CN107412174A - A kind of Rupatadine fumarate oral disintegrating tablet and preparation method thereof - Google Patents

A kind of Rupatadine fumarate oral disintegrating tablet and preparation method thereof Download PDF

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Publication number
CN107412174A
CN107412174A CN201710186551.5A CN201710186551A CN107412174A CN 107412174 A CN107412174 A CN 107412174A CN 201710186551 A CN201710186551 A CN 201710186551A CN 107412174 A CN107412174 A CN 107412174A
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CN
China
Prior art keywords
rupatadine fumarate
disintegrating tablet
oral disintegrating
flavouring
taste masking
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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
Application number
CN201710186551.5A
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Chinese (zh)
Inventor
张迪
王宇杰
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Beijing Wanquan Dezhong Medical Biological Technology Co Ltd
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Beijing Wanquan Dezhong Medical Biological Technology Co Ltd
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Priority to CN201710186551.5A priority Critical patent/CN107412174A/en
Publication of CN107412174A publication Critical patent/CN107412174A/en
Pending legal-status Critical Current

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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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • 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
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K9/2009—Inorganic compounds
    • 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
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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 application provides the Rupatadine fumarate oral disintegrating tablet and preparation method that can cover medicine bitter taste itself, oral disintegrating tablet described herein is using Rupatadine fumarate as raw material, filler, disintegrant, flavouring, lubricant etc. are auxiliary material, coating material is used under given conditions, and pass through specific preparation method, it is made using tabletting machine.The implementation of the application is intended to improve the mouthfeel of Rupatadine fumarate oral disintegrating tablet, the problems such as overcoming bulk drug to bring insufferable bitter taste or the excessive sweetener flavoring of application and caused polysaccharose substance to be taken in, assign oral disintegrating tablet quick disintegration time limited simultaneously, the Rupatadine fumarate oral disintegrating tablet that a kind of absorption is fast, bioavilability is high, side effect is low and convenient to take is provided to patient.

Description

A kind of Rupatadine fumarate oral disintegrating tablet and preparation method thereof
Technical field
The application belongs to technical field of medicine, and in particular to a kind of Rupatadine fumarate oral disintegrating tablet taste masking technology and Its preparation method.
Background technology
Rupatadine fumarate piece be Uriach drugmakers of Spain develop new, potent antiallergic, 2003 3 Months 15 days listed first in Spain, its specification is 10mg, trade name（Rupafin）.As a kind of antiallergic, Lu Pata Determine to have and be substantially better than other antiallergics（Loratadine, cetirizine, Mizolastine, Desloratadine, epinastine etc.） Performance, it has antihistamine and antagonism platelet activating factor simultaneously（PAF）Double effects, and commercially available most of anti-mistakes Quick medicine only has anti-histamine activity effect, it is clear that while have antihistamine and antagonism PAF medicine will be than only blocking wherein one Kind has more preferable clinical effectiveness, while the side effect such as Rupatadine absent cardiovascular and nervous centralis, is expected to turn into treatment allergy The first-line drug of property rhinitis and allergic urticaria, has obvious potential applicability in clinical practice.
Oral disnitegration tablet refers to be not required to water or need to use a small amount of water, and without chewing, tablet is placed in lingual surface, and it is molten rapidly to meet saliva After solution or disintegration, by means of power is swallowed, medicine can enter the tablet of stomach action.Compared with conventional tablet, oral disintegrating tablet have it is rapid-action, Bioavilability is high, convenient to take, the advantages such as first pass effect is low, based on this, its be more suitable for old man, children, dysphagia or The patient's medication drunk water under the particular surroundings such as inconvenience.
The application carries out taste masking to Rupatadine fumarate under given conditions, using coating material, and by specific Preparation method, oral disintegrating tablet is prepared using tablet press machine, have that preparation method is novel, easy industrialization, the advantages that taste masking effect is good.
The content of the invention
The purpose of the application is the mouthfeel for improving Rupatadine fumarate oral disintegrating tablet, and overcoming other tablets, flavoring is not brought Insufferable bitter taste or the excessive sweetener flavoring of application and the problems such as caused polysaccharose substance to be taken in, while assign mouth and collapse Piece quick disintegration time limited.The rich horse that a kind of absorption is fast, bioavilability is high, side effect is low and convenient to take is provided to patient Sour Rupatadine oral disintegrating tablet and preparation method.
The purpose of the application solves by following scheme：
The preparation method of Rupatadine fumarate oral disintegrating tablet, preparation process comprise the following steps：
The taste masking of first step Rupatadine fumarate is handled：
（1）Adsorb taste masking
A certain amount of Rupatadine fumarate is crossed into 100 mesh sieves, and is well mixed with silica, it is stand-by.
（2）Powder coating taste masking
The first step takes selected coating material, is dissolved with appropriate lyase and is diluted to debita spissitudo, uses high-shear homogenate machine It is standby or colloid mill fully homogenizes 10min, then taking Rupatadine fumarate powder to be placed in fluid bed makes it fully fluidize, so Coating solution is sprayed with appropriate speed afterwards, carries out powder coating, obtains Rupatadine fumarate powder coating particle, is sieved after drying It is standby.
Flavouring is crossed 80 mesh sieves by second step, weighs the flavouring of recipe quantity and the bulk drug of first step processing, and mix It is uniformly standby.
3rd step weighs the filler, disintegrant, flavouring of recipe quantity, crosses 80 mesh sieves successively, and handled with second step Material sieving is well mixed, adds adhesive softwood, the granulation of 24 mesh.50 DEG C of baking oven forced air dryings, moisture are dried to 1-3%, will dry The mesh sieve whole grain of dry particl 24, and convert the additional tabletting of yield.
Further, the coating material for taste masking is Eudragit®E100、Eudragit® EPO、Eudragit® One or more in L100, hydroxypropyl methyl cellulose.
Further, the sorbing material for taste masking is silica.
Further, sorbing material silica content is about 20-40%（Weight ratio）, preferably 25%-35%.
Further, oral disnitegration tablet described herein is by Rupatadine fumarate and filler, disintegrant, lubrication The auxiliary materials such as agent, flavouring form.
Further, filler be mannitol, microcrystalline cellulose, lactose, starch, dextrin, sorbierite etc. any one or Two or more mixtures；
Further, disintegrant is PVPP（PVPP）, sodium carboxymethyl starch（CMS-Na）, low substituted hydroxy-propyl fiber Element（L-HPC）, Ac-Di-Sol（CCNa）Deng any one or two or more mixtures；
Further, flavouring be Aspartame, stevioside, honey element, menthol, Sucralose, essence etc. any one or Two or more mixtures；
Further, lubricant be magnesium stearate, sodium stearyl fumarate, talcum powder, stearic acid etc. any one.
Embodiment
