CN103156849B - Compound pseudoephedrine hydrochloride enteric-coated tablet and preparation method thereof - Google Patents
Compound pseudoephedrine hydrochloride enteric-coated tablet and preparation method thereof Download PDFInfo
- Publication number
- CN103156849B CN103156849B CN201310092633.5A CN201310092633A CN103156849B CN 103156849 B CN103156849 B CN 103156849B CN 201310092633 A CN201310092633 A CN 201310092633A CN 103156849 B CN103156849 B CN 103156849B
- Authority
- CN
- China
- Prior art keywords
- enteric
- acetaminophen
- pseudoephedrine hydrochloride
- compound
- acetaminophen compound
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a compound pseudoephedrine hydrochloride enteric-coated tablet and a preparation method thereof. The compound pseudoephedrine hydrochloride enteric-coated tablet is composed of a compound pseudoephedrine hydrochloride core tablet and an enteric coating layer wrapped outside the core tablet, wherein the compound pseudoephedrine hydrochloride core tablet comprises acetaminophen, pseudoephedrine hydrochloride, dextromethorphan hydrobromide, chlorpheniramine maleate, filler and a disintegrating agent; the enteric coating layer comprises an enteric material, a plasticizer, an antisticking agent and an opacifier; and the compound pseudoephedrine hydrochloride enteric-coated tablet is obtained through wrapping the enteric coating layer outside the compound pseudoephedrine hydrochloride core tablet during the preparation. The compound pseudoephedrine hydrochloride enteric-coated tablet disclosed by the invention is ideal in enteric effect, capable of increasing the bioavailability and reducing the stimulation of the medicine on gastric mucosa, simple in preparation process, stable in obtained product quality and suitable for large scale production and application.
Description
Technical field
The present invention relates to a kind of Western medicine preparation technical field, relate in particular to a kind of acetaminophen compound enteric coatel tablets, the invention still further relates to the preparation method of these enteric coatel tablets.
Background technology
Acetaminophen compound preparation is conventional antipyretic-antalgic compound preparation, and its effective ingredient comprises acetaminophen, pseudoephedrine hydrochloride, dextromethorphan hydrobromide and chlorphenamine maleate.Acetaminophen has another name called acetaminophen, be the interior metabolism product of phenacetin, belong to phenyl amines, it is by suppressing hypothalamus thermotaxic centre prostaglandin synthetase, reduce the synthetic of Prostaglandin PGE1 and discharge, cause peripheral blood vessel to increase, perspire and reach antipyretic effect; Pseudoephedrine hydrochloride is collapsible nasal mucosa blood vessel, alleviates nasal obstruction symptom; Dextromethorphan hydrobromide is maincenter cough medicine, by suppressing coughing centre, produces antitussive effect; Chlorphenamine maleate is histamine (H1) receptor antagonist, and the Marjoram Extract that can cause antihistamine and capillary permeability increase, alleviate shed tears, the allergic symptom such as sneeze, watery nasal discharge.Acetaminophen compound preparation is widely used in the symptoms such as heating that treatment flu or influenza cause, headache, throat pain, muscular soreness, nasal obstruction watery nasal discharge, sneeze, cough.The main dosage form of acetaminophen compound preparation in China market is tablet, capsule and oral liquid at present, dosage form is more dull, be subject to the impact of the factors such as disintegrate, drug release, absorb, therapeutic effect is undesirable, composition chlorphenamine maleate wherein can stimulate has stimulation to gastric mucosa, if strengthen dosage in order to reach ideal treatment, the symptoms such as feeling sick may appear in pill taker, vomiting, stomachache, diarrhoea, anorexia, hyperhidrosis.
