CN104257640A - Pterostilbene composition and preparation method thereof - Google Patents
Pterostilbene composition and preparation method thereof Download PDFInfo
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- CN104257640A CN104257640A CN201410505366.4A CN201410505366A CN104257640A CN 104257640 A CN104257640 A CN 104257640A CN 201410505366 A CN201410505366 A CN 201410505366A CN 104257640 A CN104257640 A CN 104257640A
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- Prior art keywords
- pterostilbene
- ethanol
- carnosine
- sodium stearyl
- stearyl fumarate
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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
- A61K31/075—Ethers or acetals
- A61K31/085—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon
- A61K31/09—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon having two or more such linkages
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
- A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention provides a pterostilbene composition with relatively high oral bioavailability and a preparation method of the pterostilbene composition. The pterostilbene composition provided by the invention is characterized by containing pterostilbene, sodium stearyl fumarate and L-carnosine, wherein the preferred mass ratio of the pterostilbene to the sodium stearyl fumarate to the L-carnosine is 1: 1: 1. The preparation method of the pterostilbene composition comprises the following steps: dissolving the L-carnosine by using ethyl alcohol, adding the sodium stearyl fumarate to obtain accessory dispersion, dissolving the pterostilbene by using ethyl alcohol to obtain drug dispersion, uniformly mixing the accessory dispersion with the drug dispersion, recovering the ethyl alcohol, and drying to obtain the pterostilbene composition.
Description
Technical field
The present invention relates to a kind of pterostilbene composition and method of making the same, belong to medical art.
Background technology
Pterostilbene antitumor has good effect, but causes oral administration biaavailability very low owing to being insoluble in the reason such as water and intestinal permeability difference, not yet has pterostilbene oral formulations to go on the market.
Summary of the invention
The object of this invention is to provide a kind of pterostilbene composition and method of making the same with higher oral administration biaavailability.
For foregoing invention object, the invention provides following technical scheme:
Pterostilbene compositions of the present invention, is characterized in that containing pterostilbene, sodium stearyl fumarate and L-Carnosine; The mass ratio of pterostilbene, sodium stearyl fumarate and L-Carnosine is preferably 1:1:1.
The method of pterostilbene compositions of the present invention, its preparation process is as follows:
By L-Carnosine dissolve with ethanol, then add sodium stearyl fumarate, obtain adjuvant dispersion liquid; By pterostilbene dissolve with ethanol, obtain drug susbstance dispersion; By adjuvant dispersion liquid and drug susbstance dispersion mix homogeneously, reclaim ethanol, dry, to obtain final product.
Beneficial effect of the present invention is mainly:
Compositions of the present invention significantly improves the oral administration biaavailability of pterostilbene.Preparation method of composition of the present invention is simple, cost is low, is suitable for scale preparation.Preparation method of composition of the present invention is unique, and be that the accident in great many of experiments finds, the dispersion order of adjuvant and medicine and ratio all can not adjust.Therefore the present invention adopt composition, ratio and order of addition, be innovative point of the present invention.
Detailed description of the invention
Below in conjunction with embodiment, the present invention is described in further detail, but should note scope of the present invention not by any restriction of these examples.
Embodiment 1
L-Carnosine 0.1g is dissolved in the ethanol of 100mL, then adds sodium stearyl fumarate 0.1g, obtain adjuvant dispersion liquid; By pterostilbene 0.1g 50mL dissolve with ethanol, obtain drug susbstance dispersion; By adjuvant dispersion liquid and drug susbstance dispersion mix homogeneously, 40 DEG C of vacuum reclaim ethanol, and 40 DEG C of dry 6h, to obtain final product.
Embodiment 2
L-Carnosine 0.1g is dissolved in the ethanol of 100mL, then adds sodium stearyl fumarate 0.1g, obtain adjuvant dispersion liquid; By pterostilbene 0.1g 20mL dissolve with ethanol, obtain drug susbstance dispersion; By adjuvant dispersion liquid and drug susbstance dispersion mix homogeneously, 40 DEG C of vacuum reclaim ethanol, and lyophilization, to obtain final product.
Embodiment 3
L-Carnosine 0.1g is dissolved in the ethanol of 200mL, then adds sodium stearyl fumarate 0.1g, obtain adjuvant dispersion liquid; By pterostilbene 0.1g 100mL dissolve with ethanol, obtain drug susbstance dispersion; By adjuvant dispersion liquid and drug susbstance dispersion mix homogeneously, 30 DEG C of vacuum reclaim ethanol, and lyophilization, to obtain final product.
Embodiment 4
L-Carnosine 0.2g is dissolved in the ethanol of 200mL, then adds sodium stearyl fumarate 0.2g, obtain adjuvant dispersion liquid; By pterostilbene 0.1g 50mL dissolve with ethanol, obtain drug susbstance dispersion; By adjuvant dispersion liquid and drug susbstance dispersion mix homogeneously, 40 DEG C of vacuum reclaim ethanol, and 40 DEG C of dry 6h, to obtain final product.
