CN103211790B - Tamsulosin hydrochloride film-controlled slow-release micro pill capsule - Google Patents
Tamsulosin hydrochloride film-controlled slow-release micro pill capsule Download PDFInfo
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Abstract
The present invention relates to a kind of tamsulosin hydrochloride film-controlled slow-release micro pill capsules, the sustained release clothing film of its pellet is using Eurdragit NE30D and HPMC E5 as filmogen, sodium carboxymethyl starch containing high-expansion in capsule core, and the pharmaceutically acceptable common excipient of sustained release pellet, excipient preferably includes the microcrystalline cellulose of filler and lactose and the polysorbate80 as solubilizer, wherein, the percentage that sodium carboxymethyl starch accounts for capsule core weight in capsule core is 5~20%.It is sustained clothing film and includes EurdragitNE 30D, HPMC E5 and antiplastering aid talcum powder, ratio is preferably 30D: HPMC E5 of Eurdragit NE: talcum powder=30: 2: 4, and coating weight gain is preferably 19~36%.There is the capsule core for the sodium carboxymethyl starch for meeting water high-expansion due to containing, it can significantly be expanded after water suction, sustained release clothing film is caused to be stretched, thickness is thinning, and the aperture of permeable micropore becomes larger, and permeability improves, the permeability for compensating for film aging generation declines, so that middle and later periods rate of release substantially constant, latter stage residual is small, can remain stable release performance before the deadline.
Description
Technical field
The present invention relates to a kind of tamsulosin hydrochloride film-controlled slow-release micro pill capsule, it particularly relates to which a kind of capsule core contains
The tamsulosin hydrochloride film-controlled slow-release micro pill capsule of sodium carboxymethyl starch, belongs to field of pharmaceutical preparations.
Background technology
Tamsulosin hydrochloride is α1AReceptor blocker, by selectively blocking the α in prostate1AReceptor, loose forefront
Gland smooth muscle, so as to improve symptoms such as the dysuria caused by benign prostatic hyperplasis, for treating benign prostatic hyperplasis companion
The urination disorder of hair.
Tamsulosin hydrochloride is slightly molten in water, and what this product listed earliest is to take daily the spansule of 1 time, is sustained for film controlling type
Micro pill capsule.Its sustained release pellet coating membrane uses organic solvent coating solution, and the dosage of organic solvent is larger, the ring in coating process
Border pollution is very big and inflammable and explosive, and safety is relatively low.In addition, external also have listed takes daily the wax matrix sustained release tablet of 1 time,
Gradual corrosion by means of wax discharges drug.But since the drug release area of skeleton is constantly changing, drug release process is that skeleton is molten
The comprehensive effect process of erosion-drug diffusion-dissolution, therefore be difficult to maintain Zero order release, it mostly discharges, is often released the drug not in first-rate
Uniformly, early period, release was too fast, and later stage release is again incomplete.
Sustained release pellet is that drug is made multiunit slow-release system, general oral, capsule dissolving after being packed into capsule
Afterwards, sustained release pellet energy is extensive, is evenly distributed in gastrointestinal tract.Distribution area of the drug on stomach and intestine surface increases, and is ensureing medicine
Object can also effectively reduce stimulation of the drug to gastrointestinal tract while uniformly release.Micropill preparation grain size is smaller, turns in gastrointestinal tract
Fortune is not influenced by the food conveying rhythm and pace of moving things, even if when pyloric sphincter is closed, is remained to through pylorus, therefore particle is in gastrointestinal tract
Absorption do not influenced by gastric emptying generally.What is more important, the drug release behavior of pellet system is each of one dosage of composition
The summation of a pellet drug release behavior, error or defect of indivedual pellets in preparation will not generate the drug release behavior of entire preparation
It seriously affects, therefore better than the slow, Dospan being made of a unit in terms of the reproducibility and consistency of drug release rule.
Tamsulosin hydrochloride is suitable for sustained-release pellet preparation, effective blood drug concentration duration length, blood concentration fluctuation is made
Small, Small side effects, individual difference are small, patient compliance is good.
