Tolbutamide

Diabetes is a chronic metabolic disease with a high incidence worldwide. Sulfonylurea oral hypoglycemic drugs are one of the core categories of drugs for clinical blood glucose control in type 2 diabetes. As a representative of the first-generation sulfonylurea drugs, tolbutamide exerts its hypoglycemic effect by selectively acting on pancreatic β-cells to promote the release of endogenous insulin, while inhibiting hepatic glycogenolysis and gluconeogenesis. This drug is mainly targeted at patients with mild to moderate type 2 diabetes who have poor therapeutic effect after diet control. It requires that the patients' pancreatic β-cells still have a certain secretory function and there are no serious complications, making it a common option for stepwise treatment of early-stage diabetes.

At present, the global market size of first-generation sulfonylurea drugs is approximately USD 180 million. Despite the impact of new hypoglycemic drugs such as second- and third-generation sulfonylureas and DPP-4 inhibitors, the overall market size maintains a low and steady growth rate of 1.2%, with the primary care market being the main source of demand. In terms of the domestic market, tolbutamide is a Class A medical insurance variety. After the volume-based procurement, the terminal price has dropped by more than 70%. At present, domestic manufacturers are mainly generic drug companies, and nearly 30 enterprises have obtained preparation approval documents. The supply of API has basically achieved localization, and only a small amount of API for high-end preparations relies on imports.

The original research enterprise of tolbutamide is Pfizer, with the trade name Orinase. Its core compound patent expired globally in 1984. Currently, the mainstream marketed dosage form is tablet, with a conventional specification of 0.5g. The original preparation of this variety has been included in the FDA Reference Listed Drug Catalog, and is also included in the China Listed Drug Catalog. Up to now, there have been 11 tolbutamide registration numbers on the API registration platform of China CDE, among which 8 are in status A and can be legally supplied to preparation manufacturers for use. There are 27 approval numbers for tolbutamide tablets in China. (Data as of June 2025, please refer to the official CDE website for the latest information)

CATO can provide a full set of impurity reference standards for tolbutamide API. Most products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. All products meet the requirements of multiple regulatory systems such as the Chinese Pharmacopoeia and FDA, and can fully meet the demand for impurity reference standards in the process of API R&D, quality research and production.