Embodiment 5
L-Carnosine 0.1g is dissolved in the ethanol of 100mL, then adds sodium stearyl fumarate 0.2g, obtain adjuvant dispersion liquid; By pterostilbene 0.1g 50mL dissolve with ethanol, obtain drug susbstance dispersion; By adjuvant dispersion liquid and drug susbstance dispersion mix homogeneously, 40 DEG C of vacuum reclaim ethanol, and 40 DEG C of dry 6h, to obtain final product.
Embodiment 6
By the dissolve with ethanol of pterostilbene 0.1g and L-Carnosine 0.1g 200mL, then add sodium stearyl fumarate 0.1g, mix homogeneously, 40 DEG C of vacuum reclaim ethanol, and 40 DEG C of dry 6h, to obtain final product.
Embodiment 7
Disperseed by the ethanol of pterostilbene 0.1g, L-Carnosine 0.1g, sodium stearyl fumarate 0.1g 200mL, mix homogeneously, 40 DEG C of vacuum reclaim ethanol, and 40 DEG C of dry 6h, to obtain final product.
Embodiment 8
Disperseed by the ethanol of pterostilbene 0.1g and sodium stearyl fumarate 0.1g 100mL, mix homogeneously, 40 DEG C of vacuum reclaim ethanol, and 40 DEG C of dry 6h, to obtain final product.
Embodiment 9
Disperseed by the ethanol of pterostilbene 0.1g and L-Carnosine 0.1g 200mL, mix homogeneously, 40 DEG C of vacuum reclaim ethanol, and 40 DEG C of dry 6h, to obtain final product.
Embodiment 10
By pterostilbene 0.1g, sodium stearyl fumarate 0.1g and L-Carnosine 0.1g mix homogeneously, pulverize, sieve and get final product.
Embodiment 11
By pterostilbene 0.1g and sodium stearyl fumarate 0.1g mix homogeneously, pulverize, sieve and get final product.
Embodiment 12
By pterostilbene 0.1g and L-Carnosine mix homogeneously, pulverize, sieve and get final product.
Embodiment 13
The oral administration biaavailability research of pterostilbene compositions
Laboratory animal: male SD rat 112, body weight 200-300g.
Dosage regimen: experimental mouse is divided into 14 groups at random, fasting is after 12 hours, 1st group of gavage gives pterostilbene compositions 1 (preparing by embodiment 1), 2nd group of gavage gives pterostilbene compositions 2 (preparing by embodiment 2), 3rd group of gavage gives pterostilbene compositions 3 (preparing by embodiment 3), 4th group of gavage gives pterostilbene compositions 4 (preparing by embodiment 4), 5th group of gavage gives pterostilbene compositions 5 (preparing by embodiment 5), 6th group of gavage gives pterostilbene compositions 6 (preparing by embodiment 6), 7th group of gavage gives pterostilbene compositions 7 (preparing by embodiment 7), 8th group of gavage gives pterostilbene compositions 8 (preparing by embodiment 7), 9th group of gavage gives pterostilbene compositions 7 (preparing by embodiment 9), 10th group of gavage gives pterostilbene compositions 10 (preparing by embodiment 10), 11st group of gavage gives pterostilbene compositions 11 (preparing by embodiment 11), 12nd group of gavage gives pterostilbene compositions 12 (preparing by embodiment 12), 13rd group of gavage gives pterostilbene crude drug, 14th group of intravenous injection pterostilbene injection.
Above-mentionedly press 10mg/kg, administration.
Sample collecting: after administration 0,0.5,1,2,3,4,5,6,7,8,10,12,24h gets blood by eye socket, process, measures pterostilbene content.
Result: mean blood plasma concentration data 3P97 program matching, oral AUC data are compared with intravenous injection AUC data, and calculate pterostilbene bioavailability, data are in table 1.
Bioavailability after the administration of table 1 pterostilbene composition oral
| Sample | Bioavailability (%) |
| 1st group | 72.8 |
| 2nd group | 75.6 |
| 3rd group | 78.8 |
| 4th group | 46.1 |
| 5th group | 41.9 |
| 6th group | 32.5 |
| 7th group | 30.7 |
| 8th group | 27.6 |
| 9th group | 23.2 |
| 10th group | 21.1 |
| 11st group | 23.0 |
| 12nd group | 25.5 |
| 13rd group | 14.3 |
| 14th group | - |
Sum up: embodiment 1-3 is that just drying means is different with drying time, and bioavailability is slightly different, has very big market promotional value by the present invention's preparation.Embodiment 4-12 adopts to be different from composition of the present invention, ratio or order of addition, and result shows biological degree far away from bioavailability of the present invention.
