CN1555790A - Propyl gallate injection liquid and its preparation method - Google Patents
Propyl gallate injection liquid and its preparation method Download PDFInfo
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- CN1555790A CN1555790A CNA2003101146708A CN200310114670A CN1555790A CN 1555790 A CN1555790 A CN 1555790A CN A2003101146708 A CNA2003101146708 A CN A2003101146708A CN 200310114670 A CN200310114670 A CN 200310114670A CN 1555790 A CN1555790 A CN 1555790A
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- propyl ester
- gallate propyl
- injection
- gallate
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Abstract
A gallopropylate injection in the form of liquid, freeze dried powder, aseptic powder, or perfusion for preventing and treating cerebral thrombosis, coronary heart disease and paroxysmal headache is prepared through dissolving hydroxypropyl-beta-cyclodextrin in water, adding gallo propylate, stirring or grinding or ultrasonic processing, and preparing said injection. Its advantages are high safety and stability and high curative effect.
Description
Technical field:
The present invention relates to medical technical field, it is Gallate propyl ester injection and preparation method thereof in definite saying.
Technical background:
The Gallate propyl ester is the active component in the Chinese medicine Radix Paeoniae Rubra---the derivant of epicatechol gallate, be on the structure of epicatechol gallate, modify and obtain have a more medicine of Johnson ﹠ Johnson's thing effect.Chemical name: 3,4, the 5-Propylgallate, former name: injection promote blood circulation ester, injection Radix Paeoniae Rubra 801, arteries and veins green grass or young crops.The antithrombotics such as inflammatory exudation of this product antiplatelet aggregation, blood vessel dilating, enhancing fibrinolytic, reduction blood viscosity, removing free radical, inhibition blood capillary form, and antiplatelet aggregation.Safe in utilization, untoward reaction is few.Every day, maximal dose can reach 420-460mg.This product is used for prevention and treats ischemic cerebrovascular (as acute cerebral infarction, chronic brain thrombosis, lacunar infarction, cerebral blood supply insufficiency), coma sequela, cerebral trauma, cerebral concussion; Coronary heart disease, angina pectoris, hypertension, heart failure; Pulmonary heart disease; Some peripheral angiopathy (as thrombophlebitis), determined curative effect.Clinical usage is intravenous drip, the adult, once-a-day, each 120-180mg.
Because this product is ester type compound, in water, be difficult for dissolving, and phenolic hydroxyl group arranged, so instability have only a kind of dosage form of injectable powder on the present market, is dissolved with propylene glycol during application, to clinical bring constant.
Summary of the invention:
The purpose of this invention is to provide Gallate propyl ester injection and preparation method thereof, it has solved the little and instability problem of Gallate propyl ester dissolubility in water, is that solvent is made injection type with water.
It is realized by following scheme: will be the derivant of the beta-schardinger dextrin-of representative with the HP-, and place water for injection, and after the dissolving, add the Gallate propyl ester again, stirring or grinding or ultrasonic get Gallate propyl ester beta-cyclodextrin derivative inclusion complex in solution.Gallate propyl ester inclusion complex in solution is directly used in preparation Gallate propyl ester injection; Or with Gallate propyl ester inclusion complex in solution after " vacuum drying " or " lyophilization " or " spray drying ", Gallate propyl ester Benexate Hydrochloride powder, prepare Gallate propyl ester injection again.Wherein the mol ratio of Gallate propyl ester and beta-cyclodextrin derivative is 1: 1～1: 16, and optimum range is 1: 4～1: 12.
Gallate propyl ester clathrate can be used as the raw material of making injection, freeze-dried powder, aseptic powder injection, transfusion.Said injection is with Gallate propyl ester inclusion complex in solution or the Gallate propyl ester beta-cyclodextrin derivative clathrate powder that obtains by " vacuum drying ", " lyophilization " or " spray drying ", the injection of making.Said " freeze-dried powder " is Gallate propyl ester inclusion complex in solution, adds or do not add excipient, the injectable powder of making by lyophilization.Said " aseptic powder injection " is Gallate propyl ester inclusion complex in solution, and the powder that obtains by " vacuum drying " or " lyophilization " or " spray drying " adds or do not add excipient, carries out the aseptic subpackaged injectable powder of making.Said transfusion is with Gallate propyl ester inclusion complex in solution or the Gallate propyl ester beta-cyclodextrin derivative clathrate powder that obtains by " vacuum drying ", " lyophilization " or " spray drying ", ooze formulated bulk capacity injection with sodium chloride or glucose conciliation etc.
