CN103315962A - Tamsulosin sustained-release pellet preparation and preparation method thereof - Google Patents
Tamsulosin sustained-release pellet preparation and preparation method thereof Download PDFInfo
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- CN103315962A CN103315962A CN201310042463XA CN201310042463A CN103315962A CN 103315962 A CN103315962 A CN 103315962A CN 201310042463X A CN201310042463X A CN 201310042463XA CN 201310042463 A CN201310042463 A CN 201310042463A CN 103315962 A CN103315962 A CN 103315962A
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Abstract
The invention provides a tamsulosin sustained-release pellet, and the drug release of the sustained-release pellet is controlled through a blank pellet core coated with a drug-loaded sustained-release layer and then coated with an enteric coating, and the drug can be both released in an acidic or weak alkaline environment and is absorbed well in vivo. Also, release homogeneity is good, preparation technology is simple and repeatability is good.
Description
Technical field
The present invention relates to sustained-release pellet preparation of a kind of new sustained release pellet preparations and preparation method thereof, particularly a kind of tamsulosin hydrochloride and preparation method thereof.
Background technology
Tamsulosin hydrochloride is that the third generation has super-selective long-acting α-1 inhibitor to prostate smooth musculature cells, is the urinary tract infraction sexually transmitted disease (STD) that is caused by benign prostatic hyperplasia is become medicative medicine, and its daily dose is 0.2 ~ 0.8mg.Tamsulosin hydrochloride is higher to the selectivity of prostate smooth musculature cells, and its taking dose also so less causes the side effect such as causing orthostatic hypotension that raises of its blood drug level for preventing that it from absorbing fast, and it is prepared into slow releasing preparation is to select preferably.By Japanese Yamanouchi pharmaceutical development success, obtain FDA approval listing in July, 1992, trade name Harnal(Harnal).After this jointly sell tamsulosin hydrochloride with Boehringer Ingelheim, Abbott, obtained the FDA approval in 1997, trade name Flomax.This medicine can suppress the contraction of prostate smooth musculature cells specifically, alleviates rapidly the BPH clinical symptoms, good effect, less adverse effect.Sales volume rapid growth after the listing is at present domestic and international best selling variety.
Prostate is the same with other organ of human body, and is aging with advancing age and gradually, thinks theoretically, body of prostate was annual after the man entered and grows up increases by 3%, the sickness rate of hypertrophy is extremely low before 45 years old, and sickness rate raises gradually after climacteric, and produces the different urinary tract obstruction symptom of weight.Analyze according to statistics, benign prostatic hyperplasia (BPH) patient accounts for about 20% of elderly men, its sickness rate also has certain relation with race, area, Asians's occurrence probability is national less than the west, the sickness rate of external BPH is apparently higher than domestic, generally there is among the crowd of prostatic hyperplasia family history sickness rate higher, accounts for more than 1/2.Studies show that for many years, Incidence of BPH mechanism is out of proportion with hormone in vivo, dihydrotestosterone builds up relevant in prostate, after the front gland hypertrophy, can oppress the urethra in the body of gland, cause dysuria, can not alleviate for a long time easy generation bilateral ureteral, renal pelvis hydrops, the atrophy of disease excess of the kidney in late period matter can cause uremia.Before effectively medicine came out, operation was this sick Main Means for the treatment of, also is the selected Therapeutic Method of disease serious person, and effect is better, but still had the poor prognosis such as sexual dysfunction, urinary incontinence occur.Along with continually developing of prostate treatment medicine, non-operative treatment is subject to majority's favor, reduced gradually the probability of operation, although treatment benign prostatic hyperplasia market drug kinds is more at present, mainly is comprised of α acceptor inhibitor, antiandrogen medicine and plant-based medicine three major types.
At present, the tamsulosin hydrochloride Patents of having reported mainly comprises the dosage forms such as tablet, granule, micropill.
