Isolorydine clathrate and preparation method thereof

A technology of isoclidine and inclusion complex, applied in the field of isoclidine inclusion complex and preparation thereof, can solve problems such as eye irritation, and achieve the effect of improving solubility and good water solubility

Inactive Publication Date: 2017-08-04
YUNNAN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But because isocridine is insoluble in water, need to adopt hydrochloride to make eye drop in preparation process, because of containing isocridine hydrochloride (effective concentration 5mg / ml) eye drop pH value is at 4.4-5.6, Eye irritation during clinical use limits its use

Method used

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  • Isolorydine clathrate and preparation method thereof
  • Isolorydine clathrate and preparation method thereof
  • Isolorydine clathrate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1 Preparation of Isocridine Hydroxypropyl-β-cyclodextrin Inclusion Compound Solution

[0043] 1. Prescription (isocredine: hydroxypropyl-β-cyclodextrin molar ratio 1:1)

[0044] Isocridine 45mg

[0045] Hydroxypropyl-β-cyclodextrin 180mg

[0046] Second, the method

[0047] (1) Weigh 180 mg of hydroxypropyl-β-cyclodextrin, add it to 50 ml of distilled water, stir to dissolve;

[0048] (2) Weigh 45 mg of isocridine, add 50 ml of ethanol solution with a concentration of 20% by volume to dissolve and make an isocridine solution, and add the solution dropwise to the above-mentioned hydroxypropyl-β-cyclodextrin solution , the mixed solution was stirred at room temperature for 2 hours by a stirring method to obtain an isocridine hydroxypropyl-β-cyclodextrin solution;

[0049] (3) Remove the ethanol by rotary evaporation under reduced pressure, add 50 ml of distilled water to filter, remove the unincluded drug, and obtain the hydroxypropyl-β-cyclodextrin inclusion ...

Embodiment 2

[0050] Example 2 Preparation of solid isocridine hydroxypropyl-β-cyclodextrin inclusion compound

[0051] 1. Prescription (isocredine: hydroxypropyl-β-cyclodextrin molar ratio 1:1)

[0052] Isocridine 45mg

[0053] Hydroxypropyl-β-cyclodextrin 180mg

[0054] Second, the method

[0055] Steps (1), (2), (3) are the same as in Example 1.

[0056] Drying the isocredine hydroxypropyl-β-cyclodextrin inclusion compound solution under reduced pressure to obtain a solid isocredine hydroxypropyl-β-cyclodextrin inclusion compound.

Embodiment 3

[0057] Example 3 Preparation of solid isocridine hydroxypropyl-β-cyclodextrin inclusion compound

[0058] 1. Prescription (isocredine: hydroxypropyl-β-cyclodextrin molar ratio 1:1)

[0059] Isocridine 45mg

[0060] Hydroxypropyl-β-cyclodextrin 180mg

[0061] Second, the method

[0062] (1) Weigh 180 mg of hydroxypropyl-β-cyclodextrin, put it into a mortar, add 2 ml of distilled water, and grind to make a paste.

[0063] (2) Take 45 mg of isocridine, add 15 m of ethanol solution with a concentration of 20% by volume to dissolve, add the solution to the hydroxypropyl-β-cyclodextrin solution obtained in step (1), and grind the mixed solution 2 hours, obtain homogeneous paste;

[0064] (3) Concentrate and dry under reduced pressure to obtain solid isocridine hydroxypropyl-β-cyclodextrin inclusion compound.

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Abstract

The invention relates to an isolorydine clathrate and a preparation method thereof, particularly relates to an isolorydine cyclodextrin or cyclodextrin derivative clathrate, a preparation method thereof, a medicine composition comprising isolorydine cyclodextrin or cyclodextrin derivative clathrate and application to preparation of medicines thereof, and belongs to the field of medicine preparations. The isolorydine clathrate comprises isolorydine, cyclodextrin or cyclodextrin derivatives; the molecular molar ratio of isolorydine to cyclodextrin or cyclodextrin derivatives is (1 to 1)-(1 to 50). The isolorydine clathrate has the advantages that the solubility of isolorydine is improved, the clathrate has the characteristics of high water solubility and low eye irritation and the like, the problems in the prior art are solved, and the clathrate is suitably prepared into liquid preparations such as eye drops.

Description

technical field [0001] The invention relates to an isocridine inclusion compound and a preparation method thereof, in particular to an isocridine cyclodextrin or a cyclodextrin derivative inclusion compound, a preparation method thereof, an isocridine cyclodextrin or a The pharmaceutical composition of cyclodextrin derivative inclusion complex and the application in preparation of medicine belong to the field of pharmaceutical preparations. Background technique [0002] Isocorydine, alias: Isocorydine, English name: Isocorydine, molecular formula: C 20 h 23 o 4 N, molecular weight: 340.36. It is white needle-like or columnar crystal; odorless, very bitter taste. Almost insoluble in water, soluble in ethanol. Its structural formula is as follows: [0003] [0004] Isocolidine is an alkaloid extracted from the dried root of Zijinlong, a traditional herbal medicine of the Bai nationality. It is suitable for juvenile myopia, pseudomyopia and eye fatigue caused by conti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/61A61K31/473A61K9/08A61P27/02A61P27/10
CPCA61K9/0048A61K31/473
Inventor 杨竹雅张宝洪陈颖沈悦海张彬若
Owner YUNNAN UNIV OF TRADITIONAL CHINESE MEDICINE
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