• Journal of the Korea Academia-Industrial cooperation Society
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• v.11 no.7
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• pp.2451-2458
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• 2010

We prepared sustained release matrix system which contains carvedilol with Compritol 888 ATO used as lipophilic sustained release excipient and hydroxypropyl methyl cellulose (HPMC) or polyethylene oxide (PEO) used as hydrophilic sustained release polymer. Wet granulation compressed method was used for preparing carvedilol sustained release matrix tablets. When carvedilol sustained release matrix tablets were prepared, we evaluated the drug release kinetics which is affected by Compritol 888 ATO ratio, a kind of hydrophilic polymer (HPMC, PEO) and hot melt coating coagglutination (HMCC) process was done. The drug release kinetics was measured for 24 hours in pH 1.2 simulated gastric fluid and pH 6.8 simulated intestinal fluid, using a dissolution tester at $37.5^{\circ}C$ in 50 rpm. Dissolution rate of controlled release matrix tablets of carvedilol was evaluated by paddle method. We confirmed that HMCC process was very effective to controlled release of drugs. The rate of Compritol 888 ATO, as a lipidic material, can control the drug release pattern about the elution rate of 95% and 24 hours delay than that of the normal tablet.

• Journal of Pharmaceutical Investigation
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• v.40 no.5
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• pp.313-319
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• 2010

The objectives of this study were to evaluate the effect of formulation ingredients on the drug release and to optimize the novel sustained release matrix tablet formulations of bupropion hydrochloride. A three factor, three-level Box-Behnken design was used for the optimization procedure, with the amounts of PEO ($X_1$), citric acid ($X_2$) and Compritol 888 ATO ($X_3$) as the independent variables. The selected dependent variables were the cumulative percentage values of bupropion hydrochloride that had dissolved after 1, 4 and 8 hr. Various dissolution profiles of the drug from sustained release matrix tablets were obtained. Optimization was performed for $X_1$, $X_2$ and $X_3$ using the following target ranges; $30%{\leq}Y_1{\leq}45%$; $70{\leq}Y_2{\leq}85%$; $85%{\leq}Y_3{\leq}100%$. The optimized formulation for bupropion hydrochloride was achieved with 12.5% PEO ($X_1$), 2.5% citric acid ($X_2$) and 10% Compritol 888 ATO ($X_3$). The sustained release matrix tablets with the optimized formulation provided a release profile that was close to predicted values. In addition, the dissolution profiles of the sustained release matrix tablet with the optimized formulation were similar to those of the commercial product Wellbutrin$^{(R)}$ SR tablets ($f_2$=79.83).

• Journal of Pharmaceutical Investigation
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• v.40 no.6
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• pp.373-378
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• 2010

In order to develop a topical preparation which has a high occlusive property with skin moisturization, nano-structured lipid carrier (NLC) systems along with solid lipid nanoparticle (SLN) were designed. Various NLC dispersions were successfully formulated with Compritol 888 ATO as a solid lipid, Labrafil M 1944 CS as an oil, and Tween 80 as a surfactant. The increase of oil content (5 to 50%) led to the decrease in the occlusion factor in the order of SLN > NLC-5 > NLC-15 = NLC-30 > NLC-50. Particle size of lipid particulates was in the range of 100 to 160 nm. NLC-based carbogels were prepared by the employment of humectants such as urea, glycerin, and Tinocare GL to carbomer gel. NLC-30 gel formulations containing 4 or 8 % of lipid particles showed improved occlusive effect in vitro, compared to NLC-free gel base. Even though NLC-free gel base revealed comparable occlusion effect by itself, the occlusion factor of 4 % NLC-30 gel was about 2-fold higher than that of NLC-free gel base.