CN103784426B - Molten membrane of Aripiprazole mouth and preparation method thereof - Google Patents
Molten membrane of Aripiprazole mouth and preparation method thereof Download PDFInfo
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- CN103784426B CN103784426B CN201410056548.8A CN201410056548A CN103784426B CN 103784426 B CN103784426 B CN 103784426B CN 201410056548 A CN201410056548 A CN 201410056548A CN 103784426 B CN103784426 B CN 103784426B
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- aripiprazole
- cyclodextrin
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Abstract
The invention discloses molten membrane of a kind of Aripiprazole mouth and preparation method thereof, the molten membrane of described Aripiprazole mouth, Aripiprazole containing cyclodextrin parcel, wherein: described cyclodextrin is more than one in HP-β-CD or glucose group-beta-cyclodextrin, and the weight ratio of cyclodextrin and Aripiprazole is 1:1 ~ 3:1.The beneficial effect of film-like preparation of the present invention is: obtained film is even, bright and clean; Take simple, do not need drinking-water to take; Stripping rapidly, completely; And infiltration rate is fast, and bioavailability is high, good effect; Production technology is simple, and production cost is low, and added value of product is high.Aripiprazole membrane of the present invention stripping is rapid, good stability, bioavailability are high, has excellent biological effectiveness; Compliance is good, welcomes by patient; Formability is good, directly can attach to medicine-feeding part after administration, cannot spue, and psychosis can be avoided to tell medicine, Tibetan medicine; Several without dust from flying in process of production, labor protection and problem of environmental pollution may be solved.
Description
Technical field
The present invention relates to aripiprazole formulations, be specifically related to a kind of medicine film preparation and preparation method thereof.
Background technology
Aripiprazole belongs to third generation atypical antipsychotic agents, all have significant curative effect, and side effect is very little to the schizophrenia positive and negative symptoms.Existing listing dosage form is based on conventional tablet and oral cavity disintegration tablet.Owing to Tibetan medicine often occurring during schizophrenic's medication and tells medicine phenomenon, greatly have impact on curative effect of medication.Make membrane not need with water delivery service, to be placed on tongue instant, and stick and not easily spue at this place, therefore improve the compliance of clinical application, be particularly suitable for psychotic; And production technology is simple, power consumption is few, and cost is lower.
Medicine film preparation is as far back as nineteen seventies i.e. existing much research, as tranquilizer film (Chinese Journal of Pharmaceuticals, 1976,12(19)), diphenoxylate medicine film (Chinese Journal of Pharmaceuticals, 1976,12(22)), external applied contraceptive film (Chinese Journal of Pharmaceuticals, 1977,4-5(45)), nitroglycerin medicine film (Chinese Journal of Pharmaceuticals, 1977,12(5)), rhodexin film (Chinese Journal of Pharmaceuticals, 1980,4(18)), clonidine sustained release film formulation (Chinese Journal of Pharmaceuticals, 1981,3(141)) etc.Chinese Pharmacopoeia is also recorded (Pharmacopoeia of People's Republic of China 1995 editions, 2000 editions, 2005 editions, 2010 editions) using membrane as official preparation.
Patent about membrane also emerges in an endless stream, there is the edible water-soluble film (CN101516331A) containing foam reducing flavoring agent, for the film bandage (CN101389309A) of mucosal administration of actives, high dose film compositions and preparation method thereof (CN101616660A), polymer-based films and drug delivery system prepared therefrom (CN101668519A), the preparation method (CN101744791A) of edible film, for the film (CN101346135A) of the adjusted pH that activating agent is sent, for the film bandage (CN101389309A) of mucosal administration of actives, non-mucoadhesive film dosage forms (CN101626756A), disintegrable oral films (CN101384249A), membrane (CN101621990A) that can be Orally administered, for neuroleptic, film (CN101287445A) can not be collapsed by the oral fast spued, instant capacity membrane (CN100396332C) etc.The present inventor has also applied for that the patent of packaged form of the production machine of dapple medicinal film agent (CN201596139U), microporous sponge shape medicine film preparation (CN102028672B) and membrane, the packaging machine of membrane, the new of membrane is established on surface, to promote membrane development at home.
