CN102106841B - Tamsulosin hydrochloride preparation and preparation method thereof - Google Patents
Tamsulosin hydrochloride preparation and preparation method thereof Download PDFInfo
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- CN102106841B CN102106841B CN 200910155645 CN200910155645A CN102106841B CN 102106841 B CN102106841 B CN 102106841B CN 200910155645 CN200910155645 CN 200910155645 CN 200910155645 A CN200910155645 A CN 200910155645A CN 102106841 B CN102106841 B CN 102106841B
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Abstract
The invention relates to a tamsulosin hydrochloride preparation and a preparation method thereof. The preparation comprises the following components in percentage by weight: 0.1 to 2 percent of tamsulosin hydrochloride, 0.5 to 5 percent of lecithin, 55 to 80 percent of filler, 10 to 30 percent of sustained-release matrix agent, and 1 to 10 percent of adhesive matrix agent. The tamsulosin hydrochloride sustained-release capsule preparation prepared by the method can be absorbed in a body more quickly, and acts more quickly, can be used for overcoming the influence of diet on tamsulosin hydrochloride absorption, is more convenient to take, and is suitable for more people.
Description
(1) technical field: the present invention relates to a kind of oral chemicals slow releasing preparation, be specifically related to a kind of tamsulosin hydrochloride sustained-release capsule and preparation method thereof.
(2) background technology: tamsulosin hydrochloride chemical name: (R) (-) 5-{2-[[2-(2-ethoxyphenyl) ether base] amido]-the 2-methyl }-ethyl-2-methoxybenzenesulphoismide hydrochlorate, molecular formula: C
20H
28N
2O
5SHCl.
Tamsulosin hydrochloride is novel a1 receptor blocking agent, optionally blocks the smooth muscle a1 receptor of neck of bladder, prostate body of gland and tunicle, reduces smooth muscle tension force, reduces the lower urinary tract resistance, thereby improves the dysuria that causes because of prostate hyperplasia.Zoopery proves that tamsulosin is optionally blocked the epinephrine a1 receptor of rat, rabbit.Its effect is than the strong 12-22 of prazosin times, than the strong 45-140 of phentolamine doubly.To people and animal urethra, bladder and the effect of prostatic a1 receptor blocking, than the strong 2.2-98 of prazosin doubly, than the strong 40-320 of phentolamine doubly.Anesthetized dog studies show that tamsulosin hydrochloride can obviously reduce the pressure of prostatic, but anesthetized rat rhythmicity bladder contraction and intravesical pressure are had no significant effect.
Tamsulosin hydrochloride can be used for treating the symptom of unusually urinating due to the prostatic hyperplasia, as frequent micturition, nocturia increase, dysuria etc.Because this product is to reach therapeutic purposes by improving urethra, neck of bladder and prostatic smooth muscle function, be not to dwindle the hypertrophy body of gland, so be applicable to light, moderate patient and do not cause serious dysuria person.
By the exploitation of Japanese Yamanouchi drugmaker, commodity are called Harnal to the tamsulosin hydrochloride sustained-release capsule oral formulations the earliest, and extensive use at home and abroad entered Chinese market in 1996.Domestic this peroral dosage form specification is the 0.2mg/ grain, is used for the treatment of the symptom of BPH, oral meal, adult once a day, one time one.When being grown up once oral 0.2mg, blood drug level reaches the peak after 6.8 hours, and the half-life is 10.0 hours.
Because it is slower that the tamsulosin hydrochloride slow releasing preparation absorbs, peak reaching time of blood concentration is longer, and the simultaneously oral impact that also is subjected to easily diet, particularly high fat diet of tamsulosin can affect the attraction of tamsulosin.Be to accelerate the attraction of tamsulosin, all developed at present the oral cavity disintegration preparation of tamsulosin hydrochloride both at home and abroad, but oral cavity disintegration preparation needs oral 3 times on the 1st, and the treatment prostatic hyperplasia needs long-term prescription, makes troubles so also for patient's medication.
(3) summary of the invention: task of the present invention is to overcome existing tamsulosin hydrochloride slow releasing agent defective, a kind of new tamsulosin hydrochloride sustained-release capsule preparation is provided, in vivo quicker absorption has also overcome the impact that diet absorbs tamsulosin hydrochloride simultaneously.
The technical solution used in the present invention is: add lecithin in existing tamsulosin hydrochloride slow releasing agent, the component of described preparation and percentage by weight are:
Tamsulosin hydrochloride 0.08-2%
Lecithin 0.5-5%
Filler 55-80%
Sustained-release matrix agent 10-30%
Bind skeleton agent 1-10%
Said filler is dextrin, starch, sucrose;
Said sustained-release matrix agent is high molecular insoluble polymer, is selected from one or more of hypromellose, polyacrylic resin, cellulose acetate;
One or both in hypromellose, the Polyethylene Glycol are selected in the agent of said bonding skeleton.