Due to organic solvent coating solution exist pollution and safety issue, in order to overcome the pollution of organic solvent coating solution and
Safety issue, in film-controlled slow-release preparation field, aqueous dispersion packaging technique is used widely, and common aqueous dispersion has
Aquacoat, crylic acid resin aqueous dispersion, polyvinyl acetate ester aqueous dispersion etc., such as polyvinyl acetate
Ester aqueous dispersion Kollicoat SR 30D, crylic acid resin aqueous dispersion Youteqi RL/RS 30D, Youteqi NE30D with
And Aquacoat Aquacoat and Surelease, however we have found that, the salt prepared using aqueous dispersion coating
Sour Tamsulosin film controlling type sustained-release micro-pill capsules, within a period of time just prepared, release performance is good, however stores one
After the section time, release performance is begun to decline, and storage time is longer, and decline is more apparent, often after the term of validity as defined in drug
Semiduation, release performance are decreased obviously.Analyze reason, be because coating membrane during placement due to aqueous dispersion particle continue
Being combined with each other causes gradually to compact, and membrane permeability is caused to decline, and makes release slack-off, and popular saying is aging.
Invention content
What the film aging of tamsulosin hydrochloride film controlling type sustained release pellet prepared to solve aqueous dispersion coating was brought releases
The problem of putting down drop, the present invention provides a kind of film controlling type hydrochloric acid that can remain stable release performance before the deadline
Tamsulosin sustained-release micro-pill capsules, feature are to contain in the capsule core of pellet with the sodium carboxymethyl starch for meeting water high-expansion,
It is deformed upon by water swelling sustained release coating film, so as to counteract the aging of film.
Film controlling type delays the common aqueous dispersion coating material of controlled release micro pill, such as Eurdragit NE 30D at present, coating
High molecular material itself in material is not soluble in water, but is dispersed in water in particulate form and plasticizer, antiplastering aid etc. are mixed
Aqueous dispersion coating solution is made after conjunction, is sprayed on pellet surface through spray gun, this operation is referred to as being coated；It is micro- when coating just starts
These aqueous dispersions on ball surface exist with a large amount of discontinuous particle shape, increase as coating solution sprays into, these particles
It contacts with each other, deform, agglomerate, last mutual partial fusion forms a discontinuous film；Then it is heat-treated, water volatilization
Afterwards, polymer beads are then connected with each other, fusion completely forms coating membrane.It is heat-treated the film-controlled slow-release pellet being coated to aqueous dispersion
Release performance influence it is very big：If heat treatment is inadequate, such as the time is too short or temperature is too low, polymer particles in coatings
It also will continue to evaporate within subsequent storage period, continuing with film becomes between particle containing micro water between grain
It more compacts, permeability decline causes to discharge slack-off；The method for increasing heating strength in order to avoid such case, generally use
Overcome, such as increase heat treatment time or improve heat treatment temperature, but this processing easily lead to be heat-treated it is excessive,
It causes film excessively dry and compacts, even if initial stage release is qualified, however it is within subsequent storage period, and the film to compact originally can be by
Become loose in the water suction from environment and the creep of film-forming high molecular material, permeability rises, and release is caused to become faster.Put into practice table
It is bright, for film controlling type tamsulosin hydrochloride sustained release pellet, since drug release is completely by diffusion, thus film aging is caused
Permeability decline very sensitive, accomplish just right to ensure to remain stable before the deadline by heat treatment process
Release performance is highly difficult, and the temperature and time being in most cases heat-treated is inadequate, and often later stage release is apparent becomes
Slowly.
