CN-121987562-A - Deoxycholic acid injection composition and preparation method thereof

Abstract

The invention discloses a composition and a preparation method of deoxycholic acid injection, wherein the prescription comprises deoxycholic acid, sodium chloride, disodium hydrogen phosphate, sodium dihydrogen phosphate, vitamin C ethyl ether and water for injection, wherein the dosage of the vitamin C ethyl ether is 0.25-2.0%. The deoxycholic acid injection disclosed by the invention has the advantages of simple composition, stable quality, simple and efficient preparation process, no need of special equipment and filling of inert gas, low impurity level of a finished product prepared by terminal sterilization (F0 is more than or equal to 12), and good safety.

Inventors

• JI XIJING
• LIU JIANHAO
• XING ZHENZHEN
• XU CHENG
• CHEN YUANDONG
• ZHU YAFANG
• SHEN SHU

Assignees

• 江苏润恒制药有限公司

Dates

Publication Date

20260508

Application Date

20241101

Claims (6)

1. 1. A deoxycholic acid injection composition and a preparation method thereof are characterized in that the prescription composition contains vitamin C ethyl ether.
2. 2. Vitamin C ethyl ether according to claim 1, characterized in that it is used in an amount of 0.25% to 2.0%.
3. 3. Vitamin C ethyl ether according to claim 1, characterized in that it is used in an amount of 0.5% to 1.0%.
4. 4. Vitamin C ethyl ether according to claim 1, characterized in that it is used in an amount of 0.75%.
5. 5. Deoxycholic acid injection according to claim 1, characterized by consisting of deoxycholic acid, sodium chloride, disodium hydrogen phosphate, sodium dihydrogen phosphate, vitamin C ethyl ether and water for injection.
6. 6. Deoxycholic acid injection according to claim 1, the complete preparation process comprising the steps of: Sequentially adding deoxycholic acid, sodium chloride, disodium hydrogen phosphate, sodium dihydrogen phosphate and vitamin C ethyl ether into injectable water, stirring to dissolve and clarify, filtering to 0.22 μm, filling ampoule, sealing, and sterilizing with high pressure steam.

Description

Deoxycholic acid injection composition and preparation method thereof Technical Field The invention relates to the field of pharmaceutical preparations, in particular to deoxycholic acid injection and a preparation method thereof. Background Deoxycholic acid (Deoxycholic Acid) with chemical name of 3α,12α -dihydroxy-5β -cholanic acid is used for treating moderate to severe protrusion or double chin associated with submental fat in adults when the presence of submental fat has a significant psychological impact on patients. Molecular formula C 24H40O4 Molecular weight 392.58 Deoxycholic acid is white powder, odorless, soluble in ethanol, insoluble in chloroform, soluble in glacial acetic acid, soluble in sodium hydroxide solution, and soluble in water at different pH and temperature, such as water at 15deg.C, of 0.24g/L. Because deoxycholic acid is very dependent on pH and temperature, precipitation risk exists during liquid preparation. In the process of preparing the injection, if the crude drug is precipitated, various adverse effects can be generated on the injection of a finished product, 1) the drug effect is reduced, and the precipitated crude drug cannot be uniformly dispersed in the injection, so that the actual administration dose is inaccurate, and the treatment effect of the drug is affected. 2) The safety risk is that the precipitated crude drug particles may cause local irritation and inflammatory reaction during injection, and even cause serious safety problems such as vascular embolism and the like. 3) Stability problems precipitation of the drug substance may mean that the chemical stability of the injection is destroyed, thereby shortening the effective period of the injection. 4) The quality is non-uniform, so that the concentration of the medicine in the injection is non-uniform, and the medicine effect and the safety of different batches or different parts of the same batch can be different. 5) Filtering difficulties, increasing the difficulty and cost of the filtering process, may even lead to clogging and damage of the filtering equipment Therefore, a proper solubilizer needs to be found as an auxiliary material, has good compatibility with deoxycholic acid, can protect the stability of deoxycholic acid injection in the preparation production and storage environment, ensures that the dissolution of the raw material medicine is not influenced by pH and temperature, and has better safety than other similar solubilizers. Disclosure of Invention The invention mainly aims to overcome the defects of the prior art scheme of deoxycholic acid injection and provide a solubilizer with good solubilization effect and good safety. The invention also provides a prescription and a process preparation method of the injection, and the process is simple and efficient and is easy for large-scale production. The object of the invention is achieved by: a deoxycholic acid injection is characterized in that the prescription composition contains vitamin C ethyl ether. The deoxycholic acid injection comprises deoxycholic acid, sodium chloride, disodium hydrogen phosphate, sodium dihydrogen phosphate, vitamin C ethyl ether and water for injection. The amount of vitamin C ethyl ether is preferably 0.25% to 2.0%, more preferably 0.5% to 1.0%, and even more preferably 0.75%. The preparation method of the deoxycholic acid injection comprises the following steps: Sequentially adding deoxycholic acid, sodium chloride, disodium hydrogen phosphate, sodium dihydrogen phosphate and vitamin C ethyl ether into injectable water, stirring to dissolve and clarify, filtering to 0.22 μm, filling ampoule, sealing, and sterilizing with high pressure steam. Deoxycholic acid, sodium chloride, disodium hydrogen phosphate, sodium dihydrogen phosphate and vitamin C ethyl ether are all commercially available. The solubilizer vitamin C ethyl ether is applied to the product of the invention, can effectively increase the solubility of deoxycholic acid, improve the stability of the product and avoid the precipitation of raw materials due to the influence of temperature and pH in the preparation process. The vitamin C ethyl ether is a very good vitamin C derivative, is very stable in chemical substances, is a vitamin C derivative without color change, is a lipophilic and hydrophilic amphiprotic substance, is especially applied to daily cosmetics, and 3-O-ethyl ascorbate ether can easily enter the dermis layer through the stratum corneum, is decomposed by biological enzymes in the body after entering the body, so that the biological effect of the vitamin C is exerted, and the safety in the body is high. The following briefly describes the idea of the invention: In view of the very high dependence of deoxycholic acid solubility on pH and temperature, there is a risk of precipitation during the formulation. To solve this problem, the prior art of the American original developer discloses the use of sodium hydroxide and sodium dihydrogen phospha