Levodopa/benserazide orally disintegrating tablet

The technology of oral disintegrating tablet and dopasehydrazine is applied in the directions of drug combination, amide active ingredient, nervous system diseases, etc., which can solve the problems of inconvenience, difficulty in taking the whole tablet, inconvenience for patients to use, etc. Cool taste, good taste effect

CN101797244BInactive Publication Date: 2012-07-04QINGDAO UNIV OF SCI & TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Publication Date
2012-07-04
Estimated Expiration
Not applicable · inactive patent
Patent Text Reader

Abstract

The invention discloses a levodopa / benserazide orally disintegrating tablet and a preparation method thereof. The tablet comprises the main drugs including levodopa and benserazide and the auxiliary materials including microcrystalline cellulose, mannitol, lactose, crospolyvinylpyrrolidone, low-substituted hydroxypropyl cellulose, sodium cyclamate, menthol, aerosol and magnesium stearate. The tablet of the invention can effectively treat the Parkinson disease or Parkinsonism syndrome, is convenient to take, good in mouthfeel, quick in disintegration, fast in absorption and high in bioavailability and provides convenience for the Parkinson disease or Parkinsonism syndrome patients who have difficulty in taking the whole tablet or feel inconvenient to take the tablet.
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Description

1. Technical field

[0001] The invention relates to an oral compound pharmaceutical preparation for treating Parkinson's disease or Parkinson's syndrome, in particular to an orally disintegrating tablet of dopasrazide which can be disintegrated and released quickly, has good taste and is convenient to take. 2. Background technology

[0002] Dopaserazide orally disintegrating tablets are compound preparations. Dopamine deficiency in the basal ganglia of patients with Parkinson's disease or Parkinson's syndrome. Unlike dopamine, levodopa can cross the blood-brain barrier and enter the central nervous system. As a direct metabolic precursor of dopamine, it makes dopamine replacement therapy feasible. However, levodopa is rapidly decarboxylated outside the brain and transformed into dopamine, which leads to a large amount of waste of levodopa and frequent occurrence of adverse reactions. Therefore, it would be beneficial to inhibit the extracerebral decarboxylation of levodopa....

Examples

Embodiment 1

[0036] The orally disintegrating tablet of dopaserazide includes the main drug and auxiliary materials, and is characterized in that it is formulated according to the following mass percentages: 30% of the main drug levodopa, 7.5% of the main drug benserazide, and 62.5% of auxiliary materials.

[0037] Levodopa 75g (30.00%)

[0038] Benserazide 18.75g (7.50%)

[0039] Microcrystalline Cellulose 40g (16.00%)

[0040] Mannitol 67g (26.80%)

[0041] Low-substituted hydroxypropyl cellulose 3g (1.20%)

[0042] Lactose 19.25g (7.70%)

[0043] Anhydrous Citric Acid 2g (0.80%)

[0044] Cross-linked polyvinylpyrrolidone 20g (8.00%)

[0045] Cyclamate 1.5g (0.60%)

[0046] Menthol 1.5g (0.60%)

[0047] Micronized silica gel 1g (0.40%)

[0048] Magnesium Stearate 1g (0.40%)

[0049] A total of 1000 tablets were produced

[0050] Among them, lactose and mannitol are fillers, microcrystalline cellulose, cross-linked polyvinylpyrrolidone, and low-substituted hydroxypropyl cellulos...

Embodiment 2

[0058] The orally disintegrating tablet of dopaserazide comprises a main drug and auxiliary materials, and is characterized in that it is prepared according to the following mass percentages: 20% of the main drug levodopa, 5% of the main drug benserazide, and 75% of auxiliary materials.

[0059] Levodopa 50 20.00%

[0060] Benserazide 12.5g (5.00%)

[0061] Microcrystalline Cellulose 90g (36.00%)

[0062] Mannitol 5g (2.00%)

[0063] Low Substituted Hydroxypropyl Cellulose 15g (6.00%)

[0064] Lactose 66g (26.40%)

[0065] Anhydrous citric acid 1g (0.40%)

[0066] Cross-linked polyvinylpyrrolidone 2g (0.80%)

[0067] Cyclamate 1g (0.40%)

[0068] Menthol 1g (0.40%)

[0069] Micronized silica gel 5g (2.00%)

[0070] Magnesium Stearate 1.5g (0.60%)

[0071] A total of 1000 tablets were produced

[0072] The preparation method of the dopaserazide orally disintegrating tablet of the present invention is the same as that in Example 1, and the dopaserazide orally disintegr...

Embodiment 3

[0076] The orally disintegrating tablet of dopaserazide comprises a main drug and auxiliary materials, and is characterized in that it is prepared according to the following mass percentages: 20% of the main drug levodopa, 5% of the main drug benserazide, and 75% of auxiliary materials.

[0077] Levodopa 50g (20.00%)

[0078] Benserazide 12.5g (5.00%)

[0079] Microcrystalline Cellulose 90g (36.00%)

[0080] Mannitol 5g (2.00%)

[0081] Low Substituted Hydroxypropyl Cellulose 15g (6.00%)

[0082] Lactose 66g (26.40%)

[0083] Anhydrous citric acid 1g (0.40%)

[0084] Cross-linked polyvinylpyrrolidone 2g (0.80%)

[0085] Cyclamate 1g (0.40%)

[0086] Menthol 1g (0.40%)

[0087] Micronized silica gel 5g (2.00%)

[0088] Magnesium Stearate 1.5g (0.60%)

[0089] A total of 1000 tablets were produced

[0090] The preparation method of the dopaserazide orally disintegrating tablet of the present invention is the same as that in Example 1, and the dopaserazide orally disint...