For above-mentioned mechanism, the present inventor is surprised to find that by research：If the hydrochloric acid Tan Suoluo of aqueous dispersion coating
Pungent film controlling type sustained release pellet uses the capsule core of the sodium carboxymethyl starch containing high-expansion, can after being absorbed water due to sodium carboxymethyl starch
300 times of original volume are expanded to, can significantly be expanded after capsule core water suction so that pellet volume becomes larger, and release membranes is caused to be stretched, thick
Spend thinning, the aperture of permeable micropore becomes larger, and permeability improves, can compensate heat treatment deficiency cause it is penetrating caused by film aging
Property decline so that middle and later periods rate of release substantially constant, latter stage residual is small.It can additionally eliminate and be heat-treated excessive cause
The influence that film excessively compacts, the change of release performance that day caudacoria Relaxation Zone is avoided, so that drug in the entire term of validity
Rate of release substantially constant.The anti-ageing of the tamsulosin hydrochloride film-controlled slow-release pellet of aqueous dispersion coating can be greatly improved in this way
Change performance.Due to the high-expansion of sodium carboxymethyl starch in capsule core, expansive force is very big, as standing time increases, pellet water suction
Expansion rate afterwards is basically unchanged, and can cause release membranes that irreversible plastic deformation occurs after being stretched, no matter how film changes
(become loose or become and compact) can be supportted and arrive similar degree greatly, so as to which the permeability for ensureing film is basically unchanged.
Preferably, the tamsulosin hydrochloride film-controlled slow-release micro pill capsule of the present invention, the sustained release clothing film of pellet uses
EurdragitNE 30D add in a small amount of HPMC E5 as filmogen, the sodium carboxymethyl starch containing high-expansion in capsule core,
And other pharmaceutically acceptable common excipient of sustained release pellet, the excipient preferably use microcrystalline cellulose and lactose
As filler and polysorbate80 as solubilizer, wherein, sodium carboxymethyl starch accounts for the percentage of capsule core weight in capsule core
Than being 5~20%.Sustained release clothing film includes Eurdragit NE 30D, HPMC E5 and antiplastering aid talcum powder, ratio are preferably
30D: HPMC E5 of Eurdragit NE: talcum powder=30: 2: 4, coating weight gain is preferably 19~36%.
As one of the preferred embodiment of the present invention, tamsulosin hydrochloride film-controlled slow-release micro pill capsule of the invention it is micro-
Ball prescription is as follows：
First, capsule core prescription (1000 meters)
2nd, it is sustained clothing film prescription
It is preferred that sustained release clothing film coating weightening is 19~36%.
Invention also provides a kind of tamsulosin hydrochloride film-controlled slow-release micro pill capsules for improving aqueous dispersion coating to resist
The method of ageing properties, it is characterized in that the sustained release clothing film of pellet is made using aqueous dispersion Eurdragit NE 30D and HPMC E5
For filmogen, capsule core contains sodium carboxymethyl starch and the common excipient of other sustained release pellets, and the excipient preferably uses
Microcrystalline cellulose and lactose are as filler and polysorbate80 as solubilizer.Wherein, sodium carboxymethyl starch in capsule core
The percentage for accounting for capsule core weight is 5~20%, and sustained release clothing film includes aqueous dispersion Eurdragit NE 30D, HPMC E5 and resists
Stick talcum powder, weight ratio are 30D: HPMC E5 of Eurdragit NE: talcum powder=30: 2: 4, coating weight gain for 19~
36%.The above method it is preferred, be based on 1000 capsules, pellet use following prescription：
First, capsule core prescription (1000 meters)
2nd, it is sustained clothing film prescription
It is preferred that sustained release clothing film coating weightening is 19~36%.
The preparation method of film controlling type tamsulosin hydrochloride sustained release pellet of the present invention, can be according to film in the prior art
Control type delays the general technology of controlled release micro pill to prepare, including batch mixing, pill core, the slow clothing film of packet etc., it is preferred to use squeeze out rolling
Circule method prepares capsule core.The sustained release pellet made is packed into No. 0 common stomach dissolution type gelatine capsule to get to tamsulosin hydrochloride film control
Sustained-release micro-pill capsules.
Film controlling type tamsulosin hydrochloride sustained-release micro-pill capsules of the present invention have the following advantages：
1) aging of confrontation sustained release clothing film：It is formed with aqueous dispersion Eurdragit NE 30D+HPMC E5+ talcum powder
Clothing film meeting aging is sustained, the reason is that aqueous dispersion particle, which combines, promotes film aging, membrane permeability is caused to reduce, and containing has chance
The capsule core of the sodium carboxymethyl starch of water high-expansion can significantly expand after water suction, and sustained release clothing film is caused to be stretched, and thickness is thinning,
The aperture of permeable micropore becomes larger, and permeability improves, and the permeability for compensating for film aging generation declines, so that the middle and later periods discharges
Speed substantially constant, latter stage residual is small, can remain stable release performance before the deadline.