Application number 03824940.5 is that Japanese Yamanouchi pharmacy is in the patent of invention of China's application, disclose a kind of micropill slow releasing preparation of tamsulosin hydrochloride, mainly adopted the adjuvants such as Eudragit L30D-55, Polyethylene Glycol and microcrystalline Cellulose, magnesium stearate to prepare slow-releasing granules encapsulated.Wherein microcrystalline Cellulose is as the carrier of micropill, PEG or polyoxyethylene etc. are as slow-release material, Eudragit L30D-55 is as becoming the ball binding agent, magnesium stearate is as lubricant, prepared micropill/granule and medicine are lumped together, after entering in the body, the stripping duct that forms by water soluble ingredient in the micropill is drug release, thereby controlled release.Application number 200380109413.3 discloses a kind of controlled release pharmaceutical compositions of tamsulosin hydrochloride, medicine and one or more rate control polymers are mixed with micropill reach the control drug release rate, and/or reach the effect that further control discharges by single coats.Application number 200910233724.X discloses a kind of micropill of the dual clothing of pastille element ball bag of tamsulosin hydrochloride, it discharges by the control of double-layer sustained release clothing, obtained the preparation that the acid-alkali medium release meets quality standard, its shortcoming is, although adopted pastille element ball to assist control to discharge, the double-layer coatings co-controlling is high for the coating parameter request, particularly for the such small dimension medicine of Tamsulosin, rate of releasing drug is difficult to control.
Summary of the invention
The invention provides a kind of new Tamsulosin slow-release micro-pill, this slow-release micro-pill adopts the again enteric coated drug release of controlling of celphere bag carried medicine sustained-release layer, can both discharge under acidity or weakly alkaline environment, enters good absorbing in the body.And the release homogeneity is good, and preparation technology is simple, good reproducibility.
According to weight ratio, described slow-release micro-pill chief component comprises:
1) celphere 60-95%
2) carried medicine sustained-release layer
Tamsulosin and pharmaceutically acceptable salt 0.1-10% thereof
The mixture of water-insoluble or swelling polymer or enteric material I or three's arbitrary proportion
1-30%
3) coatings
Enteric material II 0.5-10%
In addition, the invention provides the slow-release micro-pill and preparation method thereof of a kind of Tamsulosin and pharmaceutically acceptable salt thereof.As the small dimension medicine, daily dose is 0.2 ~ 0.8mg only, and is insoluble in water, adopts the conventional pill core that contains to prepare uncontrollable medicine reach desirable release profiles, the slow releasing preparation that particularly all can discharge in gastrointestinal.
The slow-release micro-pill of Tamsulosin of the present invention and pharmaceutically acceptable salt thereof, according to weight ratio, its chief component comprises:
According to weight ratio, described slow-release micro-pill chief component comprises:
1) celphere 60-95%
2) carried medicine sustained-release layer
Tamsulosin and pharmaceutically acceptable salt 0.1-1% thereof
The mixture of water-insoluble or swelling polymer or enteric material I or three's arbitrary proportion
1-30%
3) coatings
Enteric material II 0.5-10%
Preferably, according to weight ratio, 1) celphere 75-90% further is 80-90%.
Preferably, according to weight ratio, 2) in the carried medicine sustained-release layer, Tamsulosin and pharmaceutically acceptable salt 0.1-0.5% thereof further are 0.1-0.3%; The mixture of water-insoluble or swelling polymer or enteric material I or three's arbitrary proportion is 3-20%, further 3-15%.Wherein, can not be any in the above-mentioned arbitrary proportion 2 be zero simultaneously.
Preferably, coatings enteric material II is 0.5-5%, further is 1-3%.
Further, in described carried medicine sustained-release layer and/or the coatings, also can comprise solubilizing agent and/or the plasticizer of 0.1-5% and/or the binding agent of 0.1-5% of 0.1-5%.Further, described pastille micropill and coatings also can comprise the antiplastering aid of 0.1-5%.The galenic pharmacies such as opacifier, antioxidant, the pigment adjuvant commonly used that further, can also comprise usual amounts.
Further, bag the first sealing coat between celphere and the carried medicine sustained-release layer, and/or bag the second sealing coat between carried medicine sustained-release layer and the coatings.Described sealing coat is mainly Pulvis Talci, stearic acid, micropowder silica gel one or both and above mixture wherein.
Wherein, described Tamsulosin and pharmaceutically acceptable salt thereof mainly are absorbed by the body at intestinal after entering in the body, namely its dosage or totally the amount of being absorbed 60% and more than be to be absorbed or to discharge at intestinal.Furthermore, can not absorb under one's belt/discharge or a small amount of absorption the/release or degraded.Among the present invention, described Tamsulosin and pharmaceutically acceptable salt thereof refer to pharmaceutically passable salt or forms such as prodrug or optical isomer of the activity form of Tamsulosin and pharmaceutically acceptable salt thereof or chemical constitution this city or its, are preferably hydrochlorate.Described celphere is inert material preparation, can make for water solublity or water-insoluble adjuvant, includes but not limited to one or both and above mixture thereof in sucrose, microcrystalline Cellulose, lactose, the starch.Be preferably sucrose or lactose.The order number is the 15-30 order, preferably from the 20-25 order.
Described insoluble polymer includes but not limited to one or both and above mixture thereof of acrylic resin or cellulose derivative apoplexy due to endogenous wind.Acrylic resin refers to methacrylic acid copolymer and first acrylate copolymer, and normal open is called acrylic resin.For example cellulose acetate, ethyl cellulose, especially one or both in the strange RL/RS series and above mixture thereof.Swelling polymer refers to, in water or in the aqueous solution, volume increase but and the speed of water fast or dissolving be far smaller than the speed of swelling.Include but not limited to one or both and above mixture in starch, sodium alginate, the polyoxyethylene.
Described enteric material I and II include but not limited to one or both and the above mixture thereof in acrylic resin or the cellulose acetate-phthalate (CAP), be preferably crylic acid resin, such as especially strange S/L is serial, include but not limited to especially strange E 100, strange EPO powder (can be made into aqueous dispersion) especially, strange L 100--55 especially, strange L 30D-55 aqueous dispersion especially, strange L 100 especially, strange S 100 especially, strange RL 100 especially, strange RL PO especially, strange RL 30D aqueous dispersion especially, especially wherein one or both reach above mixture to strange RS 100 grades.Enteric material I and II can be identical can also be different.
Described solubilizing agent includes but not limited to Tweens, spans, anion surfactant, preferably from sodium lauryl sulphate.
Described plasticizer is selected from phthalic acid ester, aliphatic dibasic acid ester etc., includes but not limited to PEG400-6000, ATBC etc., and described antiplastering aid is selected from Pulvis Talci or silicon dioxide.
Tamsulosin of the present invention and pharmaceutically acceptable salt sustained-release pellet preparation thereof are owing to having adopted carried medicine sustained-release layer and enteric layer, the method of dual controlled release discharges therefore all can realize the Tamsulosin and the pharmaceutically acceptable salt thereof that meet the expected requirements in different acid-alkali mediums.The inventor surprisingly finds, increases because medicine carrying ball wicking surface is long-pending, is beneficial to very much the later stage release control of medicine, and namely when medicine was deposited in dosage on the micropill and becomes fewer and feweri, larger surface area can be so that drug release be complete.And, owing to adopting carried medicine sustained-release layer supplementary product consumption less, be not higher than 40% of whole prescription, preferably be not higher than 25%, adjuvant is very little to the absorption of medicine, almost can ignore, the response rate reaches more than 99%, and this is very important for the Tamsulosin of low dose and pharmaceutically acceptable salt thereof.
Further, the inventor surprisingly finds, adopt the slow-release micro-pill of such scheme preparation, than the prior art enteric coated scheme of medicine carrying ball commonly used, greatly reduce the consumption of enteric material, be reduced to below 10% from the consumption of 10%-15%, preferably be lower than 5%, decrease by more than 100%, greatly saved production cost.
