Orthokoumine microemulsion and preparation method thereof

A technology of evergreen kinesine and microemulsion, applied in the field of evergreen kinesine microemulsion and its preparation, can solve the problems of low bioavailability and poor solubility of kinesine, and improve the bioavailability of drugs High degree, easy preparation, good stability

Active Publication Date: 2021-09-28
FUJIAN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The object of the present invention is to provide a kind of evergreen kinesine microemulsion and preparation method thereof, to solve the problems of poor solubility and low bioavailability of kinesine evergreen

Method used

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  • Orthokoumine microemulsion and preparation method thereof
  • Orthokoumine microemulsion and preparation method thereof
  • Orthokoumine microemulsion and preparation method thereof

Examples

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preparation example Construction

[0028] The present invention also provides a preparation method of evergreen gynecine microemulsion, comprising the following steps:

[0029] S1. Mixing polyoxyethylene hydrogenated castor oil and 1,2-propylene glycol to obtain a first mixture;

[0030] S2. Mixing the obtained first mixture with macrogol glyceride oleate to obtain a second mixture;

[0031] S3, mixing the obtained second mixture with water to obtain a third mixture;

[0032] S4. Mixing the third mixture obtained with gynecine evergreen to obtain a fourth mixture;

[0033] S5. The obtained fourth mixture is sequentially subjected to ultrasonic and centrifugation treatment to obtain evergreen gynecine microemulsion.

[0034] The frequency of the ultrasound in the method for preparing the evergreen microemulsion of the present invention is preferably 10-30KHz, more preferably 15-25KHz, and still more preferably 18-22KHz. In the present invention, the ultrasonic time is preferably 5-20 minutes, more preferably ...

Embodiment 1

[0039] Get 18 parts of polyoxyethylene hydrogenated castor oil and 19 parts of 1,2-propanediol and mix evenly;

[0040] Add 5 parts of macrogol glyceride oleate and mix well;

[0041] Add 55 parts of distilled water and mix well;

[0042] Add 0.15 parts of Gelclesine evergreen, vortex mix, ultrasonicate at a frequency of 20KHz for 10min, centrifuge at 15000r / min for 10min to get the supernatant, the supernatant is Gelkinine evergreen microemulsion.

Embodiment 2

[0044] Get 19.55 parts of polyoxyethylene hydrogenated castor oil and 19.25 parts of 1,2-propanediol and mix evenly;

[0045] Add 5 parts of macrogol glyceride oleate and mix well;

[0046] Add 56.2 parts of distilled water and mix well;

[0047] Add 0.205 parts of Gelclesine evergreen, vortex mix, ultrasonicate at a frequency of 20KHz for 10 minutes, and centrifuge at 15000r / min for 10 minutes to get the supernatant, which is the Gelsynine evergreen microemulsion.

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Abstract

The invention provides an orikoumine microemulsion and a preparation method thereof, and belongs to the technical field of medical materials. The orikoumine microemulsion is prepared by reasonably proportioning orikoumine, polyethylene glycol oleate glyceride, polyoxyethylene hydrogenated castor oil, 1, 2-propylene glycol and water. The orikoumine microemulsion overcomes the problems of poor solubility and low bioavailability of orikoumine in the prior art. The drug loading capacity of orikoumine can reach 2200mg.L <-1>, and the solubility in water is improved by 7.07 times. The orikoumine microemulsion has the advantages of high drug loading capacity, accordance with microemulsion standards, good stability, strong solubilizing ability, simple preparation and the like, can improve the bioavailability of drugs when applied to mucosal administration, is convenient and safe to prepare, and is expected to be applied clinically.

Description

technical field [0001] The invention relates to the technical field of medical materials, in particular to an evergreen gynecine microemulsion and a preparation method thereof. Background technique [0002] Gelclesine evergreen is a trace amount of yohimbine-type alkaloids in Gelkins. It has been reported in the literature that Gelclesine Evergreen is a non-toxic anti-cancer small molecule drug, which has attracted widespread attention due to its significant anti-tumor and other biological activities . In the prior art, there are many studies on Gelsynine evergreen. For example, the evaluation and screening of anti-tumor drug efficacy found that Gelsynine evergreen has a significant anti-glioma effect, and its effective anti-tumor concentration is as low as 0.273 μg·mL -1 ; Oral gavage of evergreen gynecine 2g kg to mice -1 It was found that the mice survived within 1 week after administration, and the evergreen gynecine with a mass concentration of 1% had no toxic effect ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/4375A61K36/56A61K47/10A61K47/14A61K47/44A61P35/00
CPCA61K31/4375A61K36/56A61K9/1075A61K47/14A61K47/44A61K47/10A61P35/00Y02A50/30
Inventor 吴水生蒋文文宋煜李高攀
Owner FUJIAN UNIV OF TRADITIONAL CHINESE MEDICINE
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