2) supporting role：It, can be apparent expanded after water suction using the capsule core of the sodium carboxymethyl starch with water swelling
To supporting role, can burst drug release caused by the extruding by gastrointestinal tract be avoided in gastrointestinal tract operation process in vivo.
Specific embodiment
The tamsulosin hydrochloride sustained-release micro-pill capsules of 1 common capsule core of embodiment
First, prescription
1st, capsule core prescription (1000)
2nd, it is sustained clothing film coating liquid prescription
3rd, No. 0 stomach dissolution type gelatine capsule shell 1000
2nd, preparation process：
1st, capsule core preparation process：
(1) tamsulosin hydrochloride is crossed into 60 mesh sieve；
(2) microcrystalline cellulose PH101, the lactose of recipe quantity are weighed, puts in wet granulator and is uniformly mixed；
(3) tamsulosin hydrochloride of recipe quantity is added in the polysorbate80 of recipe quantity, adds in a small amount of water, water-bath
Heating makes tamsulosin hydrochloride, polysorbate80 dissolving；
(4) above-mentioned solution is all poured into wet granulator, is uniformly mixed with microcrystalline cellulose PH101, lactose, then
Add in suitable 2% sodium carboxymethylcellulose, 10% ethanol solution softwood；
(5) it puts on extruder and squeezes out, mesh size 1.0mm, extruded velocity is 20~30rpm；
(6) round as a ball, round as a ball speed is 900~1000rpm, is dried in fluid bed；
(7) it is sieved, takes the capsule core between 16~30 mesh.
2nd, it is sustained clothing film coating liquid preparing process：
The HPMC E5 for weighing recipe quantity are dissolved in the water of recipe quantity, are stirred evenly.Add in the talcum powder of recipe quantity, stirring
Shearing is uniform, then adds in Eurdragit NE 30D, stir evenly to get.
3rd, coating (sustained release clothing film)：
Capsule core is placed in fluid bed and is coated, control clothing film weightening, coating weight gain 14.2%.
4th, it is heat-treated：
The pellet for wrapping extended release coatings is heat-treated in fluid bed under the conditions of 40 DEG C/2h.
5th, capsule is filled：
By coating micro-pill filling capsule to obtain the final product.
3rd, release, assay and result
【Release】This product is taken, according to drug release determination method (two the first methods of annex X D of China's coastal port), is used
The device of the second method of dissolution method, using water 900ml as solvent, rotating speed be 200 turns per minute, operate in accordance with the law, through 3 hours, 7
Hour and at 12 hours, take solution 10ml respectively, filter, and supplement in process container same volume, mutually synthermal immediately
Dissolution medium, precision measure subsequent filtrate 5ml, put in 10ml measuring bottles, and precision adds in inner mark solution (5.0 μ g/ml P-hydroxybenzoic acid
The aqueous solution of methyl esters) 1.0ml, scale is diluted to 0.01mol/L kaliumphosphate buffers (pH3.0)-methanol (7: 3, v/v), is shaken
It is even, as test solution；Separately precision weighs tamsulosin hydrochloride reference substance and appropriate methyl p-hydroxybenzoate respectively, adds water
It dissolves and dilutes the solution for being made and containing 0.37 μ g and 0.83 μ g in every 1ml respectively, precision measures this solution 6ml, puts 10ml measuring bottles
In, add 0.01mol/L phosphoric acid that buffer solution (pH3.0)-methanol (7: 3, v/v) is added to be diluted to scale, shake up, it is molten as reference substance
Liquid.It is measured according to high performance liquid chromatography (two annex V D of China's coastal port), is with octadecylsilane chemically bonded silica
Filler, with 0.01mol/L kaliumphosphate buffers (pH3.0)-methanol-acetonitrile (70: 20: 10, w/v/v) for mobile phase, detection
Wavelength is 225nm, column temperature：35 DEG C, flow velocity 1.3ml/min.Precision measures reference substance solution 100ul, repeats sample introduction 6 times, smooth
Suo Luoxin peak areas and R contents (%) D of internal standard peak area ratio answer≤2.0%.The accurate test solution and right of measuring respectively
According to each 100 μ l of product solution, liquid chromatograph is injected, records chromatogram.Go out every when different by internal standard method with calculated by peak area
Between burst size.This product every the burst size of 3 hours, 7 hours and 12 hours should mutually should be respectively labelled amount 15~35%,
45~65% and more than 80%, regulation should all be met.
