CN104414991A - Tranexamic acid solid sustained-release tablets and preparation method thereof - Google Patents
Tranexamic acid solid sustained-release tablets and preparation method thereof Download PDFInfo
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- CN104414991A CN104414991A CN201310398381.9A CN201310398381A CN104414991A CN 104414991 A CN104414991 A CN 104414991A CN 201310398381 A CN201310398381 A CN 201310398381A CN 104414991 A CN104414991 A CN 104414991A
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Abstract
The invention relates to the field of pharmaceutical preparations, and particularly relates to tranexamic acid solid sustained-release tablets and a preparation method thereof. The tranexamic acid solid sustained-release tablets comprise, in percentage by weight, 40-60% of tranexamic acid, 35-55% of an insoluble sustained-release framework material and 0.5-5% of a lubricant. The auxiliary materials involved in the tranexamic acid solid sustained-release tablets disclosed by the invention are low in price, easily available and large in selection range; the preparation process is simple, the preparation modes are various, the proper process can be selected according to the existing equipment, and industrialized production is promoted; the solid preparation prepared from the insoluble sustained-release framework material is low in ambient environment influence on in-vitro release, low in intra-batch and inter-batch difference, and stable in quality.
Description
Technical field
The present invention relates to field of medicine preparations, particularly relate to tranexamic acid solid slow-release tablet and preparation method thereof.
Background technology
Menorrhagia, refer to menstrual period more than 7 d or (with) menorrhagia is in the pathological phenomenon of 80 mL, it is the common sympton of child-bearing period and perimenopausal women, the cause of disease comprises dysfunctional uterine bleeding and organic disease, and worldwide the Women of Childbearing Age of about 30% has suffered from menorrhagia.In the U.S., the women of 300 ten thousand is about had to be diagnosed as menorrhagia every year; In Britain, menorrhagia accounts for 50% of the uterectomy cause of disease.Menorrhagia is a serious social problem, not only can cause serious anemia, also can affect patient's doings, sexual life and mental health, drastically influence the quality of life of patient.The menorrhagia patient of about 35% finally will select operative treatment, but select in the patient of hysterectomy all because of menorrhagia, and after the operation in patients of nearly 50%, specimens pathological section in uterus shows as normal.Clinically these be can not find to the menorrhagia patient (except menorrhagia, though do not find any endocrine function exception and organic disease through minute inspection) of reason, summarize with idiopathic menorrhagia.Based on risk and the related complication of operation, especially youth is given birth to the women of requirement or menopause nearly, operation is non-best choice also, and appropriate Drug therapy can obviously reduce operation ratio.Drug therapy has noinvasive, retains the advantage of reproductive function, and Therapeutic Method comprises takes progestogens medicine, anti-fibrinolytic treatment, non-steroidal anti-inflammatory drugs etc.Progestogens medicine treats menorrhagia at present to use maximum medicines.Research also confirms that progestational hormone medicine can be used as luteal phase replacement therapy and effectively reduces the menstrual blood volume of the too much patient of anovulatory menstruation.But for ovulatory menorrhagia patient, progestogens medicine is only effective to the patient of 20%.In Europe and Britain, tranexamic acid is as idiopathic (agnogenic) menorrhagia patient, the first-line drug having fertility requirement or the menorrhagia patient selecting hormone therapy that is unwilling in the recent period.Research shows, the too much women of severe menstrual is taking tranexamic acid 2 ~ 3g/ days, after taking 5 days continuously, reduces the activity of its endometrium activator of plasminogen, and decreases menses fibrinolytic, reach good curative effect.In addition, the tranexamic acid blood drug level in health volunteer's body lower than 10mg/mL for platelet count, clotting time etc. by ineffective.So, tranexamic acid is prepared into slow releasing preparation and will produces good curative effect to treatment menorrhagia.But tranexamic acid is soluble in water, hydrophilic is extremely strong, so how to control its drug release rate, making it maintain steady plasma-drug concentration in menstrual period becomes difficult point in this medicine preparation.
Current tranexamic acid dosage form of going on the market at home has conventional tablet, capsule, injection powder pin, injection, for general hemostasis.Domestic have one section of patent, disclose a kind of formula and the preparation method of preparing tranexamic acid slow releasing preparation, tabletting (or preparing granule or fill capsule) after the method adopts and tranexamic acid and hydrophilic gel framework material are carried out wet granulation, or adopt dry granulation tabletting, or the mode of direct powder compression.And the present invention is by research, achieve the method preparing tranexamic acid slow releasing tablet that another is different with it, tabletting or direct powder compression after namely adopting insoluble framework material to granulate, and in contrast, the mode of preparation is more versatile and flexible.
Summary of the invention
The object of the present invention is to provide the tranexamic acid slow-release solid tablet of good stability, for a long time blood drug level that maintenance is stable.
Another object of the present invention is to provide the preparation method that a kind of preparation technology is simple, be applicable to the tranexamic acid slow-release solid preparation of industrialization.
