CN104706604A - Perampanel freeze-dried oral disintegrating tablet and preparation method thereof - Google Patents
Perampanel freeze-dried oral disintegrating tablet and preparation method thereof Download PDFInfo
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- CN104706604A CN104706604A CN201310692519.6A CN201310692519A CN104706604A CN 104706604 A CN104706604 A CN 104706604A CN 201310692519 A CN201310692519 A CN 201310692519A CN 104706604 A CN104706604 A CN 104706604A
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- CN
- China
- Prior art keywords
- oral cavity
- disintegration tablet
- cavity disintegration
- lyophilizing
- lun panai
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- 238000002360 preparation method Methods 0.000 title claims abstract description 16
- PRMWGUBFXWROHD-UHFFFAOYSA-N perampanel Chemical compound O=C1C(C=2C(=CC=CC=2)C#N)=CC(C=2N=CC=CC=2)=CN1C1=CC=CC=C1 PRMWGUBFXWROHD-UHFFFAOYSA-N 0.000 title abstract description 6
- 229960005198 perampanel Drugs 0.000 title abstract description 6
- 238000004108 freeze drying Methods 0.000 claims abstract description 22
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 15
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims description 84
- 210000000214 mouth Anatomy 0.000 claims description 33
- 238000010792 warming Methods 0.000 claims description 24
- 239000007788 liquid Substances 0.000 claims description 16
- 239000011230 binding agent Substances 0.000 claims description 13
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 13
- 108010010803 Gelatin Proteins 0.000 claims description 12
- 229920000159 gelatin Polymers 0.000 claims description 12
- 239000008273 gelatin Substances 0.000 claims description 12
- 235000019322 gelatine Nutrition 0.000 claims description 12
- 235000011852 gelatine desserts Nutrition 0.000 claims description 12
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 10
- 229930195725 Mannitol Natural products 0.000 claims description 10
- 239000000594 mannitol Substances 0.000 claims description 10
- 235000010355 mannitol Nutrition 0.000 claims description 10
- 239000002245 particle Substances 0.000 claims description 10
- 229920002307 Dextran Polymers 0.000 claims description 9
- 238000007710 freezing Methods 0.000 claims description 8
- 239000007787 solid Substances 0.000 claims description 8
- 238000003756 stirring Methods 0.000 claims description 8
- 239000004376 Sucralose Substances 0.000 claims description 7
- 239000000203 mixture Substances 0.000 claims description 7
- 235000019408 sucralose Nutrition 0.000 claims description 7
- BAQAVOSOZGMPRM-QBMZZYIRSA-N sucralose Chemical compound O[C@@H]1[C@@H](O)[C@@H](Cl)[C@@H](CO)O[C@@H]1O[C@@]1(CCl)[C@@H](O)[C@H](O)[C@@H](CCl)O1 BAQAVOSOZGMPRM-QBMZZYIRSA-N 0.000 claims description 7
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 4
- 238000009472 formulation Methods 0.000 claims description 4
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 4
- 239000000758 substrate Substances 0.000 claims description 4
- 239000000811 xylitol Substances 0.000 claims description 4
- 235000010447 xylitol Nutrition 0.000 claims description 4
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 4
- 229960002675 xylitol Drugs 0.000 claims description 4
- HDTRYLNUVZCQOY-UHFFFAOYSA-N α-D-glucopyranosyl-α-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OC1C(O)C(O)C(O)C(CO)O1 HDTRYLNUVZCQOY-UHFFFAOYSA-N 0.000 claims description 3
- 108010011485 Aspartame Proteins 0.000 claims description 3
- HDTRYLNUVZCQOY-WSWWMNSNSA-N Trehalose Natural products O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-WSWWMNSNSA-N 0.000 claims description 3
- HDTRYLNUVZCQOY-LIZSDCNHSA-N alpha,alpha-trehalose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-LIZSDCNHSA-N 0.000 claims description 3
- 239000000605 aspartame Substances 0.000 claims description 3
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 claims description 3
- 235000010357 aspartame Nutrition 0.000 claims description 3
- 229960003438 aspartame Drugs 0.000 claims description 3
- 239000000686 essence Substances 0.000 claims description 2
