CN1660098A - Combination of tablet to swallow of containing Cetirizine Hydrochloride - Google Patents
Combination of tablet to swallow of containing Cetirizine Hydrochloride Download PDFInfo
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- CN1660098A CN1660098A CN 200410036471 CN200410036471A CN1660098A CN 1660098 A CN1660098 A CN 1660098A CN 200410036471 CN200410036471 CN 200410036471 CN 200410036471 A CN200410036471 A CN 200410036471A CN 1660098 A CN1660098 A CN 1660098A
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- cyclodextrin
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- cetirizine
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Abstract
An orally-taken composite medicine containing cetirizine hydrochloride is prepared from cetirizine hydrochloride, cyclodextrin or its derivative, and flavouring. It features its agreeable taste.
Description
Technical field
The invention belongs to pharmaceutical preparations technology.
Background technology
In recent years, because the variation of weather and environment, the emerge in multitude of various harmful gass, dust and other polluter becomes it and causes people to produce various anaphylactoid sensitinogens.The transition in season, field work, pollen hypersensitivity, suck harmful gas and grit etc., cause increasing crowd to suffer from various dissimilar anaphylactic diseases, as allergic rhinitis, urticaria, the asthma that red swelling of the skin, pruritus, a red point and anaphylactogen cause etc. are very common.Therefore, note environmental change, strengthen that exploitation treatment anaphylaxis medicine all is very important from self nursing.
The treatment anaphylactic disease mainly contains cetirizine, teldane, astemizole, loratadine, acrivastine, levocabastine etc. based on antihistaminic at present.
Cetirizine has the following advantages as a kind of potent antiallergic agent:
1, potent antihistamine effect is discovered rapid-action, the long action time of cetirizine, and the experimenter takes the teldane equivalence of cetirizine and the 80mg of 10mg.
2, all good this product of curative effect and safety are different from classical antihistaminic, it is rapid-action, long action time, it does not damage cognitive function or does not cause significantly drowsiness, do not cause calmness or movable impaired yet, and first generation antihistaminic is easy to see through blood brain barrier because its close ester, so can produce a series of maincenter side reactions such as drowsiness, hallucination.This product molecular structure is a polarity, is difficult for seeing through blood brain barrier, thereby has significantly reduced the maincenter sedation.
3, medicining times is few in clinical use, and this product only need be taken once every day, has reduced patient's medicining times, has improved patient's compliance.
4, the little per day for adults of dosage once need be taken this product 10mg for each, and the child only need take 2.5mg-5mg, and dosage comparatively speaking, and is smaller, and the teldane adult needs one day twice, one time 60mg.
5, the sedation of few side effects cetirizine and astemizole, teldane are similar, are starkly lower than traditional antihistaminic.But it also is different from heavy dose of astemizole and teldane, does not have cardiac toxicity under its suggestion dosage or higher dosage, can not cause drug interaction, and prolonged application can not cause obesity.
Cetirizine hydrochloride is developed by the chemical combined company of Belgium (UCB) the earliest, after this, went on the market in states such as France, Britain, Spain in succession again first in Belgium's listing in 1987, this product listing back occupies antihistaminic always in Europe first place, and the U.S. and also approved listing of Canada.Lunan Pharmacy Co. Ltd obtained the New Drug Certificate of Cetirizine hydrochloride Tablets (specification is 10mg) in 2000, authentication code is the accurate word X20000379 of traditional Chinese medicines.
Cetirizine has worldwide obtained using very widely as the very good antihistamine drug of a kind of curative effect.Because mostly dosage form commonly used clinically is conventional tablet, gerontal patient or child for a lot of dysphagias take special inconvenience, in addition, operations in the open air etc. are in particular cases anhydrous, have in the time of need taking medicine immediately, and it also is impossible taking common tablet.Thereby develop that a kind of gerontal patient of being suitable for and child patient take, and do not need the dosage form of water delivery service, meet the interests of extensive patients, have the good market demand.