Hypromellose plays slow release and adhesive effect simultaneously in the preparation of the present invention.
The tamsulosin hydrochloride sustained-release capsule preparation that the present invention relates to, its preparation method comprises the following steps:
(1) prepare blank piller: filler starch, dextrin, sucrose are adopted the standby blank piller of centrifugal coating pelletizing legal system, and size is between the 18-26 order;
(2) slow-release pill of the hydrochloric tamsulosin medicine of preparation:
A. active medicine tamsulosin hydrochloride and lecithin are dissolved in 50% the alcoholic solution, the rear adding sustained-release matrix agent that fully is mixed, mixing obtains medicament slow release skeleton solution;
B. get the agent of bonding skeleton and all dissolve with suitable quantity of water, make and bind the skeleton agent solution;
C. the blank piller with step (1) preparation places fluid bed, spray one deck medicament slow release skeleton solution, and logical hot-air dry, spray one deck binds the skeleton agent solution, logical hot-air dry; Repeat aforesaid operations, until medicine-feeding fully;
(3) preparation slow releasing capsule: the pastille slow-release piller of step (2) preparation is incapsulated, namely make the tamsulosin hydrochloride sustained-release capsule preparation.
The present invention adds lecithin in existing tamsulosin hydrochloride slow releasing agent, lecithin is with after tamsulosin hydrochloride mixes, can with the tamsulosin hydrochloride enclose, form clathrate, and because lecithin has water solublity and oil-soluble concurrently, can accelerate to have discharged the absorption of tamsulosin hydrochloride, simultaneously it has fat-solublely also reduced the impact that diet attracts tamsulosin hydrochloride, so that tamsulosin hydrochloride is taken absorption after diet substantially unaffected.
Show according to drug release determination method (two appendix XD of Chinese Pharmacopoeia version in 2005 first method) and human bioavailability test, the tamsulosin hydrochloride sustained-release capsule preparation of the present invention's preparation, early stage, rate of release was fast, quick acting more, overcome the impact that diet absorbs tamsulosin hydrochloride, and taking more conveniently, suitable crowd is more extensive.
(4) specific embodiment: the following examples are used for further specifying and describe the present invention, but and do not mean that the present invention only limits to this.
Embodiment 1: the preparation of tamsulosin hydrochloride sustained-release capsule preparation
Prescription:
Tamsulosin hydrochloride 0.2g
Lecithin 2g
Sucrose 62.5g
Starch 43.75g
Dextrin 18.75g
Hypromellose 60g
Polyacrylic resin 20g
Polyethylene glycol 6000 0.7g
Preparation method:
The preparation of I, blank piller
Get recipe quantity sucrose, starch, dextrin, mix, enter in the centrifugal coating granulator, with centrifugal coating pelletizing method, prior art and technological parameter prepare blank piller, and size is between the 18-26 order;
The preparation of II, slow-release pill
A. recipe quantity tamsulosin hydrochloride and lecithin are dissolved in 50% the alcoholic solution, the rear adding recipe quantity polyacrylic resin that fully is mixed, an amount of hypromellose get medicament slow release skeleton solution, and be for subsequent use.
B. recipe quantity polyethylene glycol 6000 and remaining hypromellose is soluble in water, make and bind the skeleton agent solution, for subsequent use.
C. the blank piller that then step I is prepared places fluid bed, spray one deck medicament slow release skeleton solution, and logical hot-air dry, and then spray one deck bonding skeleton agent solution lead to hot-air dry again; Repeat aforesaid operations, until medicine-feeding fully.
III, slow releasing capsule preparation
The slow-release pill of Step II preparation is incapsulated, use the micropill automatic capsule filler, namely get tamsulosin hydrochloride sustained-release capsule, every hydrochloric tamsulosin 0.2mg of slow releasing capsule.
Embodiment 2: the preparation of tamsulosin hydrochloride sustained-release capsule preparation
Prescription:
Tamsulosin hydrochloride 0.4g
Lecithin 5g
Sucrose 72.5g
Starch 51.75g
Dextrin 21.75g
Hypromellose 50g
Cellulose acetate 24g
Polyacrylic resin 24g
Polyethylene glycol 6000 1g
Preparation method:
The preparation of I, blank piller
Preparation method by embodiment 1 empty piller is prepared
The preparation of II, slow-release pill
A. recipe quantity tamsulosin hydrochloride and lecithin are dissolved in 50% an amount of alcoholic solution, the cellulose acetate of the rear adding recipe quantity that fully is mixed, polyacrylic resin and an amount of hypromellose get medicament slow release skeleton solution, and be for subsequent use.
