CN103156851A - Paracetamol, pseudoephedrine hydrochloride, dextromethorphan hydrobromide and chlorpheniramine maleate slow-release particles and preparation method thereof - Google Patents
Paracetamol, pseudoephedrine hydrochloride, dextromethorphan hydrobromide and chlorpheniramine maleate slow-release particles and preparation method thereof Download PDFInfo
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- CN103156851A CN103156851A CN2013100945800A CN201310094580A CN103156851A CN 103156851 A CN103156851 A CN 103156851A CN 2013100945800 A CN2013100945800 A CN 2013100945800A CN 201310094580 A CN201310094580 A CN 201310094580A CN 103156851 A CN103156851 A CN 103156851A
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Abstract
The invention discloses paracetamol, pseudoephedrine hydrochloride, dextromethorphan hydrobromide and chlorpheniramine maleate slow-release particles and a preparation method thereof. The paracetamol, pseudoephedrine hydrochloride, dextromethorphan hydrobromide and chlorpheniramine maleate slow-release particles are composed of quick-release particle cores and a slow-release coating layer, wherein the quick-release particle cores are composed of paracetamol, pseudoephedrine hydrochloride, dextromethorphan hydrobromide, chlorpheniramine maleate and a filler; and the slow-release coating layer is composed of a slow-release material, a plasticizer, a pore-forming agent and an antisticking agent. The paracetamol, pseudoephedrine hydrochloride, dextromethorphan hydrobromide and chlorpheniramine maleate slow-release particles are prepared by coating the slow-release coating layer outside the quick-release particle cores. The medicine disclosed by the invention is convenient to take, has the advantage of uniform release, can achieve the goal of persistent effect and higher curative effect, and can lower the dosage on the premise of maintaining identical drug effect, thereby reducing the side effect on the patient due to lower dosage of the medicine; and the preparation technique is simple, has the advantage of stable product quality, and is applicable to large-scale production.
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 slow-releasing granules, the invention still further relates to the preparation method of this slow-releasing granules.
Background technology
The acetaminophen compound preparation is the antipyretic-antalgic compound preparation of commonly using, 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 analgesic effect; Pseudoephedrine hydrochloride is collapsible nasal mucosa blood vessel alleviates the nasal obstruction symptom; Dextromethorphan hydrobromide is the maincenter cough medicine, produces antitussive effect by suppressing coughing centre; Chlorphenamine maleate is histamine (H1) receptor antagonist, and Marjoram Extract and the capillary permeability that can cause antihistamine increase, alleviate shed tears, the allergic symptoms such as sneeze, watery nasal discharge.The 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 on 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, the administration time interval is short, the effective blood drug concentration fluctuation is large, absorb, therapeutic effect is undesirable, if strengthen dosage in order to reach ideal treatment, hyperhidrosis, dizziness, the symptom such as weak, nauseating may appear in the pill taker.
Slow releasing preparation refers on purpose control drug release to reach a class dosage form of rational therapy effect, taking rear medicine slowly evenly discharges from dosage form, make human body obtain to treat stably blood drug level, thereby " peak valley " phenomenon of having avoided the ordinary preparation frequent drug administration to occur, safety, effectiveness and the adaptability of raising medicine.Slow-releasing granules is a kind of of slow releasing preparation, and it is compared slow releasing tablet and slow releasing capsule and takes more conveniently, flexible, and patient is taken according to various dose, is particularly suitable for old man and child.
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 slow-releasing granules by lot of experiments.This slow-releasing granules steady quality, drug release is even, and preparation technology is simple.
For achieving the above object, the technical scheme taked of the present invention is:
A kind of acetaminophen compound slow-releasing granules is comprised of immediate-release granules core and the sustained release coating layer that is wrapped in immediate-release granules core outside; Described immediate-release granules core is comprised of acetaminophen, pseudoephedrine hydrochloride, dextromethorphan hydrobromide, chlorphenamine maleate and filler, wherein, acetaminophen, pseudoephedrine hydrochloride, dextromethorphan hydrobromide and chlorphenamine maleate are active component; Described sustained release coating layer is comprised of slow-release material, plasticizer, porogen and antiplastering aid; It is characterized in that, by ratio of weight and the number of copies note:
Wherein, acetaminophen, pseudoephedrine hydrochloride, dextromethorphan hydrobromide, the chlorphenamine maleate weight ratio as active component is 22:2:1:0.15.
Wherein, the weight ratio of slow-release material and plasticizer is preferably 5:1～3:1; Most preferably, the weight ratio of slow-release material and plasticizer is 4:1.