Advantage of the present invention is: be the derivant of the beta-schardinger dextrin-of representative with the HP-, with the Gallate propyl ester wrap and or solubilising, not only solved the little problem of Gallate propyl ester water solubility, and improved Gallate propyl ester stability, both having can be made into water is the injection of solvent, also can be made into freeze-dried powder or aseptic powder injection, transfusion, need not use propylene glycol during clinical application, made things convenient for clinical application, made injection safer, more stable.
The specific embodiment:
Embodiment 1: take by weighing HP-3.7g, add in the about 60 ℃ of water of 5ml, stir and make dissolving, add 60mg Gallate propyl ester, stir or ultrasonic or grind and make dissolving, add water to 8ml, mixing, Gallate propyl ester and hydroxypropyl-beta-cyclodextrin inclusion solution.
Embodiment 2: take by weighing HP-3.7g and put in the 5ml water, stirring makes dissolving, add 60mg Gallate propyl ester, stir or ultrasonic or grind and make dissolving, add water to 8ml, mixing, get Gallate propyl ester and hydroxypropyl-beta-cyclodextrin inclusion solution, filter, gained solution is after " vacuum drying " or " spray drying " or " lyophilization ", get white powder, i.e. Gallate propyl ester and hydroxypropyl-beta-cyclodextrin inclusion.This clathrate is soluble in water, makes raw material with this, can be made into injection, powder pin, transfusion.
Embodiment 3: take by weighing HP-3.7g, add in the about 60 ℃ of water of 5ml, stirring makes dissolving, add 60mg Gallate propyl ester, stir or ultrasonic or grind and make dissolving, add water to 10ml, mixing, Gallate propyl ester and hydroxypropyl-beta-cyclodextrin inclusion solution, after filtration, fill, seal, sterilize, make injection.
Embodiment 4: take by weighing HP-3.7g, add in the about 60 ℃ of water of 5ml, stir and make dissolving, add 60mg Gallate propyl ester, stir or ultrasonic or grind and make dissolving, add water to 8ml, mixing, get Gallate propyl ester and hydroxypropyl-beta-cyclodextrin inclusion solution, add or do not add excipient (as mannitol, lactose, glucose, dextran etc.), with 0.22 μ m filtering with microporous membrane, gained solution is sub-packed in the cillin bottle, every 8ml, Gallate propyl ester freeze-dried powder is made in lyophilization.
Embodiment 5: take by weighing HP-11g and add in the about 60 ℃ of water of 50ml, stir and make dissolving, add 180mg Gallate propyl ester, stir or ultrasonic or grind and make dissolving, add sodium chloride 0.9g, dissolving adds water to 100ml, decolorizing with activated carbon, coarse filtration, fine straining, fill, sterilization, lamp inspection.Get the transfusion of Gallate propyl ester.
Embodiment 6: take by weighing HP-11g and add in about 60 ℃ of the 50ml water, stir and make dissolving, add 180mg Gallate propyl ester, stir or ultrasonic or grind and make dissolving, add glucose 5g, dissolving adds water to 100ml, decolorizing with activated carbon, coarse filtration, fine straining, fill, sterilization, lamp inspection.Get the transfusion of Gallate propyl ester.
Claims (9)
1, Gallate propyl ester injection and preparation method thereof, it is characterized in that to be the derivant of the beta-schardinger dextrin-of representative with the HP-, place water for injection, after the dissolving, add the Gallate propyl ester again, stirring or grinding or ultrasonic get Gallate propyl ester inclusion complex in solution, prepare Gallate propyl ester injection with this inclusion complex in solution.Wherein the mol ratio of Gallate propyl ester and beta-cyclodextrin derivative is 1: 1～1: 16.
