CN104490752A - Tranexamic acid composition lyophilized tablet and preparation method thereof - Google Patents
Tranexamic acid composition lyophilized tablet and preparation method thereof Download PDFInfo
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- CN104490752A CN104490752A CN201410736147.7A CN201410736147A CN104490752A CN 104490752 A CN104490752 A CN 104490752A CN 201410736147 A CN201410736147 A CN 201410736147A CN 104490752 A CN104490752 A CN 104490752A
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Abstract
The invention provides a tranexamic acid composition lyophilized tablet and a preparation method thereof, and relates to the technical field of medicines and medicine production. The tablet is prepared from tranexamic acid, starch and can sugar, wherein starch and cane sugar are used as auxiliaries, common corn starch is subjected to heating treatment to improve the adhering and disintegrating effects of the starch in the tablet, so that the moldability of the tablet can be improved. The tranexamic acid composition lyophilized tablet only needs starch and cane sugar two auxiliaries. According to the preparation method, a twice-cooling twice-heating lyophilizing process is adopted for the tranexamic acid composition lyophilized tablet, the moldability of the tablet can be better by means of twice cooling and twice heating, the solubility of the tablet can be improved, and the bioavailability of the tablet can be improved; the tablet is capable of overcoming the defect of conventional tranexamic acid tablets and reducing the types and usage of auxiliaries in the tranexamic acid tablets, is high in solubility and high in bioavailability, and can be used for guaranteeing the curative effect and safety of clinical administration.
Description
Technical field
The present invention relates to medicine and medical production technical field, be specifically related to a kind of tranexamic acid composition freeze-drying sheet and preparation method thereof.
Background technology
The effect of tranexamic acid energy competitive inhibition activator of plasminogen, stops plasminogen to be activated as fibrinolysin, thus suppresses fibrinolysis to reach haemostatic effect.Clinical to be mainly used in preventing and treating in fibrinolytic process caused by hyperfunctioning hemorrhage, as the abnormal bleeding after the organ surgeries such as uterus, thyroid, prostate, liver spleen.
Structural formula:
molecular weight: 157.21
In common tranexamic acid sheet containing supplementary product kind and quantity more, generally to use filler, lubricant, disintegrating agent, adhesive, correctives etc., according to Chinese Pharmacopoeia (2010 editions) second tranexamic acid tablet quality standard, the dissolution of tranexamic acid sheet reached more than 75% for qualified 60 minutes time, and increasing research shows that impurity in the incompatibility of the toxic and side effects of adjuvant itself, adjuvant and principal agent, adjuvant etc. all can have an impact to the safety of medicine.
Therefore, provide one can overcome above-mentioned shortcoming, select suitable adjuvant and technique, reduce supplementary product kind and consumption in tranexamic acid sheet, improve dissolution and the bioavailability of tranexamic acid sheet, ensure that the safety of clinical application all has positive effect.
Traditional lyophilizing tablet can improve dissolution and bioavailability, but still need use the adjuvant such as mannitol, gelatin.And mannitol has certain biological activity, gelatin resource-constrained and perishable.
Starch is the basic adjuvant of oral solid formulation, it is polymerized by glucose molecule, and be commonly used for adhesive, diluent and disintegrating agent in tablets, it is cheap and easy to get, to human-body safety, but being used alone starch has no report as adjuvant freeze-dry process production tranexamic acid lyophilizing sheet.
Summary of the invention
Technical problem to be solved by this invention is the defect overcoming prior art, and propose a kind of tranexamic acid composition freeze-drying sheet and preparation method thereof further, said preparation adjuvant is few, good stability, and bioavailability is high.
Technical problem to be solved by this invention realizes by the following technical solutions:
A kind of tranexamic acid composition freeze-drying sheet, adjuvant is done with starch and sucrose, produce with freeze-dry process, this tablet overcomes the shortcoming of above-mentioned common tranexamic acid sheet, decrease supplementary product kind and consumption in tranexamic acid sheet, this sheet dissolution is large, and bioavailability is high, ensure that curative effect and the safety of clinical application.