Preferably, according to weight ratio, described slow-release micro-pill chief component comprises:
1) celphere 75-90%
2) carried medicine sustained-release layer
Tamsulosin and pharmaceutically acceptable salt 0.1-0.5% thereof
The mixture of water-insoluble or swelling polymer or enteric material I or three's arbitrary proportion
3-20%
3) coatings
Enteric material II 0.5-5%
Further, preferably, according to weight ratio, described slow-release micro-pill chief component comprises:
1) celphere 80-90%
2) carried medicine sustained-release layer
Tamsulosin and pharmaceutically acceptable salt 0.1-0.3% thereof
The mixture of water-insoluble or swelling polymer or enteric material I or three's arbitrary proportion
3-15%
3) coatings
Enteric material II 1-3%
Preferably, described slow-release micro-pill mainly comprises according to weight ratio:
1) sucrose or microcrystalline Cellulose or lactose ball core 60-95%
2) carried medicine sustained-release layer
Tamsulosin and pharmaceutically acceptable salt 0.1-10% thereof
Ethyl cellulose or cellulose acetate or the mixture of strange RL/RS series or three's arbitrary proportion especially
1-30%
3) coatings
Strange RL/RS series 0.5-10% especially
Preferably, described slow-release micro-pill mainly comprises according to weight ratio:
1) sucrose or microcrystalline Cellulose or lactose ball core 60-95%
2) carried medicine sustained-release layer
Tamsulosin and pharmaceutically acceptable salt 0.1-1% thereof
Ethyl cellulose or cellulose acetate or the mixture of strange RL/RS series or three's arbitrary proportion especially
1-30%
3) coatings
Strange RL/RS series 0.5-10% especially
Preferably, described slow-release micro-pill mainly comprises according to weight ratio:
1) sucrose or microcrystalline Cellulose or lactose ball core 60-95%
2) carried medicine sustained-release layer
Tamsulosin and pharmaceutically acceptable salt 0.1-1% thereof
Ethyl cellulose or cellulose acetate or the mixture of strange RL/RS series or three's arbitrary proportion especially
3-20%
Sodium lauryl sulphate or Tween 80 0.1-5%
3) coatings
Strange RL/RS series 0.5-10% especially
Preferably, described slow-release micro-pill mainly comprises according to weight ratio:
1) sucrose or microcrystalline Cellulose or lactose ball core 60-95%
2) carried medicine sustained-release layer
Tamsulosin and pharmaceutically acceptable salt 0.1-1% thereof
Ethyl cellulose or cellulose acetate be the mixture of strange RL/RS series or three's arbitrary proportion especially
3-20%
Sodium lauryl sulphate or Tween 80 0.1-5%
3) coatings
Strange RL/RS series 0.5-10% especially
Sodium lauryl sulphate or Tween 80 0.1-5%
Preferably, described Tamsulosin and pharmaceutically acceptable salt thereof are tamsulosin hydrochloride.
It should be noted that in the mixture of above-mentioned middle N person's arbitrary proportion that arbitrarily N-1 is zero simultaneously, N is exponential quantity, the mixture that forms such as N/family macromolecule material.
The present invention also provides a kind of method for preparing Tamsulosin and pharmaceutically acceptable salt slow-release micro-pill thereof.The present invention also provides a kind of method for preparing above-mentioned slow-release micro-pill, namely at first the carried medicine sustained-release layer is added medicine to after the dissolution with solvents by being fit to, and wraps the method for enteric material again.Key step is as follows:
Step 1: take by weighing celphere, each component of carried medicine sustained-release layer by prescription, be dissolved in suitable solvent and be mixed with drug solns, add medicine to fluid bed, 30-55 ℃ of control temperature of charge made pill.
Step 2: to the processing of sieving of upper pill, sieve number 15-30 order.
Step 3: the upper pill after will sieving places in the fluid bed, further packs with the solution that contains the enteric material II for preparing in advance, and 30-55 ℃ of control temperature of charge, the dry 5-15min of continuation after coating is finished takes out, both.
