• Biomedical Science Letters
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• v.25 no.2
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• pp.170-176
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• 2019

The objective of this study was to evaluate the characteristics of the mixtures of choline alphoscerate (alpha-glycerylphosphorylcholine, alpha-GPC), in the liquid form, and sucrose ester, which formed a solid composite. The choline alphoscerate solid composites were prepared using different ratios of sucrose ester, and different preparation methods, such as air drying and rotary evaporation, were compared for their preparation efficacy. We examined the characteristics of the solid composites by using scanning electron microscopy (SEM), angle of repose, and moisture content. The ideal mixing ratio of choline alphoscerate and sucrose ester was determined as 1:3 and air drying was found to be more suitable for the preparation of solid composites than rotary evaporation. SEM measurements of the degree of dispersion and the size of particles indicated that a high-temperature air method was more suitable. These results demonstrated the successful preparation of choline alphoscerate solid composites that have potential for industrial use.

• Journal of the Korea Academia-Industrial cooperation Society
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• v.14 no.12
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• pp.6324-6329
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• 2013

The aim of this study was to prepare and evaluate tablets containing liquid choline alphoscerate, which is capable of being formulated as a solid dosage form by the adsorption of magnesium aluminum silicate. The tablets were prepared with various absorbent to choine alphoscerate ratios. The physical properties and the dissolution rate were investigated. Considering the tabletting and dissolution rate, the formula scontaining 50-75% absorbent were adequate in the tested formulations. The 62.5% absorbent formula showed superior results with the tests of hardness, friability, disintegration time, and the ratio of dissolution area under the curve. Overall, magnesium aluminum silicate can be an alternative additive to a liquid drug.

• Journal of Pharmaceutical Investigation
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• v.40 no.2
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• pp.109-115
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• 2010

The purpose of the present study was to evaluate the bioequivalence of two choline alphoscerate soft capsules, Gliatilin soft capsule (Daewoong Pharmaceuticals Co., Ltd.) and Cholicerin soft capsule (Sam Chun Dang Pharm. Co., Ltd.), according to the guidelines of Korea Food and Drug Administration (KFDA). Serum concentrations of choline after oral administration of choline alphoscerate were determined using a validated LC/MS/MS method. This method showed linear response over the concentration range of 0.5-20 ${\mu}g$/mL with correlation coefficient of 0.9999. The lower limit of quantitation using 100 ${\mu}L$ of serum was 0.5 ${\mu}g$/mL which was sensitive enough for pharmacokinetic studies. Thirty six healthy male Korean volunteers received each medicine at the choline alphoscerate dose of 1200 mg in a $2{\times}2$ crossover study. There was a one-week washout period between the doses. Blood samples were taken at predetermined time intervals up to 8 hr. $AUC_t$ (the area under the serum concentration-time curve from time 0 to 8 hr) was calculated by the linear trapezoidal rule method. $C_{max}$ (the maximum serum drug concentration) and $T_{max}$ (the time to reach $C_{max}$) were compiled from the serum concentration-time data. Analysis of variance was carried out using logarithmically transformed $AUC_t$ and $C_{max}$. No significant sequence effect was found for all of the bioavailability parameters, indicating that the crossover design was properly performed. The 90% confidence intervals of the $AUC_t$ ratio and the $C_{max}$ ratio for Cholicerin/Gliatilin were log0.9998-log1.1172 and log0.9938-1.0944, respectively. These values were within the acceptable bioequivalence intervals of log0.80-log1.25. Thus, the criteria of the KFDA guidelines for the bioequivalence was satisfied, indicating Cholicerin soft capsule and Gliatilin soft capsule are bioequivalent.