A kind of tranexamic acid composition freeze-drying sheet, is prepared from by following raw material:
A preparation method for tranexamic acid composition freeze-drying sheet, comprises step as follows:
A, take the starch of component amount, add a certain amount of purified water and stir, by pH adjusting agent, the pH value of solution is controlled between 7.0-8.0, be then heated to 72 DEG C, be incubated 20 minutes, make the corn starch solution of 5 ~ 15% (W/V);
B, measure purified water 45ml, boil, add 85g sucrose, stir, after dissolving, continue to be heated to 100 DEG C, filter with purified cotton, the appropriate hot distilled water of filter is cleaned, and washing liquid and filtrate merge, and let cool, add appropriate distilled water, make full dose become 100ml, stir evenly, obtain B solution;
The solution that C, the solution and the step B that steps A are obtained obtain mixes, and fully stirs 30 minutes, is down to room temperature and obtains Semen Maydis-sucrose solution;
D, take tranexamic acid 125 grams, add in 1L Semen Maydis-sucrose solution, stir 25 ~ 35 minutes;
Medicinal liquid is sub-packed in drug-containing dish after measuring tranexamic acid content by E, medicinal liquid, each drug-containing dish dress 1.0ml;
F, the drug-containing dish that medicinal liquid is housed is put into vacuum freezing drying oven, be cooled to subzero 45 DEG C, keep 2 hours, evacuation, then 0 DEG C is warming up to gradually, keep 2 hours, then be cooled to subzero 45 DEG C, keep 2 hours, be warming up to 0 DEG C gradually again, keep 2 ~ 4 hours, then be warming up to 28 ~ 32 DEG C of dryings 4 ~ 6 hours gradually, whole process vacuum remains on 10 handkerchiefs; Finally the drug-containing dish lid of powder charge is covered tightly, and load aluminium foil bag and carry out sealing and obtain tranexamic acid composition freeze-drying sheet.
Described starch selects corn starch, preferably the corn starch solution of 10% (W/V).
Beneficial effect of the present invention is:
The preparation method of a kind of tranexamic acid composition freeze-drying sheet of the present invention, heating process process is carried out to common corn starch, starch bonding in tablets, disintegration can be improved, improve the mouldability of tablet, in tranexamic acid composition freeze-drying sheet, dosage of sucrose is 8.5% (W/V), it is the hardness reinforcer of this tablet, and plays flavored action.Tranexamic acid composition freeze-drying sheet only needs starch and sucrose two kinds of adjuvants.The freeze-dry process of two liters falls in tranexamic acid composition freeze-drying sheet employing two, and twice cooling, twice intensification can make sheet mouldability better, which increase the dissolution of tablet, thus improve the bioavailability of tablet.
Accompanying drawing explanation
Fig. 1 is the dissolution correlation curve figure of tranexamic acid in experiment.
Detailed description of the invention
The technological means realized to make the present invention, creation characteristic, reaching object and effect is easy to understand, below in conjunction with specific embodiment, set forth the present invention further, but following embodiment being only the preferred embodiments of the present invention, and not all.Based on the embodiment in embodiment, those skilled in the art under the prerequisite not making creative work obtain other embodiment, all belong to the protection domain of this patent.
Embodiment 1
A, take the corn starch of 100g, the purified water adding 900ml stirs, and controls at 7.0-8.0, is then heated to 72 DEG C, keep 120 minutes, make the corn starch solution of 9% (W/V) by pH adjusting agent by the pH value of solution.
B, measure purified water 45ml, boil, add 85g sucrose, stir, after dissolving, continue to be heated to 100 DEG C, filter with purified cotton, the appropriate hot distilled water of filter is cleaned, and washing liquid and filtrate merge, and let cool, add appropriate distilled water, make full dose become 100m L, stir evenly, obtain B solution.
The solution that C, the solution and the step B that steps A are obtained obtain mixes, and fully stirs 30 minutes, after solution be down to room temperature obtain Semen Maydis-sucrose solution.
D, take tranexamic acid 125g, add in 1L Semen Maydis-sucrose solution, stir 30 minutes.
Medicinal liquid is sub-packed in drug-containing dish after measuring tranexamic acid content by E, medicinal liquid, each drug-containing dish dress 1.0ml.
F, the drug-containing dish that medicinal liquid is housed is put into vacuum freezing drying oven, be cooled to subzero 45 DEG C, keep 2 hours, evacuation, then 0 DEG C is warming up to gradually, keep 2 hours, then be cooled to subzero 45 DEG C, keep 2 hours, be warming up to 0 DEG C gradually again, keep 2 ~ 4 hours, then be warming up to 28 ~ 32 DEG C of dryings 4 ~ 6 hours gradually, whole process vacuum remains on 10 handkerchiefs.Finally the drug-containing dish lid of powder charge is covered tightly, and load aluminium foil bag and carry out sealing and obtain tranexamic acid composition freeze-drying sheet.
Embodiment 2
A, take the corn starch of 130g, the purified water adding 900ml stirs, and controls at 7.0-8.0, is then heated to 72 DEG C, keep 120 minutes, make the corn starch solution of 13% (W/V) by pH adjusting agent by the pH value of solution.
