CN101125134B - Hydrochloric tamsulosin sustained-release capsule and its preparation method - Google Patents
Hydrochloric tamsulosin sustained-release capsule and its preparation method Download PDFInfo
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- CN101125134B CN101125134B CN2006100301201A CN200610030120A CN101125134B CN 101125134 B CN101125134 B CN 101125134B CN 2006100301201 A CN2006100301201 A CN 2006100301201A CN 200610030120 A CN200610030120 A CN 200610030120A CN 101125134 B CN101125134 B CN 101125134B
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Abstract
The present invention provides a tamsulosin hydrochloride sustained-release capsule. The tamsulosin hydrochloride sustained-release capsule of the present invention can avoid the sudden release of the drug tablets and the performance differences generated from the gastric emptying differences, display minor food effect or do not display food effect, and obtain the stable curve of the plasma drug concentration and longer action time simultaneously, so as to reduce the occurrence of cardiovascular side effects, greatly improve the safety, effectiveness and compliance of the medication for the patients. The tamsulosin hydrochloride sustained-release capsule of the present invention can ensure the sustained and regular release of the main ingredient tamsulosin hydrochloride after the oral administration, and the present invention is characterized by convenient administration, durable function, stable efficacy, fewer side effects and so on.
Description
Technical field
The present invention relates to a kind of slow releasing capsule and preparation method thereof, especially relate to a kind of tamsulosin hydrochloride sustained-release capsule and preparation method thereof.
Background technology
Benign prostate hyperplasia (BPH) is meant the optimum adenomatous hyperplasia of prostate-urethra peripheral region cell, is the common urology department disease of a kind of old man.Tamsulosin hydrochloride is by α 1 adrenergic aceptor antagonist of Japanese Yamanouchi Pharmaceutical Co., Ltd. development, is used for the treatment of benign prostate hyperplasia, in 1993 in Japanese Initial Public Offering.
Absorption when any healing potion is oral and bioavailability all can be subjected to the influence of many factors.These factors comprise the food that is present in the gastrointestinal tract, because the holdup time when the medicine holdup time under one's belt is usually than fasting when having food to exist is long.If owing to the existence of food in the gastrointestinal tract influence of bioavailability of medicament is surpassed certain a bit, just we can say that this medicine shows " food effect ".Food effect is to need special the attention, because when medicine shows bad food effect, the patient will produce harmful effect.In addition, other factors also may be relevant with bioavailability of medicament, comprises the factor of following these non-comprehensives:
(1) specific dosage form can influence bioavailability.For example, tablet or capsular gastric retention time are obviously than the length of suspensoid, and this difference can be taken food or be changed by fasting with the experimenter.
(2) gastric pH is changing with the quantity of food during feed and the fasting, thereby can influence responsive to pH and medicine that decompose.
(3) the liver metabolism ability that is absorbed medicine (first pass effect) changes with the feed type.For example, some vegetable (as the soup dish) can stimulate the first pass effect of some drugs, but does not stimulate the first pass effect of other medicines.On the other hand, grapefruit juice can suppress the first pass effect of some drugs.
(4) during digest food, discharge into the bile of small intestinal, can increase the dissolubility of insoluble medicine, thereby improve bioavailability by gallbladder.
Other factors also can influence the absorption and the bioavailability of certain drug, for example, relies on the intestinal permeability of dissolubility, the specific site of pH, to the unstability of intestinal enzyme, to the sensitivity of first pass metabolism and to unstability of colon bacteria or the like.
At US4772475, EP 194838, among the EP 533297, disclose and comprise granose tamsulosin hydrochloride slow releasing pharmaceutical dosage form, and described granule is made up of tamsulosin hydrochloride, microcrystalline Cellulose and adjuvant with controlled-release function.Described granule discharges tamsulosin hydrochloride gradually from particle matrix, but this medicament is subject to food effect when taking, and in bioavailability on an empty stomach and when taking under the feed condition bigger difference is arranged.
