CN1535686A - Slowly-released preparation containing loratadine and pseudoephedrine sulfate and its preparation method - Google Patents

Slowly-released preparation containing loratadine and pseudoephedrine sulfate and its preparation method Download PDF

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Publication number
CN1535686A
CN1535686A CNA031094023A CN03109402A CN1535686A CN 1535686 A CN1535686 A CN 1535686A CN A031094023 A CNA031094023 A CN A031094023A CN 03109402 A CN03109402 A CN 03109402A CN 1535686 A CN1535686 A CN 1535686A
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CN
China
Prior art keywords
loratadine
sheet
pseudoephedrine sulfate
slow
sulfate
Prior art date
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Pending
Application number
CNA031094023A
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Chinese (zh)
Inventor
宿彦伟
张颖
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Beijing Dezhong Wanquan Medicines Technological Development Co Ltd
Original Assignee
Beijing Dezhong Wanquan Medicines Technological Development Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Beijing Dezhong Wanquan Medicines Technological Development Co Ltd filed Critical Beijing Dezhong Wanquan Medicines Technological Development Co Ltd
Priority to CNA031094023A priority Critical patent/CN1535686A/en
Publication of CN1535686A publication Critical patent/CN1535686A/en
Pending legal-status Critical Current

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention relates to a slowly-released preparation containing loratadine and ephedrine sulfate and its preparation method. It adopts compression coating method to compress the slowly-releasing external layer on the exterior of slowly-releasing tablet core to obtain the invented compression-coated slowly-released tablet mainly for clinically-relieving rhinallergosis and nasal obstruction due to common cold.

