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Cyclodextrin clathrate and preparation method thereof

A cyclodextrin inclusion compound and inclusion compound technology, applied in the field of biomedicine, can solve the problems of inconvenient storage and preparation, instability, etc.

Inactive Publication Date: 2014-04-30
SHANGHAI TIANLONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

The chemical properties of ligustilide are very active, and with the continuous increase of the content of ligustilide in the extract, the instability of ligustilide becomes more prominent, and it is easy to isomerize into other butenylfuralide compounds It can also be oxidized into a variety of complex products and finally disappear after being left for a long time, which brings great inconvenience to preservation and preparation

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0032] Preparation of Hydroxypropyl Beta Cyclodextrin Aqueous Solution

[0033] Dissolve 50g of hydroxypropyl beta-cyclodextrin in 50ml of water, stir evenly, add povidone K29 / 32, and dilute to 100ml with water.

[0034] Preparation of clathrate solution

[0035] Under rapid stirring, 10 g of ligustilide and the prepared aqueous solution of hydroxypropyl beta cyclodextrin were mixed until transparent, and diluted to 200 ml with water.

[0036] Preparation of clathrates by freeze-drying

[0037] The clathrate solution prepared above is placed in an ampoule suitable for freezing and with a stopper, and placed in a freeze dryer.

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Abstract

The invention provides a cyclodextrin clathrate containing ligustilide. The cyclodextrin clathrate contains ligustilide and hydroxypropyl-beta-cyclodextrin. Ligustilide is coated with hydroxypropyl-beta-cyclodextrin so that the cyclodextrin clathrate is formed. A weight ratio of ligustilide to hydroxypropyl-beta-cyclodextrin is in a range of 10-20wt%. The cyclodextrin clathrate further comprises povidone K29 / 32. A use amount of povidone K29 / 32 is 10-50wt% of that of hydroxypropyl-beta-cyclodextrin. The cyclodextrin clathrate containing ligustilide can be processed to form tablets, capsules, powder or a powder injection and can be used for preparation of drugs for treating dysmenorrhoea.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a cyclodextrin inclusion compound containing ligustilide and a preparation method thereof. Background technique [0002] Ligustilide is the main active ingredient in the volatile oils of Angelica and Chuanxiong, which are commonly used in traditional Chinese medicine, accounting for 35% and 58% of the volatile oils of Angelica and Chuanxiong respectively. It is an important indicator for evaluating the quality of Chinese medicinal materials such as Angelica and Chuanxiong. Ligustilide has a variety of biological activities such as antispasmodic, cough and asthma, menstrual regulating and pain relief, but its in-depth preparation research is almost blank. With continuous improvement, the instability becomes more prominent and becomes a bottleneck restricting high-quality preparations. [0003] The content of ligustilide in medicinal materials varies greatly depending on the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/365A61P11/06A61P11/14A61P15/00A61K47/69
Inventor 丁杰
Owner SHANGHAI TIANLONG PHARMA
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