CN106692090A - Bilastine tablets and preparation method thereof - Google Patents
Bilastine tablets and preparation method thereof Download PDFInfo
- Publication number
- CN106692090A CN106692090A CN201710078684.0A CN201710078684A CN106692090A CN 106692090 A CN106692090 A CN 106692090A CN 201710078684 A CN201710078684 A CN 201710078684A CN 106692090 A CN106692090 A CN 106692090A
- Authority
- CN
- China
- Prior art keywords
- bilastine
- mesh sieves
- disintegrant
- piece
- filler
- 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.)
- Pending
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
Abstract
The invention belongs to the technical field of medicines and relates to bilastine tablets and a preparation method thereof. The tablets are prepared by adopting a wet-process granulation process with good flowability and compression forming property; and the obtained tablets have complete and smooth surfaces, uniform color and luster and good taste.
Description
Technical field
The invention belongs to technical field of medicine.
Background technology
Bilastine（bilastine）Chemical name be 2- [4- [2- [4- [1- (2- ethoxyethyl groups) benzo dimazole-
2- yls] -1- bases] ethyl] phenyl] -2- dimethyl acetic acids are the 2nd generation histamine H1-receptors of FAES drugmakers of Spain exploitation
Antagonist, this product without liver first-pass effect, without maincenter sedation, acardia toxicity, not with cytochrome P 450 enzymes substrate phase
Interaction and there is potent antihistaminic characteristic, for treating adult and teenager（＞ 12 years old）Nettle rash and seasonal allergic effect
Property nose conjunctivitis.
The present invention is mixed using main ingredient bilastine with auxiliary material pharmaceutically, wet granule compression tablet；Prepared there is provided one kind
Process is simple, low cost, bilastine piece convenient to take and being easily achieved big production and preparation method thereof.
The content of the invention
It is an object of the invention to provide the conventional tablet that a kind of process is simple, appearance character are bright and clean.The present invention relates to
A kind of to mix main ingredient bilastine with interior plus auxiliary material, inside and outside method adds disintegrant, and tablet is obtained by wet granulation.First
Bulk drug bilastine was crushed into 100 mesh sieves crossed 80 mesh sieves with interior plus auxiliary material and mix 3 ~ 6 times, it is preferably 4 ~ 5 times, well mixed；
Wherein filler is in lactose, mannitol, sorbierite, microcrystalline cellulose, xylitol, fructose, starch and starch derivatives
Plant or several, preferably lactose and microcrystalline cellulose；Add adhesive or wetting agent, adhesive or wetting agent be hydroxypropylcellulose,
One or more in PVP, ethanol, water, preferably 30% ethanol water crosses the granulation of 20 mesh sieves.50 DEG C of forced air dryings, moisture dries
To 1 ~ 3%.Drying particle is weighed, conversion yield is additional, additional disintegrant is pregelatinized starch, sodium carboxymethyl starch, low substitution
One or more in hydroxypropyl cellulose, Ac-Di-Sol, preferably sodium carboxymethyl starch, the consumption of disintegrant are pressed
Percentage by weight is 1% ~ 10%；Additional lubricant is magnesium stearate, Magnesiumaluminumsilicate, sodium stearyl fumarate, sucrose fatty ester, list
One or more in tristerin, talcum powder, stearic acid, silica, preferably magnesium stearate and silica；It is additional
One or more in flavouring aspartame, acesulfame potassium, menthol, Mint Essence, stevioside, vanilla, preferably Ah Si
Pa Tan, Mint Essence.
The tablet appearance prepared using this method is completely bright and clean, uniform color, convenient to take, good mouthfeel.
Specific embodiment
Following examples further describe beneficial effects of the present invention, and embodiment is only used for the purpose of illustration, and this is not limited
The scope of invention, while those of ordinary skill in the art are also contained according to the obvious change made of the invention and modification
Within the scope of the invention.
（One）The preparation of normal oral tablet
Embodiment 1
Preparation technology
Bilastine was crushed into 100 sieves crossed 80 mesh sieves with interior plus auxiliary material and mix 4 times, mixing, 30% ethanol water is used as wetting
Agent, softwood processed, 20 mesh sieves granulation, 50 DEG C of forced air dryings, moisture is dried to 1 ~ 3%, and drying particle is crossed into 20 mesh sieve whole grains, weighs,
Conversion yield, additional sodium carboxymethyl starch, silica, aspartame and magnesium stearate, the scrobicula stampings of Φ 6, piece weighs 100
Mg, hardness 40-60 N.
Embodiment 2
Preparation technology
Bilastine was crushed into 100 mesh sieves crossed 80 mesh sieves with mannitol and mixed 4 times, mixed, 30% ethanol water was used as wetting
Agent, softwood processed, 20 mesh sieves granulation, 50 DEG C of forced air dryings, moisture is dried to 1 ~ 3%, and drying particle is crossed into 20 mesh sieve whole grains, weighs,
Conversion yield, additional sodium carboxymethyl starch, silica, aspartame, Mint Essence and magnesium stearate, the scrobicula stampings of Φ 6,
Piece weighs 100 mg, hardness 40-60 N.
Embodiment 3
Preparation technology
Bilastine was crushed into 100 mesh sieves crossed 80 mesh sieves with interior plus auxiliary material and mix 4 times, crushed, 100 mesh sieves of mistake, 30% ethanol
Used as wetting agent, softwood processed, 20 mesh sieves granulation, 50 DEG C of forced air dryings, moisture is dried to 1 ~ 3% to water, and drying particle is crossed into 20 mesh sieves
Whole grain, weighs, and converts yield, additional sodium carboxymethyl starch, silica, aspartame, Mint Essence and magnesium stearate, Φ 6
Scrobicula stamping, piece weighs 100 mg, hardness 40-60 N.
Embodiment 4
Preparation technology
Bilastine was crushed into 100 mesh sieves crossed 80 mesh sieves with interior plus auxiliary material and mix 4 times, 30% ethanol water was made as wetting agent
Softwood, 20 mesh sieves granulation, 50 DEG C of forced air dryings, moisture is dried to 1 ~ 3%, and drying particle is crossed into 20 mesh sieve whole grains, weighs, and conversion is received
Rate, additional hydroxypropyl cellulose（Low substitution）, silica, aspartame and magnesium stearate, the scrobicula stampings of Φ 6, piece weighs 100
Mg, hardness 40-60 N.
Embodiment 5
Preparation technology
Bilastine was crushed into 100 mesh sieves, crossing 80 mesh sieves with interior plus auxiliary material mixes 4 times, 30% ethanol water as wetting agent,
Softwood processed, 20 mesh sieves granulation, 50 DEG C of forced air dryings, moisture is dried to 1 ~ 3%, and drying particle is crossed into 20 mesh sieve whole grains, weighs, and converts
Yield, additional Ac-Di-Sol, silica, aspartame and talcum powder, the scrobicula stampings of Φ 6, piece weighs 100
Mg, hardness 40-60 N.
Embodiment 6
Preparation technology
Bilastine was crushed into 100 mesh sieves, crossing 80 mesh sieves with interior plus auxiliary material mixes 4 times, 30% ethanol water as wetting agent,
Softwood processed, 20 mesh sieves granulation, 50 DEG C of forced air dryings, moisture is dried to 1 ~ 3%, and drying particle is crossed into 20 mesh sieve whole grains, weighs, and converts
Yield, additional Ac-Di-Sol, silica, aspartame and magnesium stearate, the scrobicula stampings of Φ 6, piece weighs 100
Mg, hardness 40-60 N.
Embodiment 7
Preparation technology
Bilastine was crushed into 100 mesh sieves, crossing 80 mesh sieves with interior plus auxiliary material mixes 4 times, 30% ethanol water as wetting agent,
Softwood processed, 20 mesh sieves granulation, 50 DEG C of forced air dryings, moisture is dried to 1 ~ 3%, and drying particle is crossed into 20 mesh sieve whole grains, weighs, and converts
Yield, additional Ac-Di-Sol, silica, aspartame and magnesium stearate, the scrobicula stampings of Φ 6, piece weighs 100
Mg, hardness 40-60 N.
By the comparing of above-described embodiment 1 ~ 7, bilastine is used the preparation technology of conventional wet lay pelletizing press sheet
Simply, good fluidity, compressibility be good, low cost, is easily achieved big production, the complete bright and clean, color and luster of obtained tablet appearance
Uniformly, good mouthfeel, convenient to take.
Claims (10)
1. a kind of bilastine piece：Contain bilastine and filler, disintegrant, adhesive or wetting agent, flavouring and lubrication
Agent.
2. according to the bilastine piece described in claim 1, bilastine is crossed into 80 mesh sieves with interior plus auxiliary material, mixed 3 ~ 6 times, used
Wet granulation technology and obtain.
3. according to the bilastine piece described in claim 1, wherein filler be lactose, mannitol, sorbierite, microcrystalline cellulose,
One or more in starch and starch derivatives.
4., according to described in claim 1, the consumption of filler is 20 ~ 50% by weight percentage.
5., according to described in claim 1, disintegrant uses sodium carboxymethyl starch, PVPP, low-substituted hydroxypropyl cellulose, friendship
Connection sodium carboxymethylcellulose in one or more.
6., according to described in claim 1, the consumption of disintegrant is 1% ~ 10% by weight percentage.
7., according to described in claim 1, adhesive or wetting agent are the one kind or several in hydroxypropylcellulose, PVP, ethanol, water
Kind.
8., according to described in claim 1, lubricant is magnesium stearate, Magnesiumaluminumsilicate, sodium stearyl fumarate, sucrose fatty ester, list
One or more in tristerin, talcum powder, stearic acid, silica.
9., according to described in claim 1, the consumption of lubricant is 1% ~ 5% by weight percentage.
10., according to described in claim 1, flavouring is aspartame, sucrose, acesulfame potassium, menthol, Mint Essence, stevioside, perfume (or spice)
Hay-scented essence in one or more.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710078684.0A CN106692090A (en) | 2017-02-14 | 2017-02-14 | Bilastine tablets and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710078684.0A CN106692090A (en) | 2017-02-14 | 2017-02-14 | Bilastine tablets and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106692090A true CN106692090A (en) | 2017-05-24 |
Family
ID=58909166
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710078684.0A Pending CN106692090A (en) | 2017-02-14 | 2017-02-14 | Bilastine tablets and preparation method thereof |
Country Status (1)
| Country | Link |
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| CN (1) | CN106692090A (en) |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3453384A1 (en) | 2017-09-07 | 2019-03-13 | Alfred E. Tiefenbacher (GmbH & Co. KG) | Pharmaceutical tablet composition comprising bilastine |
| EP3470062A1 (en) * | 2017-12-18 | 2019-04-17 | Alfred E. Tiefenbacher (GmbH & Co. KG) | Pharmaceutical tablet composition comprising bilastine and magnesium aluminometasilicate |
| WO2019097091A1 (en) | 2017-12-18 | 2019-05-23 | Alfred E. Tiefenbacher (Gmbh & Co. Kg) | Pharmaceutical tablet composition comprising bilastine form 3 and a water-soluble filler |
| CN113116833A (en) * | 2020-01-15 | 2021-07-16 | 鲁南制药集团股份有限公司 | Bilastine tablet and preparation method thereof |
| CN114099450A (en) * | 2020-08-31 | 2022-03-01 | 长春海悦药业股份有限公司 | Bilastine tablet and preparation method thereof |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103356616A (en) * | 2013-06-29 | 2013-10-23 | 北京万全德众医药生物技术有限公司 | Bilastine-containing pharmaceutical composition and preparation method thereof |
| US20150057255A1 (en) * | 2013-06-24 | 2015-02-26 | Tigercat Pharma, Inc. | Use of nk-1 receptor antagonists in pruritus |
| CN104398512A (en) * | 2014-10-23 | 2015-03-11 | 万全万特制药江苏有限公司 | Bilastine-containing pharmaceutical composition and preparing method thereof |
| CN104398481A (en) * | 2014-10-29 | 2015-03-11 | 万全万特制药江苏有限公司 | Bilastine orally disintegrating tablet and preparing method thereof |
| CN104447683A (en) * | 2013-09-12 | 2015-03-25 | 天津市汉康医药生物技术有限公司 | Stable Bilastine compound |
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2017
- 2017-02-14 CN CN201710078684.0A patent/CN106692090A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US20150057255A1 (en) * | 2013-06-24 | 2015-02-26 | Tigercat Pharma, Inc. | Use of nk-1 receptor antagonists in pruritus |
| CN103356616A (en) * | 2013-06-29 | 2013-10-23 | 北京万全德众医药生物技术有限公司 | Bilastine-containing pharmaceutical composition and preparation method thereof |
| CN104447683A (en) * | 2013-09-12 | 2015-03-25 | 天津市汉康医药生物技术有限公司 | Stable Bilastine compound |
| CN104398512A (en) * | 2014-10-23 | 2015-03-11 | 万全万特制药江苏有限公司 | Bilastine-containing pharmaceutical composition and preparing method thereof |
| CN104398481A (en) * | 2014-10-29 | 2015-03-11 | 万全万特制药江苏有限公司 | Bilastine orally disintegrating tablet and preparing method thereof |
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| 马欣欣等: "比拉斯汀在荨麻疹治疗中的应用", 《国际皮肤性病学杂志》 * |
| 魏秀芝等主编: "《临床诊疗与护理》", 31 March 2016, 吉林科学出版社 * |
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3453384A1 (en) | 2017-09-07 | 2019-03-13 | Alfred E. Tiefenbacher (GmbH & Co. KG) | Pharmaceutical tablet composition comprising bilastine |
| EP3470062A1 (en) * | 2017-12-18 | 2019-04-17 | Alfred E. Tiefenbacher (GmbH & Co. KG) | Pharmaceutical tablet composition comprising bilastine and magnesium aluminometasilicate |
| WO2019097091A1 (en) | 2017-12-18 | 2019-05-23 | Alfred E. Tiefenbacher (Gmbh & Co. Kg) | Pharmaceutical tablet composition comprising bilastine form 3 and a water-soluble filler |
| WO2019097090A1 (en) | 2017-12-18 | 2019-05-23 | Alfred E. Tiefenbacher (Gmbh & Co. Kg) | Pharmaceutical tablet composition comprising bilastine and magnesium aluminometasilicate |
| ES2773756R1 (en) * | 2017-12-18 | 2021-04-12 | Tiefenbacher Alfred E Gmbh & Co Kg | Tablet pharmaceutical composition comprising bilastine form 3 and a water soluble filler |
| CN113116833A (en) * | 2020-01-15 | 2021-07-16 | 鲁南制药集团股份有限公司 | Bilastine tablet and preparation method thereof |
| CN113116833B (en) * | 2020-01-15 | 2024-01-23 | 鲁南制药集团股份有限公司 | Bilastine tablet and preparation method thereof |
| CN114099450A (en) * | 2020-08-31 | 2022-03-01 | 长春海悦药业股份有限公司 | Bilastine tablet and preparation method thereof |
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Application publication date: 20170524 |