CN110731945A - Memantine hydrochloride orally disintegrating tablet and its preparation method - Google Patents
Memantine hydrochloride orally disintegrating tablet and its preparation method Download PDFInfo
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- CN110731945A CN110731945A CN201810788675.5A CN201810788675A CN110731945A CN 110731945 A CN110731945 A CN 110731945A CN 201810788675 A CN201810788675 A CN 201810788675A CN 110731945 A CN110731945 A CN 110731945A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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Abstract
The invention discloses memantine hydrochloride orally disintegrating tablets and a preparation method thereof, the orally disintegrating tablets contain granules containing memantine hydrochloride prepared by taking microcrystalline cellulose as a substrate and adopting a fluidized bed coating process, the bad taste of memantine hydrochloride is effectively covered, and the orally disintegrating tablets are used for treating senile dementia caused by Alzheimer's disease.
Description
Technical Field
The invention discloses pharmaceutical compositions for treating senile dementia, in particular to pharmaceutical orally disintegrating tablets containing memantine hydrochloride and a preparation method thereof.
Background
Alzheimer's Disease (AD) is degenerative diseases of the central nervous system, is the most common type of senile dementia, is an irreversible progressive disorder of brain cell (neuron) deteriorations, has an implicit attack of diseases, has a chronic progressive course, and has an increasing incidence rate with age, and clinical manifestations of cognitive decline, abnormal mental behaviors, reduction of daily living capacity and the like, research make internal disorder or usurp shows that the pathogenesis of AD is related to central cholinergic injury and excitatory amino acid toxicity, data published by WHO in 2 years and 2 months show that nearly 3560 thousands of AD patients exist in the world, people are expected to turn times in 2030 (6570 thousands), and three times of the current day will be reached in 2050.
The memantine hydrochloride product can directly stimulate dopamine receptors and promote dopamine release, and a neuron regulator memantine hydrochloride with a bidirectional regulating effect acts on a glutamine system in the brain, so that the memantine hydrochloride product is a non-competitive N-methyl-D-aspartate (NMDA) antagonist with medium affinity. When the glutamic acid is released in pathological amount, the memantine hydrochloride can reduce the neurotoxic effect of the glutamic acid, and when the glutamic acid is released in a small amount, the memantine hydrochloride can improve the transfer of the glutamic acid required by the memory process.
The orally disintegrating tablet is kinds of new oral preparation forms, and may be dissolved or disintegrated to form fine granule without grit feeling in oral cavity in 15S or 30S without needing drinking water and after being taken, the medicine reaches the tissue and organ via saliva.
The orally disintegrating tablet provides novel medicine taking modes for patients, is convenient for the old and the infants to take medicines, and also has great superiority for the medicines of special environments and special crowds, such as the medicines taken by patients who cannot stand upright after operation, dysphagia patients, mental disease patients and partial disabled patients in the outdoor or field anhydrous environment.
The applicant finds that the taste of memantine hydrochloride cannot be well covered up and bitter remains still exist in the orally disintegrating tablets and the dispersible tablets prepared by the preparation methods provided by the two patents.
Disclosure of Invention
Compared with a common sustained-release preparation, the orally disintegrating tablet prepared according to the application has the advantages of good taste, no bitter taste, no sand feeling, quick disintegration and capability of improving the compliance and compliance of patients.
According to the application memantine hydrochloride orally disintegrating tablet and a preparation method thereof, the memantine hydrochloride orally disintegrating tablet comprises the following components, by weight, 5% of memantine hydrochloride, 2% to 5% of Etteke EPO, 10% to 40% of microcrystalline cellulose, 0% to 40% of other fillers, 5% to 30% of disintegrating agents, 0.1% to 5% of flavoring agents and 0.1% to 5% of lubricants.
