Absorption of Glibenclamide

D. Brockmeier, H. G. Grigoleit, and H. Leonhardt, Absorption of glibenclamide from different sites of the gastrointestinal tract, Eur. J. Clin. Pharmacol. 29 193— 197 (1985). 

Absorption of both first- and second-generation sulphonylureas is rapid and complete except for gliclazide and tolazamide, which are absorbed more slowly. The maximal plasma concentrations are usually reached within 2-4 h. The kinetics of absorption depend on the formulation and crystalline structure of the drug. Absorption of chlorpropamide may also depend on pH and therefore on food intake, which appears not to be true for the other sulphonylureas (Sartor et al., 1980). The absorption of glibenclamide, although rapid and almost complete, can be improved by an appropriate formulation (Haupt et al., 1984) which leads to a reduction in the daily dosage required. 

Compounds that may diminish the hypoglycaemic effect and thus cause an increase in the dosage requirement of sulphonylurea include rifampicin (Syvalahti et al., 1974). There is a theoretical risk of a diminished hypoglycaemic effect with corticosteroids and with oral contraceptives. It has been stated that the absorption of glibenclamide from the gastrointestinal tract may be reduced if it is taken together with guar gum. 

Uusitupa H Sedervik H, Silvasti M, Karttunen P. Effects of a gel forming diet fiber, guar gum, on die absorption of glibenclamide and metabolic control and serum lipids in patients with non-insulin-dependent (type 2) diabetes. IntJ Clin Pharmacol Ther Toxicol (1990) 28, 153-7. 

Lobenberg R, Kraemer J, Shah VP, Amidon GL, Dressman JB. Dissolution testing as a prognostic tool for oral drug absorption dissolution behavior of glibenclamides. Pharm Res 2000 17 439-444. 

Guar gum 1. Metformin 2. Glibenclamide May lead to t blood sugar levels i absorption of metformin and glibenclamide Avoid concomitant use. Monitor blood sugar closely if either drug is introduced... 

Figure 8.13 shows the rice husk/glibenclamide and wheat gluten husk/glibenclamide MESP, where can be observed that the values are very similar at lignocellulosic materials (see Figure 8.8). The negative regions were appreciated at OH groups (C-OH bonds). The absorption of the glibenclamide can be seen mainly in to the rice husk by the formation of hydrogen bonds between the OH and NH, respectively.

SLTR1/Kir6.2 Glibenclamide and glipizide that block pancreatic KAXP channels have been used for the treatment of type II diabetes. New class of insulin secretagogues includes repaglinide and nateglinide, which improve insulin secretion, action and reduce carbohydrate absorption. 

Neuvonen PJ, Kivistd KT. The effects of magnesium hydroxide on the absorption and efficacy of two glibenclamide jx-eparations. BrJCUn Pharmacol (1991) 32,215-20. 

Information about intravaginal clotrimazole is very sparse, but it appears not to interact with gliclazide or glibenclamide, and probably not with any of the other oral anti diabetics, not least because its absorption from the vagina is very small. 

In the FTIR results of rice husk/glibenclamide can be seen in Table 8.11, the principal absorption peaks appeared at 5505 cm was attributed to CH stretching, at 3368 cm" ... 

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