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Hypoglycemic effect of oral insulin in diabetic rabbits using pH-dependent coated capsules containing sodium salicylate without and with sodium cholate.

Abstract
The hypoglycemic effect of oral insulin (20 U and 40 U) capsules coated with a pH-dependent soluble polymer (Eudragit S100) and containing sodium salicylate (50 mg) without and with sodium cholate (50 mg) was studied in alloxan-hyperglycemic rabbits and compared with that of s.c. insulin injection (20 U). The capsules containing 20 U insulin + sodium salicylate (50 mg) produced a significant reduction in plasma glucose level to 82 and 73% of initial values at 2 and 3 hr after administration, respectively. The blood glucose level slowly returned to normal values at 5 hr. The AUC0-5 hr was 73.7 +/- 43.5 mg.hr/dl compared to 242 +/- 70.5 mg.hr/dl for insulin (20 U, s.c.) with a relative hypoglycemia of 30.4%. A higher dose of oral insulin (40 U) + sodium salicylate (50 mg) was more effective in reducing plasma glucose level which steadily decreased and reached 56% of the initial value by 5 hr (AUC0-5 hr = 132 +/- 41.5 mg.hr/dl and relative hypoglycemia = 27.3%). Sodium cholate (50 mg), however, slightly improved sodium salicylate effect producing an AUC0-5 hr of 139 +/- 37.3 mg.hr/dl with relative hypoglycemia of 28.7%. The relative hypoglycemia of pH-dependent coated capsules reached in the present experiment is the highest found so far.
AuthorsE A Hosny, N M Ghilzai, T A al-Najar, M M Elmazar
JournalDrug development and industrial pharmacy (Drug Dev Ind Pharm) Vol. 24 Issue 3 Pg. 307-11 (Mar 1998) ISSN: 0363-9045 [Print] England
PMID9876590 (Publication Type: Journal Article)
Chemical References
  • Blood Glucose
  • Capsules
  • Delayed-Action Preparations
  • Excipients
  • Hypoglycemic Agents
  • Insulin
  • Sodium Cholate
  • Sodium Salicylate
Topics
  • Animals
  • Area Under Curve
  • Blood Glucose (metabolism)
  • Capsules
  • Delayed-Action Preparations
  • Diabetes Mellitus, Experimental (blood, drug therapy)
  • Excipients
  • Hydrogen-Ion Concentration
  • Hypoglycemic Agents (administration & dosage, pharmacokinetics, therapeutic use)
  • Injections, Subcutaneous
  • Insulin (administration & dosage, pharmacokinetics, therapeutic use)
  • Male
  • Rabbits
  • Sodium Cholate
  • Sodium Salicylate

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