, below will be by embodiments of the invention and experimental data to of the invention and its excellent in order to be better understood from the present invention Gesture and beneficial effect are described in detail and illustrated, respectively to absorption taste masking method, powder coating taste masking method for example, but these Embodiment is not intended to limit the present invention.
Embodiment one adsorbs taste masking method
Prescription
Preparation technology
Rupatadine fumarate is crossed 100 mesh sieves by 1, and is well mixed with silica；
2 added the orange powdered flavor of 80 mesh sieves and were well mixed；
3 mannitol, microcrystalline cellulose, low-substituted hydroxypropyl cellulose for sequentially adding 80 mesh sieves are well mixed, using pure water as profit Humectant, the granulation of 24 mesh sieves, 50 DEG C of baking oven forced air dryings, moisture are dried to 1-3%, and drying particle is crossed into 24 mesh sieve whole grains, weighs, rolls over Calculate yield, additional menthol, Sucralose, magnesium stearate and low-substituted hydroxypropyl cellulose tabletting.Oral disintegrating tablet made from the prescription The micro- sweet tea of entrance, there are menthol refrigerant sense, no bitter taste, the Orally disintegrating time is less than 60S.
Embodiment two adsorbs taste masking method
Prescription
Preparation technology
Rupatadine fumarate is crossed 100 mesh sieves by 1, and is well mixed with silica；
2 added the orange powdered flavor of 80 mesh sieves and were well mixed；
3 mannitol, microcrystalline cellulose, low-substituted hydroxypropyl cellulose for sequentially adding 80 mesh sieves are well mixed, using pure water as profit Humectant, the granulation of 24 mesh sieves, 50 DEG C of baking oven forced air dryings, moisture are dried to 1-3%, and drying particle is crossed into 24 mesh sieve whole grains, weighs, rolls over Calculate yield, additional menthol, Sucralose, magnesium stearate and low-substituted hydroxypropyl cellulose tabletting.Oral disintegrating tablet made from the prescription The micro- sweet tea of entrance, there are menthol refrigerant sense, no bitter taste, the Orally disintegrating time is less than 60S.
The powder coating taste masking method of embodiment three
Prescription
Preparation technology
1 by a certain amount of hydroxypropyl methyl cellulose, Eudragit®E100 is added to appropriate ethanol（70%）In,
10min is fully homogenized using high-shear homogenate machine or colloid mill, it is standby；
2 weigh appropriate Rupatadine fumarate powder and are placed in fluid bed and it is fully fluidized, and then spray bag with appropriate speed Clothing liquid, powder coating is carried out, obtain Rupatadine fumarate powder coating particle, it is standby that 0.5mm sieves are crossed after drying；
3 added the orange powdered flavor of 80 mesh sieves and were well mixed；
4 mannitol, microcrystalline cellulose, low-substituted hydroxypropyl cellulose for sequentially adding 80 mesh sieves are well mixed, using pure water as profit Humectant, the granulation of 24 mesh sieves, 50 DEG C of baking oven forced air dryings, moisture are dried to 1-3%, and drying particle is crossed into 24 mesh sieve whole grains, weighs, rolls over Calculate yield, additional menthol, Sucralose, magnesium stearate and low-substituted hydroxypropyl cellulose tabletting.Oral disintegrating tablet made from the prescription The micro- sweet tea of entrance, there are menthol refrigerant sense, no bitter taste, the Orally disintegrating time is less than 60S.
Example IV powder coating taste masking method
Prescription
Preparation technology
1 by a certain amount of ethyl cellulose, Eudragit®EPO、Eudragit®NE30D is added to appropriate ethanol（70%） In, 10min is fully homogenized using high-shear homogenate machine or colloid mill, it is standby；
2 weigh appropriate Rupatadine fumarate powder and are placed in fluid bed and it is fully fluidized, and then spray bag with appropriate speed Clothing liquid, powder coating is carried out, obtain Rupatadine fumarate powder coating particle, it is standby that 0.5mm sieves are crossed after drying；
3 added the orange powdered flavor of 80 mesh sieves and were well mixed；
4 mannitol, microcrystalline cellulose, low-substituted hydroxypropyl cellulose for sequentially adding 80 mesh sieves are well mixed, using pure water as profit Humectant, the granulation of 24 mesh sieves, 50 DEG C of baking oven forced air dryings, moisture are dried to 1-3%, and drying particle is crossed into 24 mesh sieve whole grains, weighs, rolls over Calculate yield, additional menthol, Sucralose, magnesium stearate and low-substituted hydroxypropyl cellulose tabletting.Oral disintegrating tablet made from the prescription The micro- sweet tea of entrance, there are menthol refrigerant sense, no bitter taste, the Orally disintegrating time is less than 60S.
Comparative example
Prescription
Preparation technology
Rupatadine fumarate is crossed 100 mesh sieves by 1, standby.
2 added the orange powdered flavor of 80 mesh sieves and were well mixed.
3 mannitol, microcrystalline cellulose, low-substituted hydroxypropyl cellulose for sequentially adding 80 mesh sieves are well mixed, with pure water For wetting agent, the granulation of 24 mesh sieves, 50 DEG C of baking oven forced air dryings, moisture is dried to 1-3%, and drying particle is crossed into 24 mesh sieve whole grains, claimed Weight, convert yield, additional menthol, Sucralose, magnesium stearate and low-substituted hydroxypropyl cellulose tabletting.Mouth made from the prescription Disintegrating tablet enters that bitter taste sense is stronger, and the Orally disintegrating time is less than 60S.

Claims (9)

1. the preparation method of Rupatadine fumarate oral disintegrating tablet, preparation process comprise the following steps：
The taste masking of first step Rupatadine fumarate is handled：
Adsorb taste masking
A certain amount of Rupatadine fumarate is crossed into 100 mesh sieves, and is well mixed with silica, it is stand-by；
Powder coating taste masking
The first step takes selected coating material, is dissolved with appropriate solvent and is diluted to debita spissitudo, uses high-shear homogenate machine It is standby or colloid mill fully homogenizes 10min, then taking Rupatadine fumarate powder to be placed in fluid bed makes it fully fluidize, so Coating solution is sprayed with appropriate speed afterwards, carries out powder coating, obtains Rupatadine fumarate powder coating particle, is sieved after drying It is standby；
Flavouring is crossed 80 mesh sieves by second step, weighs the flavouring of recipe quantity and the bulk drug of first step processing, and be well mixed It is standby；
3rd step weighs the filler, disintegrant, flavouring of recipe quantity, crosses 80 mesh sieves, and the material handled with second step successively Sieving is well mixed, adds adhesive softwood, the granulation of 24 mesh；50 DEG C of baking oven forced air dryings, moisture are dried to 1-3%, by drying 24 mesh sieve whole grains of grain, and convert the additional tabletting of yield.
2. according to claim 1, the coating material for taste masking is Eudragit®E100、Eudragit® EPO、 Eudragit®One or more in L100, hydroxypropyl methyl cellulose.
3. according to claim 1, the sorbing material for taste masking is silica.
4. according to claim 3, sorbing material silica content is about 20-40%（Weight ratio）, preferably 25%-35%.
5. according to claim 1, oral disnitegration tablet described herein is by Rupatadine fumarate and filler, disintegration The auxiliary materials such as agent, lubricant, flavouring form.
6. according to claim 5, filler is that mannitol, microcrystalline cellulose, lactose, starch, dextrin, sorbierite etc. are any One or more kinds of mixtures.
7. according to claim 5, disintegrant is PVPP（PVPP）, sodium carboxymethyl starch（CMS-Na）, low substitution Hydroxypropyl cellulose（L-HPC）, Ac-Di-Sol（CCNa）Deng any one or two or more mixtures.
8. according to claim 5, flavouring is Aspartame, stevioside, honey element, menthol, Sucralose, essence etc. Any one or two or more mixtures.
9. according to claim 5, lubricant is that magnesium stearate, sodium stearyl fumarate, talcum powder, stearic acid etc. are any one Kind.
CN201710186551.5A 2017-03-27 2017-03-27 A kind of Rupatadine fumarate oral disintegrating tablet and preparation method thereof Pending CN107412174A (en)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111298134A (en) * 2020-02-26 2020-06-19 江苏艾立康药业股份有限公司 Rupatadine fumarate solid preparation composition and preparation method thereof

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CN1985816A (en) * 2005-12-22 2007-06-27 汕头大学医学院 Oral disintegrated rupatadine tablet and its preparing method
CN106491545A (en) * 2016-09-22 2017-03-15 万特制药(海南)有限公司 Fluoxetine hydrochloride oral disintegrating tablet and preparation method thereof

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111298134A (en) * 2020-02-26 2020-06-19 江苏艾立康药业股份有限公司 Rupatadine fumarate solid preparation composition and preparation method thereof

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