Enteric coated preparation refers to and do not discharge under one's belt at the appointed time or discharge hardly medicine, and enters in intestinal, can be most of in a part of intestinal or all discharge the preparation of medicine, and enteric coatel tablets belong to a kind of of enteric coated preparation.Enteric coated preparation can avoid medicine to be subject to the destruction of gastric enzyme or gastric acid, avoids medicine to produce intense stimulus to gastric mucosa, and delayed release effect is provided, and the main medicine by intestinal absorption is passed to this position with maximum concentration as far as possible, has improved bioavailability.
Summary of the invention
In order to overcome the deficiencies in the prior art, the present invention to adjuvant screening and process optimization, provides a kind of acetaminophen compound enteric coatel tablets by lot of experiments.This enteric coatel tablets steady quality, medicine discharges in intestinal, and bioavailability is high, can reduce the stimulation of medicine to stomach, and preparation technology is simple, is suitable for large-scale production and application.
For achieving the above object, the technical scheme that the present invention takes is:
A kind of acetaminophen compound enteric coatel tablets, enteric coat layer outer with being wrapped in it by acetaminophen compound label forms, described acetaminophen compound label comprises acetaminophen, pseudoephedrine hydrochloride, dextromethorphan hydrobromide, chlorphenamine maleate, filler and disintegrating agent, acetaminophen wherein, pseudoephedrine hydrochloride, dextromethorphan hydrobromide and chlorphenamine maleate are active component, its weight ratio is 22:2:1:0.15, described enteric coat layer comprises enteric material, plasticizer, antiplastering aid and opacifier, it is characterized in that, remember by ratio of weight and the number of copies, the consumption of each composition is:
Preferably, remember by ratio of weight and the number of copies, the consumption of each composition is:
Wherein, described filler is dextrin; Described disintegrating agent is low-substituted hydroxypropyl cellulose; Described enteric material is selected from least one in III acrylic resin, Hydroxypropyl Methylcellulose Phathalate and PVAP; Described plasticizer is polyethylene glycol 6000; Described antiplastering aid is magnesium stearate; Described opacifier is titanium dioxide.
Wherein, described enteric material is preferably III acrylic resin and Hydroxypropyl Methylcellulose Phathalate; Most preferably, III acrylic resin and Hydroxypropyl Methylcellulose Phathalate weight ratio are 3:1.
Acetaminophen compound enteric coatel tablets of the present invention can be prepared as follows:
(1) by prescription, measuring acetaminophen, pseudoephedrine hydrochloride, dextromethorphan hydrobromide, chlorphenamine maleate mixs homogeneously with filler, disintegrating agent, take dehydrated alcohol as binding agent, 20～30 mesh sieves are granulated, and dry rear tabletting, obtains acetaminophen compound label;
(2) with 80% dissolve with ethanol enteric material, plasticizer, antiplastering aid and opacifier, make enteric coating liquid;
(3) enteric coating liquid preparing is evenly sprayed to the acetaminophen compound sheet wicking surface that step (1) prepares, after being dried, obtains acetaminophen compound enteric coatel tablets.
The acetaminophen compound enteric coatel tablets that the present invention relates to have following beneficial effect:
(1) enteric is satisfactory for result, can improve bioavailability, reduces the stimulation of medicine to gastric mucosa;
(2) selected adjuvant is common, and preparation technology is simple, and products obtained therefrom steady quality is applicable to large-scale production and application.
The specific embodiment
Below in conjunction with embodiment, the specific embodiment of the present invention is further described, advantage and disadvantage of the present invention will be more clear along with description.But these embodiment are only exemplary, scope of the present invention are not formed to any restriction.It will be understood by those skilled in the art that lower without departing from the spirit and scope of the present invention and can the details of technical solution of the present invention and form be modified or be replaced, but these modifications and replacement all fall within the scope of protection of the present invention.
A preparation method for acetaminophen compound enteric coatel tablets, comprises the following steps:
(1) by prescription, measuring acetaminophen, pseudoephedrine hydrochloride, dextromethorphan hydrobromide, chlorphenamine maleate mixs homogeneously with filler, disintegrating agent, take dehydrated alcohol as binding agent, 20～30 mesh sieves are granulated, and dry rear tabletting, obtains acetaminophen compound label;
(2) with 80% dissolve with ethanol enteric material, plasticizer, antiplastering aid and opacifier, make enteric coating liquid;
(3) enteric coating liquid preparing is evenly sprayed to the acetaminophen compound sheet wicking surface that step (1) prepares, after being dried, obtains acetaminophen compound enteric coatel tablets.
The preparation of embodiment 1～6 acetaminophen compound enteric coatel tablets
The supplementary material of according to the form below, by above-mentioned preparation method, makes the acetaminophen compound enteric coatel tablets of six embodiment.Wherein, "/" representative is not used.
The dissolution determination of test example 1 embodiment 1～6 gained acetaminophen compound enteric coatel tablets
According to dissolution method (60 page of second method of Chinese Pharmacopoeia two appendix of version in 2000), precision takes appropriate acetaminophen compound enteric coatel tablets, dissolution medium is respectively: pH1.2 simulated gastric fluid and pH6.8 simulated intestinal fluid, take respectively simulated gastric fluid and simulated intestinal fluid as solvent, and measure dissolution.The results are shown in Table 1 and table 2.
Table 1 embodiment 1～6 acetaminophen compound enteric coatel tablets dissolution investigation table in simulated gastric fluid
| ? | 30min | 1h | 2h | 3h | 4h |
| Embodiment 1 | 7.7% | 8.6% | 9.5% | 10.1% | 11.2% |
| Embodiment 2 | 7.9% | 8.8% | 10.0% | 11.2% | 12.5% |
| Embodiment 3 | 8.3% | 9.4% | 10.3% | 11.4% | 12.6% |
| Embodiment 4 | 5.5% | 6.4% | 7.3% | 8.3% | 9.0% |
| Embodiment 5 | 6.8% | 7.6% | 8.5% | 9.7% | 10.8% |
| Embodiment 6 | 7.9% | 9.0% | 9.9% | 10.8% | 11.8% |
As can be seen from Table 1, the stripping in pH1.2 simulated gastric fluid of the prepared acetaminophen compound enteric coatel tablets of embodiment 1～6 is slow, 4h stripping is the highest by only 12.6%, there is good acid resistance, wherein the acetaminophen compound enteric coatel tablets 4h stripping of embodiment 4 is minimum, illustrates that the acetaminophen compound enteric coatel tablets acid resistance of using III acrylic resin and Hydroxypropyl Methylcellulose Phathalate to make as the enteric material of coating is best.
Table 2 embodiment 1～6 acetaminophen compound enteric coatel tablets dissolution investigation table in simulated intestinal fluid
| ? | 5min | 10min | 15min | 20min | 30min | 40min | 50min | 60min |
| Embodiment 1 | 15.8% | 48.7% | 62.5% | 71.8% | 77.4% | 80.0% | 84.2% | 87.3% |
| Embodiment 2 | 16.5% | 47.7% | 60.2% | 68.8% | 73.6% | 78.9% | 81.2% | 85.4% |
| Embodiment 3 | 14.8% | 44.0% | 57.6% | 67.7% | 71.4% | 75.5% | 79.1% | 83.9% |
| Embodiment 4 | 18.0% | 57.3% | 69.7% | 77.4% | 85.1% | 87.6% | 89.3% | 90.5% |
| Embodiment 5 | 16.3% | 48.8% | 61.9% | 73.0% | 79.5% | 84.2% | 85.1% | 87.0% |
| Embodiment 6 | 15.1% | 43.2% | 58.7% | 66.5% | 74.8% | 78.3% | 82.1% | 87.4% |
As can be seen from Table 2, the prepared acetaminophen compound enteric coatel tablets of embodiment 1～6 discharge rapidly in pH6.8 simulated intestinal fluid, can reach the object of rapid release, wherein acetaminophen compound enteric coatel tablets dissolution in 60min of embodiment 4 is the highest, illustrates that acetaminophen compound enteric coatel tablets rapid release effect in intestinal of using III acrylic resin and Hydroxypropyl Methylcellulose Phathalate to make as the enteric material of coating is best.
The preparation of embodiment 7～13 acetaminophen compound enteric coatel tablets
The supplementary material of according to the form below, by above-mentioned preparation method, each embodiment makes respectively acetaminophen compound enteric coatel tablets.
The III acrylic resin of embodiment 7 and the weight ratio of Hydroxypropyl Methylcellulose Phathalate are 4:1,
The III acrylic resin of embodiment 8 and the weight ratio of Hydroxypropyl Methylcellulose Phathalate are 3:1,
The III acrylic resin of embodiment 9 and the weight ratio of Hydroxypropyl Methylcellulose Phathalate are 2:1,
The III acrylic resin of embodiment 10 and the weight ratio of Hydroxypropyl Methylcellulose Phathalate are 1:1,
The III acrylic resin of embodiment 11 and the weight ratio of Hydroxypropyl Methylcellulose Phathalate are 1:2,
The III acrylic resin of embodiment 12 and the weight ratio of Hydroxypropyl Methylcellulose Phathalate are 1:3,
The III acrylic resin of embodiment 13 and the weight ratio of Hydroxypropyl Methylcellulose Phathalate are 1:4.
The acetaminophen compound enteric coatel tablets dissolution determination of test example 2 embodiment 7～13 gained
Assay method is with test example 1.Measurement result is in Table 3 and table 4.
Table 3 embodiment 7～13 acetaminophen compound enteric coatel tablets dissolution investigation table in simulated gastric fluid
| ? | 30min | 1h | 2h | 3h | 4h |
| Embodiment 7 | 5.8% | 6.7% | 7.3% | 8.6% | 9.8% |
| Embodiment 8 | 4.8% | 5.5% | 6.3% | 7.0% | 8.6% |
| Embodiment 9 | 5.7% | 6.8% | 8.0% | 9.6% | 10.1% |
| Embodiment 10 | 5.5% | 6.4% | 7.3% | 8.3% | 9.0% |
| Embodiment 11 | 6.0% | 6.9% | 7.8% | 8.7% | 9.5% |
| Embodiment 12 | 6.3% | 7.2% | 8.4% | 9.3% | 10.2% |
| Embodiment 13 | 6.6% | 7.5% | 8.4% | 9.7% | 10.5% |
As known from Table 3, the stripping in pH1.2 simulated gastric fluid of the prepared acetaminophen compound enteric coatel tablets of embodiment 8 is the slowest, when the weight ratio that enteric material III acrylic resin and Hydroxypropyl Methylcellulose Phathalate be described is 3:1, prepared acetaminophen compound enteric coatel tablets acid resistance is best.
Table 4 embodiment 7～13 acetaminophen compound enteric coatel tablets dissolution investigation table in simulated intestinal fluid
| ? | 5min | 10min | 15min | 20min | 30min | 40min | 50min | 60min |
| Embodiment 7 | 18.4% | 55.9% | 70.1% | 76.3% | 81.5% | 85.6% | 88.3% | 90.2% |
| Embodiment 8 | 20.1% | 62.4% | 71.6% | 80.3% | 86.0% | 89.7% | 92.5% | 94.8% |
| Embodiment 9 | 19.0% | 56.8% | 68.3% | 75.5% | 80.2% | 83.4% | 86.6% | 89.7% |
| Embodiment 10 | 18.0% | 57.3% | 69.7% | 77.4% | 85.1% | 87.6% | 89.3% | 90.5% |
| Embodiment 11 | 17.3% | 53.8% | 67.4% | 75.0% | 79.3% | 84.1% | 87.6% | 89.2% |
| Embodiment 12 | 16.8% | 48.6% | 63.0% | 74.1% | 78.5% | 82.6% | 85.4% | 88.3% |
| Embodiment 13 | 16.6% | 46.1% | 60.0% | 71.3% | 76.8% | 81.8% | 85.6% | 87.9% |
As known from Table 3, the prepared acetaminophen compound enteric coatel tablets of embodiment 8 discharge rapidly in pH6.8 simulated intestinal fluid, in 60min, dissolution is the highest, when the weight ratio that enteric material III acrylic resin and Hydroxypropyl Methylcellulose Phathalate be described is 3:1, prepared acetaminophen compound enteric coatel tablets rapid release effect in intestinal is best.