B. recipe quantity polyethylene glycol 6000, remaining hypromellose are dissolved in the suitable quantity of water, make and bind the skeleton agent solution, for subsequent use.
C. the blank piller that then step I is prepared places fluid bed, spray one deck medicament slow release skeleton solution, and then logical hot-air dry sprays one deck and binds the skeleton agent solution, more logical hot-air dry; Repeat aforesaid operations, until medicine-feeding fully.
III, slow releasing capsule preparation
The slow-release pill of Step II preparation is incapsulated, use the micropill automatic capsule filler, namely get tamsulosin hydrochloride sustained-release capsule, every hydrochloric tamsulosin 0.4mg of slow releasing capsule.
Embodiment 3: the preparation of tamsulosin hydrochloride sustained-release capsule preparation
Prescription:
Tamsulosin hydrochloride 1g
Lecithin 4g
Sucrose 80g
Starch 48g
Dextrin 25g
Hypromellose 70g
Polyacrylic resin 25g
Polyethylene glycol 6000 2g
Preparation method: be prepared into tamsulosin hydrochloride sustained-release capsule by embodiment 1 method, every hydrochloric tamsulosin 1mg of slow releasing capsule.
Embodiment 4
Get the tamsulosin hydrochloride sustained-release capsule of embodiment 1 preparation, according to drug release determination method (two appendix XD of Chinese Pharmacopoeia version in 2005 first method), with dissolution method the 3rd subtraction unit, with hydrochloride buffer 250ml as solvent, rotating speed is that per minute 100 turns, in accordance with the law operation.Calculate every in the release of different time.And the tamsulosin hydrochloride sustained-release capsule Harnal of producing with Japanese Yamanouchi Pharmaceutical Co., Ltd
Lot number KO25NO1 (lot number of the repackaged products 010507A) compares test, the results are shown in Table 1.
Table 1 tamsulosin hydrochloride sustained-release capsule and Harnal capsule release profiles are relatively
By as seen from Table 1, embodiment 1 prepared tamsulosin hydrochloride sustained-release capsule is compared with the Harnal capsule, discharges obviously faster than Harnal capsule (KO25NO1) before 5 hours, and is basically identical after 8 hours.
Embodiment 5
Embodiment 1 prepared tamsulosin hydrochloride sustained-release capsule is carried out the uniformity test of release, and result of the test sees Table 2.
The uniformity test of table 2 tamsulosin hydrochloride sustained-release capsule
Illustrate by the prepared acid hydrochloride salt tamsulosin sustained release capsule release of the inventive method even.
Embodiment 6
The human bioavailability test of the tamsulosin hydrochloride sustained-release capsule of embodiment 1 preparation and Harnal capsule (lot number KO25NO1).
Three experimenters in morning 7:00 take tamsulosin hydrochloride sustained-release capsule and the Harnal capsule (lot number KO25NO1) of embodiment 1 preparation, wherein two experimenters distinguish tamsulosin hydrochloride sustained-release capsule and the Harnal capsules (lot number KO25NO1) that (medicine) being taken before meal prepares with embodiment 1, another experimenter takes the tamsulosin hydrochloride sustained-release capsule of embodiment 1 preparation after the meal, after taking medicine 1,2,3,4,6,8,10h respectively takes a blood sample 6mL in the heparin test tube, measure the wherein concentration of tamsulosin after the separated plasma, result such as following table 3:
Table 3 tamsulosin hydrochloride sustained-release capsule of the present invention and Harnal capsule (lot number KO25NO1) human bioavailability relatively
From human bioavailability, the tamsulosin hydrochloride sustained-release capsule of the present invention's preparation absorbs obvious tamsulosin hydrochloride sustained-release capsule faster than routine, and substantially is not subjected to food effect.Conclusion: the tamsulosin hydrochloride sustained-release capsule of the present invention preparation is quick acting more, and takes more conveniently, and suitable crowd is more extensive.
Claims (2)
1. a tamsulosin hydrochloride preparation is characterized in that described preparation contains tamsulosin hydrochloride and lecithin, and the component of described preparation and percentage by weight are:
Tamsulosin hydrochloride 0.08-2%
Lecithin 0.5-5%
Filler 55-80%
Sustained-release matrix agent 10-30%
Bind skeleton agent 1-10%
Said filler is the mixture of dextrin, starch and sucrose;
Said sustained-release matrix agent is high molecular insoluble polymer, is selected from one or more of hypromellose, polyacrylic resin, cellulose acetate;
One or both in hypromellose, the Polyethylene Glycol are selected in the agent of said bonding skeleton.
