DOI QR코드

DOI QR Code

Preparation and Evaluation of Solid Composites Containing Choline Alphoscerate

  • Kim, Hoon (Department of Pharmaceutics & Biotechnology, Konyang University) ;
  • Cho, Seong-Wan (Department of Pharmaceutics & Biotechnology, Konyang University)
  • Received : 2019.02.21
  • Accepted : 2019.04.15
  • Published : 2019.06.30

Abstract

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.

Keywords

References

  1. Barbagallo SG, Barbagallo M, Giordano M, Meli M, Panzarasa R. Alpha-Glycerophosphocholine in the mental recovery of cerebral ischemic attacks. An Italian multicenter clinical trial. Ann NY Acad Sci. 1994. 717: 253-269. https://doi.org/10.1111/j.1749-6632.1994.tb12095.x
  2. Cummings JL, Benson F. Subcortical dementia: Review of an emerging concept. Arch Neurol. 1984. 41: 874-879. https://doi.org/10.1001/archneur.1984.04050190080019
  3. Doggrell SA, Evans S. Treatment of dementia with neurotransmission modulation. Expert Opin Investig Drugs. 2003. 12: 1633-1654. https://doi.org/10.1517/13543784.12.10.1633
  4. Fossati T, Colombo M, Castiglioni C, Abbiati G. Determination of plasma choline by high-performance liquid chromatography with a postcolumn enzyme reactor and electrochemical detection. J Chromatogr B Biomed Appl. 1994. 656: 59-64. https://doi.org/10.1016/0378-4347(94)00070-0
  5. Gatti G, Barzaghi N, Acuto G, Fossati T, Perucca E, Abbiatti G. A comparative study of free plasma choline levels following intramuscular administration of L-${\alpha}$-glycerylphosphorylcholine and citicoline in normal volunteers. Int J Clin Pharmacol Ther. 1992. 30: 331-335.
  6. Grossman H, Bergmann C, Parker S. Dementia: A brief review. Mt Sinai J Med. 2006. 73: 985-992.
  7. Kidd PM. Alzheimer's disease, amnestic mild cognitive impairment, and age-associated memory impairment: current understanding and progress toward integrative prevention. Altern Med Rev. 2008. 13: 85-115.
  8. Majahabulin S. Enzymatic synthesis of sugar fatty acid esters in organic solvent and in supercritical carbon dioxide and their antimicrobial activity. J Supercrit Fluids. 2008. 45: 338-345. https://doi.org/10.1016/j.supflu.2008.01.002
  9. Moreno DJ. Cognitive improvement in mild to moderate Alzheimer's dementia after treatment with the acetylcholine precursor choline alfoscerate: a multicenter, double-blind, randomized, placebo-controlled trial. Clin. Ther. 2003. 25: 178-193. https://doi.org/10.1016/S0149-2918(03)90023-3
  10. Parnetti L, Mignini F, Tomassoni D, Traini E, Amenta F. Cholinergic precursors in the treatment of cognitive impairment of vascular origin: ineffective approaches or need for re-evaluation. J Neurol Sci. 2007. 257: 264-269. https://doi.org/10.1016/j.jns.2007.01.043
  11. Park SY, Choi SU, Lee KH, Yang JB, Cho, SW, Ro JE, Kim HG, Khadka P, Lee JH, Cho CW. Discriminative measurement and pharmacokinetic evaluation of choline alphoscerate against endogenous choline in human. Bull Korean Chem Soc. 2015. 36: 2089-2094. https://doi.org/10.1002/bkcs.10409
  12. Sheard NF, Tayek JA, Bistrian BR, Blackburn GL, Zeisel SH. Plasma choline concentration in humans fed parenterally. Am J Clin Nutr. 1986. 43: 219-224. https://doi.org/10.1093/ajcn/43.2.219
  13. Sheard NF, Zeisel SH. An in vitro study of choline uptake by intestine from neonatal and adult rats. Pediatr Res. 1986. 20: 768-72. https://doi.org/10.1203/00006450-198608000-00014
  14. Trainia E, Bramantib V, Amenta F. Choline alphoscerate (alphaglyceryl-phosphoryl-choline) an old choline-containing phospholipid with a still interesting profile as cognition enhancing agent. Curr Alzheimer Res. 2013. 10: 1070-1079. https://doi.org/10.2174/15672050113106660173