CN106511274A - Ginsenoside Rh2 ester lipidosome and preparation method and application - Google Patents
Ginsenoside Rh2 ester lipidosome and preparation method and application Download PDFInfo
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- CN106511274A CN106511274A CN201611059434.4A CN201611059434A CN106511274A CN 106511274 A CN106511274 A CN 106511274A CN 201611059434 A CN201611059434 A CN 201611059434A CN 106511274 A CN106511274 A CN 106511274A
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- ginsenoside
- ester
- lecithin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/127—Liposomes
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
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Abstract
The invention discloses ginsenoside Rh2 ester lipidosome and a preparation method and application. The ginsenoside Rh2 ester lipidosome comprises, by mass percentage, 0.2-0.7% of ginsenoside Rh2 ester, 5-10% of lecithin and 1-2% of cholesterol. The preparation method comprises the steps of weight the ginsenoside Rh2 ester, the lecithin and the cholesterol according to the proportions; adding absolute ethyl alcohol, and taking a water bath at the temperature of 50-55 DEG C till the materials are dissolved; injecting 0.01-0.02 M of a phosphate buffer solution while stirring is conducted; conducting hydration for 20-25 minutes at the temperature of 45-50 DEG C; conducting rotary evaporation to remove ethyl alcohol; conducting ultrasonic treatment for 25-35 minutes, so that the ginsenoside Rh2 ester lipidosome is obtained; and introducing N<2>, conducting sealing, and placing the ginsenoside Rh2 ester lipidosome into a refrigerator for refrigerated preservation. The invention further relates to application of the ginsenoside Rh2 ester lipidosome to preparation of injection or preparations in acceptable dosage forms. The ginsenoside Rh2 ester lipidosome and the preparation method and application are simple in preparation process and high in safety and further have the beneficial effects of being high in targeting performance, slow release property and bioavailability.
Description
Technical field
The present invention relates to pharmaceutical technology field, and in particular to a kind of ginsenoside Rh2's ester (Rh2-O) liposome and its preparation
Method.
Background technology
Ginsenoside is located away from the root of Radix Ginseng, is the topmost active component of Radix Ginseng.Research shows that ginsenoside has
Various pharmacological activities, such as the generation development of the various diseases of scalable, cancer, hypertension and atherosclerosiss etc..However, day
Right ginsenoside's absorption difference, and it is rapid to degrade in digestion.Rear major part can be in the little enteral quilt of people by oral administration for ginsenoside
Metabolism, separately has sub-fraction ginsenoside be absorbed into carrying out metabolism in people's liver, excretes with bile, only very small amount
Ginsenoside form derivative of fatty acid with internal fatty acid esterification in the liver and can stay in the body for a long time, enter
And be absorbed into blood circulation and be immediately used by the body generation pharmacologically active, it may be said that bioavailability of the ginsenoside in human body is very
It is low.
The relatively low oral bioavailability rate of ginsenoside may be higher with its own polarity and poor membrane permeability have
Close.Therefore we are to low activity, the structure of the poor ginsenoside of bioavailability carries out autotelic modification, and synthesis obtains film
The preferable ginsenoside Rh2's ester of permeability, makes liposome and improves its biological activity and bioavailability in vivo.
Liposome is the vesicle with lipid bilayer Rotating fields being self-assembly of by amphiphilics such as phospholipid,
Each vesicle contains one or more aqueous favorings and hydrophobic phase.Due to the parents characteristic of phospholipid quasi-molecule, liposome can be encapsulated
Many kinds of substance, including water solublity, fat-soluble and amphipathic medicine or functional compounds, liposome is wide in pharmaceuticals industry application
It is general, as which has the features such as targeting, slow release effect, low toxicity side effect.Liposome is mainly as medicine and active substance
Carrier is used in pharmaceuticals industry, transports the materials such as cancer therapy drug, hormone medicine.
Chinese patent literature CN105603036A disclose it is a kind of by spawn culture, choose raw material, biofermentation conversion,
Filter pressing, sterilizing, dry production are with curative effect height, purity height, the method for the ginsenoside Rh2 of good absorbing.
It is catalyst choice by the glycosyl hydrolase of aspergillus oryzae that Chinese patent literature CN104561219A is disclosed a kind of
Property catalyzing hydrolysis ginsenoside Rg3, it is rare and the ginsenoside Rh2 with higher pharmacological action to prepare the content in Radix Ginseng
Method, the method have the advantages that high selectivity, high conversion, reaction condition are gentle.
Chinese patent literature CN105287611A discloses a kind of application of ginsenoside Rh2 in Treg cells are suppressed,
Demonstrate ginsenoside Rh2, can also further to strengthen so as to improve the balance of T cell in human body by suppressing Treg cells
Autoimmune function, so as to reaching antitumor or improving the effect of immunodeficiency diseasess.
By document disclosed above can be seen that it is at present most all research ginsenoside Rh2 production method and its
Application in cell, but ginsenoside Rh2 bioavailability itself is low.Therefore, the preferable people of this research synthesis membrane permeability
Ginseng saponin Rh2 esters, make liposome and improve its biological activity and bioavailability in vivo.
