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Anidulafungin nanoparticles, and preparation method thereof

A technology of anidungin and nanoparticles, which is applied in the field of medicine, can solve the problems of difficulty in making oral preparations, easy degradation, and low bioavailability, and achieve the effects of facilitating absorption, low drug degradation rate, and protecting drugs

Inactive Publication Date: 2014-07-02
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the physical properties of anidulungin being insoluble in water, on the one hand, it is difficult to make it into oral preparations; , and is easily degraded in the process of gastrointestinal absorption
Therefore, there are currently no reports on oral anidulungin formulations

Method used

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  • Anidulafungin nanoparticles, and preparation method thereof
  • Anidulafungin nanoparticles, and preparation method thereof
  • Anidulafungin nanoparticles, and preparation method thereof

Examples

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preparation example Construction

[0051] The preparation method of the anifungin nanoparticles provided by the invention is as follows: take a carrier and an oil phase solvent to prepare an oil phase; take anidulungin, water and latent solvent to prepare an inner water phase; mix the oil phase and the inner water phase through the second First ultrasonic emulsification to obtain colostrum; take surfactant and water to prepare an external water phase; mix colostrum and external water phase to undergo second ultrasonic emulsification to obtain double emulsion, dry and wash to obtain.

[0052] In the preparation method of the anidfungin nanoparticles provided by the present invention, when the volume ratio of the inner water phase to the oil phase is 1:3-1:20, the emulsification effect is better.

[0053] In order to improve the emulsification effect, the volume ratio of the oil phase to the external water phase in the preparation method of the anidfungin nanoparticles provided by the present invention is 1:3-1:30...

Embodiment 1

[0078] The preparation of embodiment 1 Anifungin nanoparticles

[0079] Weigh 120mg of lactide-glycolide copolymer and dissolve it in 120mL of dichloromethane, let it dissolve fully, and it becomes the oil phase; weigh 200mg of anidifungin and dissolve it in 40mL of water and ethanol (volume ratio is 1:3) In the mixed liquid, it is the inner water phase; the oil phase is placed in an ultrasonic cell pulverizer for the first ultrasonic emulsification, the time is 6min, and the power is 50W. During the ultrasonic process, the inner water phase is added dropwise to the oil phase to form colostrum W / O; Weigh 0.36g of polyvinyl alcohol and dissolve it in 360mL of purified water to form the external water phase; add the colostrum dropwise into the external water phase, and perform the second ultrasonic emulsification for 3 minutes, with a power of 400W, to form double emulsion W / O / W; use magnetic stirring to evaporate to remove the oil phase solvent; collect the solid by ultracentr...

Embodiment 2

[0080] The preparation of embodiment 2 Anifungin nanoparticles

[0081]Weigh 600 mg of lactide-co-glycolide copolymer and dissolve it in 120 mL of dichloromethane, place it to fully dissolve, and it is an oil phase; weigh 2 g of Anifungin and dissolve it in 40 mL of water-ethanol-glycerin (volume ratio is 2: 3:3) in the mixed liquid, which is the inner water phase; put the oil phase in the ultrasonic cell pulverizer for the first ultrasonic emulsification, the time is 5min, the power is 400W, and the inner water phase is added dropwise to the oil phase during the ultrasonic process to form Colostrum W / O; weigh 8g of polyvinyl alcohol and dissolve it in 360mL of purified water to form the external water phase; add the colostrum dropwise into the external water phase, and perform the second ultrasonic emulsification for 4 minutes, with a power of 50W, to form Double emulsion W / O / W; use magnetic stirring to evaporate and remove the oil phase solvent; collect the solid by ultracen...

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Abstract

The invention belongs to the technical field of medicine, and especially relates to anidulafungin nanoparticles, and a preparation method thereof. The anidulafungin nanoparticles comprise anidulafungin, a carrier, and a surfactant; and particle size of the anidulafungin nanoparticles ranges from 50 to 500nm. The preparation method comprises following steps: an oil phase and an internal water phase are prepared respectively; the oil phase is mixed with the internal water phase, and an obtained mixture is subjected to first ultrasonic emulsification so as to obtain an initial emulsion; an external water phase is prepared; the initial emulsion is mixed with the external water phase, and an obtained mixed material is subjected to second ultrasonic emulsification so as to obtain a composite emulsion; the composite emulsion is dried and washed so as to obtain the anidulafungin nanoparticles. According to the anidulafungin nanoparticles, anidulafungin is encapsulated by a nanoparticle carrier system, so that stability, dissolution rate, and bioavailability are increased. In addition, a cosolvent is introduced in preparation processes of the anidulafungin nanoparticles, and is removed in subsequent steps, so that a solubility problem of anidulafungin is solved, and quality of the anidulafungin nanoparticles is improved.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to anidfungin nanoparticles and a preparation method. Background technique [0002] Anifungin, the English name is Anidulafungin, and the molecular formula is C 58 h 73 N 7 o 17 , the molecular weight is 1140.24, and the density is 1.47g / cm 3 , the boiling point is 1477°C at 760mmHg atmospheric pressure, the flash point is 847°C, its structure is shown in formula I, it belongs to amphotericin B derivatives, the solid form is white powder, easy to decompose, insoluble in water, slightly soluble in ethanol, Soluble in dimethyl sulfoxide. [0003] [0004] Formula I [0005] Anifungin is an antifungal drug that belongs to the class of anti-infective drugs systemic antifungal drugs. It mainly treats candidemia and other forms of candida infection (abdominal abscess, peritonitis) and esophageal candidiasis. Research presented at the 2005 ICAAC meeting showed that anidifungin ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K38/12A61P31/10
Inventor 徐春莲郑春莲马亚平袁建成
Owner HYBIO PHARMA