CN104257640B - A kind of Pterostilene composition and its preparation method - Google Patents
A kind of Pterostilene composition and its preparation method Download PDFInfo
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- CN104257640B CN104257640B CN201410505366.4A CN201410505366A CN104257640B CN 104257640 B CN104257640 B CN 104257640B CN 201410505366 A CN201410505366 A CN 201410505366A CN 104257640 B CN104257640 B CN 104257640B
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- Prior art keywords
- pterostilene
- ethanol
- composition
- carnosine
- auxiliary material
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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)
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- 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 present invention provides a kind of Pterostilene composition and its preparation method with higher oral administration biaavailability. The Pterostilene composition of the present invention, it is characterised in that containing Pterostilene, sodium stearyl fumarate and L-Carnosine; The mass ratio of Pterostilene, sodium stearyl fumarate and L-Carnosine is preferably 1:1:1. The method of Pterostilene composition of the present invention, its preparation process is as follows: by L-Carnosine dissolve with ethanol, then adds sodium stearyl fumarate, obtains auxiliary material dispersion liquid; By Pterostilene dissolve with ethanol, obtain drug susbstance dispersion; Auxiliary material dispersion liquid and drug susbstance dispersion are mixed, reclaims ethanol, dry, to obtain final product.
Description
Technical field
The present invention relates to a kind of Pterostilene composition and its preparation method, belong to medical art.
Background technology
Pterostilene is antitumor has good effect, but causes oral administration biaavailability very low owing to being insoluble in the reason such as water and enteron aisle perviousness difference, not yet has Pterostilene oral preparations to list.
Summary of the invention
It is an object of the invention to provide a kind of Pterostilene composition and its preparation method with higher oral administration biaavailability.
For foregoing invention object, the present invention provides following technical scheme:
The Pterostilene composition of the present invention, it is characterised in that containing Pterostilene, sodium stearyl fumarate and L-Carnosine; The mass ratio of Pterostilene, sodium stearyl fumarate and L-Carnosine is preferably 1:1:1.
The method of Pterostilene composition of the present invention, its preparation process is as follows:
By L-Carnosine dissolve with ethanol, then add sodium stearyl fumarate, obtain auxiliary material dispersion liquid; By Pterostilene dissolve with ethanol, obtain drug susbstance dispersion; Auxiliary material dispersion liquid and drug susbstance dispersion are mixed, reclaims ethanol, dry, to obtain final product.
The useful effect of the present invention is mainly:
The composition of the present invention significantly improves the oral administration biaavailability of Pterostilene. The preparation method of composition of the present invention is simple, cost is low, is suitable for mass-producing preparation. The preparation method of composition of the present invention is unique, is that the accident in a large amount of experiment finds, the dispersion order of auxiliary material and medicine and ratio all can not adjust. Therefore composition, ratio and the order of addition that the present invention adopts is the innovative point of the present invention.
Embodiment
Below in conjunction with embodiment, the present invention is described in further detail, but should notice that the scope of the present invention is 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 auxiliary material dispersion liquid; By Pterostilene 0.1g 50mL dissolve with ethanol, obtain drug susbstance dispersion; Auxiliary material dispersion liquid and drug susbstance dispersion being mixed, 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 auxiliary material dispersion liquid; By Pterostilene 0.1g 20mL dissolve with ethanol, obtain drug susbstance dispersion; Auxiliary material dispersion liquid and drug susbstance dispersion being mixed, 40 DEG C of vacuum reclaim ethanol, and lyophilize, 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 auxiliary material dispersion liquid; By Pterostilene 0.1g 100mL dissolve with ethanol, obtain drug susbstance dispersion; Auxiliary material dispersion liquid and drug susbstance dispersion being mixed, 30 DEG C of vacuum reclaim ethanol, and lyophilize, 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 auxiliary material dispersion liquid; By Pterostilene 0.1g 50mL dissolve with ethanol, obtain drug susbstance dispersion; Auxiliary material dispersion liquid and drug susbstance dispersion being mixed, 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 auxiliary material dispersion liquid; By Pterostilene 0.1g 50mL dissolve with ethanol, obtain drug susbstance dispersion; Auxiliary material dispersion liquid and drug susbstance dispersion being mixed, 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 Pterostilene 0.1g and L-Carnosine 0.1g 200mL, then adding sodium stearyl fumarate 0.1g, mix, 40 DEG C of vacuum reclaim ethanol, and 40 DEG C of dry 6h, to obtain final product.
Embodiment 7
Being disperseed by the ethanol of Pterostilene 0.1g, L-Carnosine 0.1g, sodium stearyl fumarate 0.1g 200mL, mix, 40 DEG C of vacuum reclaim ethanol, and 40 DEG C of dry 6h, to obtain final product.