The poorly water-soluble of Aripiprazole is (under room temperature, dissolubility <1 μ g/ml), there is dispersion uneven and can not the problem of Fast Stripping when preparing membrane, need to improve its solubility property to improve uniformity, to accelerate drug-eluting, thus raising bioavailability, ensure safety and the effectiveness of medicine.Increasing drug solubility, enhanced stability and taste masking by the clathration of cyclodextrin is a kind of known method.CN100335047C discloses a kind of aqueous injectable of Aripiprazole, and wherein aripiprazole inclusion forms inclusion complex in beta-schardinger dextrin-, and the weight ratio of beta-schardinger dextrin-and Aripiprazole is 10:1 ~ 100:1, and the pH of preparation is 3.5 to 5.But membrane is thin, light, little, because the molten film of mouth needs to dissolve rapidly in mouth usually, weight can not be too large; To gain in weight: or film is too large, uses inconvenience; Or film is too thick, cannot dissolve rapidly.Thus the weight of a slice film is generally at below 100mg, is generally 20 ~ 60mg.The dosage of Aripiprazole is that 5mg or 10mg(accounts for 10 ~ 25% of solid amount in film usually); In prescription, macromolecule filming material at least needs to account for more than 30% of total solid in film usually, otherwise physical strength does not reach instructions for use; So the amount of the cyclodextrin that can add in prescription is subject to certain restrictions.If add enough cyclodextrin, improve the solubility property of medicine, will reduce the consumption of macromolecule filming material in prescription, the physical property of obtained film can not meet the demands, can be very crisp, easy fracture, fragmentation.
Summary of the invention
The object of the present invention is to provide molten membrane of a kind of Aripiprazole mouth and preparation method thereof, to overcome the above-mentioned defect that prior art exists.
The molten membrane of Aripiprazole mouth of the present invention, the Aripiprazole containing cyclodextrin parcel, wherein:
Described cyclodextrin is more than one in HP-β-CD or glucose group-beta-cyclodextrin, and the weight ratio of cyclodextrin and Aripiprazole is 1:1 ~ 3:1, preferably 1.2:1 ~ 1.5:1;
The method of cyclodextrin parcel Aripiprazole, comprises the steps:
By cyclodextrin and hydrochloric acid solution mixed dissolution, add Aripiprazole, at 55 ~ 65 DEG C, stir 0.5 ~ 1.5h, the Aripiprazole of described cyclodextrin parcel can be obtained;
The concentration of described hydrochloric acid solution is 0.08M ~ 0.12M, preferably 0.1M;
The weight of cyclodextrin and the w/v of described hydrochloric acid solution are:
Cyclodextrin: hydrochloric acid solution=1g: 0.9 ~ 1.1ml;
Preferably: cyclodextrin: hydrochloric acid solution=1g: 1ml;
Preferably, the described molten membrane of Aripiprazole mouth, comprises the component of following percentage by weight:
The Aripiprazole 20 ~ 70% of cyclodextrin parcel
Macromolecule filming material 30 ~ 80%
Other adjuvant 0 ~ 20%
The percentage ratio sum of said components content is 100%;
Described macromolecule filming material comprise in hydroxypropyl emthylcellulose (HPMC), hydroxypropyl cellulose (HPC), polyvinyl alcohol (PVA), polyvinylpyrrolidone (PVP), sodium alginate, polyoxyethylene (PEO), Bletilla glucomannan, corn starch or carrageenan more than one; Preferred HPMC, HPC, PVA or PEO.
Other adjuvants described comprise plasticizer, as PEG, glycerol or Tween 80 etc.; Correctives, as sweeting agent, acidic flavoring agent, aromatic, gummy macromolecular material, lecithin, cephalin, phosphatidic acid, pigment, antioxidant or antiseptic etc.