- 239000000413 hydrolysate Substances 0.000 claims description 2
- 239000004615 ingredient Substances 0.000 claims description 2
- 239000003814 drug Substances 0.000 abstract description 4
- 206010015037 epilepsy Diseases 0.000 abstract description 2
- 239000000853 adhesive Substances 0.000 abstract 1
- 230000001070 adhesive effect Effects 0.000 abstract 1
- 239000011814 protection agent Substances 0.000 abstract 1
- 238000012360 testing method Methods 0.000 description 6
- 239000004576 sand Substances 0.000 description 5
- 206010010904 Convulsion Diseases 0.000 description 3
- 108010009736 Protein Hydrolysates Proteins 0.000 description 2
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 2
- 230000001037 epileptic effect Effects 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 239000012528 membrane Substances 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 239000002994 raw material Substances 0.000 description 2
- UUDAMDVQRQNNHZ-UHFFFAOYSA-N (S)-AMPA Chemical compound CC=1ONC(=O)C=1CC(N)C(O)=O UUDAMDVQRQNNHZ-UHFFFAOYSA-N 0.000 description 1
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical group O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- 206010061334 Partial seizures Diseases 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 210000004720 cerebrum Anatomy 0.000 description 1
- 230000018044 dehydration Effects 0.000 description 1
- 238000006297 dehydration reaction Methods 0.000 description 1
- 238000009792 diffusion process Methods 0.000 description 1
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 description 1
- 238000007599 discharging Methods 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000007831 electrophysiology Effects 0.000 description 1
- 238000002001 electrophysiology Methods 0.000 description 1
- 230000008451 emotion Effects 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 210000003238 esophagus Anatomy 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 208000028316 focal seizure Diseases 0.000 description 1
- 239000003825 glutamate receptor antagonist Substances 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- 229960003943 hypromellose Drugs 0.000 description 1
- 229960001021 lactose monohydrate Drugs 0.000 description 1
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 229940057948 magnesium stearate Drugs 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 210000005036 nerve Anatomy 0.000 description 1
- 230000001537 neural effect Effects 0.000 description 1
- 230000036963 noncompetitive effect Effects 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 238000012827 research and development Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000004408 titanium dioxide Substances 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
The invention relates to a perampanel freeze-dried oral disintegrating tablet and a preparation method thereof. The perampanel freeze-dried oral disintegrating tablet comprises, by weight, 1-20 parts of a framework propping agent, 1-50 parts of an adhesive, 0.1-8 parts of a freeze drying protection agent and 2-12 parts of perampanel. The perampanel freeze-dried oral disintegrating tablet is convenient for patients to take and improves the medicine taking compliance of epilepsy patients, and the preparation method has the advantages of simplicity and short time.
Description
Technical field
The present invention relates to oral formulations field, be specifically related to pyrrole Lun Panai oral cavity disintegration tablet and preparation method thereof, relate to pyrrole Lun Panai lyophilizing oral cavity disintegration tablet and preparation method thereof more specifically.
Background technology
Partial seizures Ye Cheng focal seizure, clinical and electroencephalogram changes prompting at first, first cerebral hemisphere partial nerve unit is activated, then occur discharging simultaneously and rapidly, be rapidly to the diffusion of surrounding normal brain district, produce a series of electro physiology and neuro chemistry change, reduce that to neuronal energy exhaustion and metabolism outbreak is stopped automatically.