Claims (5)
1. a pterostilbene compositions, is characterized in that containing pterostilbene, sodium stearyl fumarate and L-Carnosine.
2. pterostilbene compositions according to claim 1, is characterized in that pterostilbene in described compositions, the mass ratio of sodium stearyl fumarate and L-Carnosine is 1:1:1.
3. prepare a method for pterostilbene compositions described in claim 1, it is characterized in that its preparation process is as follows:
By L-Carnosine dissolve with ethanol, then add sodium stearyl fumarate, obtain adjuvant dispersion liquid; By pterostilbene dissolve with ethanol, obtain drug susbstance dispersion; By adjuvant dispersion liquid and drug susbstance dispersion mix homogeneously, reclaim ethanol, dry, to obtain final product.
4. the preparation method of pterostilbene compositions as claimed in claim 3, is characterized in that its preparation process is as follows: described is dissolved in the ethanol of 100mL by L-Carnosine 0.1 g, then adds sodium stearyl fumarate 0.1 g, obtains adjuvant dispersion liquid; By pterostilbene 0.1 g 50mL dissolve with ethanol, obtain drug susbstance dispersion; By adjuvant dispersion liquid and drug susbstance dispersion mix homogeneously, 40 DEG C of vacuum reclaim ethanol, and 40 DEG C of dry 6h, to obtain final product.
5. the preparation method of pterostilbene compositions as claimed in claim 3, is characterized in that its preparation process is as follows: be dissolved in the ethanol of 100mL by L-Carnosine 0.1 g, then adds sodium stearyl fumarate 0.1 g, obtain adjuvant dispersion liquid; By pterostilbene 0.1 g 20mL dissolve with ethanol, obtain drug susbstance dispersion; By adjuvant dispersion liquid and drug susbstance dispersion mix homogeneously, 40 DEG C of vacuum reclaim ethanol, and lyophilization, to obtain final product.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410505366.4A CN104257640B (en) | 2014-09-28 | 2014-09-28 | A kind of Pterostilene composition and its preparation method |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410505366.4A CN104257640B (en) | 2014-09-28 | 2014-09-28 | A kind of Pterostilene composition and its preparation method |
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| Publication Number | Publication Date |
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| CN104257640A true CN104257640A (en) | 2015-01-07 |
| CN104257640B CN104257640B (en) | 2016-06-01 |
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| CN201410505366.4A Expired - Fee Related CN104257640B (en) | 2014-09-28 | 2014-09-28 | A kind of Pterostilene composition and its preparation method |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110075094A (en) * | 2019-02-27 | 2019-08-02 | 延边大学 | Pterostilbene is preparing the application in drug or health care product |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101618021A (en) * | 2009-08-12 | 2010-01-06 | 河北科技大学 | Chitosan coating medicine slow release microsphere and preparation method thereof |
| CN101912377A (en) * | 2010-08-10 | 2010-12-15 | 王晓琴 | Application of pterostilbene to preparation of medicament for treating cervical cancer |
| CN102120996A (en) * | 2010-12-03 | 2011-07-13 | 西北农林科技大学 | Method for generating pterostilbene by utilizing grape resveratrol-oxygen-methyl transferase to catalyze resveratrol |
-
2014
- 2014-09-28 CN CN201410505366.4A patent/CN104257640B/en not_active Expired - Fee Related
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101618021A (en) * | 2009-08-12 | 2010-01-06 | 河北科技大学 | Chitosan coating medicine slow release microsphere and preparation method thereof |
| CN101912377A (en) * | 2010-08-10 | 2010-12-15 | 王晓琴 | Application of pterostilbene to preparation of medicament for treating cervical cancer |
| CN102120996A (en) * | 2010-12-03 | 2011-07-13 | 西北农林科技大学 | Method for generating pterostilbene by utilizing grape resveratrol-oxygen-methyl transferase to catalyze resveratrol |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110075094A (en) * | 2019-02-27 | 2019-08-02 | 延边大学 | Pterostilbene is preparing the application in drug or health care product |
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| CN104257640B (en) | 2016-06-01 |
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| C41 | Transfer of patent application or patent right or utility model | ||
| CB03 | Change of inventor or designer information |
Inventor after: Hao Lei Inventor after: Xu Yunling Inventor after: Wei Xianjuan Inventor after: Hao Kun Inventor after: Ge Gang Inventor after: Hao Xia Inventor before: Luo Ruixue |
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Effective date of registration: 20160503 Address after: Shibei District People's road 266033 in Shandong province Qingdao Haici medical group Qingdao Haici Hospital No. 4 Applicant after: Hao Lei Address before: 215000 Jiangsu City, Suzhou hi tech Zone Jinfeng Road, building 8, No. 15 Applicant before: Suzhou Pu Luo Da Biotechnology Co., Ltd. |
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