WO2004/056354A discloses a kind of controlled release tamsulosin hydrochloride medicament, but it is just in order to discharge at intestinal, do not relate to food effect, and it is mixed together the heart of forming preparation with medicine and adjuvant, can't make that medicine discharges reposefully, and owing to the excessive patient of being unfavorable for of excipient substance consumption takes, and can not show very little food effect or not show food effect.WO2004/066991A discloses a kind of intestinal slow-releasing granules that is used for oral cavity disintegration tablet, but special because of its prescription, can't be applied to the other drug preparation.
Up to now, in the prior art without any about tamsulosin hydrochloride being prepared into the record of the pharmaceutical dosage form that can overcome food effect, thereby and current also without any a kind of technology can be general be applied to the food effect that various medicines overcome medicine.
Summary of the invention
Technical problem to be solved by this invention is to overcome above-mentioned weak point, the novel form of research design tamsulosin hydrochloride.
The inventor finds in experiment: tamsulosin hydrochloride is a kind of medicine with food effect, its bioavailability and medicinal effectiveness have been influenced thus, thereby need to increase its dosage or increase medicining times, can produce bigger side effect inevitably, thereby influence drug safety and patient's adaptability.In order to overcome the food effect that it has, the inventor attempts to obtain new pharmaceutical preparation, and finish the present invention thus by adopting special formula and technology.
The invention provides a kind of tamsulosin hydrochloride sustained-release capsule.It comprises: celphere, medicated layer and extended release coatings film.Its medicated layer comprises tamsulosin hydrochloride, binding agent and pH regulator agent, and the extended release coatings film comprises slow-release material, plasticizer and antiplastering aid.Described tamsulosin hydrochloride sustained-release capsule consists of by weight percentage:
Celphere 20-80%
Tamsulosin hydrochloride 0.01-5%
Binding agent 0-10%
PH regulator agent 0-20%
Slow-release material 1-20%
Plasticizer 0-20%
Antiplastering aid 0-10%
Another object of the present invention has provided the preparation method of tamsulosin hydrochloride sustained-release capsule, comprises the steps: the preparation of pastille coating solution, the medicine carrying of celphere, the preparation of sustained release coating liquid, the sustained release coating that contains pill core and capsule fill.
Tamsulosin hydrochloride sustained-release capsule of the present invention, its celphere material are that particle diameter is the neutral spherical sugar pill of 300-1000 μ m.
Tamsulosin hydrochloride sustained-release capsule of the present invention, its medicated layer comprise tamsulosin hydrochloride, binding agent and pH regulator agent.Its shared percentage by weight of tamsulosin hydrochloride is 0.01-5% (w/w).
Binding agent in the medicated layer specifically can be selected from: one or more in polyvinyl pyrrolidone, Pulvis Talci, magnesium stearate, hydroxy propyl cellulose, sodium carboxymethyl cellulose, HYDROXY PROPYL METHYLCELLULOSE, hydroxyethyl-cellulose and the methylcellulose.Adhesive consumption can account for the 0-10% of ball core gross weight according to actual release behavior needs.
PH regulator agent in the medicated layer of the present invention specifically can be selected from: one or more in potassium dihydrogen phosphate, sodium dihydrogen phosphate, sodium hydrogen phosphate, sodium acetate, ammonium acetate, citric acid, fumaric acid and the sodium hydroxide.The consumption of pH regulator agent can be regulated according to actual release behavior needs, accounts for the 0-20% of ball core gross weight.
Extended release coatings film among the present invention can comprise slow-release material, plasticizer and antiplastering aid in order to the release of control active medicine from piller.
Plasticizer among the present invention in the extended release coatings film is used to improve the pliability of film, is selected from triethyl citrate, tributyl citrate, dibutyl sebacate, polyethylene glycol 6000, Macrogol 4000 and the diethyl phthalate one or more.
Antiplastering aid among the present invention in the extended release coatings film can be used for preventing the inter-adhesive of ball core in the coating process, and antiplastering aid can be selected from Pulvis Talci and magnesium stearate.
Among the present invention in the extended release coatings film slow-release material be high molecular insoluble polymer, can be selected among ethyl cellulose, cellulose acetate, Eudrugit (acrylic resin) RS, Eudrugit RL, Eudrugit RS 30D, Eudrugit RL 30D, Eudrugit NE 30D and the Surelease (Aquacoat) one or more.
