The effect of pH on the in-vitro dissolution of three second-generation sulphonylurea preparations: mechanism of antacid-sulphonylurea interaction
| Autor: | Pertti J. Neuvonen, Pasi Lehto, Kari T. K. Ivistö, Kari Laine |
|---|---|
| Rok vydání: | 1996 |
| Předmět: |
Sodium
medicine.medical_treatment Pharmaceutical Science chemistry.chemical_element Pharmacology 030226 pharmacology & pharmacy Dosage form Glibenclamide 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Antacid Glyburide medicine Hypoglycemic Agents Solubility Sodium bicarbonate Chemistry Magnesium Hydrogen-Ion Concentration 030220 oncology & carcinogenesis Antacids Glipizide Nuclear chemistry medicine.drug Tablets |
| Zdroj: | The Journal of pharmacy and pharmacology. 48(9) |
| ISSN: | 0022-3573 |
| Popis: | Simultaneously administered magnesium hydroxide or sodium bicarbonate can increase the rate and extent of absorption of non-micronized glibenclamide and glipizide. To clarify the mechanism of this interaction we have studied the effect of pH on the dissolution of two different formulations of glibenclamide (micronized and non-micronized) and one formulation of glipizide. One tablet of each sulphonylurea preparation was placed in a dissolution chamber containing continuously mixed dissolution medium at pH 2, pH 6 or pH 9; 5 mL of the medium was replaced every 2 min. The amount of glibenclamide dissolved from the non-micronized formulation within 2 h, was 1.2, 4.5 and 76% at pH 2, pH 6 and pH 9, respectively (P < 001), whereas 21, 29 and 100% was dissolved from the micronized formulation (P < 001). The amount of glipizide dissolved within 2 h at pH 2, pH 6 and pH 9 was 3.9, 24 and 92%, respectively (P < 001). We conclude that the elevated pH of the gastric contents is the most likely explanation for the interactions previously demonstrated between antacids and sulphonylureas after their concomitant ingestion. |
| Databáze: | OpenAIRE |
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