CN1565430A - Allicin cyclodextrin clathrate compound, formulation and its preparation method - Google Patents
Allicin cyclodextrin clathrate compound, formulation and its preparation method Download PDFInfo
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- CN1565430A CN1565430A CN 03124592 CN03124592A CN1565430A CN 1565430 A CN1565430 A CN 1565430A CN 03124592 CN03124592 CN 03124592 CN 03124592 A CN03124592 A CN 03124592A CN 1565430 A CN1565430 A CN 1565430A
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- garlicin
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Abstract
The invention discloses a garlicin cyclodextrin clathrate compound, preparation and the process for preparing same, wherein the allicin, cyclodextrin or their derivatives (such as beta-cyclodextrin, hydroxypropyl-beta-cyclodextrin) can be used for preparing garlicin cyclodextrin clathrate compound, which can be used for preparing various preparations of different oral preparation, suppositorium, spray, and injection.
Description
Technical field
The present invention relates to medical technical field, definitely utilize cyclodextrin or derivatives thereof and garlicin to form clathrate or improve dissolubility, the stability of garlicin in water saying so by adding cyclodextrin or derivatives thereof, reduce zest, cover bad stink, thereby make garlicin cyclodextrin clathrate and preparation thereof.
Background technology
Bulbus Allii is the underground bulb of Liliaceae allium Bulbus Allii.Acrid in the mouth, warm in nature, return spleen, stomach, lung meridian, have the detoxifcation parasite killing, the effect of detumescence, dysentery relieving, in China as the history in existing thousands of years of medication among the people.Garlicin is the main effective ingredient in the Bulbus Allii volatile oil, modern study is thought: Bulbus Allii have stronger antibiotic, protozoacide, infusorian, antiviral, antitumor, antioxidation, slow down aging, prevent and treat atherosclerosis, effect such as protect the liver, be a kind of extremely promising medicine, have great exploitation and be worth.
The existing dosage form of garlicin is garlicin injection (2ml: 30mg at present, 5ml: 60mg), the garlicin enteric coatel tablets, garlicin enteric soft gelatin capsule, garlicin is an oily liquids, and volatile, almost insoluble in water, less stable, special garlic odour is arranged, the human body mucosa is had zest, and garlicin is made injection need add solubilizing agent and stabilizing agent, to increase its dissolubility and stability in water, pain during this injection intramuscular injection, during intravenous drip, must be through dilution, troublesome poeration, and cause liquid medicine contamination and malpraxis easily, influence medicine quality and patient safety, not only can increase its water solublity, stability and be made into cyclodextrin clathrate, cover bad smell, reduce zest, and can make the liquid medicine solidification, be convenient to preparation processing.Therefore we use the modern pharmaceutical technology, adopt novel enclose rings of material dextrin or derivatives thereof that its enclose is formed cyclodextrin clathrate and makes corresponding dosage forms, clinical safety, stable, the evident in efficacy medicine of providing is provided, benefit the common people, this is significant to inheriting and develop motherland's medicine legacy.
Summary of the invention
The purpose of this invention is to provide a kind of garlicin cyclodextrin clathrate and preparation thereof, it has good absorbing, bioavailability height, curative effect height, the little characteristics of side effect.
The present invention selects the cyclodextrin or derivatives thereof, as HP-, hydroxyethyl-, methyl-beta-schardinger dextrin-, iodic acid group-beta-cyclodextrin, by glucoside-beta-schardinger dextrin-of other plant extract or synthetic etc. as the enclose material, garlicin is made cyclodextrin clathrate.
Garlicin cyclodextrin clathrate of the present invention, the weight ratio of garlicin and cyclodextrin or derivatives thereof is: 1: any ratio in the 1-200 scope.
The preparation method of garlicin clathrate can adopt any in solvent method, polishing, ultrasonic method, freeze-drying, the spray drying method etc. among the present invention.
The preparation of garlicin clathrate of the present invention: garlicin can carry out enclose with The suitable solvent dissolving back adding, also can directly add.
The made garlicin cyclodextrin clathrate of the present invention can be prepared into various dosage forms, as oral formulations (comprising tablet, capsule, granule, pill, mixture, drop pill etc.), injection (comprising injection, aseptic powder injection or freeze-dried powder and transfusion etc.) also can be made into suppository, spray etc.
The said oral formulations of the present invention can be conventional formulation, also can be slow releasing preparation/controlled release preparation.
In " injection " of the present invention, can contain antioxidant, antioxidant is nitrogen, carbon dioxide gas, sodium sulfite, sodium pyrosulfite, sodium thiosulfate, disodiumedetate, cysteine etc.
In " injection " of the present invention, can contain the excipient of 3-20%.
The present invention's said " injection " can adopt clathrates such as garlicin hydroxypropyl-beta-cyclodextrin inclusion.