But because cetirizine has very serious pained mouthfeel, be developed to a kind of oral cavity disintegration tablet of rapid disintegrate in the oral cavity or oral liquid preparation, can influence patient's medication emotion and compliance to a great extent, especially to the infant patient, the difficulty of drug administration is the difficult problem of puzzlement infants ' parents always.Skin allergic disease is also comparatively common in infant, develops the cetirizine that a kind of infant takes like a shot and takes dosage form, is from the go on the market target of numerous pharmacy corporations struggles over nearly 20 years of cetirizine.
Summary of the invention
We are through a large amount of, experimental study repeatedly, on the basis of multiple correctives on probation, chemical constitution according to cetirizine, physicochemical property and cyclodextrin and derivant thereof must be covered effect to the bag of medicine and effect and to a lot of Chinese medicine bad smells, creationary proposition, with cetirizine with cyclodextrin or cyclodextrin derivative enclose after the reuse correctives carry out the way of flavoring, and discovery has beyond thought effect in test, after being cyclodextrin or cyclodextrin derivative and a lot of correctives use in conjunction, not only played synergitic effect on the cetirizine bitterness covering, and mouthfeel is greatly improved.This will greatly facilitate the old man and child patient is taken, and improves the compliance of child patient medication greatly, for the pediatrician provides excellent selection.The resulting pharmaceutical composition that contains cetirizine of the present invention, its characteristics be with active component with cyclodextrin or cyclodextrin derivative enclose after, mix with correctives again.We find in test, and independent cyclodextrin inclusion compound or independent correctives use, and no matter how much dose all can't reach of the present invention effect on, and after the two is share, beyond thought effect occurred.Effectively covering its pained taste of cetirizine hydrochloride is technical barrier to be solved by this invention, with the derivant of cyclodextrin or Cyclodextrin and correctives use in conjunction in contain cetirizine can be oral pharmaceutical preparation in be key problem in technology of the present invention and necessary technology feature.We find in test, the derivant of cyclodextrin or Cyclodextrin and the use in conjunction of correctives are used in oral liquids such as oral solid formulations such as oral cavity disintegration tablet, chewable tablet or oral administration solution, syrup, all obtained good effect, announced our part experiment prescription as follows below:
The specific embodiment
The invention will be further elaborated below by specific embodiment.
Embodiment: (recipe quantity is 1000 consumptions)
Eight kinds of concrete prescriptions:
Embodiment 1:
Cetirizine hydrochloride 2g
Beta-schardinger dextrin-10g
Mannitol 60g
Low-substituted hydroxypropyl cellulose 10g
Aspartame 0.5g
Distilled water is an amount of
Pulvis Talci 0.5g
Preparation technology:
Principal agent crosses 120 mesh sieves and beta-schardinger dextrin-is dissolved in 60～80 ℃ of hot water, keep more than the 60min, and cooling, beta-schardinger dextrin-is separated out after-filtration, and oven dry is sieved; Crospolyvinylpyrrolidone, aspartame are crossed 100 mesh sieves, take by weighing by recipe quantity, and mix homogeneously, the adding distilled water is an amount of, granulates, oven dry, granulate adds the recipe quantity Pulvis Talci, and mixing, tabletting are promptly.
Embodiment 2:
Cetirizine hydrochloride 5g
Dimethyl-20g
Lactose 50g
Crosslinked carboxymethyl fecula sodium 20g
Herba Menthae essence 1g
Distilled water is an amount of
Magnesium stearate 0.5g
Preparation technology:
Principal agent is crossed 120 mesh sieves and dimethyl-fully grinds mixing, lactose, crosslinked carboxymethyl fecula sodium, Herba Menthae essence are crossed 100 mesh sieves, take by weighing mix homogeneously by recipe quantity, it is an amount of to add distilled water, granulates oven dry, granulate, add the recipe quantity magnesium stearate, mixing, tabletting are promptly.
