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Match of organic medicine and beta-cyclodextrin derivative and its preparing process

A technology of beta-cyclodextrin and organic medicines, applied in botany equipment and methods, drug combinations, pharmaceutical formulations, etc., can solve the problems of dilution and redissolution instability, inability to dissolve completely, irreversibility, etc.

Inactive Publication Date: 2002-11-13
刘 云清 +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The inclusion compound prepared by the above method improves the solubility of the drug to a certain extent, but the solid powder inclusion compound cannot be completely dissolved when it is dissolved in water, or insoluble matter is precipitated when the solution is diluted with water, which is characterized in that it is resistant to dilution and Redissolution unstable, irreversible

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0017] In the present invention, more than 50 examples of various representative drugs in the Pharmacopoeia and the List of Essential Drugs are used as an example to prepare complexes with β-CD substitutes of hydroxypropyl, hydroxyethyl, sulfoalkyl, ether, methyl, and ethyl, Demonstrate the general applicability and effectiveness of the method.

[0018] 1. Antimalarial drugs: sesquiterpene lactone artemisinin and its derivatives

[0019] Artemisinin, Artesunate, Artemoter, etc.

[0020] Critical value: Molecular ratio 3-9.

[0021] 2. Macrolide antibiotics

[0022] Erythromycin, Medicamycin, Roxithromycin, Azithromycin, Clarithromycin, etc.

[0023] Critical value: Molecular ratio 6-18.

[0024] 3. Azole antifungal drugs

[0025] Itraconazole, Ketoconazole, Miconazole, Clotrimazole, etc.

[0026] Critical value: Molecular ratio 3-18.

[0027] 4. Alkaloid analgesics

[0028] Lappaconitine, Rotundine, etc.

[0029] 5. Anti-anxiety and sedative hypnotics such as azepines...

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Abstract

A mating member of organic mecicine and beta-cyclodextrin derivative is prepared from beta-CD (hydroxypropyl beta-cyclodextrin-HP-beta-CD) and organic medicinal materials or other organic molecules through recognizing and assembling in the existance of water to obtain water-soluble coordination compound. Its advantages are easy dissolving in water, high dissolving speed and infinite diluting stability.

Description

Technical field [0001] The invention relates to a complex of organic medicine and beta cyclodextrin derivatives and a preparation method thereof. Background technique [0002] When the solubility of drugs in water is below the X% order of magnitude, the development and bioavailability of pharmaceutical preparations will be limited and affected, and insoluble and insoluble in water in the Pharmacopoeia and Essential Drug List account for about one-third, increasing Its solubility in water is of great significance to improve drug efficacy. It is a method that has been studied extensively for many years by utilizing the synergistic effect of beta cyclodextrin (β-CD) or its derivatives and drugs to increase the water solubility of drugs. However, the low solubility of β-CD itself limits its application, especially when β-CD is injected intravenously, it can cause blood urea nitrogen to increase, and when it is absorbed by renal tubules, it will crystallize out due to its low wa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/02A61K9/00A61K9/08A61K9/12A61K9/14A61K9/19A61K9/20A61K9/48A61K31/045A61K31/138A61K31/167A61K31/337A61K31/357A61K31/366A61K31/40A61K31/426A61K31/43A61K31/4422A61K31/495A61K31/496A61K31/519A61K31/522A61K31/566A61K31/573A61K31/585A61K31/635A61K31/7048A61K31/7052A61K38/00A61K47/08A61K47/40A61K47/48A61P9/00A61P11/12A61P11/14A61P25/04A61P29/00A61P31/04A61P31/10A61P33/06A61P35/00A61P37/06C08B37/00C08B37/16
CPCA61K9/0019A61K47/40B82Y5/00C08B37/0012C08B37/0015A61K47/6951A61P11/12A61P11/14A61P25/04A61P29/00A61P31/04A61P31/10A61P33/06A61P35/00A61P37/06A61P9/00A01N25/00
Inventor 刘云清刘西瑛刘炜刘彤
Owner 刘 云清
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