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Oral lipid based multiparticulate pastilles: design and effect of pore former
Ashlesha P. Pandit,Ganesh Divase,Tushar Chavan,Kishanchandra Khandelwal 한국약제학회 2015 Journal of Pharmaceutical Investigation Vol.45 No.1
The purpose of this research work was todesign and develop droplet solidification apparatus for lipidbased pastilles. Oral lipid based multiparticulate pastillesof solid lipid glycerol monostearate were formulated tocontrol the release of highly water soluble drug metoprololsuccinate. The apparatus was optimized at 14G needle sizeand metallic surface base plate cooled at 4 ˚C. Pastilleswere evaluated for their size, shape, contact angle, density,flow properties, friability, crushing strength, drug content,thermal properties, in vitro and in vivo drug release. Pastilleswere hemispherical in shape of size 3.1–4.3 mm. Contact angle was found to be more than 120˚. Drugrelease was controlled for 8 h. Scanning electron microscopystudy revealed the smooth external surface with poresto ingress dissolution media to enhance the drug releaserate. Increased quantity of pore former enhanced the dissolutionrate. Other operating variables like contact angleand height of needle from base plate were found to affectthe size of pastilles. The dissolution of optimized batch ofpastilles was best fitted to first order kinetic model. In vivopharmacokinetic study showed correlation with in vitrodrug release profile.
Ashlesha P. Pandit,Tushar T. Chavan,Kishanchandra R. Khandelwal 한국약제학회 2015 Journal of Pharmaceutical Investigation Vol.45 No.6
The objective of present investigation was to enhance solubility, dissolution rate and bioavailability of poorly water soluble drug atorvastatin using solid lipid glycerol monostearate and surfactant poloxamer-407. Oral pastilles of glycerol monostearate and poloxamer were formulated by pastillation technique and optimized by central composite design. Hemispherical pastilles were evaluated for drug content, saturation solubility study, thermal properties and in vitro, ex vivo and in vivo drug release study. Formulation F4 at high level of glycerol monostearate (1000 mg) and poloxamer-407 (400 mg) showed 25-fold and 3-fold increased in solubility and dissolution rate, respectively. X-Ray diffraction and scanning electron microscopic study proved the decrease in crystallinity of atorvastatin and confirmed the conversion of crystalline to amorphous form, respectively. Ex vivo study revealed that maximum amount of released drug was absorbed through the everted intestine. In vivo study in rats showed higher HMG CoA to mevalonate ratio of pastilles than plain drug. This indicated better bioavailability and hyperlipidemic activity of pastilles than atorvastatin. Thus, the solubility, dissolution rate and bioavailability of atorvastatin were enhanced successfully using lipid carrier system.
Vinita C. Patole,Ashlesha P. Pandit 한국약제학회 2018 Journal of Pharmaceutical Investigation Vol.48 No.3
An attempt was made to formulate mesalamineloaded alginate microspheres by emulsion cross linking method for local treatment of ulcerative colitis. Microspheres were filled in HPMC capsules enteric coated with Eudragit FS-30D. The effect of process variables like drug-alginate concentration ratio and emulsifier concentration was optimized. Microspheres were evaluated for particle size, shape and entrapment efficiency. Spherical shaped microspheres were confirmed by scanning electron microscopy. In vitro drug release study showed a burst drug release pattern in the initial hour necessitating encapsulation of alginate microspheres. In vivo study in rats performed by colonic inflammatory lesions demonstrated remarkable reduction in ulcer index treated with microspheres. Histopathological study confirmed no signs of ulceration or bleeding. Microspheres (drug:alginate concentration, 1:1) was then filled in HPMC capsule shells, enteric coated with Eudragit FS 30D to gain 30 mg weight. Due to solubility of Eudragit FS30D above pH 7, an encapsulated system released alginate microspheres at colon region. Capsules with weight gain of 30 mg coating polymer (B3) resisted the drug release at intestinal region for about 6 h with 10% drug release. In vitro drug release of formulation B3 showed 64.89 and 90.52% drug release within 10 h, in phosphate buffer pH 7.4 and in presence of rat faecal content in simulated colonic fluid, respectively. The later rapid drug release was due to action of colonic microflora at alginate microspheres. Therefore, mesalamine-loaded alginate microspheres enteric coated in HPMC capsules can be potential delivery system for local treatment of ulcerative colitis.