CN1241568C - Compound paracetamol and chlorphenamine maleate slow releasing tablet and its preparation - Google Patents
Compound paracetamol and chlorphenamine maleate slow releasing tablet and its preparation Download PDFInfo
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- CN1241568C CN1241568C CN 200310107090 CN200310107090A CN1241568C CN 1241568 C CN1241568 C CN 1241568C CN 200310107090 CN200310107090 CN 200310107090 CN 200310107090 A CN200310107090 A CN 200310107090A CN 1241568 C CN1241568 C CN 1241568C
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- Prior art keywords
- chlorphenamine maleate
- slow releasing
- caffeine
- lubricant
- acetaminophen
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Abstract
The present invention relates to a compound paracetamol and chlorphenamine maleate slow releasing tablet and a preparation method thereof. The tablet is prepared from a tablet core prepared from 30% to 80% of paracetamol, 0.5% to 4% of chlorpheniramine maleate, 2% to 10% of caffeine, 1% to 10% of artificial bezoar, a slow releasing framework material, a lubricator, an adhesive and a flow aiding agent, and a moistureproof film. The slow releasing tablet can effectively overcome the defect of the existing preparation. A novel framework material is used for manufacturing a slow releasing preparation for constantly releasing a medicament. Effective blood medicament concentration in a body can maintain 12 hours. Administration times can be reduced. The tablet is taken twice every day. The slow releasing tablet has the advantages of smooth blood medicament concentration and small side effect.
Description
Technical field
The present invention relates to a kind of compound paracetamol and chlorphenamine maleate slow releasing tablet and preparation method.
Background technology
Adopt acetaminophen, chlorphenamine maleate, caffeine, the electuary and the capsule of the treatment flu that artificial Calculus Bovis's compositions is made are listed in the nonprescription drugs range of management by country.Because the component drug half-life in the said composition is short, the acetaminophen half-life is 75-180 minute, and the chlorphenamine maleate half-life is 2-15 hour, and the caffeine half-life is 3-4 hour.Because the component half-life is short, oral post-absorption is fast, and therefore elimination is also fast in vivo, and in order to keep effective blood drug concentration, day three balance administrations of clothes can make the Wave crest and wave trough phenomenon of producing in the hematopoietic, appreciable impact therapeutic effect, and the inconvenience of taking medicine like this.In order to satisfy the needs of clinical development, be badly in need of the slow releasing agent of development and exploitation said composition.
Summary of the invention:
The purpose of this invention is to provide a kind of compound paracetamol and chlorphenamine maleate slow releasing tablet and preparation method.The present invention can overcome the defective of existing preparation effectively, selects for use novel framework material to make slow releasing preparation, can constant release.Effective blood drug concentration can be kept 12 hours in the body, can reduce medicining times, took secondary every day, and blood drug level is steady, and side effect is little.
The label and the damp-proof membrane that the present invention includes effective active components acetaminophen, chlorphenamine maleate, caffeine, artificial Calculus Bovis constitute.
Described label quality is formed:
Acetaminophen 30%-80%
Chlorphenamine maleate 0.5%-4%
Caffeine 2%-10%
Artificial Calculus Bovis 1%-10%
Sustained-release matrix material 10%-50%
Binding agent 1%-8%
Lubricant 0.5%-3%
Fluidizer 1%-5%
It is Opadry model opadry II that described damp-proof membrane is formed, slightly soluble type coating materials, coating weightening finish 2%-6% in accordance with regulations.
Described sustained-release matrix material is: hydroxypropyl methylcellulose K4M, K15M, K100M, hydroxypropyl methylcellulose E4M, hydroxypropyl methylcellulose F4M, carbomer 934 p, 974P, 940P, 971P, ethyl cellulose, sodium alginate, chitosan or magnesium stearate.
Described binding agent is: 30 POVIDONE K 30 BP/USP 30, ethyl cellulose or hydroxy methocel.
Described lubricant is: magnesium stearate, calcium stearate, or Macrogol 4000 or polyethylene glycol 6000.
Described fluidizer is: Pulvis Talci or silica gel.
Preparation of the present invention comprises the steps:
1, a step system granule method tabletting
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 in next step granulation of atomize, dried granule is added lubricant, tabletting behind the fluidizer, the bag damp-proof membrane, 40 ℃ of dryings 8 hours are made slow releasing preparation.
2, moist granulation method tabletting
Get the acetaminophen of metering, chlorphenamine maleate, caffeine, artificial Calculus Bovis, sustained-release matrix material, binding agent polyvidone, mix homogeneously.Put in the wet granulator, add dehydrated alcohol and make soft material in right amount, 1530 μ m screen cloth system granules.Put 60 ℃ of baking box inner dryings 1～2 hour.Use 1400 μ m screen cloth granulate.Add lubricant, tabletting behind the fluidizer, the bag damp-proof membrane is made slow releasing preparation.
Advantage of the present invention: utilize advanced matrix type slow-release material, make the compound paracetamol and chlorphenamine maleate slow releasing tablet, this product can reduce medicining times, every day twice, each a slice.Its drug release feature is not subjected to the gastrointestinal factor affecting, constant release in the release in vitro degree is measured 1-8 hour, Higuchi equation, blood drug level is steady, thereby reduced the toxic and side effects after taking medicine effectively, improved patient's compliance, be fit to the needs of clinical application development.
Description of drawings:
Fig. 1: compound paracetamol and chlorphenamine maleate slow releasing tablet cumulative release curve chart of the present invention.
The specific embodiment
Embodiment 1
The label prescription:
Acetaminophen 375g
Chlorphenamine maleate 4.5g
Caffeine 22.5g
Artificial Calculus Bovis 15g
Carbomer 934 P 159g
30 POVIDONE K 30 BP/USP 30 18g
Magnesium stearate 3g
Pulvis Talci 3g
Preparation technology (one) method: with acetaminophen, chlorphenamine maleate, caffeine, the artificial Calculus Bovis pulverizes each usefulness of sieving.30 POVIDONE K 30 BP/USP 30, magnesium stearate, Pulvis Talci is sieving for standby respectively.With chlorphenamine maleate, acetaminophen, caffeine; the artificial Calculus Bovis, carbomer 934 P, 30 POVIDONE K 30 BP/USP 30 places in the fluid bed; abundant mixing, with the dehydrated alcohol be wetting agent under atomize, a step is made granule; behind the fluid bed inner drying; add magnesium stearate, tabletting behind the Pulvis Talci mixing, bag damp-proof membrane; weightening finish 3%, dry back discharging is put 40 ℃ of hothouse inner dryings and was got final product in 8 hours.
Carry out the cumulative release experiment with the above-mentioned compound paracetamol and chlorphenamine maleate slow releasing tablet that obtains, the results are shown in Table 1:
Table 1:0～10 hour cumulative release (%)
| Time h | Acetaminophen | Caffeine | Chlorphenamine |
| 0 | 0 | 0 | 0 |
| 2 | 28.52 | 33.25 | 12.48 |
| 4 | 55.85 | 57.35 | 37.37 |
| 6 | 79.11 | 77.95 | 53.19 |
| 8 | 88.36 | 89.31 | 78.32 |
| 10 | 95.82 | 97.87 | 90.17 |
Carry out the cumulative release experiment with the above-mentioned compound paracetamol and chlorphenamine maleate slow releasing tablet that obtains, cumulative release was mapped to the time, saw Fig. 1, and Fig. 1 is the wet distiller line chart of compound paracetamol and chlorphenamine maleate slow releasing tablet accumulation of the present invention.
Preparation technology (two) method: with acetaminophen, chlorphenamine maleate, caffeine, the artificial Calculus Bovis pulverizes sieving for standby.30 POVIDONE K 30 BP/USP 30, magnesium stearate, Pulvis Talci is sieving for standby respectively.With chlorphenamine maleate, acetaminophen, caffeine, the artificial Calculus Bovis, carbomer 934 P, 30 POVIDONE K 30 BP/USP 30 places in the wet granulator.Add dehydrated alcohol and make soft material in right amount.1530 μ m screen cloth system granules.Put 60 ℃ of drying baker inner dryings 1 hour.1400 μ m screen cloth granulate are used in dry back.Add magnesium stearate, tabletting behind the Pulvis Talci mixing, the bag damp-proof membrane increases to 3%, discharging after dry 20 minutes.Put to solidify in 40 ℃ of hothouses and got final product in 8 hours.
Embodiment 2
The label prescription
Acetaminophen 3750g
Chlorphenamine maleate 45g
Caffeine 225g
Artificial Calculus Bovis 150g
Carbomer 934 P 159g
30 POVIDONE K 30 BP/USP 30 18g
Magnesium stearate 3g
Pulvis Talci 3g
Preparation technology's one method: with acetaminophen, chlorphenamine maleate, caffeine, the artificial Calculus Bovis pulverizes sieving for standby.30 POVIDONE K 30 BP/USP 30, magnesium stearate, Pulvis Talci is sieving for standby respectively.With chlorphenamine maleate, acetaminophen, caffeine; the artificial Calculus Bovis, carbomer 934 P, 30 POVIDONE K 30 BP/USP 30 places in the fluid bed; abundant mixing, with the dehydrated alcohol be wetting agent under atomize, a step is made granule; behind the fluid bed inner drying, add magnesium stearate, tabletting behind the Pulvis Talci mixing; the bag damp-proof membrane; weightening finish 3%, discharging after dry back 20 minutes, 40 ℃ of hothouse inner dryings got final product in 8 hours.
Preparation technology (two) method: with acetaminophen, chlorphenamine maleate, caffeine, the artificial Calculus Bovis pulverizes sieving for standby.30 POVIDONE K 30 BP/USP 30, magnesium stearate, Pulvis Talci is sieving for standby respectively.With chlorphenamine maleate, acetaminophen, caffeine, the artificial Calculus Bovis, carbomer 934 P, 30 POVIDONE K 30 BP/USP 30 places in the wet granulator.Add dehydrated alcohol and make soft material in right amount.1530 μ m screen cloth system granules.Put 60 ℃ of drying baker inner dryings 2 hours.1400m screen cloth granulate is used in dry back.Add magnesium stearate, tabletting behind the Pulvis Talci mixing, the bag damp-proof membrane increases to 3%, the discharging after 20 minutes of coating pan inner drying.Put to solidify in 40 ℃ of hothouses and got final product in 8 hours.
Embodiment 3:
The label prescription
Acetaminophen 1125g
Chlorphenamine maleate 13.5g
Caffeine 67.5g
Artificial Calculus Bovis 45g
Hydroxypropyl methylcellulose 4KM 477g
30 POVIDONE K 30 BP/USP 30 54g
Magnesium stearate 9g
Pulvis Talci 9g
Preparation technology (one): with acetaminophen, chlorphenamine maleate, caffeine, the artificial Calculus Bovis pulverizes sieving for standby.30 POVIDONE K 30 BP/USP 30, magnesium stearate, Pulvis Talci is sieving for standby respectively.With chlorphenamine maleate, acetaminophen, caffeine; the artificial Calculus Bovis, carbomer 934 P, 30 POVIDONE K 30 BP/USP 30 places in the fluid bed; abundant mixing, with dehydrated alcohol: water (1: 1) be wetting agent under atomize, one goes on foot and makes granule; behind the fluid bed inner drying; add magnesium stearate, tabletting behind the Pulvis Talci mixing, bag damp-proof membrane; weightening finish 3%, dry back discharging is put 40 ℃ of hothouse inner dryings and was got final product in 8 hours.
Preparation technology (two): with acetaminophen, chlorphenamine maleate, caffeine, the artificial Calculus Bovis pulverizes sieving for standby.30 POVIDONE K 30 BP/USP 30, magnesium stearate, Pulvis Talci is sieving for standby respectively.With chlorphenamine maleate, acetaminophen, caffeine, the artificial Calculus Bovis, carbomer 934 P, 30 POVIDONE K 30 BP/USP 30 places in the wet granulator.Add dehydrated alcohol: water (1: 1) is made soft material in right amount.1530 μ m screen cloth system granules.Put 60 ℃ of drying baker inner dryings 2 hours.1400 μ m screen cloth granulate are used in dry back.Add magnesium stearate, tabletting behind the Pulvis Talci mixing, the bag damp-proof membrane increases to 3%, the discharging after 20 minutes of coating pan inner drying.Put to solidify in 40 ℃ of hothouses and got final product in 8 hours.
Claims (4)
1, a kind of compound paracetamol and chlorphenamine maleate slow releasing tablet, it comprises effective active components acetaminophen, chlorphenamine maleate, caffeine and artificial Calculus Bovis, it is characterized in that it also comprises the label that sustained-release matrix material, binding agent, lubricant and fluidizer are made, and the label outside there is damp-proof membrane;
Described label quality is formed:
Acetaminophen 30%-80%
Chlorphenamine maleate 0.5%-4%
Caffeine 2%-10%
Artificial Calculus Bovis 1%-10%
Sustained-release matrix material 10%-50%
Binding agent 1%-8%
Lubricant 0.5%-3%
Fluidizer 1%-5%
It is Opadry model opadry II that described damp-proof membrane is formed, slightly soluble type coating materials;
Described sustained-release matrix material is hydroxypropyl methylcellulose K4M or carbomer 934 p; Described binding agent is a 30 POVIDONE K 30 BP/USP 30; Described lubricant is a magnesium stearate; Described fluidizer is a Pulvis Talci.