The preparation method of slow releasing capsule of the present invention comprises the following steps:
(a) binding agent and pH regulator agent are dissolved in to be mixed with viscosity in the solvent be 10mpa.s---the solution of 40mpa.s;
(b) tamsulosin hydrochloride is dissolved in the solution that step (a) makes, must contains drug solns;
(c) celphere is added fluid bed, the drug solns that contains that makes with step (b) carries out coating, makes the pastille piller of tamsulosin hydrochloride after the drying;
(d) plasticizer and antiplastering aid are dissolved or dispersed in make coating solution in the slow-release material;
(e) the pastille piller with the tamsulosin hydrochloride of (c) adds fluid bed, and the coating solution that makes with step (d) carries out coating, and the coating process should continue to stir coating solution, makes the slow-release pill of tamsulosin hydrochloride after the drying;
(f) the tamsulosin hydrochloride slow-release pill that step (e) is made incapsulates, and makes the slow releasing capsule of tamsulosin hydrochloride.
Drug release determination method (2005 editions two appendix XD first methods of Chinese Pharmacopoeia), the drug release characteristics of the measurement device preparation of the present invention of employing dissolution method (2005 editions two appendix XC second methods of Chinese Pharmacopoeia).
The present invention has selected following 4 kinds of dissolution mediums to simulate intravital gastrointestinal tract environment, to estimate the situation that influences that this preparation medicine release characteristic is subjected to factors such as gastrointestinal peristalsis, pH value and food:
Medium A (SGF, simulated gastric fluid do not contain pepsin): pH 1.2
HCl is an amount of
NaCl 0.2％
An amount of 1000ml of water
Medium B (SIF, simulated intestinal fluid do not contain pancreatin): pH6.8
KH
2PO
4 6.8g
NaOH is an amount of
An amount of 1000ml of water
Medium C (FeSSIF, simulated intestinal fluid, feed state): pH5
Acetic acid 0.144M
NaOH is an amount of
Sodium taurocholate 15mM
Lecithin 4mM
KCl 0.19M
An amount of 1000ml of distilled water
Final medium pH=5
Osmotic pressure (osmolarity)=485-535mOsm; Buffer capacity=75 ± 2mEQ/L/pH medium D (FaSSIF, simulated intestinal fluid, state on an empty stomach): pH6.8
KH
2PO4 0.029M
NaOH is an amount of
Sodium taurocholate 5mM
Lecithin 1.5mM
KCl 0.22M
An amount of 1000ml of distilled water
Final medium pH=6.8
Osmotic pressure=280-310mOsm; Buffer capacity=10 ± 2mEQ/L/pH
Above-mentioned medium A is represented standard gastric juice condition; Medium B represents standard intestinal juice condition; Medium C represents the feed state, and medium D represents state on an empty stomach.
The above results shows that preparation of the present invention discharges medicine lentamente in the medium of four kinds of simulated in vivo environment selecting, and release characteristic is subjected to the influence of medium very little, constant speed discharges medicine equably in clinical use, for the patient provides more steady and persistent curative effect, reduce the generation of untoward reaction.
The present invention adopts on the piller surface and coats the polymer sustained release coating film with semi-permeable performance, accurately controls the lasting release of active medicine tamsulosin hydrochloride.Slow-release pill is with after external test solution or human body fluid contact, moisture content can enter slow-release pill inside by the polymer sustained release coating film with semi-permeable performance, medicament active composition is dissolved, at the inner medicament active composition solution that forms supersaturation concentration of slow-release pill, the medicament active composition of supersaturation concentration is by the polymer sustained release coating film of semi-permeable performance, and the equivalent that forms in the unit interval discharges.The polymer that applied in any combination of the present invention is different is accurately controlled the release of medicine.
Tamsulosin hydrochloride sustained-release capsule of the present invention has following advantage simultaneously: the performance difference that (1) can overcome gastrointestinal tract difference transfer time and irregular gastric emptying difference is produced; (2) can be distributed in the whole gastrointestinal tract, specific surface area is big, can promote fully and evenly absorbs, and bioavailability improves, and the plasma peaks fluctuation is little, can reduce blood concentration fluctuation and the side effect that produces; (3) drug dose is dispersed in a large amount of pillers, and the failure of part coating can not cause as the serious toxicity that tablet medicine is prominent due to releasing, even lethal action, and this depends on used pharmaceutical compound; (4) medicine is dispersed in each piller, has reduced gastrointestinal tract mucous stimulation.