B, measure purified water 45ml, boil, add 85g sucrose, stir, after dissolving, continue to be heated to 100 DEG C, filter with purified cotton, the appropriate hot distilled water of filter is cleaned, and washing liquid and filtrate merge, and let cool, add appropriate distilled water, make full dose become 100m L, stir evenly, obtain B solution.
The solution that C, the solution and the step B that steps A are obtained obtain mixes, and fully stirs 30 minutes, after solution be down to room temperature obtain Semen Maydis-sucrose solution.
D, take tranexamic acid 125 grams (by 1000 calculations), add 1L Semen Maydis-sucrose solution, stir 30 minutes.
Medicinal liquid is sub-packed in drug-containing dish after measuring tranexamic acid content by E, medicinal liquid, each drug-containing dish dress 1.0ml.
F, the drug-containing dish that medicinal liquid is housed is put into vacuum freezing drying oven, be cooled to subzero 45 DEG C, keep 2 hours, evacuation, then 0 DEG C is warming up to gradually, keep 2 hours, then be cooled to subzero 45 DEG C, keep 2 hours, be warming up to 0 DEG C gradually again, keep 2 ~ 4 hours, then be warming up to 28 ~ 32 DEG C of dryings 4 ~ 6 hours gradually, whole process vacuum remains on 10 handkerchiefs.Finally the drug-containing dish lid of powder charge is covered tightly, and load aluminium foil bag and carry out sealing and obtain tranexamic acid composition freeze-drying sheet.
Experimental data
The tranexamic acid composition freeze-drying sheet that above-described embodiment is obtained carries out following quality research test:
1, hardness, friability contrast test
Get tranexamic acid composition freeze-drying sheet prepared by above-described embodiment respectively and tranexamic acid ordinary tablet (commercially available) detects friability and hardness by " Chinese Pharmacopoeia " version in 2010 two annex X G inspection techniques, carried out comparative study, the results are shown in following table:
| Sample | Hardness/N | Friability |
| Execute example 1 | 65 | <1％ |
| Execute example 2 | 69 | <1％ |
| Ordinary tablet (commercially available) | 68 | <1％ |
Experimental data shows, tranexamic acid composition freeze-drying sheet and ordinary tablet (commercially available) without significant difference, meet " Chinese Pharmacopoeia " version in 2010 to the requirement of tablet on friability and hardness.
2, dissolution contrast test
(No. 1 to No. 3 is embodiment 1 to get tranexamic acid sheet (commercially available) and each 6 of tranexamic acid composition freeze-drying sheet, No. 4 to No. 6 is embodiment 2), press Chinese Pharmacopoeia (2010 editions) second dissolution method annex X C first method respectively, with water 1000ml for dissolution medium, rotating speed is 100 turns per minute, operate in accordance with the law, respectively when 10min, 20min, 40min, 60min, 90min, get solution 10ml to filter, get continuous worry liquid, if desired, dilute with water makes the solution about containing tranexamic acid 0.125mg in every 1ml, as need testing solution; Separately get tranexamic acid reference substance, accurately weighed, add aqueous solution and dilute the solution made about containing tranexamic acid 0.125mg in every 1ml, product solution in contrast; According to the chromatographic condition under assay item, precision measures need testing solution and each 100ul of reference substance solution, respectively injection liquid chromatography, and record chromatogram, by the stripping quantity of the every sheet of external standard method calculated by peak area.Result is as follows:
One, tranexamic acid sheet (commercially available)
Two, tranexamic acid lyophilizing sheet (No. 1 to No. 3 is embodiment 1, and No. 4 to No. 6 is embodiment 2)
Respectively with catch cropping Dissolution profiles during average dissolution pair, as Fig. 1.
Four, result judges
Judge according to Chinese Pharmacopoeia (2010 editions) second tranexamic acid tablet quality standard, the dissolution of tranexamic acid sheet (commercially available) reached more than 75% for qualified 60 minutes time, actual measurement is 76.1%, and tranexamic acid lyophilizing sheet dissolution 20 minutes time reaches 76.9%.It can thus be appreciated that the time that tranexamic acid lyophilizing sheet dissolution reaches 75% decreased for about 66.7% (40 minutes) time than tranexamic acid sheet (commercially available).So the tranexamic acid lyophilizing sheet blood drug level peaking time is shorter than tranexamic acid sheet (commercially available), and bioavailability is higher, better efficacy.
