CN103230379A - Orally disintegrating sustained-release preparation containing tamsulosin hydrochloride and preparation method thereof - Google Patents
Orally disintegrating sustained-release preparation containing tamsulosin hydrochloride and preparation method thereof Download PDFInfo
- Publication number
- CN103230379A CN103230379A CN2013101113110A CN201310111311A CN103230379A CN 103230379 A CN103230379 A CN 103230379A CN 2013101113110 A CN2013101113110 A CN 2013101113110A CN 201310111311 A CN201310111311 A CN 201310111311A CN 103230379 A CN103230379 A CN 103230379A
- Authority
- CN
- China
- Prior art keywords
- coating
- medicine carrying
- preparation
- tamsulosin hydrochloride
- medicine
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Images
Landscapes
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Belonging to the field of medicines, the invention particularly relates to a preparation method of a sustained release tablet containing tamsulosin hydrochloride. The dosage form is an oral preparation that is prepared by taking tamsulosin hydrochloride as an active component and using acceptable auxiliary materials in an orally disintegrating tablet. The preparation not only has the characteristics of rapid disintegrating speed, rapid onset, and high patient compliance of orally disintegrating tablets, but also has the advantages of long action time, significantly reduced adverse reactions during instantaneous release of drugs, and stable blood concentration.
Description
Technical field
The invention belongs to field of medicaments, be specifically related to a kind of slow releasing preparation that contains tamsulosin hydrochloride, it is with the characteristic of oral cavity disintegration tablet.
Background technology
Quickening along with the aging society process, Seniors has been the colony that can not be ignored, many infirmitiess of age place on the agenda gradually, wherein, male prostatic hyperplasia is one of more commonly encountered diseases of occurrence probability, strengthen the exploitation dynamics in this class drug development and market, to improving man's quality of life, the development that promotes person in middle and old age's medication market has significance.
Tamsulosin hydrochloride, have another name called tamsulosin hydrochloride or hydrochloric acid Tan Suoluoxin, chemical name is { 2-[2-(O-ethoxyl oxygen base) ethylamino-] propyl group }-2-methoxybenzenesulphoismide hydrochlorate, be a kind of the prostate smooth muscle to be had optionally α-1 blocker, it has therapeutical effect to the urinary tract infraction pathological changes that is caused by benign prostatic hyperplasia, and its chemical constitution is
Compare with other α-1 blocker, it has higher selectivity to the prostate smooth muscle, taking dose is therefore less (daily dose is 0.2-0.8mg) also, since the hydrochloric acid Tamsulosin at disease be mostly middle-aging male colony, avoid using non-operative treatment, the compliance that improves the patient also is the key of this type of disease for the treatment of.Middle-older patient is swallowed difficulty, and conventional tablet can not satisfy the compliance of this types of populations, therefore is made into mouth and collapses slow releasing tablet.But too fast because of its absorption, cause the blood drug level rising to cause side effect such as erect type hypotension, so it is prepared into slow releasing preparation.
At present, the relevant patent of the tamsulosin hydrochloride of having reported mainly comprises dosage forms such as tablet, granule, capsule, micropill.
CN200910233724.x discloses a kind of pellet preparations of tamsulosin hydrochloride, and its preparation method is plain ball medicine carrying, reuse double-layer coatings controlled release.Its shortcoming is that dosage is less in the tamsulosin hydrochloride prescription, adopts and extrudes the plain ball of round as a ball preparation, and adjuvant and crude drug cause the content inequality easily not with mix homogeneously.
US4772475 discloses the many granules unit controlled release form that comprises Tamsulosin, microcrystalline Cellulose, the disintegrate in gastrointestinal tract of release key-course.Its control releasing layer material is polyacrylic resin or cellulose family, as hypromellose, and ethyl cellulose.
Summary of the invention
The objective of the invention is to disclose a kind of mouth that contains tamsulosin hydrochloride collapse slow releasing tablet and preparation method thereof, what be specifically related to is to be active component with the tamsulosin hydrochloride, adds the oral formulations of acceptable auxiliary preparation in the oral cavity disintegration tablet.Not only external disintegrate is rapid, patient's compliance height, and also blood drug level is stable, and effect is lasting, discharges fully.
The present invention adopts novel device to prepare micropill, blank pill pericardium clothing medicine carrying, and the method for sustained release coating controlled release prepares the medicine carrying micropill, mixes with adjuvant again, tabletting, the preparation mouth collapses slow releasing preparation, and preparation method is stable, guarantee the content uniformity of small dose drug, do not produced dust, be applicable to production.
