CN102008451A - Method for preparing adhesive pellets by extrusion and spheronization - Google Patents

Method for preparing adhesive pellets by extrusion and spheronization Download PDF

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CN102008451A
CN102008451A CN2010105908984A CN201010590898A CN102008451A CN 102008451 A CN102008451 A CN 102008451A CN 2010105908984 A CN2010105908984 A CN 2010105908984A CN 201010590898 A CN201010590898 A CN 201010590898A CN 102008451 A CN102008451 A CN 102008451A
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microcrystalline cellulose
medicament
adhesive
medicine
filler
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CN102008451B (en
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关世侠
彭灿
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Guangzhou University of Chinese Medicine
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Guangzhou University of Chinese Medicine
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Abstract

The invention relates to a medicinal preparation characterized by a special physical shape, in particular to a method for preparing adhesive pellets by extrusion and spheronization, which comprises the following steps: (1) sieving a medicament and a filler with a 100-mesh sieve and uniformly mixing the medicament and the filler according to a medicament to filler weigh ratio of 1-2:10-30, adding an adhesive in an amount which is 0.5 to 30 times the weight of the added medicament to prepare a soft material, extruding, spheronizing, drying and sieving with a 24-to-40-mesh sieve, and obtaining the medicament-loaded pellets; or dissolving the medicament in the adhesive in an amount which is 0.5 to 30 times the weight of the medicament, adding the filler according to a medicament to filler weigh ratio of 1-2:10-30 to prepare the soft material, extruding spheronizing, drying and sieving with the 24-to-40-mesh sieve and obtaining the medicament-loaded pellets; and (2), placing the medicament-loaded pellets in a coating pan, adding powdered adhesive according to a medicament to adhesive weigh ratio of 1-2:10-20, wetting by spraying a proper amount of water or ethanol at concentration of 40 to 60 percent, coating the adhesive on the outer layer of the medicinal pellets at the temperature of 65 to 80 DEG C by a powder lamination coating process, placing the pellets in an oven at 40 DEG C and drying the pellets for 12 hours.

Description

The method that spheronization prepares adhesive pellet is extruded in a kind of employing
Technical field
The present invention relates to a kind ofly be shaped as the pharmaceutical product of feature, be specifically related to the adhesive pellet of site-specific delivery of drugs with specific physical.
Background technology
Micropill (piller) is meant that diameter is the coccoid peroral dosage form of 1~2.5mm.Adopt different prescriptions, micropill can be made rapid release, slow release or controlled release micro pill, it can directly use, but also capsule or be pressed into tablet and use.In recent years along with modern micropill preparation technology's development, the utilization of micropill aspect long-acting, controlled release preparation is more and more; The preparation method of micropill can be classified as following a few class substantially at present: extrude spheronization, centrifugal granulation, solution/suspension lamination method, powder lamination method, spray drying method, compacting spherical container shaping method, spheroidal crystal technology and high-speed stirred-coating pan pill method.Wherein, extrude-extrusion granulator is round as a ball after spheronization is utilized wet method system soft material, need make soft material flexible, make it to be easy to round as a ball globulate, its advantage is to need not to volatilize solvent, can prepare the consistent continuously rounding micropill of surface texture, and can reach the effect that postpones or modify release by adding one deck controlled release clothing layer.
Owing to be subjected to physiological effects such as gastric emptying, small intestinal transhipment in the processes such as medicine absorbs in vivo, distribution, metabolism, cause medicine in the too short defective that just is excreted of the diseased region time of staying, reduced bioavailability of medicament to a great extent.Patent Office of the People's Republic of China disclosed the patent application (publication number is CN 101700227A) of a kind of " matrine colon targeted adhesive pellet and preparation method thereof " on May 5th, 2010, and the preparation method of the matrine colon targeted adhesive pellet described in this patent application is made up of following steps:
1) takes by weighing matrine, filler and adhesive agent in proportion, cross 100 mesh sieve mix homogeneously, add suitable amount of adhesive and prepare soft material, put extruder with soft material and prepare micropill, dry 12h-24 under 40-60 ℃;
2) above-mentioned micropill is placed coating pan, take by weighing isolation coat wax material and antiplastering aid in proportion, adopt melt coating technology, repeatedly add wax material and antiplastering aid on a small quantity, the coating temperature is 55-80 ℃, coating pan rotating speed 20-50r/min;
3) with step 2) preparation micropill put in the coating tube, take by weighing macromolecule coating material, plasticizer, antiplastering aid, porogen and solvent in proportion, adopt the fluidized coating method: rotation speed of fan 20%-70%, the coating temperature is 20-60 ℃, inlet temperature is 20-70 ℃, atomizing pressure 0.2-08Mpa; Inclusion casing piller is placed 40 ℃ of baking ovens 24h that wears out.
