Olanzapine medicine absorbed through oral mucosa

An oral mucosa and olanzapine technology, which is applied in the field of olanzapine drugs, can solve the problems of difficulty in quickly controlling the symptoms of schizophrenia in the acute phase, patients with mental illness not cooperating with treatment, and difficulty in guaranteeing treatment effects, so as to avoid the first pass of the liver. effect, improved bioavailability, fast-acting effect

CN102451162AInactive Publication Date: 2012-05-16重庆市力扬医药开发有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Publication Date
2012-05-16
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to an olanzapine medicine absorbed through an oral mucosa. The medicine is composed of olanzapine taken as an effective medicinal component and auxiliary components acceptable in oral mucosa medicines, wherein, the auxiliary components comprise a disintegrant, a filling agent, a flavoring agent, an adhesive, a mucosa absorption enhancer, and a lubricant. Specifically, the medicine includes the following preparation forms employed currently: sublingual tablets, toroches, buccal tablets, buccal adhesive tablets, and buccal patches, etc. Able to be completely or mainly absorbed by a sublingual mucosa and / or a buccal mucosa, the medicine of the invention has the advantages of no irritation on the oral cavity, ability to substantially improve medicinal bioavailability and treatment effect, as well as convenient administration, and can bring patients good compliance.
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Description

technical field

[0001] The present invention relates to a medicine absorbed through oral mucosa, specifically a kind of olanzapine medicine which can be absorbed through oral mucosa, including sublingual tablet, buccal tablet, buccal tablet, oral adhesive tablet and oral patch etc. Pharmaceutical preparations absorbed wholly or mainly by oral mucosa such as sublingual mucosa and / or buccal mucosa. Background technique

[0002] Olanzapine is suitable for the acute and maintenance treatment of schizophrenia and other psychosis with severe positive and / or negative symptoms, and can also relieve the secondary affective symptoms of schizophrenia and related diseases. The recommended starting dose of this product is 10mg per day, which can be taken before or after meals. Dosage ranges from 5 to 20 mg per day. The daily dose should be determined according to the clinical situation. Doses in excess of 10 mg daily should be preceded by appropriate clinical evaluation.

[0003] Ola...

Examples

Embodiment 1

[0023] Embodiment 1 (sublingual tablet)

[0024] composition:

[0025] Olanzapine 2.5g

[0026] Microcrystalline Cellulose 30g

[0027] Mannitol 25g

[0028] Sodium carboxymethyl starch 3g

[0029] Magnesium stearate 0.5g

[0030]

[0031] Made into 1000 pieces

[0032] Preparation method: Olanzapine is micronized with a jet mill to a particle size of D 90 ≤50μm, weighed according to the prescription, mixed evenly with the prescription amount of auxiliary ingredients such as microcrystalline cellulose and mannitol, directly compressed into tablets, and the hardness is controlled at 3-5kg, that is to say.

Embodiment 2

[0033] Embodiment 2 (sublingual tablet)

[0034] composition:

[0035] Olanzapine 5g

[0036] Starch 20g

[0037] Microcrystalline Cellulose 30g

[0038] 10g pregelatinized starch

[0039] Crospovidone 4g (half inside and outside)

[0040] Talc powder 0.5g

[0041]

[0042] Made into 1000 pieces

[0043] Preparation method: Olanzapine is micronized with a jet mill to a particle size of D 90 ≤30μm, mix the prescribed amount of olanzapine with auxiliary ingredients such as starch and microcrystalline cellulose, granulate with pure water as wetting agent, dry, granulate, add crospovidone and talc powder, mix Evenly, press into tablets, the hardness is controlled at 3-5kg, that is to say.

Embodiment 3

[0044] Embodiment 3 (sublingual tablet)

[0045] composition:

[0046] Olanzapine 3.5g

[0047] Lactose 30g

[0048] 40g pregelatinized starch

[0049] Croscarmellose Sodium 6g

[0050] Stevioside 5g

[0051] Peppermint Oil 0.1g

[0052] Talc powder 1.5g

[0053]

[0054]Made into 1000 pieces

[0055] Preparation method: use a ball mill to pulverize olanzapine to a particle size of D 90 ≤80μm, after uniformly mixing olanzapine, lactose, pregelatinized starch and other auxiliary ingredients, directly compressing tablets, the hardness is controlled at 2-4kg, that is.