CN103610645B - A kind of pharmaceutical composition of fexofenadine hydrochloride and preparation method - Google Patents

A kind of pharmaceutical composition of fexofenadine hydrochloride and preparation method Download PDF

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CN103610645B
CN103610645B CN201310606048.2A CN201310606048A CN103610645B CN 103610645 B CN103610645 B CN 103610645B CN 201310606048 A CN201310606048 A CN 201310606048A CN 103610645 B CN103610645 B CN 103610645B
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composition
mass percentage
percentage content
fexofenadine hydrochloride
content
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CN103610645A (en
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金璐
杜军
单瑞平
桂盼
蒋定宇
杨必伟
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Zhejiang Sansheng Mandi Pharmaceutical Co ltd
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ZHEJIANG WANSHENG PHARMACEUTICAL Co Ltd
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Abstract

The pharmaceutical composition that the present invention relates to a kind of fexofenadine hydrochloride, said composition consists of the following composition: active component fexofenadine hydrochloride, content 1%-12%; Suspending agent content is 1%-10%; Filler content is 5%-85%; Levels of sweetener is 1%-10%; Essence content is 0.01%-10%; The glidant of convention amount, wherein said composition exists with the form of dry suspensoid agent. Fexofenadine hydrochloride dry suspensoid agent of the present invention have decentralization high, be evenly distributed, absorb fast, the advantage such as bioavilability is high, and mouthfeel is good and stablize.