According to memantine hydrochloride orally disintegrating tablets and the preparation method thereof, memantine hydrochloride and microcrystalline cellulose are coated after a wet granulation process, and are uniformly mixed with additional materials for tabletting, so that the memantine hydrochloride orally disintegrating tablets have the following additional technical characteristics:
, the memantine hydrochloride orally disintegrating tablets comprise 5% of memantine hydrochloride, 0-40% of Ewing EPO 2-5%, 10-40% of microcrystalline cellulose, 0-40% of other fillers, 5-30% of disintegrating agents, 0.1-5% of flavoring agents and 0.1-5% of lubricants by weight, and the memantine hydrochloride orally disintegrating tablets comprise the following steps:
s101: firstly, preparing the Etteki EPO into a coating solution for later use;
s102: then, fully and uniformly mixing the memantine hydrochloride and the microcrystalline cellulose, adding a wetting agent, and uniformly stirring to obtain a soft material; granulating, drying, and grading to obtain main medicinal granule.
S103: coating granules by using microcrystalline cellulose granules containing memantine hydrochloride as a substrate and adopting a fluidized bed; stopping coating when the ratio of memantine hydrochloride to UttyQi EPO is 1 to (0.5-1); preferably, the ratio of memantine hydrochloride to the Ettky EPO is 1: 1;
s104: converting the dosage of the filler, the disintegrant, the flavoring agent and the lubricant, adding the mixture into the coated particles obtained in S103, and fully and uniformly mixing to obtain total mixed materials for tabletting.
, the memantine hydrochloride orally disintegrating tablets, wherein the filler is mannitol.
, the memantine hydrochloride orally disintegrating tablets comprise or more of croscarmellose sodium, sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose and crospovidone.
, the memantine hydrochloride orally disintegrating tablets, the lubricant comprising magnesium stearate.
, the memantine hydrochloride orally disintegrating tablets are prepared by the step S101, wherein the pretreatment mode is to pass through a screen in advance, and the mesh number of the screen is 60-80 meshes.
, the preparation method of the memantine hydrochloride orally disintegrating tablets comprises the step S101, wherein the preparation ratio of the coating liquid with a certain concentration is that sodium dodecyl sulfate is 1% -2%, stearic acid is 2% -3%, Ewing EPO is 5% -10%, talcum powder is 2% -5%, and purified water is 80% -90%.
, the wetting agent in step S102 is purified water in the memantine hydrochloride orally disintegrating tablets.
, the memantine hydrochloride orally disintegrating tablets have the wet granules with the particle size of 30-40 meshes in the step S102.
, the stable memantine hydrochloride orally disintegrating tablets preparation method, in the step S102, the moisture content of the dry granules is 1% -3%, and the particle size of the dry granules after finishing is 40-60 mesh.
, in the step S103, the temperature of the fluidized bed for coating the granules is set to 40-60 ℃, and the granules are cured for 1-2 hours after coating.
Another objects of the present application are to provide memantine hydrochloride orally disintegrating tablets prepared by the above preparation method, which have fast disintegrating time in oral cavity, no taste and gritty feeling, and good mouthfeel.
DETAILED DESCRIPTION OF EMBODIMENT (S) OF INVENTION
The present application is further illustrated by examples, and examples of orally disintegrating tablets of memantine hydrochloride and their preparation are provided, but the present application is not limited thereto.
The tablets compressed in the following examples, unless otherwise specified, were compressed on a tablet press of the same type , weighing 100mg and having a hardness controlled in the range of 20-40N.
EXAMPLE 15 preparation of orally disintegrating tablets of Memantine hydrochloride of the specification
1. Microcrystalline cellulose particles containing memantine hydrochloride
2. Memantine hydrochloride orally disintegrating tablet
The preparation process comprises the following steps:
(1) preparing a coating solution: weighing sodium dodecyl sulfate, stearic acid and Uygur with the prescription amount for later use, adding SDS into purified water, stirring for dissolving, adding stearic acid and Uygur, stirring for 1.5h, adding talcum powder, and continuing stirring for 30min for later use:
(2) preparing a soft material: weighing pretreated memantine hydrochloride and microcrystalline cellulose in a prescription amount, and uniformly mixing in a wet granulator; adding appropriate amount of purified water as wetting agent into wet granulator, and stirring to obtain soft material
(3) And (3) wet granulation: the soft mass was passed through a 40 mesh sieve to make wet granules.
(4) And (3) drying the particles: drying the wet granules at 50-55 ℃ until the water content of the granules is about 1-3%, and grading the granules by using a 60-mesh screen.
