CN105362245A - Tablet composition with solifenacin and preparation method of tablet composition - Google Patents
Tablet composition with solifenacin and preparation method of tablet composition Download PDFInfo
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- CN105362245A CN105362245A CN201410435887.7A CN201410435887A CN105362245A CN 105362245 A CN105362245 A CN 105362245A CN 201410435887 A CN201410435887 A CN 201410435887A CN 105362245 A CN105362245 A CN 105362245A
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- tablet composition
- active component
- silicon dioxide
- pregelatinized starch
- tablet
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Abstract
The invention discloses a formula of a medicine composition with solifenacin and a preparation method of the tablet composition. The active component of the medicine composition is (1S)-(3R)-1-azabicyalo[2.2.2]oct-3-yl3,4-dihydro-l-phenyl-2-(1H)-isoquinoline carboxylic acid succinate (solifenacin). The preparation method includes the steps of smashing the active component and corresponding auxiliaries respectively, conducting physical mixing, conducting direct tabletting on dry powder, wrapping film coatings on tablets, and obtaining the medicine composition. The tablets can be used for treating or improving symptoms of overactive bladder including frequent micturition, urgent urination, acute urinary incontinence and other urinary tract symptoms.
Description
Technical field
The present invention relates to formula of a kind of YM-905 solid tablet and preparation method thereof, belong to chemical medicine pharmaceutical field.
Background technology
Overactive bladder is the syndrome formed with the symptoms such as urgent micturition, frequent micturition, urge incontinence etc.According to statistics, its sickness rate women, apparently higher than male, shows according to correlational study: total M1-55 the hypotype that the m receptor of detrusor of bladder is known at present.What wherein play a major role is M2 and M3 two hypotypes, and M3 receptor plays a major role in the contraction of mediation detrusor.The Etiological of overactive bladder is caused by the over-activity due to the m receptor of detrusor of bladder as can be seen here.It is reported, the M3 receptor of a series of quinuclidine derivatives to detrusor of bladder comprising succinic acid YM-905 or its salt has splendid selection antagonism, can be used as preventive or the therapeutic agent of the urinary disorders such as overactive bladder thus.These disease serious various aspects affecting minimal invasive treatment, reduce patients ' life quality, cause and bear at heart, also can cause other diseases etc. to patient.
At present, succinic acid YM-905 technology of preparing is succeeded in developing by external professional R&D team is up-to-date, is bought and the patented right to use by my company, and the domestic new drug registration that there is no containing this composition is declared.And the existing Therapeutic Method for overactive bladder has following several clinically: Drug therapy, Spinal injury, behavior therapy and other.There is all drawbacks in existing Therapeutic Method: takes effect slow; Patient's cure rate is low; Therapeutic Method is loaded down with trivial details; Clinical application degree difference etc.Therefore, various countries' medical treatment R&D team all takes much count of the exploitation of the new method for the treatment of overactive bladder.
Research finds, succinic acid YM-905 composition has the curative effect obviously treating or improve overactive bladder symptom.Compared with existing Therapeutic Method clinically, there is the advantages such as curative effect is obvious, Therapeutic Method is easy, non-evident effect, there is wide clinical expansion prospect of the application.
Lactose is a kind of excellent tablet filler, and the tablet made is bright and clean, attractive in appearance, and hardness is suitable for, and release medicine is very fast, and the assay of little effect principal agent, storage of a specified duration does not extend the disintegration of tablet, is particularly useful for drawing moist medicine.Lactose is soluble in water, moist without drawing, the mobility that tool is good, compressibility, stable in properties, can with most drug compatibility.Its mobility, compressibility are good, can for direct powder compression.
Microcrystalline Cellulose is the white group white powder of odorless, tasteless, and adhesion type is good, has lubrication, bonding and the effect of disintegrate concurrently.Have good compressibility, have stronger adhesion, the tablet be pressed into has and has hardness more greatly, and " dry adhesives " that can be used as direct powder compression uses.The dissolution of that new component of rope succinic acid profit can be improved, accelerate curative effect.
Pregelatinized Starch is again modified starch, odorless, and micro-have special mouthfeel, has mobility and direct compressibility, is commonly used for the binding agent of oral tablet and capsule, diluent and disintegrating agent at pharmaceutical field.Its good disintegrative is conducive to the release of succinic acid YM-905 composition, increases rate of releasing drug thus is conducive to the raising of bioavailability.
By the analysis to several composition of YM-905 solid tablet, can find that they can play auxiliary film-making and improve the effect of dissolution, disintegration in solid tablet, and then improve the bioavailability of patient to succinic acid YM-905 effective ingredient, route of administration is easy, has clinical expansion prospect and meaning.
