Freeze dried powder injecta of doxofylline and its preparation

A technology of doxofylline and freeze-dried powder injection, which is applied in the field of medicine, can solve the problems of inconvenient transportation of water injection and infusion, inconvenient use of diabetic patients, and influence on stability, so as to facilitate transportation and storage, prolong storage period, The effect of improving stability

Inactive Publication Date: 2005-06-29
武汉安士医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the injections of doxofylline only have water injection and glucose infusion. Due to the vast territory of China, the water injection is easy to freeze in winter, which affects its stability and brings about safety problems in drug use. Both water injection and infusion are inconvenient to transport. situation, its storage period is short, and glucose infusion is inconvenient for diabetic patients

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1: Under clean conditions, respectively take 100 g of doxofylline, 40 g of sorbitol, 20 g of cysteine, and 10 g of 2-hydroxypropyl β-cyclodextrin in an appropriate amount of water for injection at 20 ° C, and stir to dissolve; Adjust the acidity with succinic acid and sodium hydroxide, add 0.5g of activated carbon for needles, stir for 20min, filter and decarbonize with a 10μm titanium filter rod, after passing the pH and content determination, filter with a 0.45-0.8um microporous membrane, and then use 0.2 ~0.22um microporous membrane filtration; sterilization, depyrogenation, packaged in vials according to the dose, so that the unit dose of doxofylline in each vial is 0.1g, add a rubber stopper, put the packaged vials into In a freeze dryer, pre-freeze for 2 hours, make the temperature reach -40°C, make the vacuum degree in the machine 10Pa, low-temperature vacuum drying for 18 hours, raise the temperature to 18°C, vacuum dry for 5 hours, plug and cap. , contr...

Embodiment 2

[0021] Example 2: Under clean conditions, respectively take 300 g of doxofylline, 30 g of sodium succinate, 90 g of lysine, 30 g of 2-hydroxypropyl β-cyclodextrin, and 0.2 g of L-cysteine ​​hydrochloride Dissolve by stirring in an appropriate amount of water for injection at 20°C; adjust the acidity with gluconic acid, filter with a 5μm titanium filter rod, add water for injection, and after the pH value and content determination are qualified, sterilize by ultrafiltration twice, remove the heat source, and divide by dose. Packed in vials, so that the unit dose of doxofylline in each vial is 0.3g, add a rubber stopper, place the subpackaged vials in a freeze dryer, freeze for 3 hours, and make the temperature reach -45 ℃, Make the vacuum degree in the machine 10Pa, vacuum dry at low temperature for 30 hours, raise the temperature to 10°C, vacuum dry for 10 hours, plug and cap, and control the weight percentage of its moisture within 0.01 to 3.2%, and the pH value in Between 5 ...

Embodiment 3

[0022] Example 3: Under clean conditions, take doxofylline 600g, xylitol 10g, disodium hydrogen phosphate 10g, valine 30g, 2-hydroxypropyl β-cyclodextrin 5g, nicotinamide 20g, Dissolve 2 g of sodium sulfite in an appropriate amount of water for injection at 20°C; adjust the acidity with succinic acid and sodium hydroxide, filter and decarbonize with a 10 μm titanium filter rod, add water for injection, stir well, and after the pH value and content are qualified, the solution is passed twice. Filter and sterilize, remove the heat source, and pack it into vials according to the dosage, so that the unit dose of doxofylline in each vial is 0.3g, add a rubber stopper, place the packed vials in a freeze dryer, and freeze 2 hours, make the temperature reach -40°C, make the vacuum degree in the machine 10Pa, low temperature vacuum drying for 30 hours, raise the temperature to 10°C, vacuum dry for 10 hours, control the weight percentage of its moisture content at 0.01~3.2%, The pH valu...

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PUM

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Abstract

The invention relates to a freeze dried powder injection of doxofylline and its preparation, wherein the injection comprises Doxofylline 0.05-0.5g, and at least one pharmaceutically acceptable excipient, pH modifier, anti-oxidant agent, and stabilizer, and is provided in the form of unit amount in the container. The advantages of the invention include easy medicament transport and preservation, prevention of freezing of the liquid injection in winter, increased medicament stability, thus can be applied for effectively treating bronchial asthma, lungs disease of bronchospasm, and chronic clogged pulmonary diseases.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a doxofylline freeze-dried powder injection preparation and a preparation method thereof. Background technique [0002] Doxofylline is a new generation of methylxanthine derivatives with anti-inflammatory and bronchodilatory effects. It relaxes bronchial smooth muscle by inhibiting the concentration of calcium ions in smooth muscle cells and phosphodiesterase, and by inhibiting various inflammatory mediators, cytokines (platelet activating factor PAF, etc.) release, thereby controlling airway inflammation and reducing airway hyperresponsiveness, restoring lung function, and significantly improving the condition of patients with chronic obstructive pulmonary disease; the antiasthmatic effect of doxofylline is theophylline It is 10-15 times higher than that of aminophylline, and the side effects are significantly less than theophylline and aminophylline, and it is not n...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/522A61P11/00A61P11/16
Inventor 刘力刘珍陈祺
Owner 武汉安士医药科技有限公司
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