2. the preparation method of tamsulosin hydrochloride preparation according to claim 1 is characterized in that, the following step of preparation tamsulosin hydrochloride preparation process:
(1) prepares blank piller: filler starch, dextrin, sucrose are adopted the standby blank piller of centrifugal coating pelletizing legal system;
(2) preparation pastille slow-release piller:
A. active medicine tamsulosin hydrochloride and lecithin are dissolved in 50% the alcoholic solution, the rear adding sustained-release matrix agent that fully is mixed obtains medicament slow release skeleton solution;
B. get the agent of bonding skeleton and be dissolved in the suitable quantity of water, make and bind the skeleton agent solution;
C. the blank piller with step (1) preparation places fluid bed, and spray one deck medicament slow release skeleton solution leads to hot-air a few minutes drying, and spray one deck binds the skeleton agent solution, logical hot-air a few minutes drying; Repeat aforesaid operations, until medicine-feeding fully;
(3) preparation slow releasing capsule: the pastille slow-release piller of step (2) preparation is incapsulated, namely make the tamsulosin hydrochloride sustained-release capsule preparation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN 200910155645 CN102106841B (en) | 2009-12-24 | 2009-12-24 | Tamsulosin hydrochloride preparation and preparation method thereof |
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| CN 200910155645 CN102106841B (en) | 2009-12-24 | 2009-12-24 | Tamsulosin hydrochloride preparation and preparation method thereof |
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| CN102106841A CN102106841A (en) | 2011-06-29 |
| CN102106841B true CN102106841B (en) | 2013-01-09 |
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| CN110755396B (en) * | 2019-12-06 | 2022-04-08 | 北京悦康科创医药科技股份有限公司 | Ibuprofen sustained-release pellet and preparation method thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1358088A (en) * | 1999-06-28 | 2002-07-10 | 圣诺菲-合成实验室公司 | Pharmaceuticla dosage forms for controlled telease producing at least timed pulse |
| CN1691965A (en) * | 2003-03-06 | 2005-11-02 | 山之内制药株式会社 | Pharmaceutical composition for controlled release and manufacturing method thereof |
| CN101125134A (en) * | 2006-08-16 | 2008-02-20 | 常州市第四制药厂有限公司 | Hydrochloric tamsulosin sustained-release capsule and its preparation method |
| CN101204387A (en) * | 2006-12-19 | 2008-06-25 | 北京德众万全药物技术开发有限公司 | Novel tamsulosin hydrochloride sustained release capsules |
-
2009
- 2009-12-24 CN CN 200910155645 patent/CN102106841B/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1358088A (en) * | 1999-06-28 | 2002-07-10 | 圣诺菲-合成实验室公司 | Pharmaceuticla dosage forms for controlled telease producing at least timed pulse |
| CN1691965A (en) * | 2003-03-06 | 2005-11-02 | 山之内制药株式会社 | Pharmaceutical composition for controlled release and manufacturing method thereof |
| CN101125134A (en) * | 2006-08-16 | 2008-02-20 | 常州市第四制药厂有限公司 | Hydrochloric tamsulosin sustained-release capsule and its preparation method |
| CN101204387A (en) * | 2006-12-19 | 2008-06-25 | 北京德众万全药物技术开发有限公司 | Novel tamsulosin hydrochloride sustained release capsules |
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Inventor after: Xu Chunling Inventor after: Wang Ruwei Inventor after: Xu Xiuhui Inventor after: Lu Zhenyu Inventor after: Ye Jianfeng Inventor after: Xia Yajun Inventor before: Wang Ruwei Inventor before: Xu Chunling Inventor before: Xia Yajun Inventor before: Ye Jianfeng Inventor before: Lu Zhenyu Inventor before: Xu Xiuhui |
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Free format text: CORRECT: INVENTOR; FROM: WANG RUWEI XU CHUNLING XIA YAJUN YE JIANFENG LU ZHENYU XU XIUHUI TO: XU CHUNLING WANG RUWEI XU XIUHUI LU ZHENYU YE JIANFENG XIA YAJUN |
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Effective date of registration: 20121106 Address after: Hangzhou City, Zhejiang province Binjiang District 310052 River Street No. 568 bin Kang Road Applicant after: Hangzhou Conba Pharmaceutical Co., Ltd. Address before: Hangzhou City, Zhejiang province Binjiang District 310052 River Street No. 568 bin Kang Road Applicant before: Hangzhou Conba Pharmaceutical Co., Ltd. Applicant before: Zhejiang Modern Chinese Medicine and Natural Medicine Academy Co., Ltd. |
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