Preparation and Characterization of the Biological Compound Effervescent Granule of Calcium Acetate

Curr Pharm Biotechnol. 2019;20(11):934-944. doi: 10.2174/1389201020666190628144637.

Abstract

Objective: Calcium acetate (Ca(CH3COO)2) is commonly used in calcium supplement for medicine, which is used as an auxiliary agent to treat osteoporosis. An effervescent granule is widely used in medical industry due to its palatability. The purpose of this study is to develop a new preparation of compound effervescent granule of the biological calcium acetate (Ca(CH3COO)2 effervescent granule), overcoming the disadvantages of the previous other dosage forms of calcium and thus enhancing the therapeutic efficacy.

Methods: The biological Ca(CH3COO)2 effervescent granule was prepared by the wet granulation method. The formulation was optimized by the orthogonal experiment. The effervescent base was comprised of various amounts of citric acid and sodium bicarbonate. Other ingredients were added for optimal performance of effervescent granule. The performed Ca(CH3COO)2 effervescent granule was evaluated for the particle size, repose angle, pH value of solution, calcium acetate content and effervescence time. The in vivo effects of Ca(CH3COO)2 effervescent granule on the bone microarchitecture were investigated via Micro-CT detection, and the serum calcium level was also investigated.

Results: The optimized formulation of the biological Ca(CH3COO)2 effervescent granules was composed of calcium acetate, citric acid, sodium bicarbonate, PEG6000, aspartame, PVP ethanol solution, lactose and vitamin D. Our findings reveal that this biological Ca(CH3COO)2 effervescent granule exhibited prominent effect on preventing the bone-mass loss and did better in enhancing the bone microarchitecture compared to the other calcium preparations.

Conclusion: The biological Ca(CH3COO)2 effervescent granule is a novel dosage form among so many kinds of calcium preparations. It may perform better functions in the dairy calcium supplement.

Keywords: Calcium acetate; blood calcium; bone mineral density; effervescent granules; micro-CT; orthogonal optimization..

MeSH terms

  • Acetates / chemistry*
  • Biological Availability
  • Calcium Compounds / chemistry
  • Citric Acid / chemistry
  • Dietary Supplements*
  • Dosage Forms
  • Drug Compounding / methods*
  • Particle Size
  • Polyethylene Glycols / chemistry
  • Sodium Bicarbonate / chemistry

Substances

  • Acetates
  • Calcium Compounds
  • Dosage Forms
  • Citric Acid
  • Polyethylene Glycol 6000
  • Polyethylene Glycols
  • Sodium Bicarbonate
  • calcium acetate