Thus, tamsulosin hydrochloride is made once-a-day slow releasing capsule, dosage is the 0.1mg/ grain---the 0.8mg/ grain, can avoid the prominent performance difference that is produced with gastric emptying difference of releasing of medicinal tablet, and show very little food effect or do not show food effect.Can reduce blood concentration fluctuation, keep stable curative effect, and reduce side effect (orthostatic hypotension) as far as possible, and improving safety, effectiveness and compliance that the patient takes medicine, its bioavailability and medicinal effectiveness etc. all are better than or are equal to commercially available tamsulosin hydrochloride sustained-release capsule now.
Description of drawings:
Fig. 1 is example 1 a tamsulosin hydrochloride sustained-release capsule release curve;
Fig. 2 is example 2 tamsulosin hydrochloride sustained-release capsule release curves;
Fig. 3 is example 3 tamsulosin hydrochloride sustained-release capsule release curves;
Fig. 4 is example 4 tamsulosin hydrochloride sustained-release capsule release curves;
Fig. 5 is example 5 tamsulosin hydrochloride sustained-release capsule release curves.
Among the above-mentioned figure:
_ medium A-■-medium B-▲-medium C-*-medium D.
The specific embodiment
The present invention is further elaborated below in conjunction with specific embodiment, but do not limit the present invention.
Celphere 300g (commercially available)
Tamsulosin hydrochloride 0.6g
Hypromellose (E5) 10g
Potassium dihydrogen phosphate 50g
Eudrugit?NE?30D 240g
Triethyl citrate 5g
Pulvis Talci 25g
Preparation method:
(a), be dissolved in the 500ml deionized water with potassium dihydrogen phosphate 50g; Under the mechanical agitation condition, add hypromellose (E5) 10g, make to be dissolved to transparent settled solution;
(b), be dissolved in the solution that step (a) makes with tamsulosin hydrochloride 0.3g;
(c) celphere is added fluid bed, the drug solns that contains that makes with step (b) carries out fluidized bed coating, makes the pastille piller of tamsulosin hydrochloride after the drying;
(d) triethyl citrate and the Pulvis Talci with recipe quantity is scattered in the 100ml water, and the high shear dispersing emulsification machine was sheared 5 minutes, adds the Eudrugit NE 30D of recipe quantity, the mechanical agitation mixing;
(e) the pastille piller with tamsulosin hydrochloride adds fluid bed, and the coating solution that makes with step (d) carries out coating, and the coating process should continue to stir coating solution, makes the slow-release pill of tamsulosin hydrochloride after the drying;
(f) the tamsulosin hydrochloride slow-release pill that step (e) is made incapsulates, and makes the slow-release pill of tamsulosin hydrochloride.
The mensuration of release:
Get this product, according to drug release determination method (2005 editions two appendix XD first methods of Chinese Pharmacopoeia), adopt the device of dissolution method (2005 editions two appendix XC first methods of Chinese Pharmacopoeia), capsule is put into the commentaries on classics basket, use following dissolution medium respectively: medium A (SGF, simulated gastric fluid does not contain pepsin);
Medium B (SIF, simulated intestinal fluid do not contain pancreatin);
Medium C (FeSSIF, simulated intestinal fluid, feed state);
Each 500ml of medium D (FaSSIF, simulated intestinal fluid, state on an empty stomach), rotating speed is that per minute 50 changes, operation in accordance with the law, 1,2,3,4, got solution 10ml respectively in 5 hours, and in process container, replenish above-mentioned solvent 10ml immediately, filter with 0.45 μ m microporous filter membrane, as need testing solution.Other 2 hours the acid hydrochloride salt tamsulosin hydrochloride reference substance of 105 ℃ of dryings of learning from else's experience is an amount of, the accurate title, decide, add dissolving of water-acetonitrile (65: 35) solution and dilution and make the solution that contains 0.5mg among every 1ml approximately, shake up, measure an amount of, thin up is made the solution that contains 0.4 μ g among every 1ml approximately, in contrast product solution.Using HPLC Agilent 1100 systems, measure the medicine that discharges by the HPLC method, use octadecylsilane chemically bonded silica to be filler, adopt the mode of isocratic elution, is eluant with acetonitrile-perchloric acid solution (35: 65), detects wavelength 225nm.Get each 80 μ l of above-mentioned solution respectively, inject chromatograph of liquid, operation goes out every burst size at different time by external standard method with calculated by peak area in accordance with the law.