Embodiment 3:
Cetirizine hydrochloride 15g
Hydroxypropyl 80g
Mannitol 90g
Carboxymethyl starch sodium 15g
Fructus Citri Limoniae essence 1g
Distilled water is an amount of
Magnesium stearate 1g
Preparation technology:
With embodiment 2, the Fructus Citri Limoniae essence in the present embodiment also can replace with chocolate essence.
Embodiment 4:
Cetirizine hydrochloride 5g
Ethoxy beta-schardinger dextrin-20g
Mannitol 90g
Crospolyvinylpyrrolidone 8g
Fructus Citri tangerinae essence 1g
Distilled water is an amount of
Magnesium stearate 1g
Preparation technology:
With embodiment 2.
Embodiment 5
Cetirizine hydrochloride 10g
Carboxymethyl beta-schardinger dextrin-40g
Glucose 70g
Cross-linking sodium carboxymethyl cellulose 20g
Fructus Citri tangerinae essence 1g
Cyclamate 0.5g
Distilled water is an amount of
Micropowder silica gel 1g
Preparation technology:
With embodiment 2.
Embodiment 6
Cetirizine hydrochloride 3g
Methyl gamma-cyclodextrin 10g
Mannitol 70g
Cross-linking sodium carboxymethyl cellulose 10g
Fructus Citri tangerinae essence 1g
Distilled water is an amount of
Magnesium stearate 1g
Preparation technology:
With embodiment 2.
Embodiment 7
Cetirizine hydrochloride 3g
Gamma-cyclodextrin 10g
Mannitol 70g
Fructus Citri tangerinae essence 1g
Distilled water is an amount of
Preparation technology:
With embodiment 2.
Embodiment 8
The cetirizine hydrochloride oral administration solution
Cetirizine hydrochloride 15g
Glucosyl group alpha-cyclodextrin 60g
Sucrose 70g
Fructus Citri tangerinae essence 1g
5% benzalkonium bromide 5ml
Sodium acetate-hac buffer (pH7.0) is an amount of
Sterile distilled water 1000ml
Preparation technology:
Earlier cetirizine hydrochloride and glucosyl group alpha-cyclodextrin are dissolved in an amount of hot distilled water, 60 ℃ of temperature are bathed more than the 30min, the sucrose and the Fructus Citri tangerinae essence that add recipe quantity add 5% benzalkonium bromide solution of an amount of and recipe quantity of sodium acetate-hac buffer, and distilled water adds to 1000ml and gets final product.Glucosyl group alpha-cyclodextrin in the present embodiment also can replace with alpha-cyclodextrin or malt-base alpha-cyclodextrin.
Embodiment 9
Cetirizine hydrochloride 15g
Dimethyl-60g
Fructose 70g
Fructus Citri Limoniae essence 1g
Sodium acetate-hac buffer (pH7.0) is an amount of
Methyl hydroxybenzoate 2g
Sterile distilled water 1000ml
Preparation technology:
With embodiment 8.
Embodiment 10
Cetirizine hydrochloride 15g
Dimethyl-60g
Chocolate essence 1g
Sterile distilled water 1000ml
Preparation technology:
Elder generation is dissolved in cetirizine hydrochloride and glucosyl group alpha-cyclodextrin in an amount of hot distilled water, and 60 ℃ of temperature are bathed more than the 30min, add the sucrose and the Fructus Citri tangerinae essence of recipe quantity, and distilled water adds to 1000ml and gets final product with NaOH solution adjusting pH5～8.
Claims (7)
1. a combination of oral medication that contains cetirizine hydrochloride is characterized in that it except containing the active ingredient hydrochloric acid cetirizine, also contains following two kinds of compositions: the derivant of cyclodextrin or cyclodextrin and correctives.
2. combination of oral medication as claimed in claim 1 is characterized in that they are oral solid preparation or oral liquid preparation.
3. the derivant of cyclodextrin as claimed in claim 1 or cyclodextrin, they are alpha-cyclodextrin, beta-schardinger dextrin-, gamma-cyclodextrin, glucosyl group alpha-cyclodextrin, malt-base alpha-cyclodextrin, dimethyl-, hydroxypropyl, ethoxy beta-schardinger dextrin-, carboxymethyl beta-schardinger dextrin-, methyl gamma-cyclodextrin, hydroxypropyl gamma-cyclodextrin.
