• 대한의생명과학회지
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• 제25권2호
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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.

• 한국산학기술학회논문지
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• 제14권12호
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• pp.6324-6329
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• 2013

본 연구에서는 액상 형태인 콜린알포세레이트를 알루미늄마그네슘규산화합물에 흡착시켜 고형의 제형화가 가능한 콜린알포세레이트를 함유하는 정제의 제조하고 평가하였다. 정제는 콜린알포세레이트 대비 흡착제의 비율을 달리하여 제조하고, 물리적 특성 및 용출률을 조사하였다. 정제의 타정성과 용출률을 고려할 때 흡착제는 주성분 대비 50~75%가 적절하였다. 주성분 대비 62.5%의 흡착제를 사용한 제제에서 정제의 경도, 붕해, 마손도 시험, 용출곡선하면적 비율 결과가 가장 우수하였다. 알루미늄마스네슘규산화합물은 액상 약물의 고형화 설계 시 좋은 소재가 될 수 있을 것이다.

• Journal of Pharmaceutical Investigation
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• 제40권2호
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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.