Pyrrole Lun Panai (perampanel) is noncompetitive amino-3-hydroxyl-5-methyl-4-isoxazole-propanoic acid (AMPA) glutamate receptor antagonist, is applicable to the partial seizure Patients with Epilepsy for the treatment of more than 12 years old and 12 years old.It is researched and developed by Japanese Wei Cai company, chemical name: 2-[4-(1,3-benzodioxole-5-ylmethyl) piperazine-1-base] pyrimidine 3/4 hydrate, and structural formula is as follows:
What pyrrole Lun Panai had gone on the market is thin membrane coated tablet, and the adjuvant of this thin membrane coated tablet is lactose monohydrate, low-substituted hydroxypropyl cellulose, polyvidone, microcrystalline Cellulose, magnesium stearate, hypromellose, Polyethylene Glycol, Pulvis Talci, titanium dioxide.
Due to the difference of the state of an illness, may there is the situation taking coated tablet difficulty in epileptic patient, need with water delivery service taking in process, improperly may cause esophagus sense of discomfort, affect the emotion of patient if taken.So research and development one does not need water delivery service, the medicament taken fast, be very necessary for epileptic patient.
Summary of the invention
The object of the invention there is provided a kind of pyrrole Lun Panai lyophilizing oral cavity disintegration tablet and preparation method thereof.
A kind of pyrrole Lun Panai lyophilizing oral cavity disintegration tablet provided by the invention is primarily of pyrrole Lun Panai and substrate composition, and this lyophilizing oral cavity disintegration tablet substrate comprises: skeletal support agent 1 ~ 20 weight portion, binding agent 1 ~ 50 weight portion, freeze drying protectant 0.1 ~ 8 weight portion;
Effective ingredient: pyrrole Lun Panai 2 ~ 12 weight portion.
The invention provides a kind of pyrrole Lun Panai lyophilizing oral cavity disintegration tablet, it is characterized in that the particle diameter of pyrrole Lun Panai is less than or equal to 10 μm.
The invention provides a kind of pyrrole Lun Panai lyophilizing oral cavity disintegration tablet, it is characterized in that skeletal support agent is selected from: one or more in mannitol, xylitol, trehalose.
Skeletal support agent is that for keeping pill shapes, mannitol can play the effect of skeletal support, and its mouthfeel is better in order to prevent tablet after lyophilizing dehydration from subsiding.Inventor finds that xylitol and trehalose may be used for the skeletal support of lyophilizing sheet equally in an experiment.
The invention provides a kind of pyrrole Lun Panai lyophilizing oral cavity disintegration tablet, it is characterized in that binding agent is selected from: one or both in gelatin, gelatin hydrolysate.
The invention provides a kind of pyrrole Lun Panai lyophilizing oral cavity disintegration tablet, it is characterized in that freeze drying protectant is dextran.
The invention provides a kind of pyrrole Lun Panai lyophilizing oral cavity disintegration tablet, it is characterized in that the oral specification of pyrrole Lun Panai lyophilizing oral cavity disintegration tablet is: any one in 2mg, 4mg, 6mg, 8mg, 10mg, 12mg.
The invention provides a kind of pyrrole Lun Panai lyophilizing oral cavity disintegration tablet, it is characterized in that this lyophilizing oral cavity disintegration tablet also containing correctives 0 ~ 0.08 weight portion,
Correctives is selected from: one or more in sucralose, aspartame, essence.
Pyrrole Lun Panai lyophilizing oral cavity disintegration tablet of the present invention is adopted and is prepared with the following method, and preparation process is as follows:
Skeletal support agent, binding agent, freeze drying protectant are added to the water abundant dissolving, add pyrrole Lun Panai, stir;
Draw medicinal liquid, add mould by formulation amount;
Mould is placed in-40 DEG C ~-120 DEG C environment quick-freezings;
Freeze drying box put into by solid medicinal liquid, evacuation under-20 DEG C ~-50 DEG C low temperature environments, vacuum 10 ~ 20Pa, keeps 2 ~ 3 hours;
Be warming up to-10 DEG C ~-15 DEG C, keep 3 ~ 4 hours;
Be warming up to 5 DEG C ~ 15 DEG C, keep 1 ~ 2 hour;
Be warming up to 20 DEG C ~ 30 DEG C, keep 1 ~ 2 hour;
Outlet, overlay film, shears, and prints lot number.
