Preparation method of lincomycin hydrochloride injection

Abstract

The invention discloses a preparation method of a lincomycin hydrochloride injection. The preparation method comprises the following steps of: (a) heating water for injection to 55-65 DEG C and dissolving raw powder of lincomycin hydrochloride; (b) regulating the pH of anhydrous sodium bicarbonate to be neutral, adding EDTA-2Na (ethylenediaminetetraacetic acid-disodium), fully and uniformly stirring, then removing pyrogen with 0.02% of activated carbon for injection and determining the content; and (c) filtering through a microporous filtering film, filling under a class-100 environment and circulating steam at the temperature of 100-105 DEG C for 15 minutes for sterilizing twice. According to the preparation method disclosed by the invention, a lincomycin B component can be degraded in the preparation process of the injection by improving the methods for regulating the temperature of liquid medicine, performing secondary sterilization and the like in the preparation process, so that the content of the lincomycin B component in the injection is reduced, the quality of a product is improved, and thus high cost caused by particular extraction and purification against raw materials is also avoided.

Description

technical field

[0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to a lincomycin hydrochloride injection and a preparation method thereof. Background technique

[0002] Lincomycin hydrochloride injection is a sterilized aqueous solution of lincomycin hydrochloride, which is a commonly used antibiotic drug in clinical practice. It is mainly used to treat sensitive Staphylococcus, Streptococcus, Streptococcus pneumoniae and anaerobic bacteria Respiratory tract infection, skin and soft tissue infection, female reproductive tract infection, pelvic cavity infection and abdominal cavity infection. Lincomycin contains two components, A and B, of which the main component is A component. The A and B components in lincomycin are quite different in pharmacology. Compared with the A component, the B component has lower antibacterial activity and higher toxicity. Therefore, the content of component B in the finished product is...

Examples

Embodiment 1

[0016] Weigh 6kg of lincomycin hydrochloride original powder, 8g of EDTA-2Na, 172g of anhydrous sodium bicarbonate, and about 19000ml of water for injection.

[0017] a. Heat the water for injection to 60°C, dissolve the original powder of lincomycin hydrochloride, adjust the pH value of the liquid to 4.1-4.5 with hydrochloric acid, make the liquid acidic, stir well, and mix it with lincomycin The mixed alcohol residual reaction, then add water for injection to 20000ml.

[0018] b. Use 5000 Dalton ultrafiltration equipment for ultrafiltration, and add formula amount of anhydrous sodium bicarbonate to the solution after ultrafiltration to reduce irritation and pain during administration, add EDTA-2Na, and stir well Finally, depyrogenate with 0.02% activated carbon for needles, measure content and pH value.

[0019] c. After the drug solution is qualified, it is filtered through a 0.2μm microporous membrane, filled in a 100-grade environment, sterilized once by circulating stea...

Embodiment 2

[0022] Weigh 3kg of lincomycin hydrochloride original powder, 6g of EDTA-2Na, appropriate amount of anhydrous sodium bicarbonate, and about 19000ml of water for injection.

[0023] a. Heat the water for injection to 60°C, dissolve the original powder of lincomycin hydrochloride, adjust the pH value of the liquid to 4.5-5.5 with hydrochloric acid, make the liquid acidic, stir well, and mix it with lincomycin The mixed alcohol residual reaction, then add water for injection to 20000ml.

[0024] b. Use 5000 Dalton ultrafiltration equipment for ultrafiltration, add appropriate amount of anhydrous sodium bicarbonate to the solution after ultrafiltration to adjust the pH value to neutral, add EDTA-2Na, stir well and use 0.02% activated carbon for needles to remove Pyrogen, measured content, pH value;

[0025] c. After the drug solution is qualified, it is filtered through a 0.2μm microporous membrane, and after filling in a 100-grade environment, it is sterilized once by circulatin...

Embodiment 3

[0031] Comparison of the injection prepared in the examples of the present invention with the injection prepared according to the prior art.

