CN1223338C - Cetirizine hydrochloride gel - Google Patents

Cetirizine hydrochloride gel Download PDF

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Publication number
CN1223338C
CN1223338C CN 03129155 CN03129155A CN1223338C CN 1223338 C CN1223338 C CN 1223338C CN 03129155 CN03129155 CN 03129155 CN 03129155 A CN03129155 A CN 03129155A CN 1223338 C CN1223338 C CN 1223338C
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CN
China
Prior art keywords
cetirizine hydrochloride
preparation
cetirizine
administration
gel
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CN 03129155
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Chinese (zh)
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CN1457765A (en
Inventor
胡晋红
刘继勇
朱全刚
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Second Military Medical University SMMU
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Second Military Medical University SMMU
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Publication date
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Priority to CN 03129155 priority Critical patent/CN1223338C/en
Publication of CN1457765A publication Critical patent/CN1457765A/en
Application granted granted Critical
Publication of CN1223338C publication Critical patent/CN1223338C/en
Anticipated expiration legal-status Critical
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Abstract

The present invention relates to an external preparation of cetirizine hydrochloride of antihistamine medicaments, namely a gelling agent and a preparation technology thereof, which belongs to the technical field of medicaments. The cetirizine hydrochloride is a medicament clinically and generally used. The existing preparation is an oral preparation such as tablets, capsules, solution, etc. Because the cetirizine hydrochloride has a central inhibition function, a patient orally takes the medicament and has adverse reactions such as somnolence, vertigo, headache, etc. The cetirizine hydrochloride is used as a main medicament; different auxiliary materials are added and prepared into the gelling agent; the administration is carried out by skin or mucosae; the external preparation avoids a first pass effect on a liver and stimulation to gastrointestinal tracts due to oral administration, reduces a systemic blood medical concentration, reduces the central inhibition function, and enhances the medical concentration of local affected positions such as the skin, the nasal mucous membranes, etc. Moreover, the external preparation has the advantages of the reduction of administration times, convenient use, the enhancement of the compliance of patient medication and the like, and provides a new administration preparation for the clinical application of cetirizine.

Description

Cetirizine hydrochloride gel
Technical field:
The present invention relates to medical technical field, is a kind of exterior-applied formulation---gel and preparation method thereof of antihistaminic cetirizine hydrochloride (Cetirizine Hydrochloride).
Background technology:
Cetirizine hydrochloride is a second filial generation antihistaminic, and allergic disease such as skin urticaria, allergic asthma, allergic rhinitis and the anaphylaxis conjunctivitis etc. of skin, respiratory system and eyes are all had the good curing effect.At present, the pharmaceutical dosage form of this medicine has regular dosage forms such as tablet, capsule, solution, and route of administration is oral.Compare untoward reaction such as though the central nervous system of cetirizine hydrochloride is active lower, that oral this medicine still has is drowsiness, dizzy, headache with other antihistaminic.
Summary of the invention:
The invention provides a kind of topical administration formulations of cetirizine hydrochloride---gel and preparation method thereof.
Gel can be avoided the contingent liver first-pass effect of oral administration by skin (or mucosa) administration and gastrointestinal is stimulated, and reduces systemic blood concentration, reduces central inhibitory action; Improve the drug level in local affected parts such as skin, nasal mucosa; And have the minimizing administration number of times, and easy to use, improve the advantages such as compliance of patient's medication.Therefore, cetirizine hydrochloride is made the external-use gel preparation,, not only can keep its excellent curative, and can reduce the untoward reaction that its maincenter suppresses by skin or mucosa delivery.
Cetirizine hydrochloride gel is made up of medicine, polymer-based material, solvent, wetting agent, penetration enhancer and antiseptic, also can contain nertralizer.Medicine is a cetirizine hydrochloride; Polymer-based material is selected from carbopol, sodium carboxymethyl cellulose, hypromellose, hydroxypropyl cellulose, polyvinylpyrrolidone, when selecting carbopol for use, must add nertralizer; Solvent is a water; Wetting agent is a glycerol; Antiseptic is selected from ethyl hydroxybenzoate, benzalkonium bromide; Nertralizer is selected from sodium hydroxide or triethanolamine; Penetration enhancer is selected from Mentholum, Camphora, azone, limonene, propylene glycol, can select 1-2 kind chemical compound wherein simultaneously for use.
The percentage by weight of each component is: cetirizine hydrochloride 0.2-1%, and polymer-based material 0.1-5%, wetting agent 5-15%, antiseptic 0.01-0.5%, nertralizer 0.04-6%, penetration enhancer 0.5-20%, surplus is a water.
Preparation method of the present invention is: polymer-based material is added water-soluble expand, adds medicine, wetting agent, antiseptic, nertralizer and penetration enhancer respectively, add water to ormal weight, stir by said ratio, gel.
The present invention makes gel with cetirizine hydrochloride, by skin or mucosa delivery, not only can avoid the GI irritation of oral administration, reduce systemic blood concentration, reduce central inhibitory action, and prolonged action time, reduce administration number of times, improved the compliance of patient's medication.This preparation process thereof is simple, and is easy to use, for the clinical practice of cetirizine hydrochloride provides a kind of new dosage form.
The specific embodiment:
Embodiment 1 preparation cetirizine hydrochloride gel
Prescription and proportioning:
Carbopol 740 1g Mentholum 8g
Cetirizine hydrochloride 1g propylene glycol 10ml
Glycerol 5ml triethanolamine 1.5g
Ethyl hydroxybenzoate 0.1g distilled water adds to 100g
Preparation method is: carbopol 740 is added 40 times the abundant swelling of distilled water, add cetirizine hydrochloride, glycerol, Mentholum, propylene glycol, ethyl hydroxybenzoate and triethanolamine respectively by said ratio, adding distil water stirs to 100g, gel.The hydrochloric cetirizine 10mg of the every gram of finished product gel.
Embodiment 2 preparation cetirizine hydrochloride gels
Prescription and proportioning:
Hypromellose 1.5g azone 5ml
Cetirizine hydrochloride 1g propylene glycol 15ml
Glycerol 10ml ethyl hydroxybenzoate 0.1g
Distilled water adds to 100g
Preparation method is: hypromellose is added 50 times the abundant swelling of distilled water, add cetirizine hydrochloride, glycerol, azone, propylene glycol, ethyl hydroxybenzoate respectively by said ratio, adding distil water stirs to 100g, gel.The hydrochloric cetirizine 10mg of the every gram of finished product gel.
Embodiment 3 preparation cetirizine hydrochloride gels
Prescription and proportioning:
Polyvinylpyrrolidone 2g ethyl hydroxybenzoate 0.1g
Cetirizine hydrochloride 1g glycerol 8ml
Distilled water adds to 100g
Preparation method is: polyvinylpyrrolidone is added 50 times the abundant swelling of distilled water, add cetirizine hydrochloride, glycerol, ethyl hydroxybenzoate respectively by said ratio, adding distil water stirs to 100g, gel.The hydrochloric cetirizine 10mg of the every gram of finished product gel.

