Preparation method of doxofylline injection

A technology of doxofylline and injection, applied in the field of medicine, can solve the problems of inconvenient clinical use, increased substance content and the like, and achieve the effects of low equipment cost, good repeatability, huge social and economic benefits

Active Publication Date: 2019-06-04
浙江长典药物技术开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The water injection is placed at 0-10°C to precipitate crystals. Although it can still be used after being heated at high temperature, it is obviously extremely inconvenient to use clinically and will lead to an increase in the content of related substances.

Method used

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  • Preparation method of doxofylline injection
  • Preparation method of doxofylline injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Dissolve 11.6g of hydroxypropyl-β-cyclodextrin (molecular weight: 1541) in 100mL of water for injection; adjust the pH to 2 with phosphoric acid, then add 0.25g of L-serine, stir to dissolve, and obtain serine-containing hydroxyl Propyl-β-cyclodextrin aqueous solution; then add 2g doxofylline, stir at 35°C and 300prm for 1.5h, then adjust the pH to 5.2 with sodium hydroxide solution, filter through a 0.45μm microporous membrane, and dilute with 5mL Each branch was packed in vials, and autoclaved for 30 minutes to obtain the doxofylline injection of Example 1.

Embodiment 2

[0043] Dissolve 10.2g of hydroxypropyl-β-cyclodextrin in 100mL of water for injection; adjust the pH to 2.5 with phosphoric acid, then add 0.38g of L-serine, stir to dissolve, and obtain hydroxypropyl-β-cyclodextrin containing serine Cyclodextrin aqueous solution; then add 2g doxofylline, stir at 30°C and 200prm for 1h, then adjust the pH to 5.6 with sodium hydroxide solution, filter through a 0.45μm microporous membrane, and pack in cillin at 5mL / cartridge In the bottle, autoclave 30min obtains the doxofylline injection of embodiment 2.

Embodiment 3

[0045] Dissolve 12.9g of hydroxypropyl-β-cyclodextrin in 100mL of water for injection; use phosphoric acid to adjust the pH=2.3, then add 0.12g of L-serine, stir to dissolve, and obtain hydroxypropyl-β-cyclodextrin containing serine Cyclodextrin aqueous solution; then add 2g doxofylline, stir at 40°C and 400prm for 1.5h, then adjust the pH to 5.2 with sodium hydroxide solution, filter through a 0.45μm microporous membrane, and pack in 5mL / cartridge In the vial, autoclave for 30 minutes to obtain the doxofylline injection of Example 3.

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Abstract

The invention discloses a preparation method of doxofylline injection. The method comprises the following steps of enabling hydroxypropyl-beta-cyclodextrin to dissolve in water for injection, and regulating the pH value with acid; adding amino acids, and performing stirring until a dissolving state is obtained so as to obtain an hydroxypropyl-beta-cyclodextrin aqueous solution containing amino acids; adding doxofylline, performing stirring, and regulating the pH value with alkali; and performing filtration with a 0.45[mu]m millipore filter, performing subpacking in vials, and performing hot pressing for sterilization. The concentration of the doxofylline injection is greater than that of injection for sale, and the doxofylline injection has excellent low temperature decentralized stabilityand chemical stability.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a doxofylline pharmaceutical preparation, in particular to a preparation method of doxofylline injection. Background technique [0002] Doxofylline is a purine alkaloid substance, which was first developed and marketed by Italian ABC Company. It is obtained by introducing a dioxolane structure at the N-7 position of theophylline; it was launched in my country in 1998. [0003] The chemical name of doxofylline is: 7-(1,3-dioxolan-2-ylmethyl)theophylline, and its molecular weight is 266.26. Doxofylline is white needle crystal or crystalline powder, slightly soluble in water, ethanol and acetone, slightly soluble in 0.1mol / L hydrochloric acid solution. Doxofylline for injection, doxofylline tablets, doxofylline capsules and doxofylline raw materials have all been recorded in the second part of the Chinese Pharmacopoeia 2015 edition. [0004] Like aminophylline, doxofylline relaxes ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/522A61K47/69A61K47/18A61P11/00A61P11/06
Inventor 陈宇东
Owner 浙江长典药物技术开发有限公司
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