[0032] For the lincomycin in the injections prepared in Example 1, Example 2 and Comparative Example, the contents of component A and component B were measured by high-performance liquid chromatography, and the test results are shown in Table 1 as follows. The content and color grade of the prepared injection were stored under the same conditions for 3 years, and tested according to the provisions of the Pharmacopoeia. The qualified rate of the test is shown in Table 1.

[0033] Table 1:

[0034]

[0035] The test results show that the method of the invention can reduce the content of lincomycin B in the finished product from 4.0% to about 3.0%, which is more than 1% lower than the original process.

technical field

[0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to a lincomycin hydrochloride injection and a preparation method thereof. Background technique

[0002] Lincomycin hydrochloride injection is a sterilized aqueous solution of lincomycin hydrochloride, which is a commonly used antibiotic drug in clinical practice. It is mainly used to treat sensitive Staphylococcus, Streptococcus, Streptococcus pneumoniae and anaerobic bacteria Respiratory tract infection, skin and soft tissue infection, female reproductive tract infection, pelvic cavity infection and abdominal cavity infection. Lincomycin contains two components, A and B, of which the main component is A component. The A and B components in lincomycin are quite different in pharmacology. Compared with the A component, the B component has lower antibacterial activity and higher toxicity. Therefore, the content of component B in the finished product is...

Examples

Embodiment 1

[0016] Weigh 6kg of lincomycin hydrochloride original powder, 8g of EDTA-2Na, 172g of anhydrous sodium bicarbonate, and about 19000ml of water for injection.

[0017] a. Heat the water for injection to 60°C, dissolve the original powder of lincomycin hydrochloride, adjust the pH value of the liquid to 4.1-4.5 with hydrochloric acid, make the liquid acidic, stir well, and mix it with lincomycin The mixed alcohol residual reaction, then add water for injection to 20000ml.

[0018] b. Use 5000 Dalton ultrafiltration equipment for ultrafiltration, and add formula amount of anhydrous sodium bicarbonate to the solution after ultrafiltration to reduce irritation and pain during administration, add EDTA-2Na, and stir well Finally, depyrogenate with 0.02% activated carbon for needles, measure content and pH value.

[0019] c. After the drug solution is qualified, it is filtered through a 0.2μm microporous membrane, filled in a 100-grade environment, sterilized once by circulating stea...

Embodiment 2

[0022] Weigh 3kg of lincomycin hydrochloride original powder, 6g of EDTA-2Na, appropriate amount of anhydrous sodium bicarbonate, and about 19000ml of water for injection.

[0023] a. Heat the water for injection to 60°C, dissolve the original powder of lincomycin hydrochloride, adjust the pH value of the liquid to 4.5-5.5 with hydrochloric acid, make the liquid acidic, stir well, and mix it with lincomycin The mixed alcohol residual reaction, then add water for injection to 20000ml.

[0024] b. Use 5000 Dalton ultrafiltration equipment for ultrafiltration, add appropriate amount of anhydrous sodium bicarbonate to the solution after ultrafiltration to adjust the pH value to neutral, add EDTA-2Na, stir well and use 0.02% activated carbon for needles to remove Pyrogen, measured content, pH value;

[0025] c. After the drug solution is qualified, it is filtered through a 0.2μm microporous membrane, and after filling in a 100-grade environment, it is sterilized once by circulatin...

Embodiment 3

[0031] Comparison of the injection prepared in the examples of the present invention with the injection prepared according to the prior art.

[0032] For the lincomycin in the injections prepared in Example 1, Example 2 and Comparative Example, the contents of component A and component B were measured by high-performance liquid chromatography, and the test results are shown in Table 1 as follows. The content and color grade of the prepared injection were stored under the same conditions for 3 years, and tested according to the provisions of the Pharmacopoeia. The qualified rate of the test is shown in Table 1.

[0033] Table 1:

[0034]

[0035] The test results show that the method of the invention can reduce the content of lincomycin B in the finished product from 4.0% to about 3.0%, which is more than 1% lower than the original process.

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