Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

A kind of preparation method of acyclovir freeze-dried preparation for injection

A technology of freeze-dried powder for injection and injection, which is applied in freeze-dried delivery, antiviral agents, inorganic non-active ingredients, etc., can solve the problems of excessive solute in the upper layer, poor clarity, loose structure, etc., to avoid side effects and clarity. Good, loose product effect

Inactive Publication Date: 2012-02-22
NORTH CHINA PHARMA COMPANY
View PDF0 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Acyclovir freeze-dried powder injection is prepared according to the conventional method. Due to the large temperature gradient inside the product during pre-freezing, the upper layer has more solutes and higher density, while the lower layer has low density and loose structure.
Therefore, the appearance of the produced product shrinks, and the reconstitution is slow and the clarity is poor
In order to solve this problem, some researchers proposed to pre-freeze by reheating. However, due to the large temperature difference between the disintegration temperature (-30°C) and the eutectic point (-8°C) of aciclovir, it is difficult to freeze Difficult to shape during drying and takes a long time to freeze-dry
For example, adding excipients such as mannitol and dextran 40 to the prescription can slightly improve the appearance of the product to a certain extent, but it still cannot solve the problems of slow reconstitution and poor clarity of the product

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Taking 100 bottles of acyclovir freeze-dried powder for injection as an example, the specific preparation method is as follows:

[0021] Dissolve 25g of acyclovir and 80ml (1mol / L) of sodium hydroxide solution in the water for injection, stir while adding, wait for the volume of the feed solution to be 250ml after the dissolution of the raw materials, and control the pH value of the intermediate to 11.5. Add 0.1% activated carbon for needles, stir at 50°C for 30 minutes, lower the temperature of the feed liquid to 25°C, then filter with a 0.22um filter membrane, measure the pH value, fill it with half stopper after the content is qualified, and then perform low-temperature freeze-drying according to the following procedures :

[0022] (a) Pre-freezing: When the temperature of the product is lowered to -10°C, the temperature difference oscillation freezing is started, the amplitude is -6°C to -15°C, and the time is 30 minutes, and then the product is cooled to -33°C, and...

Embodiment 2

[0026] Prepare 0.25g acyclovir injection according to conventional methods, then carry out low-temperature freeze-drying according to the following procedures:

[0027] (a) Cool the acyclovir injection to -12°C first, then shake and freeze it at the amplitude of -6°C to -15°C for 20 minutes; For the amplitude, shake and freeze for 40 minutes; then lower the product temperature to -50°C and keep it warm for 1 hour.

[0028] (b) Sublimation drying: Vacuumize the box to 10 Pa, raise the temperature of the product to -33~-35 °C, and keep it warm for 6 hours; fill it with nitrogen intermittently, and shake it for 1.5 hours with the air pressure in the box at 15~20 Pa as the amplitude ;Then raise the temperature of the product to -23°C and keep it warm for 15 hours;

[0029] (c) Re-drying: Gradually raise the temperature of the drug to 38° C. and keep it warm for 2 hours.

Embodiment 3

[0031] Prepare 0.25g acyclovir injection according to conventional methods, then carry out low-temperature freeze-drying according to the following procedures:

[0032] (a) Pre-freezing: When the temperature of the product is lowered to -12°C, start the shaking operation, the amplitude is -6°C to -15°C, the time is 40 minutes, and then the product is cooled to -34°C, and then the shaking operation is performed, the amplitude is -25°C to -35°C for 50 minutes, then lower the product temperature to -40°C and hold for 2 hours.

[0033] (b) Sublimation drying: After the pre-freezing process of the product is completed, start the vacuum machine to evacuate to 12 Pa, raise the temperature of the product to -33°C, keep it warm for 7 hours, and then start to pour nitrogen into the box intermittently to control the vacuum at Between 15 Pa and 20 Pa, after repeating (that is, oscillating) for 1 hour, then raise the temperature of the product to -25°C and keep it warm for 18 hours.

[00...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses a preparation method of acyclovir freeze-dried powder injection, which comprises the following steps: (a) pre-freezing: first cooling the acyclovir injection to -10°C to -12°C, and starting temperature difference oscillation Freeze; then cool down to -30°C to -33°C, shake and freeze for 40 to 60 minutes. (b) Sublimation drying: vacuumize the box to 10-15 Pa, raise the temperature of the product to -33--35°C, and keep it warm for 6-8 hours; fill it with nitrogen intermittently, with the air pressure in the box as the amplitude of 15-20 Pa, Shake for 1-1.5 hours, then raise the temperature of the product to -23-27°C, and keep it warm for 15-18 hours; (c) re-drying: gradually raise the temperature of the medicine to 38-40°C, and keep it warm for 1-2 hours. The aciclovir freeze-dried preparation prepared by the method of the invention has the characteristics of loose product, stable quality, fast reconstitution, good clarity and the like.

Description

Technical field: [0001] The invention relates to a preparation method of medicine, in particular to a preparation method of acyclovir pharmaceutical preparation. Background technique: [0002] Acyclovir (chemical name 9-(2-hydroxyethoxymethyl)guanine) is an acyclic nucleoside antiviral drug, mainly used for various infections caused by herpes simplex virus, and can be used for primary Or recurrent skin, mucous membrane, external genital infection and HSV infection in immunocompromised persons. It is the drug of choice for the treatment of HSV encephalitis, and it is superior to adenosine vidarabine in reducing morbidity and mortality. It can also be used for herpes zoster, Epstein-Barr virus, and immunodeficiency patients complicated by chickenpox, herpes zoster and other infections. It has the advantages of high selectivity, broad spectrum, high efficiency and low toxicity. Oral absorption of acyclovir is only 15% to 37%, the bioavailability is low, and the plasma concen...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/522A61K47/02A61P31/12A61P31/22
Inventor 赵辉刘书睿李晓斌张西果梁凤林李汉起王志良赵霞路玉锋
Owner NORTH CHINA PHARMA COMPANY
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com