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Effect of bioadhesive polymers, sodium salicylate, polyoxyethylene-9-lauryl ether, and method of preparation on the relative hypoglycemia produced by insulin enteric-coated capsules in diabetic beagle dogs.

Abstract
The hypoglycemic effect of oral insulin capsules coated with pH-dependent Eudragit S100 and containing various absorption promoters was studied in hyperglycemic beagle dogs. The absorption enhancers used were bioadhesive polymers, sodium salicylate, and non-ionic surfactants. A comparative study of the bioadhesive polymers, polycarbophil (PC), hydroxypropyl methylcellulose (HPMC), and carbopol 934 in insulin-coated capsules revealed no significant difference between the insulin capsules containing these polymers, giving relative hypoglycemia (RH) values ranging from 4.3 +/- 2.3% to 6.5 +/- 5.1%. It was also found that the method of preparation of the mixture of the bioadhesive polymer with insulin either by physical mixing or freeze-drying did not affect the RH values obtained. Sodium salicylate, when used in insulin enteric-coated capsules (50 mg) mixed with insulin as a physical mixture, or prepared by wet granulation using 10% polyvinyl pyrollidone (PVP), or by freeze-drying, produced RH values ranging from 7.3 +/- 2.9% to 9.4 +/- 3.7%. When sodium salicylate (100 mg) was used with insulin in freeze-dried granules an RH value of 10 +/- 2.6% was produced. As the dose of insulin increased from 6 to 9 U/kg, the area under curve (AUC) of the enteric-coated capsules containing 50 mg sodium salicylate increased from 73.2 +/- 27.8% to 121.4 +/- 102.7% reduction, but the RH did not change significantly. Insulin capsules containing polyoxyethylene-9-lauryl ether (POELE) used in its optimum concentration (2%), found in these experiments, produced RH of 9.5 +/- 6.8% when prepared as granules by wetting with a few drops of absolute alcohol in the presence of PC (50 mg). Insulin capsules containing lower (1%) or higher (3%) concentrations of POELE and prepared with PC, 50 mg by wet granulation produced lower RH of about 6%. The enteric-coated oral insulin capsules containing insulin (6 or 9 U/kg) and sodium salicylate (50 mg) as an absorption promoter, together with the bioadhesive polymer polycarbophil (50 mg), and prepared either by wet granulation using ethanol or by freeze-drying, are the best formulations to be used. They achieved a reduction in plasma glucose levels of about 25-30% and RH of about 10%. Also insulin (9 U/kg) capsules containing 2% POELE produced a 28% reduction in plasma glucose levels and RH of 9.6 +/- 6.8%.
AuthorsE A Hosny, H I al-Shora, M M A Elmazar
JournalDrug development and industrial pharmacy (Drug Dev Ind Pharm) Vol. 28 Issue 5 Pg. 563-70 (May 2002) ISSN: 0363-9045 [Print] England
PMID12098845 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Acrylates
  • Acrylic Resins
  • Adjuvants, Pharmaceutic
  • Blood Glucose
  • Capsules
  • Drug Carriers
  • Hypoglycemic Agents
  • Insulin
  • Tablets, Enteric-Coated
  • Polidocanol
  • Hypromellose Derivatives
  • Polyethylene Glycols
  • calcium polycarbophil
  • Methylcellulose
  • carbopol 934P
  • Sodium Salicylate
Topics
  • Acrylates (chemistry)
  • Acrylic Resins (chemistry)
  • Adjuvants, Pharmaceutic
  • Administration, Oral
  • Animals
  • Blood Glucose (metabolism)
  • Capsules
  • Diabetes Mellitus, Experimental (blood)
  • Dogs
  • Drug Carriers
  • Drug Compounding
  • Hypoglycemic Agents (administration & dosage, pharmacology)
  • Hypromellose Derivatives
  • Injections, Subcutaneous
  • Insulin (administration & dosage, pharmacology)
  • Male
  • Methylcellulose (analogs & derivatives, chemistry)
  • Polidocanol
  • Polyethylene Glycols (chemistry)
  • Sodium Salicylate (chemistry)
  • Tablets, Enteric-Coated

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