Preferably, the described molten membrane of Aripiprazole mouth, comprises the component of following percentage by weight:
The Aripiprazole 30 ~ 50% of cyclodextrin parcel
Macromolecule filming material 45 ~ 70%
Other adjuvant 0 ~ 5%
The percentage ratio sum of said components content is 100%.
Described cyclodextrin is the one of HP-β-CD or glucose group-beta-cyclodextrin;
Described macromolecule filming material comprise in hydroxypropyl emthylcellulose (HPMC), hydroxypropyl cellulose (HPC), polyvinyl alcohol (PVA), polyvinylpyrrolidone (PVP), sodium alginate, polyoxyethylene (PEO), Bletilla glucomannan, corn starch or carrageenan more than one; Preferred HPMC, PVA or PEO.
Other adjuvants described comprise plasticizer, as PEG, glycerol or Tween 80 etc.; Correctives, comprises sweeting agent, acidic flavoring agent, aromatic, gummy macromolecular material, lecithin, cephalin or phosphatidic acid etc.; And pigment, antioxidant or antiseptic etc.
The preparation method of the molten membrane of Aripiprazole mouth of the present invention, comprises the steps:
(1) by cyclodextrin and hydrochloric acid solution mixed dissolution, add Aripiprazole, at 55 ~ 65 DEG C, stir 0.5 ~ 1.5h, the Aripiprazole of described cyclodextrin parcel can be obtained;
The concentration of described hydrochloric acid solution is 0.08M ~ 0.12M, preferably 0.1M;
The weight of cyclodextrin and the w/v of described hydrochloric acid solution are:
Cyclodextrin: hydrochloric acid solution=1g: 0.9 ~ 1.1ml;
Preferably: cyclodextrin: hydrochloric acid solution=1g: 1ml;
The concentration of described hydrochloric acid solution is 0.08M ~ 0.12M, preferably 0.1M;
(2) add purified water and other adjuvants, stir into full-bodied solution, cross 60 ~ 100 mesh sieves, removing insoluble matter, vacuum defoamation;
(3) then by above-mentioned solution extension in stainless steel band, 60 ~ 90 DEG C of dryings 10 ~ 20 minutes, obtain the described molten membrane of Aripiprazole mouth.
Inventor experimental studies have found that through a large amount of, HP-β-CD or the enclose effect of glucose group-beta-cyclodextrin to medicine best, when enclose, when the ratio of cyclodextrin and described hydrochloric acid solution is cyclodextrin: hydrochloric acid solution=1g: 0.9 ~ 1.1ml, preferably: cyclodextrin: during hydrochloric acid solution=1g: 1ml, 0.5 ~ 1.5h enclose best results is stirred at 55 ~ 65 DEG C, by under so specific condition, pharmaceutical pack be combined in cyclodextrin, the ratio of cyclodextrin and medicine can be controlled in 1:1 ~ 3:1.Like this, clathrate mixes with macromolecule filming material, the membrane of preparation, and its stripping and physical property all can meet the requirement of clinical application.
The beneficial effect of film-like preparation of the present invention is: obtained film is even, bright and clean; Take simple, do not need drinking-water to take; Stripping rapidly, completely; And infiltration rate is fast, and bioavailability is high, good effect; Production technology is simple, and production cost is low, and added value of product is high.Aripiprazole membrane of the present invention stripping is rapid, good stability, bioavailability are high, has excellent biological effectiveness; Compliance is good, welcomes by patient; Formability is good, directly can attach to medicine-feeding part after administration, cannot spue, and psychosis can be avoided to tell medicine, Tibetan medicine; Several without dust from flying in process of production, labor protection and problem of environmental pollution may be solved.
Fig. 1 is the stripping curve of embodiment 1.
Fig. 2 is the stripping curve of embodiment 2.
Fig. 3 is the stripping curve of comparative example 1.
Fig. 4 is the stripping curve of comparative example 2.