The result: the release curve is seen accompanying drawing 1
Celphere 300g (commercially available)
Tamsulosin hydrochloride 0.6g
Potassium dihydrogen phosphate 50g
Hypromellose (E5) 15g
Surelease 400g
PEG4000 15g
Pulvis Talci 25g
Preparation method:
(a), be dissolved in the 500ml deionized water with potassium dihydrogen phosphate 50g; Under the mechanical agitation condition, add hypromellose (E5) 15g, make to be dissolved to transparent settled solution;
(b), be dissolved in the solution that step (a) makes with tamsulosin hydrochloride 0.3g;
(c) celphere is added fluid bed, the drug solns that contains that makes with step (b) carries out fluidized bed coating, makes the pastille piller of tamsulosin hydrochloride after the drying;
(d) 15g PEG4000 is dissolved in the 250ml deionized water, under the mechanical agitation condition, adds the 25g Pulvis Talci, add the Surelease aqueous dispersion solution of recipe quantity again, the mechanical agitation mixing;
(e) the pastille piller with tamsulosin hydrochloride adds fluid bed, and the coating solution that makes with step (d) carries out coating, and the coating process should continue to stir coating solution, makes the slow-release pill of tamsulosin hydrochloride after the drying;
(f) the tamsulosin hydrochloride slow-release pill that step (e) is made incapsulates, and makes the slow-release pill of tamsulosin hydrochloride.
The mensuration of release: with embodiment 1
The result: the release curve is seen accompanying drawing 2
Celphere 300g (commercially available)
Tamsulosin hydrochloride 0.6g
PVP?K30 20g
Potassium dihydrogen phosphate 50g
Eudrugit?RL100 30g
Eudrugit?RS100 70g
Dibutyl sebacate 10g
Pulvis Talci 25g
Preparation method:
(a), be dissolved in the 500ml deionized water with potassium dihydrogen phosphate 50g; Under the mechanical agitation condition, add PVPK30 20g, make to be dissolved to transparent settled solution;
(b), be dissolved in the solution that step (a) makes with tamsulosin hydrochloride 0.3g;
(c) celphere is added fluid bed, the drug solns that contains that makes with step (b) carries out fluidized bed coating, makes the pastille piller of tamsulosin hydrochloride after the drying;
(d) with the Eudrugit RL100 and the Eudrugit RS100 of recipe quantity, add under the mechanical agitation condition in 95% the alcoholic solution, dissolve fully to Eudrugit; 10g dibutyl sebacate and 25g Pulvis Talci are joined in this mixed solution the mechanical agitation mixing under the mechanical agitation condition;
(e) the pastille piller with tamsulosin hydrochloride adds fluid bed, and the coating solution that makes with step (d) carries out coating, and the coating process should continue to stir coating solution, makes the slow-release pill of tamsulosin hydrochloride after the drying;
(f) the tamsulosin hydrochloride slow-release pill that step (e) is made incapsulates, and makes the slow-release pill of tamsulosin hydrochloride.
The mensuration of release; With embodiment 1
The result: the release curve is seen accompanying drawing 3
Celphere 300g (commercially available)
Tamsulosin hydrochloride 0.6g
Hypromellose (E5) 10g
Sodium acetate 10g
Eudrugit?RL100 80g
Eudrugit?RS100 20g
Triethyl citrate 10g
Pulvis Talci 25g
Preparation method:
(a) with the sodium acetate of recipe quantity, be dissolved in the deionized water of 500ml, with the hypromellose (E5) of 10g, add wherein under the mechanical agitation condition, make to be dissolved to transparent settled solution;
(b), be dissolved in the solution that step (a) makes with tamsulosin hydrochloride 0.3g;
(c) celphere is added fluid bed, the drug solns that contains that makes with step (b) carries out fluidized bed coating, makes the pastille piller of tamsulosin hydrochloride after the drying;
(d) with the Eudrugit RL100 and the Eudrugit RS100 of recipe quantity, add under the mechanical agitation condition in 95% the alcoholic solution, dissolve fully to Eudrugit; 10g triethyl citrate and 25g Pulvis Talci are joined in this mixed solution the mechanical agitation mixing under the mechanical agitation condition;
(e) the pastille piller with tamsulosin hydrochloride adds fluid bed, and the coating solution that makes with step (d) carries out coating, and the coating process should continue to stir coating solution, makes the slow-release pill of tamsulosin hydrochloride after the drying;
(f) the tamsulosin hydrochloride slow-release pill that step (e) is made incapsulates, and makes the slow-release pill of tamsulosin hydrochloride.