The hollow micropill that the present invention relates to uses extrudes spheronization technique, its particle size range is 0.5-2mm, the ball core comprises one or more in microcrystalline Cellulose, lactose, sucrose, the hypromellose, one or both in preferably microcrystalline cellulose, lactose, the hypromellose.
The content of the active ingredient hydrochloric acid Tamsulosin that the present invention relates to accounts for the 0.1%-0.4% of whole content.
Micropill medicated layer among the present invention is made up of active ingredient hydrochloric acid Tamsulosin and a kind of coating material.Active component is dissolved in the solvent of coating solution, this solvent is one or more in water, ethanol, acetone or its mixture.
The coating material that relates among the present invention is a kind of in ethyl cellulose/hypromellose, preferred hypromellose, and the mass ratio of active component and coating material is 0.02: 5-1: 10.
For increasing the dissolubility of principal agent, event needs to add solubilizing agent, its preferably sodium dodecyl sulfate, hexadecanol among the present invention, octadecanol, one or more in the polyoxyethylene sorbitan monoleate, more preferably sodium lauryl sulphate, hexadecanol, one or more in the polyoxyethylene sorbitan monoleate, addition is 1%-3%;
The sustained release coating layer that relates among the present invention adopts multifunctional fluidized bed coating, and every 100g celphere coating amount is preferably medicine layer weightening finish 5-10g, the slow release layer preferred 1-30g that increases weight.
Orally disintegrating is with adjuvant filler preferred mannitol among the present invention, microcrystalline Cellulose, a Lactose hydrate, Icing Sugar, one or more in the pregelatinized Starch, more preferably mannitol, a Lactose hydrate, one or more in the Icing Sugar.Band medicine micropill collapses adjuvant preferred mass ratio with mouth and is, band medicine micropill: mannitol: lactose hydrate: microcrystalline Cellulose: magnesium stearate is 100: 10: 19: 60: 1-100: 40: 40: 19: 1, and behind the mix homogeneously, by theoretical sheet weight sheet.
It is tablet that above-mentioned tamsulosin hydrochloride mouth collapses slow releasing preparation.
The active substance of the low content among the present invention (≤4%) tamsulosin hydrochloride is wrapped in the ball wicking surface and can reaches good slow release effect, pass through fluidized bed coating simultaneously, the coating time is short, no dust, particularly can guarantee the content uniformity of active component, stability is high between batch, is applicable to big production.
Description of drawings
The dynamic disintegration tester in Fig. 1 oral cavity
The specific embodiment
Prescription
Preparation technology takes by weighing the recipe quantity microcrystalline Cellulose, and sucrose adds water soft material processed in right amount behind the mix homogeneously, extrudes spheronizator and prepares piller, and dry back crosses 20 orders and 30 mesh sieves get the blank pill heart (0.5-0.7mm);
The coating prescription
Preparation technology takes by weighing blank pill heart 100g according to prescription configuration coating solution, put into multifunctional fluidized bed in, 5% medicated layer (main content is 0.2g/100g) coating 10g, dry 5min, the strange NE30D coating of 12.5% You Te 25g gets slow release band medicine micropill:
Mouth collapses prescription
Preparation technology: take by weighing recipe quantity band medicine micropill, mannitol, the lactose hydrate, Icing Sugar is used the three-dimensional mixer mixing, behind mixed powder and the recipe quantity magnesium stearate mix homogeneously, by theoretical sheet weight sheet.
According to " the Chinese pharmacopoeia appendix, the disintegration of detection oral cavity disintegration tablet, in the dynamic disintegration tester in oral cavity (as shown in Figure 1), disintegration time of the present invention is 35S, meets requirement disintegration of the oral cavity disintegration tablet of Chinese Pharmacopoeia regulation.
Prescription
Preparation technology takes by weighing the recipe quantity microcrystalline Cellulose, and sucrose adds water soft material processed in right amount behind the mix homogeneously, extrudes spheronizator and prepares piller, and dry back crosses 20 orders and 30 mesh sieves get the blank pill heart (0.5-0.7mm);
The coating prescription
Preparation technology takes by weighing blank pill heart 100g according to prescription configuration coating solution, put into multifunctional fluidized bed in, 5% medicated layer (main content is 0.2g/100g) coating 15g, dry 5min, the strange NE30D coating of 12.5% You Te 25g gets slow release band medicine micropill:
Orally disintegrating tablet prescription
Preparation technology: take by weighing recipe quantity band medicine micropill, mannitol, the lactose hydrate, microcrystalline Cellulose is used the three-dimensional mixer mixing, behind mixed powder and the recipe quantity magnesium stearate mix homogeneously, by theoretical sheet weight sheet
After measured, the disintegration time of embodiment 2 is 28S, meets requirement disintegration of the oral cavity disintegration tablet of Chinese Pharmacopoeia regulation.
