CN101632651B - Oral instant membrane of risperidone and preparation method thereof - Google Patents
Oral instant membrane of risperidone and preparation method thereof Download PDFInfo
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- CN101632651B CN101632651B CN2009100752727A CN200910075272A CN101632651B CN 101632651 B CN101632651 B CN 101632651B CN 2009100752727 A CN2009100752727 A CN 2009100752727A CN 200910075272 A CN200910075272 A CN 200910075272A CN 101632651 B CN101632651 B CN 101632651B
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- risperidone
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Abstract
The invention relates to an oral instant membrane of risperidone and a preparation method thereof, thereby being used for improving the using performance of the risperidone. The technical scheme is as follows: the instant membrane comprises 2-60 parts by weight of risperidone, 25-98 parts by weight of water-soluble pharmaceutical polymer excipients, additives and 0.1-25 parts by weight of water. The oral instant membrane solves the problems that the existing risperidone is clinically difficult to swallow, is not applicable to children and elderly patients for administration and can not be conveniently taken under the situation of having no water. The oral instant membrane can be dissolved on the tongue, the hidden trouble of choking can not be happened no matter how young a baby is, the active ingredients can be absorbed sublingually and absorbed by buccal mucosa, and the onset of action is more rapid in comparison with orally disintegrating tablets. In addition, the oral instant membrane has good compliance, thereby being particularly suitable for elderly people, children and patients with difficult swallowing.
Description
Technical field
The present invention relates to oral instant membrane of a kind of medicine and preparation method thereof, exactly relate to a kind of oral instant membrane of risperidone, belong to medical technical field.
Background technology
(Resperidone RIS), is benzo-isoxazole derivant to risperidone, and its chemical name is a 3-[2-[4-(6-fluoro-1,-2-benzoisoxazole-3-yl)-and piperidino] ethyl]-6,7,8,9-tetrahydrochysene-2-methyl-4H-pyrido [1,2-α] pyrimidin-4-one, structural formula is as follows:
Risperidone is a kind of novel atypical antipsychotic of being developed by Belgian Janssen Pharmaceutica.Be applicable to the tangible positive symptom (as hallucination, vain hope, disturbance in thinking, be hostile to and suspect) of the acute and chronic schizophrenia of treatment and other various psychotic disease states and tangible negative symptoms (indifferent and hypologia) as bradykinesia, amorphous type, social activity, also can be used for alleviating the emotion symptom relevant, as depression, sense of guilt, anxiety with schizophrenia.
At present, the clinical common formulations of risperidone is conventional tablet, oral liquid, oral cavity disintegration tablet.Conventional tablet is owing to be difficult to swallow, and juvenile crowd and gerontal patient are when taking this class dosage form medicine, and be not too suitable, do not having to make things convenient for the patient to take under the situation of water.Though oral cavity disintegration tablet has solved the problems referred to above to a certain extent,, have higher requirements to producing, pack, storing because oral cavity disintegration tablet is easy to moisture absorption.Need special Measuring glass when oral liquid is taken, carry also inconvenience, influenced the extensive use of risperidone oral formulations.
Summary of the invention
Technical problem to be solved by this invention provide a kind of taking convenience, onset rapidly, be convenient to preserve, the instant film of risperidone orally of stable in properties, the present invention also will provide the preparation method of the oral instant membrane of this risperidone.
The object of the present invention is achieved like this:
A kind of oral instant membrane of risperidone, described oral instant membrane component contain risperidone, water-soluble pesticide high polymer adjuvant, additive and water, and each components contents is counted by mass parts:
Risperidone 2～60,
Water-soluble pesticide high polymer adjuvant 25～98;
Water 0.1～25;
Described water solublity pharmaceutical polymers is a kind of or its mixture in polyvidone, gelatin, Lac, arabic gum, agar, modified starch, dextrin, hydroxypropyl emthylcellulose, hydroxypropyl cellulose, cellulose acetate-phthalate, acrylic resin, Polyethylene Glycol or the polyvinyl alcohol;
Described additive is flavoring agent, coloring agent, opacifier, plasticizer, antiseptic, pH mediator agent and disintegrating agent, and addition is:
Flavoring agent 0.05～20;
Coloring agent 0.01～3;
Opacifier 0.01～3;
Plasticizer 0.5%～15;
Antiseptic 0.05～3%;
PH mediator agent 0.1～6;
Disintegrating agent 0.5～15.
The oral instant membrane of above-mentioned risperidone, described flavoring agent are selected from a kind of or its mixture in aspartame, sucrose, stevioside, saccharin sodium, fructose, essence, spice, sucralose, Polacrilin Potassium (polacrilin potassium), the kayexalate.
The oral instant membrane of above-mentioned risperidone, described coloring agent is selected from color lake, pigment, FD﹠amp; A kind of or its mixture in the C dyestuff.
The oral instant membrane of above-mentioned risperidone, described plasticizer is selected from propylene glycol, Oleum Ricini, Polyethylene Glycol, silicone oil, glycerol, diethyl phthalate or dibutyl ester.
The oral instant membrane of above-mentioned risperidone, described opacifier are titanium dioxide.
The oral instant membrane of above-mentioned risperidone, described antiseptic are selected from a kind of or its mixture in sodium benzoate, potassium sorbate, Buddhist nun uncle tortoise beetle ester, the Ethyl Hydroxybenzoate.
The oral instant membrane of above-mentioned risperidone, described PH mediator agent are selected from a kind of or its mixture in citric acid, lactic acid, citric acid or the tartaric acid.
The oral instant membrane of above-mentioned risperidone, described disintegrating agent are selected from a kind of or its mixture in microcrystalline Cellulose, carboxymethyl starch sodium, cross-linking sodium carboxymethyl cellulose, pregelatinized Starch, polyvinylpolypyrrolidone or the low-substituted hydroxypropyl cellulose.
The oral instant membrane of above-mentioned risperidone, described hydroxypropyl emthylcellulose are that viscosity is lower than 50 centipoises, and preferred viscosity is the 3-20 centipoise.
A kind of method for preparing the oral instant membrane of above-mentioned risperidone, it carries out as follows:
A, will under agitation be scattered in 40～90% the ethanol except that the component the water soluble polymer adjuvant, supersound process is to dissolving;
B, the water soluble polymer adjuvant is under agitation added in the above-mentioned solution, fully disperse gel;
C, the degassing are evenly coated above-mentioned risperidone gel on the flat board, air blast, heat drying, and heating-up temperature is 50～70 ℃, cuts, and gets the oral instant membrane of risperidone.
The instant film of risperidone orally of the present invention preparation has solved the clinical common formulations of present risperidone such as conventional tablet, oral liquid, oral cavity disintegration tablet is difficult to swallow, juvenile crowd and gerontal patient take not too suitable, and problem such as do not having conveniently to take under the situation of water, it can dissolve on tongue, no matter the hidden danger of being choked can not take place in how little baby, effective ingredient absorbs in Sublingual and buccal mucosa, and onset is also wanted rapidly than oral cavity disintegration tablet.In addition, the present invention's compliance of taking medicine is good, the patient of suitable especially old man, child and dysphagia.
The specific embodiment
The invention will be further described below in conjunction with specific embodiment.
Embodiment 1
Component weight (g)
Risperidone 10
Hydroxypropyl emthylcellulose (5 centipoise) 500
70% ethanol 1000
Specific operation process: risperidone under agitation is scattered in 70% the ethanol, supersound process is to dissolving, hydroxypropyl emthylcellulose (5 centipoise) is under agitation added above-mentioned solution, fully disperse gel, the degassing, evenly coat above-mentioned risperidone gel on the flat board, air blast, heat drying, heating-up temperature is 60 ℃, and cutting gets the risperidone oral instant membrane.