The present invention's said " injection " mainly contains garlicin cyclodextrin clathrate, water for injection.
The present invention's said " freeze-dried powder " mainly contains garlicin cyclodextrin clathrate and proppant or excipient, waits one or more to mix as " mannitol ", " lactose ", " dextran ", " sorbitol " and uses, get by lyophilization.
The present invention's said " aseptic powder injection " mainly contains garlicin cyclodextrin clathrate and suitable proppant or excipient, wait one or more to mix as " mannitol ", " lactose ", " dextran ", " sorbitol " and use, the powder that obtains by " lyophilization " or " spray drying " carries out aseptic subpackaged getting.
The present invention's said " transfusion " mainly contains garlicin cyclodextrin clathrate, water for injection and the instrumentality that oozes such as an amount of, oozes instrumentality as acceptable etc. on sodium chloride, glucose and other pharmaceuticss, gets through preparation.
The invention solves the problem such as water solublity, zest, bad smell of garlicin, stability improves greatly.Garlicin clathrate of the present invention can be used for making various preparations, has advantage efficiently, made oral formulations can be routine/release preparation, made injection has solubilizing agents such as no organic solvent, no tween 80, avoided the toxicity of tween 80, unit volume Chinese medicine content height, good effect, the advantage that toxic and side effects is low to body.Overcome and contained the infringement of tween 80 in the existing preparation human body.
Concrete enforcement
Following enforcement is traded in order to further specify the present invention, can be for reference, but do not limit the scope of the invention thus.
Embodiment 1: the preparation of garlicin Benexate Hydrochloride: amount takes by weighing garlicin, beta-schardinger dextrin-according to the above ratio; Add suitable quantity of water/second alcohol and water, heating is stirred/ultrasonicly slowly drip above-mentioned garlicin solution down, continue to stir/ultrasonic to the stipulated time, and cold preservation 24 hours, sucking filtration, washing, the precipitate cold drying, promptly.
Embodiment 2: the preparation of garlicin hydroxypropyl-beta-cyclodextrin inclusion: amount takes by weighing garlicin, HP-according to the above ratio, and garlicin is standby with an amount of ethanol/ethanol solution; HP-adds the suitable quantity of water dissolving, stir/the ultrasonic following above-mentioned garlicin solution that slowly drips, continue to stir/ultrasonic to the stipulated time, membrane filtration with reuse 0.22 μ behind the membrane filtration of 0.45 μ, the solution of gained is after vacuum drying/spray drying/lyophilization, get white powder, i.e. garlicin hydroxypropyl-beta-cyclodextrin inclusion.
Embodiment 3: the preparation of garlicin hydroxyethyl-clathrate: amount takes by weighing garlicin, hydroxyethyl-according to the above ratio, and garlicin is standby with an amount of ethanol/ethanol solution; HP-adds the suitable quantity of water dissolving, stir/the ultrasonic following above-mentioned garlicin solution that slowly drips, continue to stir/ultrasonic to the stipulated time, membrane filtration with reuse 0.22 μ behind the membrane filtration of 0.45 μ, the solution of gained is after vacuum drying/spray drying/lyophilization, get white powder, i.e. garlicin hydroxyethyl-clathrate.
Embodiment 4: get an amount of garlicin cyclodextrin clathrate and an amount of auxiliary materials and mixing pelletizing press sheet, get various garlicin sheets.Mixing tabletting after selecting for use different materials to granulate can get the release sheet.
Embodiment 5: get an amount of garlicin cyclodextrin clathrate and appropriate amount of auxiliary materials mixing, directly granulate/make micropill after, encapsulated, promptly get capsulae allitridi.After made micropill carried out coating with different coating materials, mixing, encapsulated, promptly get garlicin release capsule.
Embodiment 6: get an amount of garlicin cyclodextrin clathrate and an amount of substrate mixing and make suppository.
Embodiment 7: get an amount of garlicin hydroxypropyl-beta-cyclodextrin inclusion and be dissolved in the water for injection, add an amount of lactose and 0.1-0.2% active carbon, stirred 10-40 minute, behind the depyrogenation, filtering decarbonization is with 0.22 μ m filtering with microporous membrane, transfer to ormal weight with water for injection, gained solution is sub-packed in the cillin bottle, carries out lyophilization, gets the garlicin freeze-dried powder.
Embodiment 8: get an amount of garlicin hydroxypropyl-beta-cyclodextrin inclusion and be dissolved in the water for injection, add an amount of mannitol and 0.1-0.2% active carbon, stirred 10-40 minute, behind the depyrogenation, filter carbon removal, with 0.22 μ m filtering with microporous membrane, transfer to ormal weight with water for injection, gained solution is sub-packed in the cillin bottle, carries out lyophilization, gets the garlicin freeze-dried powder.
