Molecular Formula | C9H17NO4 |
Molar Mass | 203.24 |
CN201911218912.5
application date:
2019-12-03
Public/Announcement Number:
CN110801448A
Public/announcement date:
2020.02.18
applicant (patent):
Zhuhai Yibang Pharmaceutical Co., Ltd.
inventor:
Hao Shan Wu , Zhong guixiong , Jiang Lijuan
National and provincial code:
CN440404
Abstract:
The invention relates to the field of chemical drug raw material manufacturing, and provides acetyl-L-carnitine chloride for injection and a preparation method thereof. The acetyl-L-carnitine chloride is obtained by mixing Levocarnitine and glacial acetic acid, and reacting Dropwise with acetyl chloride; dissolve mannitol and acetyl-L-carnitine chloride with water for injection, adjust the pH value to 6.0~7.5, dilute the solution, add activated carbon adsorption, filter, fill to obtain lyophilizate; Pre-freeze, sublimate, drying, packaging, to obtain acetyl-L-carnitine chloride for injection. The Levocarnitine for Injection has the advantages of high purity, high stability, its formula, simple process, short synthesis period, has a wide range of applications.
Xiang Rongfeng , wear cyan , Li Xiong , Tang Min , Yu Ming-Jie , Chen Yongchuan
Abstract:
Objective to determine the concentration of acetyl-L-carnitine in human plasma by LC-MS/MS and study its pharmacokinetics in healthy volunteers. Methods blood samples were collected from healthy subjects at 0-24 h after single administration of 0.5,1.0,1.5g and multiple administration of 0.5g. The pharmacokinetic parameters were calculated by determining the absolute concentration of acetyl-L-carnitine in plasma after single and multiple doses. The protein was analyzed by LC-MS/MS after precipitation with methanol using midrazide as internal standard. ESI ion source positive mode monitoring, detection ions m/z 204.3 & rarr;145.2 (acetyl-L-carnitine),m/z 147.2 & rarr;58.2 (midronic hydrazine); the chromatographic column was EC 250/4.6 NUCLEOSIL100-5CN, and the mobile phase was methanol -10mmol · L-1 ammonium acetate solution (containing 0.1% formic acid)(85:15). Results the linear range of acetyl-L-Carnitine was 20-3 000 μg · L-1 (r = 0.999 1), and the limit of quantification was 20 μg · L-1. Intra-assay, inter-assay precision and matrix effect RSD were less than 15%. The main pharmacokinetic parameters of single dose group (0.5,1.0,1.5g) were as follows: (4181.77±2 473.24)μg · h · AUC0-t,(6099.54±1939.41) L-1 μg · h · L-1 and (8 064.71±3 575.99)μg · h · L-1,Cmax was (611.42±270.76)μg · L-1,(830.92±233.19)μg · L-1 and (1 004.67±414.95)μg · L-1,t1/2z was (4.50±2.93)h,(6.25±3.65)h and (5.76±3.94)h; the main pharmacokinetic parameters after multiple administration were (13728.82±6493.04)μg · h · AUC0-t on L-1,Cmax (1 129.00±374.05)μg · L-1,t1/2z is (8.57±4.42)h. Conclusion The method is accurate, sensitive, specific and suitable for the pharmacokinetic study of acetyl-L-carnitine in human. There were significant differences in pharmacokinetic parameters after single and multiple doses of Chloroacetyl-L-carnitine tablets, and there was no difference between genders. Healthy subjects had good tolerance to the drug.expand
Key words:
acetyl-L-carnitine pharmacokinetics plasma
DOI:
CNKI:SUN:XDYD.0.2019-01-007
year:
2019
CN 01128215
application date:
Sep 27, 2001
Public/Announcement Number:
CN 1408704 A
applicant (patent):
Beijing lanbeigun Biomedical Technology Co., Ltd.
inventor:
, Fu Ji Feng , Li Shuming
National and provincial code:
Beijing; 11
cited:
Abstract:
The invention provides a simple method for preparing acetyl-L-carnitine hydrochloride, and belongs to the field of drug synthesis. It is characterized by taking Levocarnitine internal salt as the starting material, glacial acetic acid as the solvent, under the action of Catalyst, the reaction at lower temperature can be directly crystallized to obtain acetyl Levocarnitine hydrochloride crude product, then the product is obtained by recrystallization. This method has the advantages of simple process, low energy consumption, few side reactions and good product quality.
sovereignty:
1. The preparation method of acetyl-L-carnitine hydrochloride is characterized by taking L-carnitine hydrochloride as a starting material, acetic anhydride as an acylating agent, and reacting at 70~75 ° C. For 1~3 hours under the action of a catalyst, cool down to 20~25 ℃, wash with ether beating, add alcohol and stir for 2~3 hours for crystallization, the obtained crude product is dissolved by heating with a single alcohol or a mixed solvent and decolorized by adding activated carbon, and then recrystallized to obtain a refined product. Where: (1) molar ratio of Levocarnitine hydrochloride to acetic anhydride is 1: 1 to 1.5; (2) the weight ratio of L-carnitine hydrochloride to catalyst is 10: 1~1.5; (3) catalyst can be selected from p-toluenesulfonic acid, trifluoroacetic acid, perchloric acid; (4) ether, methyl tert-butyl ether and isopropyl ether can be selected for beating and washing; (5) ethanol, isopropyl alcohol and n-butyl alcohol can be selected for adding alcohol in the process of precipitating crude product; (6) The solvent selected for recrystallization can be ethanol, isopropanol, ethanol-isopropanol, isopropanol-water, ethanol-acetone, isopropanol-acetone, ethanol-water; (7) the amount of recrystallization solvent is 2 to 10 times (V/W) the weight of the crude product. (8) the amount of activated carbon added is 5-15% by weight of the crude acetyl-L-carnitine hydrochloride.
toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |