CN100544722C - The levodropropizine pharmaceutical composition that uses in a kind of oral cavity - Google Patents

The levodropropizine pharmaceutical composition that uses in a kind of oral cavity Download PDF

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Publication number
CN100544722C
CN100544722C CNB200610032393XA CN200610032393A CN100544722C CN 100544722 C CN100544722 C CN 100544722C CN B200610032393X A CNB200610032393X A CN B200610032393XA CN 200610032393 A CN200610032393 A CN 200610032393A CN 100544722 C CN100544722 C CN 100544722C
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levodropropizine
oral cavity
magnesium stearate
buccal tablet
gelatine size
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CN101161240A (en
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朱志宏
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Hunan Jiudian Pharmaceutical Co Ltd
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Abstract

The invention provides a kind of novel form of levodropropizine, by levodropropizine and corresponding auxiliary material form can be in the oral cavity buccal and slow dissolved buccal tablet.The present invention has to make the effective ingredient levodropropizine medicine that works be stranded in lesions position, and drug level increases relatively in the oral cavity partial scope, so advantages such as relative prolongations action time.

Description

The levodropropizine pharmaceutical composition that uses in a kind of oral cavity
Invention field
The invention belongs to the chemical drugs invention field, relate to the pharmaceutical composition that a kind of main component is a levodropropizine, promptly a kind of novel form of the levodropropizine that in the oral cavity, uses.
Background technology
Cough is a kind of common clinical, and the common anti-tussitives multiaction is in maincenter, as opiates narcoticness cough medicine morphine, codeine etc. at present; Non-narcotic analgesics such as dromethan, Glaucine, pentoxyverine, ASA-158/5 etc.; Though suchlike cough medicine kind is many, how unsatisfactory curative effect is, and side effect is very big.Someone thinks, comparatively ideal cough medicine should reduce sensorineural sensitivity in the lung, and blocking-up has the sensory nerve conduction (as the local anaesthesia medicine) in myelin or the nonmedullated nerve, but the local anaesthesia medicine has the lung of inhibition protective reflex and brings out side effect such as bronchoconstriction.
By gondola Dompe company (commodity be called Levotuss) and Mediolanum company (trade name Danka) exploitation, in Italy go on the market the earliest by in October, 1988 for levodropropizine, is used for the treatment of all kinds cough, is a kind of peripheral antitussive drugs.Levodropropizine is a chipal compounds, does not almost have the maincenter sedation of its raceme dropropizine and analog antitussive thereof, and the cardiovascular system respiratory system of unifying is not produced any obvious effect, its better tolerance, and no drug dependence and stability are high.The domestic levodropropizine preparation that has gone on the market has conventional tablet, capsule, oral liquid etc. at present.Yet conventional tablet and capsule are unfavorable for old man or child and swallow, though oral liquid taking convenience but character are not very stable relatively and store trouble, dosage and pharmacokinetics character are not as capsule and tablet, so the inventor has invented a kind of new dosage form at this Study of Defects, i.e. buccal or the levodropropizine pharmaceutical composition chewed in the oral cavity, can make medicine be stranded in lesions position, drug level increases relatively, prolong action time relatively, thereby reach the minimizing drug dose, be easy to absorb, the holding time is long and improve the purpose of therapeutic effect.
Summary of the invention
Purpose of the present invention aims to provide a kind of pharmaceutical composition of levodropropizine, and a kind of novel form of the levodropropizine that can use in the oral cavity has and can make medicine be stranded in lesions position, and drug level increases relatively, and action time is advantage such as prolongation relatively.
Levodropropizine pharmaceutical composition of the present invention is by levodropropizine and be used to suck the chemical medicine thing and prepare required corresponding adjuvant and form.
The weight ratio of levodropropizine pharmaceutical composition levodropropizine of the present invention and adjuvant is a levodropropizine 5~20%, and adjuvant is 95~80%.
The used adjuvant of levodropropizine pharmaceutical composition of the present invention is made up of in diluent, correctives, binding agent, the lubricant one or more.
Diluent can be one or more the mixture in cane sugar powder, mannitol, calcium sulfate two water things, lactose, starch, pregelatinized Starch, dextrin, microcrystalline Cellulose, magnesium oxide, magnesium carbonate, the calcium carbonate.
Correctives can be one or more the mixture in Mentholum, protein sugar, cane sugar powder, mannitol, citric acid, cyclodextrin glucose oligomer, the various natural or artificial essence.
Binding agent can be one or more the mixture in starch slurry, dextrin, hydroxypropyl methylcellulose, hydroxypropyl cellulose, methylcellulose, polyvinylpyrrolidone, acrylic resin, mucialga of arabic gummy, gelatine size, the microcrystalline Cellulose.
Lubricant can be one or more the mixture in magnesium stearate, Pulvis Talci, micropowder silica gel, Macrogol 4000, the magnesium laurylsulfate.
Above-mentioned various adjuvant and consumption thereof are selected according to preparation method and subjective demand, with reference to open source information and use the prior art of this professional field can obtain the pharmaceutical composition of gratifying levodropropizine, this medicine uses in the oral cavity, every day three times, twice medication interval should be more than 6 hours.
The specific embodiment
Embodiment 1:
Supplementary material g
Levodropropizine 60
Protein sugar 120
Cane sugar powder 900
Hydroxypropyl methylcellulose (15cp) 5
Mentholum 15
Magnesium stearate 5
70% ethanol is an amount of
With the supplementary material pulverize separately, sieve, standby.Take by weighing supplementary material by recipe quantity.With adjuvant (except magnesium stearate and the Mentholum) mixing, add the levodropropizine mixing more earlier.Ethanol system soft material with 70% is granulated, and 50~55 ℃ were toasted about 2 hours, and the granulate that sieves adds the magnesium stearate mixing, sprays into Mentholum 95% alcoholic solution, seals about 6 hours promptly.1000 of tablettings.
Test example 1: Bioavailability of Human Body development test
Test objective: the relative bioavailability that is intended to study Levodropropizine lozenge.
Content of the test: adopt binary cycle to intersect (2 * 2) EXPERIMENTAL DESIGN at random, 18 experimenters are divided into 2 groups at random, every group 9 people.Every group of experimenter takes the Levodropropizine lozenge sample of embodiment 1 gained according to testing program and as the levodropropizine sheet that has gone on the market (specification is the conventional tablet of 60mg/ sheet) of reference preparation in different tests.
Result of the test: the main pharmacokinetic parameter C of reference preparation and test preparation Max, T Max, AUC 0 → 12And AUC 0 → ∞(mean ± standard deviation) is respectively: 200.1 ± 25.9 and 228.4 ± 31.7ng/ml; 0.67 ± 0.18 and 0.76 ± 0.23h; 624.8 ± 134.6 and 654.4 ± 128.0ng.h/ml; 674.2 ± 151.8 and 687.2 ± 156.2ng.h/ml.T MaxThrough the Mann-Whitney check, different preparation differences do not have significance, C Max, AUC 0 → 12And AUC 0 → ∞After to number conversion, carry out variance analysis, the result shows that both do not have the significance meaning with the different cycles differences between different preparations.Test preparation to the relative bioavailability F of reference preparation (with AUC 0 → 12As estimating foundation) be 101% ± 6%, this shows that both have bioequivalence when dosage is identical.
Embodiment 2
Supplementary material g
Levodropropizine 60
Beta-schardinger dextrin-200
Lactose 30
Steviosin 8
Magnesium stearate 4
5% gelatine size is an amount of
With the supplementary material pulverize separately, sieve, standby; Take by weighing supplementary material by recipe quantity; Beta-schardinger dextrin-adding levodropropizine soluble in water is ground to form pasty state, and oven dry is pulverized, and sieves; With said mixture and all the other auxiliary materials and mixing (except the magnesium stearate), add gelatine size, granulate, baking, granulate adds magnesium stearate, mixing; 1000 of tablettings.
Embodiment 3
Supplementary material g
Levodropropizine 60
Starch 360
Sucrose 60
Polyvinylpyrrolidone 5
Pulvis Talci 5
5% gelatine size is an amount of
With the supplementary material pulverize separately, sieve, standby; Take by weighing supplementary material by recipe quantity; Starch adding levodropropizine soluble in water is ground to form pasty state, and oven dry is pulverized, and sieves; With said mixture and all the other auxiliary materials and mixing, add gelatine size, granulate baking, granulate, 1000 of tablettings.

Claims (2)

1, a kind of buccal tablet of levodropropizine, it is an amount of to it is characterized in that every of described buccal tablet contains levodropropizine 60mg, beta-schardinger dextrin-200mg, lactose 30mg, steviosin 8mg, magnesium stearate 4mg and 5% gelatine size.
2, levodropropizine buccal tablet according to claim 1 is characterized in that this buccal tablet is to be prepared from by following method:
A, to take by weighing levodropropizine 60g, beta-schardinger dextrin-200g, lactose 30g, steviosin 8g, magnesium stearate 4g and 5% gelatine size an amount of;
B, with supplementary material pulverize separately except that 5% gelatine size that A step is taken by weighing, sieve, standby;
C, beta-schardinger dextrin-is soluble in water adds levodropropizine and grinds to form pasty state, and oven dry is pulverized, and sieves;
D, C is gone on foot gained mixture and lactose, steviosin mixing, it is an amount of to add 5% gelatine size, granulate, and baking, granulate adds magnesium stearate, mixing again; Tabletting becomes 1000 of buccal tablets of the present invention.
CNB200610032393XA 2006-10-12 2006-10-12 The levodropropizine pharmaceutical composition that uses in a kind of oral cavity Active CN100544722C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CNB200610032393XA CN100544722C (en) 2006-10-12 2006-10-12 The levodropropizine pharmaceutical composition that uses in a kind of oral cavity

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CNB200610032393XA CN100544722C (en) 2006-10-12 2006-10-12 The levodropropizine pharmaceutical composition that uses in a kind of oral cavity

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CN101161240A CN101161240A (en) 2008-04-16
CN100544722C true CN100544722C (en) 2009-09-30

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Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101766583B (en) * 2008-12-29 2012-11-28 北京德众万全药物技术开发有限公司 Medicinal effervescent tablet for treating cough and preparation method thereof
EP3673902B1 (en) * 2012-02-19 2022-01-05 Quest Products, LLC Alkalized acacia gum adhesive for oral adhering discs
CN103381272A (en) * 2012-05-03 2013-11-06 贵州大学 Method for improving levodropropizine taste by cyclodextrin clathration
CN103381145A (en) * 2012-05-03 2013-11-06 贵州大学 Method for improving levodropropizine taste by solid dispersion
TR201722102A2 (en) * 2017-12-27 2019-07-22 Biofarma Ilac Sanayi Ve Ticaret Anonim Sirketi A Pharmaceutical Product Containing Levodropropizine

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