CN101491524A - Medicine combination capable of improving cetirizine preparation stability - Google Patents
Medicine combination capable of improving cetirizine preparation stability Download PDFInfo
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- CN101491524A CN101491524A CNA2008100032948A CN200810003294A CN101491524A CN 101491524 A CN101491524 A CN 101491524A CN A2008100032948 A CNA2008100032948 A CN A2008100032948A CN 200810003294 A CN200810003294 A CN 200810003294A CN 101491524 A CN101491524 A CN 101491524A
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- cetirizine
- stabilizing agent
- levo
- pharmaceutically acceptable
- alkali compounds
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Abstract
The invention discloses an oral preparation composition prepared by being matched with an alkaline compound taken as a stabilizing agent in cetirizine. The stability of an oral preparation added with the stabilizing agent is greatly improved.
Description
Technical field
The invention provides a kind of pharmaceutical composition that can improve the cetirizine preparation stability, relate to the technical field of improving cetirizine preparation medicine stability.
Background technology
Cetirizine (cetirizine) is the long-acting amine H1 of peripheral tissues receptor antagonist.Pharmacological evaluation shows that it has higher pharmacologically active to allergic rhinitis, pollenogenic asthma, chronic urticaria and some other physical urticaria.Simultaneously, reduced penetration power, to central nervous system's side effect minimizing to blood brain barrier.
As document " cetirizine hydrochloride and adjuvant Study of Interaction " (Zhang Ziran, Jiang Lingtao. West China pharmaceutical journal .2002,17 (5): report 394～395): because cetirizine has higher chemism, there is multiple adjuvant can not tolerate its chemism under high temperature, illumination acceleration environment or in the long-term storage process and the chemical stain phenomenon takes place, cause the medicine related substance to increase.This is the unstable and phenomenon that causes of cetirizine raw material itself no thanks to.Other increases has document announcement lactose and primary amine compounds to take place to interact and variable color, and they have directly influenced the outward appearance and the inherent quality of preparation.
At present, solve cetirizine oral formulations quality stability problem, mainly by avoiding as much as possible using and its generation bigger adjuvant that interacts, use some interact less or not with its generation interaction adjuvant, this is being subjected to certain limitation to the especially exploitation of novel form of formulation development of cetirizine aspect selection of adjuvant.
Summary of the invention
The object of the present invention is to provide a kind of compositions that can improve the cetirizine preparation stability of energy, solve the preparation of cetirizine oral formulations and be subjected to the restriction of adjuvant, the problem of quality stability difference.
We add the chemism that alkali compounds can reduce cetirizine at unexpected discovery the in the oral formulations process of development cetirizine, reduce the interaction of itself and adjuvant, improve the stability of its oral formulations.
That is, the present invention is the alkali compounds that adds in the cetirizine preparation as stabilizing agent, it is characterized in that, comprises cetirizine or its pharmaceutically acceptable salt and at least a alkali compounds as stabilizing agent.Its described cetirizine (comprising its pharmaceutically acceptable salt) is 1: 0.1～5 with the alkali compounds weight ratio, preferentially selecting cetirizine (comprising its pharmaceutically acceptable salt) and alkali compounds weight ratio for use is 1: 0.2～2, add other proper quantity of medicinal auxiliary material again, form a kind of new cetirizine pharmaceutical preparation.The use level that each component of pharmaceutic adjuvant is can be according to different dosage form selection suitable does not have special qualification to this.
Wherein described cetirizine or its pharmaceutically acceptable salt comprise its levo form, d-isomer and raceme.
Stabilizing agent recited above is an alkali compounds, at least a as in carbonate, bicarbonate, the hydroxide, and wherein embodiment of the present invention is preferably used is a kind of in sodium carbonate, sodium bicarbonate, the sodium hydroxide or is used in combination.
From preparation prescription of the present invention, can produce the oral formulations of various dosage forms,, for example, powder, granule, granula subtilis, tablet, dry syrup, capsule, oral cavity disintegration tablet etc. be arranged as preparation.These preparations can utilize the conventional method in this technical field, as methods such as pulverizing, classification, mixing (dosing), mixing, pelletize, drying, granulate, tablettings.As above-mentioned preparation, needs according to different dosage form, can also add arbitrarily different pharmaceutically acceptable pharmaceutic adjuvants, comprising (but being not limited to): diluent/filler: microcrystalline Cellulose, lactose, mannitol, erythrose, dextrin, sucrose, dextran, sorbitol, glycine; Disintegrating agent: low-substituted hydroxypropyl cellulose, carboxymethyl starch sodium, crospolyvinylpyrrolidone, cross-linking sodium carboxymethyl cellulose etc.; Binding agent: polyvinylpyrrolidone, hydroxypropyl cellulose, gelatin, xanthan gum, arabic gum, methylcellulose, carboxymethyl cellulose, polyvinyl alcohol, Polyethylene Glycol, extra large bath acid, extra large bath hydrochlorate etc.; Correctives: sucralose, A Siba are sweet, glucide, stevioside, sucrose, acesulfame-K, essence etc.; Lubricant: magnesium stearate, calcium stearate, zinc stearate, stearic acid, sodium stearyl fumarate, sodium laurylsulfate, lauryl alcohol sulfate sulfatase magnesium, hydrogenated castor wet goods.
Inventor of the present invention is by adding the product of stabilizing agent (following mask body embodiment) and two kinds of different formulation that do not add stabilizing agent (as following comparative example), through two kinds of products being carried out the stability test examination, the experimental data that obtains shows, it is good to add the product stability that stabilizing agent makes, and the product that does not add stabilizing agent all has degraded in various degree in process of the test.
