Panaxatriol supersaturated self-microemulsion and preparation method thereof

A technology of panaxatriol and self-microemulsion, which is applied in the field of medicine, can solve the problems of panaxatriol dosage forms and applications that have not been documented or reported, and achieve the effects of improving bioavailability, improving bioavailability, and inhibiting growth

Active Publication Date: 2019-12-31
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese Patent No. 200710143390.8 discloses an invention patent named "Silibinin Supersaturated Self-Microemulsion Composition and Its Preparation Method", which is about preparing silybin into a supersaturated self-microemulsion to improve its stability research; Chinese Patent No. 201210443006.7 discloses an invention patent titled "a 20(S)-protopanaxadiol self-microemulsion composition and its preparation method and application", which is to prepare protopanaxadiol into Self-microemulsion oral preparation capsules, through in vivo experiments, verify that its dosage form can improve the absorption of protodiol in the body, but there is no literature record or report on the dosage form and application of panaxatriol

Method used

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  • Panaxatriol supersaturated self-microemulsion and preparation method thereof
  • Panaxatriol supersaturated self-microemulsion and preparation method thereof
  • Panaxatriol supersaturated self-microemulsion and preparation method thereof

Examples

Experimental program
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Effect test

example 1

[0039] Prescription Screening:

[0040] Prescription 1: The selected oil phase, emulsifier, co-emulsifier, and polymer are ethyl oleate, Tween 80, 1,2-propylene glycol, and hydroxypropylmethylcellulose (HPMC), and the respective mass percentages are oil Phase: emulsifier: co-emulsifier: panaxatriol: hydroxypropylmethylcellulose = 20%: 54%: 24%: 1%: 1%.

[0041] Prescription 2: The selected oil phase, emulsifier, co-emulsifier, and polymer are ethyl oleate, Tween 80, 1,2-propylene glycol, and carboxymethylcellulose sodium (CMC-Na), respectively, with their respective mass percentages It is oil phase: emulsifier: co-emulsifier: panaxatriol: sodium carboxymethylcellulose=20%: 54%: 24%: 1%: 1%.

[0042] Prescription 3: The selected oil phase, emulsifier, co-emulsifier, and polymer are ethyl oleate, Tween 80, 1,2-propylene glycol, and polyvinylpyrrolidone (PVP), and the respective mass percentages are oil Phase: emulsifier: co-emulsifier: panaxatriol: polyvinylpyrrolidone = 20%: ...

example 2

[0059] Weigh panaxatriol, ethyl oleate, Tween 80, 1,2-propanediol, panaxatriol and hydroxypropylmethylcellulose according to the ratio of the composition of the preferred prescription 1 (as shown in Table 3), and carry out according to the preparation method Vortex and mix well to prepare panaxatriol supersaturated self-microemulsion; the prepared panaxatriol supersaturated self-microemulsion can be packed into hard gelatin capsules to obtain capsules convenient for oral administration.

[0060] table 3

[0061]

[0062] Particle size determination:

[0063] The prepared prescription 1 panaxatriol supersaturated self-microemulsion was diluted 50 times with distilled water, and stirred evenly. Get an appropriate amount of diluted solution, measure the diluted S-SEDDS particle size and distribution by a particle size analyzer (Malvern-ZEN3700 USA), the laser particle size analyzer measurement results show that the average particle size of prescription 1 is 22.42 ± 1.5nm, pol...

example 3

[0075] Weigh panaxatriol, ethyl oleate, Tween 80, 1,2-propanediol, panaxatriol and hydroxypropyl methylcellulose according to the ratio of the formula composition in Table 5, and vortex and mix according to the preparation method (1) to prepare Obtain panaxatriol supersaturated self-microemulsion; the prepared panaxatriol supersaturated self-microemulsion can be packed into hard gelatin capsules to obtain capsules that are convenient for oral administration.

[0076] table 5

[0077]

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Abstract

The invention belongs to the technical field of medicines, and relates to a panaxatriol supersaturated self-microemulsion and a preparation method thereof. The panaxatriol supersaturated self-microemulsion consists of panaxatriol and a supersaturated self-microemulsion system, wherein the supersaturated self-microemulsion system is composed of an oil phase, an emulsifier, a co-emulsifier and polymers. The panaxatriol supersaturated self-microemulsion specifically consists of the following ingredients in the following percent weight in volume: 0.1-10% of the panaxatriol, 10-50% of the oil phase, 30-70% of the emulsifier, 10-30% of the co-emulsifier, and 0.5-10% of water-soluble cellulose. Compared with conventional self-microemulsions, the panaxatriol supersaturated self-microemulsion is capable of effectively delaying drug precipitation so as to improve emulsion stability; and moreover, the panaxatriol supersaturated self-microemulsion prepared by the preparation method is capable of effectively improving bioavailability of the panaxatriol in vivo. Pharmacokinetic experiments have proven that the bioavailability of the panaxatriol supersaturated self-microemulsion is improved by 2.7 times compared with bulk drugs.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a panaxatriol supersaturated self-microemulsion and a preparation method thereof. Background technique [0002] As the main active ingredient of ginseng plants, ginsenosides have good pharmacological effects in many aspects. Ginsenosides are triterpenoid saponins, which can be divided into dammarane-type tetracyclic triterpene saponins and oleanane-type pentacyclic triterpene saponins according to their core structures. The content of tetracyclic triterpene ginsenosides accounts for the vast majority of ginsenosides, which has attracted people's attention and research. And this kind of saponins can be hydrolyzed to produce different saponins. Protopanaxatriol is a kind of saponins after the decomposition of saponins. This kind of saponins can be hydrolyzed with strong acid to generate panaxatriol (panaxadiol) with three -OH groups. Panaxatriol has a protective effect on the card...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/58A61K47/10A61K47/14A61K47/26A61K47/38A61K47/44A61P9/10
CPCA61K9/1075A61K31/58A61K47/44A61K47/14A61K47/26A61K47/10A61K47/38A61P9/10
Inventor 韩静田园园韩阳
Owner SHENYANG PHARMA UNIVERSITY
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