【Assay】It is measured according to high performance liquid chromatography (two annex V D of China's coastal port).
Chromatographic condition is filler with octadecylsilane chemically bonded silica with system suitability；With 0.01mol/L phosphorus
Sour potassium buffer solution (pH3.0) is mobile phase A, and acetonitrile is Mobile phase B, and according to the form below carries out gradient elution；Column temperature：33~35 DEG C, stream
Speed is 1.3ml/min, Detection wavelength 225nm.Precision measures reference substance solution 25ul, repeats sample introduction 6 times, Tamsulosin peak face
Product and R contents (%) D of internal standard peak area ratio answer≤1.5%.
Measuring method takes this product 20, puts in 50ml measuring bottles, precision add in 20ml inner mark solutions (0.13mg/ml to hydroxyl
Butyl benzoate methanol solution), it shakes 40 minutes, ultrasound 30 minutes, centrifugation, precision measures supernatant 5ml, puts 25ml measuring bottles
In, scale is diluted to 0.01mol/L potassium phosphate buffers (pH3.0), is shaken up, filters, takes subsequent filtrate as test sample
Solution；Precision weighs tamsulosin hydrochloride reference substance and appropriate butyl p-hydroxybenzoate respectively, adds 0.01mol/L biphosphates
Potassium buffer solution (pH3.0)-methanol (7: 3, v/v) dissolves and is diluted in every 1ml the solution respectively containing 0.04mg and 0.026mg,
As reference substance solution, precision measures test solution and each 25 μ l of reference substance solution, injects liquid chromatograph, records chromatography
Figure；By internal standard method with calculated by peak area to get.
As a result such as table 1：
1 embodiment 1 of table discharges and content results
The result shows that 1 capsule core of embodiment is free of the tamsulosin hydrochloride sustained-release micro-pill capsules of intumescent material, initial release
Good, as standing time increases, the continuous aging of film, rate of release is slack-off, remains apparent increase.
4th, expansion rate measures
Assay method：It is added in into 100ml measuring bottles and is preheated to 37 DEG C of distillation appropriate amount of water, be dipped in 37 DEG C of water-baths and with steaming
It is spare after distilled water constant volume to scale；3 500ml beakers are taken, the distilled water that 300ml is preheated to 37 DEG C is separately added into, is immersed in 37
It is spare in DEG C water-bath；Capsule 10 to be measured is taken, capsule shells is removed, pellet in capsule is poured out, is put in above-mentioned 100ml measuring bottles, it is fast
Distilled water in the pipette, extract measuring bottle that speed is 0.01ml with minimum scale value is until liquid level is fallen after rise to measuring bottle scale, then accurately
The volume of water in pipette is read, the average external volume of pellet in every capsule is calculated, is denoted as V0.30 capsules to be measured are taken, are divided into 3
Group, removes capsule shells, pellet in capsule is poured out, puts in above-mentioned 3 500ml beakers and impregnates respectively, exist respectively by every group 10
3h, 7h, 12h respectively take out 1 group, filtration, and the water of pellet surface residual is blotted with filter paper, put again constant volume cross it is above-mentioned
In the measuring bottle of 100ml, rapidly with distilled water in above-mentioned pipette, extract measuring bottle until liquid level is fallen after rise to measuring bottle scale, then accurately
The volume of water in pipette is read, the average external volume of pellet in every capsule is calculated, is denoted as VT.When each sampling is calculated as follows
Between the expansion rate put, the results are shown in Table 2.
