Supermolecule water soluble freeze drying matter of indissoluble medicament and method of preparing the same

A technology for insoluble drugs and supramolecules, applied in the field of drugs, can solve the problems of microbial contamination, organic solvent residues, etc., and achieve the effects of short production cycle, improved safety and investment saving.

Active Publication Date: 2010-03-24
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to overcome the safety problems such as organic solvent residues and microbial contamination in the prior art, and provide a brand-new supramolecular water-soluble freeze-dried product of insoluble drugs that is safe, low-cost, easy to guarantee, and suitable for industrialization. Preparation

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] formula:

[0023] Artemether (fine powder 0.5μm~10μm) 12g

[0024] Hydroxypropyl-β-cyclodextrin 460g

[0025]

[0026] Water for injection 1000ml

[0027] The artemether is pulverized by a low-temperature pulverizer (0° C. to 10° C.) to obtain artemether with a particle size of 0.5 μm to 10 μm. Separately weigh the prescribed amount of hydroxypropyl-β-cyclodextrin, dissolve it in 1000ml of water to make a concentration of 46%, heat it to 50°C-60°C, add the prescribed amount of artemether, stir to dissolve, pour Packed and freeze-dried to obtain the finished product.

Embodiment 2

[0029] formula:

[0030] Artemether (fine powder 1.0μm~20μm) 12g

[0031] Sulfobutyl ether-β-cyclodextrin 460g

[0032]

[0033] Water for injection 1000ml

[0034] The artemether is pulverized by a low-temperature pulverizer (0° C. to 10° C.) to obtain artemether with a particle size of 1.0 μm to 20 μm. Separately weigh the prescribed amount of sulfobutyl ether-β-cyclodextrin, dissolve it in 1000ml of water to make a concentration of 46%, heat it to 60°C-65°C, add the prescribed amount of artemether, stir to dissolve, Filling and freeze-drying to obtain the finished product.

Embodiment 3

[0036] formula:

[0037] Artemisinin (fine powder 0.5μm~10μm) 12g

[0038] Hydroxypropyl-β-cyclodextrin 350g

[0039]

[0040] Water for injection 1000ml

[0041] The artemisinin is pulverized by a low-temperature pulverizer (0° C. to 10° C.) to obtain artemisinin with a particle size of 0.5 μm to 10 μm. Separately weigh the prescribed amount of hydroxypropyl-β-cyclodextrin, dissolve it in 1000ml of water to make a concentration of 35%, heat it to 55°C-65°C, add the prescribed amount of artemisinin, stir to dissolve, pour Packed and freeze-dried to obtain the finished product.

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PUM

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Abstract

The invention relates to a super molecule water soluble freeze-drying substance of difficult soluble drug and making method through dispensing difficult soluble drug and water soluble cyclodextrin derivative with weight ratio at 1:1-80 to form stable super molecule self-assembled water soluble substance, which is characterized by the following: the invention overcomes secure problems of organic solvent remaining in current technology and microbial contamination; the technology is simpler than current technology with short production circle and security, low production cost and supporting quality to be for industrialization. The invention has merits of stable composition and is easy to dissolve in water at fast dissolving speed and of stable injection compatibility with common clinic fluidinfusion, which guarantees drug having consistent physicochemical property before and after disintegrating because of characteristic of low-temperature micronizing technology and improves security ofagent because of not adding organic solvent, surface active agent and latent solvent.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a supramolecular water-soluble freeze-dried product of insoluble medicines and a preparation method thereof. Background technique [0002] With the development of high-throughput screening and combinatorial chemistry, most of the active compounds are usually poorly soluble compounds, and more than 40% of the candidate drugs failed in the drug development process due to poor solubility and poor biopharmaceutical properties. . Although traditional methods such as salt formation, solubilization, particle size reduction, polymorphism or solvation are widely used to enhance dissolution and improve oral absorption and bioavailability, these methods have their own limitations. For neutral compounds and some weak acids and bases, making salts is impractical. The more commonly used simple particle size reduction method has problems such as the limit of particle size reduction and the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/40A61K9/19
Inventor 陈云建黄照昌张嗣昆
Owner KPC PHARM INC
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