Embodiment 8
Being disperseed by the ethanol of Pterostilene 0.1g and sodium stearyl fumarate 0.1g 100mL, mix, 40 DEG C of vacuum reclaim ethanol, and 40 DEG C of dry 6h, to obtain final product.
Embodiment 9
Being disperseed by the ethanol of Pterostilene 0.1g and L-Carnosine 0.1g 200mL, mix, 40 DEG C of vacuum reclaim ethanol, and 40 DEG C of dry 6h, to obtain final product.
Embodiment 10
Pterostilene 0.1g, sodium stearyl fumarate 0.1g and L-Carnosine 0.1g are mixed, pulverizes, sieve and get final product.
Embodiment 11
Pterostilene 0.1g and sodium stearyl fumarate 0.1g is mixed, pulverizes, sieve and get final product.
Embodiment 12
Pterostilene 0.1g and L-Carnosine are mixed, pulverizes, sieve and get final product.
Embodiment 13
The oral administration biaavailability research of Pterostilene composition
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 Pterostilene composition 1 (preparing by embodiment 1), 2nd group of gavage gives Pterostilene composition 2 (preparing by embodiment 2), 3rd group of gavage gives Pterostilene composition 3 (preparing by embodiment 3), 4th group of gavage gives Pterostilene composition 4 (preparing by embodiment 4), 5th group of gavage gives Pterostilene composition 5 (preparing by embodiment 5), 6th group of gavage gives Pterostilene composition 6 (preparing by embodiment 6), 7th group of gavage gives Pterostilene composition 7 (preparing by embodiment 7), 8th group of gavage gives Pterostilene composition 8 (preparing by embodiment 7), 9th group of gavage gives Pterostilene composition 7 (preparing by embodiment 9), 10th group of gavage gives Pterostilene composition 10 (preparing by embodiment 10), 11st group of gavage gives Pterostilene composition 11 (preparing by embodiment 11), 12nd group of gavage gives Pterostilene composition 12 (preparing by embodiment 12), 13rd group of gavage gives Pterostilene bulk drug, 14th group of intravenous injection Pterostilene injection liquid.
Above-mentioned press 10mg/kg, administration.
Sample collecting: after administration 0,0.5,1,2,3,4,5,6,7,8,10,12,24h get blood by eye socket, process, measure Pterostilene content.
Result: mean blood plasma concentration data 3P97 program matching, oral AUC data, compared with intravenous injection AUC data, calculate Pterostilene bioavailability, and data are in table 1.
Bioavailability after table 1 Pterostilene composition oral administration
| 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 time of drying, and bioavailability is slightly different, has very big market promotional value by the present invention's preparation. Embodiment 4-12 is the composition, ratio or the order of addition that adopt and be different from the present invention, and result display biology degree is far away from the bioavailability of the present invention.
Claims (3)
1. a Pterostilene composition, it is characterised in that main active ingredient is Pterostilene, sodium stearyl fumarate and L-Carnosine; In described composition, the mass ratio of Pterostilene, sodium stearyl fumarate and L-Carnosine is 1:1:1; Described composition is realized by following steps: by L-Carnosine dissolve with ethanol, then adds sodium stearyl fumarate, obtains auxiliary material dispersion liquid; By Pterostilene dissolve with ethanol, obtain drug susbstance dispersion; Auxiliary material dispersion liquid and drug susbstance dispersion are mixed, reclaims ethanol, dry, to obtain final product.
2. the preparation method of Pterostilene composition as claimed in claim 1, it is characterised in that its preparation process is as follows: described is dissolved in the ethanol of 100mL by L-Carnosine 0.1g, then adds sodium stearyl fumarate 0.1g, obtains auxiliary material dispersion liquid; By Pterostilene 0.1g 50mL dissolve with ethanol, obtain drug susbstance dispersion; Auxiliary material dispersion liquid and drug susbstance dispersion being mixed, 40 DEG C of vacuum reclaim ethanol, and 40 DEG C of dry 6h, to obtain final product.
3. the preparation method of Pterostilene composition as claimed in claim 1, it is characterised in that its preparation process is as follows: be dissolved in the ethanol of 100mL by L-Carnosine 0.1g, then adds sodium stearyl fumarate 0.1g, obtains auxiliary material dispersion liquid; By Pterostilene 0.1g 20mL dissolve with ethanol, obtain drug susbstance dispersion; Auxiliary material dispersion liquid and drug susbstance dispersion being mixed, 40 DEG C of vacuum reclaim ethanol, and lyophilize, 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 CN104257640A (en) | 2015-01-07 |
| CN104257640B true 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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| 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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| CN101618021B (en) * | 2009-08-12 | 2011-04-06 | 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 |
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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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