Summary of the invention
The object of the invention is to provide a kind of formula and preparation process for the treatment of the solid tablet of overactive bladder symptom, it is characterized in that: with succinic acid YM-905 for functional component, add lactose, microcrystalline Cellulose, pregelatinized Starch, in silicon dioxide three kinds or four kinds of compositions as pharmaceutic adjuvant, through dressing sieve, weigh, mixing, tabletting, coating obtains succinic acid YM-905 sheet solid tablet.It is obvious that this tablet has therapeutic effect, and route of administration is easy, without the advantage of other side effect.
Product preparation process implementation step of the present invention is as follows:
1, by succinic acid YM-905 raw material pulverizing, 80 mesh sieves are crossed, for subsequent use after weighing by the percentage by weight of formula;
2, by various adjuvant, pulverize respectively, cross 80 mesh sieves, weigh rear for subsequent use respectively by the percentage by weight of formula;
3, will, according to formula ratio load weighted succinic acid YM-905 powder and each adjuvant powder, equal increments method be adopted to carry out sufficient physical mixed;
4, the material mixed is put in tablet machine, under temperature 18 DEG C-26 DEG C, humidity 45%-65% condition, adopt the pressure of 70-90N to carry out tabletting;
5, the plain sheet will suppressed, is placed in film coater, carries out coating, to obtain final product under the condition of 0.25kg/min.
detailed description of the invention case
Case study on implementation 1
Succinic acid YM-905 5g
Lactose 74.3g
Pregelatinized Starch 20g
Silicon dioxide 0.7g
Namely succinic acid YM-905 powder and lactose, pregelatinized Starch, silicon dioxide dressing sieve, mixing, tabletting, coating are obtained YM-905 sheet solid tablet 1.
Case study on implementation 2
Succinic acid YM-905 5g
Lactose 47.25g
Microcrystalline Cellulose 37.25g
Pregelatinized Starch 10g
Silicon dioxide 0.5g
Namely succinic acid YM-905 powder and lactose, microcrystalline Cellulose, pregelatinized Starch, silicon dioxide dressing sieve, mixing, tabletting, coating are obtained YM-905 sheet solid tablet 2.
Case study on implementation 3
Succinic acid YM-905 5g
Microcrystalline Cellulose 84g
Pregelatinized Starch 10.5g
Silicon dioxide 0.5g
Namely succinic acid YM-905 powder and microcrystalline Cellulose, pregelatinized Starch, silicon dioxide dressing sieve, mixing, tabletting, coating are obtained YM-905 sheet solid tablet 3.
YM-905 sheet solid tablet index test scheme
1. drying (calcination) weightlessness=(W1-W2)/W1*100%
W1: the example weight that dry (calcination) is front
W2: the example weight after dry (calcination)
W1-W2: the example weight of less loss in dry (calcination)
2. test disintegration: the solid tablet in above-mentioned case study on implementation is carried out numbering 1,2,3, after disintegration time tester water temperature temperature control 37 ± 1 DEG C is constant, respectively get 6,1,2, No. 3 sample tablet respectively and be placed in disintegration time mensuration instrument screen cloth, start disintegration tester, observe phenomena is also noted down.
Specific experiment result is as follows:
| Sample number into spectrum | Tablet appearance | Loss on drying | Calcination loss | Disintegration |
| Solid tablet 1 | Tablet compactibility is better, smooth in appearance, and hardness is not enough, and compressive resistance is little | 0.369% | 0.083% | 13min |
| Solid tablet 2 | Tablet surface is smooth, and hardness is better, and tablet compactibility is general | 0.324% | 0.076% | 14min |
| Solid tablet 3 | Flap-type is better, and hardness is moderate, and mouldability is better, smooth in appearance | 0.351% | 0.079% | 11min |
Claims (7)
1. the tablet composition containing YM-905, is characterized in that: said composition contains active component and other pharmaceutic adjuvants, and percentage by weight sum shared by both is 100%; Wherein active component is 1
s)-(3
r)-l-azabicyclo [2.2.2] oct-3-yl 3,4-dihydro-l-phenyl-2 (1
h)-isoquinolinecarboxylic acid ester succinate (YM-905), adjuvant is that the three kinds or more in lactose, microcrystalline Cellulose, pregelatinized Starch, silicon dioxide combines.
2. containing the tablet composition of YM-905, its preparation technology is characterised in that: adopt dry powder direct tabletting method, and active component and other pharmaceutic adjuvants are pulverized respectively, the two carries out sufficient physical mixed, then carries out tabletting, film coating and get final product.
3. the active component according to YM-905 tablet composition according to claim 1 is characterized in that: character, for white is to off-white color crystalline powder, is soluble in methanol, chloroform and water, is soluble in dimethyl formamide, acetic acid, dimethyl formamide be dissolved in ethanol; It is consistent that its infrared spectrum differentiates to differentiate all to prepare solution with standard substance with HPLC method; Its addition is 2.5%-5%.
4. according to YM-905 tablet composition according to claim 1, it is characterized in that: pharmaceutic adjuvant is made up of lactose, pregelatinized Starch, silicon dioxide, its addition is respectively 65%-75%, 15%-20%, 0.3%-0.7%.