Wherein, described filler is silicified microcrystalline cellulose; Described slow-release material is carboxymethylethylcellulose or ethyl cellulose; Described plasticizer is sodium lauryl sulphate or ethyl oleate; Described porogen is Macrogol 4000; Described antiplastering aid is glyceryl monostearate.
Wherein, described slow-release material is preferably carboxymethylethylcellulose; Described plasticizer is preferably ethyl oleate.
Acetaminophen compound slow-releasing granules of the present invention can prepare as follows:
(1) get acetaminophen, pseudoephedrine hydrochloride, dextromethorphan hydrobromide, chlorphenamine maleate and filler mix homogeneously, take 85% ethanol as binding agent, make 10～14 purpose immediate-release granules cores, standby;
(2) with 80% dissolve with ethanol slow-release material, plasticizer, porogen, antiplastering aid, make sustained release coating liquid;
(3) the sustained release coating liquid for preparing evenly is sprayed at the immediate-release granules wicking surface that step (1) prepares, obtains the acetaminophen compound slow-releasing granules after drying.
The acetaminophen compound slow-releasing granules that the present invention relates to has following beneficial effect:
(1) drug release is even, and the purpose that can reach long-acting, increases curative effect also can reduce dosage when keeping equal drug effect, thereby reduces the side effect that drug administration brings to the patient;
(2) taking convenience can according to the various dose administration, facilitate old man and children taking.
(3) selected adjuvant is common, and preparation technology is simple, and the products obtained therefrom steady quality is fit 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 consisted of 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 modify or replace details and the form of technical solution of the present invention, but these modifications and replacement all fall within the scope of protection of the present invention.
A kind of preparation method of acetaminophen compound slow-releasing granules comprises the following steps:
(1) get acetaminophen, pseudoephedrine hydrochloride, dextromethorphan hydrobromide, chlorphenamine maleate and filler mix homogeneously, take 85% ethanol as binding agent, make 10～14 purpose immediate-release granules cores, standby;
(2) with 80% dissolve with ethanol slow-release material, plasticizer, porogen, antiplastering aid, make sustained release coating liquid;
(3) the sustained release coating liquid for preparing evenly is sprayed at the immediate-release granules wicking surface that step (1) prepares, obtains the acetaminophen compound slow-releasing granules after drying.
The preparation of embodiment 1～4 acetaminophen compound slow-releasing granules
The supplementary material of according to the form below by above-mentioned preparation method, makes the acetaminophen compound slow-releasing granules of four embodiment.Wherein, "/" representative is not used.
The drug release determination of test example 1 embodiment 1～4 gained acetaminophen compound slow-releasing granules
According to " slow, controlled release preparation guideline " in Pharmacopoeia of the People's Republic of China version (two ones) appendix in 2010, take 0.25% sodium lauryl sulphate as release medium, precision takes the prepared acetaminophen compound slow-releasing granules of embodiment 1～4 appropriate (approximately 100mg) respectively, measure according to Pharmacopoeia of the People's Republic of China version appendix XD first method in 2010, measure peak area with the HPLC method, calculate drug level and cumulative release percentage rate.Measurement result sees Table 1.
Table 1 embodiment 1～4 acetaminophen compound slow-releasing granules release investigation table (dissolution medium: 0.25% sodium lauryl sulphate)
| ? | 1h | 2h | 4h | 8h | 12h | 16h | 20h | 24h |
| Embodiment 1 | 17.3% | 37.5% | 56.2% | 74.6% | 88.1% | 100.1% | ? | ? |
| Embodiment 2 | 15.8% | 30.0% | 48.7% | 64.2% | 78.9% | 91.1% | 100.0% | ? |
| Embodiment 3 | 19.0% | 39.3% | 60.5% | 81.8% | 95.4% | 100.2% | ? | ? |
| Embodiment 4 | 18.1% | 36.9% | 55.4% | 75.3% | 89.6% | 100.0% | ? | ? |
As can be seen from Table 1, the prepared slow-releasing granules rate of release of embodiment 1～4 is suitable, and release is steady, can keep the medicine effective blood drug concentration of long period, reduces medicining times; Wherein the slow-releasing granules of embodiment 2 slowly discharged in 20 hours, illustrated and used carboxymethylethylcellulose to be slow-release material, used ethyl oleate to be the made acetaminophen compound slow-releasing granules best results of plasticizer.
The preparation of embodiment 5～7 acetaminophen compound slow-releasing granules
The supplementary material of according to the form below, by above-mentioned preparation method, each embodiment makes respectively the acetaminophen compound slow-releasing granules.The slow-release material of embodiment 5 and the weight ratio of plasticizer are 5:1, and the slow-release material of embodiment 6 and the weight ratio of plasticizer are 4:1, and the slow-release material of embodiment 7 and the weight ratio of plasticizer are 3:1.
The acetaminophen compound slow-releasing granules drug release determination of test example 2 embodiment 5～7 gained
Assay method is with test example 1.Measurement result sees Table 2.
Table 2 embodiment 5～7 acetaminophen compound slow-releasing granules release investigation table (dissolution mediums: 0.25% sodium lauryl sulphate)
| ? | 1h | 2h | 4h | 8h | 12h | 16h | 20h | 24h |
| Embodiment 5 | 16.9% | 33.5% | 51.2% | 69.3% | 82.4% | 95.6% | 100.0% | ? |
| Embodiment 6 | 14.5% | 28.1% | 44.8% | 59.7% | 73.2% | 82.9% | 91.0% | 100.1% |
| Embodiment 7 | 17.6% | 35.2% | 52.9% | 68.4% | 81.1% | 92.3% | 100.0% | ? |
As known from Table 2; the acetaminophen compound slow-releasing granules of embodiment 6 slowly discharged in 24 hours; illustrate when using carboxymethylethylcellulose to be slow-release material; use ethyl oleate to be plasticizer; when the ratio of slow-release material and the weight of plasticizer was 4:1, the slow release effect of prepared acetaminophen compound slow-releasing granules slow release was best.
Claims (6)
1. acetaminophen compound slow-releasing granules is comprised of immediate-release granules core and the sustained release coating layer that is wrapped in immediate-release granules core outside; Described immediate-release granules core is comprised of acetaminophen, pseudoephedrine hydrochloride, dextromethorphan hydrobromide, chlorphenamine maleate and filler, wherein, acetaminophen, pseudoephedrine hydrochloride, dextromethorphan hydrobromide, chlorphenamine maleate are active component; Described sustained release coating layer is comprised of slow-release material, plasticizer, porogen and antiplastering aid; It is characterized in that, by ratio of weight and the number of copies note:
Wherein, acetaminophen, pseudoephedrine hydrochloride, dextromethorphan hydrobromide, the chlorphenamine maleate weight ratio as active component is 22:2:1:0.15.
2. according to acetaminophen compound slow-releasing granules claimed in claim 1, it is characterized in that: the weight ratio of slow-release material and plasticizer is 5:1～3:1.
3. according to acetaminophen compound slow-releasing granules claimed in claim 2, it is characterized in that: the weight ratio of releasing material and plasticizer is 4:1.
4. according to acetaminophen compound slow-releasing granules claimed in claim 1, it is characterized in that: described filler is silicified microcrystalline cellulose; Described slow-release material is carboxymethylethylcellulose or ethyl cellulose; Described plasticizer is sodium lauryl sulphate or ethyl oleate; Described porogen is Macrogol 4000; Described antiplastering aid is glyceryl monostearate.
5. according to acetaminophen compound slow-releasing granules claimed in claim 4, it is characterized in that: described slow-release material is carboxymethylethylcellulose; Described plasticizer is ethyl oleate.
6. prepare the method for the described acetaminophen compound slow-releasing granules of claim 1～5 any one, comprise the following steps:
(1) get acetaminophen, pseudoephedrine hydrochloride, dextromethorphan hydrobromide, chlorphenamine maleate and filler mix homogeneously, take 85% ethanol as binding agent, make 10～14 purpose immediate-release granules cores, standby;
(2) with 80% dissolve with ethanol slow-release material, plasticizer, porogen, antiplastering aid, make sustained release coating liquid;
(3) the sustained release coating liquid for preparing evenly is sprayed at the immediate-release granules wicking surface that step (1) prepares, obtains the acetaminophen compound slow-releasing granules after drying.
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1511514A (en) * | 2002-12-27 | 2004-07-14 | 上海兴康医药研究开发有限公司 | Acetaminophen granule with slow releasing action and its preparing method |
| CN1589782A (en) * | 2003-08-28 | 2005-03-09 | 安徽省新药研究院 | Dimethyl biguanidine hydrochloride slow release particle and its preparation method |
| CN1634060A (en) * | 2004-10-11 | 2005-07-06 | 贵阳云岩西创药物科技开发有限公司 | Gelatin formulation of dextromethorphan hydrobromide and its preparing method |
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1511514A (en) * | 2002-12-27 | 2004-07-14 | 上海兴康医药研究开发有限公司 | Acetaminophen granule with slow releasing action and its preparing method |
| CN1589782A (en) * | 2003-08-28 | 2005-03-09 | 安徽省新药研究院 | Dimethyl biguanidine hydrochloride slow release particle and its preparation method |
| CN1634060A (en) * | 2004-10-11 | 2005-07-06 | 贵阳云岩西创药物科技开发有限公司 | Gelatin formulation of dextromethorphan hydrobromide and its preparing method |
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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. |
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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. |