Fig. 5 is the stripping curve of comparative example 3.
Detailed description of the invention
Embodiment 1
Prescription:
Preparation method:
Get the 0.1M hydrochloric acid solution that HP-β-CD adds 30ml, stirring and dissolving, then add Aripiprazole, at 60 DEG C, stir 1h, add purified water 300ml subsequently, then add titanium dioxide, HPMC and HPC, be stirred into full-bodied solution, cross 80 mesh sieves, removing insoluble matter, vacuum defoamation.Again by the extension of film liquid on stainless steel band, 80 DEG C of dry 15min.According to assay result, after cutting into certain size, peel off from stainless steel band, pack and get final product.
The medicine film preparation obtained, thickness is 0.065mm, and every sheet is containing Aripiprazole 5mg or 10mg.Oral every day 1 time, within first week, be initial dose 5mg/ day, second week increases to 10mg/ day, and medication is after 2 weeks, and can increase dosage according to the curative effect of individuality and tolerance situation, every day, maximal dose should more than 30mg.
This mouthful of molten film appearance uniform, bright and clean.Possess enough intensity and toughness, physical strength meets the demands.
Determination of Content Uniformity: get this product 1, put in 100ml measuring bottle, add mobile phase to dissolve, be diluted to scale, shake up, place, get supernatant liquid filtering, get subsequent filtrate as need testing solution, measure content by HPLC method, and press Chinese Pharmacopoeia version in 2010 two annex Ⅹ E mensuration uniformity of dosage units (A+1.80S answers≤20.0).The results are shown in Table 1.Result shows, the Aripiprazole mouth molten film content uniformity of preparation is better.
Table 1 embodiment 1 Determination of Content Uniformity result
| Uniformity of dosage units test sample | Content (%) |
| 1 | 100.03 |
| 2 | 98.20 |
| 3 | 98.74 |
| 4 | 98.52 |
| 5 | 99.31 |
| 6 | 101.20 |
| 7 | 100.39 |
| 8 | 100.60 |
| 9 | 98.69 |
| 10 | 99.10 |
| Meansigma methods | 99.5 |
| RSD | 1.0% |
| A+1.8*S | 2.3 |
Get this product 6, clamp with paperclip respectively, adopt dissolution method (Chinese Pharmacopoeia version in 2010 two annex Ⅹ C the 3rd methods) device, with pH4.0 acetate buffer solution 500ml for dissolution medium, rotating speed is 50 turns per minute, from test sample contact dissolution medium, timing immediately, respectively through 1,2,5,10,15,30 and 60 minute time, get solution 1ml, filter, get subsequent filtrate, measure according to high performance liquid chromatography (Chinese Pharmacopoeia version in 2010 two annex V D) and calculate the stripping quantity of every sheet.Its In Vitro Dissolution curve is shown in Fig. 1.As seen from Figure 1, the In Vitro Dissolution of the molten film of Aripiprazole mouth of the present invention is very fast, in 3min stripping more than 85%, 5min time dissolve completely.
Embodiment 2
Prescription:
Preparation method:
Get the 0.1M hydrochloric acid solution that glucose group-beta-cyclodextrin adds 24ml, stirring and dissolving, then add Aripiprazole, at 60 DEG C, stir 1h, add purified water 300ml subsequently, then add all the other adjuvants, be stirred into full-bodied solution, cross 80 mesh sieves, removing insoluble matter, vacuum defoamation.Again by the extension of film liquid on stainless steel band, 90 DEG C of dry 15min.According to assay result, after cutting into certain size, peel off from stainless steel band, pack and get final product.
The medicine film preparation obtained, thickness is 0.065mm, and every sheet is containing Aripiprazole 5mg or 10mg.Oral every day 1 time, within first week, be initial dose 5mg/ day, second week increases to 10mg/ day, and medication is after 2 weeks, and can increase dosage according to the curative effect of individuality and tolerance situation, every day, maximal dose should more than 30mg.
