Name | Colesevelam Hydrochloride |
Synonyms | chloride Colesevelam COLESEVALAM hydrochloride propan-1-amine Colesevelam HCL prop-2-en-1-amine colesevelam hcl API N-allyldecan-1-amine N-propyldecan-1-amine 2-(chloromethyl)oxirane 2-(chloromethyl)oxirane Colesevelam Hydrochloride Colesevelam hydrochloride 6-(allylamino)hexyl-trimethyl-ammonium trimethyl-[6-(propylamino)hexyl]ammonium Colesevelam and Colesevelam Hydrochloride 2-Propen-1-amine polymer with (chloromethyl)oxirane, N-2-propenyl-1-decanamine and N,N,N-trimethyl-6-(2-propenylamino)-1-hexanaminium chloride hydrochloride |
CAS | 182815-44-7 |
EINECS | 806-925-3 |
InChI | InChI=1/C13H29N.C12H29N2.C3H5ClO.C3H9N/c1-3-5-6-7-8-9-10-11-13-14-12-4-2;1-5-10-13-11-8-6-7-9-12-14(2,3)4;4-1-3-2-5-3;1-2-3-4/h14H,3-13H2,1-2H3;13H,5-12H2,1-4H3;3H,1-2H2;2-4H2,1H3/q;+1; |
Molecular Formula | C31H67Cl3N4O |
Molar Mass | 618.24888 |
Storage Condition | Room Temprature |
Overview | Colevelam hydrochloride (Colesevelam hydrochloride) is a non-absorbent polymer oral drug. It is a new type of treatment developed by an American company. Hyperlipidemia drug, it is suitable for the treatment of high serum total cholesterol (TC) or triglyceride (TG) levels. Clinical studies have shown that patients take the drug orally within 6 to 24 weeks, coleveren alone can reduce the level of low-density lipoprotein cholesterol (LDL-C) by 9 ~ 19%. When combined with other drugs, it can reduce the LDL-C level by 10 ~ 16%. |
Introduction | The chemical name of calevilene hydrochloride is: 2-propanilene-1-and epichlorohydrin, N-2-propyl-1-decylamine and, N,N,N-trimethyl-6-(2-propaniline-amine)-1-hexylamine copolymer hydrochloride. English name Colesevelam hydrochloride. Its chemical structure is shown in Figure 1. It is a hydrophilic, water-insoluble polymer with a light yellow powder. Figure 1 is the structure diagram of collevelam hydrochloride. |
Mechanism of action | In the process of human digestion, cholesterol is the only precursor of bile acid. When bile acid is secreted into the intestine, the intestine will absorb a large amount of bile acid, and then re-enter the liver through the hepatic-intestinal circulation. The drug can combine bile acid and hepatobiliary acid, the main component of bile acid. Since collevelam hydrochloride is a non-absorbent polymer, it can combine with bile acid in a large amount in the intestine, thereby preventing the reabsorption of bile acid. The large consumption of bile acid will promote the liver cholesterol 7-α-hydroxylase in the intestine. Up-regulation of enzyme, that is, on the one hand, it increases the consumption of bile acid, on the other hand, it promotes the conversion of cholesterol into bile acid, and makes cholesterol biosynthesis enzyme (hydroxymethylglutaryl coenzyme A reductase), the activity in liver cells increases, and increase liver low-density lipoprotein (LDL) receptors. These compensatory effects increase the clearance of low-density lipoprotein cholesterol in the blood, thereby reducing serum LDL-C levels. |
clinical effect | clinical display, this product is an oral drug, which can be combined with bile acids. it is a polymer hydrogel and cannot be absorbed by the human body. because the drug has great absorption, it can be used as a good lipid-lowering drug. because this product and cholesterol are discharged with the human body and are not absorbed by the human body, therefore, compared with the traditional bile acid chelating agent, the human body has better adaptability and fewer reports of adverse reactions. This product is mainly used for the treatment of moderately elevated cholesterol levels, or when it is not suitable for use with statins, it is used in combination with other drugs to improve the effect of the drug. At present, there are already such drugs and statins on the market. Clinical studies have shown that for patients with primary TC, this product can be used alone or in combination with statin lipid-lowering drugs to reduce the level of total cholesterol and LDL-C in the human body, at the same time, the level of HDL cholesterol was increased. Eight studies with a duration of 2-50 weeks showed that the maximum effect of this product can be achieved in 2-4 weeks after medication. In the entire long-term study, the effect has always been maintained. |
Adverse reactions | The effects of collevelam hydrochloride on the nervous system mainly include adverse reactions that can cause, headache and weakness; adverse reactions in ear, nose and throat mainly include pharyngitis, rhinitis and sinusitis; gastrointestinal can cause abdominal pain, abdominal muddy, indigestion, constipation, nausea and flatulence and other adverse reactions; musculoskeletal system can cause muscle pain and back pain and other adverse reactions; respiratory system cough; can cause skin damage, infection and other syndromes. |
prospect | with the continuous development of global social economy, aging is an important challenge facing all countries, and the following human health problems will become more and more serious, and the number of patients with hyperlipidemia will continue to increase. therefore, hypolipidemic drugs have a good market prospect and continue to maintain a strong growth momentum. it is expected to maintain a double-digit growth every year, the global market value of lipid-lowering drugs will reach more than US $100 billion by 2012. In 2000, corlevelam hydrochloride has been approved by the U.S. Food and Drug Administration (FDA) for clinical application, and the effect is significant. The sales in the first year of listing on the U.S. market reached 80 million US dollars. It can not only be used to treat hyperlipidemia, It can also be used to treat diabetes, and it can also be used to treat lipid-lowering and low-density lipoprotein. Based on the above advantages of Coraiwei Hydrochloride, we expect that the drug will also have a good application prospect in the domestic market. The in-depth research on the drug has great social significance and huge economic benefits. Therefore, we plan to conduct synthetic research on the drug, trying to find a process route suitable for industrial production. The expected goal is that the reaction raw materials are cheap and easy to obtain, the reaction is simple, the operation is simple and has a high yield. |
References | [1] Zhang Wei, Ren Lianjie, Zhou Changming, Lu Wen, Han Chunxia. Study on Determination of Organic Amine Impurities in Collevelen Hydrochloride Tablets by High Performance Cation Exchange Chromatography [J]. Chinese Journal of Biochemical Drugs, 2014,34(08):170-172 175. [2] he jun. study on the synthesis process of colevilam hydrochloride [D]. Nanjing University of Science and Technology, 2013. |