CN1554362A - Compound slow-release Anfennamin micro pill and preparing method - Google Patents
Compound slow-release Anfennamin micro pill and preparing method Download PDFInfo
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- CN1554362A CN1554362A CNA2003101193785A CN200310119378A CN1554362A CN 1554362 A CN1554362 A CN 1554362A CN A2003101193785 A CNA2003101193785 A CN A2003101193785A CN 200310119378 A CN200310119378 A CN 200310119378A CN 1554362 A CN1554362 A CN 1554362A
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Abstract
The compound slow-releasing Anfennamin micro pill consists of medicine core comprising acetaminophenol, Chlorpheniramine, caffeine, artificial bezoar; fixed isolating film; outer slow releasing coating; mixed anti-sticking agent, plasticizer and lubricant capsulized. The slow releasing agent can reduce the medicine taking time number effectively, and has medicine releasing characteristic not affected by the pH value in gastrointestinal tract. The present invention results in stable blood medicine concentration, reduced toxic side effect and raised patient's compliance.
Description
Technical field:
The present invention relates to a kind of preparation method of compound paracetamol and chlorphenamine maleate slow-release micro-pill.
Background technology:
Adopt acetaminophen; caffeine; chlorphenamine maleate; the electuary of the treatment flu that artificial Calculus Bovis's compositions is made; capsule; be listed in national nonprescription drugs range of management; but be between 3～4 hours because the active component biological half-life in the said composition is short; the oral administration post-absorption is fast; therefore; eliminate also fast in vivo; in order to keep effective blood drug level; need day three balance administrations of clothes; so promptly produced the blood drug level peak valley phenomenon; thereby; just produced significantly untoward reaction, therefore, the research slow releasing preparation can solve the deficiency that above preparation exists effectively; also be to satisfy clinical needs simultaneously, more effective; it more safely is the extensive patients service.
Summary of the invention:
The object of the present invention is to provide a kind of compound paracetamol and chlorphenamine maleate slow-release micro-pill and preparation method, it is by using the ethylcellulose aqueous dispersion or using " Youteqi " EudragitRS and RL coats the surface of compound paracetamol and chlorphenamine maleate pill as slow-release material, this coated micropill medicine that influences that acid and alkali alkali changes in release medium slowly releases from the film formed space of slow release, and by regulating thickness, slowly blend and ooze material soon and regulate drug release rate, thereby obtain good release curve and repeatability, the compound paracetamol and chlorphenamine maleate slow-release micro-pill of stability, and provide a kind of technology simple, easy operating has preparation technology's method of fine controllability.
What the present invention includes effective active components acetaminophen, chlorphenamine maleate, caffeine, artificial Calculus Bovis contains pill core and fixed layer isolating membrane, and outer sustained release coating film mixes antiplastering aid, plasticizer and lubricant and carries out the capsule fill and constitute; The pill that is become directly is 0.6mm～0.9mm; Fixed layer isolating membrane weightening finish 2～5%: outer sustained release coating film weightening finish 3%～8%; Lubricant 1～2%.
The described pill core weight that contains is formed:
Acetaminophen 50%～80%
Chlorphenamine maleate 0.5%～5%
The artificial Calculus Bovis 1%～10%.
Described coating membrane weight is formed:
The ethylcellulose aqueous dispersion; Or
10%～20% alcoholic solution slow-release material: the mixture of polypropylene acid resin
Antiplastering aid 20～30%/slow-release material
What the filmogen of described fixed layer isolating membrane adopted is that kinematic viscosity is the hypromellose of 5～50 centipoises.
Described outer sustained release coating membrane material polypropylene acid resin mixture is an EudragitRS:EudragitRL weight ratio 1～3: 1.
Described antiplastering aid is a Pulvis Talci.
Described lubricant is Pulvis Talci or micropowder silica gel.
Described plasticizer is phthalic acid diethyl ester, Fructus Citri Limoniae triethylenetetraminehexaacetic acid fat or Polyethylene Glycol-6000.
The preparation method of compound paracetamol and chlorphenamine maleate slow-release micro-pill comprises the steps:
System pastille pill: get the acetaminophen of metering, chlorphenamine maleate, caffeine, artificial Calculus Bovis, sustained-release matrix material, binding agent, mix homogeneously; Put in the fluid bed with the dehydrated alcohol be lubricant at next step system pastille pill of atomize, again the piller that makes is sieved to such an extent that be the finished product ball between 0.6mm～0.9mm.
The fixed layer isolating membrane: with kinematic viscosity is that the hypromellose of 5～50 centipoises is dissolved in pure water (1～3: 1～3) in the mixed solvent, concentration is 5～25%, using the coating method setting inlet temperature of spray of fluid bed tangent line or end spray is 50 ℃～60 ℃, air intake air-flow relative humidity is 40%～70%, the spray gun atomizing pressure is 2～4bar, and air inflow is 3000～4000m
3/ h, hydrojet speed 100～240g/min.Operating process at first with the pill preheating, is treated to begin coating after temperature of charge reaches 35 ℃～45 ℃, coating weightening finish 2～5%, and coating finishes the back material in fluid bed inner drying 10 minutes, discharging.
The outer release membranes clothing that coats:
(1): slow-release material is the ethylcellulose aqueous dispersion
Using the coating method setting inlet temperature of spray of fluid bed tangent line or end spray is 50 ℃～60 ℃, and air intake air-flow relative humidity is 40%～70%, and the spray gun atomizing pressure is 2～4bar, and air inflow is 3000～4000m
3/ h, hydrojet speed 100～240g/min are in pill: it is that 100: 3～8 ratio coats the outer release membranes of pill, i.e. pill weightening finish 3%～8% that ethyl cellulose contains the thing gross weight admittedly.
Operating process: at first with the pill preheating, treat to begin coating after temperature of charge reaches 35 ℃～45 ℃, constantly stir sustained release coating liquid in the coating process, coating finishes the back material fluid bed inner drying 10 minutes, discharging adds 1～2% Pulvis Talci or micropowder silica gel mix homogeneously again; The finished product pill placed in the hothouse to place naturally got final product in 12 hours; Or
(2): slow-release material is a polypropylene acid resin mixture
Polypropylene acid resin mixture with " Youteqi " EudragitRS:RL weight ratio 3～1: 1 is dissolved in 95% ethanol earlier, fully dissolving, and configuration concentration is 10%～20% polypropylene acid resin alcoholic solution.
Slowly add plasticizer and 20～30% antiplastering aids that are equivalent to " Youteqi " EudragitRS and RL polypropylene acid resin slow-release material weight 6～15%, add concentration 95% ethanol again and be 10～25 times of solid content and fully stir and get final product;
Using the coating method setting inlet temperature of spray of fluid bed tangent line or end spray is 50 ℃～60 ℃, and air intake air-flow relative humidity is 40%～70%, and the spray gun atomizing pressure is 2～4bar, and air inflow is 3000～4000m
3/ h, hydrojet speed 100～240g/min are in pill: it is that 100: 3～8 ratio coats the outer release membranes of pill, i.e. pill weightening finish 3%～8% that polypropylene acid resin mixture contains the thing gross weight admittedly.
Operating process: at first with the pill preheating, treat to begin coating after temperature of charge reaches 35 ℃～45 ℃, constantly stir sustained release coating liquid in the coating process, coating finishes the back material fluid bed inner drying 10 minutes, discharging adds 1～2% Pulvis Talci or micronization silica gel mix homogeneously again; The finished product pill placed in the hothouse to place naturally to solidify in 12 hours get final product.
Advantage of the present invention: utilize advanced micropill slow-release material packaging technique to make the compound paracetamol and chlorphenamine maleate slow-release micro-pill, thereby make each capsule form hundreds of unit that slowly discharge and stopped the whole release wild effect that causes because of instabilities individually, just solved and made the existing defective of tablet.And this product can effectively reduce medicining times, takes twice every day, each two.Its drug release feature is not subjected to the variable effect of gastrointestinal pH, through to constant speed release medicine in this product of mensuration of preparation release in vitro degree 1～10 hour, blood drug level is steady, thereby has reduced the toxic and side effects after taking medicine effectively, improve patient's compliance, be fit to the needs of clinical application development.
Description of drawings:
Fig. 1, for compound paracetamol and chlorphenamine maleate slow-release micro-pill embodiment 1 release profiles of the present invention.
The specific embodiment
Contain pill core:
Acetaminophen 112.5kg
Chlorphenamine maleate 1.35kg
Caffeine 6.75kg
Artificial Calculus Bovis 4.5kg
The above-mentioned pill core 10kg that contains
Sulisi (ethylcellulose aqueous dispersion) 1.6kg
Preparation technology: (use B-5L multifunction granulating coating machine, Chongqing spacious mansion pharmaceutical machine company limited is produced)
1. slow-release material is the ethylcellulose aqueous dispersion.
2. use the coating method of spray of fluid bed tangent line or end spray, setting inlet temperature is 50 ℃～60 ℃, and air intake air-flow relative humidity is 40%～70%, and the spray gun atomizing pressure is 2～4bar, and air inflow is 3000～4000m
3/ h, hydrojet speed 100～240g/min are in pill: it is that 100: 5 ratio coats the outer release membranes of pill, i.e. pill weightening finish 5% that ethyl cellulose contains the thing gross weight admittedly.
Operating process:
At first with the pill preheating, treat to begin coating after temperature of charge reaches 35 ℃～45 ℃, constantly stir sustained release coating liquid in the coating process, coating finishes the back material fluid bed inner drying 10 minutes, and discharging adds 2% Pulvis Talci mix homogeneously again.
3. solidify: the finished product pill is placed to place naturally in the hothouse got final product in 12 hours.
The prescription that contains pill core 5kg sustained release coating liquid:
Eudragit RS (Youteqi) 0.2kg
Eudragit RL (Youteqi) 0.1kg
Pulvis Talci 0.06kg
Phthalic acid diethyl ester 0.035kg
Ethanol (95%v/v) 4.45kg
Preparation method:
1. earlier " Youteqi " EudragitRS:EudragitRL polypropylene acid resin mixture is dissolved in 95% ethanol, fully dissolving.
2. slowly add phthalic acid diethyl ester plasticizer and Pulvis Talci antiplastering aid, add concentration 95% ethanol again, stir by recipe quantity.
3. use the coating method of spray of fluid bed tangent line or end spray, setting inlet temperature is 50 ℃～60 ℃, and air intake air-flow relative humidity is 40%～70%, and the spray gun atomizing pressure is 2～4bar, and air inflow is 3000～4000m
3/ h, hydrojet speed 100～240g/min.
Operating process is at first with the pill preheating, treat to begin coating after temperature of charge reaches 35 ℃～45 ℃, constantly stir sustained release coating liquid in the coating process, coating finishes the back material fluid bed inner drying 10 minutes, discharging adds 2% Pulvis Talci or micropowder silica gel mix homogeneously again.
4. solidify: the finished product pill is placed to place naturally in the hothouse got final product in 12 hours.
Table 1:0～12 hour cumulative release (%)
| | Acetaminophen | Caffeine | It is quick to pounce on youngster |
| ????0 | ????0 | ????0 | ????0 |
| ????1 | ????15.33 | ????17.73 | ????12 |
| ????2 | ????33.63 | ????34.54 | ????20.99 |
| ????3 | ????49.81 | ????47.01 | ????33.66 |
| ????4 | ????63.38 | ????58.98 | ????48 |
| ????5 | ????69.68 | ????71.97 | ????58.49 |
| ????6 | ????91.75 | ????86.03 | ????72.72 |
| ????8 | ????100.1 | ????103.93 | ????85 |
| ????10 | ????101.2 | ????102.28 | ????95.18 |
| ????12 | ????102 | ????103.55 | ????101.42 |
Claims (7)
1, a kind of compound paracetamol and chlorphenamine maleate slow-release micro-pill, it is characterized in that it comprises that effective active components acetaminophen, chlorphenamine maleate, caffeine and artificial Calculus Bovis's contains pill core and fixed layer isolating membrane, outer sustained release coating film mixes antiplastering aid, plasticizer and lubricant and carries out capsule fill formation; The pill that is become directly is 0.6mm～0.9mm; Fixed layer isolating membrane weightening finish 2～5%; Outer sustained release coating film weightening finish 3%～8%; Lubricant 1～2%;
The described pill core weight that contains is formed:
Acetaminophen 50%～80%
Caffeine 10%～40%
Chlorphenamine maleate 0.5%～5%
The artificial Calculus Bovis 1%～10%
Described coating membrane weight is formed:
The ethylcellulose aqueous dispersion; Or
10%～20% alcoholic solution slow-release material: the mixture of polypropylene acid resin
Antiplastering aid 20～30%/slow-release material
Plasticizer 6～15%/slow-release material.
2, according to the described compound paracetamol and chlorphenamine maleate slow-release micro-pill of claim 1, what it is characterized in that the filmogen of described fixed layer isolating membrane adopts is that kinematic viscosity is the hypromellose of 5～50 centipoises.
3,, it is characterized in that described outer sustained release coating membrane material polypropylene acid resin mixture is EudragitRS: EudragitRL weight ratio 1～3: 1 according to the described compound paracetamol and chlorphenamine maleate slow-release micro-pill of claim 1.
4,, it is characterized in that described antiplastering aid is a Pulvis Talci according to the described compound paracetamol and chlorphenamine maleate slow-release micro-pill of claim 1.
5, according to the described compound paracetamol and chlorphenamine maleate slow-release micro-pill of claim 1, it is characterized in that described lubricant Pulvis Talci or micropowder silica gel.
6,, it is characterized in that described plasticizer is phthalic acid diethyl ester, Fructus Citri Limoniae triethylenetetraminehexaacetic acid fat or Polyethylene Glycol-6000 according to the described compound paracetamol and chlorphenamine maleate slow-release micro-pill of claim 1.
7, the preparation method of the described compound paracetamol and chlorphenamine maleate slow-release micro-pill of claim 1 is characterized in that it comprises the steps:
System pastille pill: get the acetaminophen of metering, chlorphenamine maleate, caffeine, artificial Calculus Bovis, sustained-release matrix material, binding agent, mix homogeneously; Put in the fluid bed with the dehydrated alcohol be wetting agent at next step system pastille pill of atomize, again the piller that makes is sieved to such an extent that be the finished product ball between 0.6mm～0.9mm;
The fixed layer isolating membrane: with kinematic viscosity is the pure water (1～3: 1～3) in the mixed solvent that the hypromellose of 5～50 centipoises is dissolved in, concentration is 5～25%, using the coating method setting inlet temperature of spray of fluid bed tangent line or end spray is 50 ℃～60 ℃, air intake air-flow relative humidity is 40%～70%, the spray gun atomizing pressure is 2～4bar, and air inflow is 3000～4000m
3/ h, hydrojet speed 100～240g/min.Operating process at first with the pill preheating, is treated to begin coating after temperature of charge reaches 35 ℃～45 ℃, coating weightening finish 2～5%, and coating finishes the back material in fluid bed inner drying 10 minutes, discharging;
The outer release membranes clothing that coats:
(1): slow-release material is the ethylcellulose aqueous dispersion
Using the coating method setting inlet temperature of spray of fluid bed tangent line or end spray is 50 ℃～60 ℃, and air intake air-flow relative humidity is 40%～70%, and the spray gun atomizing pressure is 2～4bar, and air inflow is 3000～4000m
3/ h, hydrojet speed 100～240g/min are in pill: it is that 100: 3～8 ratio coats the outer release membranes of pill, i.e. pill weightening finish 3%～8% that ethyl cellulose contains the thing gross weight admittedly;
Operating process: at first with the pill preheating, treat to begin coating after temperature of charge reaches 35 ℃～45 ℃, constantly stir sustained release coating liquid in the coating process, coating finishes the back material fluid bed inner drying 10 minutes, discharging adds 1～2% Pulvis Talci or silica gel mix homogeneously again; The finished product pill placed in the hothouse to place naturally got final product in 12 hours; Or
(2): slow-release material is a polypropylene acid resin mixture
Polypropylene acid resin mixture with " Youteqi " EudragitRS:EudragitRL weight ratio 3～1: 1 is dissolved in 95% ethanol earlier, fully dissolving, and configuration concentration is 10%～20% polypropylene acid resin alcoholic solution;
Slowly add plasticizer and 20～30% antiplastering aids that are equivalent to " Youteqi " EudragitRS and RL polypropylene acid resin slow-release material weight 6～15%, add concentration 95% ethanol again and be 10～25 times of solid content and fully stir and get final product;
Using the coating method setting inlet temperature of spray of fluid bed tangent line or end spray is 50 ℃～60 ℃, and air intake air-flow relative humidity is 40%～70%, and the spray gun atomizing pressure is 2～4bar, and air inflow is 3000～4000m
3/ h, hydrojet speed 100～240g/min are in pill: it is that 100: 3～8 ratio coats the outer release membranes of pill, i.e. pill weightening finish 3%～8% that polypropylene acid resin mixture contains the thing gross weight admittedly;
Operating process: at first with the pill preheating, treat to begin coating after temperature of charge reaches 35 ℃～45 ℃, constantly stir sustained release coating liquid in the coating process, coating finishes the back material fluid bed inner drying 10 minutes, discharging adds 1～2% Pulvis Talci or micropowder silica gel mix homogeneously again; The finished product pill placed in the hothouse to place naturally to solidify in 12 hours get final product.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2003101193785A CN1554362A (en) | 2003-12-24 | 2003-12-24 | Compound slow-release Anfennamin micro pill and preparing method |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2003101193785A CN1554362A (en) | 2003-12-24 | 2003-12-24 | Compound slow-release Anfennamin micro pill and preparing method |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102614220A (en) * | 2012-04-14 | 2012-08-01 | 辽宁王牌速效制药有限公司 | Preparing method of paracetamol, caffein, atificial cow-bezoar and chlorphenamine maleate capsule content functional pellet |
| CN103156855A (en) * | 2013-03-21 | 2013-06-19 | 青岛正大海尔制药有限公司 | Paracetamol and caffeine slow-release capsule and preparation method thereof |
| CN105250240A (en) * | 2015-08-25 | 2016-01-20 | 江苏先科药业有限公司 | Oral sustained-release preparation containing hydrocodone and chlorpheniramine |
-
2003
- 2003-12-24 CN CNA2003101193785A patent/CN1554362A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102614220A (en) * | 2012-04-14 | 2012-08-01 | 辽宁王牌速效制药有限公司 | Preparing method of paracetamol, caffein, atificial cow-bezoar and chlorphenamine maleate capsule content functional pellet |
| CN102614220B (en) * | 2012-04-14 | 2013-08-21 | 辽宁王牌速效制药有限公司 | Preparing method of paracetamol, caffein, atificial cow-bezoar capsule content functional pellet |
| CN103156855A (en) * | 2013-03-21 | 2013-06-19 | 青岛正大海尔制药有限公司 | Paracetamol and caffeine slow-release capsule and preparation method thereof |
| CN105250240A (en) * | 2015-08-25 | 2016-01-20 | 江苏先科药业有限公司 | Oral sustained-release preparation containing hydrocodone and chlorpheniramine |
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