Formulation of cores for the controlled release of glucose for prevention of hypoglycemia in diabetes patients

Ceska Slov Farm. 2014 Oct;63(5):206-12.

Abstract

Hypoglycemic episodes are a frequent and serious complication in both types of diabetes mellitus. The risk of hypoglycemic conditions can be managed by a coated pellet dosage form, which can release glucose in a delayed regime to achieve the maximum estimated effect of antidiabetics. The pellet cores, intended for coating with ethylcellulose, were prepared consisting of four osmotically active excipients: crosscarmellose (Ac-Di-Sol®), a mixture of microcrystalline cellulose and carmellose sodium (Avicel® RC 591), carboxymethyl starch sodium (Vivastar® P 5000) and macrogol 6000, respectively. The aim of this study was to increase the glucose content in the pellets to minimize their volume and to improve the administration to the patients. The content of glucose in the pellet cores was increased from 45 to 75 or 80%, respectively, for all compositions. All pellet samples had satisfactory mechanical and flow properties required for the coating process. The highest values of sphericity were achieved in the lower mean particle size sample containing 80% of glucose, 15% of Avicel® PH 101 and 5% of carboxymethyl starch sodium and the higher mean particle size sample containing 75% of glucose and 25% of Avicel® RC 591.

MeSH terms

  • Cellulose / analogs & derivatives
  • Cellulose / chemistry
  • Chemistry, Pharmaceutical / methods*
  • Delayed-Action Preparations
  • Diabetes Mellitus / physiopathology
  • Excipients / chemistry*
  • Glucose / administration & dosage*
  • Glucose / chemistry
  • Humans
  • Hypoglycemia / prevention & control*
  • Particle Size

Substances

  • Delayed-Action Preparations
  • Excipients
  • ethyl cellulose
  • Cellulose
  • Glucose