(5) Coating the granules: coating the granules obtained in the step (5) in a multifunctional fluidized bed, controlling the temperature of the materials to be 25-35 ℃, and stopping coating when the ratio of the memantine hydrochloride to the Uttyzky EPO is 1: 1; drying and solidifying for 2 hours until the water content is 1-3%, and finishing the granules by using a 60-mesh screen; and (5) standby.
(6) Total mixing: weighing the coating granules containing memantine hydrochloride, mannitol, microcrystalline cellulose, low-substituted hydroxypropyl cellulose, acesulfame potassium and magnesium stearate according to the prescription amount, uniformly mixing and tabletting.
EXAMPLE 25 preparation of orally disintegrating tablets of Memantine hydrochloride of the specification
1. Microcrystalline cellulose particles containing memantine hydrochloride
2 Memantine hydrochloride orally disintegrating tablet
The preparation process comprises the following steps:
(1) preparing a coating solution: weighing sodium dodecyl sulfate, stearic acid and Uygur with the prescription amount for later use, adding SDS into purified water, stirring for dissolving, adding stearic acid and Uygur, stirring for 1.5h, adding talcum powder, and continuing stirring for 30min for later use:
(2) preparing a soft material: weighing pretreated memantine hydrochloride and microcrystalline cellulose in a prescription amount, and uniformly mixing in a wet granulator; adding appropriate amount of purified water as wetting agent into wet granulator, and stirring to obtain soft material
(3) And (3) wet granulation: the soft mass was passed through a 40 mesh sieve to make wet granules.
(4) And (3) drying the particles: drying the wet granules at 50-55 ℃ until the water content of the granules is about 1-3%, and grading the granules by using a 60-mesh screen.
(5) Coating the granules: coating the granules obtained in the step (4) in a multifunctional fluidized bed, controlling the temperature of the materials to be 25-35 ℃, and stopping coating when the ratio of the memantine hydrochloride to the Uttyzky EPO is 1: 0.5; drying and solidifying for 2 hours until the water content is 1-3%, and finishing the granules by using a 60-mesh screen; and (5) standby.
(6) Total mixed pressing sheet: weighing the coating granules containing memantine hydrochloride, mannitol, microcrystalline cellulose, low-substituted hydroxypropyl cellulose, acesulfame potassium and magnesium stearate according to the prescription amount, uniformly mixing and tabletting.
EXAMPLE 35 preparation of orally disintegrating tablets of Memantine hydrochloride of the specification
Prescription composition
The preparation process comprises the following steps:
total mixed pressing sheet: weighing the coating granules containing memantine hydrochloride, mannitol, microcrystalline cellulose, crospovidone, acesulfame and magnesium stearate according to the prescription amount, uniformly mixing and tabletting.
EXAMPLE 45 preparation of orally disintegrating tablets of Memantine hydrochloride of the specification
Prescription composition
The preparation process comprises the following steps:
total mixed pressing sheet: weighing the coating granules containing memantine hydrochloride, mannitol, microcrystalline cellulose, crospovidone, acesulfame and magnesium stearate according to the prescription amount, uniformly mixing and tabletting.
And (3) analyzing an experimental result:
EXAMPLES 1 to 4 examination of disintegration time
EXAMPLES 1 to 4 taste examination
Taste evaluation criteria: 0: no pungent taste; 1: a least irritating taste; 2: a slightly pungent taste; 3: a more pungent taste; 4: strong pungent taste 5: intolerable pungent taste
Taste; 3: a more pungent taste; 4: strong pungent taste 5: intolerable pungent taste
And (3) comprehensive evaluation: has good taste, no bitter taste, no gritty sensation, and rapid oral cavity disintegration.
Claims (9)
1, Memantine hydrochloride orally disintegrating tablets, which comprise the following components in percentage by weight:
5 percent of memantine hydrochloride, 2 to 5 percent of Ettky EPO, 10 to 40 percent of microcrystalline cellulose, 0 to 40 percent of other fillers, 5 to 30 percent of disintegrating agent, 0.1 to 5 percent of flavoring agent and 0.1 to 5 percent of lubricant.