In sum, known when using III acrylic resin and Hydroxypropyl Methylcellulose Phathalate as enteric material, and both weight ratios are while being 3:1, prepared acetaminophen compound enteric coatel tablets acid resistance in gastric juice is good, in intestinal juice, stripping is rapid, and dissolution is high, and effect is best.
Claims (2)
1. acetaminophen compound enteric coatel tablets, enteric coat layer outer with being wrapped in it by acetaminophen compound label forms, described acetaminophen compound label consists of acetaminophen, pseudoephedrine hydrochloride, dextromethorphan hydrobromide, chlorphenamine maleate, filler and disintegrating agent, acetaminophen wherein, pseudoephedrine hydrochloride, dextromethorphan hydrobromide and chlorphenamine maleate are active component, its weight ratio is 22:2:1:0.15, described enteric coat layer consists of enteric material, plasticizer, antiplastering aid and opacifier, described enteric material is that the weight ratio of III acrylic resin and Hydroxypropyl Methylcellulose Phathalate is 3:1, described disintegrating agent is low-substituted hydroxypropyl cellulose, described plasticizer is polyethylene glycol 6000, described antiplastering aid is magnesium stearate, described opacifier is titanium dioxide, it is characterized in that: count by ratio of weight and the number of copies, the consumption of each composition is:
2. prepare the method for acetaminophen compound enteric coatel tablets claimed in claim 1, comprise the following steps:
(1) by prescription, measuring acetaminophen, pseudoephedrine hydrochloride, dextromethorphan hydrobromide, chlorphenamine maleate mixs homogeneously with filler, disintegrating agent, take dehydrated alcohol as binding agent, 20～30 mesh sieves are granulated, and dry rear tabletting, obtains acetaminophen compound label;
(2) with 80% dissolve with ethanol enteric material, plasticizer, antiplastering aid and opacifier, make enteric coating liquid;
(3) enteric coating liquid preparing is evenly sprayed to the acetaminophen compound sheet wicking surface that step (1) prepares, after being dried, obtains acetaminophen compound enteric coatel tablets.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310092633.5A CN103156849B (en) | 2013-03-21 | 2013-03-21 | Compound pseudoephedrine hydrochloride enteric-coated tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310092633.5A CN103156849B (en) | 2013-03-21 | 2013-03-21 | Compound pseudoephedrine hydrochloride enteric-coated tablet and preparation method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103156849A CN103156849A (en) | 2013-06-19 |
| CN103156849B true CN103156849B (en) | 2014-08-20 |
Family
ID=48580715
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310092633.5A Active CN103156849B (en) | 2013-03-21 | 2013-03-21 | Compound pseudoephedrine hydrochloride enteric-coated tablet and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103156849B (en) |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1679525A (en) * | 2005-01-12 | 2005-10-12 | 复旦大学 | Oral disintegrant of compound paracetamol |
| CN1850083A (en) * | 2006-02-28 | 2006-10-25 | 江西聚仁堂药业有限公司 | Dispersible tablet for treating cold and its preparing process |
| CN101658521A (en) * | 2008-08-26 | 2010-03-03 | 北京科信必成医药科技发展有限公司 | Paracetamol, pseudoephedrine and chlorphenamine compound sustained release preparation |
| CN102641254B (en) * | 2012-05-07 | 2013-10-09 | 山东新华制药股份有限公司 | Preparation method of aspirin enteric-coated sustained-release preparation |
-
2013
- 2013-03-21 CN CN201310092633.5A patent/CN103156849B/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| CN103156849A (en) | 2013-06-19 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN104042588B (en) | Containing the multilayer tablet of methanesulfonic acid dabigatran etcxilate | |