The content of the invention
It is an object of the invention to make up not enough present in the problems referred to above, there is provided a kind of ginsenoside Rh2's ester liposome
Preparation method, be ginsenoside Rh2's ester further research and its application establish solid foundation.
The present invention is achieved by the following technical solutions.
A kind of ginsenoside Rh2's ester liposome of the present invention, with ginsenoside Rh2's ester as active component, lecithin,
Cholesterol is membrane material, is prepared from using alcohol injection.
Described ginsenoside Rh2's ester liposome, it is characterised in that by mass percentage, the consumption of ginsenoside Rh2's ester
For 0.2-0.7%；The consumption of lecithin is 5-10%；The consumption of cholesterol is 1-2%.
The preparation method of ginsenoside Rh2's ester liposome of the present invention, it is characterised in that described preparation method is such as
Under.
Weigh ginsenoside Rh2's ester, lecithin, cholesterol according to the above ratio, add dehydrated alcohol in 50-55 DEG C of water-bath extremely
It is molten, to be injected in the phosphate buffer of 0.01-0.02M while stirring, 45-50 DEG C of aquation 20-25min, rotary evaporation remove ethanol,
Ultrasonic 25-35min, obtains ginsenoside Rh2's ester liposome, is filled with N2Sealing, is placed in refrigerator cold-storage preservation, standby.
Lecithin of the present invention is selected from soybean lecithin, Egg Yolk Lecithin (PC-98T), stearic bicine diester lecithin, phosphatidyl gallbladder
One or more in alkali, phosphatidylinositols, PHOSPHATIDYL ETHANOLAMINE.
Cholesterol of the present invention selected from glucocorticoid, mineralocorticoid, vitamin D, the one kind in bile acid or
It is two or more.
Application of the ginsenoside Rh2's ester liposome of the present invention in the preparation for preparing injection or receptible dosage form.
The injection preparation method is as follows：100 parts of ginsenoside Rh2's ester liposome is weighed, liposome is placed in into extrusion
Extruded by 0.1-0.2 m extruded films in device, liposome solutions are obtained, add trehalose 10%, Calcium Disodium Versenate
0.05% stirring dissolves which, surplus water for injection constant volume, adjusts PH to 6.6-7.0 with hydrochloric acid or sodium hydroxide solution, then Jing
The membrane filtration of 0.22 m, sterile filling in 121 DEG C of steam sterilizations 15 minutes, are obtained small-volume injection in ampere bottle.
A kind of ginsenoside Rh2's ester liposome of the present invention, its envelop rate are 75.3-85.7%.
It is an advantage of the current invention that ginsenoside Rh2's ester liposome is produced using alcohol injection, not only preparation technology letter
It is single, it is safe, and with the high feature of targeting, slow-releasing, bioavailability.
Specific embodiment
For the ease of the understanding of those skilled in the art, with reference to example to further instruction of the present invention, embodiment party
The content that formula is referred to not limitation of the invention.
Embodiment 1.
Ginsenoside Rh2 ester 6mg, lecithin 50mg, cholesterol 10mg is weighed, and dehydrated alcohol 10ml is added in 50 DEG C of water-baths
To molten, injected in the phosphate buffer aqueous vehicles of 15ml 0.02M while stirring, 45 DEG C of aquations 20min, rotary evaporation are removed
Ethanol, ultrasonic 30min, power 100% obtain ginsenoside Rh2's ester liposome, are filled with N2Sealing, is placed in refrigerator cold-storage preservation.
Embodiment 2.
Ginsenoside Rh2 ester 9mg, lecithin 75mg, cholesterol 15mg is weighed, and dehydrated alcohol 15ml is added in 45 DEG C of water-baths
To molten, injected in the phosphate buffer aqueous vehicles of 20ml 0.02M while stirring, 50 DEG C of aquations 25min, rotary evaporation are removed
Ethanol, ultrasonic 25min, power 90% obtain ginsenoside Rh2's ester liposome, are filled with N2Sealing, is placed in refrigerator cold-storage preservation.
Embodiment 3.
Ginsenoside Rh2 ester 21mg, lecithin 175mg, cholesterol 35mg is weighed, and dehydrated alcohol 10ml is added in 50 DEG C of water
Bathe to molten, injected in the phosphate buffer aqueous vehicles of 15ml 0.02M while stirring, 45 DEG C of aquations 20min, rotary evaporation are removed
Ethanol, ultrasonic 30min, power 100% is gone to obtain ginsenoside Rh2's ester liposome, be filled with N2Sealing, is placed in refrigerator cold-storage guarantor
Deposit.
Embodiment 4.
100 parts of ginsenoside Rh2's ester liposome is weighed, liposome is placed in extruder and is extruded by 0.2 m extruded films,
Prepared liposome solutions, add trehalose 10g, Calcium Disodium Versenate 0.05g stirrings to dissolve which, use water for injection constant volume
To 100ml, PH is adjusted to 6.8 with hydrochloric acid or sodium hydroxide solution, then the membrane filtration of 0.22 m of Jing, sterile filling is in ampere bottle
In, in 121 DEG C of steam sterilizations 15 minutes, small-volume injection is obtained.
