piperidines and gliquidone

Pharmaceutical counterfeiting is becoming a serious problem in the world, especially in developing countries including China. Herein an isocratic reversed-phase high performance liquid chromatography (RP-HPLC) method was developed for screening counterfeit medicines and adulterated dietary supplement products. The developed method could be employed to separate and determine simultaneously six anti-diabetic drugs (glipizide, gliclazide, glibenclamide, glimepiride, gliquidone, repaglinide) on an isocratic solvent system using an Alltima C18 column (5 microm, 150 mmx4.6 mm) with an isocratic mobile phase of methanol-phosphate buffer (pH 3.0; 0.01 mol/L) (70:30, v/v), at a flow rate of 1.0 mL/min and at a wavelength of 230 nm. The proposed method was successfully applied to the analysis of medicinal and dietary supplement samples purchased from the local market in China.

Topics: Carbamates; Chromatography, High Pressure Liquid; Gliclazide; Glipizide; Glyburide; Hypoglycemic Agents; Molecular Structure; Piperidines; Reproducibility of Results; Sulfonylurea Compounds

A novel ester of succinic acid (1,2,3-tri(methylsuccinyl)glycerol ester; 3SMG) was found to stimulate insulin release and to potentiate the insulinotropic action of gliquidone and repaglinide when administered intravenously to normal anaesthetized rats in a dose as low as 0.07 mumol g-1 body wt. The ester failed, however, to augment plasma insulin concentration when given enterally. The design of succinic acid esters of high insulinotropic potential might thus allow efficient stimulation of insulin secretion in non-insulin-dependent diabetes, without requiring unpractical high dosage and without running the risk of an undesirable increase in gluconeogenesis.

Topics: Animals; Blood Glucose; Carbamates; Drug Synergism; Esters; Hypoglycemic Agents; Insulin; Male; Piperidines; Rats; Rats, Wistar; Stereoisomerism; Succinates; Sulfonylurea Compounds