5. according to YM-905 tablet composition according to claim 1, it is characterized in that: pharmaceutic adjuvant is made up of lactose, microcrystalline Cellulose, pregelatinized Starch, silicon dioxide, its addition is respectively 45%-50%, 35%-40%, 10%-15%, 0.3%-0.6%.
6. according to YM-905 tablet composition according to claim 1, it is characterized in that: pharmaceutic adjuvant is made up of microcrystalline Cellulose, pregelatinized Starch, silicon dioxide, its addition is respectively as 80%-85%, 10-15%, 0.3%-0.7%.
7. according to dry powder sheeting method according to claim 2, it is characterized in that: under temperature 18 DEG C-26 DEG C, humidity 45%-65% condition, YM-905 xeraphium and other pharmaceutic adjuvants were carried out 80 mesh sieve dressing sieve process respectively, the moisture content of powder is at 3%-5%, above-mentioned YM-905 and pharmaceutic adjuvant is taken again according to percentage by weight, and adopted equal increments method to carry out sufficient physical mixed, mixture being carried out tableting pressure is again 70-90N, adopt film coating pre-mix dose to carry out coating under the condition of 0.25kg/min, to obtain final product.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410435887.7A CN105362245A (en) | 2014-08-30 | 2014-08-30 | Tablet composition with solifenacin and preparation method of tablet composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410435887.7A CN105362245A (en) | 2014-08-30 | 2014-08-30 | Tablet composition with solifenacin and preparation method of tablet composition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105362245A true CN105362245A (en) | 2016-03-02 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410435887.7A Pending CN105362245A (en) | 2014-08-30 | 2014-08-30 | Tablet composition with solifenacin and preparation method of tablet composition |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104523628A (en) * | 2014-12-24 | 2015-04-22 | 乐普药业股份有限公司 | Succinic acid solifenacin tablet capable of achieving direct powder compression and preparation method of succinic acid solifenacin tablet |
| CN113456639A (en) * | 2020-03-31 | 2021-10-01 | 江苏康缘药业股份有限公司 | Anti-arrhythmia pharmaceutical composition and preparation method thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008128028A2 (en) * | 2007-04-11 | 2008-10-23 | Dr. Reddy's Laboratories Ltd. | Solifenacin compositions |
| WO2010097243A2 (en) * | 2009-02-27 | 2010-09-02 | Krka, D. D., Novo Mesto | Process for forming solid oral dosage forms of solifenacin and its pharmaceutically acceptable salts |
| CN102887894A (en) * | 2011-07-18 | 2013-01-23 | 天津市医药集团技术发展有限公司 | Crystal form of solifenacin succinate and preparation method thereof |
| CN103585123A (en) * | 2013-10-09 | 2014-02-19 | 北京万全德众医药生物技术有限公司 | Solifenacin succinate-containing orally disintegrating tablet and preparation method thereof |
-
2014
- 2014-08-30 CN CN201410435887.7A patent/CN105362245A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008128028A2 (en) * | 2007-04-11 | 2008-10-23 | Dr. Reddy's Laboratories Ltd. | Solifenacin compositions |
| WO2010097243A2 (en) * | 2009-02-27 | 2010-09-02 | Krka, D. D., Novo Mesto | Process for forming solid oral dosage forms of solifenacin and its pharmaceutically acceptable salts |
| CN102887894A (en) * | 2011-07-18 | 2013-01-23 | 天津市医药集团技术发展有限公司 | Crystal form of solifenacin succinate and preparation method thereof |
| CN103585123A (en) * | 2013-10-09 | 2014-02-19 | 北京万全德众医药生物技术有限公司 | Solifenacin succinate-containing orally disintegrating tablet and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 张志荣: "《药剂学》", 31 December 2007, 北京：高等教育出版社 * |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104523628A (en) * | 2014-12-24 | 2015-04-22 | 乐普药业股份有限公司 | Succinic acid solifenacin tablet capable of achieving direct powder compression and preparation method of succinic acid solifenacin tablet |
| CN104523628B (en) * | 2014-12-24 | 2017-08-25 | 乐普药业股份有限公司 | It is a kind of can direct powder compression butanedioic acid Solifenacin tablet and preparation method thereof |
| CN113456639A (en) * | 2020-03-31 | 2021-10-01 | 江苏康缘药业股份有限公司 | Anti-arrhythmia pharmaceutical composition and preparation method thereof |
| WO2021196982A1 (en) * | 2020-03-31 | 2021-10-07 | 江苏康缘药业股份有限公司 | Anti-arrhythmic pharmaceutical composition and preparation method therefor |
| CN113456639B (en) * | 2020-03-31 | 2024-01-26 | 江苏康缘药业股份有限公司 | Anti-arrhythmia pharmaceutical composition and preparation method thereof |
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Application publication date: 20160302 |
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