The described method of above-mentioned patent application obtains micropill, though also have certain adhesive attraction, remain in following deficiency according to inventor's research: 1, adhesive agent and active ingredient are mixed and made into soft material, extruding-round as a ball-dry run in a large amount of heat releases and aquation disperse, the adhesion property and the toughness of obtained micropill significantly reduce; 2, the special adhesion that becomes behind the adhesive agent thermosol, the soft material surface forms many spines in extrusion, and the roundness of round as a ball back pill is also obviously relatively poor.
Summary of the invention
Technical problem to be solved by this invention provides a kind of improved spheronization of extruding, to improve the adhesive pellet adhesion characteristics.
The technical scheme that the present invention addresses the above problem is as follows:
The method that spheronization prepares adhesive pellet is extruded in a kind of employing, and this method is made up of following steps:
1, the method that spheronization prepares adhesive pellet is extruded in a kind of employing, and this method is made up of following steps:
(1) by medicine: the weight ratio of filler=1-2: 10-30 is crossed 100 mesh sieve mix homogeneously with medicine and filler, and the 0.5-30 binding agent doubly that adds drug weight is made soft material, through extrude, round as a ball and dry back crosses 24~40 mesh sieves, the medicine carrying micropill; Perhaps medicine is dissolved in behind the 0.5-30 binding agent doubly proportioning by medicine: filler=1-2: 10-30 and adds filler and make soft material, through extrude, round as a ball and dry back crosses 24~40 mesh sieves, the medicine carrying micropill;
(2) the medicine carrying micropill is placed coating pan, weight ratio by medicine: adhesive agent=1-2: 10-20 adds powdered adhesive agent, spray is the ethanol moistening of 40%-60% with suitable quantity of water or concentration, be 65 ℃~80 ℃ in temperature and adopt powder lamination coating method down, place 40 ℃ of dry 12h of baking oven to get final product at last at the outer parcel of medicament pellet adhesive agent;
In the above-mentioned steps,
Described filler is the mixture of microcrystalline Cellulose and lactose, or the mixture of microcrystalline Cellulose, lactose and starch; Binding agent is water or ethanol; Described adhesive agent is: the mixture of carbomer and microcrystalline Cellulose, the weight ratio of the two are carbomer: microcrystalline Cellulose=2-10: 90-98; The perhaps mixture of hypromellose and microcrystalline Cellulose, the weight ratio of the two is hypromellose: microcrystalline Cellulose=2-10: 90-98; The perhaps mixture of hypromellose, carbomer and microcrystalline Cellulose, three's weight ratio is a hypromellose: carbomer: microcrystalline Cellulose=2-5: 2-5: 90-96.
Medicine of the present invention can be various chemical drugss, also can be the dry powder of the extract of the water solublity of raw material of Chinese medicine or pure dissolubility.
Because the method for the invention adopts powder lamination coating method adhesive agent to be wrapped in the skin of medicament pellet, avoided dexterously adhesive agent extruding-round as a ball-dry run in a large amount of heat releases and aquation disperse, therefore compared with prior art adhesion property significantly improves, the obvious time of staying of prolong drug in gastrointestinal tract, and prepared micropill also has the good advantage of roundness.
The specific embodiment
Example 1
Present embodiment is a kind of preparation method of Hirudo adhesive pellet, and this method is as described below:
1) the dry powder 5g of water intaking trematodiasis extract, add microcrystalline Cellulose 145g and lactose 5g and adopt equivalent incremental method uniform mixing, cross 100 mesh sieves, adding 100mL water prepares soft material and places and extrude-spheronizator, extrude also round as a ball with the technological parameter of extruded velocity 20rpm, round as a ball speed 200rpm and round as a ball time 5min, dry 18h under 50 ℃ crosses 30 mesh sieves then, makes the micropill that is loaded with Hirudo.
