Loperamide

Diarrhea is a highly prevalent digestive system symptom worldwide, especially traveler's diarrhea and diarrhea associated with chronic intestinal dysfunction, which often cause significant interference to patients' daily work and quality of life. Loperamide is an opioid receptor agonist antidiarrheal drug. By activating μ-opioid receptors on the gastrointestinal wall, it inhibits the release of acetylcholine and prostaglandins, slows intestinal peristalsis, prolongs the transit time of intestinal contents, and at the same time enhances the tone of the anal sphincter, reducing symptoms of fecal incontinence and urgent defecation. Clinically, it is mainly used to control the symptoms of acute and chronic diarrhea, and can also be used in patients with ileostomy to reduce the volume and frequency of defecation and increase the consistency of feces. The applicable population covers adults and children over 2 years old.

As a commonly used basic antidiarrheal drug in clinical practice, the global market size of loperamide is stable at around USD 320 million, with a compound annual growth rate maintained at a steady level of 2.1%. The market pattern is dominated by generic drugs, accounting for more than 85%. Among them, China and India are the world's major producers of loperamide API, supplying nearly 70% of the global market demand. In terms of the domestic market, this variety has been included in the National Medical Insurance Catalog (Class A), and is also a commonly used antidiarrheal drug in primary medical institutions. The winning bid price of preparations in relevant batches of centralized procurement has dropped by about 42%, which further drives the stable demand for upstream APIs.

The original research enterprise of loperamide is Johnson & Johnson, and the original research brand name is Imodium. Its core compound patent expired worldwide in 1993. The core dosage form of the original research is capsule with a specification of 2mg. This dosage form has been included in the *Catalogue of Chemical Reference Preparations* of China, and is also included in the FDA Reference Preparation Catalogue. In terms of domestic API registration, 7 enterprises including Xi'an Janssen have obtained A-status registration numbers for loperamide API at present. The domestically approved preparation varieties cover capsules, granules and oral solutions, which can meet the clinical medication needs in different scenarios. (Data as of August 2024, please refer to the official website of CDE for the latest information)

In response to the demand for loperamide quality research and production quality control, CATO can provide a full set of impurity reference standards for this API. Most products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. All products comply with the compliance requirements of multiple regulations including the Chinese Pharmacopoeia and FDA, and can effectively support pharmaceutical enterprises to complete relevant work such as API associated declaration and quality stability research.