Embodiment 2
Component weight (g)
Risperidone 10
Hydroxypropyl emthylcellulose (20 centipoise) 500
70% ethanol 1000
Specific operation process: risperidone under agitation is scattered in 70% the ethanol, supersound process is to dissolving, hydroxypropyl emthylcellulose (20 centipoise) is under agitation added above-mentioned solution, fully disperse gel, the degassing, evenly coat above-mentioned risperidone gel on the flat board, air blast, heat drying, heating-up temperature is 60 ℃, and cutting gets the risperidone oral instant membrane.
Embodiment 3
Component weight (g)
Risperidone 10
Hydroxypropyl emthylcellulose (50 centipoise) 500
70% ethanol 1000
Specific operation process: risperidone under agitation is scattered in 70% the ethanol, supersound process is to dissolving, hydroxypropyl emthylcellulose (50 centipoise) is under agitation added above-mentioned solution, fully disperse gel, the degassing, evenly coat above-mentioned risperidone gel on the flat board, air blast, heat drying, heating-up temperature is 60 ℃, and cutting gets the risperidone oral instant membrane.
Embodiment 4
Component weight (g)
Risperidone 300
Hydroxypropyl emthylcellulose (5 centipoise) 500
Microcrystalline Cellulose 10
Aspartame 10
Strawberry essence 10
70% ethanol 1000
Specific operation process: risperidone, aspartame, strawberry essence under agitation be scattered in 70% the ethanol, supersound process is to dissolving, hydroxypropyl emthylcellulose (5 centipoise) is under agitation added above-mentioned solution, fully disperse gel, microcrystalline Cellulose is under agitation added gel, the degassing, above-mentioned risperidone gel is evenly coated on the flat board, air blast, heat drying, heating-up temperature is 60 ℃, cutting gets the risperidone oral instant membrane.
Embodiment 5
Component weight (g)
Risperidone 30
Hydroxypropyl emthylcellulose (5 centipoise) 500
Polacrilin potassium 30
Sucralose 10
Citric acid 10
Macrogol 200 30
70% ethanol 1000
Specific operation process: risperidone, sucralose, citric acid, polacrilin potassium under agitation be scattered in 70% the ethanol, supersound process is to dissolving, hydroxypropyl emthylcellulose (5 centipoise) is under agitation added above-mentioned solution, fully disperse gel, Macrogol 200 is under agitation added gel, the degassing, above-mentioned risperidone gel is evenly coated on the flat board, air blast, heat drying, heating-up temperature is 60 ℃, cutting gets the risperidone oral instant membrane.
Embodiment 6
Component weight (g)
Risperidone 20
Hydroxypropyl emthylcellulose (5 centipoise) 500
The certain kind of berries red 5
Strawberry essence 10
Citric acid 10
Sodium benzoate 5
PEG400 10
Aspartame 10
70% ethanol 1000
Specific operation process: risperidone, aspartame, citric acid, strawberry essence, the certain kind of berries is red, sodium benzoate under agitation is scattered in 70% the ethanol, supersound process is to dissolving, hydroxypropyl emthylcellulose (5 centipoise) is under agitation added above-mentioned solution, fully disperse gel, PEG400 is under agitation added gel, the degassing, above-mentioned risperidone gel is evenly coated on the flat board, air blast, heat drying, heating-up temperature is 60 ℃, cutting gets the risperidone oral instant membrane.
Claims (5)
1. the oral instant membrane of a risperidone, it is characterized in that, it is raw material with the risperidone, the chemical name of described risperidone is: 3-[2-[4-(6-fluoro-1 ,-2-benzoisoxazole-3-yl)-piperidino] ethyl]-6,7,8,9-tetrahydrochysene-2-methyl-4H-pyrido [1,2-α] pyrimidin-4-one, molecular formula is: C
23H
27FN
4O
2Molecular weight is: 410.49;
The 10g risperidone under agitation is scattered in the ethanol of 1000g70%, ultrasonic to dissolving, the hydroxypropyl emthylcellulose of 500g 5 centipoises is under agitation added above-mentioned solution, fully disperse gel, the degassing, above-mentioned risperidone gel is evenly coated on the flat board, air blast, heat drying, heating-up temperature is 60 ℃, and cutting gets the risperidone oral instant membrane.
2. the oral instant membrane of a risperidone, it is characterized in that, it is raw material with the risperidone, the chemical name of described risperidone is: 3-[2-[4-(6-fluoro-1 ,-2-benzoisoxazole-3-yl)-piperidino] ethyl]-6,7,8,9-tetrahydrochysene-2-methyl-4H-pyrido [1,2-α] pyrimidin-4-one, molecular formula is: C
23H
27FN
4O
2Molecular weight is: 410.49;
The 10g risperidone under agitation is scattered in the ethanol of 1000g70%, ultrasonic to dissolving, the hydroxypropyl emthylcellulose of 500g 20 centipoises is under agitation added above-mentioned solution, fully disperse gel, the degassing, above-mentioned risperidone gel is evenly coated on the flat board, air blast, heat drying, heating-up temperature is 60 ℃, and cutting gets the risperidone oral instant membrane.
3. the oral instant membrane of a risperidone, it is characterized in that, it is raw material with the risperidone, the chemical name of described risperidone is: 3-[2-[4-(6-fluoro-1 ,-2-benzoisoxazole-3-yl)-piperidino] ethyl]-6,7,8,9-tetrahydrochysene-2-methyl-4H-pyrido [1,2-α] pyrimidin-4-one, molecular formula is: C
23H
27FN
4O
2Molecular weight is: 410.49;
The 10g risperidone under agitation is scattered in the ethanol of 1000g70%, ultrasonic to dissolving, the hydroxypropyl emthylcellulose of 500g50 centipoise is under agitation added above-mentioned solution, fully disperse gel, the degassing, above-mentioned risperidone gel is evenly coated on the flat board, air blast, heat drying, heating-up temperature is 60 ℃, and cutting gets the risperidone oral instant membrane.
4. the oral instant membrane of a risperidone, it is characterized in that, it is raw material with the risperidone, the chemical name of described risperidone is: 3-[2-[4-(6-fluoro-1 ,-2-benzoisoxazole-3-yl)-piperidino] ethyl]-6,7,8,9-tetrahydrochysene-2-methyl-4H-pyrido [1,2-α] pyrimidin-4-one, molecular formula is: C
23H
27FN
4O
2Molecular weight is: 410.49;
300g risperidone, 10g aspartame, 10g strawberry essence under agitation are scattered in the ethanol of 1000g70%, ultrasonic to dissolving, the hydroxypropyl emthylcellulose of 500g5 centipoise is under agitation added above-mentioned solution, fully disperse gel, the 10g microcrystalline Cellulose is under agitation added gel, the degassing, above-mentioned risperidone gel is evenly coated on the flat board, air blast, heat drying, and heating-up temperature is 60 ℃, cutting gets the risperidone oral instant membrane.
5. the oral instant membrane of a risperidone, it is characterized in that, it is raw material with the risperidone, the chemical name of described risperidone is: 3-[2-[4-(6-fluoro-1 ,-2-benzoisoxazole-3-yl)-piperidino] ethyl]-6,7,8,9-tetrahydrochysene-2-methyl-4H-pyrido [1,2-α] pyrimidin-4-one, molecular formula is: C
23H
27FN
4O
2Molecular weight is: 410.49;
30g risperidone, 10g sucralose, 10g citric acid, 30g polacrilin potassium under agitation are scattered in the ethanol of 1000g70%, ultrasonic to dissolving, the hydroxypropyl emthylcellulose of 500g5 centipoise is under agitation added above-mentioned solution, fully disperse gel, the 30g Macrogol 200 is under agitation added gel, the degassing, above-mentioned risperidone gel is evenly coated on the flat board, air blast, heat drying, and heating-up temperature is 60 ℃, cutting gets the risperidone oral instant membrane.
The oral instant membrane of 6 one kinds of risperidones, it is characterized in that, it is raw material with the risperidone, the chemical name of described risperidone is: 3-[2-[4-(6-fluoro-1 ,-2-benzoisoxazole-3-yl)-piperidino] ethyl]-6,7,8,9-tetrahydrochysene-2-methyl-4H-pyrido [1,2-α] pyrimidin-4-one, molecular formula is: C
23H
27FN
4O
2Molecular weight is: 410.49;
20g risperidone, 10g aspartame, 10g citric acid, 10g strawberry essence, the 5g certain kind of berries is red, 5g sodium benzoate under agitation is scattered in the ethanol of 1000g70%, ultrasonic to dissolving, the hydroxypropyl emthylcellulose of 500g5 centipoise is under agitation added above-mentioned solution, fully disperse gel, the 10g PEG400 is under agitation added gel, the degassing, above-mentioned risperidone gel is evenly coated on the flat board, air blast, heat drying, heating-up temperature is 60 ℃, cutting gets the risperidone oral instant membrane.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009100752727A CN101632651B (en) | 2009-08-31 | 2009-08-31 | Oral instant membrane of risperidone and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009100752727A CN101632651B (en) | 2009-08-31 | 2009-08-31 | Oral instant membrane of risperidone and preparation method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101632651A CN101632651A (en) | 2010-01-27 |
| CN101632651B true CN101632651B (en) | 2010-12-08 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2009100752727A Expired - Fee Related CN101632651B (en) | 2009-08-31 | 2009-08-31 | Oral instant membrane of risperidone and preparation method thereof |
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| TWI605837B (en) * | 2011-01-27 | 2017-11-21 | Kowa Co Ltd | Pharmaceutical composition containing water-insoluble drug and pharmaceutical preparation |
| EP2524687A3 (en) * | 2011-05-20 | 2012-12-12 | Nitto Denko Corporation | Edible jelly-form composition, jelly-form preparation and method for producing jelly-form preparation |
| CN103750323A (en) * | 2014-01-26 | 2014-04-30 | 宁夏医科大学 | Oral lutein instant membrane and preparation method thereof |
| CN104000800A (en) * | 2014-04-28 | 2014-08-27 | 万特制药(海南)有限公司 | Asenapine maleate oral instant membrane and making method thereof |
| CN104434886A (en) * | 2014-11-18 | 2015-03-25 | 段珍波 | Risperidone oral rapidly disintegrating film preparation and preparation method thereof |
| CN104398474A (en) * | 2014-11-21 | 2015-03-11 | 内蒙古医科大学附属医院 | Nasal gel agent containing risperidone and preparation method of nasal gel agent |
| CN104546806A (en) * | 2015-01-05 | 2015-04-29 | 万特制药(海南)有限公司 | Oral cavity instant film containing risperidone and preparation method for oral cavity instant film |
| CN105997949B (en) * | 2016-06-02 | 2019-04-09 | 云南省药物研究所 | A kind of bulleyaconitine A orodispersible film preparation and its preparation process |
| CN107028917B (en) * | 2017-03-30 | 2020-07-17 | 武汉华夏理工学院 | Risperidone instant and/or quick-release solid oral film agent for gastrointestinal administration and preparation method thereof |
| CN108685876B (en) * | 2017-04-11 | 2022-10-04 | 齐鲁制药有限公司 | Oral film-shaped pharmaceutical composition containing risperidone |
| CN107823191B (en) * | 2017-11-16 | 2021-04-09 | 广州迈达康医药科技有限公司 | Paliperidone oral instant membrane preparation and preparation process thereof |
| CN115381773A (en) * | 2022-09-23 | 2022-11-25 | 南京正科医药股份有限公司 | Risperidone oral liquid |
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2009
- 2009-08-31 CN CN2009100752727A patent/CN101632651B/en not_active Expired - Fee Related
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| CN101632651A (en) | 2010-01-27 |
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