Further, described suitable solvent refers to dissolve alcohol, ketone and/or other micromolecule organic solvents of each component of pastille micropill and/or the mixture that dissolves each other with arbitrary ratio with water, includes but not limited to 75% ethanol, 95% ethanol, acetone, methanol, dehydrated alcohol etc.Equally, the solution that contains enteric material can be selected alcohol, ketone and/or other micromolecule organic solvents that can dissolve this enteric material and/or the mixture that dissolves each other with arbitrary ratio with water.
Preferably, have step 4) the micropill that step 3 prepares is added the moderate lubrication agent, encapsulated such as Pulvis Talci or micropowder silica gel etc., and get final product.
Further, after finishing coating, step 1/3 carries out carrying out again step 2/ step 4 after the first sealing coat/second sealing coat coating and the drying.
Further, at encapsulated before measurement intermediate medicament contg, calculate loading according to the medicine specification, take by weighing.
Be, the suitable solvent of using in the preparation method among the present invention is removed in preparation with should be noted that, though have residual also seldom, therefore, ignore.Even moisture is had certain requirement, but generally all be not counted in the final prescription.
Description of drawings
Fig. 1 is the accumulative total release profiles of embodiment 1.Wherein abscissa is time (h), and vertical coordinate is medicine accumulative releasing degree (%).
The specific embodiment
Further explain and describe by the following examples content of the present invention.Described embodiment only in order to help to understand content of the present invention, should not be understood to the restriction to purport of the present invention and protection domain.
Drug release determination method of the present invention is referring to two appendix XD of Chinese Pharmacopoeia version in 2010 first method.
Tamsulosin hydrochloride slow releasing capsule (5000)
1) sucrose ball core 605g
2) carried medicine sustained-release layer
Tamsulosin hydrochloride 1g
Cellulose acetate 33.75g
3) coatings
Eudragit L100-55 11.25g
Sodium lauryl sulphate 7.5g
Take by weighing recipe quantity 2) each component in the carried medicine sustained-release layer, be dissolved in 95% alcoholic solution of about 600g and be prepared into medicinal liquid,
Take by weighing 3) the about 500g of each component of coatings, purified water, above adjuvant is mixed with coating solution,
Celphere is placed fluid bed, the control temperature of charge is 30-35 ℃, adjust fluidized state, the about 2h of time spent that adds medicine to, dry 10min after medicine-feeding finishes, pill sieves in the taking-up, sieve number 18-30 order, get on 30 orders 18 now part carry out packing of enteric coating, the dry 5-15min of continuation after coating is finished, take out
Survey the intermediate medicament contg, calculate loading according to the medicine specification, take by weighing, the micropill of making is incapsulated and get final product.
Tamsulosin hydrochloride slow releasing capsule (5000)
1) sucrose ball core 505g
2) carried medicine sustained-release layer
Tamsulosin hydrochloride 1g
Ethyl cellulose 101g
Sodium lauryl sulphate 7.5g
The ATBC(tributyl 2-acetylcitrate) 3.5g
3) coatings
Eudragit L100-55 9g
Sodium lauryl sulphate 7.5g
TEC 4g
4) Pulvis Talci 12g
Preparation method
Step 1: take by weighing each component by prescription, be dissolved in each component of carried medicine sustained-release layer approximately that 500g95% ethanol is mixed with upper drug solns, add medicine to fluid bed, 30-55 ℃ of control temperature of charge made pill,
Step 2: to the processing of sieving of upper pill, sieve number 15-30 order,
Step 3: get an approximately 550g dissolving coatings component of ethanol; Upper pill after sieving is placed in the fluid bed,, 45-55 ℃ of control temperature of charge, the dry 15min of continuation after coating is finished,
Step 4: with approximately 1/2 measuring the water that Pulvis Talci adds 3 times, spray into behind the high speed homogenization machine homogenize 10min, dry 5min takes out,
It is encapsulated that the micropill that step 5) prepares step 3 adds the 6g Pulvis Talci, and get final product.
