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

Method for preparing goserelin slow-release implant

A technology of sustained-release implants and goserelin, which is applied in the pharmaceutical field, can solve the problems of reducing time cost and short solvent removal time, so as to improve production efficiency, shorten drying time, and facilitate removal

Active Publication Date: 2014-04-02
SALUS PHARMA TECH SHANGHAI
View PDF3 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In view of the above-mentioned technical problems, the object of the present invention is to provide a novel preparation method of goserelin sustained-release implants, which can effectively remove organic solvents and overcome the residual defects of existing goserelin implants solvents, And the solvent removal takes a short time, thus reducing the time cost

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

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Method for preparing goserelin slow-release implant
  • Method for preparing goserelin slow-release implant
  • Method for preparing goserelin slow-release implant

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1: Primary screening of low boiling point solvents

[0039] Commonly used organic solvents with a lower boiling point than acetic acid are: liquid ammonia, liquid sulfur dioxide, methylamine, dimethylamine, petroleum ether, ethyl ether, pentane, methylene chloride, carbon disulfide, solvent naphtha, acetone, 1,1-dichloro Ethane, chloroform, methanol, tetrahydrofuran, hexane, trifluoroacetic acid, 1,1,1-trichloroethane, carbon tetrachloride, ethyl acetate, ethanol, butanone, benzene, cyclohexane, acetonitrile, Isopropanol, ethylene glycol dimethyl ether, trichloroethylene, triethylamine, propionitrile, heptane, water, nitromethane, 1,4-dioxane, toluene, nitroethane, pyridine, 4 -Methyl-2-pentanone.

[0040] Combining the physical and chemical properties of goserelin and PLGA, especially their solubility in the above-mentioned solvents, the above-mentioned solvents were initially screened.

[0041] During the test, it was found that, except for water, ethanol, ether, a...

Embodiment 2

[0053] Example 2: Comparison of the effect of mixed solvent and single solvent acetic acid

[0054] In view of the fact that the solvent used in the preparation process of goserelin implants also has a significant impact on the release, related substances, content uniformity, content and residual solvent of the product, the mixed solvent and acetic acid obtained by preliminary screening in Example 1 The experiment is compared.

[0055] Choose a mixed solvent (acetic acid and ethanol) and a single solvent acetic acid to test. The experimental design is shown in Table 3.

[0056] Table 3 Comparison test prescription of mixed solvent and single solvent acetic acid

[0057]

[0058] Preparation Process:

[0059] 1. Dissolve. Weigh the prescription amount of goserelin, PLGA 5002A and PLGA 7502A powder or granules, add an appropriate amount of mixed solvent according to the prescription amount, and dissolve it completely into a solution under the action of stirring;

[0060] 2. Dry. Dryin...

Embodiment 3

[0225] Example 3: Using mixed solvents (acetic acid and ether) to prepare goserelin sustained-release implants

[0226] prescription:

[0227]

[0228] Preparation Process:

[0229] 1. Dissolve. Weigh the prescription amount of goserelin, PLGA 5002A and PLGA 7502A powder or granules, add an appropriate amount of mixed solvent according to the prescription amount, and dissolve it completely into a solution under the action of stirring;

[0230] 2. Dry. Drying is carried out according to the drying method in the formulation design. The process parameters for the solution to remove the solvent by freeze-drying are: pre-freeze at -20°C for 4 hours, and then at 1°C / hour, the descending rate is reduced to -50°C, and stored for 20 hours Afterwards, the temperature is raised to room temperature at 20°C / hour to prepare porous spongy fine powder;

[0231] 3. Forming. Place the collected particles or fine powder in a hot melt extruder, and extrude them under the conditions of a melting temper...

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

PropertyMeasurementUnit
wavelengthaaaaaaaaaa
wavelengthaaaaaaaaaa
separationaaaaaaaaaa
Login to View More

Abstract

The invention provides a method for preparing a goserelin slow-release implant, which comprises the step of preparing acetic acid and an organic solvent of which the boiling point is lower than that of the acetic acid into a mixed solvent, thereby dissolving goserelin and a pharmaceutically-acceptable carrier. The goserelin slow-release implant prepared by the method has the advantage that medicaments are stable, are uniformly distributed and can be stably released for a long time; and moreover, the time consumed by the preparation method is short, so that the time cost is reduced. In addition, the invention also provides the medical implant prepared by the method.

Description

Technical field [0001] The invention belongs to the field of pharmacy. Specifically, the present invention relates to a preparation method of goserelin sustained-release implant. Background technique [0002] Many drugs in the body have a short half-life and are very unstable in clinical practice. The drug stays in the body for a short time during the administration of conventional pharmaceutical preparations, and can only be administered frequently, which is inconvenient to use; and the peak-to-valley effect of the blood concentration is obvious. Severe adverse reactions may even lead to repeated episodes of the disease. Therefore, in order to effectively treat diseases, it is necessary to provide an appropriate drug delivery system to keep the blood drug concentration in the body relatively stable for a long time after drug administration, and to maintain it in the range between the minimum therapeutic level and the poisoning level, thereby improving the efficacy and safety of...

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): A61K38/08A61K9/00A61P35/00A61P15/00A61P29/00
Inventor 王诺田武王成伟
Owner SALUS PHARMA TECH SHANGHAI
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