The specific embodiment:
Embodiment 1
With 5g levo-cetirizine hydrochloride (levo form), 70g microcrystalline Cellulose, 40g mannitol, 30g crospolyvinylpyrrolidone, 5g sucralose, 2.0g sodium bicarbonate mix homogeneously, spray purified water and carry out pelletize in right amount, dried granule adds the 0.75g magnesium stearate, fully mix, make levo-cetirizine hydrochloride orally disintegrating tablets.
Embodiment 2
With 10g cetirizine hydrochloride (raceme), 40g microcrystalline Cellulose, 850g pregelatinized Starch, 2.2g sodium carbonate, 4.5g stevioside mix homogeneously, spray an amount of pelletize of polyvinylpyrrolidonesolution solution, make the cetirizine hydrochloride granule.
Embodiment 3
With 5g levo-cetirizine hydrochloride (levo form), 60g microcrystalline Cellulose, 60g lactose, 1.5g sodium bicarbonate, 1.0 sodium carbonate mix homogeneously, spray purified water and carry out pelletize in right amount, dried granule adds the 1.3g magnesium stearate, fully mixes, and makes the levo-cetirizine hydrochloride tablet.
Embodiment 4
With 10g cetirizine hydrochloride (raceme), 200g mannitol, 200g lactose, 10g sucralose, 2.6g sodium hydroxide mix homogeneously, spray methocel solution and carry out pelletize, dried granule adds 3g magnesium stearate and 3g straw essence, fully mixes, and makes chewing tablet of cetirizine hydrochloride.
Embodiment 5
With 5g levo-cetirizine hydrochloride (levo form), 70g microcrystalline Cellulose, 40g mannitol, 30g crospolyvinylpyrrolidone, 5g sucralose, 10g sodium bicarbonate mix homogeneously, spray purified water and carry out pelletize in right amount, dried granule adds the 0.75g magnesium stearate, fully mix, make levo-cetirizine hydrochloride orally disintegrating tablets.
Comparative example 1～4 is not except that adding in prescription the stabilizing agent alkali compounds, and all the other are identical with embodiment 1～4 respectively.
Comparative example 1
With 5g levo-cetirizine hydrochloride (levo form), 70g microcrystalline Cellulose, 40g mannitol, 30g crospolyvinylpyrrolidone, 5g sucralose mix homogeneously, spray purified water and carry out pelletize in right amount, dried granule adds the 0.75g magnesium stearate, fully mix, make levo-cetirizine hydrochloride orally disintegrating tablets.
Comparative example 2
With 10g cetirizine hydrochloride (raceme), 40g microcrystalline Cellulose, 850g pregelatinized Starch, 4.5g stevioside mix homogeneously, spray an amount of pelletize of polyvinylpyrrolidonesolution solution, make the cetirizine hydrochloride granule.
Comparative example 3
With 5g levo-cetirizine hydrochloride (levo form), 60g microcrystalline Cellulose, 60g lactose mix homogeneously, spray purified water and carry out pelletize in right amount, dried granule adds the 1.3g magnesium stearate, fully mixes, and makes the levo-cetirizine hydrochloride tablet.
Comparative example 4
With 10g cetirizine hydrochloride (raceme), 200g mannitol, 200g lactose, 10g sucralose mix homogeneously, spray methocel solution and carry out pelletize, dried granule adds 3g magnesium stearate and 3g straw essence, fully mixes, and makes chewing tablet of cetirizine hydrochloride.
EXPERIMENTAL DESIGN: this experiment with the various formulation products in example of formulations 1～5 of the present invention and the control formulation comparative example 1～4 in long term test (25 ℃ ± 2 ℃ of temperature, relative humidity 60% ± 10%) carry out stability test under the condition and investigate, 0 month and the contrast stability data after 24 months are as follows:
。
Claims (5)
1. pharmaceutical composition that improves the cetirizine preparation stability, said composition comprises cetirizine or its pharmaceutically acceptable salt and at least a alkali compounds as stabilizing agent.
2. the described compositions of claim 1 is characterized in that, described cetirizine or its pharmaceutically acceptable salt comprise its levo form, d-isomer and raceme.
3. the described compositions of claim 1 is characterized in that, employed stabilizing agent is an alkali compounds, at least a as in carbonate, bicarbonate, the hydroxide.
4. the described compositions of claim 1 is characterized in that, employed cetirizine or its pharmaceutically acceptable salt and alkali compounds weight ratio are 1: 0.1～5.
5. the described compositions of claim 1 is characterized in that, employed cetirizine or its pharmaceutically acceptable salt and alkali compounds weight ratio are 1: 0.2～2.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008100032948A CN101491524A (en) | 2008-01-26 | 2008-01-26 | Medicine combination capable of improving cetirizine preparation stability |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008100032948A CN101491524A (en) | 2008-01-26 | 2008-01-26 | Medicine combination capable of improving cetirizine preparation stability |
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| Publication Number | Publication Date |
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| CN101491524A true CN101491524A (en) | 2009-07-29 |
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| Application Number | Title | Priority Date | Filing Date |
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| CNA2008100032948A Pending CN101491524A (en) | 2008-01-26 | 2008-01-26 | Medicine combination capable of improving cetirizine preparation stability |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101669913B (en) * | 2009-09-25 | 2012-09-05 | 海南康芝药业股份有限公司 | Levocetirizine dihydrochloride granule and preparation and detection methods thereof |
-
2008
- 2008-01-26 CN CNA2008100032948A patent/CN101491524A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101669913B (en) * | 2009-09-25 | 2012-09-05 | 海南康芝药业股份有限公司 | Levocetirizine dihydrochloride granule and preparation and detection methods thereof |
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| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Open date: 20090729 |