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Ligustilide cyclodextrin or its derivatives clathrate, its preparation method and pharmaceutical formulation

A technology of ligustilide and pharmaceutical preparations, which is applied in drug delivery, drug combination, and pharmaceutical formulations to achieve good dissolution, increased stability, and high bioavailability

Inactive Publication Date: 2006-02-15
钱忠明 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] No matter what kind of disease is being treated, without exception, the pharmaceutical preparations used need to be released quickly and achieve the therapeutic effect quickly. The

Method used

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  • Ligustilide cyclodextrin or its derivatives clathrate, its preparation method and pharmaceutical formulation
  • Ligustilide cyclodextrin or its derivatives clathrate, its preparation method and pharmaceutical formulation

Examples

Experimental program
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Effect test

Embodiment 1

[0032] (1) Preparation of ligustilide hydroxypropyl-β-cyclodextrin inclusion compound

[0033] Weigh 40g (0.0258mol) of hydroxypropyl-β-cyclodextrin into 100ml of distilled water, fully stir to dissolve; take 1g (0.0052mol) of cis-ligustilide and dilute with 2ml of absolute ethanol, add the above-mentioned hydroxypropyl Base-β-cyclodextrin solution, magnetically stirred for 30 minutes, the stirring speed should be such that the liquid does not splash out, observe the solution until it is clear and transparent, and the liquid ligustilide hydroxypropyl-β-cyclodextrin inclusion compound is obtained . The liquid can be made into liquid dosage forms such as water injection, oral liquid, syrup and the like. Another part of the above-mentioned liquid ligustilide hydroxypropyl-β-cyclodextrin inclusion compound was taken and packed into vials, and freeze-dried to obtain a white freeze-dried powder for future use.

[0034] (2) Detection of inclusion degree

[0035] Since the inclusio...

Embodiment 2

[0044] Example 2: Weigh 100 g (0.0646 mol) of hydroxypropyl-β-cyclodextrin, add 150 ml of distilled water, and stir to dissolve. In addition, weigh 5 g (0.0263 mol) of ligustilide and add 10 ml of 95% ethanol to dilute it, pour it into the above-mentioned hydroxypropyl-β-cyclodextrin solution, and stir the mixture with magnetic force for 30 minutes, and the stirring speed is such that the liquid does not splash. Preferably, observe the solution until it is clear and transparent, concentrate, and dry under reduced pressure to obtain solid ligustilide hydroxypropyl-β-cyclodextrin inclusion compound. The solid clathrate can be prepared into solid dosage forms such as tablets and capsules according to the solid preparation method.

[0045] According to the method described in Example 1, the clathrate degree, water solubility and stability of the clathrate obtained were detected. The measurement results show that the inclusion complex is complete; 1g of the inclusion complex freez...

Embodiment 3

[0046] Example 3: Weigh 40g (0.0258mol) of hydroxypropyl-β-cyclodextrin, pour it into 100ml of distilled water, stir to dissolve; take another 0.5g (0.0026mol) of cis-ligustilide, and pour it into the above-mentioned hydroxypropyl-β-cyclodextrin Propyl-β-cyclodextrin solution; placed in an ultrasonic generator, ultrasonically oscillating at 40KHz for 20 minutes, observe the solution until it is clear and transparent, pour it out and freeze-dry to obtain solid cis-ligustilide hydroxypropyl - β-cyclodextrin inclusion complex. The solid clathrate can be prepared into solid dosage forms such as granules and dispersible tablets according to the solid preparation method.

[0047] According to the method described in Example 1, the clathrate degree, water solubility and stability of the clathrate obtained were detected. The measured results show that the inclusion complex is complete; 1g of the inclusion compound freeze-dried powder can be completely dissolved by gradually adding 1....

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Abstract

The invention discloses a ligustilide cyclodextrin or its derivatives inclusion compound, which comprises molecular molar ratio of 1:1-10 ligustilide and cyclodextrin or cyclodextrin derivative. The invention also discloses the process for preparing the inclusion compound, which comprises, dissolving the cyclodextrin or cyclodextrin derivatives into water, producing solution with a concentration of 5-80%, charging ligustilide, stirring, ultrasonic oscillating or grinding.

Description

technical field [0001] The present invention relates to an inclusion compound of medicinal ingredients, its preparation method and related pharmaceutical preparations, in particular to a cyclodextrin or cyclodextrin derivative inclusion compound of ligustilide, its preparation method and related pharmaceutical preparations. Background technique [0002] Ligustilide is a water-insoluble oily substance with the following structure: [0003] [0004] Because there are asymmetric double bonds outside the ring in the structure of ligustilide, it can be divided into two isomers, cis and trans. Due to the particularity of its own structure, the cis structure is a steric dominant conformation, which is more stable than the trans form. In nature, the content of (Z)-ligustilide in medicinal materials is about 10 times that of (E)-ligustilide. Pharmacological studies have shown that ligustilide has strong pharmacological effects on the cardiovascular system, circulatory system and...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61K9/00A61P9/10A61P43/00
Inventor 钱忠明汪程远杜俊蓉
Owner 钱忠明
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