Embodiment 9: get an amount of garlicin hydroxypropyl-beta-cyclodextrin inclusion and be dissolved in the water for injection, add the 0.1-0.2% active carbon, stirred 10-40 minute, behind the depyrogenation, filter carbon removal, with 0.22 μ m filtering with microporous membrane, transfer to ormal weight with water for injection, the packing of gained solution, flowing steam sterilization 30 minutes gets injection.
Embodiment 10: get an amount of garlicin hydroxy propyl-Beta-thick spermatophore compound of ring and be dissolved in the water for injection, add an amount of glucose for injection and 0.1-0.3% active carbon, stirred 10-40 minute, behind the depyrogenation, filter carbon removal, with 0.22 μ m filtering with microporous membrane, transfer to ormal weight with water for injection, gained solution is sub-packed in the infusion bottle, sterilizes 30 minutes for 115 ℃, gets the garlicin glucose injection.
Embodiment 11: get an amount of garlicin hydroxypropyl-beta-cyclodextrin inclusion and be dissolved in the water for injection, add an amount of sodium chloride for injection and 0.1-0.3% active carbon, stirred 10-40 minute, behind the depyrogenation, filter carbon removal, with 0.22 μ m filtering with microporous membrane, transfer to ormal weight with water for injection, gained solution is sub-packed in the infusion bottle, sterilizes 30 minutes for 115 ℃, gets the garlicin sodium chloride injection.
Claims (10)
1. a garlicin cyclodextrin clathrate, preparation and preparation method is characterized in that: utilize cyclodextrin with and derivant beta-schardinger dextrin-, HP-, hydroxyethyl-, methyl-beta-schardinger dextrin-, sulfonic acid group-beta-cyclodextrin, use by a kind of/multiple mixing of the glucose group-beta-cyclodextrin of other plant extract/synthetic; Form clathrate with garlicin, be prepared into the garlicin cyclodextrin clathrate, improve dissolubility and the stability of garlicin in water, and make oral formulations, suppository, spray, the various preparations of injection.
2. garlicin cyclodextrin clathrate according to claim 1, preparation and preparation method is characterized in that: used " cyclodextrin/its derivant " and the weight ratio of " garlicin " are 1-200: any in 1.
3. garlicin cyclodextrin clathrate according to claim 1, preparation and preparation method is characterized in that: said oral formulations comprises tablet, pill, mixture, drop pill, capsule, can be conventional formulation, also can be the release preparation; Said injection comprises injection, freeze-dried powder, aseptic powder injection, transfusion.
4. according to claim 1,3 described garlicin cyclodextrin clathrate, preparation and preparation method, it is characterized in that: said " injection " mainly contains garlicin cyclodextrin clathrate and water for injection.
5. according to claim 1,3 described garlicin cyclodextrin clathrate, preparation and preparation method, it is characterized in that: said " freeze-dried powder " mainly contains garlicin cyclodextrin clathrate, suitable proppant/excipient, gets by lyophilization.
6. according to claim 1,3 described garlicin cyclodextrin clathrate and preparations thereof, it is characterized in that: said " aseptic powder injection " mainly contains garlicin cyclodextrin clathrate, suitable proppant/excipient, and the powder that obtains by lyophilization/spray drying carries out aseptic subpackaged getting.
7. according to claim 1,3 described garlicin cyclodextrin clathrate, preparation and preparation method, it is characterized in that: said " transfusion " mainly contains garlicin cyclodextrin clathrate, water for injection, the instrumentality (as the instrumentality that oozes such as acceptable on sodium chloride, glucose and other pharmaceuticss) that oozes such as an amount of.
8. garlicin cyclodextrin clathrate according to claim 1, preparation and preparation method is characterized in that: the preparation of said garlicin cyclodextrin clathrate can be adopted any of solvent method, polishing, freeze-drying, spray drying method, ultrasonic method.
9. garlicin cyclodextrin clathrate according to claim 1, preparation and preparation method, it is characterized in that: in the said injection, can contain antioxidant (as nitrogen, carbon dioxide gas, sodium sulfite, sodium pyrosulfite, sodium thiosulfate, disodiumedetate, cysteine).
10. garlicin cyclodextrin clathrate according to claim 1, preparation and preparation method, it is characterized in that: in the said injection, can contain 3-20% excipient (as mannitol, lactose, dextran, sorbitol a kind of/several mixing use).
