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Process for preparing houttuyninum sodium injection

A technology of houttuyfonate sodium and injection, which is applied in the field of medicine, and can solve the problems that intravenous or intramuscular injection cannot be administered, and β-cyclodextrin cannot be injected intravenously, etc.

Inactive Publication Date: 2002-07-24
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Some authors have studied houttuyfotin β-cyclodextrin inclusion compound (I) (Chinese Journal of Pharmaceutical Sciences 1999, 34(3): 167-169). Although the solubility of I has increased, β-cyclodextrin It cannot be injected intravenously, and the prepared dosage form can only be used orally or externally, and cannot be administered intravenously or intramuscularly

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0004] Example 1: Weigh 6 g of hydroxypropyl β-cyclodextrin, place it in 6 ml of distilled water, and stir to dissolve. Another 0.3 g of sodium houttuyfonate is added to the above-mentioned hydroxypropyl β-cyclodextrin solution, and stirred or ground for 30 minutes at room temperature to obtain a sodium houttuyfonate solution. (The weight ratio of drug to hydroxypropyl β-cyclodextrin is 1:20). This solution was concentrated to 5ml to obtain a 60mg / ml houttuyfonate sodium solution.

Embodiment 2

[0005] Example 2: Weigh 10 g of hydroxypropyl β-cyclodextrin, place it in 100 ml of water for injection, and stir to dissolve. Another 1g of houttuyfonate sodium was added to the above hydroxypropyl β-cyclodextrin solution, stirred at room temperature for 30 minutes, filtered, and the resulting solution was vacuum dried, spray-dried, or freeze-dried to obtain a white powder, namely Houttuyfonate sodium hydroxypropyl β-cyclodextrin inclusion compound. The infrared spectrum of the inclusion compound is not only different from sodium houttuyfonate and hydroxypropyl β-cyclodextrin, but also different from the mixture of sodium houttuyfonate and hydroxypropyl β-cyclodextrin. (The weight ratio of drug to hydroxypropyl β-cyclodextrin is 1:10). This clathrate is easily soluble in water and can be used as a raw material to make injections, powder injections or infusions.

Embodiment 3

[0006] Example 3: Weigh 3 g of hydroxypropyl β-cyclodextrin, place it in 20 ml of water for injection, and stir to dissolve. Another 0.1g of houttuyfonate sodium was added to the above hydroxypropyl β-cyclodextrin solution and stirred at room temperature for 20 minutes to obtain a clear and transparent solution (the weight ratio of drug to hydroxypropyl β-cyclodextrin was 1: 30).

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PUM

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Abstract

A houttuyninum sodium injection is prepared through dissolving hydroxypropyl beta-cyclodextrin in water for injection while stirring, adding houttuyninium sodium, stirring or grinding and vacuum (or spray) drying or freeze drying. Its advantages are high safety and high stability.

Description

Technical field: [0001] The invention relates to the technical field of medicine, and to be precise, it is a preparation method of houttuyfonate sodium injection. Background technique: [0002] Houttuyfonate sodium, also known as houttuyfonate, is a sodium bisulfite adduct of decanoyl acetaldehyde. It is the first effective antibacterial and anti-inflammatory drug used in clinical practice in China (Zheng Junmin et al. Synthetic houttuyfonate more Research on crystal form and bioavailability, Journal of Shenyang College of Pharmacy, 1981, Issue 13, P51), pharmacological experiments show that its inhibitory concentration against influenza bacillus is 1.25mg / ml, resistant Staphylococcus aureus is 0.08mg / ml, typhoid bacillus 1.25mg / ml, Mycobacterium tuberculosis 16ug / ml, the inhibitory concentration against Candida albicans, Cryptococcus neoformans, rubella rubrum, Trichophyton… etc. are all 2ug / ml; it can also increase the phagocytic ability of white blood cells and increase prepar...

Claims

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Application Information

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IPC IPC(8): A61K31/121A61P31/04
Inventor 邓意辉
Owner SHENYANG PHARMA UNIVERSITY
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