| CN101926865B (en) | Spina date seed depression-resolving and nerve-soothing composition and preparation method thereof | |
| CN104000789A (en) | Adefovir dipivoxil dispersible tablet and preparation method thereof | |
| CN104958279A (en) | Loratadine oral quickly-soluble film and preparation method thereof | |
| CN103156849B (en) | Compound pseudoephedrine hydrochloride enteric-coated tablet and preparation method thereof | |
| CN100542528C (en) | Bicyclol micronization and controlled release formulations for oral administration | |
| CN103156852B (en) | Paracetamol, pseudoephedrine hydrochloride, dextromethorphan hydrobromide and chlorpheniramine maleate enteric capsule and preparation method thereof | |
| CN103142538B (en) | PGMS (Propylene Glycol Mannate Sulfate) enteric tablet and preparation method thereof | |
| CN103142606B (en) | Paracetamol and caffeine enteric tablet and preparation method thereof | |
| CN103142535B (en) | Alginic sodium diester enteric tablet and preparation method thereof | |
| CN103156853B (en) | Paracetamol and caffeine enteric capsule and preparation method thereof | |
| CN103156851B (en) | Pseudoephedrine hydrochloride slow-release particles and preparation method thereof | |
| CN103142549B (en) | Mannose ester enteric capsule and preparation method thereof | |
| CN103156850B (en) | Dextromethorphan hydrobromide slow-release capsule and preparation method thereof | |
| CN105727104A (en) | Medicine composition with effects of diminishing inflammation and relieving cough and method for preparing medicine composition | |
| CN103127030B (en) | Propylene glycol alginate sodium sulfate enteric capsule and preparation method thereof | |
| CN103301074A (en) | Diammonium glycyrrhizinate enteric-coated pellet as well as preparation method and preparation thereof | |
| CN106110132A (en) | A kind of compositions with removing heat from the lung and dissipating phlegm antitussive effect and preparation method thereof | |
| CN101797253B (en) | Bergenin and cetirizine dihydrochloride compound oral administration preparation | |
| CN110833540A (en) | Salicorol, caffeine and chlorphenamine maleate tablet and preparation method thereof | |
| CN103156854B (en) | Paracetamol and caffeine slow-release particles and preparation method thereof | |
| CN103977354A (en) | Chinese medicinal extract with anti-depression effect and preparation method and application thereof | |
| CN105395519B (en) | A kind of Topiroxostat spansule and preparation method thereof | |
| CN113181128A (en) | Salicophenol caffeine and chlorphenamine maleate three-layer tablet and preparation method thereof | |
| CN103230391A (en) | Bicyclol solid preparation |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| CB02 | Change of applicant information | ||
| CB02 | Change of applicant information |
Address after: 266103 Qingdao economic and Technological Development Zone, unity Road, No. 3601, Shandong Applicant after: Qingdao Zhengda Haier Pharmaceutical Co., Ltd. Address before: 266103 Haier Road, Shandong, Qingdao, No. 1 Applicant before: Qingdao Zhengda Haier Pharmaceutical Co., Ltd. |
|
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CP01 | Change in the name or title of a patent holder | ||
| CP01 | Change in the name or title of a patent holder |
Address after: 266103 3601 Tuen Jie Road, Qingdao economic and Technological Development Zone, Shandong Patentee after: Zhengda Pharmaceutical (Qingdao) Co., Ltd. Address before: 266103 3601 Tuen Jie Road, Qingdao economic and Technological Development Zone, Shandong Patentee before: Qingdao Zhengda Haier Pharmaceutical Co., Ltd. |