2, Gallate propyl ester injection according to claim 1 and preparation method thereof is characterized in that: the optimum range of Gallate propyl ester and beta-schardinger dextrin-mol ratio is 1: 4～1: 12.
3, Gallate propyl ester injection according to claim 1 and preparation method thereof is characterized in that: said injection comprises " injection ", " freeze-dried powder ", " aseptic powder injection ", " transfusion ".
4, Gallate propyl ester injection according to claim 1 and preparation method thereof, it is characterized in that: said beta-cyclodextrin derivative mainly is meant: the beta-schardinger dextrin-substituent of hydroxypropyl, ethoxy, methyl, ethyl, sulfoalkyl, wherein preferred hydroxypropyl.
5, Gallate propyl ester injection according to claim 3 and preparation method thereof is characterized in that: said " injection " is with Gallate propyl ester inclusion complex in solution or Gallate propyl ester beta-cyclodextrin derivative clathrate powder, the injection of making.
6, Gallate propyl ester injection according to claim 3 and preparation method thereof, it is characterized in that: said " freeze-dried powder " is Gallate propyl ester inclusion complex in solution, add or do not add pharmaceutically acceptable excipient, the injectable powder that lyophilizing is made after the degerming after filtration.
7, Gallate propyl ester injection according to claim 3 and preparation method thereof, it is characterized in that: said " aseptic powder injection " is Gallate propyl ester beta-cyclodextrin derivative clathrate powder, add or do not add pharmaceutically acceptable excipient, carry out the aseptic subpackaged injectable powder of making.
8, Gallate propyl ester injection according to claim 3 and preparation method thereof, it is characterized in that: said " transfusion " is Gallate propyl ester inclusion complex in solution or Gallate propyl ester beta-cyclodextrin derivative clathrate powder, ooze formulated bulk capacity injection with sodium chloride or glucose conciliation etc.
9, according to claim 5,7 and 8 described Gallate propyl ester injections and preparation method thereof, it is characterized in that: Gallate propyl ester beta-cyclodextrin derivative clathrate powder is a Gallate propyl ester inclusion complex in solution, the powder that obtains by " vacuum drying ", " lyophilization " or " spray drying ".
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2003101146708A CN1555790A (en) | 2003-12-31 | 2003-12-31 | Propyl gallate injection liquid and its preparation method |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2003101146708A CN1555790A (en) | 2003-12-31 | 2003-12-31 | Propyl gallate injection liquid and its preparation method |
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| CN1555790A true CN1555790A (en) | 2004-12-22 |
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| Application Number | Title | Priority Date | Filing Date |
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| CNA2003101146708A Pending CN1555790A (en) | 2003-12-31 | 2003-12-31 | Propyl gallate injection liquid and its preparation method |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104510709A (en) * | 2013-09-30 | 2015-04-15 | 瑞阳制药有限公司 | Small-volume propyl gallate freeze-dried powder injection, preparation method and producing apparatus thereof |
| CN107648211A (en) * | 2017-11-10 | 2018-02-02 | 大连医科大学附属第医院 | Application of the gallic acid in angiocardiopathy is prevented and treated |
| CN110680807A (en) * | 2019-08-01 | 2020-01-14 | 广东健信制药股份有限公司 | Preparation method of propyl gallate for injection |
-
2003
- 2003-12-31 CN CNA2003101146708A patent/CN1555790A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104510709A (en) * | 2013-09-30 | 2015-04-15 | 瑞阳制药有限公司 | Small-volume propyl gallate freeze-dried powder injection, preparation method and producing apparatus thereof |
| CN107648211A (en) * | 2017-11-10 | 2018-02-02 | 大连医科大学附属第医院 | Application of the gallic acid in angiocardiopathy is prevented and treated |
| CN110680807A (en) * | 2019-08-01 | 2020-01-14 | 广东健信制药股份有限公司 | Preparation method of propyl gallate for injection |
| CN110680807B (en) * | 2019-08-01 | 2021-07-13 | 广东健信制药股份有限公司 | Preparation method of propyl gallate for injection |
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