2) the gained micropill is placed coating pan, add hypromellose 5g and the blended powder of microcrystalline Cellulose 95g, spray is with the suitable quantity of water moistening, employing powder lamination coating method on the micropill surface that is loaded with Hirudo, places 40 ℃ of dry 12h of baking oven promptly to get the Hirudo adhesive pellet described powder wrapped then under 70 ℃ condition.
Example 2
Present embodiment is a kind of preparation method of matrine adhesive pellet, and this method is as described below:
1) gets matrine 10g, add microcrystalline Cellulose 100g, lactose 5g and starch 5g, adopt equivalent incremental method uniform mixing, cross 100 mesh sieves, add 190mL water and prepare soft material and place and extrude-spheronizator, extrude and round as a ball, then at 50 ℃ of dry 20h down with the technological parameter of extruded velocity 25rpm, round as a ball speed 250rpm and round as a ball time 7min, cross 30 mesh sieves, make the micropill that is loaded with matrine.
2) the gained micropill is placed coating pan, add carbomer 3g and the blended powder of microcrystalline Cellulose 55g, spray is with the suitable quantity of water moistening, employing powder lamination coating method on the micropill surface that is loaded with matrine, places 40 ℃ of dry 12h of baking oven promptly to get the matrine adhesive pellet described powder wrapped then under 70 ℃ condition.
Example 3
Present embodiment is a kind of preparation method of metronidazole adhesive pellet, and this method is as described below:
1) gets metronidazole 7.5g, add microcrystalline Cellulose 95g, lactose 2.5g and starch 2.5g, adopt equivalent incremental method uniform mixing, cross 100 mesh sieves, add 75mL water and prepare soft material and place and extrude-spheronizator, extrude and round as a ball, then at 50 ℃ of dry 20h down with the technological parameter of extruded velocity 15rpm, round as a ball speed 150rpm and round as a ball time 3min, cross 30 mesh sieves, make the micropill that is loaded with metronidazole.
2) the gained micropill is placed coating pan, add hypromellose 2.5g, carbomer 2.5g and the blended powder of microcrystalline Cellulose 90g, spray is with the suitable quantity of water moistening, employing powder lamination coating method on the micropill surface that is loaded with metronidazole, places 40 ℃ of dry 12h of baking oven promptly to get the metronidazole adhesive pellet described powder wrapped then under 70 ℃ condition.
Example 4
Present embodiment is a kind of preparation method of ketoprofen adhesive pellet, and this method is as described below:
1) gets ketoprofen 3.5g, add microcrystalline Cellulose 90g, lactose 7.5g and starch 2.5g, adopt equivalent incremental method uniform mixing, cross 100 mesh sieves, add 105mL water and prepare soft material and place and extrude-spheronizator, extrude and round as a ball, then at 50 ℃ of dry 20h down with the technological parameter of extruded velocity 25rpm, round as a ball speed 150rpm and round as a ball time 10min, cross 30 mesh sieves, make the micropill that is loaded with ketoprofen.
2) the gained micropill is placed coating pan, add hypromellose 3g and the blended powder of microcrystalline Cellulose 65g, spray is with an amount of 40% ethanol moistening, employing powder lamination coating method on the micropill surface that is loaded with metronidazole, places 40 ℃ of dry 12h of baking oven promptly to get the metronidazole adhesive pellet described powder wrapped then under 70 ℃ condition.
Example 5
Present embodiment is a kind of preparation method of colchicine adhesive pellet, and this method is as described below:
1) gets colchicine 4.5g, be dissolved in the 85ml40% alcoholic solution; Take by weighing microcrystalline Cellulose 100g and lactose 10g in proportion, adopt equivalent incremental method uniform mixing, after crossing 100 mesh sieves, be mixed with soft material with the alcoholic solution of colchicine, place to extrude-spheronizator, extrude and round as a ball, then at 50 ℃ of dry 24h down with the technological parameter of extruded velocity 20rpm, round as a ball speed 200rpm and round as a ball time 6min, cross 30 mesh sieves, make the micropill that is loaded with colchicine.
2) the gained micropill is placed coating pan, add hypromellose 4g and the blended powder of microcrystalline Cellulose 76g, spray is with an amount of 40% ethanol moistening, employing powder lamination coating method on the micropill surface that is loaded with colchicine, places 40 ℃ of dry 12h of baking oven promptly to get the colchicine adhesive pellet described powder wrapped then under 60 ℃ condition.
Example 6
Present embodiment is a kind of preparation method of doxycycline hydrochloride adhesive pellet, and this method is as described below:
1) gets doxycycline hydrochloride 3.5g, be dissolved in the 105ml40% alcoholic solution; Take by weighing microcrystalline Cellulose 80g, lactose 5g and starch 15g in proportion, adopt equivalent incremental method uniform mixing, after crossing 100 mesh sieves, be mixed with soft material with the alcoholic solution of doxycycline hydrochloride, place to extrude-spheronizator, extrude and round as a ball, then at 65 ℃ of dry 24h down with the technological parameter of extruded velocity 15rpm, round as a ball speed 250rpm and round as a ball time 4min, cross 30 mesh sieves, make the micropill that is loaded with doxycycline hydrochloride.
2) the gained micropill is placed coating pan, add hypromellose 2g and the blended powder of microcrystalline Cellulose 58g, spray is with an amount of 40% ethanol moistening, employing powder lamination coating method on the micropill surface that is loaded with doxycycline hydrochloride, places 40 ℃ of dry 12h of baking oven promptly to get the doxycycline hydrochloride adhesive pellet described powder wrapped then under 60 ℃ condition.
Example 7
Present embodiment is a kind of preparation method of glipizide adhesive pellet, and this method is as described below:
1) gets glipizide 5g, be dissolved in the 110ml water; Take by weighing microcrystalline Cellulose 90g, lactose 5g and starch 5g in proportion, adopt equivalent incremental method uniform mixing, after crossing 100 mesh sieves, prepare soft material with the aqueous solution of glipizide, place to extrude-spheronizator, extrude and round as a ball, then at 65 ℃ of dry 24h down with the technological parameter of extruded velocity 25rpm, round as a ball speed 350rpm and round as a ball time 6min, cross 30 mesh sieves, make the micropill that is loaded with glipizide.
2) the gained micropill is placed coating pan, add hypromellose 5g and the blended powder of microcrystalline Cellulose 90g, spray is with the suitable quantity of water moistening, employing powder lamination coating method on the micropill surface that is loaded with glipizide, places 40 ℃ of dry 12h of baking oven promptly to get the glipizide adhesive pellet described powder wrapped then under 60 ℃ condition.
Example 8
Present embodiment is a kind of preparation method of nifedipine adhesive pellet, and this method is as described below:
1) gets nifedipine 5g, add microcrystalline Cellulose 115g and lactose 5g and adopt equivalent incremental method uniform mixing, cross 100 mesh sieves, adding the 55mL40% alcoholic solution prepares soft material and places and extrude-spheronizator, extrude also round as a ball with the technological parameter of extruded velocity 20rpm, round as a ball speed 200rpm and round as a ball time 5min, dry 18h under 50 ℃ crosses 30 mesh sieves then, makes the micropill that is loaded with nifedipine.
2) the gained micropill is placed coating pan, add hypromellose 3.5g and the blended powder of microcrystalline Cellulose 35g, spray is with an amount of 40% ethanol moistening, employing powder lamination coating method on the micropill surface that is loaded with nifedipine, places 40 ℃ of dry 12h of baking oven promptly to get the nifedipine adhesive pellet described powder wrapped then under 70 ℃ condition.
Example 9
Present embodiment is a kind of preparation method of nimodipine adhesive pellet, and this method is as described below:
1) gets nimodipine 7.5g, add microcrystalline Cellulose 100g, lactose 5g and starch 3g, adopt equivalent incremental method uniform mixing, cross 100 mesh sieves, add the 105mL40% alcoholic solution and prepare soft material and place and extrude-spheronizator, extrude and round as a ball, then at 50 ℃ of dry 18h down with the technological parameter of extruded velocity 20rpm, round as a ball speed 250rpm and round as a ball time 8min, cross 30 mesh sieves, make the micropill that is loaded with nimodipine.
2) the gained micropill is placed coating pan, add hypromellose 4.5g and the blended powder of microcrystalline Cellulose 96g, spray is with an amount of 50% ethanol moistening, employing powder lamination coating method on the micropill surface that is loaded with nimodipine, places 40 ℃ of dry 12h of baking oven promptly to get the nimodipine adhesive pellet described powder wrapped then under 70 ℃ condition.
Example 10
Present embodiment is a kind of preparation method of aminosallcylic acid adhesive pellet, and this method is as described below:
1) gets aminosallcylic acid 8g, add microcrystalline Cellulose 90g, lactose 6g and starch 3g, adopt equivalent incremental method uniform mixing, cross 100 mesh sieves, add 80mL water and prepare soft material and place and extrude-spheronizator, extrude and round as a ball, then at 50 ℃ of dry 18h down with the technological parameter of extruded velocity 20rpm, round as a ball speed 300rpm and round as a ball time 12min, cross 30 mesh sieves, make the micropill that is loaded with aminosallcylic acid.
2) the gained micropill is placed coating pan, add hypromellose 2g, carbomer 2.5g and the blended powder of microcrystalline Cellulose 80g, spray is with an amount of 60% ethanol moistening, employing powder lamination coating method on the micropill surface that is loaded with aminosallcylic acid, places 40 ℃ of dry 12h of baking oven promptly to get the aminosallcylic acid adhesive pellet described powder wrapped then under 70 ℃ condition.
Example 11
Present embodiment is for adopting the effect example of the made adhesive pellet of the inventive method.According to document A novel in situ methodto test polymers and coated microparticles for bioadhesion (Int J Pharm, 1989,52 (3): 265~270) adhesion property of the relevant micropill of Jie Shaoing is investigated and treatise novel pharmaceutical formulation and new technique (People's Health Publisher, the micropill roundness assay method of 2005:460-461) addressing, can adopt the peaceful boundary's stability method that faces of the adhesion method that exsomatizes respectively the adhesiveness and the roundness of micropill to be tested, the concrete method of inspection is as described below.
1 is subjected to the reagent product:
Be subjected to reagent product 1: get the prepared Hirudo adhesive pellet of the foregoing description 1.
Be subjected to reagent product 2: get the prepared matrine adhesive pellet of the foregoing description 2.
Be subjected to reagent product 3: get the prepared metronidazole adhesive pellet of the foregoing description 3.
Be subjected to reagent product 4: adopt traditional prepared Hirudo adhesive pellet of round as a ball+solution/suspension lamination method of extruding, its preparation method is as described below:
Take by weighing the dry powder 5g of Hirudo extract, add microcrystalline Cellulose 100g and lactose 5g and adopt equivalent incremental method uniform mixing, cross 100 mesh sieves, adding 100mL water prepares soft material and places and extrude-spheronizator, extrude also round as a ball with the technological parameter of extruded velocity 20rpm, round as a ball speed 200rpm and round as a ball time 5min, dry 18h under 50 ℃ crosses 30 mesh sieves then, makes the micropill that is loaded with Hirudo.Take by weighing hypromellose 5g, be dissolved in the 100ml water and make dispersion liquid, utilize coating pan slowly spraying under 60-85 ℃ of temperature, make it evenly to be wrapped in medicine carrying micropill surface, 40 ℃ of dry 12h cross the 24-40 mesh sieve, make the Hirudo adhesive pellet.
Be subjected to reagent product 5: adopt traditional prepared Hirudo adhesive pellet of spheronization of extruding, its preparation method is as described below:
Take by weighing Hirudo extract dry powder 5g, microcrystalline Cellulose 100g, lactose 5g and hypromellose 5g in proportion, according to equivalent incremental method uniform mixing, with water is binding agent, make routinely and do wet moderate soft material and place and extrude-spheronizator, extrude also round as a ball with the technological parameter of extruded velocity 20rpm, round as a ball speed 200rpm and round as a ball time 5min, cross the 24-40 mesh sieve, 40 ℃ of-60 ℃ of dry 12h make the Hirudo adhesive pellet.