Tamsulosin hydrochloride slow releasing capsule (5000)
1) sucrose ball core 660g
2) carried medicine sustained-release layer
Tamsulosin hydrochloride 10g
Sodium alginate 300g
3) coatings
Eudragit L100-55 10g
TEC 5g
4) micropowder silica gel 4g
Pulvis Talci 10g
Preparation method
Step 1: take by weighing each component by prescription, be dissolved in each component of carried medicine sustained-release layer approximately that 300g ethanol is mixed with upper drug solns, add medicine to fluid bed, 40-45 ℃ of control temperature of charge made pill,
Step 2: the water with 2 times of micropowder silica gel addings, spray into behind the high speed homogenization machine homogenize 5min, dry 5min takes out,
Step 3: to the processing of sieving of upper pill, sieve number 15-30 order,
Step 4: get an approximately 100g dissolving coatings component of ethanol; Upper pill after sieving is placed in the fluid bed,, 40-45 ℃ of control temperature of charge, the dry 10min of continuation after coating is finished,
Step 5: the water with 2 times of Pulvis Talci addings, spray into behind the high speed homogenization machine homogenize 5min, dry 5min takes out.Encapsulated, and get final product.
Tamsulosin hydrochloride slow releasing capsule (5000)
1) sucrose ball core 606g
2) carried medicine sustained-release layer
Tamsulosin hydrochloride 1g
Polyoxyethylene 270g
PEG400 40g
3) coatings
Eudragit L100-55 50g
Sodium lauryl sulphate 1g
TEC 5g
4) Pulvis Talci 18g
Micropowder silica gel 10g
Preparation method
Step 1: take by weighing each component by prescription, be dissolved in each component of carried medicine sustained-release layer approximately that 650g acetone is mixed with upper drug solns, add medicine to fluid bed, 30-35 ℃ of control temperature of charge made pill,
Step 2: the water with 2 times of micropowder silica gel addings, spray into behind the high speed homogenization machine homogenize 5min, dry 5min takes out,
Step 3: to the processing of sieving of upper pill, sieve number 15-30 order,
Step 4: get an approximately 550g dissolving coatings component of 70% ethanol; Upper pill after sieving is placed in the fluid bed,, 30-35 ℃ of control temperature of charge, the dry 15min of continuation after coating is finished,
Step 5: the water with 2 times of 8g Pulvis Talci addings, spray into behind the high speed homogenization machine homogenize 5min, dry 5min takes out,
It is encapsulated that the micropill that step 6) prepares step 3 adds the 10g micropowder silica gel, and get final product.
The accumulative releasing degree of each example
According to the above embodiments the present invention is described in detail.It should be noted that, above embodiment is just to illustrating the present invention.Under the prerequisite that does not depart from spirit of the present invention and essence, those skilled in the art can design multiple alternative of the present invention and improvement project, and it all should be understood to be within protection scope of the present invention.
Claims (10)
1. a Tamsulosin and pharmaceutically acceptable salt slow-release micro-pill thereof is characterized in that, according to weight ratio, described slow-release micro-pill chief component comprises:
1) celphere 60-95%
2) carried medicine sustained-release layer
Tamsulosin and pharmaceutically acceptable salt 0.1-10% thereof
The mixture of water-insoluble or swelling polymer or enteric material I or three's arbitrary proportion
1-30%
3) coatings
Enteric material II 0.5-10%
Wherein, can not be any in the mixture of described arbitrary proportion 2 be zero simultaneously.
2. slow-release micro-pill as claimed in claim 1 is characterized in that, according to weight ratio, described slow-release micro-pill chief component comprises:
1) celphere 60-95%
2) carried medicine sustained-release layer
Tamsulosin and pharmaceutically acceptable salt 0.1-1% thereof
The mixture of water-insoluble or swelling polymer or enteric material I or three's arbitrary proportion
1-30%
3) coatings
Enteric material II 0.5-10%.
