Method for preparing polymer aqueous solution formulation of taxane anti-tumor medicament

A technology of anti-tumor drugs and taxanes, which is applied in the directions of anti-tumor drugs, drug combinations, and pharmaceutical formulations, can solve the problems of ethanol irritation of surfactants, prone to allergic reactions, and harsh storage conditions, and achieves improved compliance. It is beneficial to the distribution and metabolism, and the effect of convenient medication

Inactive Publication Date: 2009-05-27
石茂光
View PDF1 Cites 14 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The problems of this preparation are as follows: ① Tween-80, as a cosolvent, can accelerate the oxidation of the main drug, thereby producing a variety of oxidation products of docetaxel, so the storage conditions for docetaxel injection are relatively harsh , must be stored in a refrigerator at 2-8 ° C, thus bringing a certain burd

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 polymer aqueous solution formulation of taxane anti-tumor medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Raw and auxiliary materials used in the reagent: paclitaxel 50mg, soybean lecithin 1.5g, sodium deoxycholate 1.8g, absolute ethanol 30ml, trehalose 80mg. Phosphate buffer saline (PBS, pH=7.4) 10ml.

[0052] Description of the preparation process: 1. Weigh paclitaxel, soybean lecithin, and sodium deoxycholate and dissolve them in absolute ethanol. 2. Rotate evaporation at 40°C to remove all ethanol, so that drugs, phospholipids, etc. form a dry light yellow film on the bottom of the bottle. 3. Add the PBS solution dissolved with trehalose, and dissolve the film with ultrasound or vibration. A light yellow homogeneous transparent solution was obtained. 4. Dialyze overnight with a semi-permeable membrane with a permeability limit of 8000, and replace the external fluid at intervals. A colorless homogeneous transparent solution was obtained. 5. Filter with a 0.22 μm microporous membrane. 6. Subpackage, label after freeze-drying, and store at room temperature.

[0053]...

Embodiment 2

[0055] Raw and auxiliary materials used in the reagent: 30 mg of docetaxel, 1.90 g of soybean lecithin, 1.40 g of sodium deoxycholate, PBS (pH7.2), 0.40 g of trehalose.

[0056] Description of the preparation process: the preparation process is the same as in Example 1.

[0057] Preparation traits: colorless, transparent and uniform solution, which can be stored for about 60 days. The shape of the freeze-dried product did not change significantly.

[0058] Diluted with 5% glucose solution and 0.9% normal saline respectively according to the concentration of 100mg drug / 500ml, 150mg drug / 500ml, 200mg drug / 500ml, it can exist stably for more than 3 months.

Embodiment 3

[0060] Raw and auxiliary materials used in the reagent: 30 mg of docetaxel, 0.61 g of hydroxypropyl-β-cyclodextrin, 80 mg of PEG-8000, 40 mg of F-6840 mg, 40 mg of sorbitol, and an appropriate amount of ethanol.

[0061] Description of the preparation process: 1. Accurately weigh docetaxel and F-68, dissolve in absolute ethanol, and freeze to aid in dissolution. A homogeneous colorless and transparent solution was prepared. 2 Accurately weigh hydroxypropyl-β-cyclodextrin, PEG, and sorbitol, and dissolve them in water for injection to obtain a uniform colorless and transparent solution. Slowly transfer the ethanol solution of the drug into the polymer solution in 3 portions. Avoid the appearance of air bubbles, vortices and white flocs. Mixed homogeneous colorless transparent solution. 4 Filter with a 0.22 μm microporous membrane. Pack in 5 aliquots, label after freeze-drying, and store at room temperature.

[0062] Preparation traits: colorless, transparent and uniform so...

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 relates to a developed injection preparation product. A preparation method for a polymer aqueous solution preparation for insoluble medicines of a taxanes antitumor medicine is used to prepare and produce a solution preparation product of the insoluble medicines, thereby the requirements for injection medicine are satisfied. The preparation method adopts technologies in multiple aspects such as surfactant solubilization, hydroxypropyl-beta-cyclodextrin inclusion and PEG cosolvent, PEG-modified phospholipid, additional protective agents, and the like. By adopting the technological method, the solubility of the insoluble medicines in aqueous solution can be dramatically enhanced such as paclitaxel and docetaxel, the dissolving ability of the insoluble medicines in the aqueous solution is enhanced from 2 mg/ml reported in literature to or exceeding 6 mg/ml.

Description

1. Technical field [0001] The invention relates to a method for preparing an aqueous solution preparation of insoluble drugs, which can prepare polymer aqueous solution preparations and freeze-dried products of insoluble drugs, and meet the requirements of injection medicine. Taxane drugs are used as inventions to study insoluble drugs. Process for the preparation of drug-soluble polymer solution formulations. 2. Background technology [0002] The solubilization of poorly soluble drugs is one of the important topics in pharmaceutical research. In pre-prescription research and prescription screening, drug solubility is the first item to be investigated; the development of liquid preparations is closely related to the size of drug solubility. Common methods for solubilizing insoluble drugs include adjusting the pH value, applying co-solvents, co-solvents, formation of micelles or mixed micelles, inclusion, liposome encapsulation and emulsification or microemulsion. Each of t...

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
IPC IPC(8): A61K9/08A61K31/337A61K47/48A61K47/34A61K47/40A61P35/00A61K47/10A61K47/24A61K47/61A61K47/69
Inventor 石正国
Owner 石茂光
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