Claims (2)

1, a kind of cetirizine hydrochloride gel, form by medicine, polymer-based material, solvent, wetting agent, penetration enhancer and antiseptic, it is characterized in that medicine is a cetirizine hydrochloride, polymer-based material is selected from carbopol, sodium carboxymethyl cellulose, hypromellose, hydroxypropyl cellulose, polyvinylpyrrolidone, when polymer matrix material selection carbopol, must add nertralizer, nertralizer is selected from sodium hydroxide or triethanolamine; Solvent is a water; Wetting agent is a glycerol; Antiseptic is selected from ethyl hydroxybenzoate, benzalkonium bromide; Penetration enhancer is selected from Mentholum, Camphora, azone, limonene, propylene glycol, can select 1-2 kind chemical compound wherein simultaneously for use; The percentage by weight of each component is: cetirizine hydrochloride 0.2-1%, and polymer-based material 0.1-5%, wetting agent 5-15%, antiseptic 0.01-0.5%, surplus is a water, nertralizer 0.04-6%, penetration enhancer 0.5-20%.
2, by the described cetirizine hydrochloride gel of claim 1, it is characterized in that the ratio of each component is: carbopol 7401g, cetirizine hydrochloride 1g, glycerol 5ml, Mentholum 8g, propylene glycol 10ml, triethanolamine 1.5g, ethyl hydroxybenzoate 0.1g, distilled water add to 100g.
CN 03129155 2003-06-10 2003-06-10 Cetirizine hydrochloride gel Expired - Fee Related CN1223338C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN 03129155 CN1223338C (en) 2003-06-10 2003-06-10 Cetirizine hydrochloride gel

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN 03129155 CN1223338C (en) 2003-06-10 2003-06-10 Cetirizine hydrochloride gel

Publications (2)

Publication Number Publication Date
CN1457765A CN1457765A (en) 2003-11-26
CN1223338C true CN1223338C (en) 2005-10-19

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Family Applications (1)

Application Number Title Priority Date Filing Date
CN 03129155 Expired - Fee Related CN1223338C (en) 2003-06-10 2003-06-10 Cetirizine hydrochloride gel

Country Status (1)

Country Link
CN (1) CN1223338C (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100425237C (en) * 2005-09-28 2008-10-15 哈尔滨医科大学 Compound cetirizine hydrochloride gel
CN103393592B (en) * 2013-08-05 2015-10-21 四川国康药业有限公司 A kind of Sodium Azulenesulfonate gel and its production and use
CN106176578A (en) * 2016-08-04 2016-12-07 长沙原道医药科技开发有限公司 Sinomenine hydrochloride gel prepared by a kind of organic solvent and preparation method thereof
CN106176577A (en) * 2016-08-04 2016-12-07 长沙原道医药科技开发有限公司 Sinomenine hydrochloride gel prepared by a kind of inorganic solvent and preparation method thereof
CN114886843B (en) * 2022-05-26 2023-08-11 中国人民解放军南部战区总医院 Cetirizine hydrochloride liposome gel for treating androgenetic alopecia and preparation method and application thereof

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