• Archives of Pharmacal Research
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• 제29권10호
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• pp.921-927
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• 2006

Prolonged release micro particles of clarithromycin (CL) were prepared using Eudragit RL 100 and RS 100 by spray-drying and casting-drying techniques. For the characterization of those microparticles, preparation yield, particle size distribution, X-ray diffraction, thermal behavior, active agent content and in vitro dissolution from the microparticles were performed. HPLC was used for the assay of clarithromycin and the assay method was validated. All the formulations obtained showed prolonged release when compared to pure clarithromycin. Microparticles prepared by spray-drying method had a slower release compared to those of casting drying method. Spray-drying method seems to be a more suitable method to prepare microparticles for prolongation in release.

• Journal of Pharmaceutical Investigation
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• 제37권3호
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• pp.193-196
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• 2007

This study aimed to evaluate and develop $Eudragit^{(R)}$-coated pellets based on the dissolution using the paddle method. As coating materials, two types of $Eudragit^{(R)}$ were applied to obtain either sustained release form or fast released form. The dissolution test was carried out in phosphate buffer solution (pH 6.5) at $37^{\circ}C$, 100 rpm. In order to develop a sustained release preparation containing felodipine, a comparative dissolution study was done using commercial product as a control. The dissolution at 30 min of felodipine from $Eudragit^{(R)}$ RS or RL-coated pellets were 0.96% and 99.65, respectively. The weight ratio of $Eudragit^{(R)}$ RL pellets to RS pellets altered the dissolution rate, but did not optimize the dissolution rate. However, the sustained dissolution of felodipine from pellets was optimized by varying the coating ratios of $Eudragit^{(R)}$ RS. It is suggested that the coating ratio of pellets is the main factor which controls dissolution rate. Taken together, $Eudragit^{(R)}$ RS 30D-coated pellets showed the most comparable dissolution rate pattern to commercial product, $Splendil^{(R)}$. This sustained release pellets for oral delivery system of felodipine was simply manufactured, and drug release behavior was highly reproducible.

• Archives of Pharmacal Research
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• 제26권7호
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• pp.569-574
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• 2003

Controlled-release amitriptyline pellets (ATP) were formulated and its oral bioavailability was assessed in human volunteers after oral administration under fasting conditions. Core pellets were prepared using a CF granulator by two different methods (powder layering and solvent spraying) and coated with Eudragit RS or RL 100. Physical characteristics and dissolution rates of core pellets and coated pellets were evaluated to optimize the formulation. Powder layering method resulted in a better surface morphology than solvent spraying method. However, physical properties of the products were poorer when prepared by powder layering method with respect to hardness, friability and density. The dissolution profile of amitriptyline coated with Eudragit RS 100 was comparable to that of commercially available amitriptyline enteric-coated pellets ($Saroten^{\circledR}$ retard). After the oral administration of both products at the dose of 50 mg, the mean maximum concentrations ($C_{max}$) were 36.4 and 29.7 ng/mL, and the mean areas under the concentration-time curve ($AUC_{0-96}$) were 1180.2 and 1010.7 ng.h/mL for ATP and Saroten retard, respectively. The time to reach the maximum concentrations ($T_{max}$) was 6 h for both formulations. Statistical evaluation suggested that ATP was bioequivalent to Saroten retard.