Description

A kind of slow releasing preparation that contains loratadine and pseudoephedrine sulfate and preparation method thereof
Technical field
The invention relates to a kind of new prescription composition and preparation method of slow releasing tablet that is used to alleviate allergic rhinitis and cold symptoms clinically.
Loratadine is a kind of long lasting tricyclic antidepressants antihistamine drug, clinical showing, its selectively acting is in the periphery histamine H1-receptor, no central nervous system's inhibitory action, therefore the antihistaminic that belongs to no drowsiness effect was taken once and then can effectively be alleviated allergic rhinitis in one day; Pseudoephedrine sulfate is traditional sympathomimetic amine, takes four times in one day, can effectively suppress nasal mucosa hyperemia.Both effectively combine, make and took twice slow releasing preparation in one day, can bring into play the antihistamine effect of loratadine and the dual function that alleviates nasal congestion of pseudoephedrine sulfate simultaneously, the related symptoms that also permanent rapidly alleviation allergic rhinitis and flu cause, few side effects, and taking convenience.
Background technology
The development and production of Schering Plough pharmaceutical Co. Ltd the product of commodity CLARITIN-D by name, CLARITIN-D 12HOUR and two kinds of specifications of CLARITIN-D 24 HOUR are arranged, obtain import drugs in China in 1999 and produce certification (CLARITIN-D 12HOUR), by the packing listing of Shanghai Schering Plough pharmaceutical Co. Ltd, commodity are called Clarinase, its specification is loratadine 5mg, pseudoephedrine sulfate 120mg, form by label and coatings two parts, coatings is an immediate release section, sulfur acid pseudoephedrine 60mg, loratadine 5mg, discharge the performance drug effect after taking medicine immediately, and kept 6 hours; Label is a slow-released part, and sulfur acid pseudoephedrine 60mg can begin to disengage taking medicine in back 6 hours, continue to keep back 6 hours drug effect, and loratadine itself is exactly the long-acting type medicine, can 12 hours effective relief of symptoms after taking.
Schering Corp China and U. S. application the patent of CLARITIN-D 24 HOUR, the patent No. is respectively 93,118, and 769 and 5,314,697, specification is pseudoephedrine sulfate 240mg, loratadine 10mg, pseudoephedrine sulfate is a slow-released part, in the matrix type label, loratadine is an immediate release section, adopts the coating mode to be wrapped in outside the label.
The main adjuvant of CLARITIN-D 12 HOUR has that lactose, starch, polyvinylpyrrolidone, arabic gum, microcrystalline Cellulose, sucrose, calcium sulfate, white beeswax, babassu are cured, Pulvis Talci and magnesium stearate etc.Its label is surrounded by wax material outward, delays the release of medicine; Immediate release drug is in coatings, and outermost layer is a sugarcoating layer.
Because the pseudoephedrine sulfate specification is bigger in the skin, and the loratadine specification is 5mg, by the coating wayward uniformity of dosage units of adding medicine to, and sugar coating length consuming time, production efficiency is low.
Goal of the invention
Because the coating sheeting equipment of external existing molding, domestic also have producer successfully to copy this pressed coated equipment, and we study adjustment to prescription, adopts the method for pressed coated to prepare slow releasing tablet.Adopt pressed coated technology, not only can solve the gentle problem of releasing of rapid release in the preparation, and can better solve the uniformity problem of clothing layer Chinese medicine, enhance productivity.
Detailed Description Of The Invention
The commodity that we produce with reference to Schering-Plough company are called the specification of CLARITIN-D 12 HOUR, and prescription is adjusted, and adopt the method for pressed coated to prepare slow releasing tablet, and the sheet core segment is a slow-released part, sulfur acid pseudoephedrine 60mg; Compacting clothing layer segment is immediate release section, contains loratadine 5mg, pseudoephedrine sulfate 60mg.
Adopting polymethylacrylic acid latex (gastric disintegrable type, 30%) is binding agent, is easy to granulate; Glyceryl Behenate plays the retardance slow releasing function; Hypromellose E50-LV regulates the outer field release of slow releasing tablet, improves slice, thin piece hardness simultaneously; Sucrose plays the bonding agent effect; Calcium sulfate, lactose are filler; Magnesium stearate is a lubricant.
1. prescription is formed:
(1) immediate release section is outer forms:
The mg/ sheet
Loratadine 5
Pseudoephedrine sulfate 60
Hypromellose E50-LV 75
Sucrose 15
Lactose 137
Magnesium stearate 3