2. The memantine hydrochloride orally disintegrating tablets of claim 1, wherein the preparation method comprises the following steps:
s101: firstly, preparing the Etteki EPO into a coating solution for later use;
s102: then, fully and uniformly mixing the memantine hydrochloride and the microcrystalline cellulose, adding a wetting agent, and uniformly stirring to obtain a soft material; granulating, drying, and grading to obtain main medicinal granule;
s103: coating granules by using microcrystalline cellulose granules containing memantine hydrochloride as a substrate and adopting a fluidized bed; stopping coating when the ratio of memantine hydrochloride to UttyQi EPO is 1 to (0.5-1); preferably, the ratio of memantine hydrochloride to the Ettky EPO is 1: 1;
s104: converting the dosage of the filler, the disintegrant, the flavoring agent and the lubricant, adding the mixture into the coated particles obtained in S103, and fully and uniformly mixing to obtain total mixed materials for tabletting.
3. The memantine hydrochloride orally disintegrating tablets of claim 1, said bulking agent being mannitol.
4. The memantine hydrochloride orally disintegrating tablets of claim 1, said disintegrant comprising or several of croscarmellose sodium, sodium carboxymethyl starch, low substituted hydroxypropyl cellulose, and crospovidone.
5. The memantine hydrochloride orally disintegrating tablets of claim 1, said lubricant comprising magnesium stearate.
6. The method for preparing memantine hydrochloride orally disintegrating tablets of claim 2, wherein the concentration coating solution of step S101 is prepared from sodium dodecyl sulfate 0.8-1%, stearic acid 1-2%, Ewing EPO 5-10%, talc powder 2-5%, and purified water 80-90%, and the preparation method comprises suspending the sodium dodecyl sulfate, stearic acid, and Ewing EPO in purified water, adding talc powder, and stirring.
7. The method for preparing memantine hydrochloride orally disintegrating tablets of claim 2, wherein said wetting agent is purified water in said step S102.
8. The method for preparing memantine hydrochloride orally disintegrating tablets of claim 2, wherein in step S102, the wet granules have a particle size of 30-40 mesh, the dry granules have a moisture content of 1% -3%, and the particle size of the dry granules after finishing is 40-60 mesh.
9. The method for preparing memantine hydrochloride orally disintegrating tablets of claim 2, wherein in step S103, the tablet is cured for 1-2 h after coating.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810788675.5A CN110731945A (en) | 2018-07-18 | 2018-07-18 | Memantine hydrochloride orally disintegrating tablet and its preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810788675.5A CN110731945A (en) | 2018-07-18 | 2018-07-18 | Memantine hydrochloride orally disintegrating tablet and its preparation method |
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| Publication Number | Publication Date |
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| CN110731945A true CN110731945A (en) | 2020-01-31 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201810788675.5A Pending CN110731945A (en) | 2018-07-18 | 2018-07-18 | Memantine hydrochloride orally disintegrating tablet and its preparation method |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1679525A (en) * | 2005-01-12 | 2005-10-12 | 复旦大学 | Oral disintegrant of compound paracetamol |
| CN1709229A (en) * | 2005-06-10 | 2005-12-21 | 北京阜康仁生物制药科技有限公司 | Memantine hydrochloride orally disintegrating tablet and its preparing method |
| WO2015117999A1 (en) * | 2014-02-05 | 2015-08-13 | Sanovel Ilac Sanayi Ve Ticaret A.S. | Orally disintegrating tablet formulations of memantine |
-
2018
- 2018-07-18 CN CN201810788675.5A patent/CN110731945A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1679525A (en) * | 2005-01-12 | 2005-10-12 | 复旦大学 | Oral disintegrant of compound paracetamol |
| CN1709229A (en) * | 2005-06-10 | 2005-12-21 | 北京阜康仁生物制药科技有限公司 | Memantine hydrochloride orally disintegrating tablet and its preparing method |
| WO2015117999A1 (en) * | 2014-02-05 | 2015-08-13 | Sanovel Ilac Sanayi Ve Ticaret A.S. | Orally disintegrating tablet formulations of memantine |
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Application publication date: 20200131 |
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