CN1813730A - Fexofenadine hydrochloride dropping pill and its preparing method - Google Patents
Fexofenadine hydrochloride dropping pill and its preparing method Download PDFInfo
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- CN1813730A CN1813730A CN 200510061655 CN200510061655A CN1813730A CN 1813730 A CN1813730 A CN 1813730A CN 200510061655 CN200510061655 CN 200510061655 CN 200510061655 A CN200510061655 A CN 200510061655A CN 1813730 A CN1813730 A CN 1813730A
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- fexofenadine hydrochloride
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Abstract
The present invention discloses a medicine fexofenadine hydrochloride dripping pills preparation for effectively curing seasonal allergic rhinitis and chronic idiopathic urticaria and its preparation process. It is made up by using fexofenadine hydrochloride and matrix for making dripping pills.
Description
Technical field
The invention belongs to the pharmaceutical technology field, particularly a kind of by fexofenadine hydrochloride (Fexofenadine Hydrochloride) and the formulated fexofenadine hydrochloride dropping pill of drop pill substrate.
Background technology
Anaphylaxis claims allergy or allergy again, and the anaphylactic disease sickness rate is higher always.In recent years, because the variation of living habit and environment, anaphylactic disease is increasing.Nearly 100,000,000 people of China's Allergic Rhinitis, urticaria in various degree appears in about simultaneously 20% crowd.Allergic rhinitis divides slight and middle severe two kinds of degree.Middle severe then disturbs the patient to live, and causes quality of life to descend, and work efficiency reduces, and school grade descends, and influence is slept, amusement, and the patient is very worried.As untimely treatment, can cause sinusitis, otitis media, nasal polyp, bronchial asthma etc. have a strong impact on patient's body Health and Living quality, and cause heavy financial burden for family and society.All the time, antihistaminic all is widely used in the treatment of anaphylactic disease, especially for use in allergic rhinitis and urticaria treatment field.
Fexofenadine hydrochloride is an Aventis company development product, and this medicine is the active metabolite of terfenadine, and its major advantage is a cardiac toxicity of having removed its parent drug terfenadine.This medicine at first went on the market in the U.S. in 1997.Fexofenadine hydrochloride, chemistry (+) 4-[4-[4-(hydroxyl diphenyl methyl) by name-piperidino]-the 1-hydroxybutyl]-α, the alpha-alpha-dimethyl phenyl acetic acid hydrochlorate.High selectivity periphery histamine H
1Receptor antagonist.Suppress mastocyte and discharge various inflammatory mediators; No anticholinergic effect, no α
1-adrenergic receptor and β-adrenergic receptor retardation; Do not see through blood brain barrier, do not have calm and other central nervous system's side effect.Absorb in the fexofenadine hydrochloride body soon, oral back reached peak concentration in 1-1.5 hour, and biological half-life is 11-14 hour, its effect rapidly, lasting, be suitable for taking medicine once in one day, improved the acceptability that the patient takes medicine.Fexofenadine hydrochloride has shown the good clinical therapeutic effect, is used for the treatment of seasonal allergic rhinitis and chronic idiopathic urticaria, and this medicine becomes a line medicine of the above-mentioned disease of treatment.External clinical trial is presented in the therapeutic evaluation of alleviating seasonal allergic rhinitis, and the curative effect of fexofenadine 60mg/ time (2 times/day) or 120mg/ time (1 time/day) is suitable with the loratadine of 10mg/ time (1 time/day); The curative effect of 120mg/ time (1 time/day) is suitable with the cetirizine of 10mg/ time (1 time/day).The fexofenadine hydrochloride clinical efficacy is good, and the effect selectivity is strong, takes a long view, and fexofenadine hydrochloride can improve patient's quality of life better than loratadine.Effect is rapid, and action time is lasting, only need take once, and improve patient's compliance in one day.Side effect is little, acardia toxic action, no sedation.Fexofenadine hydrochloride is the metabolite of terfenadine the human liver, directly uses the former, can alleviate the damage of medicine to liver, thereby it is applicable to the liver patient that declines.Fexofenadine hydrochloride is mainly used in the treatment seasonal allergic rhinitis, be applicable to adult and the child more than six years old, can effectively alleviate the sneeze, the rhinorrhea that cause by seasonal allergic rhinitis, nose, Hubei Province, throat itch, pruritus, symptoms such as blood-shot eye illness, to by the caused non-compound skin symptom of chronic urticaria, can obviously alleviate pruritus and rubella symptom.
At present, use clinically the fexofenadine hydrochloride oral formulations be mainly tablet.Because shortcomings such as the tablet producing technology technology has, and makes tablet exist disintegration time long, and onset is slow, and bioavailability is lower, thereby influence giving full play to of drug effect.Fexofenadine hydrochloride dropping pill bioavailability height of the present invention, disintegrate is molten loose fast, the dissolution height, steady quality, release fast, produce effects fast can sublingual administration, also can swallow, and is easy to carry and use.Preparation process of the present invention is simple, and workshop does not have dust, uses supplementary product kind few, and production process is short, and cost is low.
Summary of the invention
The object of the invention provides a kind of medicine fexofenadine hydrochloride dropping pill and preparation technology thereof of antiallergic action.
The invention is characterized in by fexofenadine hydrochloride and drop pill substrate formulated.
The weight ratio of each composition is:
Fexofenadine hydrochloride: drop pill substrate=1: 1～1: 10
The present invention can be achieved through the following technical solutions:
Get fexofenadine hydrochloride, pulverize, sieve.Fexofenadine hydrochloride mixes by weight 1: 1～1: 10 with drop pill substrate, and heating and melting stirs, and splashes in dimethicone or other drop pill coolant, separates drop pill, absorbs coolant, drying, promptly.
Utilize the drop pill of method preparation of the present invention, its main feature is:
1. the quick stripping of medicine, the dissolution height, rapid-action, the bioavailability height, side effect is little.Limit for length during disintegration of tablet, absorption difference, onset is slow, and bioavailability is lower, thereby influences giving full play to of drug effect.Fexofenadine hydrochloride dropping pill is after medicine and the fusion of drop pill substrate medicine to be dispersed in the substrate, solidify by system of dripping and quenching, medicine is scattered in the substrate with molecularity or superfine crystal state, help absorption of human body, bring into play curative effect rapidly, improve bioavailability, reduce side effect.
2. increased administering mode, can swallow, but also sublingual administration as adopting the sublingual administration administration, and dissolves rapidly after saliva contacts, absorb by oral mucosa, directly enter blood circulation without gastrointestinal tract and liver, not only avoided the liver sausage first-pass effect, and it is rapid to have reached onset, improve bioavailability, reduce the purpose of side effect.
2. medicine stability is good.Dropping pill formulation by medicine and substrate heating and melting after, splash in the immiscible liquid coolant and make, reduce with the air contact area, be difficult for oxidation, substrate is non-water thing, is difficult for causing drug hydrolysis, stability of drug is increased, thereby guaranteed drug quality.
3. drop pill production technology, production equipment are simple, with short production cycle, the production efficiency height, and cost is low.
4. in the main production process of drop pill, used material all is to carry out under liquid state, has reduced dust pollution, helps labor protection and environmental protection, helps the GMP management.
The fexofenadine hydrochloride dropping pill crude drug is a fexofenadine hydrochloride, chemistry (+) 4-[4-[4-(hydroxyl diphenyl methyl) by name-piperidino]-the 1-hydroxybutyl]-α, the alpha-alpha-dimethyl phenyl acetic acid hydrochlorate.
Molecular formula: C
32H
39NO
4HCl
Molecular weight: 538.13
The specific embodiment
Further the present invention can be described by the following examples, but not limited by embodiment.
Embodiment: per 1000 fexofenadine hydrochloride dropping pill supplementary material proportionings
| The embodiment sequence number | Fexofenadine hydrochloride | Polyethylene glycol 6000 | Macrogol 4000 | Carboxymethyl starch sodium | Poloxamer |
| 1 | 5g | 45g | 5g | ||
| 2 | 5g | 30g | |||
| 3 | 5g | 25g | 5g | ||
| 4 | 10g | 20g | 5g | 2g | |
| 5 | 10g | 15g | 2g | 3g | |
| 6 | 10g | 25g | 5g |
Claims (3)
1. fexofenadine hydrochloride dropping pill and preparation technology thereof is characterized in that by fexofenadine hydrochloride (Fexofenadine Hydrochloride) and drop pill substrate formulated.The weight ratio of each composition is:
Fexofenadine hydrochloride: drop pill substrate=1: 1～1: 10
2. fexofenadine hydrochloride dropping pill according to claim 1, it is characterized in that described drop pill substrate is a kind of or several compatibilities in polyethylene glycols, carboxymethyl starch sodium, poloxamer, sodium carboxymethyl cellulose, stearic acid, sodium stearate, the polyoxyethylene monostearate, the content of each compatibility composition all is not equal to zero.
3. according to claim 1 described fexofenadine hydrochloride dropping pill, it is characterized in that preparation method is as follows: get fexofenadine hydrochloride, pulverize, sieve.Fexofenadine hydrochloride mixes by weight 1: 1～1: 10 with drop pill substrate, and heating and melting stirs, and splashes in dimethicone or other drop pill coolant, separates drop pill, absorbs coolant, drying, promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510061655 CN1813730A (en) | 2005-11-22 | 2005-11-22 | Fexofenadine hydrochloride dropping pill and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510061655 CN1813730A (en) | 2005-11-22 | 2005-11-22 | Fexofenadine hydrochloride dropping pill and its preparing method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1813730A true CN1813730A (en) | 2006-08-09 |
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ID=36906164
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200510061655 Pending CN1813730A (en) | 2005-11-22 | 2005-11-22 | Fexofenadine hydrochloride dropping pill and its preparing method |
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| CN (1) | CN1813730A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101843616A (en) * | 2010-06-04 | 2010-09-29 | 西安万隆制药有限责任公司 | Composition of fexofenadine hydrochloride and microcrystalline cellulose and preparation method thereof |
| CN103463085A (en) * | 2013-09-22 | 2013-12-25 | 广东环球制药有限公司 | Rapidly released fexofenadine pills and preparation method thereof |
-
2005
- 2005-11-22 CN CN 200510061655 patent/CN1813730A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101843616A (en) * | 2010-06-04 | 2010-09-29 | 西安万隆制药有限责任公司 | Composition of fexofenadine hydrochloride and microcrystalline cellulose and preparation method thereof |
| CN101843616B (en) * | 2010-06-04 | 2011-07-27 | 西安万隆制药有限责任公司 | Composition of fexofenadine hydrochloride and microcrystalline cellulose and preparation method thereof |
| CN103463085A (en) * | 2013-09-22 | 2013-12-25 | 广东环球制药有限公司 | Rapidly released fexofenadine pills and preparation method thereof |
| CN103463085B (en) * | 2013-09-22 | 2015-04-15 | 广东环球制药有限公司 | Rapidly released fexofenadine pills and preparation method thereof |
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Addressee: Chen Qian Document name: Notification that Application Deemed to be Withdrawn |
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Open date: 20060809 |