3. slow-release micro-pill as claimed in claim 2, it is characterized in that, according to weight ratio, celphere 75-90% and/or, Tamsulosin and pharmaceutically acceptable salt 0.1-0.5% thereof and/or, the mixture of water-insoluble or swelling polymer or enteric material I or three's arbitrary proportion be 3-20% and/or, the enteric material II is 0.5-5%.
4. slow-release micro-pill as claimed in claim 3, it is characterized in that, in carried medicine sustained-release layer and/or the coatings, also comprise solubilizing agent and/or the plasticizer of 0.1-5% and/or the binding agent of 0.1-5% of 0.1-5%, described pastille micropill and coatings also comprise the antiplastering aid of 0.1-5%.
5. slow-release micro-pill claimed in claim 4 is characterized in that, bag the first sealing coat between celphere and the carried medicine sustained-release layer, and/or bag the second sealing coat between carried medicine sustained-release layer and the coatings.
6. such as each described slow-release micro-pill of claim 5, it is characterized in that, described celphere is the inert material preparation, can for water solublity or the water-insoluble adjuvant is made and/or, one or both of described insoluble polymer acrylic resin or cellulose derivative apoplexy due to endogenous wind and above mixture thereof and/or, one or both in described enteric material I and II acrylic resin or the cellulose acetate-phthalate (CAP) and above mixture thereof.
7. such as each described slow-release micro-pill of claim 1-6, it is characterized in that, described slow-release micro-pill mainly comprises according to weight ratio:
1) sucrose or microcrystalline Cellulose or lactose ball core 60-95%
2) carried medicine sustained-release layer
Tamsulosin and pharmaceutically acceptable salt 0.1-10% thereof
Ethyl cellulose or cellulose acetate or the mixture of strange RL/RS series or three's arbitrary proportion especially
1-30%
3) coatings
Strange RL/RS series 0.5-10% especially.
8. slow-release micro-pill as claimed in claim 7 is characterized in that,
1) sucrose or microcrystalline Cellulose or lactose ball core 60-95%
2) carried medicine sustained-release layer
Tamsulosin and pharmaceutically acceptable salt 0.1-1% thereof
Ethyl cellulose or cellulose acetate or the mixture of strange RL/RS series or three's arbitrary proportion especially
3-20%
Sodium lauryl sulphate or Tween 80 0.1-5%
3) coatings
Strange RL/RS series 0.5-10% especially.
9. such as each described slow-release micro-pill of claim 1-8, described Tamsulosin pharmaceutically acceptable salt is hydrochlorate.
10. preparation method such as each described slow-release micro-pill of claim 1-9, key step is as follows:
Step 1: take by weighing celphere, each component of carried medicine sustained-release layer by prescription, be dissolved in suitable solvent and be mixed with drug solns, add medicine to fluid bed, 30-55 ℃ of control temperature of charge made pill;
Step 2: to the processing of sieving of upper pill, sieve number 15-30 order;
Step 3: the upper pill after will sieving places in the fluid bed, further packs with the solution that contains enteric material for preparing in advance, and 30-55 ℃ of control temperature of charge, the dry 5-15min of continuation after coating is finished takes out, both.
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| CN103919735A (en) * | 2014-05-04 | 2014-07-16 | 翰宇药业（武汉）有限公司 | Tamsulosin hydrochloride sustained-release pellet 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 |
| CN114504560A (en) * | 2022-03-10 | 2022-05-17 | 河南省人民医院 | Tamsulosin hydrochloride sustained release preparation and preparation method thereof |
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| CN103919735A (en) * | 2014-05-04 | 2014-07-16 | 翰宇药业（武汉）有限公司 | Tamsulosin hydrochloride sustained-release pellet 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 |
| CN114504560A (en) * | 2022-03-10 | 2022-05-17 | 河南省人民医院 | Tamsulosin hydrochloride sustained release preparation and preparation method thereof |
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Application publication date: 20130925 |