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KMID : 0369820150450010023
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Jorunal of Korean Pharmaceutical Sciences
2015 Volume.45 No. 1 p.23 ~ p.33
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Oral lipid based multiparticulate pastilles: design and effect of pore former
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Pandit Ashlesha P.
Divase Ganesh
Chavan Tushar
Khandelwal Kishanchandra
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Abstract
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The purpose of this research work was to design and develop droplet solidification apparatus for lipid based pastilles. Oral lipid based multiparticulate pastilles of solid lipid glycerol monostearate were formulated to control the release of highly water soluble drug metoprolol succinate. The apparatus was optimized at 14G needle size and metallic surface base plate cooled at 4 °C. Pastilles were evaluated for their size, shape, contact angle, density, flow properties, friability, crushing strength, drug content, thermal properties, in vitro and in vivo drug release. Pastilles were hemispherical in shape of size 3.1?4.3 mm. Contact angle was found to be more than 120°. Drug release was controlled for 8 h. Scanning electron microscopy study revealed the smooth external surface with pores to ingress dissolution media to enhance the drug release rate. Increased quantity of pore former enhanced the dissolution rate. Other operating variables like contact angle and height of needle from base plate were found to affect the size of pastilles. The dissolution of optimized batch of pastilles was best fitted to first order kinetic model. In vivo pharmacokinetic study showed correlation with in vitro drug release profile.
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KEYWORD
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Pastille, Pellet, Solid lipid glycerol monostearate, Pore former, Contact angle, Crushing strength
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