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Medicine hydrochloric acid fasudil composite dry suspension for treating ischemic cerebrovascular disease

A technology for fasudil hydrochloride and cerebrovascular disease, applied in the field of medicine, can solve the problems of solubility difference of crystalline drugs, large surface free energy per unit, easy hydration of the surface between particles, etc., and achieves good fluidity and bioavailability. High, safe and reliable effect in clinical application

Inactive Publication Date: 2015-12-09
杨献美
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compounds with different crystal structures are in different energy states due to the difference in molecular arrangement order. Generally, amorphous drugs have greater potential energy, and the bonding strength between particles is smaller than that of crystal forms. The total unit surface free The energy is large, and the surface between the particles is easy to hydrate, resulting in a difference in solubility from that of crystalline drugs

Method used

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  • Medicine hydrochloric acid fasudil composite dry suspension for treating ischemic cerebrovascular disease
  • Medicine hydrochloric acid fasudil composite dry suspension for treating ischemic cerebrovascular disease
  • Medicine hydrochloric acid fasudil composite dry suspension for treating ischemic cerebrovascular disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Preparation of Fasudil Hydrochloride Crystals

[0028] (1) Dissolve fasudil hydrochloride in a mixed solvent of methanol and propyl acetate, the required amount of solvent per gram of fasudil hydrochloride is 120ml, and the volume ratio of methanol to propyl acetate is 5:3;

[0029] (2) After heating to 30°C to dissolve, add seed crystals after cooling to room temperature;

[0030] (3) Cool to below -5°C, stir and crystallize, the crystallization temperature is -10°C, filter, dry, collect crystals to obtain fasudil hydrochloride crystals.

[0031] The prepared Fasudil hydrochloride crystals use Cu-Kα rays to measure the X-ray powder diffraction pattern obtained as figure 1 shown.

Embodiment 2

[0032] Example 2: The preparation of Fasudil hydrochloride dry suspension, the steps are as follows:

[0033] Prescription: Fasudil hydrochloride crystalline form compound that the embodiment 1 of 3 parts by weight makes, the mannitol of 18 parts by weight, the sodium alginate of 4 parts by weight, the locust bean gum of 1.5 parts by weight, the stearin of 0.9 parts by weight Sodium alcohol sulfonate, 0.25 parts by weight of stevia, 95% ethanol by weight.

[0034] Preparation:

[0035] (1) Processing of raw and auxiliary materials: sieve Fasudil hydrochloride through 100 mesh;

[0036] (2) Weighing: Weighing according to the prescription;

[0037] (3) Granulation: Add fasudil hydrochloride, mannitol, sodium alginate, locust bean gum, sodium stearyl sulfonate and stevia into the wet mixing granulator, dry mix for 10 minutes, and mix 95 % ethanol is added to the wet mixing granulator for wet mixing and cutting, and 18 mesh granulation is selected to make soft materials;

...

Embodiment 3

[0041] Example 3: The preparation of Fasudil hydrochloride dry suspension, the steps are as follows:

[0042] Prescription: Fasudil hydrochloride crystalline form compound that the embodiment 1 of 3 parts by weight makes, the mannitol of 19 parts by weight, the sodium alginate of 5 parts by weight, the locust bean gum of 1.6 parts by weight, the stearin of 0.95 parts by weight Sodium alcohol sulfonate, the stevioside of 0.3 weight part, the 95% ethanol of 9.5 weight part.

[0043] Preparation:

[0044] (1) Processing of raw and auxiliary materials: sieve Fasudil hydrochloride through 100 mesh;

[0045] (2) Weighing: Weighing according to the prescription;

[0046] (3) Granulation: Add fasudil hydrochloride, mannitol, sodium alginate, locust bean gum, sodium stearyl sulfonate and stevia into the wet mixing granulator, dry mix for 10 minutes, and mix 95 % ethanol is added to the wet mixing granulator for wet mixing and cutting, and 18 mesh granulation is selected to make so...

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Abstract

The invention discloses medicine hydrochloric acid fasudil composite dry suspension for treating ischemic cerebrovascular disease, and belongs to the technical field of medicine. The composite dry suspension is prepared from hydrochloric acid fasudil, mannitol, sodium alginate, locust bean gum, sodium stearyl alcohol sulfonate, steviosin and 95% ethyl alcohol. Hdrochloric acid fasudil is a new-crystal-form compound; an X-ray powder diffraction pattern obtained through measurement of Cu-K alpha rays is shown in figure 1, and hydrochloric acid fasudil is different from hydrochloric acid fasudil reported in the prior art; it is found through experiments that the new-crystal-form compound is high in purity, mobility and stability, low in impurity content, not prone to moisture absorption and safe and reliable in clinical application; the dry suspension prepared from the new-crystal-form compound is high in stability and bioavailability and quite suitable for clinical application.

Description

technical field [0001] The invention belongs to the technical field of medicines, and relates to a dry suspension of fasudil hydrochloride composition for treating ischemic cerebrovascular disease. Background technique [0002] Fasudil hydrochloride (fasudilhydrochloride, 1) is a new type of isoquinoline sulfonamide derivatives jointly developed by Asahi Kasei Co., Ltd. and Nagoya University. As a RHO kinase inhibitor and novel intracellular Ca 2+ Antagonist, the drug can dilate blood vessels by increasing the activity of myosin light chain phosphatase, reduce the tension of endothelial cells, improve the microcirculation of brain tissue, protect ischemic brain tissue, and at the same time antagonize inflammatory factors and protect nerves against apoptosis , promote nerve regeneration. In June 1995, it was listed by Asahi Kasei Corporation of Japan, and it was listed in China in 2004. It is mainly used to improve the symptoms of ischemic cerebrovascular diseases caused by...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/551C07D401/12A61P9/10
Inventor 杨献美
Owner 杨献美
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