Calculation formula：Expansion rate (%)=(VT-V0)/V0× 100%
Expansion rate result after the placement for a long time of 2 room temperature of table
The experimental results showed that capsule core is free of the tamsulosin hydrochloride sustained-release micro-pill capsules of intumescent material, pellet expansion rate
Very little, and as room temperature is placed for a long time, expansion rate reduces therewith, does not offset the effect of sustained release clothing film aging.
Tamsulosin hydrochloride sustained-release micro-pill capsules of the embodiment 2 containing 5% sodium carboxymethyl starch
First, prescription
1st, capsule core prescription (1000)
2nd, it is sustained clothing film coating liquid prescription：With embodiment 1
3rd, No. 0 stomach dissolution type gelatine capsule shell 1000
2nd, preparation process：
1st, capsule core preparation process：
(1) tamsulosin hydrochloride is crossed into 60 mesh sieve；
(2) microcrystalline cellulose PH101, sodium carboxymethyl starch, the lactose of recipe quantity are weighed, puts in wet granulator and mixes
It is even；
(3) tamsulosin hydrochloride of recipe quantity is added in the polysorbate80 of recipe quantity, adds in a small amount of water, water-bath
Heating makes tamsulosin hydrochloride, polysorbate80 dissolving；
(4) above-mentioned solution is all added in wet granulator, then adds in suitable 2% sodium carboxymethylcellulose 10%
Ethanol solution softwood；
(5) it puts on extruder and squeezes out, mesh size 1.0mm, extruded velocity is 20~30rpm；
(6) round as a ball, round as a ball speed is 900~1000rpm, is dried in fluid bed；
(7) it is sieved, takes the capsule core between 16~30 mesh.
2nd, it is sustained clothing film coating liquid preparing process：With embodiment 1.
3rd, coating (sustained release clothing film)：
Capsule core is placed in fluid bed and is coated, control clothing film weightening, coating weight gain 19.2%.
4th, it is heat-treated：With embodiment 1.
5th, capsule is filled：By coating micro-pill filling capsule to obtain the final product.
3rd, release, assay and result
Assay method：With embodiment 1,3 are the results are shown in Table
3 embodiment 2 of table discharges and content results
The result shows that tamsulosin hydrochloride sustained-release micro-pill capsules of the capsule core of embodiment 2 containing sodium carboxymethyl starch 5% are initial
Release performance is good, and as standing time increases, releasing effect is still fine, and end point release remains equal very little.
4th, swelling rate test
Experimental method：With embodiment 1,4 are the results are shown in Table
Expansion rate result after the placement for a long time of 4 room temperature of table
The experimental results showed that the tamsulosin hydrochloride sustained release pellet glue of capsule core sodium carboxymethyl starch containing intumescent material 5%
Capsule, pellet expansion rate is larger, and under room temperature is placed for a long time, expansion rate remains unchanged, and counteracts the aging of sustained release clothing film.
Tamsulosin hydrochloride sustained-release micro-pill capsules of the embodiment 3 containing 10% sodium carboxymethyl starch
First, prescription
1st, capsule core prescription (1000)
2nd, it is sustained clothing film coating liquid prescription：With embodiment 1
3rd, No. 0 stomach dissolution type gelatine capsule shell 1000
2nd, preparation process：
1st, capsule core preparation process：With embodiment 2.
2nd, it is sustained clothing film coating liquid preparing process：With embodiment 1.
3rd, coating (sustained release clothing film)：
Capsule core is placed in fluid bed and is coated, control clothing film weightening, coating weight gain 24.5%, 27.7%.
4th, it is heat-treated：With embodiment 1.
5th, capsule is filled：By coating micro-pill filling capsule to obtain the final product.
3rd, release, assay and result
Assay method：With embodiment 1,5 are the results are shown in Table
5 embodiment 3 of table discharges and content results
The result shows that tamsulosin hydrochloride sustained-release micro-pill capsules initial release performance of the capsule core containing sodium carboxymethyl starch 10%
Good, as standing time increases, releasing effect is still fine, and end point release remains equal very little.
