Pioglitazone HCl is the hydrochloride salt preparation of Pioglitazone, a specific ligand of PPAR-γ (peroxisome proliferator-activated receptor-γ). Pioglitazone is a thiazolidinedione compound described to produce antiinflammatory and antiarteriosclerotic  effects. Pioglitazone is demonstrated to prevent L-NAME-induced coronary inflammation and arteriosclerosis and to suppress increased TNF-α mRNA produced by aspirin-induced gastric mucosal injury. Pioglitazone Hydrochloride is an activator of PPAR γ.
Pioglitazone achieves long-lasting control of blood sugar by directly reducing insulin resistance and improving beta cell function. Pioglitazone is a highly selective and potent peroxisome proliferator-activated receptor gamma (PPARγ) agonist. The receptor is a protein found in fat, skeletal muscle and liver tissue of insulin-sensitive tissues.
The absolute bioavailability of pioglitazone was 99%. After oral administration, pioglitazone was detected in the blood for 30 min in the fasting period, and the peak concentration was reached in 2 h. The food will delay the peak concentration time to 3 to 4 hours, and the plasma t1/2 is 3 to 7 hours. Pioglitazone binds primarily to serum albumin, is metabolized by hydroxylation and oxidation, and is mostly excreted as bile into protoplasts or metabolites and removed from the feces. Pioglitazone increases insulin levels in islets and has no effect on insulin secretion. Pioglitazone prevents beta cell reduction by reducing cell death, and this evidence suggests that pioglitazone has a protective effect on beta cells.
Pioglitazone reduces hyperinsulinemia and plasma free fatty acid levels. A decrease in plasma insulin levels indicates that pioglitazone reduces the burden on pancreatic beta cells. Since high levels of free fatty acids have toxic effects on the pancreas, lowering free fatty acid levels also has a protective effect on pancreatic beta cell function. Therefore, the basic physiological link to type 2 diabetes is to reduce insulin resistance, improve beta cell function and control blood sugar.

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