This mouthful of molten film appearance uniform, bright and clean.Possess enough intensity and toughness, physical strength meets the demands.
Determination of Content Uniformity: get this product 1, put in 100ml measuring bottle, add mobile phase to dissolve, be diluted to scale, shake up, place, get supernatant liquid filtering, get subsequent filtrate as need testing solution, measure content by HPLC method, and press Chinese Pharmacopoeia version in 2010 two annex Ⅹ E mensuration uniformity of dosage units (A+1.80S answers≤20.0).The results are shown in Table 2.Result shows, the Aripiprazole mouth molten film content uniformity of preparation is better.
Table 2 embodiment 2 Determination of Content Uniformity result
| Uniformity of dosage units test sample | Content (%) |
| 1 | 99.97 |
| 2 | 100.29 |
| 3 | 101.38 |
| 4 | 101.56 |
| 5 | 101.22 |
| 6 | 102.52 |
| 7 | 100.90 |
| 8 | 100.48 |
| 9 | 102.33 |
| 10 | 100.45 |
| Meansigma methods | 101.1 |
| RSD | 0.8% |
| A+1.8*S | 2.7 |
Get this product 6, clamp with paperclip respectively, adopt dissolution method (Chinese Pharmacopoeia version in 2010 two annex Ⅹ C the 3rd methods) device, with pH4.0 acetate buffer solution 500ml for dissolution medium, rotating speed is 50 turns per minute, from test sample contact dissolution medium, timing immediately, respectively through 1,2,5,10,15,30 and 60 minute time, get solution 1ml, filter, get subsequent filtrate, measure according to high performance liquid chromatography (Chinese Pharmacopoeia version in 2010 two annex V D) and calculate the stripping quantity of every sheet.Its In Vitro Dissolution curve is shown in Fig. 2.As seen from Figure 2, the In Vitro Dissolution of the molten film of Aripiprazole mouth of the present invention is very fast, stripping more than 80% in 3min.Substantially dissolve during 5min completely.
Comparative example 1
Prescription is with embodiment 1.
Preparation method:
Get the purified water that HP-β-CD adds 30ml, stirring and dissolving, then add Aripiprazole, all the other are with embodiment 1.
The medicine film preparation obtained, thickness is about 0.065mm, and every sheet is containing Aripiprazole 5mg or 10mg.
This mouthful of molten film possesses certain intensity and toughness, and physical strength meets the demands substantially.But outward appearance is uneven, visible insoluble granule.
Measure uniformity of dosage units according to method described in embodiment 1, the results are shown in Table 3.Result shows, the molten film of Aripiprazole mouth prepared according to the present embodiment method, content uniformity is poor.
Table 3 comparative example 1 Determination of Content Uniformity result
| Uniformity of dosage units test sample | Content (%) |
| 1 | 99.11 |
| 2 | 110.25 |
| 3 | 105.24 |
| 4 | 103.22 |
| 5 | 102.52 |
| 6 | 98.53 |
| 7 | 95.22 |
| 8 | 92.13 |
| 9 | 91.00 |
| 10 | 107.69 |
| Meansigma methods | 100.5 |
| RSD | 6.4% |
| A+1.8*S | 12.1 |
Get this product 6, measure In Vitro Dissolution curve according to method described in embodiment 1, the results are shown in Figure 3.As seen from Figure 3, the molten film of Aripiprazole mouth prepared according to the present embodiment method, dissolves completely after stripping more than 80%, 30min during 10min.In Vitro Dissolution is comparatively slow, has larger difference with embodiment 1.
Comparative example 2
Prescription is with embodiment 1.
Preparation method:
Get the 0.1M hydrochloric acid solution that HP-β-CD adds 330ml, stirring and dissolving, then add Aripiprazole, stir 1h at 60 DEG C, add titanium dioxide, HPMC and HPC subsequently, all the other are with embodiment 1.
The medicine film preparation obtained, thickness is about 0.065mm, and every sheet is containing Aripiprazole 5mg or 10mg.
