CN1813727A - Triprolidine hydrochloride dropping pill and its preparing method - Google Patents
Triprolidine hydrochloride dropping pill and its preparing method Download PDFInfo
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- CN1813727A CN1813727A CN 200510061706 CN200510061706A CN1813727A CN 1813727 A CN1813727 A CN 1813727A CN 200510061706 CN200510061706 CN 200510061706 CN 200510061706 A CN200510061706 A CN 200510061706A CN 1813727 A CN1813727 A CN 1813727A
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- triprolidine hydrochloride
- drop pill
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Abstract
The present invention discloses a triprolidine hydrochloride dripping pills preparation for effectively curing the diseases of allergic rhinitis, allergic conjunctivitis, eczema, neurodermatitis, urticaria, cutaneous pruritus and pollenosis, etc. and its preparation process. It is made up by using triprolidine hydrochloride and matrix for making dripping pills through a preparation process.
Description
Technical field
The invention belongs to the pharmaceutical technology field, particularly a kind of by triprolidine hydrochloride (TriprolidineHydrochloride) and the formulated triprolidine 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.In China, the sickness rate of anaphylactic disease by several years ago 30% fast increase till now 50%, all might take place to the middle-aged and elderly people each age group from neonate.Become the major issue that influences human health.Histamine is to cause inflammation and a class material of anaphylactic disease, is one of important chemical mediator of type (a clinical the most common class allergic disease).Different according to the receptor in target cell of striving unexpectedly with histamine, antihistamine drug is divided into H
1Receptor antagonist and H
2Receptor antagonist.All the time, antihistaminic all is widely used in the treatment of anaphylactic disease, especially for use in allergic rhinitis and urticaria treatment field.
Triprolidine hydrochloride, call into proactidil (triprolidine hydrochloride), AH-611, gram quick etc.Main and the histamine of triprolidine hydrochloride is striven the H on the effector lymphocyte unexpectedly
1Receptor makes forfeiture of group amine and H
1Receptors bind, thus anaphylaxis suppressed.After the oral absorption, decompose at liver, through renal excretion, the half-life is 14 hours in the body, has potent, long-acting and characteristics such as low toxicity and central nerve inhibition.Triprolidine hydrochloride is the efficient Claritin of a new generation, there is not drowsiness side effect, be widely used in anaphylactic diseases such as the various allergic rhinitises of treatment, anaphylaxis conjunctivitis, eczema, neurodermatitis, urticaria, skin pruritus, asthma and pollinosis clinically, curative effect is good, rapid-action, side effect is little.
The triprolidine hydrochloride oral formulations is tablet, capsule in the market.Because this class conventional formulation fabricating technology has, and makes that this class oral formulations disintegration time is long, onset is slow, and bioavailability is lower, thereby influences giving full play to of drug effect.Triprolidine 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, sublingual administration can reduce extensive first pass metabolism, 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 triprolidine hydrochloride dropping pill and preparation technology thereof of antiallergic action.
The invention is characterized in by triprolidine hydrochloride and drop pill substrate formulated.
The weight ratio of each composition is:
Triprolidine hydrochloride: drop pill substrate=1: 1~1: 20
The present invention can be achieved through the following technical solutions:
Get triprolidine hydrochloride, pulverize, sieve.Triprolidine hydrochloride mixes by weight 1: 1~1: 20 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.Triprolidine hydrochloride dropping pill is to utilize solid dispersion technology, to after medicine and the fusion of drop pill substrate medicine 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, the performance curative effect improves bioavailability rapidly, reduces 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. increased administering mode, can swallow, but also sublingual administration.As adopt the sublingual administration administration, and and after contacting, saliva dissolves rapidly, 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.
4. drop pill production technology, production equipment are simple, with short production cycle, the production efficiency height, and cost is low.
5. 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 specific embodiment
Further the present invention can be described by the following examples, but not limited by embodiment.
Embodiment: per 1000 triprolidine hydrochloride dropping pill supplementary material proportionings
The embodiment sequence number | Triprolidine hydrochloride | Polyethylene glycol 6000 | Macrogol 4000 | Carboxymethyl starch sodium | Poloxamer |
1 | 2.5g | 40g | 5g | 2g | |
2 | 2.5g | 35g | |||
3 | 2.5g | 25g | 5g | ||
4 | 2.5g | 20g | 8g | ||
5 | 2.5g | 15g | 5g | 2g | |
6 | 2.5g | 15g | 3g |
Claims (3)
1. triprolidine hydrochloride dropping pill and preparation technology thereof is characterized in that by triprolidine hydrochloride (Triprolidine Hydrochloride) and drop pill substrate formulated.The weight ratio of each composition is:
Triprolidine hydrochloride: drop pill substrate=1: 1~1: 20.
2. triprolidine 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 triprolidine hydrochloride dropping pill, it is characterized in that preparation method is as follows: get triprolidine hydrochloride, pulverize, sieve.Triprolidine hydrochloride mixes by weight 1: 1~1: 20 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 200510061706 CN1813727A (en) | 2005-11-28 | 2005-11-28 | Triprolidine hydrochloride dropping pill and its preparing method |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN 200510061706 CN1813727A (en) | 2005-11-28 | 2005-11-28 | Triprolidine hydrochloride dropping pill and its preparing method |
Publications (1)
Publication Number | Publication Date |
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CN1813727A true CN1813727A (en) | 2006-08-09 |
Family
ID=36906162
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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CN 200510061706 Pending CN1813727A (en) | 2005-11-28 | 2005-11-28 | Triprolidine hydrochloride dropping pill and its preparing method |
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CN (1) | CN1813727A (en) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN106872632A (en) * | 2017-03-23 | 2017-06-20 | 南京济群医药科技股份有限公司 | A kind of RT HPLC detection method of triprolidine hydrochloride about material |
-
2005
- 2005-11-28 CN CN 200510061706 patent/CN1813727A/en active Pending
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN106872632A (en) * | 2017-03-23 | 2017-06-20 | 南京济群医药科技股份有限公司 | A kind of RT HPLC detection method of triprolidine hydrochloride about material |
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C06 | Publication | ||
PB01 | Publication | ||
C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
WD01 | Invention patent application deemed withdrawn after publication |