Pyrrole Lun Panai indissoluble in water, so the consumption that will reduce water when dosing as far as possible, improves the speed of mixing.
Specific embodiment
Following examples are to better the present invention is described, not in order to limit protection scope of the present invention.
By mouthfeel test and Selection pyrrole Lun Panai raw material particle size:
Lyophilizing oral cavity disintegration tablet is disintegrate in the oral cavity, so mouthfeel is very important, time wherein in the oral cavity without grittiness, user more takes like a shot and takes medicine.The present invention has investigated pyrrole Lun Panai particle diameter to the impact of sand feeling when taking medicine, concrete grammar: the kind of fixing skeletal support agent, binding agent, freeze drying protectant, correctives and consumption; Pyrrole Lun Panai, through micronization, chooses 1 μm, 5 μm, 10 μm, 20 μm four kinds of particle diameters; Make the lyophilizing oral cavity disintegration tablet of the every sheet of 0.2ml containing pyrrole Lun Panai 2mg.In preparation, the consumption of each component is in table 1.
Table 1: the formulation components table investigating pyrrole Lun Panai particle diameter
| Composition | Content (g) |
| Pyrrole Lun Panai | 2 |
| Mannitol | 10 |
| Gelatin | 10 |
| Dextran | 0.1 |
| Sucralose | 0.01 |
Preparation process: skeletal support agent mannitol, binding agent gelatin, freeze drying protectant dextran, correctives sucralose are added to the water abundant dissolving, add pyrrole Lun Panai, stir, be dissolved to 0.2L;
Draw medicinal liquid, in each bubble-cap model, inject 0.2ml;
Mould is placed in-40 DEG C ~-120 DEG C environment quick-freezings;
Freeze drying box put into by solid medicinal liquid, evacuation under-20 DEG C ~-50 DEG C low temperature environments, vacuum 10 ~ 20Pa, keeps 3 hours;
Be warming up to-10 DEG C ~-15 DEG C, keep 3 hours;
Be warming up to 5 DEG C ~ 15 DEG C, keep 1 hour;
Be warming up to 20 DEG C ~ 30 DEG C, keep 1 hour;
Outlet, overlay film, shears, and prints lot number.
The lyophilizing oral cavity disintegration tablet of each particle diameter gets 3, carries out mouthfeel test with 27 years old healthy male, and lyophilizing sheet fills in mouthfeel after disintegrate in the oral cavity, then spue, and gargle twice with clear water, carried out the mouthfeel test of next tablet again every ten minutes, result of the test sees the following form 2.
Table 2: the pyrrole Lun Panai lyophilizing oral cavity disintegration tablet mouthfeel test of different-grain diameter
| Pyrrole Lun Panai particle diameter (μm) | Mouthfeel |
| 1 | Without sand feeling |
| 5 | Without sand feeling |
| 10 | Without sand feeling |
| 20 | Slightly sand feeling |
According to above-mentioned mouthfeel result of the test, the present invention selects pyrrole Lun Panai particle diameter for being less than or equal to 10 μm.
Lyophilizing oral cavity disintegration tablet prepared by the pyrrole Lun Panai raw material adopting particle diameter to be less than or equal to 10 μm.
Embodiment one
Each amounts of components in preparation:
Skeletal support agent mannitol, binding agent gelatin, freeze drying protectant dextran are added to the water abundant dissolving, add pyrrole Lun Panai, stir, be dissolved to 0.2L;
Draw medicinal liquid, in each bubble-cap model, inject 0.2ml;
Mould is placed in-50 DEG C of environment quick-freezings;
Freeze drying box put into by solid medicinal liquid, evacuation under-30 DEG C of low temperature environments, vacuum 10 ~ 20Pa, keeps 3 hours;
Be warming up to-10 DEG C ~-15 DEG C, keep 3 hours;
Be warming up to 5 DEG C ~ 15 DEG C, keep 1 hour;
Be warming up to 20 DEG C ~ 30 DEG C, keep 1 hour;
Outlet, overlay film, shears, and prints lot number.
Embodiment two
Each amounts of components in preparation:
Skeletal support agent mannitol, binding agent gelatin, freeze drying protectant dextran, correctives aspartame are added to the water abundant dissolving, add pyrrole Lun Panai, stir, be dissolved to 0.2L;
Draw medicinal liquid, in each bubble-cap model, inject 0.2ml;
Mould is placed in-40 DEG C of environment quick-freezings;
Freeze drying box put into by solid medicinal liquid, evacuation under-20 DEG C of low temperature environments, vacuum 10 ~ 20Pa, keeps 3 hours;
Be warming up to-10 DEG C ~-15 DEG C, keep 4 hours;
Be warming up to 5 DEG C ~ 15 DEG C, keep 2 hours;
Be warming up to 20 DEG C ~ 30 DEG C, keep 2 hours;
Outlet, overlay film, shears, and prints lot number.
Embodiment three
Each amounts of components in preparation:
Skeletal support agent mannitol, binding agent gelatin hydrolysate, freeze drying protectant dextran, correctives sucralose are added to the water abundant dissolving, add pyrrole Lun Panai, stir, be dissolved to 0.2L;
Draw medicinal liquid, in each bubble-cap model, inject 0.2ml;
Mould is placed in-60 DEG C of environment quick-freezings;
Freeze drying box put into by solid medicinal liquid, evacuation under-50 DEG C of low temperature environments, vacuum 10 ~ 20Pa, keeps 3 hours;
Be warming up to-10 DEG C ~-15 DEG C, keep 4 hours;
Be warming up to 5 DEG C ~ 15 DEG C, keep 1 hour;
Be warming up to 20 DEG C ~ 30 DEG C, keep 2 hours;
Outlet, overlay film, shears, and prints lot number.
Embodiment four
Each amounts of components in preparation:
Skeletal support agent mannitol and xylitol, binding agent gelatin, freeze drying protectant dextran, correctives sucralose are added to the water abundant dissolving, add pyrrole Lun Panai, stir, be dissolved to 0.4L;
Draw medicinal liquid, in each bubble-cap model, inject 0.4ml;
Mould is placed in-80 DEG C of environment quick-freezings;
Freeze drying box put into by solid medicinal liquid, evacuation under-25 DEG C of low temperature environments, vacuum 10 ~ 20Pa, keeps 3 hours;
Be warming up to-10 DEG C ~-15 DEG C, keep 4 hours;
Be warming up to 5 DEG C ~ 15 DEG C, keep 1 hour;
Be warming up to 20 DEG C ~ 30 DEG C, keep 2 hours;
Outlet, overlay film, shears, and prints lot number.
Embodiment five
Each amounts of components in preparation:
Skeletal support agent mannitol, binding agent gelatin and gelatin hydrolysate, freeze drying protectant dextran, correctives sucralose and essence are added to the water abundant dissolving, add pyrrole Lun Panai, stir, be dissolved to 0.4L;
Draw medicinal liquid, in each bubble-cap model, inject 0.4ml;
Mould is placed in-120 DEG C of environment quick-freezings;
Freeze drying box put into by solid medicinal liquid, evacuation under-20 DEG C of low temperature environments, vacuum 10 ~ 20Pa, keeps 3 hours;
Be warming up to-10 DEG C ~-15 DEG C, keep 4 hours;
Be warming up to 5 DEG C ~ 15 DEG C, keep 2 hours;
Be warming up to 20 DEG C ~ 30 DEG C, keep 2 hours;
Outlet, overlay film, shears, and prints lot number.
Claims (8)
1. a pyrrole Lun Panai lyophilizing oral cavity disintegration tablet is primarily of pyrrole Lun Panai and substrate composition, and it is characterized in that, this lyophilizing oral cavity disintegration tablet substrate comprises:
Skeletal support agent 1 ~ 20 weight portion, binding agent 1 ~ 50 weight portion, freeze drying protectant 0.1 ~ 8 weight portion;
Effective ingredient: pyrrole Lun Panai 2 ~ 12 weight portion.
2. lyophilizing oral cavity disintegration tablet as claimed in claim 1, is characterized in that the particle diameter of pyrrole Lun Panai is less than or equal to 10 μm.
3. lyophilizing oral cavity disintegration tablet as claimed in claim 1, is characterized in that skeletal support agent is selected from:
One or more in mannitol, xylitol, trehalose.
4. lyophilizing oral cavity disintegration tablet as claimed in claim 1, is characterized in that binding agent is selected from: one or both in gelatin, gelatin hydrolysate.
5. lyophilizing oral cavity disintegration tablet as claimed in claim 1, is characterized in that freeze drying protectant is dextran.
6. lyophilizing oral cavity disintegration tablet as claimed in claim 1, is characterized in that the content of pyrrole Lun Panai is: any one in 2mg, 4mg, 6mg, 8mg, 10mg, 12mg.
7. the lyophilizing oral cavity disintegration tablet as described in any one of claim 1 ~ 6, is characterized in that this lyophilizing oral cavity disintegration tablet also containing correctives 0 ~ 0.08 weight portion,
Correctives is selected from: one or more in sucralose, aspartame, essence.
8. a preparation method for the lyophilizing oral cavity disintegration tablet described in claim 1 ~ 7, step is as follows:
Skeletal support agent, binding agent, freeze drying protectant are added to the water abundant dissolving, add pyrrole Lun Panai, stir;
Draw medicinal liquid, add mould by formulation amount;
Mould is placed in-40 DEG C ~-120 DEG C environment quick-freezings;
Freeze drying box put into by solid medicinal liquid, evacuation under-20 DEG C ~-50 DEG C low temperature environments, vacuum 10 ~ 20Pa, keeps 2 ~ 3 hours;
Be warming up to-10 DEG C ~-15 DEG C, keep 3 ~ 4 hours;
Be warming up to 5 DEG C ~ 15 DEG C, keep 1 ~ 2 hour;
Be warming up to 20 DEG C ~ 30 DEG C, keep 1 ~ 2 hour;
Outlet, overlay film, shears, and prints lot number.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310692519.6A CN104706604A (en) | 2013-12-12 | 2013-12-12 | Perampanel freeze-dried oral disintegrating tablet and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310692519.6A CN104706604A (en) | 2013-12-12 | 2013-12-12 | Perampanel freeze-dried oral disintegrating tablet and preparation method thereof |
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| CN104706604A true CN104706604A (en) | 2015-06-17 |
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| CN201310692519.6A Pending CN104706604A (en) | 2013-12-12 | 2013-12-12 | Perampanel freeze-dried oral disintegrating tablet and preparation method thereof |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105287411A (en) * | 2015-09-22 | 2016-02-03 | 美吉斯制药（厦门）有限公司 | Perampanel dispersible tablet and preparation method thereof |
| CN106389367A (en) * | 2016-11-16 | 2017-02-15 | 杭州朱养心药业有限公司 | Perampanel coated tablet pharmaceutical composition |
| CN106619557A (en) * | 2017-02-21 | 2017-05-10 | 佛山市弘泰药物研发有限公司 | Perampanel gastric-soluble micro pellets and preparation method thereof |
| CN106692092A (en) * | 2017-02-20 | 2017-05-24 | 佛山市弘泰药物研发有限公司 | Fycompa tablet and preparation method thereof |
| CN106860409A (en) * | 2017-02-20 | 2017-06-20 | 佛山市弘泰药物研发有限公司 | A kind of pyrrole Lun Panai oral disintegrating tablets and preparation method thereof |
| WO2020124090A1 (en) * | 2018-12-14 | 2020-06-18 | Eisai R&D Management Co., Ltd. | Aqueous based pharmaceutical formulations of 1,2-dihydropyridine compounds |
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| CN1689649A (en) * | 2004-04-30 | 2005-11-02 | 量子高科（北京）研究院有限公司 | Oral cavity quick dissolving preparation and production method thereof |
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