The mensuration of release: with embodiment 1
The result: the release curve is seen accompanying drawing 4
Celphere 300g (commercially available)
Tamsulosin hydrochloride 0.6g
Hypromellose (E5) 20g
Sodium acetate 10g
Eudrugit?NE?30D 240g
Triethyl citrate 10g
Pulvis Talci 25g
Preparation method:
(a) with the sodium acetate of recipe quantity, be dissolved in the deionized water of 500ml, with the hypromellose (E5) of 20g, add wherein under the mechanical agitation condition, make to be dissolved to transparent settled solution;
(b), be dissolved in the solution that step (a) makes with tamsulosin hydrochloride 0.3g;
(c) celphere is added fluid bed, the drug solns that contains that makes with step (b) carries out fluidized bed coating, makes the pastille piller of tamsulosin hydrochloride after the drying;
(d) triethyl citrate and the Pulvis Talci with recipe quantity is scattered in the 100ml water, and the high shear dispersing emulsification machine was sheared 5 minutes, adds the Eudrugit NE 30D of recipe quantity, the mechanical agitation mixing;
(e) the pastille piller with tamsulosin hydrochloride adds fluid bed, and the coating solution that makes with step (d) carries out coating, and the coating process should continue to stir coating solution, makes the slow-release pill of tamsulosin hydrochloride after the drying;
(f) the tamsulosin hydrochloride slow-release pill that step (e) is made incapsulates, and makes the slow-release pill of tamsulosin hydrochloride.
The mensuration of release: with embodiment 1
The result: the release curve is seen accompanying drawing 5
Claims (6)
1. tamsulosin hydrochloride sustained-release capsule, it is characterized in that it comprises: celphere, medicated layer and extended release coatings film, its medicated layer comprise tamsulosin hydrochloride, binding agent and pH regulator agent, and the extended release coatings film comprises slow-release material, plasticizer and antiplastering aid; Its preparation method comprises the steps: the preparation of pastille coating solution, the medicine carrying of celphere, the preparation of sustained release coating liquid, the sustained release coating that contains pill core and capsule fill.
2. a kind of tamsulosin hydrochloride sustained-release capsule according to claim 1, it is characterized in that described binding agent is one or more in polyvinyl pyrrolidone, Pulvis Talci, magnesium stearate, hydroxypropyl cellulose, sodium carboxymethyl cellulose, hydroxypropyl emthylcellulose, hydroxyethyl-cellulose or the methylcellulose.
3. a kind of tamsulosin hydrochloride sustained-release capsule according to claim 1, it is characterized in that described pH regulator agent is one or more in potassium dihydrogen phosphate, sodium dihydrogen phosphate, sodium hydrogen phosphate, sodium acetate, ammonium acetate, citric acid, fumaric acid or the sodium hydroxide.
4. a kind of tamsulosin hydrochloride sustained-release capsule according to claim 1, it is characterized in that, described slow-release material is high molecular insoluble polymer, is selected among ethyl cellulose, cellulose acetate, Eudrugit RS, Eudrugit RL, Eudrugit RS 30D, Eudrugit RL 30D or the Eudrugit NE 30D one or more.
5. the described a kind of tamsulosin hydrochloride sustained-release capsule of claim 1, it is characterized in that described plasticizer is selected from: one or more in triethyl citrate, tributyl citrate, dibutyl sebacate, polyethylene glycol 6000, Macrogol 4000, the diethyl phthalate.