2, a kind of compound paracetamol and chlorphenamine maleate slow releasing tablet, it comprises effective active components acetaminophen, chlorphenamine maleate, caffeine and artificial Calculus Bovis, it is characterized in that it also comprises the label that sustained-release matrix material, binding agent, lubricant and fluidizer are made, and the label outside there is damp-proof membrane;
It is characterized in that described label quality composition:
Acetaminophen 62.5%
Chlorphenamine maleate 0.75%
Caffeine 3.75%
The artificial Calculus Bovis 2.5%
Sustained-release matrix material 26.5%
Binding agent 3%
Lubricant 0.5%
Fluidizer 0.5%
It is Opadry model opadry II that described damp-proof membrane is formed, slightly soluble type coating materials;
Described sustained-release matrix material is hydroxypropyl methylcellulose K4M or carbomer 934 p; Described binding agent is a 30 POVIDONE K 30 BP/USP 30; Described lubricant is a magnesium stearate; Described fluidizer is a Pulvis Talci.
3,, it is characterized in that described Opadry model opadryII coating materials coating weightening finish 2%-6% according to claim 1 or 2 described compound paracetamol and chlorphenamine maleate slow releasing tablet.
4, the preparation method of claim 1 or 2 described compound paracetamol and chlorphenamine maleate slow releasing tablet is characterized in that it comprises the steps:
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 in next step granulation of atomize, dried granule is added lubricant, tabletting behind the fluidizer, the bag damp-proof membrane, discharging after dry 20 minutes, 40 ℃ of dryings 8 hours are made slow releasing preparation; Or
Get the acetaminophen of metering, chlorphenamine maleate, caffeine, artificial Calculus Bovis, sustained-release matrix material, binding agent polyvidone, mix homogeneously; Put in the wet granulator, add dehydrated alcohol and make soft material, 1530 μ m screen cloth system granules; Put 60 ℃ of baking box inner dryings 1～2 hour; Use 1400 μ m screen cloth granulate; Add lubricant, tabletting behind the fluidizer, the bag damp-proof membrane, discharging after dry 20 minutes, 40 ℃ of dryings 8 hours are made slow releasing preparation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200310107090 CN1241568C (en) | 2003-11-24 | 2003-11-24 | Compound paracetamol and chlorphenamine maleate slow releasing tablet and its preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200310107090 CN1241568C (en) | 2003-11-24 | 2003-11-24 | Compound paracetamol and chlorphenamine maleate slow releasing tablet and its preparation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1543956A CN1543956A (en) | 2004-11-10 |
| CN1241568C true CN1241568C (en) | 2006-02-15 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200310107090 Expired - Fee Related CN1241568C (en) | 2003-11-24 | 2003-11-24 | Compound paracetamol and chlorphenamine maleate slow releasing tablet and its preparation |
Country Status (1)
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| CN (1) | CN1241568C (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103110638A (en) * | 2013-02-19 | 2013-05-22 | 青岛正大海尔制药有限公司 | Paracetamol and caffeine sustained release preparation and preparation method thereof |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101244064B (en) * | 2007-02-14 | 2012-10-10 | 中山大学 | Pharmaceutical combination for preventing and treating motion sickness and preparations thereof |
| CN101596158B (en) * | 2008-06-04 | 2011-03-30 | 北京科信必成医药科技发展有限公司 | Compound slow release preparation of acetyl aminophenol, pseudoephedrine and dextromethorphan |
| CN102475719A (en) * | 2010-11-29 | 2012-05-30 | 神威药业有限公司 | Drug composition for treating children upper respiratory tract infection, and preparation method thereof |
| CN109464467A (en) * | 2019-01-07 | 2019-03-15 | 安徽东盛友邦制药有限公司 | A kind of paracetamol caffein atificial cow-bezoar and preparation method thereof with slow releasing function |
-
2003
- 2003-11-24 CN CN 200310107090 patent/CN1241568C/en not_active Expired - Fee Related
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103110638A (en) * | 2013-02-19 | 2013-05-22 | 青岛正大海尔制药有限公司 | Paracetamol and caffeine sustained release preparation and preparation method thereof |
| CN103110638B (en) * | 2013-02-19 | 2014-06-25 | 青岛正大海尔制药有限公司 | Paracetamol and caffeine sustained release preparation and preparation method thereof |
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| Publication number | Publication date |
|---|---|
| CN1543956A (en) | 2004-11-10 |
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| PB01 | Publication | ||
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| C14 | Grant of patent or utility model | ||
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Granted publication date: 20060215 Termination date: 20151124 |