Be subjected to reagent product 6: adopt traditional prepared matrine adhesive pellet of round as a ball+solution/suspension lamination method of extruding, its preparation method is as described below:
Take by weighing matrine 10g, add microcrystalline Cellulose 100g, lactose 5g and starch 5g, adopt equivalent incremental method uniform mixing, cross 100 mesh sieves, add 90mL water and prepare soft material and place and extrude-spheronizator, extrude and round as a ball, then at 50 ℃ of dry 20h down with the technological parameter of extruded velocity 25rpm, round as a ball speed 250rpm and round as a ball time 7min, cross 30 mesh sieves, make the micropill that is loaded with matrine.Take by weighing carbomer 3g, be dissolved in the 100ml water and make dispersion liquid, utilize coating pan slowly spraying under 60-85 ℃ of temperature, make it evenly to be wrapped in medicine carrying micropill surface, 70 ℃ of dry 12h cross the 24-40 mesh sieve, make the matrine adhesive pellet.
Be subjected to reagent product 7: adopt traditional prepared metronidazole adhesive pellet of spheronization of extruding, its preparation method is as described below:
Take by weighing metronidazole 7.5g, microcrystalline Cellulose 95g, lactose 2.5g, starch 2.5g and carbomer 2.5g in proportion, according to equivalent incremental method uniform mixing, with water is binding agent, make routinely and do wet moderate soft material and place and extrude-spheronizator, extrude also round as a ball with the technological parameter of extruded velocity 15rpm, round as a ball speed 150rpm and round as a ball time 3min, cross the 24-40 mesh sieve, 40 ℃ of dry 12h make the metronidazole adhesive pellet.
2 experimental techniques
Adhesion method is measured the stripped adhesiveness that respectively is subjected to the reagent product 2.1 exsomatize
Get 35 of 200g left and right sides SD rats, male and female all can, be divided into experimental group 1, experimental group 2, experimental group 3, matched group 1, matched group 2, matched group 3 and matched group 4 at random by 5 every group, and give above-mentioned reagent product 1~7 adhesiveness that exsomatizes as follows that is subjected to successively and test.
Respectively 35 SD rats are put to death and take out small intestinals, vertically cut off, wash out content, be fixed on the polyethylene tube of vertical incision with the phosphate buffer of pH7.80.Get above-mentioned each 50 of the reagent product that are subjected to, evenly be layered on the rat small intestine mucosa, polyethylene tube places in 20 ℃ of exsiccators that saturated KNO3 is housed, place and to make the abundant aquation of micropill behind the 30min and interact with mucous membrane of small intestine, then polyethylene tube is taken out and tilt 45 °, with the phosphate buffer flushing rat small intestine mucosa 5min (constant flow pump drives, and flow velocity is about 20mlmin-1) of pH 7.80, counting is trapped in the micropill number on the rat small intestine mucosa, calculates its stripped adhesiveness.
Figure BDA0000038599770000071
In the formula: n 1---the micropill sum; n 2---the flushing 5min after on mucous membrane of small intestine observed micropill number.
To record the resulting adhesion percentage rate of each group experiment is recorded in the following table 1.
2.2 plane marginal stability method is measured the stripped adhesiveness that respectively is subjected to the reagent product
Take by weighing the above-mentioned experiment medicine that is subjected to reagent product 1~3 each 15g as experimental group 1~3, take by weighing above-mentioned reagent product 4~7 each 15g that are subjected to again and organize 1~4 experiment medicine in contrast.The experiment medicine of each group is placed on the smooth plates, then a dull and stereotyped side is lifted, measure at micropill begin to roll top rake plane and the formed angle of horizontal plane (φ), this angle is more little, shows that the micropill roundness is good more.Record each micropill and begin to roll behind top rake plane and the formed angle of horizontal plane (φ), be weighted mean deviation by group and be recorded in following table 1.
3. result
Table 1
Figure BDA0000038599770000072
Have data shown in the table of going up to compare with matched group as can be seen, utilize the adhesive pellet of this patent method preparation, its stripped adhesion rate is up to more than 90%, and roundness also has tangible improvement.Observe from experimental result, utilize the adhesive pellet of traditional method preparation, its stripped adhesion property and roundness are all not very good, and the present invention can effectively improve the quality of micropill, is suitable for Application and Development.