4. correctives as claimed in claim 1, they are in chocolate essence, Fructus Citri Limoniae essence, Fructus Citri tangerinae essence, cyclamate, aspartame, sucrose, fructose or the glucose one or more.
5. oral solid formulation as claimed in claim 2 is characterized in that also containing filler, disintegrating agent or lubricant.
6. filler as claimed in claim 5 is preferably one or more in mannitol, lactose, the glucose, disintegrating agent is preferably one or more in low-substituted hydroxypropyl cellulose, crosslinked carboxymethyl fecula sodium, carboxymethyl starch sodium, crospolyvinylpyrrolidone or the cross-linking sodium carboxymethyl cellulose, and lubricant is preferably magnesium stearate, micropowder silica gel or Pulvis Talci.
7. oral liquid as claimed in claim 2 is characterized in that also containing antiseptic.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410036471 CN1660098A (en) | 2004-12-09 | 2004-12-09 | Combination of tablet to swallow of containing Cetirizine Hydrochloride |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410036471 CN1660098A (en) | 2004-12-09 | 2004-12-09 | Combination of tablet to swallow of containing Cetirizine Hydrochloride |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1660098A true CN1660098A (en) | 2005-08-31 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410036471 Pending CN1660098A (en) | 2004-12-09 | 2004-12-09 | Combination of tablet to swallow of containing Cetirizine Hydrochloride |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009054432A1 (en) * | 2007-10-26 | 2009-04-30 | Daiichi Sankyo Company, Limited | Intraorally rapidly disintegrating pharmaceutical composition, and method for production thereof |
| CN101147800B (en) * | 2006-09-19 | 2010-09-29 | 沈阳市万嘉生物技术研究所 | Casein phosphopeptide cyclodextrin inclusion compound without bitter and its preparation method |
| CN101417005B (en) * | 2008-10-29 | 2013-01-23 | 重庆医科大学 | Gentian bitterness concealing technique in oral liquid |
| CN103463089A (en) * | 2013-08-26 | 2013-12-25 | 王大光 | Cetirizine hydrochloride oral solution and preparation method thereof |
| JP2016094364A (en) * | 2014-11-14 | 2016-05-26 | ニプロ株式会社 | Stabilized intraorally disintegrating formulation in which bitter taste is reduced |
| CN106177973A (en) * | 2014-06-11 | 2016-12-07 | 广东东阳光药业有限公司 | A kind of cetirizine hydrochloride solid preparation and preparation method thereof |
-
2004
- 2004-12-09 CN CN 200410036471 patent/CN1660098A/en active Pending
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101147800B (en) * | 2006-09-19 | 2010-09-29 | 沈阳市万嘉生物技术研究所 | Casein phosphopeptide cyclodextrin inclusion compound without bitter and its preparation method |
| WO2009054432A1 (en) * | 2007-10-26 | 2009-04-30 | Daiichi Sankyo Company, Limited | Intraorally rapidly disintegrating pharmaceutical composition, and method for production thereof |
| CN101417005B (en) * | 2008-10-29 | 2013-01-23 | 重庆医科大学 | Gentian bitterness concealing technique in oral liquid |
| CN103463089A (en) * | 2013-08-26 | 2013-12-25 | 王大光 | Cetirizine hydrochloride oral solution and preparation method thereof |
| CN103463089B (en) * | 2013-08-26 | 2016-03-02 | 王大光 | A kind of Cetirizine hydrochloride oral solution compositions |
| CN106177973A (en) * | 2014-06-11 | 2016-12-07 | 广东东阳光药业有限公司 | A kind of cetirizine hydrochloride solid preparation and preparation method thereof |
| JP2016094364A (en) * | 2014-11-14 | 2016-05-26 | ニプロ株式会社 | Stabilized intraorally disintegrating formulation in which bitter taste is reduced |
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