Prescription
Preparation technology takes by weighing the recipe quantity microcrystalline Cellulose, and sucrose adds water soft material processed in right amount behind the mix homogeneously, extrudes spheronizator and prepares piller, and dry back crosses 20 orders and 30 mesh sieves get the blank pill heart (0.5-0.7mm);
The drug layer prescription
Preparation technology takes by weighing blank pill heart 100g according to prescription configuration coating solution, puts into
Change in the bed, 5% medicated layer (main content is 0.2g/100g) coating 15g, dry 5min,
NE30D coating 30g gets slow release band medicine micropill
Orally disintegrating tablet prescription
Preparation technology: take by weighing recipe quantity band medicine micropill, mannitol, the lactose hydrate,
Element is used the three-dimensional mixer mixing, behind mixed powder and the recipe quantity magnesium stearate mix homogeneously, by theoretical sheet weight sheet
After measured, be 50S the disintegration of embodiment 3, meets Chinese Pharmacopoeia rule
Disintegration.
Claims (9)
1. a mouth that contains tamsulosin hydrochloride collapses slow releasing preparation, it is characterized in that this dosage form is by blank pill pericardium clothing medicine carrying, the method of sustained release coating controlled release prepares the medicine carrying micropill, adds the slow releasing preparation that acceptable auxiliary is formed in the oral cavity disintegration tablet, and described medicine is tamsulosin hydrochloride.
2. celphere according to claim 1 is characterized in that using and extrudes spheronization technique, and it comprises in microcrystalline Cellulose, lactose, sucrose, the hypromellose one or more.
3. drug-loaded layer coating according to claim 1 is made up of active ingredient hydrochloric acid Tamsulosin and a kind of coating material, and the mass ratio of active component and coating material is 0.02: 5-1: 10.
4. medicine carrying coatings according to claim 1 is dissolved in active component in the solvent of coating solution, and described solvent is one or more in water, ethanol, the acetone.
5. medicine carrying coatings according to claim 3, coating material is one or more in ethyl cellulose, the hypromellose.
6. medicine carrying micropill according to claim 1 also comprises solubilizing agent, sodium lauryl sulphate, hexadecanol, octadecanol, one or more in the polyoxyethylene sorbitan monoleate.
7. adopt multifunctional fluidized bed coating according to the described sustained release coating of claim 1, every 100g celphere coating amount is preferably medicine layer weightening finish 5-10g, the slow release layer preferred 1-30g that increases weight.
8. Orally disintegrating according to claim 1 is with the preferred mannitol of adjuvant filler, microcrystalline Cellulose, a Lactose hydrate, Icing Sugar, one or more in the pregelatinized Starch.
9. collapse adjuvant preferred mass ratio according to the described medicine carrying micropill of claim 1 and mouth and be medicine carrying micropill: mannitol: lactose hydrate: microcrystalline Cellulose: magnesium stearate is 100: 10: 19: 60: 1-100: 40: 40: 19: 1.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013101113110A CN103230379A (en) | 2013-04-02 | 2013-04-02 | Orally disintegrating sustained-release preparation containing tamsulosin hydrochloride and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013101113110A CN103230379A (en) | 2013-04-02 | 2013-04-02 | Orally disintegrating sustained-release preparation containing tamsulosin hydrochloride and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103230379A true CN103230379A (en) | 2013-08-07 |
Family
ID=48878499
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2013101113110A Pending CN103230379A (en) | 2013-04-02 | 2013-04-02 | Orally disintegrating sustained-release preparation containing tamsulosin hydrochloride and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103230379A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105287395A (en) * | 2015-11-19 | 2016-02-03 | 哈尔滨圣吉药业股份有限公司 | Tamsulosin hydrochloride sustained-release pellets and preparation method thereof |
| CN109908097A (en) * | 2017-12-13 | 2019-06-21 | 北京万全德众医药生物技术有限公司 | Linkou County Mo Fanse collapses sustained release tablets |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1473035A (en) * | 2001-07-27 | 2004-02-04 | ֮����ҩ��ʽ���� | Compositions containing substained-release fine grains for tablets quickly disintegrable in oral cavity and process for producing same |