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| Application Number | Priority Date | Filing Date | Title |
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| CN 03124592 CN1565430A (en) | 2003-06-22 | 2003-06-22 | Allicin cyclodextrin clathrate compound, formulation and its preparation method |
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| CN 03124592 CN1565430A (en) | 2003-06-22 | 2003-06-22 | Allicin cyclodextrin clathrate compound, formulation and its preparation method |
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| CN1565430A true CN1565430A (en) | 2005-01-19 |
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Cited By (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101485446B (en) * | 2009-02-26 | 2010-08-11 | 北京工商大学 | Preparation method of garlic oil cyclodextrin or cyclodextrin derivate inclusion compound |
| CN102302442A (en) * | 2011-07-26 | 2012-01-04 | 兰州大学 | Allicin vaginal suppository and preparation method thereof |
| US8101802B2 (en) | 2006-11-11 | 2012-01-24 | Ecospray Limited | Allylic polysulfanes |
| CN104522307A (en) * | 2014-12-25 | 2015-04-22 | 北京资源亚太饲料科技有限公司 | Method for preparing allicin soluble clathrate granules |
| CN105231261A (en) * | 2015-10-09 | 2016-01-13 | 定远县玉强米业有限公司 | anti-ageing cooked rice and making method thereof |
| CN105341646A (en) * | 2015-10-09 | 2016-02-24 | 定远县玉强米业有限公司 | Donkey-hide gelatin blood tonifying cooked rice and preparation method thereof |
| CN105341645A (en) * | 2015-10-09 | 2016-02-24 | 定远县玉强米业有限公司 | Haw cooked rice and preparation method thereof |
| CN105341644A (en) * | 2015-10-09 | 2016-02-24 | 定远县玉强米业有限公司 | Nut brain-strengthening cooked rice and preparation method thereof |
| CN105360889A (en) * | 2015-10-09 | 2016-03-02 | 定远县玉强米业有限公司 | Steamed rice capable of reducing blood glucose and preparation method thereof |
| CN107789345A (en) * | 2016-09-07 | 2018-03-13 | 汤臣倍健股份有限公司 | Flavoring allicin cyclodextrin complexes and preparation method thereof |
| CN112957538A (en) * | 2021-02-20 | 2021-06-15 | 北京邦塞科技有限公司 | Antibacterial bone cement and preparation method thereof |
| WO2024027219A1 (en) * | 2022-08-04 | 2024-02-08 | 中科中山药物创新研究院 | Crystal form of allicin-cyclodextrin inclusion complex cocrystal, preparation method therefor and use thereof |
-
2003
- 2003-06-22 CN CN 03124592 patent/CN1565430A/en active Pending
Cited By (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8101802B2 (en) | 2006-11-11 | 2012-01-24 | Ecospray Limited | Allylic polysulfanes |
| CN101485446B (en) * | 2009-02-26 | 2010-08-11 | 北京工商大学 | Preparation method of garlic oil cyclodextrin or cyclodextrin derivate inclusion compound |
| CN102302442A (en) * | 2011-07-26 | 2012-01-04 | 兰州大学 | Allicin vaginal suppository and preparation method thereof |
| CN102302442B (en) * | 2011-07-26 | 2013-02-20 | 兰州大学 | Allicin vaginal suppository and preparation method thereof |
| CN104522307A (en) * | 2014-12-25 | 2015-04-22 | 北京资源亚太饲料科技有限公司 | Method for preparing allicin soluble clathrate granules |
| CN105341646A (en) * | 2015-10-09 | 2016-02-24 | 定远县玉强米业有限公司 | Donkey-hide gelatin blood tonifying cooked rice and preparation method thereof |
| CN105231261A (en) * | 2015-10-09 | 2016-01-13 | 定远县玉强米业有限公司 | anti-ageing cooked rice and making method thereof |
| CN105341645A (en) * | 2015-10-09 | 2016-02-24 | 定远县玉强米业有限公司 | Haw cooked rice and preparation method thereof |
| CN105341644A (en) * | 2015-10-09 | 2016-02-24 | 定远县玉强米业有限公司 | Nut brain-strengthening cooked rice and preparation method thereof |
| CN105360889A (en) * | 2015-10-09 | 2016-03-02 | 定远县玉强米业有限公司 | Steamed rice capable of reducing blood glucose and preparation method thereof |
| CN107789345A (en) * | 2016-09-07 | 2018-03-13 | 汤臣倍健股份有限公司 | Flavoring allicin cyclodextrin complexes and preparation method thereof |
| CN107789345B (en) * | 2016-09-07 | 2022-06-28 | 汤臣倍健股份有限公司 | Corrective allicin-cyclodextrin compound and preparation method thereof |
| CN112957538A (en) * | 2021-02-20 | 2021-06-15 | 北京邦塞科技有限公司 | Antibacterial bone cement and preparation method thereof |
| WO2024027219A1 (en) * | 2022-08-04 | 2024-02-08 | 中科中山药物创新研究院 | Crystal form of allicin-cyclodextrin inclusion complex cocrystal, preparation method therefor and use thereof |
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