(2) the slow-released part label is formed:
The mg/ sheet
Pseudoephedrine sulfate 60
Glyceryl Behenate 140
Calcium sulfate 20
Latex liquid of polymethacrylic resin (30%) 10
Magnesium stearate 2
(3) slow releasing tablet is formed:
The mg/ sheet
Slow-released part label 232
Immediate release section skin 295
2. preparation technology:
(1) sheet core segment: in the prescription ratio, with principal agent and adjuvant pulverize, sieve, behind the mixing, with latex liquid of polymethacrylic resin system soft material, the granulation of sieving, oven dry back add the magnesium stearate mixing, and be standby.
(2) preparation of coatings part is with the sheet core segment.Principal agent and adjuvant are sieved, behind the mixing, granulate with 60% alcoholic solution, and the oven dry back adds the magnesium stearate mixing, and is standby.
(3) adopt the pressed coated machine to carry out tabletting, label 232mg, outer 295mg, the heavy 527mg of theoretical sheet.
Embodiment
1. prescription is formed
(1) the outer layer segment of rapid release is formed:
The mg/ sheet
Loratadine 5
Pseudoephedrine sulfate 60
Hypromellose E50-LV 85
Sucrose 16
Lactose 132
Magnesium stearate 2
(2) the slow releasing tablet core segment is formed:
The mg/ sheet
Pseudoephedrine sulfate 60
Glyceryl Behenate 130
Calcium sulfate 30
Latex liquid of polymethacrylic resin (30%) 12
Magnesium stearate 3
(3) slow releasing tablet is formed:
The mg/ sheet
Slow releasing tablet core segment 235
The outer layer segment 300 of rapid release
2. preparation technology:
(1) sheet core segment: in the prescription ratio, with principal agent and adjuvant pulverize, sieve, behind the mixing, with latex liquid of polymethacrylic resin system soft material, the granulation of sieving, oven dry back add the magnesium stearate mixing, with 8mm scrobicula punching press film-making core.
(2) preparation of pressed coated layer segment is with the sheet core segment.Principal agent and adjuvant are sieved, behind the mixing, granulate with 60% alcoholic solution, and the oven dry back adds the magnesium stearate mixing, and is standby.
(3) pressed coated: adopt pressed coated machine 11mm scrobicula punching press system coating.Label 235mg, outer 300mg, the heavy 535mg of theoretical sheet.
3. drug release determination
Slow releasing tablet with reference to above-mentioned prepared, according to drug release determination method (two appendix XD first methods of Chinese Pharmacopoeia version in 2000), adopt dissolution method (two appendix XC first methods of Chinese Pharmacopoeia version in 2000) device, with 0.01mol/L hydrochloric acid solution 900ml is solvent, rotating speed is that per minute 100 changes, sampling and measuring, release is table 1 as a result, and 2.The result shows, self-control slow releasing tablet and comparison film release behavior basically identical.
Table 1 pseudoephedrine sulfate drug release determination result (%)
Time
Sample 123456 average ± SD
(hour)
0.5 45.8 43.3 44.0 45.1 42.4 46.9 44.6±1.67
1 47.6 49.0 50.9 50.0 47.9 48.4 49.0±1.25
2 50.4 52.2 56.2 56.9 51.2 50.8 52.9±2.85
From
4 58.0 64.2 64.3 64.6 63.9 58.7 62.3±3.06
System
6 68.8 79.4 77.0 77.3 79.1 67.5 74.9±5.28
Sheet
8 79.4 89.7 88.3 89.1 90.2 76.8 85.6±5.89
10 88.3 94.3 93.5 94.4 95.6 85.0 91.9±4.21
12 89.5 94.3 95.1 94.6 93.4 89.1 92.7±2.67
0.5 51.4 53.7 43.5 46.8 48.1 45.1 48.1±3.88
1 53.1 53.8 46.7 51.0 50.0 51.2 51.0±2.53
2 52.7 52.5 46.2 48.9 51.1 51.6 50.5±2.51
Right
4 55.1 56.9 48.9 55.8 53.8 52.6 53.8±2.85
According to
6 72.7 59.6 69.6 70.6 64.4 61.9 66.5±5.26
Sheet
8 93.4 82.0 90.4 93.3 80.9 80.8 86.8±6.20
10 97.2 94.1 96.6 98.3 90.8 95.1 95.4±2.70
12 101.1 105.4 96.6 101.8 101.7 100.3 101.1±2.83
Remarks: comparison film is Clarinase , by the packing of Shanghai Schering Plough pharmaceutical Co. Ltd.Lot number: 01CJRPD002
Table 2 loratadine drug release determination result (%)
Time
Sample 123456 average ± SD
(little
The time)
0.5 71.3 68.2 75.6 75.2 69.3 72.4 72.0±2.99
1 92.0 95.0 97.6 98.6 95.6 93.3 95.3±2.49
2 95.1 97.6 100.0 100.5 98.3 95.7 97.9±2.20
From
4 96.2 95.8 98.8 99.9 96.9 96.0 97.3±1.71
System
6 95.4 96.7 97.3 99.0 97.3 96.4 97.0±1.19
Sheet
8 93.7 94.3 95.4 96.7 96.1 94.9 95.2±1.14
10 93.1 98.2 97.4 98.1 98.6 93.8 96.5±2.43
12 95.1 93.9 98.1 99.1 95.5 95.9 96.3±1.95
0.5 85.7 89.6 84.3 83.7 85.1 72.0 83.4±5.96
1 96.3 98.6 92.8 97.0 92.0 82.5 93.2±5.83
To 2 93.4 95.5 94.3 96.9 93.5 97.0 95.1 ± 1.62
According to 4 99.8 99.5 95.6 96.9 93.5 98.0 97.2 ± 2.43
Sheet 6 99.5 98.8 99.0 98.0 94.6 97.2 97.8 ± 1.79
8 100.8 99.6 99.5 98.9 94.6 96.3 98.3±2.35
10 100.2 99.7 99.5 100.2 95.0 97.4 98.7±2.06
12 100.6 99.9 98.4 99.5 95.2 97.7 98.6±1.97
Remarks: comparison film is Clarinase , by the packing of Shanghai Schering Plough pharmaceutical Co. Ltd.Lot number: 01CJRPD002