4th, expansion rate is tested
Experimental method：With embodiment 1,6 are the results are shown in Table
Expansion rate result after the placement for a long time of 6 room temperature of table
The experimental results showed that the tamsulosin hydrochloride sustained release pellet glue of capsule core sodium carboxymethyl starch containing intumescent material 10%
Capsule, pellet expansion rate is larger, and under room temperature is placed for a long time, expansion rate remains unchanged, and counteracts the aging of sustained release clothing film.
Tamsulosin hydrochloride sustained-release micro-pill capsules of the embodiment 4 containing 15% sodium carboxymethyl starch
First, prescription
1st, capsule core prescription (1000)
2nd, it is sustained clothing film coating liquid prescription：With embodiment 1
3rd, No. 0 stomach dissolution type gelatine capsule shell 1000
2nd, preparation process
1st, capsule core preparation process：With embodiment 2.
2nd, it is sustained clothing film coating liquid preparing process：With embodiment 1
3rd, coating (sustained release clothing film)：
Capsule core is placed in fluid bed and is coated, control clothing film weightening, coating weight gain 32.3%.
4th, it is heat-treated：With embodiment 1.
5th, capsule is filled：By coating micro-pill filling capsule to obtain the final product.
3rd, release, assay and result
Assay method：With embodiment 1,7 are the results are shown in Table
7 embodiment 4 of table discharges and content results
The result shows that tamsulosin hydrochloride sustained-release micro-pill capsules initial release performance of the capsule core containing sodium carboxymethyl starch 15%
Good, as standing time increases, releasing effect is still fine, and end point release remains equal very little.
4th, expansion rate is tested
Experimental method：With embodiment 1,8 are the results are shown in Table
Expansion rate after the placement for a long time of 8 room temperature of table
The result shows that tamsulosin hydrochloride sustained-release micro-pill capsules of the capsule core containing sodium carboxymethyl starch 15%, pellet expansion rate
Larger, under room temperature is placed for a long time, expansion rate remains unchanged, and counteracts the aging of sustained release clothing film.
Tamsulosin hydrochloride sustained-release micro-pill capsules of the embodiment 5 containing 20% sodium carboxymethyl starch
First, prescription
1st, capsule core prescription (1000)
2nd, it is sustained clothing film coating liquid prescription：With embodiment 1
3rd, No. 0 stomach dissolution type gelatine capsule shell 1000
2nd, preparation process
1st, capsule core preparation process：With embodiment 2
2nd, it is sustained clothing film coating liquid preparing process：With embodiment 1.
3rd, coating (sustained release clothing film)：
Capsule core is placed in fluid bed and is coated, control clothing film weightening, coating weight gain 35.7%.
4th, it is heat-treated：With embodiment 1.
5th, capsule is filled：By coating micro-pill filling capsule to obtain the final product.
3rd, release, assay and result
Assay method：With embodiment 1,9 are the results are shown in Table
9 embodiment 5 of table discharges and content results
The result shows that tamsulosin hydrochloride sustained-release micro-pill capsules initial release performance of the capsule core containing sodium carboxymethyl starch 20%
Good, as standing time increases, releasing effect is still fine, and end point release remains equal very little.
4th, expansion rate is tested
Experimental method：With embodiment 1,10 are the results are shown in Table
Expansion rate after the placement for a long time of 10 room temperature of table
The result shows that tamsulosin hydrochloride sustained-release micro-pill capsules of the capsule core containing sodium carboxymethyl starch 20%, pellet expansion rate
Larger, under room temperature is placed for a long time, expansion rate remains unchanged, and counteracts the aging of sustained release clothing film.
Claims (1)
1. a kind of method for the tamsulosin hydrochloride film-controlled slow-release micro pill capsule anti-aging property for improving aqueous dispersion coating, special
Sign is based on 1000 capsules, and the pellet uses following prescription：
Capsule core prescription：
It is sustained clothing film prescription：
It is 19~36% to be sustained clothing film coating weightening.
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| CN101695478A (en) * | 2009-10-23 | 2010-04-21 | 江苏大学 | Tamsulosin hydrochloride sustained-release pellets and preparation method thereof |
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