6. the preparation method of a tamsulosin hydrochloride sustained-release capsule as claimed in claim 1 is characterized in that, this method comprises the following steps:
(a) binding agent and pH regulator agent are dissolved in are mixed with the solution that viscosity is 10mpa.s-40mpa.s in the solvent;
(b) tamsulosin hydrochloride is dissolved in the solution that step (a) makes, must contains drug solns;
(c) celphere is added fluid bed, the drug solns that contains that makes with step (b) carries out coating, makes the pastille piller of tamsulosin hydrochloride after the drying;
(d) plasticizer and antiplastering aid are dissolved or dispersed in make coating solution in the slow-release material;
(e) the pastille piller with the tamsulosin hydrochloride of (c) adds fluid bed, and the coating solution that makes with step (d) carries out coating, and the coating process should continue to stir coating solution, makes the slow-release pill of tamsulosin hydrochloride after the drying;
(f) the tamsulosin hydrochloride slow-release pill that step (e) is made incapsulates, and makes the slow releasing capsule of tamsulosin hydrochloride.
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| CN101695478B (en) * | 2009-10-23 | 2012-01-18 | 江苏大学 | Tamsulosin hydrochloride sustained-release pellets and preparation method thereof |
| CN102106841B (en) * | 2009-12-24 | 2013-01-09 | 杭州康恩贝制药有限公司 | Tamsulosin hydrochloride preparation and preparation method thereof |
| CN104873478A (en) * | 2015-06-06 | 2015-09-02 | 鲁南贝特制药有限公司 | Tamsulosin hydrochloride sustained-release capsule and preparation method thereof |
| CN105412020A (en) * | 2015-12-07 | 2016-03-23 | 黑龙江省智诚医药科技有限公司 | Tamsulosin hydrochloride sustained-release pellet and preparation method thereof |
| JP2019524683A (en) * | 2016-07-15 | 2019-09-05 | ハンミ ファーマシューティカルズ カンパニー リミテッド | Oral pharmaceutical formulation comprising tamsulosin hydrochloride-containing sustained release pellets with improved content uniformity |
| CN110455932B (en) * | 2018-05-08 | 2022-04-22 | 人福普克药业（武汉）有限公司 | Method for determining enzyme dissolution of bexarotene soft capsules |
| CN110711184B (en) * | 2019-11-12 | 2022-01-04 | 中国药科大学 | Tamsulosin hydrochloride sustained-release particles and preparation method thereof |
| CN111643484A (en) * | 2020-07-04 | 2020-09-11 | 上海安必生制药技术有限公司 | Tamsulosin hydrochloride sustained release preparation and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1176653C (en) * | 2002-08-26 | 2004-11-24 | 鲁南制药股份有限公司 | Slow-releasing Anixidan capsule |
| CN1194694C (en) * | 2002-08-26 | 2005-03-30 | 鲁南制药股份有限公司 | Slow-releasing maclobemide capsule |
| CN1205933C (en) * | 2002-08-26 | 2005-06-15 | 鲁南制药股份有限公司 | Slow-releasing acipimox capsule |
-
2006
- 2006-08-16 CN CN2006100301201A patent/CN101125134B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1176653C (en) * | 2002-08-26 | 2004-11-24 | 鲁南制药股份有限公司 | Slow-releasing Anixidan capsule |
| CN1194694C (en) * | 2002-08-26 | 2005-03-30 | 鲁南制药股份有限公司 | Slow-releasing maclobemide capsule |
| CN1205933C (en) * | 2002-08-26 | 2005-06-15 | 鲁南制药股份有限公司 | Slow-releasing acipimox capsule |
Non-Patent Citations (1)
| Title |
|---|
| JP特开2005-200399A 2005.07.28 |
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| CN101125134A (en) | 2008-02-20 |
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Assignee: Pharmaceutical Co., Ltd., Changzhou Pharmaceutical Factory No.4 Assignor: Changzhou City No.4 Pharmaceutical Factory Co., Ltd. Contract record no.: 2011320001105 Denomination of invention: Tamsulosin hydrochloride sustained-release capsule and preparation method thereof Granted publication date: 20100915 License type: Exclusive License Open date: 20080220 Record date: 20110825 |