Claims (2)

1. the method that spheronization prepares adhesive pellet is extruded in an employing, and this method is made up of following steps:
(1) by medicine: the weight ratio of filler=1-2: 10-30 is crossed 100 mesh sieve mix homogeneously with medicine and filler, and the 0.5-30 binding agent doubly that adds drug weight is made soft material, through extrude, round as a ball and dry back crosses 24~40 mesh sieves, the medicine carrying micropill; Perhaps
Medicine is dissolved in behind the 0.5-30 binding agent doubly proportioning by medicine: filler=1-2: 10-30 adds filler and make soft material, through extrude, round as a ball and dry back crosses 24~40 mesh sieves, the medicine carrying micropill;
(2) the medicine carrying micropill is placed coating pan, weight ratio by medicine: adhesive agent=1-2: 10-20 adds powdered adhesive agent, spray is the ethanol moistening of 40%-60% with suitable quantity of water or concentration, be 65 ℃~80 ℃ in temperature and adopt powder lamination coating method down, place 40 ℃ of dry 12h of baking oven to get final product at last at the outer parcel of medicament pellet adhesive agent;
In the above-mentioned steps,
Described filler is the mixture of microcrystalline Cellulose and lactose, or the mixture of microcrystalline Cellulose, lactose and starch; Binding agent is water or ethanol; Described adhesive agent is: the mixture of carbomer and microcrystalline Cellulose, the weight ratio of the two are carbomer: microcrystalline Cellulose=2-10: 90-98; Or the mixture of hypromellose and microcrystalline Cellulose, the weight ratio of the two is hypromellose: microcrystalline Cellulose=2-10: 90-98; Or the mixture of hypromellose, carbomer and microcrystalline Cellulose, three's weight ratio is a hypromellose: carbomer: microcrystalline Cellulose=2-5: 2-5: 90-96.
2. the method that spheronization prepares adhesive pellet is extruded in a kind of employing according to claim 1, it is characterized in that, described medicine is the dry powder of the extract of the water solublity of chemical drugs or raw material of Chinese medicine or pure dissolubility.
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CN103211780A (en) * 2013-04-17 2013-07-24 沈阳药科大学 Oral mesalazine colon-specific adhesive pellet
CN105902500A (en) * 2016-04-27 2016-08-31 上海理工大学 Mesalazine enteric positioned controlled-release preparation and preparation method thereof
CN107019680A (en) * 2017-04-11 2017-08-08 珠海润都制药股份有限公司 A kind of preparation technology of sodium rabeprazole enteric-coated capsule
CN111436648A (en) * 2019-01-16 2020-07-24 深圳波顿香料有限公司 Preparation method of pellet for cigarette and application of pellet in cigarette filter

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CN101700227A (en) * 2009-09-27 2010-05-05 宁夏医科大学 Matrine colon targeted adhesive pellet and preparation method thereof

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WO2008010690A1 (en) * 2006-07-21 2008-01-24 Handok Pharmaceuticals Co., Ltd. Gastric retention-type pellet and the preparation method thereof
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Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103211780A (en) * 2013-04-17 2013-07-24 沈阳药科大学 Oral mesalazine colon-specific adhesive pellet
CN103211780B (en) * 2013-04-17 2015-10-14 沈阳药科大学 Oral mesalazine colon-specific adhesive pellet
CN105902500A (en) * 2016-04-27 2016-08-31 上海理工大学 Mesalazine enteric positioned controlled-release preparation and preparation method thereof
CN105902500B (en) * 2016-04-27 2019-11-29 上海理工大学 A kind of mesalazine enteric positioning controlled-release preparation and preparation method thereof
CN107019680A (en) * 2017-04-11 2017-08-08 珠海润都制药股份有限公司 A kind of preparation technology of sodium rabeprazole enteric-coated capsule
CN107019680B (en) * 2017-04-11 2019-03-05 珠海润都制药股份有限公司 A kind of preparation process of sodium rabeprazole enteric-coated capsule
CN111436648A (en) * 2019-01-16 2020-07-24 深圳波顿香料有限公司 Preparation method of pellet for cigarette and application of pellet in cigarette filter

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