GASTRORETENTIVE NIZATIDINE LOADING MICROBALLOONS FOR TREATMENT OF PEPTIC ULCER
Keywords:
Microballoons, Gastro retentive system, Nizatidine, BuoyancyAbstract
Objective: The aim of the present work was to formulate a controlled release dosage form of water soluble drug such as Nizatidine to increase its gastric retention in the stomach and consequently, enhance its absorption and improve its bioavailability.
Methods: Microballoons were prepared by emulsion non solvent evaporation method using ethyl cellulose 7 CP in different ratios. The prepared microballoons were evaluated for yield percentage, entrapment efficiency, in vitro buoyancy and in vitro dissolution.
Results: Results showed that as drug to polymer ratio increased from 1:1 to 1:5 yield percentage, entrapment efficiency, in vitro buoyancy increased from 70.4+1.5 to87.2+1.8, from 71.5+2.1 to 90.2+2.6 and from 82.1+3.2 to 93.2+2.6, respectively, while the amount of drug released decreased from 88.1+2.1 to 68.9+1.8. When stirring rate increased from 800 rpm to 1600 rpm, the three parameters decreased from 93.2+2.7 to 81.5, from 96.4+3.5 to 82.6+1.7 and from 97+5.4 to 88.2+4.1, respectively, while the amount released increased from 63.1+2.6 to 73.8+1.2. When Span 80 concentrations increased from 0.1% to 2% the three parameters decreased from 95.2+2.6, to 81.6+3.2, from 97.6+1.8 to 82.4+1.8 and from 97.3+5.2 to 89.1+4.6, respectively, and the amount released percentage increased from 61.2+2.6 to 76.1+1.6. All drug release showed Higuchi diffusion models. The increase in the mean Tmax and the decrease in the mean Cmax of microballoons compared to the plain drug indicate a sustained release of microballoons and reflects a high improvement in its bioavailability.
Conclusion: It is evident from this study that microballoons are promising gastric prolonging the delivery system for nizatidine and have good stability.
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References
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