Leuprorelin slow-controlled drug release stick and preparation method thereof

A technology of leuprolide and drug release, which is applied in the direction of pharmaceutical formulations, antineoplastic drugs, drug combinations, etc., can solve problems such as inability to take out implants, polymer toxicity, and impact on patient compliance, achieving minimal side effects , high curative effect and easy operation

Active Publication Date: 2013-12-18
薛飞
View PDF2 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the implanted drug delivery system also has disadvantages: 1. When implanting, it is necessary to make a small local incision, or use a special syringe to push the implant in. If the material is not degradable, it may cause inflammation and require surgery to remove it. Therefore, patient compliance is affected; 2. The implant cannot be removed due to displacement; 3. Polymer toxicity may occur

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

[0024] The present invention lies in the preparation of the leuprolide medicine stick, and the medicine stick with sustained and controlled release is prepared by mixing the polymer material with the leuprolide, and the specific steps are as follows:

[0025] 1. Dissolve 1.114g of PLGA with high molecular weight (15000 Da) and 0.076g of PLGA with low molecular weight (1900 Da) with organic solvent ethyl acetate;

[0026] 2. Mix 0.375g of leuprolide acetate with the above solution to obtain a uniform suspension system;

[0027] 3. Dry the above suspension under vacuum conditions to remove the organic solvent to obtain a solid;

[0028] 4. Press the obtained solid at a temperature of 45° C. and a pressure of 30 kg to form a white or off-white medicinal stick with a diameter of 1.0 mm and a length of 1.5 cm.

[0029] This embodiment does not lather easily during drying and has a medium texture.

Embodiment 2

[0031] 1. Dissolve 0.749g of PLGA with high molecular weight (molecular weight: 10000 Da) and PLGA with low molecular weight (molecular weight: 1900 Da) and 0.052g with organic solvent ethyl acetate;

[0032] 2. Mix 0.252g of leuprolide acetate with the above solution to obtain a uniform suspension system;

[0033] 3. Dry the above suspension under vacuum conditions, remove the organic solvent, and obtain a solid;

[0034] 4. Press the obtained solid at a temperature of 35° C. and a pressure of 30 kg to form a white or off-white medicinal stick with a diameter of 1.0 mm and a length of 1.5 cm.

[0035] The medicinal stick made by this embodiment has lower temperature requirements in the pressing process and softer texture.

Embodiment 3

[0037] 1. Dissolve 0.749g of PLGA with high molecular weight (100000 Da) and 0.062g of PLGA with low molecular weight (1900 Da) with organic solvent ethyl acetate;

[0038] 2. Mix 0.252g of leuprolide acetate with the above solution to obtain a uniform suspension system;

[0039] 3. Dry the above suspension under vacuum conditions, remove the organic solvent, and obtain a solid;

[0040] 4. Press the obtained solid at a temperature of 90° C. and a pressure of 30 kg to form a white or off-white medicinal stick with a diameter of 1.0 mm and a length of 1.5 cm.

[0041] The medicine stick temperature that this embodiment is made requires higher, and texture is harder.

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
molecular weightaaaaaaaaaa
molecular weightaaaaaaaaaa
Login to view more

Abstract

The invention provides a leuprorelin slow-controlled drug release stick and a preparation method thereof. The preparation method comprises the following steps of mixing raw leuprorelin, high molecular weight type resin and low molecular weight type resin to obtain a solution or suspension; drying the solution in a vacuum manner; evaporating to remove a solvent to obtain a solid; pressing the solid to obtain a drug stick. The preparation method provided by the invention is simple in process and preparation is easy to carry out; the prepared leuprorelin stick is innocuous and unpoisonous to a human body, has no side effect, and is high in curative effect and is small in dose.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to the field of sustained-release implants, in particular to a leuprolide sustained-controlled release drug stick and a preparation method thereof. Background technique [0002] Sustained-release preparations mean that by delaying the release rate of the drug from the dosage form, the absorption rate of the drug into the body is reduced, so as to achieve a better therapeutic effect. However, the release rate of the drug from the preparation is affected by the external environment such as pH value. [0003] Sustained release and controlled release are collectively referred to as sustained and controlled release, which is a relatively new field in the field of pharmaceutical preparation research. Foreign countries began to study oral sustained-release and controlled-release preparations in the 1950s, and the number of drugs approved by the medical community for listing gradually inc...

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 Applications(China)
IPC IPC(8): A61K9/00A61K38/08A61P35/00
Inventor 薛飞吴学燊
Owner 薛飞
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap