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Specific clindamycin hydrochloride superfine powdered lyophilized preparation and preparation method thereof

A technology of clindamycin hydrochloride and lincomycin hydrochloride, which is applied in the field of medicine, can solve the problems of large toxic and side effects, small specific surface area, and low clarity, and achieve improved utilization, large specific surface area, and good clarity Effect

Inactive Publication Date: 2014-11-12
浙江磐谷药源有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The existing clindamycin hydrochloride has the disadvantages of low clarity, poor stability, low purity, many impurities, large particles, small specific surface area, poor solubility, large toxic and side effects, and easy allergies

Method used

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  • Specific clindamycin hydrochloride superfine powdered lyophilized preparation and preparation method thereof
  • Specific clindamycin hydrochloride superfine powdered lyophilized preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] 80 kg of chloroform, 11 kg of N,N-dimethylformamide (DMF), 10 kg of lincomycin hydrochloride (HPLC purity 99.6%), antioxidant tetrakis[β-(3,5-di 50 grams of tert-butyl-4-hydroxyphenyl) propionic acid] pentaerythritol ester was added to the reaction kettle, and then 12 kilograms of solid phosgene was added in batches, and at 40 ° C, the reaction was incubated for 24 hours, and the hydrochloric acid in the reaction system was detected by HPLC. The content of lincomycin is less than 1.0%, and after the reaction is completed, the temperature of the reaction solution is lowered to 0°C.

[0026] Add 40 kg of purified water and 40 L of 20% sodium hydroxide aqueous solution to the reaction solution, heat up, hydrolyze at 35° C., leave to stand for stratification, and extract the organic phase twice with 40 kg of chloroform for the aqueous phase. Combine the organic phases, wash them with water, concentrate the organic phases under reduced pressure at 55°C to get chloroform, add...

Embodiment 2

[0033] In turn, 90 kg of chloroform, 13 kg of N,N-dimethylformamide (DMF), 10 kg of lincomycin hydrochloride (HPLC purity 99.6%), and the antioxidant tetrakis[β-(3,5-di 55 grams of tert-butyl-4-hydroxyphenyl)propionic acid]pentaerythritol ester was added to the reaction kettle, and then 13 kilograms of solid phosgene was added in batches, and at 45° C., the insulation reaction was carried out for 22 hours, and the hydrochloric acid in the reaction system was detected by HPLC. The content of lincomycin is less than 1.0%, and after the reaction is completed, the temperature of the reaction solution is lowered to 2°C.

[0034]Add 50 kg of purified water and 30 L of aqueous sodium hydroxide solution with a mass concentration of 25% to the reaction solution, raise the temperature, perform hydrolysis at 35°C, leave to stand and separate the layers, and extract the organic layer twice with 40 kg of chloroform in the aqueous phase , combine the organic phases, wash with water, concent...

Embodiment 3

[0041] 100 kg of chloroform, 15 kg of N,N-dimethylformamide (DMF), 10 kg of lincomycin hydrochloride (HPLC purity 99.6%), antioxidant tetrakis[β-(3,5-di 60 grams of tert-butyl-4-hydroxyphenyl) propionate] pentaerythritol ester was added to the reaction kettle, and then 14 kg of solid phosgene was added in batches, and at 50 ° C, the reaction was incubated for 18 hours, and the hydrochloric acid in the reaction system was detected by HPLC. The content of lincomycin is less than 1.0%, and after the reaction is completed, the temperature of the reaction solution is lowered to 5°C.

[0042] Add 60 kg of purified water and 25 L of aqueous sodium hydroxide solution with a mass concentration of 30% to the reaction solution, raise the temperature, perform hydrolysis at 35°C, stand and separate the layers, and extract the organic layer twice with 40 kg of chloroform in the aqueous phase , combine the organic phases, wash with water, concentrate the organic phase under reduced pressure ...

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Abstract

The invention discloses a specific clindamycin hydrochloride superfine powdered lyophilized preparation and a preparation method thereof. The preparation method uses clindamycin hydrochloride and triphosgene as raw materials, and comprises the following steps: performing chlorination reaction in the system of trichloromethane, N,N-dimethylformamide and antioxidant; hydrolyzing and alcoholizing to obtain clindamycin hydrochloride ethylate; decoloring and dealcoholizing to obtain high-purity clindamycin hydrochloride; and performing air-jet superfine crushing, and lyophilizing to obtain the specific clindamycin hydrochloride superfine powdered lyophilized preparation. The specific clindamycin hydrochloride superfine powdered lyophilized preparation has the advantages of good clarity, high stability, high purity, few impurities, small particles, large specific surface area, good solubility, small toxic and side effect, allergy prevention and the like.

Description

technical field [0001] The invention relates to a clindamycin hydrochloride special ultrafine powder freeze-dried preparation and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Clindamycin hydrochloride, the English name is clindamycin hydrochloride, the chemical name is 6-(1-methyl-trans-4-propyl-L-2-pyrrolidinecarboxamido)-1-thio-7(S) -Chloro-6,7,8-trideoxy-L-threo-a-D-galactopyranoside hydrochloride, the molecular formula is C18H33ClN2O5S·HCl, and the molecular weight is 461.44. [0003] Clindamycin hydrochloride is an antibiotic drug, which is a derivative of lincomycin. Its antibacterial spectrum is the same as that of lincomycin, but its antibacterial activity is 4-8 times stronger than that of lincomycin. Clindamycin hydrochloride is suitable for moderate and severe infections caused by Streptococcus, Staphylococcus and anaerobic bacteria (including Bacteroides fragilis, Clostridium perfringens, Actinomyces, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/7056A61P31/04
Inventor 傅苗青李凤生
Owner 浙江磐谷药源有限公司
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