This mouthful of molten film possesses certain intensity and toughness, and physical strength meets the demands substantially.But outward appearance is uneven, visible insoluble granule.
Measure uniformity of dosage units according to method described in embodiment 1, the results are shown in Table 4.Result shows, the molten film of Aripiprazole mouth prepared according to the present embodiment method, content uniformity is poor.
Table 4 comparative example 2 Determination of Content Uniformity result
| Uniformity of dosage units test sample | Content (%) |
| 1 | 109.11 |
| 2 | 97.52 |
| 3 | 99.65 |
| 4 | 101.53 |
| 5 | 106.23 |
| 6 | 100.24 |
| 7 | 93.26 |
| 8 | 96.78 |
| 9 | 107.67 |
| 10 | 103.24 |
| Meansigma methods | 101.5 |
| RSD | 5.0% |
| A+1.8*S | 10.7 |
Get this product 6, measure In Vitro Dissolution curve according to method described in embodiment 1, the results are shown in Figure 4.As seen from Figure 4, the molten film of Aripiprazole mouth prepared according to the present embodiment method, dissolves completely after stripping more than 80%, 30min during 15min.In Vitro Dissolution is comparatively slow, has larger difference with embodiment 1.
Comparative example 3
Prescription:
Aripiprazole 20g
HP-β-CD 62g
HPMC18g
Preparation method:
Get the purified water that HP-β-CD adds 330ml, stirring and dissolving, then add Aripiprazole, stir 1h, then add HPMC at 60 DEG C, high-speed stirred evenly becomes full-bodied solution, and all the other are with embodiment 1.
The medicine film preparation obtained, thickness is about 0.065mm, and every sheet is containing Aripiprazole 5mg or 10mg.
This mouthful of molten film outward appearance is comparatively even, but film is very crisp, cuts, frangible when packing, easily split, yield rate is low.
Measure uniformity of dosage units according to method described in embodiment 1, the results are shown in Table 5.Result shows, the molten film of Aripiprazole mouth prepared according to the present embodiment method, content uniformity can meet the demands.
Table 5 comparative example 3 Determination of Content Uniformity result
| Uniformity of dosage units test sample | Content (%) |
| 1 | 100.23 |
| 2 | 98.56 |
| 3 | 103.26 |
| 4 | 101.54 |
| 5 | 99.14 |
| 6 | 100.52 |
| 7 | 101.77 |
| 8 | 102.35 |
| 9 | 97.67 |
| 10 | 102.11 |
| Meansigma methods | 100.7 |
| RSD | 1.8% |
| A+1.8*S | 4.0 |
Get this product 6, measure In Vitro Dissolution curve according to method described in embodiment 1, the results are shown in Figure 5.As seen from Figure 5, the molten film of Aripiprazole mouth prepared according to the present embodiment method, dissolves completely after stripping more than 80%, 15min during 10min.In Vitro Dissolution is slower than embodiment 1.
Claims (7)
1. the molten membrane of Aripiprazole mouth, is characterized in that, the Aripiprazole containing cyclodextrin parcel, wherein:
Described cyclodextrin is more than one in HP-β-CD or glucose group-beta-cyclodextrin, and the weight ratio of cyclodextrin and Aripiprazole is 1:1 ~ 3:1;
The method of cyclodextrin parcel Aripiprazole, comprises the steps:
By cyclodextrin and hydrochloric acid solution mixed dissolution, add Aripiprazole, at 55 ~ 65 DEG C, stir 0.5 ~ 1.5h, the Aripiprazole of described cyclodextrin parcel can be obtained;
The concentration of described hydrochloric acid solution is 0.08M ~ 0.12M;
The weight of cyclodextrin and the w/v of described hydrochloric acid solution are:
Cyclodextrin: hydrochloric acid solution=1g: 0.9 ~ 1.1ml.
2. the molten membrane of Aripiprazole mouth according to claim 1, is characterized in that, the weight ratio 1.2:1 ~ 1.5:1 of cyclodextrin and Aripiprazole.
3. the molten membrane of Aripiprazole mouth, is characterized in that, comprises the component of following percentage by weight:
The Aripiprazole 20 ~ 70% of cyclodextrin parcel
Macromolecule filming material 30 ~ 80%
Other adjuvant 0 ~ 20%
The percentage ratio sum of said components content is 100%; Wherein:
Described cyclodextrin is more than one in HP-β-CD or glucose group-beta-cyclodextrin, and the weight ratio of cyclodextrin and Aripiprazole is 1:1 ~ 3:1;
The method of the Aripiprazole of cyclodextrin parcel, comprises the steps:
By cyclodextrin and hydrochloric acid solution mixed dissolution, add Aripiprazole, at 55 ~ 65 DEG C, stir 0.5 ~ 1.5h, the Aripiprazole of described cyclodextrin parcel can be obtained;
The concentration of described hydrochloric acid solution is 0.08M ~ 0.12M;
The weight of cyclodextrin and the w/v of described hydrochloric acid solution are:
Cyclodextrin: hydrochloric acid solution=1g: 0.9 ~ 1.1ml.
4. the molten membrane of Aripiprazole mouth according to claim 3, is characterized in that, the weight ratio 1.2:1 ~ 1.5:1 of cyclodextrin and Aripiprazole.
5. the molten membrane of Aripiprazole mouth according to claim 3, it is characterized in that, described macromolecule filming material comprise in hydroxypropyl emthylcellulose (HPMC), hydroxypropyl cellulose (HPC), polyvinyl alcohol (PVA), polyvinylpyrrolidone (PVP), sodium alginate, polyoxyethylene (PEO), Bletilla glucomannan, corn starch or carrageenan more than one.
6. the molten membrane of Aripiprazole mouth according to claim 3, is characterized in that, other adjuvants described comprise plasticizer, correctives, gummy macromolecular material, lecithin, cephalin, phosphatidic acid, pigment, antioxidant or antiseptic;
Described plasticizer is selected from PEG, glycerol or Tween 80, and described correctives is selected from sweeting agent, acidic flavoring agent or aromatic.
7. the molten membrane of Aripiprazole mouth according to claim 3, is characterized in that, comprise the component of following percentage by weight:
The Aripiprazole 30 ~ 50% of cyclodextrin parcel
Macromolecule filming material 45 ~ 70%
Other adjuvant 0 ~ 5%
The percentage ratio sum of said components content is 100%.
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| CN105078910B (en) * | 2015-09-22 | 2018-05-22 | 成都欣捷高新技术开发有限公司 | It is a kind of containing according to lyophilized oral formulations of piperazine azoles and preparation method thereof |
| CN107375945B (en) * | 2017-08-29 | 2020-10-13 | 沈阳药科大学 | Donepezil cyclodextrin inclusion compound and oral instant film agent containing same |
| CN111991373B (en) | 2020-09-21 | 2022-04-08 | 力品药业(厦门)股份有限公司 | Aripiprazole orally-dissolving film and preparation method thereof |
| TW202304441A (en) * | 2021-05-26 | 2023-02-01 | 大陸商上海博志研新藥物技術有限公司 | Cariprazine oral soluble film composition, preparation method and use thereof |
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2014
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Non-Patent Citations (2)
| Title |
|---|
| "Aripiprazole-Cyclodextrin Binary Systems for Dissolution Enhancement: Effect of Preparation Technique, Cyclodextrin Type and Molar Ratio";Shaimaa M. Badr-Eldin et al.;《Iranian Journal of Basic Medical Sciences》;20131231;第16卷(第12期);第1223-1231页 * |
| "Formulation development and evaluation of mouth dissolving film of domperidone";Pratikkumar Joshi et al.;《Journal of Pharmacy & Bioallied Sciences》;20120331;第4卷(第5期);第108-109页 * |
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