| CN1758903A (en) * | 2003-01-27 | 2006-04-12 | 安斯泰来制药有限公司 | Enteric sustained-release fine particles for tamsulosin or its salt and process for producing the same |
| WO2010001574A1 (en) * | 2008-07-01 | 2010-01-07 | 沢井製薬株式会社 | Process for production of spherical microparticles comprising tamsulosin hydrochloride |
-
2013
- 2013-04-02 CN CN2013101113110A patent/CN103230379A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1473035A (en) * | 2001-07-27 | 2004-02-04 | ֮����ҩ��ʽ���� | Compositions containing substained-release fine grains for tablets quickly disintegrable in oral cavity and process for producing same |
| CN1758903A (en) * | 2003-01-27 | 2006-04-12 | 安斯泰来制药有限公司 | Enteric sustained-release fine particles for tamsulosin or its salt and process for producing the same |
| WO2010001574A1 (en) * | 2008-07-01 | 2010-01-07 | 沢井製薬株式会社 | Process for production of spherical microparticles comprising tamsulosin hydrochloride |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105287395A (en) * | 2015-11-19 | 2016-02-03 | 哈尔滨圣吉药业股份有限公司 | Tamsulosin hydrochloride sustained-release pellets and preparation method thereof |
| CN109908097A (en) * | 2017-12-13 | 2019-06-21 | 北京万全德众医药生物技术有限公司 | Linkou County Mo Fanse collapses sustained release tablets |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP5886632B2 (en) | Immediate release pharmaceutical composition comprising oxycodone and naloxone | |
| KR101156054B1 (en) | A stable and control-released pharmaceutical composition comprising eperisone | |
| AU2014299447B2 (en) | Pharmaceutical capsule composite formulation comprising tadalafil and tamsulosin | |
| CN103596556A (en) | Rapid dissolve tablet compositions for vaginal administration | |
| WO2021129735A1 (en) | Solid preparation, and preparation method therefor and use thereof | |
| EP3813831B1 (en) | Extended release compositions comprising trihexyphenidyl | |
| US20160228386A1 (en) | Pharmaceutical Formulation | |
| CN106420738B (en) | A kind of sustained release preparation of levamlodipine or its salt and preparation method thereof | |
| CN103230379A (en) | Orally disintegrating sustained-release preparation containing tamsulosin hydrochloride and preparation method thereof | |
| Bijank et al. | Formulation development studies of bilayer tablet glipizide: A novel and evolutionary approach in the treatment of diabetes | |
| CN102319225B (en) | Trimetazidine hydrochloride sustained release tablet and preparation method thereof | |
| CN111202731B (en) | Combined application, medicinal composition and application thereof | |
| CN109646417B (en) | Trimetazidine sustained release tablet and preparation method thereof | |
| CN115192572B (en) | Brivaracetam medicament, preparation method and application thereof | |
| JP2022541948A (en) | Stable pharmaceutical composition containing esomeprazole and sodium bicarbonate | |
| CN115919867B (en) | Aidenafil citrate oral sustained-release preparation and preparation method and application thereof | |
| CN108186696B (en) | Bilobalide double-layer controlled release tablet and preparation method thereof | |
| TWI746418B (en) | Pharmaceutical dosage forms comprising sodium 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1h-1,2,3-triazol-1-yl)-1h-pyrazol-5-olate | |
| CN100482227C (en) | Sustained release compound capsules and its preparation method | |
| CN103040798A (en) | Bezafibrate slow release pharmaceutical composition | |
| CN101766608B (en) | Compound pseudoephedrine hydrochloride slow release preparation and preparing method thereof | |
| CN101756991B (en) | Sustained-release pills of alfuzosin hydrochloride | |
| Kolli et al. | DESIGN, DEVELOPMENT OF CARVEDILOL FLOATING PULSATILE DRUG DELIVERY SYSTEM | |
| KR20230152051A (en) | FORMULATION OF A MULTILAYERED PELLET COMPRISING MELATONIN | |
| Sharma et al. | Formulation and evaluation of controlled release osmotic tablet of carvedilol phosphate |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| DD01 | Delivery of document by public notice |
Addressee: Song Xuemei Document name: Notification of Passing Examination on Formalities |
|
| DD01 | Delivery of document by public notice | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20130807 |
|
| WD01 | Invention patent application deemed withdrawn after publication |