Description

A kind of pharmaceutical composition of fexofenadine hydrochloride and preparation method
Technical field
The present invention relates to pharmaceutical, particularly a kind of novel form of fexofenadine hydrochloride and preparation method thereof.
Background technology
CAS registration number: 138452-21-8
Fexofenadine is the active metabolite of RMI 9918, is a kind of potent H1 receptor antagonist, do not have its predecessor thatThe cardiac toxic of sample. Decapacitation blocking-up H1 is subject to external, and in vivo and in vitro also shows, Fexofenadine is surely by mast cell, basophillaThe allergic inflammation reaction of granulocyte, epithelial cell, eosinophil and cell mediated. Confirm fexofenadine toolThere is anti-inflammatory activity, and can suppress in vitro the expression of ICAM-1 in nasal epithelial cells. Be used for the treatment of seasonal mistakeQuick property rhinitis and chronic idiopathic urticaria.
Fexofenadine has capsule, tablet, oral disnitegration tablet, oral administration mixed suspension for the conventional dosage forms of selection of clinical. Capsule, sheetAgent is a kind of general formulation, absorbs in vivo and must could pass through intestines and stomach arrival blood circulation through processes such as disintegration, strippings,And capsule, tablet are in process of production, are often difficult to disintegration because the reason such as auxiliary material, technique causes tablet, medicine is difficult to stripping, fromAnd make medicine not reach due therapeutic action. In addition, for the disease of children and dysphagia, capsule, tablet are difficult to accept.Disintegration fast in oral cavity that oral disnitegration tablet can be under anhydrous condition (or only having a small amount of water to exist), enters and disappears with swallowing actChange road, in oral cavity, without mucosa absorption, absorption in body, metabolic process are consistent with conventional tablet. Oral disnitegration tablet medicine requiresEfficiently, the medicine of low dosage, be not suitable for bitterness sense or the heavier medicine of excitant taste, preparation process complexity, disintegration time limited andDissolution rate is difficult to control, Chen Bengao. Although oral administration mixed suspension has overcome above shortcoming, must add anticorrosion at oral administration mixed suspensionAgent, to prevent the growth of bacterium, and be inconvenient to produce, storage and transport.
Summary of the invention
The present invention, in order to overcome the deficiencies in the prior art, provides a kind of dry suspensoid agent, has taking convenience, and decentralization is high, distributionEvenly, absorb soon, the advantage such as bioavilability is high, and mouthfeel is good and stablize, can overcome the shortcoming of conventional medicament composition,Layoutprocedure is simple simultaneously, but does not affect drug effect and other performances.
On the one hand, the invention provides a kind of pharmaceutical composition of fexofenadine hydrochloride, it is characterized in that, said composition by withLower one-tenth is grouped into: active component fexofenadine hydrochloride, mass percentage content 1%-12%; Suspending agent mass percentage contentFor 1%-10%; Filler mass percentage content is 5%-85%; Sweetener mass percentage content is 1%-10%; Essence qualityDegree is 0.01%-10%; The glidant of convention amount, wherein, said composition exists with the form of dry suspensoid agent.
Preferably, suspending agent is selected from PVP, xanthans, and bentonite, natural gum, polyethylene glycol, sodium carboxymethylcellulose,Methylcellulose, Hydroxypropyl methylcellulose, one or more in Tween-80, carragheen, carbopol and sodium alginate make simultaneouslyWith.
Preferably, filler is selected from lactose, sucrose, microcrystalline cellulose, sweet mellow wine, dextrin, calcium monohydrogen phosphate and pregelatinized starchIn one or more.
Preferably, sweetener be selected from a kind of of saccharin sodium, xylitol, Aspartame, stevioside, Sucralose, honey element orMultiple use simultaneously, content is 1%-10%; Essence is selected from the one of flavoring orange essence, flavoring apple essence, orange flavor, butter essenceOr multiple.
A pharmaceutical composition for fexofenadine hydrochloride, is characterized in that, said composition consists of the following composition: active one-tenthPoint fexofenadine hydrochloride, sodium carboxymethylcellulose, sweet mellow wine, sucrose, Aspartame, orange flavor, butter essence andSilica, wherein the mass percentage content of fexofenadine hydrochloride is 6%; The degree of sodium carboxymethylcellulose is5%; The mass percentage content of sweet mellow wine is 42%; The mass percentage content of sucrose is 40%; The mass percent of AspartameContent is 5%; Orange flavor mass percentage content is 0.5%; Butter essence mass percentage content is 0.5%; SilicaMass percentage content be 1.0%, wherein, said composition exists with the form of dry suspensoid agent.
A pharmaceutical composition for fexofenadine hydrochloride, is characterized in that, said composition consists of the following composition: active one-tenthDivide fexofenadine hydrochloride, xanthans, sweet mellow wine, sucrose, Aspartame, orange flavor, butter essence and silica,Wherein the mass percentage content of fexofenadine hydrochloride is 6%; The mass percentage content of xanthans is 5%; The matter of sweet mellow wineAmount degree is 42%; The mass percentage content of sucrose is 40%; The mass percentage content of Aspartame is 5%; SweetOrange essence mass percentage content is 0.5%; Butter essence mass percentage content is 0.5%; The mass percent of silica containsAmount is 1.%, and wherein, said composition exists with the form of dry suspensoid agent.
On the other hand, the invention provides a kind of preparation method of fexofenadine hydrochloride pharmaceutical composition, comprise the following steps:(1) fexofenadine hydrochloride and suspending agent are crossed to 80 mesh sieves; (2) by filler, sweetener, essence respectively becomes with glidantDivided 100 mesh sieves; (3) the each composition after sieving mixes, packing and get final product.
Preferably, the content 1%-12% of active component fexofenadine hydrochloride; Suspending agent content is 1%-10%; Filler contentFor 5%-85%; Levels of sweetener is 1%-10%; Essence content is 0.01%-10%; The glidant of convention amount.
Preferably, suspending agent is selected from PVP, xanthans, and bentonite, natural gum, polyethylene glycol, sodium carboxymethylcellulose,Methylcellulose, Hydroxypropyl methylcellulose, one or more in Tween-80, carragheen, carbopol and sodium alginate. Sweet tasteAgent be selected from saccharin sodium, xylitol, Aspartame, stevioside, Sucralose, honey element one or more use simultaneously, containAmount is 1%-10%. Essence is selected from the one of flavoring orange essence, flavoring apple essence, orange flavor, butter essence. Filler be selected from lactose,One in sucrose, microcrystalline cellulose, sweet mellow wine, dextrin, calcium monohydrogen phosphate and pregelatinized starch.
In a preferred mode, fexofenadine hydrochloride dry suspensoid agent, wherein contains active ingredient hydrochloric acid fexofenadineHydrochloride, content 1%-12%; Suspending agent content is 1%-10%; Filler content is 5%-60%; Levels of sweetener is 1%-0%;Essence content is 0.01%-10%; The glidant of convention amount.
Suspending agent is selected from PVP, xanthans, bentonite, natural gum, polyethylene glycol, sodium carboxymethylcellulose, methyl fiberElement, Hydroxypropyl methylcellulose, one or more in Tween-80, carragheen, carbopol and sodium alginate etc. use simultaneously, containAmount is 1%-10%.
Filler is selected from the one in lactose, sucrose, microcrystalline cellulose, sweet mellow wine, dextrin, calcium monohydrogen phosphate and pregelatinized starchOr multiple. Preferably, their use amount accounts for the 5%-60% of the mass percent of total dry suspending agent.
Sweetener is selected from one or more whiles of saccharin sodium, xylitol, Aspartame, stevioside, Sucralose, honey elementUse, content is 1%-10%; Essence be selected from flavoring orange essence, flavoring apple essence, orange flavor, butter essence one or more withIn time, is used, and content is 0.01%-10%;
The preparation method of fexofenadine hydrochloride dry suspensoid agent, comprises the following steps: (1) is by fexofenadine hydrochloride and helping80 mesh sieves are crossed in outstanding agent; (2) by filler, sweetener, the each composition of essence and glidant is crossed 100 mesh sieves; (3) after sievingEach composition mixes, packing and get final product.
The present invention do not specify down, and the degree using is all mass percentage content.
Beneficial effect
The invention provides a kind of novel form and preparation method thereof, not only can obtain by this novel form and preparation method thereof the side of takingJust, decentralization is high, be evenly distributed, and absorbs soon, and bioavilability is high, and the pharmaceutical preparation that mouthfeel is good and stable also can simultaneouslyTo facilitate production and transport, storage and clinical use.
Detailed description of the invention
Below by embodiment, technical scheme of the present invention is further elaborated. These examples of implementation are only used for illustrating the present inventionMode how to realize, claim is not done to further restriction.
Embodiment 1:
Product prescription (table 1):
Make altogether 1000 bags of techniques: fexofenadine hydrochloride and suspending agent are crossed to 80 mesh sieves, by filler, sweetener, essenceCross 100 mesh sieves with the each composition of glidant, the each composition after sieving mixes, packing and get final product.
Embodiment 2:
Product prescription (table 2):
Make altogether 1000 bags of techniques: fexofenadine hydrochloride and suspending agent are crossed to 80 mesh sieves, by filler, sweetener, essenceCross 100 mesh sieves with the each composition of glidant, the each composition after sieving mixes, packing and get final product.
Temperature and illumination experiment
Get this product (lot number 090401) of examples of implementation 1 and 2, by commercially available back, at the temperature of 60 DEG C, place 35 days, inThe 5th day and the 0th day sampling, to its settling volume ratio, related substance and activity substance content detect, and with 0 day relatively,The results are shown in Table 3. This product (lot number 090401) of getting examples of implementation 1 and 2, is placed in tool plug vial, in illumination isUnder the condition of 4500lx ± 500lx, place 35 days, in the 5th day and sampling in the 0th day, to its proterties, uniformity, content, relevantMaterial detects, and with 0 day relatively, the results are shown in Table 3.
Can find out from following form, the in the situation that of high temperature 35 days, active material is without obvious decline, settling volume than and relevantMaterial, without obvious rising, shows that this formula is more stable under the environment of high temperature and illumination.
Table 3: the temperature of the sample of examples of implementation 1 and 2 and illumination experiment result comparison sheet
The present invention not only can obtain taking convenience by this novel form and preparation method thereof, and decentralization is high, be evenly distributed, and absorbsHurry up, bioavilability is high, and the pharmaceutical preparation that mouthfeel is good and stable can also facilitate production and transport, storage and clinical making simultaneouslyWith.

Claims (2)

1. a pharmaceutical composition for fexofenadine hydrochloride, is characterized in that, said composition is divided into groups by following one-tenthBecome: active component fexofenadine hydrochloride, sodium carboxymethylcellulose, sweet mellow wine, sucrose, A SibaSweet, orange flavor, butter essence and silica, the wherein mass percent of fexofenadine hydrochlorideContent is 6%; The degree of sodium carboxymethylcellulose is 5%; The mass percentage content of sweet mellow wineBe 42%; The mass percentage content of sucrose is 40%; The mass percentage content of Aspartame is 5%;Orange flavor mass percentage content is 0.5%; Butter essence mass percentage content is 0.5%; DioxyThe mass percentage content of SiClx is 1%, and wherein, said composition exists with the form of dry suspensoid agent, wherein,Said composition is prepared by the following method, and described method is made up of the following step: (1) is by FexofenadineDetermine hydrochloride and sodium carboxymethylcellulose and cross 80 mesh sieves; (2) by sweet mellow wine, sucrose, Aspartame,Orange flavor, the each composition of butter essence and silica is crossed 100 mesh sieves; (3) the each composition after sieving is mixedClose evenly packing and get final product.
2. a pharmaceutical composition for fexofenadine hydrochloride, is characterized in that, said composition is divided into groups by following one-tenthBecome: active component fexofenadine hydrochloride, xanthans, sweet mellow wine, sucrose, Aspartame, sweet orangeEssence, butter essence and silica, wherein the mass percentage content of fexofenadine hydrochloride is 6%;The mass percentage content of xanthans is 5%; The mass percentage content of sweet mellow wine is 42%; The matter of sucroseAmount degree is 40%; The mass percentage content of Aspartame is 5%; Orange flavor quality percentageBe 0.5% than content; Butter essence mass percentage content is 0.5%; The mass percent of silicaContent is 1%, and wherein, said composition exists with the form of dry suspensoid agent; Wherein, said composition by asBelow legal system is standby, and described method is made up of the following step: (1) is by fexofenadine hydrochloride and xanthanGlue is crossed 80 mesh sieves; (2) by sweet mellow wine, sucrose, Aspartame, orange flavor, butter essence and twoThe each composition of silica is crossed 100 mesh sieves; (3) the each composition after sieving mixes, packing and get final product.
CN201310606048.2A 2013-11-25 2013-11-25 A kind of pharmaceutical composition of fexofenadine hydrochloride and preparation method Active CN103610645B (en)

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CN106806346B (en) * 2015-12-01 2020-09-11 国药集团广东环球制药有限公司 Fexofenadine hydrochloride dry suspension preparation and preparation method thereof
CN107536804A (en) * 2016-06-28 2018-01-05 浙江普利药业有限公司 Fexofenadine hydrochloride dry suspensoid agent and preparation method thereof
CN114432241B (en) * 2021-12-21 2023-07-14 上海奥全生物医药科技有限公司 Rapidly-dispersed suspension composition, preparation method and application thereof

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US6723348B2 (en) * 2001-11-16 2004-04-20 Ethypharm Orodispersible tablets containing fexofenadine
CN1813683B (en) * 2005-12-07 2011-08-31 范敏华 Azithromycin for suspension and its preparing method
DOP2006000274A (en) * 2005-12-14 2007-10-15 Sanofi Aventis Us Llc FEXOFENADINE SUSPENSION FORMULATION
FR2959130A1 (en) * 2010-04-21 2011-10-28 Sanofi Aventis PROCESS FOR PREPARING PHARMACEUTICAL COMPOSITIONS FOR ORAL ADMINISTRATION COMPRISING ONE OR MORE ACTIVE INGREDIENTS AND COMPOSITIONS COMPRISING SAME

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Address after: 311305 No.1 Wangjiashan Road, Qingshanhu Street, Lin'an City, Hangzhou City, Zhejiang Province

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