In order to realize foregoing invention object, the present invention adopts following technical scheme:
Tranexamic acid solid slow-release tablet, described tranexamic acid solid slow-release tablet comprises tranexamic acid 40% ~ 60% by weight percentage, insoluble sustained-release matrix material 35% ~ 55%, lubricant 0.5% ~ 5%.
Described insoluble sustained-release matrix material is one kind of multiple mixing in octadecanol, stearic acid, Brazil wax, hydrogenated vegetable oil, ethyl cellulose.
Described lubricant is one or more mixing in magnesium stearate, stearic acid, silicon dioxide, Pulvis Talci, the stearic sodium of fumaric acid, Polyethylene Glycol.
Can also comprise not higher than 3% binding agent, binding agent be selected from polyvidone, hypromellose, sucrose, gelatin, sodium carboxymethyl cellulose one or more mixing.
The invention also discloses the preparation method of tranexamic acid solid slow-release tablet, carry out tabletting again after tranexamic acid and pharmaceutical adjunct being granulated by wet granulation, dry granulation or melt granulation technique and obtain.
Tranexamic acid solid slow-release tablet disclosed in this invention compared with prior art has following following advantage:
(1) the adjuvant low price related in compositions, easily obtains, and large (2) preparation technology of the range of choice is simple, and preparation method is varied, can according to the suitable technique of existing equipment choice, and is conducive to industrialization and produces; (3) solid preparation adopting insoluble sustained-release matrix material to be prepared from, release in vitro is little by the impact of surrounding, in batch, the little and steady quality of differences between batches.
Detailed description of the invention
Below by specific embodiment, the present invention is described further.
Embodiment 1: prepare 2000 tranexamic acid slow releasing tablets, adopt following material:
Prescription: tranexamic acid 500g
Octadecanol 500g
Magnesium stearate 10g
Preparation technology: pulverized by tranexamic acid, crosses 120 mesh sieves, for subsequent use; Octadecanol is melt into liquid state under 70-80 DEG C of condition; Under 70-80 DEG C of heat-retaining condition, add wherein by the tranexamic acid after pulverizing while stirring, make abundant mix homogeneously, incline rapidly mixture in pallet, make to be cooled to room temperature, sample solidifies; Solid pulverizer after solidifying is crushed to below 30 orders, finally adds magnesium stearate, after mix homogeneously, tabletting, to obtain final product.
Embodiment 2: prepare 2000 tranexamic acid slow releasing tablets, adopt following material:
Prescription: tranexamic acid 539g
Brazil wax 431g
Polyvidone 20g
Magnesium stearate 10g
Preparation technology: pulverized by tranexamic acid, crosses 120 mesh sieves, for subsequent use; Brazil wax is crossed 80 orders, for subsequent use; Polyvidone water is mixed with the solution of 10% concentration, as binding agent; By tranexamic acid and Brazil wax mix homogeneously, add binding agent soft material, cross 30 orders and granulate, wet granular is dried to moisture lower than 4% under 50-60 DEG C of condition; Discharging, cross 30 mesh sieve granulate, finally add magnesium stearate, after mix homogeneously, tabletting, to obtain final product.
Embodiment 3: prepare 2000 tranexamic acid slow releasing tablets, adopt following material:
Prescription: tranexamic acid 461g
Ethyl cellulose 532g
Magnesium stearate 8g
Preparation technology: pulverized by tranexamic acid, crosses 120 mesh sieves, for subsequent use; Ethyl cellulose is crossed 80 orders, for subsequent use; Get the ethyl cellulose of 5% recipe quantity, be mixed with the solution of 10% concentration with 95% ethanol, as binding agent; By tranexamic acid and the ethyl cellulose mix homogeneously remaining 95% recipe quantity, add binding agent soft material, cross 30 orders and granulate, wet granular is dried to moisture lower than 4% under 50-60 DEG C of condition; Discharging, cross 30 mesh sieve granulate, finally add magnesium stearate, after mix homogeneously, tabletting, to obtain final product.
Experimental example:
The dissolved corrosion that the sample prepare embodiment 1,2,3 and LYSTEDA carry out in external different medium contrasts.Their Dissolution Test in vitro condition is:
Adopt Chinese Pharmacopoeia 2010 editions annex XC dissolution determination method second methods; Dissolution medium is respectively 0.1mol/L hydrochloric acid solution, pH4.5 acetate buffer, pH6.8 phosphate buffer, water; Dissolution medium volume is 900mL, and rotating speed is 50 turns, in 0.5,1,2,3,4h sampling, calculate cumulative leaching rate, compare the f2 similar factors of each sample and control formulation LYSTEDA, will the results are shown in following form:
(1) dissolution medium: water
F2 similar factors: embodiment 1 is 82, embodiment 2 is 90, and embodiment 3 is 72.
(2) dissolution medium: pH4.5 acetate buffer
F2 similar factors: embodiment 1 is 84, embodiment 2 is 88, and embodiment 3 is 74.