More than show and describe ultimate principle of the present invention, principal character and advantage of the present invention.The technical staff of the industry should understand; the present invention is not restricted to the described embodiments; what describe in above-described embodiment and description is only preference of the present invention; be not used for limiting the present invention; without departing from the spirit and scope of the present invention; the present invention also has various changes and modifications, and these changes and improvements all fall in the claimed scope of the invention.Application claims protection domain is defined by appending claims and equivalent thereof.
Claims (2)
1. a tranexamic acid composition freeze-drying sheet, is characterized in that, is prepared from by following raw material:
2. a preparation method for tranexamic acid composition freeze-drying sheet according to claim 1, is characterized in that, comprise step as follows:
A, take the starch of component amount, add a certain amount of purified water and stir, by pH adjusting agent, the pH value of solution is controlled between 7.0-8.0, be then heated to 72 DEG C, be incubated 20 minutes, make the corn starch solution of 5 ~ 15% (W/V);
B, measure purified water 45ml, boil, add 85g sucrose, stir, after dissolving, continue to be heated to 100 DEG C, filter with purified cotton, the appropriate hot distilled water of filter is cleaned, and washing liquid and filtrate merge, and let cool, add appropriate distilled water, make full dose become 100ml, stir evenly, obtain B solution;
The solution that C, the solution and the step B that steps A are obtained obtain mixes, and fully stirs 30 minutes, is down to room temperature and obtains Semen Maydis-sucrose solution;
D, take tranexamic acid 125 grams, add in 1L Semen Maydis-sucrose solution, stir 25 ~ 35 minutes;
Medicinal liquid is sub-packed in drug-containing dish after measuring tranexamic acid content by E, medicinal liquid, each drug-containing dish dress 1.0ml;
F, the drug-containing dish that medicinal liquid is housed is put into vacuum freezing drying oven, be cooled to subzero 45 DEG C, keep 2 hours, evacuation, then 0 DEG C is warming up to gradually, keep 2 hours, then be cooled to subzero 45 DEG C, keep 2 hours, be warming up to 0 DEG C gradually again, keep 2 ~ 4 hours, then be warming up to 28 ~ 32 DEG C of dryings 4 ~ 6 hours gradually, whole process vacuum remains on 10 handkerchiefs; Finally the drug-containing dish lid of powder charge is covered tightly, and load aluminium foil bag and carry out sealing and obtain tranexamic acid composition freeze-drying sheet.
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| CN201410736147.7A CN104490752A (en) | 2014-12-05 | 2014-12-05 | Tranexamic acid composition lyophilized tablet and preparation method thereof |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106265581A (en) * | 2016-09-30 | 2017-01-04 | 上海信谊万象药业股份有限公司 | A kind of tranexamic acid sheet and preparation method thereof |
| CN113667706A (en) * | 2021-10-22 | 2021-11-19 | 中国人民解放军军事科学院军事医学研究院 | Tranexamic acid-loaded cross-linked porous starch and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
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| JPS61242556A (en) * | 1985-04-19 | 1986-10-28 | Hatoya Seika:Kk | Preparation of snack using fruits |
| US20020173016A1 (en) * | 2001-03-27 | 2002-11-21 | Helmut Wurst | High-throughput nucleic acid polymerase devices and methods for their use |
| CN1390539A (en) * | 2002-07-25 | 2003-01-15 | 于航 | Freeze-dried tranexamine powder injection and its preparing prcess |
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2014
- 2014-12-05 CN CN201410736147.7A patent/CN104490752A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS61242556A (en) * | 1985-04-19 | 1986-10-28 | Hatoya Seika:Kk | Preparation of snack using fruits |
| US20020173016A1 (en) * | 2001-03-27 | 2002-11-21 | Helmut Wurst | High-throughput nucleic acid polymerase devices and methods for their use |
| CN1390539A (en) * | 2002-07-25 | 2003-01-15 | 于航 | Freeze-dried tranexamine powder injection and its preparing prcess |
Non-Patent Citations (1)
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| 刘晓睿等: "口腔速溶片的研究进展", 《中南药学》 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106265581A (en) * | 2016-09-30 | 2017-01-04 | 上海信谊万象药业股份有限公司 | A kind of tranexamic acid sheet and preparation method thereof |
| CN113667706A (en) * | 2021-10-22 | 2021-11-19 | 中国人民解放军军事科学院军事医学研究院 | Tranexamic acid-loaded cross-linked porous starch and preparation method thereof |
| CN113667706B (en) * | 2021-10-22 | 2022-02-18 | 中国人民解放军军事科学院军事医学研究院 | Tranexamic acid-loaded cross-linked porous starch and preparation method thereof |
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Application publication date: 20150408 |