Claims (5)
1. a kind of ginsenoside Rh2's ester liposome, is characterized in that by mass percentage, and the consumption of ginsenoside Rh2's ester is 0.2-
0.7%；The consumption of lecithin is 5-10%；The consumption of cholesterol is 1-2%.
2. ginsenoside Rh2's ester liposome according to claim 1, is characterized in that described lecithin is Semen sojae atricolor lecithin
One kind or two in fat, Egg Yolk Lecithin (PC-98T), stearic bicine diester lecithin, phosphatidylcholine, phosphatidylinositols or PHOSPHATIDYL ETHANOLAMINE
More than kind.
3. ginsenoside Rh2's ester liposome according to claim 1, is characterized in that described cholesterol for sugared cortical hormone
One or more in element, mineralocorticoid, vitamin D or bile acid.
4. the ginsenoside Rh2's ester liposome described in claim 1,2 or 3 is in the preparation for preparing injection or receptible dosage form
In application.
5. the preparation method of the ginsenoside Rh2's ester liposome described in claim 1,2 or 3, is characterized in that：
Weigh ginsenoside Rh2's ester, lecithin, cholesterol according to the above ratio, add dehydrated alcohol in 50-55 DEG C of water-bath to molten,
Injected in the phosphate buffer of 0.01-0.02M while stirring, 45-50 DEG C of aquation 20-25min, rotary evaporation remove ethanol, surpassed
Sound 25-35min, obtains ginsenoside Rh2's ester liposome, is filled with N2Sealing, is placed in refrigerator cold-storage preservation.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201611059434.4A CN106511274A (en) | 2016-11-28 | 2016-11-28 | Ginsenoside Rh2 ester lipidosome and preparation method and application |
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| CN201611059434.4A CN106511274A (en) | 2016-11-28 | 2016-11-28 | Ginsenoside Rh2 ester lipidosome and preparation method and application |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110974861A (en) * | 2019-12-24 | 2020-04-10 | 贵州大学 | Blumea balsamifera oil liposome |
| CN111956614A (en) * | 2018-11-29 | 2020-11-20 | 上海参素药物技术有限公司 | Paclitaxel liposome and preparation method thereof |
| CN112754994A (en) * | 2019-11-05 | 2021-05-07 | 泰州医药城国科化物生物医药科技有限公司 | Ginsenoside liposome and preparation method thereof |
| CN115444822A (en) * | 2021-06-09 | 2022-12-09 | 厦门本素药业有限公司 | Ginsenoside epirubicin liposome, preparation method and application thereof |
| CN115444821A (en) * | 2021-06-09 | 2022-12-09 | 厦门本素药业有限公司 | Ginsenoside vincristine liposome, preparation method and application thereof |
| CN117017921A (en) * | 2023-10-08 | 2023-11-10 | 吉林农业大学 | Ginsenoside liposome and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103417479A (en) * | 2012-05-16 | 2013-12-04 | 吉林大学 | Ginsenoside Rg3 liposome and preparation method thereof |
-
2016
- 2016-11-28 CN CN201611059434.4A patent/CN106511274A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103417479A (en) * | 2012-05-16 | 2013-12-04 | 吉林大学 | Ginsenoside Rg3 liposome and preparation method thereof |
Cited By (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111956614A (en) * | 2018-11-29 | 2020-11-20 | 上海参素药物技术有限公司 | Paclitaxel liposome and preparation method thereof |
| CN111956614B (en) * | 2018-11-29 | 2022-09-30 | 上海参素药物技术有限公司 | Paclitaxel liposome and preparation method thereof |
| CN112754994A (en) * | 2019-11-05 | 2021-05-07 | 泰州医药城国科化物生物医药科技有限公司 | Ginsenoside liposome and preparation method thereof |
| CN110974861A (en) * | 2019-12-24 | 2020-04-10 | 贵州大学 | Blumea balsamifera oil liposome |
| CN110974861B (en) * | 2019-12-24 | 2022-02-01 | 贵州大学 | Blumea balsamifera oil liposome |
| CN115444822A (en) * | 2021-06-09 | 2022-12-09 | 厦门本素药业有限公司 | Ginsenoside epirubicin liposome, preparation method and application thereof |
| CN115444821A (en) * | 2021-06-09 | 2022-12-09 | 厦门本素药业有限公司 | Ginsenoside vincristine liposome, preparation method and application thereof |
| CN115444822B (en) * | 2021-06-09 | 2024-02-27 | 厦门本素药业有限公司 | Ginsenoside epirubicin liposome, and preparation method and application thereof |
| CN115444821B (en) * | 2021-06-09 | 2024-02-27 | 厦门本素药业有限公司 | Ginsenoside vincristine liposome, and preparation method and application thereof |
| CN117017921A (en) * | 2023-10-08 | 2023-11-10 | 吉林农业大学 | Ginsenoside liposome and preparation method thereof |
| CN117017921B (en) * | 2023-10-08 | 2024-03-15 | 吉林农业大学 | Ginsenoside liposome and preparation method thereof |
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Application publication date: 20170322 |