Claims (2)

1. a slow releasing tablet that contains loratadine and pseudoephedrine sulfate is made up of immediate release section skin and slow-released part label, and wherein the immediate release section skin comprises loratadine and pseudoephedrine sulfate, and the slow-released part label is a pseudoephedrine sulfate.
It is characterized by:
A. the slow-released part label is formed:
The mg/ sheet
Pseudoephedrine sulfate 40-80
Glyceryl Behenate 94-186
Calcium sulfate 13-27
Latex liquid of polymethacrylic resin (30%) 6-14
Magnesium stearate 1.3-2.7
B. the outer field composition of immediate release section:
The mg/ sheet
Loratadine 5
Pseudoephedrine sulfate 40-80
Hypromellose E50-LV 56-104
Sucrose 11-19
Lactose 91-183
Magnesium stearate 1.5-3.5
Sheet core segment and coatings are partly separately granulated separately, and be standby.Adopt the pressed coated machine to carry out compressed tablets.
2. contain loratadine 5mg in the immediate release section skin described in the claim 1, pseudoephedrine sulfate 60mg, sulfur acid pseudoephedrine 60mg in the slow-released part label.
A. the slow-released part label is formed:
The mg/ sheet
Pseudoephedrine sulfate 60
Glyceryl Behenate 140
Calcium sulfate 20
Latex liquid of polymethacrylic resin (30%) 10
Magnesium stearate 2
B. the outer field composition of immediate release section:
The mg/ sheet
Loratadine 5
Pseudoephedrine sulfate 60
Hypromellose E50-LV 75
Sucrose 15
Lactose 137
Magnesium stearate 3
Sheet core segment and coatings are partly separately granulated separately, adopt the pressed coated machine to carry out compressed tablets.
CNA031094023A 2003-04-09 2003-04-09 Slowly-released preparation containing loratadine and pseudoephedrine sulfate and its preparation method Pending CN1535686A (en)

Priority Applications (1)

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Publications (1)

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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101596157A (en) * 2008-06-04 2009-12-09 北京科信必成医药科技发展有限公司 The compound slow release preparation of a kind of pseudoephedrine, chlorphenamine and dextromethorphan
CN101596156B (en) * 2008-06-04 2011-09-28 北京科信必成医药科技发展有限公司 Compound sustained-release preparation for paracetamol and pseudoephedrine
CN102247368A (en) * 2011-05-19 2011-11-23 安徽永生堂药业有限责任公司 Compound acrivastine sustained release tablets, and preparation method thereof
CN102283849A (en) * 2011-06-29 2011-12-21 北京阜康仁生物制药科技有限公司 Medicinal composition containing azatadine
CN101015519B (en) * 2007-02-27 2012-03-21 重庆医药工业研究院有限责任公司 Loratadine oral compound medication composition

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101015519B (en) * 2007-02-27 2012-03-21 重庆医药工业研究院有限责任公司 Loratadine oral compound medication composition
CN101596157A (en) * 2008-06-04 2009-12-09 北京科信必成医药科技发展有限公司 The compound slow release preparation of a kind of pseudoephedrine, chlorphenamine and dextromethorphan
CN101596156B (en) * 2008-06-04 2011-09-28 北京科信必成医药科技发展有限公司 Compound sustained-release preparation for paracetamol and pseudoephedrine
CN102247368A (en) * 2011-05-19 2011-11-23 安徽永生堂药业有限责任公司 Compound acrivastine sustained release tablets, and preparation method thereof
CN102283849A (en) * 2011-06-29 2011-12-21 北京阜康仁生物制药科技有限公司 Medicinal composition containing azatadine

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