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Pharmaceutical composition containing 13 glycerides, and preparation and application thereof

The technology of a pharmaceutical preparation and composition is applied in the application field of preparing anti-tumor and improving the immune function of the body, and can solve the problems such as the complex composition of coix seed oil

Active Publication Date: 2016-01-27
ZHEJIANG KANGLAITE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It can be seen that the complexity of coix seed oil components will inevitably make the quality control and clinical drug safety in the actual production process face great challenges

Method used

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  • Pharmaceutical composition containing 13 glycerides, and preparation and application thereof
  • Pharmaceutical composition containing 13 glycerides, and preparation and application thereof
  • Pharmaceutical composition containing 13 glycerides, and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0146] The preparation of embodiment 1 coix seed oil

[0147] Take 1000g of coix seed with moisture ≤10% and grind it into 100 mesh, extract with supercritical carbon dioxide, extraction temperature 50°C, extraction pressure 22Mpa, separation temperature 40°C, separation pressure 8Mpa, carbon dioxide flow rate 500L / h, continuous extraction for 3 hours, separation Obtain coix seed crude oil; add 46% petroleum ether by weight of coix seed crude oil, and 1% sodium hydroxide aqueous alkali refining; get the organic phase after liquid separation, first add 5% activated neutral alumina to filter, and the filtrate Heat to 45°C, add 4% activated kaolin to filter, remove solvent under reduced pressure, then add 10% activated neutral alumina, filter, sterilize under reduced pressure and dry heat at 170°C, cool and filter to obtain coix seed oil.

Embodiment 2

[0149] Add 8000 mg of coix seed oil to 10 ml of n-hexane to ultrasonically dissolve, and then prepare a 50 mg / mL coix seed oil solution with mobile phase acetone. Use CHEETAH-HP100 high-performance liquid phase preparative chromatograph to carry out separation; mobile phase: n-hexane: acetone = 94:6 (v / v); each separation injection volume: 15ml; chromatographic column: VenusilXBPsilica (20*250mm, 10μm) ; Flow rate: 18mL / min; ELSD detector: drift tube temperature 45°C, carrier gas flow rate 2.0L / min. Collect the chromatographic peak fraction with a retention time of 15.8 min. The receiving solution was concentrated under reduced pressure at 30°C and then transferred to a 10ml sample bottle with nitrogen gas at room temperature and blown dry with nitrogen gas to obtain 1,3-dioleic acid diglyceride.

[0150] At room temperature, colorless oil;

[0151] Q-TOF / MS: quasi-molecular ion peak [M+Na] + =m / z643.5277 (Calcd.=643.5272, C 39 h72 o 5 Na), degree of unsaturation=4,

[01...

Embodiment 3

[0157] Add 8000 mg of coix seed oil to 10 ml of n-hexane to ultrasonically dissolve, and then prepare a 50 mg / mL coix seed oil solution with mobile phase acetone. Utilize CHEETAH-HP100 high-performance liquid phase preparative chromatograph to carry out separation; Mobile phase: n-hexane: acetone=94:6 (v / v); Each separation injection volume: 15ml; Chromatographic column: VenusilXBPsilica (20*250mm, 10μm) ; Flow rate: 18mL / min. ELSD detector: drift tube temperature 45°C, carrier gas flow rate 2.0L / min. The chromatographic peak fraction with a retention time of 17 min was collected, the receiving solution was concentrated under reduced pressure at 30°C, and then transferred to a 10ml sample bottle with nitrogen gas at room temperature and blown dry with nitrogen gas to obtain 1-linoleic acid-3-oleic acid diglyceride.

[0158] At room temperature, colorless oil;

[0159] Q-TOF / MS: quasi-molecular ion peak [M+Na] + =m / z641.5121 (Calcd.=641.5115, C 39 h 70 o 5 Na), degree of ...

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Abstract

The invention relates to a pharmaceutical composition containing glycerides. Particularly, the pharmaceutical composition is composed of the following 13 compounds: 1,3-dioleic acid diglyceride, 1-linoleic acid-3-oleic acid diglyceride, 1,2-dioleic acid diglyceride, 1-oleic acid-2-linoleic acid diglyceride, 1,2-dilinolein, trilinolein, 1-olein-2,3-dilinolein, 1-palmitin-2,3-dilinolein, 1,3-diolein-2-linolein, 1-palmitin-2-linolein-3-olein, 1,3-dipalmitin-2-linolein, glyceryl trioleate, and 1-palmitin-2,3-diolein. The invention also discloses a preparation of the pharmaceutical composition, a preparing method of the pharmaceutical composition and an application of the pharmaceutical composition as anti-tumor drugs and drugs for improving the body immune functions.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular, the invention relates to a pharmaceutical composition containing 13 kinds of glycerides, a preparation, a preparation method and its application in preparing medicines for anti-tumor and improving body immune function. Background technique [0002] Coix seed is the mature and dry seed kernel of Coixlacryma-jobi L.varma-yuen (Roman.) Stapf, a plant of the genus Coix in the Poaceae family. Modern studies have found that coix seed has pharmacological effects such as analgesia, anti-inflammation, immune regulation, anti-ulcer, lowering blood fat and weight loss. In recent years, scholars at home and abroad have studied the chemical composition of coix seed by TLC, HPLC-MS, GC and other methods, and found that it contains a variety of active components, mainly including coixenolide, triglycerides, fatty acids, lactams, etc. Coix seed lactone, sugars, sterols, triterpenoids and other compounds. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/231A61P35/00A61P37/04A61K31/23
CPCA61K47/10A61K47/24A61K31/23A61K35/17A61K31/231A61K45/06A61K9/0019A61K9/4858A61P1/16A61P1/18A61P13/08A61P15/00A61P35/00A61P37/00A61P37/04A61K2300/00
Inventor 李大鹏
Owner ZHEJIANG KANGLAITE PHARM CO LTD
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