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Abstract
Paliperidone is a SR (5-HT2) receptor antagonist and D2DR inhibitor was BCS class II drug with low water solubility and the absolute oral bioavailability of Paliperidone following Paliperidone administration is 28%. So, it is essential to improve the solubility to enhance its bioavailability. Nanosuspension technique is a modern and a more innovative approach used widely to increase the solubility of the drug moieties. Nanosuspension of Paliperidone by solvent evaporation method using various polymers such as SLS, Pluronic F127, PVP-K90, PVA, and methanol. IR spectroscopic studies indicated that there are no drug-excepient interactions. All the prepared formulations were found to be having drug content within acceptable limits in the range of 79.26 to 97.52 % and Entrapment efficiency was found to be in the range of 82.16%-96.20% respectively. From the in vitro dissolution studies by comparing to other all the formulations F9 is the best formulation which showed 99.86% of drug released respectively within 60 min and follows Zero order release kinetics.
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References
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References
1. Chen J, Park H, Park K. Synthesis of superporous hydrogels: hydrogels with fast swelling and superabsorbent properties. J.Biomed.Mater.Res.1999; 44(1):53-62.
2. Jun Chen, William E. Blevins, Haesun Park, Kinam Park , Gastric retention properties of superporous hydrogel composites. J.Cont.release.2000; 64:39-51.
3. Chingunpituk, J., Nanosuspension technology for drug delivery. Walailak Journal of science and technology. 2007; 4:139–153.
4. Pouton, C. W. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and ‘self-micro emulsifying’ drug delivery systems. European Journal of Pharmaceutical Sciences. 2000; 11:S93–S98.
5. Varshosaz J, Talari R, Mostafavi SA, Nokhodchi A. Dissolution enhancement of gliclazide using in situ micronization by solvent change method. Powder Technology. 2008; 187:222–230.
6. Pahala S, Joan MA, Samuel HY. Solubilization of rapamycin. International Journal of Pharmaceutics and biopharmaceutics.2001; 213: 25–29.
7. Wong S.M, Kellaway I.W, Murdan S. Enhancement of the dissolution rate and oral absorption of a poorly water soluble drug by formation of surfactant containing micro particles. International Journal of Pharmaceutics. 2006; 317: 61-68.
8. Parikh R.K.,Manusun SN.S.,Gohel M.C. and Soniwala M.M. Dissolution enhancement of Nimesulide using complexation and salt formation techniques. Indian drugs. 2005; 42(3):149-154.