose K4M, hydroxyl propyl cellulose, chitosan, carbopol 934P and sodium carboxymethylcellulose and subjected to various evaluation parameters such as mucoadhesive strength, in vitro drug release profile, swelling characteristics and physical properties. It was evident from the study that the formulation containing HPMC K4M and carbopol 934P in combination exhibited maximum mucoadhesive strength of 144.42 gms, in vitro residence time was 8.73 h and in vitro drug release was found to be 75.03% in 10 h with non-Fickian diffusion mechanism. So, the optimized formulation F(2) was further subjected to in vivo retention time in rabbit by X-ray technique, SEM and Accelerated stability studies. Regarding all the properties evaluated, the formulation containing HPMC K4M and carbopol 934P in combination was found to be the best to achieve the aim of this study.
Aim of the present work is to develop non-chewable antacid tablets using different disintegrating agents viz., microcrystalline cellulose, sodium starch glycolate (Primogel®), and cross-linked sodium carboxymethylcellulose (cros-car-mellose sodium®). These agents were used alone, and in combinations, both 50% intra-granularly, and 50% extra-granularly. To cover all these variables in the formulations, seven different formulations were designed. Use of different disintegrating agents have shown varying effect on disintegration time and pattern. The disintegration time for formulation I and III did not comply with the official disintegration test in distilled water, as well as in simulated gastric fluid. All formulations, except formulation I and III, showed nearly equivalent to 30 min of Rosset-Rice time for neutralization. The graphical representation shows that when the base is available in full strength, it neutralizes the acid at a faster rate, and then the amount of base goes on reducing progressively, resulting in decrease in the rate of neutralization. Based on't' values, formulation II and VI show that the theoretical acid-consuming capacity, and the observed acid-consuming capacity values are almost equal.
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