Unlock instant, AI-driven research and patent intelligence for your innovation.

A kind of 20(s)-protopanaxadiol microsphere and its preparation method and application

A technology of protopanaxadiol and panaxadiol phospholipids is applied in pharmaceutical formulations, medical preparations with inactive ingredients, medical preparations containing active ingredients, etc. The effect of improved compliance, smooth surface and simple preparation method

Active Publication Date: 2016-11-09
怡瑞达(上海)医药科技有限公司
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, long-term use of these drugs has the side effects of reducing the synthesis of monoamine transmitters and inhibiting sexual function

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A kind of 20(s)-protopanaxadiol microsphere and its preparation method and application
  • A kind of 20(s)-protopanaxadiol microsphere and its preparation method and application
  • A kind of 20(s)-protopanaxadiol microsphere and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Dissolve 20mg of 20(S)-protopanaxadiol and 100mg of PLGA in 1mL of a mixed solvent composed of ethyl acetate-dichloromethane (1:4 by volume) to obtain an oil phase; The obtained oil phase was slowly injected into 50mL of water phase (an aqueous solution with a mass percent concentration of 0.5% formed by polyvinyl alcohol with a degree of polymerization of 500 and an alcoholysis degree of 88%); emulsified at a high speed of 1300r / min for 5min; Continue to stir at 850r / min for 4h to completely volatilize the organic solvents (ethyl acetate and dichloromethane) in the system; centrifuge (3000r / min, 10min) to separate, wash the collected solid with distilled water 3 times, and finally ℃ vacuum drying for 36 hours, the obtained white powder is the 20(S)-protopanaxadiol microspheres described in the invention.

[0034] 1. Appearance evaluation

[0035] Suspend an appropriate amount of the obtained 20(S)-protopanaxadiol microspheres in a solution of 0.02% (w / w) Tween 80 and ...

Embodiment 2

[0068] Dissolve 20mg of 20(S)-protopanaxadiol and 160mg of PLGA in 2mL of a mixed solvent composed of ethyl acetate-dichloromethane (1:4 by volume) to obtain an oil phase; The obtained oil phase was slowly injected into 50mL of water phase (an aqueous solution with a mass percent concentration of 0.25% formed by polyvinyl alcohol with a degree of polymerization of 500 and an alcoholysis degree of 88%); emulsified at a high speed of 1000r / min for 10min; Continue stirring at 1500r / min for 4h to completely volatilize the organic solvents (ethyl acetate and dichloromethane) in the system; centrifuge (3000r / min, 10min) to separate, wash the collected solid with distilled water 3 times, and finally ℃ vacuum drying for 36 hours, the obtained white powder is the 20(S)-protopanaxadiol microspheres described in the invention. The appearance and performance evaluation results of the microspheres obtained in this example are the same as those described in Example 1.

Embodiment 3

[0070] Dissolve 20mg of 20(S)-protopanaxadiol and 80mg of PLGA in 1mL of a mixed solvent composed of ethyl acetate-dichloromethane (1:4 by volume) to obtain an oil phase; The obtained oil phase was slowly injected into 50mL of water phase (an aqueous solution with a mass percent concentration of 0.1% formed by polyvinyl alcohol with a degree of polymerization of 500 and an alcoholysis degree of 88%); emulsified at a high speed of 1300r / min for 10min; Continue to stir at 850r / min for 4h to completely volatilize the organic solvents (ethyl acetate and dichloromethane) in the system; centrifuge (3000r / min, 10min) to separate, wash the collected solid with distilled water 3 times, and finally ℃ vacuum drying for 36 hours, the obtained white powder is the 20(S)-protopanaxadiol microspheres described in the invention. The appearance and performance evaluation results of the microspheres obtained in this example are the same as those described in Example 1.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
particle sizeaaaaaaaaaa
particle sizeaaaaaaaaaa
particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention discloses a 20 (S)-protopanaxadiol microsphere and a preparation method and application thereof. The microsphere is prepared from 20 (S)-protopanaxadiol and polylactic acid-glycolic acid or a 20 (S)-protopanaxadiol phospholipid complex and polylactic acid-glycolic acid and nano hydroxyapatite, and has an average particle size of 1-5 mum. The microsphere is prepared by an emulsified solvent evaporation method including the steps of preparation of an oil phase, emulsification after injection of the oil phase into an aqueous phase, solvent evaporation and post processing. The experimental results show that: the in-vitro long-term release curve of the 20 (S)-protopanaxadiol microsphere is in accordance with Higuchi equation without obvious burst release, the in-vitro long-term release is about 30 days, and the in-vitro long-term release effect can be achieved. The microsphere is expected to be used as an active ingredient for preparation of a sustained release agent of a drug for preventing or treating depression, and has a broad application prospect.

Description

technical field [0001] The invention relates to a 20(S)-protopanaxadiol microsphere and its preparation method and application. Background technique [0002] According to the statistics of the World Health Organization, depression may become the second largest disease after heart disease by 2020. Patients with depression are high-risk groups for suicide, and about 10% to 15% of patients may commit suicide because of this. For this kind of disease that seriously threatens human health, chemical synthetic drugs are often used clinically for treatment. In terms of treatment, western medicine antidepressants (such as commonly used amitriptyline, fluoxetine, etc.) mainly inhibit monoamines in the brain. The reabsorption of transmitters increases the content of NE, 5-HT and other transmitters in the brain. However, long-term use of these drugs has the side effects of reducing the synthesis of monoamine transmitters and inhibiting sexual function. Judging from the existing resear...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/575A61K47/34A61P25/24
Inventor 王冰陶建生陈玉玺张彤骆慧琳臧传琪
Owner 怡瑞达(上海)医药科技有限公司