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Asarin medical composition, preparation method and application thereof

The technology of a composition and Asarum, which is applied in the field of medicine, can solve the problems of low utilization rate of raw materials, complicated preparation method, low drug load and the like, and achieves the effects of being suitable for industrial production, simple in preparation method and prolonging action time.

Active Publication Date: 2012-08-22
南通集智知识产权服务有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, there are many types of pharmaceutical excipients used in the microemulsion, and the quality is difficult to control in actual production, and the long-term storage stability of its pharmaceutical preparations will be affected.
[0006] Chinese patent application 2009100599248 discloses an injection of asarone, which is a micellar solution, and preliminarily solves the problem of large particle size of common asarone preparations
But this scheme still has the following problems: (1) raw material utilization rate is low
(2) The drug loading is low, the drug loading of the Asarone injection prepared by the technical scheme of the invention is only about 7%, and the practicability is not high when large doses are used
(3) The preparation method is more complicated, and the method that needs to apply ultrasonic centrifugation during preparation cannot be applied to large-scale industrial production
[0008] Chinese patent application 200610020247 discloses a kind of asarone soft capsule preparation, which needs to use macromolecular substances such as vegetable oil, and also needs to use Tween and other excipients that have side effects in the medicament.
[0009] In summary, the existing technology is still unsatisfactory in improving the dissolution of asarone, and there are many problems

Method used

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  • Asarin medical composition, preparation method and application thereof
  • Asarin medical composition, preparation method and application thereof
  • Asarin medical composition, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031]

[0032]Dissolve asarone, soybean lecithin, chenodeoxycholic acid, and ethylene glycol in 5L of ethyl acetate, and stir until fully dissolved. Ethyl acetate is recovered under reduced pressure to obtain the pharmaceutical composition of the present invention.

[0033] 20,000 drop pills were prepared with five times the amount of PEG6000 as the drop pill matrix and simethicone as the cooling agent.

Embodiment 2

[0035]

[0036]

[0037] Dissolve asarone, soybean lecithin, and chenodeoxycholic acid in 1L of ethyl acetate, heat to 60°C and stir until fully dissolved. Ethyl acetate was recovered under reduced pressure to obtain the pharmaceutical composition of the present invention, which was dissolved in water and the particle size was measured to be 16nm.

[0038] Using ten times the amount of gelatin as the capsule shell liquid, the filling composition is prepared into 20,000 soft capsules.

Embodiment 3

[0040]

[0041] Dissolve asarone, soybean lecithin, sodium glycocholate, and propylene glycol in 10L of ethanol, and stir until fully dissolved. The ethanol was recovered under reduced pressure, and fully stirred and mixed at 60° C. to obtain the pharmaceutical composition of the present invention, which was dissolved in water and measured to have a particle size of 17 nm.

[0042] Prepare 50,000 dropping pills according to the method of Example 1.

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Abstract

The invention discloses an asarin medical composition which comprises asarin, phospholipid, bile acid and / or salt thereof, and water-soluble polyalcohol. The invention further discloses a preparation method of the medical composition. The invention also provides an oral preparation prepared from the medical composition.

Description

technical field [0001] The invention discloses a pharmaceutical composition of asarone, and further discloses an oral preparation of the pharmaceutical composition of asarone, which belongs to the field of medicine. Background technique [0002] Asarone, extracted from the volatile oil of Shichangpu, can also be synthesized by chemical methods. Studies have found that asarone has the effects of relieving cough, eliminating phlegm, relieving asthma, sedation, antispasmodic, anticonvulsant, etc., and can also inhibit the growth of pneumococcus, staphylococcus aureus and Escherichia coli. [0003] The solubility of asarone in water is very low, depending on the temperature, its solubility is between 0.1-1mg / ml, and the solubility in common organic solvents such as ethanol and methanol can only reach 1.87mg / ml, 1.76mg / ml , it can be seen that water or common organic solvents cannot solve the dissolution problem of asarone. [0004] In order to make asarone easily soluble in wa...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/28A61K47/24A61K47/10A61K47/34A61K31/09A61K9/20A61K9/48A61P11/00A61P31/00A61P11/06A61P1/16A61P25/08A61P11/14A61P11/10A61P25/20A61P31/04A61K47/14
Inventor 郝守祝
Owner 南通集智知识产权服务有限公司