Diphenoxylate

Chronic diarrhea, as a common chronic disease in the gastroenterology department, has a protracted course that easily leads to nutrient loss and reduced quality of life in patients. For a long time, there has been a clinical lack of oral treatment options that combine antidiarrheal efficacy and good tolerability. Diphenoxylate is a synthetic pethidine derivative antidiarrheal drug. It acts directly on the intestinal smooth muscle, inhibits intestinal mucosal receptors to weaken peristalsis, and at the same time increases intestinal segmental contraction to prolong the residence time of intestinal contents, promoting the reabsorption of water and electrolytes by the intestinal mucosa. It is clinically mainly used for the symptomatic treatment of acute and chronic functional diarrhea and chronic enteritis, and the applicable population covers adults and children over 2 years old. The dosage should be strictly controlled in accordance with medical advice to avoid adverse reactions.

At present, the global market size of diphenoxylate API is approximately USD 120 million, and the compound annual growth rate from 2023 to 2028 is expected to remain around 3.2%. The growth momentum mainly comes from the improvement of the penetration rate of chronic diarrhea diagnosis and treatment in primary medical institutions and the reserve demand for commonly used diarrhea drugs in emerging markets. The competitive landscape is characterized by the dominance of generic drugs. More than 70% of the global API production capacity is concentrated in China and India. There are 6 diphenoxylate API manufacturers in China that have passed GMP certification, among which 3 hold DMF filing qualifications. Their products are mainly supplied to domestic preparation manufacturers and exported to Southeast Asia and Africa, and have not yet been included in the national centralized volume-based procurement scope.

The original research enterprise of diphenoxylate is GD Searle LLC of the United States, and the original research trade name is Diphenoxylate. The core compound patent expired globally in 1977, and there is currently no valid core patent restriction. The main dosage form approved by the original research is compound tablet, each containing 2.5mg of diphenoxylate hydrochloride and 25μg of atropine sulfate. This compound preparation has been included in the FDA Reference Listed Drug Catalog, and is also included in China's *Catalog of Reference Preparations for Chemical Drugs (10th Batch)*. According to the domestic API registration platform, there are currently 5 registration numbers for diphenoxylate hydrochloride API, among which 3 are in A status and can be directly associated with preparation applications. There are 32 manufacturers of compound diphenoxylate tablets approved for marketing in China, all of which are generic drugs. (Data as of October 2024, please refer to the official website of CDE for the latest information)

CATO provides a full set of impurity reference standards for diphenoxylate, and most products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. The products fully comply with the compliance requirements of multiple regulations such as the Chinese Pharmacopoeia and FDA, and can fully meet the use needs of different scenarios such as API R&D, quality research and consistency evaluation.