(3) dissolution medium: pH6.8 phosphate buffer
F2 similar factors: embodiment 1 is 81, embodiment 2 is 92, and embodiment 3 is 72.
(4) dissolution medium: 0.1mol/L hydrochloric acid solution
F2 similar factors: embodiment 1 is 81, embodiment 2 is 88, and embodiment 3 is 72.
Above result shows, obtained tablet can reach slow releasing in 3h, and compared with listing control formulation, in medium, In-vitro release curves is similar, thus tentatively can predict its in vivo with control formulation bioequivalence.
Claims (5)
1. tranexamic acid solid slow-release tablet, is characterized in that described tranexamic acid solid slow-release tablet comprises tranexamic acid 40% ~ 60% by weight percentage, insoluble sustained-release matrix material 35% ~ 55%, lubricant 0.5% ~ 5%.
2. tranexamic acid solid slow-release tablet according to claim 1, is characterized in that described insoluble sustained-release matrix material is one kind of multiple mixing in octadecanol, stearic acid, Brazil wax, hydrogenated vegetable oil, ethyl cellulose.
3. tranexamic acid solid slow-release tablet according to claim 1, is characterized in that described lubricant is one or more mixing in magnesium stearate, stearic acid, silicon dioxide, Pulvis Talci, the stearic sodium of fumaric acid, Polyethylene Glycol.
4. tranexamic acid solid slow-release tablet according to claim 1, it is characterized in that comprising not higher than 3% binding agent, binding agent is selected from one or more mixing in polyvidone, hypromellose, sucrose, gelatin, sodium carboxymethyl cellulose.
5., according to the preparation method of the tranexamic acid solid slow-release tablet described in claim 1 ~ 4, it is characterized in that obtaining by carrying out tabletting again after the granulation of wet granulation, dry granulation or melt granulation technique.
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Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104804718A (en) * | 2015-05-04 | 2015-07-29 | 中国石油集团渤海钻探工程有限公司 | Sustained-release solid acid for water injection wells in oil fields, and preparation method of sustained-release solid acid |
| 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 |
| CN110721169A (en) * | 2019-11-29 | 2020-01-24 | 湖南洞庭药业股份有限公司 | Preparation method of tranexamic acid tablets |
| CN112641718A (en) * | 2020-12-25 | 2021-04-13 | 山东大学 | Taste-masking compound based on porous carrier and preparation method and application thereof |
| CN113663118A (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 | Application of esterified modified starch hemostatic material |
| RU2814336C1 (en) * | 2022-04-20 | 2024-02-28 | Асена Фармасьютик Сас | High-dose composition of tranexamic acid and methods for its preparation |
| CN117731649A (en) * | 2023-12-21 | 2024-03-22 | 博济医药科技股份有限公司 | Tranexamic acid pharmaceutical composition and preparation process thereof |
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| US20050025825A1 (en) * | 2003-07-31 | 2005-02-03 | Xanodyne Pharmacal, Inc. | Tranexamic acid formulations with reduced adverse effects |
| CN102525878A (en) * | 2010-12-31 | 2012-07-04 | 北京万全阳光医学技术有限公司 | Tranexamic acid sustained-release solid composition and preparation method thereof |
| CN103054861A (en) * | 2012-12-29 | 2013-04-24 | 北京阜康仁生物制药科技有限公司 | Compound solid preparation containing tranexamic acid |
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| US20050025825A1 (en) * | 2003-07-31 | 2005-02-03 | Xanodyne Pharmacal, Inc. | Tranexamic acid formulations with reduced adverse effects |
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| CN103054861A (en) * | 2012-12-29 | 2013-04-24 | 北京阜康仁生物制药科技有限公司 | Compound solid preparation containing tranexamic acid |
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Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104804718A (en) * | 2015-05-04 | 2015-07-29 | 中国石油集团渤海钻探工程有限公司 | Sustained-release solid acid for water injection wells in oil fields, and preparation method of sustained-release solid acid |
| 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 |
| CN110721169A (en) * | 2019-11-29 | 2020-01-24 | 湖南洞庭药业股份有限公司 | Preparation method of tranexamic acid tablets |
| CN112641718A (en) * | 2020-12-25 | 2021-04-13 | 山东大学 | Taste-masking compound based on porous carrier and preparation method and application thereof |
| CN112641718B (en) * | 2020-12-25 | 2022-07-29 | 山东大学 | Taste-masking compound based on porous carrier and preparation method and application thereof |
| CN113663118A (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 | Application of esterified modified starch hemostatic material |
| RU2814336C1 (en) * | 2022-04-20 | 2024-02-28 | Асена Фармасьютик Сас | High-dose composition of tranexamic acid and methods for its preparation |
| CN117731649A (en) * | 2023-12-21 | 2024-03-22 | 博济医药科技股份有限公司 | Tranexamic acid pharmaceutical composition and preparation process thereof |
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