CN106265663A - A kind of stable bepotastine sheet and preparation method thereof - Google Patents
A kind of stable bepotastine sheet and preparation method thereof Download PDFInfo
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- CN106265663A CN106265663A CN201510237433.3A CN201510237433A CN106265663A CN 106265663 A CN106265663 A CN 106265663A CN 201510237433 A CN201510237433 A CN 201510237433A CN 106265663 A CN106265663 A CN 106265663A
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- bepotastine
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- disintegrating agent
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Abstract
The present invention relates to a kind of tablet containing bepotastine or its benzene sulfonate and preparation method thereof, belong to technical field of medicine.Described tablet contains bepotastine or its benzene sulfonate, diluent, binding agent, disintegrating agent and lubricant, described bepotastine or the preparation method of the tablet of its benzene sulfonate comprise the following steps: 1) obtain the step of blank granules, it is specially diluent, binding agent and/or disintegrating agent mix homogeneously, add appropriate wetting agent and/or adhesive is pelletized；2) obtain the step of tabletting granule, be specially and blank granules is mixed homogeneously with crude drug, lubricant and/or disintegrating agent；3) step of compression forming, specifically by suitable equipment by tabletting particles compress molding.The advantages such as the bepotastine sheet using the present invention to prepare has favorable reproducibility, and stripping property is good, and medicine stability is good, and technological operation is easy.
Description
Technical field
The present invention relates to a kind of bepotastine sheet, specifically, a kind of containing bepotastine or the tablet of its benzene sulfonate.The advantages such as the invention still further relates to the preparation method of bepotastine sheet, the sample using the method to prepare has favorable reproducibility, and stripping property is good, and medicine stability is good, and technological operation is easy.The invention belongs to preparation technique field.
Background technology
Bepotastine besilate is a kind of potent, long-acting histamine H 1 receptor antagonist, to 5-HT2, α 1, α 2 without affinity, it is possible to during suppression allergic inflammation, eosinophilic granulocyte is to the infiltration of inflammation part, the generation of suppression activation eosinophilic granulocyte IL-5.Bepotastine besilate is used for treating allergic rhinitis, and urticaria (eczema, dermatitis, skin pruritus, prurigo, dermatosis) and skin pruritus etc., clinical practice is extensive.
Bepotastine besilate is solid at normal temperatures, has two kinds of isomers of R, S, and wherein S-configuration has pharmacologically active.Bepotastine besilate is unstable under wet heat condition, easily produces R-isomer impurities, and then affects the treatment.Patent about bepotastine preparation has multiple, and as patent CN103547265A provides bepotastine oral cavity disintegration tablet and preparation method thereof, it is by by bepotastine or its salt, water-insoluble macromolecule wet granulation, and the tabletting such as the most additional disintegrating agent obtains.Patent CN103860516A provides a kind of bepotastine sheet utilizing polyvidone effectively to control dissolution and preparation method thereof, its by by crude drug, in add adjuvant mix after wet granulation obtain.Patent CN103816121A and CN1612734A all refer to by medicine and solubilizing composition or water-soluble metal chloride is soluble in water obtains liquid preparation.These patents have all used wet method, and it inevitably makes medicine directly contact with water, thus affects the stability of preparation.
The present invention passes through experimentation, has invented a kind of containing bepotastine or the tablet of its benzene sulfonate and preparation technology.The advantages such as the present invention fundamentally solves preparation stabilization sex chromosome mosaicism, has favorable reproducibility, and stripping property is good, and medicine stability is good, and technological operation is easy.
Summary of the invention
It is an object of the invention to provide a kind of bepotastine sheet and preparation method thereof, preparation technology is easy and simple to handle, favorable reproducibility, and stripping property is good, better stability of preparation.
The present invention furthers investigate, found that: by diluent, binding agent and/or disintegrating agent mix homogeneously, add appropriate wetting agent and/binding agent carries out granulation and obtains blank granules, then being mixed homogeneously with crude drug, lubricant and/or disintegrating agent by blank granules, compression forming can realize above-mentioned purpose.
The present invention relates to a kind of bepotastine sheet, specifically, it contains bepotastine or its benzene sulfonate, binding agent, diluent, disintegrating agent and lubricant.
The invention still further relates to the preparation method of a kind of bepotastine sheet, it is characterized in that, comprise the steps of 1) obtain the step of blank granules, it is specially diluent, binding agent and/or disintegrating agent mix homogeneously, add appropriate wetting agent and/binding agent is pelletized；2) obtain the step of tabletting granule, be specially and blank granules is mixed homogeneously with crude drug, lubricant and/or disintegrating agent；3) step of compression forming, specifically by suitable equipment by tabletting particles compress molding.
The invention still further relates to the preparation method of a kind of bepotastine sheet, it is characterised in that comprise the following steps: 1) obtain the step of blank granules, it is specially diluent and binding agent mix homogeneously, adds appropriate wetting agent and/or binding agent, pelletize；2) obtain the step of tabletting granule, be specially uniform with crude drug and mix lubricant for blank granules；3) step of compression forming, is specially, with tablet machine, tabletting is used particles compress molding.
The invention still further relates to a kind of bepotastine sheet, it is characterised in that in described blank granules preparation process, described blank granules is by obtaining diluent, binding agent and/or disintegrating agent and suitable wetting agent mixing granulation.A kind of bepotastine sheet, it is characterised in that in described blank granules preparation process, described blank granules be by diluent and binding agent and suitable wetting agent mixes, wet granulation and obtain.
The present invention relates to a kind of bepotastine sheet, it is characterised in that in the preparation process of described tabletting granule, described tabletting granule is by being obtained by mixing blank granules with crude drug, lubricant and/or disintegrating agent.A kind of bepotastine sheet, it is characterised in that in the preparation process of described tabletting granule, the described granule for tabletting is by obtaining blank granules and crude drug and mix lubricant.
Tablet stripping property prepared by the present invention is good, good stability, and technological operation is easy.
Accompanying drawing explanation: accompanying drawing 1 is bepotastine sheet stripping curve in reference fluid；Accompanying drawing 2,3 and 4 is for there being related substance growth pattern.
Embodiment
The present invention elaborates the present invention by following example and comparative example, and described embodiment is not considered as circumscribed.
Embodiment 1: preparation embodiment
Preparation technology:
(1) 73g lactose, 28g microcrystalline Cellulose and 4g hypromellose being crossed 80 mesh sieve mix homogeneously, add suitable quantity of water soft material, 24 mesh are pelletized, are obtained blank granules 1；
(2) above-mentioned blank granules 1 is mixed homogeneously with 10g crude drug and 2g Pulvis Talci, obtain tabletting granule；
(3) tabletting machine, 120mg tablet weight, hardness 70～90N, Opadry coating.
Embodiment 2: preparation embodiment
Preparation technology:
(1) 85g mannitol, 41g microcrystalline Cellulose, 5g cross-linking sodium carboxymethyl cellulose being crossed 80 mesh sieve mix homogeneously, add the aqueous solution soft material containing 3g hydroxypropylcellulose, 20 mesh are pelletized, are obtained blank granules 1；
(2) above-mentioned blank granules 1 is mixed homogeneously with 11g crude drug and 2g magnesium stearate, obtain tabletting granule；
(3) tabletting machine, 150mg tablet weight, hardness 60～80N, Opadry coating.
Embodiment 3: preparation embodiment
Preparation technology:
(1) 70g mannitol, 40g microcrystalline Cellulose, 10g cross-linking sodium carboxymethyl cellulose and 5g sodium carboxymethyl cellulose being crossed 80 mesh sieve mix homogeneously, add water soft material processed, and 24 mesh are pelletized, and obtain blank granules 1；
(2) above-mentioned blank granules 1 is mixed homogeneously with 9g crude drug and 2g silicon dioxide, obtain tabletting granule；
(3) tabletting machine, 140mg tablet weight, hardness 70～90N, Opadry coating.
Embodiment 4: comparative example
Embodiment 4a:(1) crude drug of recipe quantity, lactose, microcrystalline Cellulose and hypromellose in embodiment 1 are crossed 80 mesh sieve mix homogeneously, add suitable quantity of water soft material, 24 mesh are pelletized, are obtained granule 1；(2) by granule 1 and recipe quantity Pulvis Talci mix homogeneously, tabletting granule is obtained；(3) with embodiment 1.
Embodiment 4b:(1) crude drug of recipe quantity, mannitol, microcrystalline Cellulose and cross-linking sodium carboxymethyl cellulose in embodiment 2 are crossed 80 mesh sieve mix homogeneously, add the aqueous solution soft material containing recipe quantity hydroxypropylcellulose, 20 mesh are pelletized, are obtained granule 1；(2) granule 1 is mixed homogeneously with recipe quantity magnesium stearate, obtain tabletting granule；(3) with embodiment 2.
Embodiment 4c:(1) crude drug of recipe quantity, mannitol, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose and sodium carboxymethyl cellulose in embodiment 3 are crossed 80 mesh sieve mix homogeneously, add water soft material processed, and 24 mesh are pelletized, and obtain granule 1；(2) by granule 1 and recipe quantity silicon dioxide mix homogeneously, tabletting granule is obtained；(3) with embodiment 3.
Dissolution is investigated
Algoscopy: take this product, according to dissolution method (Chinese Pharmacopoeia two annex XC the second methods of version in 2010), with 900ml water as dissolution medium, rotating speed is 50rpm, operates in accordance with the law, and when 30min, sampling detects and calculates the stripping quantity of every.
Embodiment 1 and embodiment 4a being carried out dissolution investigation, samples in 5min, 10min, 15min and 30min, and result drawn together with control formulation, result is shown in accompanying drawing 1.
Study on the stability
Take the embodiment of the present invention 1～4 sample, according to annex XIXC medicine stability guideline in Chinese Pharmacopoeia version in 2010, accelerated stability investigation is carried out after simulation commercially available back, and 0 month after placing, 1 month, 3 months and sampling in 6 months, investigating its stability, result sees attached list 1, has related substance growth pattern to see accompanying drawing 2,3 and 4.
Result of the test shows that sample stripping property prepared by the present invention is good, good stability.
Use embodiment that the present invention is set forth.It should be appreciated that embodiment is only used to illustrate the present invention.On the premise of without departing from protection scope of the present invention, those skilled in the art can design replacement and improvement project according to the present invention, is considered as within the scope of the present invention.
Table 1 study on the stability table
Claims (10)
1. the present invention relates to a kind of bepotastine sheet, specifically, its comprise bepotastine or its benzene sulfonate, diluent, binding agent, disintegrating agent and
Lubricant.Wherein the mass ratio of crude drug is 3%～20%, and the mass ratio of diluent is 40%～90%, and the mass ratio of binding agent is
1～10%, the mass ratio of disintegrating agent is 0%～8%, and the consumption of lubricant is 0.2～4%.
Bepotastine sheet the most according to claim 1, its diluent is one or both in mannitol, microcrystalline Cellulose and lactose.
Bepotastine sheet the most according to claim 1, its binding agent is in hydroxypropyl methylcellulose, hydroxypropyl cellulose and sodium carboxymethyl cellulose
One or both.
Bepotastine sheet the most according to claim 1, its disintegrating agent is the one in cross-linking sodium carboxymethyl cellulose and low-substituted hydroxypropyl cellulose
Or two kinds.
Bepotastine sheet the most according to claim 1, its lubricant is one or both in magnesium stearate, Pulvis Talci and silicon dioxide.
6. the preparation method of a bepotastine sheet, it is characterised in that comprise the following steps: 1) obtain the step of blank granules, it is specially diluent,
Binding agent and/or disintegrating agent mix homogeneously, add appropriate wetting agent, pelletize；2) obtaining the step of tabletting granule, being specially will
Blank granules is mixed homogeneously with crude drug, lubricant and/or disintegrating agent；3) step of compression forming, will pressure specifically by suitable equipment
Sheet particles compress molding.
7. a bepotastine sheet, it is characterised in that in described blank granules preparation process, described blank granules is by by diluent, viscous
Mixture and/or disintegrating agent and suitable wetting agent mixing granulation and obtain.
8. a bepotastine sheet, it is characterised in that in described blank granules preparation process, described blank granules is by diluent, viscous
Mixture and/or disintegrating agent and the mixing of suitable wetting agent, wet granulation and obtain.
9. a bepotastine sheet, it is characterised in that in the preparation process of described tabletting granule, described tabletting granule is by by blank
Granule is mixed homogeneously with crude drug, lubricant and/or disintegrating agent and is obtained.
10. a bepotastine sheet, it is characterised in that in the preparation process of described tabletting granule, described tabletting granule is by inciting somebody to action
Blank granules and crude drug, mix lubricant and obtain.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510237433.3A CN106265663A (en) | 2015-05-12 | 2015-05-12 | A kind of stable bepotastine sheet and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510237433.3A CN106265663A (en) | 2015-05-12 | 2015-05-12 | A kind of stable bepotastine sheet and preparation method thereof |
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| CN106265663A true CN106265663A (en) | 2017-01-04 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510237433.3A Pending CN106265663A (en) | 2015-05-12 | 2015-05-12 | A kind of stable bepotastine sheet and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108309947A (en) * | 2018-04-04 | 2018-07-24 | 南京海纳医药科技股份有限公司 | A kind of tablet and preparation method thereof of benzene sulphur bepotastine |
-
2015
- 2015-05-12 CN CN201510237433.3A patent/CN106265663A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108309947A (en) * | 2018-04-04 | 2018-07-24 | 南京海纳医药科技股份有限公司 | A kind of tablet and preparation method thereof of benzene sulphur bepotastine |
| CN108309947B (en) * | 2018-04-04 | 2020-07-17 | 南京海纳医药科技股份有限公司 | Bepotastine besilate tablet and preparation method thereof |
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| C06 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20170104 |
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| WD01 | Invention patent application deemed withdrawn after publication |