CN105012276A - Imidafenacin oral fast dissolving film and preparation method and application thereof - Google Patents
Imidafenacin oral fast dissolving film and preparation method and application thereof Download PDFInfo
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- CN105012276A CN105012276A CN201410175098.4A CN201410175098A CN105012276A CN 105012276 A CN105012276 A CN 105012276A CN 201410175098 A CN201410175098 A CN 201410175098A CN 105012276 A CN105012276 A CN 105012276A
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- imidafenacin
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- instant membrane
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Abstract
The invention belongs to the technical field of medicine, and particularly relates to an imidafenacin oral fast dissolving film and a preparation method and application thereof. The film agent comprises, by weight, 0.1%-3% of imidafenacin, 40%-85% of film-forming materials, 15%-50% of filling agents, 1%-10% of plasticizers, 0.1%-4% of sweetening agents and 0-5% of disintegrating agents. When the imidafenacin oral fast dissolving film is placed on the tongue, the film can be dissolved rapidly in saliva, medicine can be released, medicine taking through water is not needed, the danger of blocking throats does not exist, the imidafenacin oral fast dissolving film is suitable for being taken by elderly patients, the adaptability of the patients is improved, and carrying is convenient.
Description
Technical field
The invention belongs to medical art, being specifically related to a kind of imidafenacin is oral instant membrane of effective ingredient and its production and use.
Background technology
Imidafenacin is the novel diphenyl butanamide class anticholinergic agent developed jointly by Japanese ONO Pharmaceutical Co., Ltd. and the pharmacy of Fructus Pruni woods, has height bladder selectivity, for the treatment of overactive bladder, goes on the market in June, 2007 in Japan.Imidafenacin has diphenyl butanamide structure, it is a kind of new and effective anticholinergic agent, its selectively acting is in M3 and M1 receptor, block choline to the contraction of detrusor, detrusor is made to relax, every day 2 times, each serving using 0.1mg imidafenacin, significantly can improve the symptoms such as the urgent micturition caused by overactive bladder, frequent micturition, urine taboo.Imidafenacin has and suppresses smooth muscle of bladder to shrink and suppress acetylcholine to dissociate dual function, and is better than salivary gland to the selectivity of bladder, in cerebral tissue but alkali receptor affinity is lower, therefore maincenter and periphery untoward reaction less.
Conventional tablet is for child, old people and swallow the crowd of having any problem and be obviously not too suitable for.Oral instant membrane (oral fast dissolving films) is that a kind of new drug delivery system, the high polymer that adopts as carrier more, its size, shape, thickness are similar to stamp, be placed on tongue, energy rapid solution, release medicine in saliva, suitable child and old people.
Patent (CN101983054, CN101983055) describes the preparation method of imidafenacin oral cavity disintegration tablet.Oral cavity disintegration tablet adopts the technique such as freeze-dry process or wet granulation to prepare usually, preparation technology is more complicated, usually needing special installation, adopt the preparation of wet granule compression tablet technique usually to there is disintegrate slow, there is the shortcomings such as undesirable, the frangible and easy moisture absorption of outward appearance in the preparation of lyophilization technique usually.Patent (CN101983054, CN101983055) adopts repeatedly fluidized bed granulation, coating, complex operation, production cost is higher, and because imidafenacin adopts polyvidone or gastric solubility macromolecule to be coated to, use fluid bed, wet granulation technology prepare oral cavity disintegration tablet, when patient takes, though the very fast disintegrate of tablet energy, but still there is larger coating granule after disintegrate, in oral cavity, grittiness is comparatively strong, affects patient medication compliance.
Oral instant membrane is identical with normal film agent and process for producing same, and preparation technology is simple.The usual hardness of oral cavity disintegration tablet is lower, and mechanical strength is little, brings difficulty to finished product packing, transport.Oral instant membrane has higher mechanical strength, to ensure the integrity of its product in packaging, transport, use procedure, does not have breakage.
Imidafenacin is prepared into oral instant membrane by the present invention, the grittiness after there will not be oral cavity disintegration tablet to take, and better can improve patient compliance.For those swallow tablets or the inconvenient individuality of pill, imidafenacin oral instant membrane can improve the compliance of administration greatly.Without the need to water delivery service after imidafenacin oral instant membrane entrance, can dissolve within the several seconds under the effect of saliva.
Summary of the invention
The invention provides a kind of meter Da Naxin oral instant membrane and preparation method thereof, to realize fater disintegration, quick release, easy to carry, improve the compliance of patient.This oral instant membrane comprises the adjuvant that active constituents of medicine and pharmacy are suitable for, and the adjuvant that described pharmacy is suitable for comprises filmogen, sweeting agent, filler etc.Described active constituents of medicine is: imidafenacin.
Meter Da Naxin oral instant membrane can rapid solution, dispersion in water, specifically refers to dissolve completely in 60 seconds in 25 DEG C of water.
To achieve the above object of the invention, the technical solution used in the present invention is: a kind of oral instant membrane, and each Ni lead-free solder alloy is:
Preferred:
Described filmogen to be selected from gelatin, arabic gum, xanthan gum, agar, sodium alginate, polyvinyl alcohol (PVA), hypromellose (HPC), methylcellulose, sodium carboxymethyl cellulose and hydroxypropyl emthylcellulose (HPMC), polyvinylpyrrolidone (PVP) one or more mixture.A kind of or the mixture of 2 kinds in preferred hydroxypropyl emthylcellulose and polyvinyl alcohol.
Hydroxypropyl emthylcellulose preferred viscosities is 3 ~ 50 centipoises, more preferably 3 ~ 10 centipoises.Most preferably 5 centipoises.
The preferred alcoholysis degree of polyvinyl alcohol is the product of 87 ~ 89%.Polyvinyl alcohol add the formation contributing to film.
If filmogen is the mixture of hydroxypropyl level methylcellulose and polyvinyl alcohol, then hydroxypropyl level methylcellulose and polyvinyl alcohol weight ratio are 1:10 ~ 10:1, and preferably, hydroxypropyl level methylcellulose and polyvinyl alcohol weight ratio are 1:5 ~ 5:1; More preferably, hydroxypropyl level methylcellulose and polyvinyl alcohol weight ratio are 1:3 ~ 3:1.
The described filler for this oral instant membrane to be selected from mannitol, lactose, sorbitol, microcrystalline Cellulose, pregelatinized Starch, dextrin and starch one or more mixture.
The described sweeting agent for this oral instant membrane to be selected from aspartame, stevioside, fructose, sucrose and maltose one or more mixture.
Described plasticizer is selected from the mixture of one or more in Polyethylene Glycol (PEG), glycerol or Tween 80.
Described disintegrating agent is selected from the one in carboxymethyl starch sodium, polyvinylpolypyrrolidone, low-substituted hydroxypropyl cellulose.
Solvent adopts 10% ethanol water (percentage by weight) solution, and membrane dry run is fast, and film good moldability, membrane smooth surface.The preparation method of oral instant membrane of the present invention, comprises the following steps:
1) imidafenacin is added dissolve with ethanol, stir and obtain containing drug solns;
2) water soluble film-forming material is added in 10% ethanol water under stirring, fully stir, dissolve, obtain polymer gel;
3) in above-mentioned polymer gel, add the filler of recipe quantity, plasticizer, disintegrating agent stirring;
4) step 3 will be added containing drug solns) in polymer gel solution, mix homogeneously;
5) by the solution left standstill for preparing or ultrasonic removing bubble;
6) by above-mentioned macromolecule glue blade coating on plastic sheeting;
7) heat drying, heat drying temperature is 50 ~ 70 DEG C;
8) membrane is peeled off from plastic sheeting, after cutting into certain size, pack and get final product.
Detailed description of the invention
Subordinate's embodiment is prepared according to preparation process of the present invention, cuts into 2cm × 2cm film.
embodiment 1
embodiment 2
embodiment 3
embodiment 4
embodiment 5
embodiment 6
Example prepares sample, is immersed in the water, manual time-keeping, observes membrane solution time.
Table 1 embodiment sample solution time
| Embodiment | Solution time (second) |
| 1 | 25 |
| 2 | 28 |
| 3 | 34 |
| 4 | 36 |
| 5 | 24 |
Experimental result shows, embodiment of the present invention sample energy rapid solution, release medicine.
Claims (10)
1. an imidafenacin oral instant membrane, is characterized in that, comprises active component imidafenacin and pharmacy adjuvant applicatory, and the adjuvant that described pharmacy is suitable for comprises filmogen, filler, plasticizer, sweeting agent; The percentage by weight of each component is counted: imidafenacin 0.1-3%; Filmogen 40-85%; Filler 15-50%; Plasticizer 1-10%; Sweeting agent 0.1-4%.
2. imidafenacin oral instant membrane as claimed in claim 1, described filmogen to be selected from gelatin, arabic gum, xanthan gum, agar, sodium alginate, polyvinyl alcohol (PVA), hypromellose (HPC), methylcellulose, sodium carboxymethyl cellulose, hydroxypropyl emthylcellulose (HPMC), polyvinylpyrrolidone (PVP) one or more mixture.
3. imidafenacin oral instant membrane as claimed in claim 2, described filmogen to be selected from hydroxypropyl emthylcellulose, polyvinyl alcohol one or more mixture.
4. imidafenacin oral instant membrane as claimed in claim 2 or claim 3, the viscosity of described filmogen hypromellose is 3 ~ 50 centipoises; Be more preferably 3 ~ 10 centipoises; Most preferably be 5 centipoises; The preferred alcoholysis degree of polyvinyl alcohol is the product of 87 ~ 89%.
5. imidafenacin oral instant membrane as claimed in claim 1, described filler to be selected from mannitol, lactose, sorbitol, microcrystalline Cellulose, pregelatinized Starch, dextrin, starch one or more mixture.
6. imidafenacin oral instant membrane as claimed in claim 1, described sweeting agent to be selected from aspartame, stevioside, fructose, sucrose, maltose one or more mixture.
7. imidafenacin oral instant membrane as claimed in claim 1, described plasticizer is selected from the mixture of one or more in Polyethylene Glycol, glycerol or Tween 80.
8. imidafenacin oral instant membrane as claimed in claim 1, also comprises disintegrating agent; Described disintegrating agent is selected from carboxymethyl starch sodium, polyvinylpolypyrrolidone, low-substituted hydroxypropyl cellulose.
9. the preparation method of imidafenacin oral instant membrane as claimed in claim 1, comprises the following steps:
1) imidafenacin is added dissolve with ethanol, stir and obtain containing drug solns;
2) water soluble film-forming material is added in 10% ethanol water under stirring, fully stir, dissolve, obtain polymer gel;
3) in step 2) in add filler in polymer gel, plasticizer, disintegrating agent stir;
4) step 3 will be added containing drug solns) in polymer gel solution, mix homogeneously;
5) by the solution left standstill for preparing or ultrasonic removing bubble;
6) by above-mentioned macromolecule glue blade coating on plastic sheeting;
7) heat drying, heat drying temperature is 50 ~ 70 DEG C;
8) membrane is peeled off from plastic sheeting, after cutting into certain size, pack and get final product.
10. the purposes of imidafenacin medicine oral instant membrane as claimed in claim 1 in preparation treatment urinary incontinence medicine.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410175098.4A CN105012276A (en) | 2014-04-29 | 2014-04-29 | Imidafenacin oral fast dissolving film and preparation method and application thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410175098.4A CN105012276A (en) | 2014-04-29 | 2014-04-29 | Imidafenacin oral fast dissolving film and preparation method and application thereof |
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| Publication Number | Publication Date |
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| CN105012276A true CN105012276A (en) | 2015-11-04 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410175098.4A Pending CN105012276A (en) | 2014-04-29 | 2014-04-29 | Imidafenacin oral fast dissolving film and preparation method and application thereof |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105997949A (en) * | 2016-06-02 | 2016-10-12 | 云南省药物研究所 | Oral dissolving film preparation containing bulleyaconitine A and preparation technology of oral dissolving film preparation |
| WO2016163403A1 (en) * | 2015-04-07 | 2016-10-13 | ニプロ株式会社 | Oral film preparation |
| CN107106512A (en) * | 2015-11-25 | 2017-08-29 | 缇碧艾姆株式会社 | Stop blooding and Wound protection film in oral cavity |
| CN108272776A (en) * | 2018-04-11 | 2018-07-13 | 苏州大学 | Amitriptyline Hydrochloride oral quick-dissolving film preparation |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101983054A (en) * | 2008-01-31 | 2011-03-02 | 杏林制药株式会社 | Orally rapidly disintegrating tablet comprising imidafenacin |
| CN102652739A (en) * | 2011-12-17 | 2012-09-05 | 东莞达信生物技术有限公司 | Palonosetron oral cavity membrane preparation and preparation method thereof |
| CN102846581A (en) * | 2012-09-28 | 2013-01-02 | 天津市聚星康华医药科技有限公司 | Ambroxol hydrochloride oral fast-dissolving film and preparation method thereof |
| CN103479594A (en) * | 2013-09-29 | 2014-01-01 | 扬子江药业集团四川海蓉药业有限公司 | Imidafenacin film-coated tablet and preparation method thereof |
-
2014
- 2014-04-29 CN CN201410175098.4A patent/CN105012276A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101983054A (en) * | 2008-01-31 | 2011-03-02 | 杏林制药株式会社 | Orally rapidly disintegrating tablet comprising imidafenacin |
| CN102652739A (en) * | 2011-12-17 | 2012-09-05 | 东莞达信生物技术有限公司 | Palonosetron oral cavity membrane preparation and preparation method thereof |
| CN102846581A (en) * | 2012-09-28 | 2013-01-02 | 天津市聚星康华医药科技有限公司 | Ambroxol hydrochloride oral fast-dissolving film and preparation method thereof |
| CN103479594A (en) * | 2013-09-29 | 2014-01-01 | 扬子江药业集团四川海蓉药业有限公司 | Imidafenacin film-coated tablet and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 《天津药学》 * |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016163403A1 (en) * | 2015-04-07 | 2016-10-13 | ニプロ株式会社 | Oral film preparation |
| CN107106512A (en) * | 2015-11-25 | 2017-08-29 | 缇碧艾姆株式会社 | Stop blooding and Wound protection film in oral cavity |
| CN105997949A (en) * | 2016-06-02 | 2016-10-12 | 云南省药物研究所 | Oral dissolving film preparation containing bulleyaconitine A and preparation technology of oral dissolving film preparation |
| CN108272776A (en) * | 2018-04-11 | 2018-07-13 | 苏州大学 | Amitriptyline Hydrochloride oral quick-dissolving film preparation |
| CN108272776B (en) * | 2018-04-11 | 2020-12-08 | 苏州大学 | Amitriptyline hydrochloride oral instant film agent |
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