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Oral cavity rapid disintegrating tablet medicament and method of preparing the same

A technology for oral fast disintegrating tablet and medicine, applied in the field of oral fast disintegrating tablet medicine and preparation thereof, can solve the problems of patients being unable to take care of themselves, inconvenient to use injections, etc., and achieve shortened drug dissolution time, good appearance and good wear resistance. Effect

Inactive Publication Date: 2008-06-11
DONGGUAN TAILI BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, for long-term rehabilitation users, the use of injections is extremely inconvenient, and patients cannot perform self-care

Method used

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  • Oral cavity rapid disintegrating tablet medicament and method of preparing the same
  • Oral cavity rapid disintegrating tablet medicament and method of preparing the same
  • Oral cavity rapid disintegrating tablet medicament and method of preparing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1 Preparation of Limoraban Citrate

[0024] Add 46.4g of rimoraban and 25.5g of anhydrous citric acid into a 500ml reaction flask, add 300ml of absolute ethanol, heat to reflux for 30min, add 2g of activated carbon, and then reflux for 30min. Filtrate while it is hot, cool the filtrate at room temperature first, and then freeze it in the refrigerator to precipitate white crystals, filter, and dry under reduced pressure to obtain 43.8 g of limoraban citrate product, with a yield of 79.7%. The reaction process is shown in the following formula:

[0025]

Embodiment 2

[0026] Example 2 Preparation of Limoraban Lactate

[0027] Add 46.4g of rimoraban and 11.5g of lactic acid into a 500ml reaction flask, add 300ml of absolute ethanol, heat to reflux for 30min, add 2g of activated carbon, and then reflux for 30min. Filtrate while it is hot, cool the filtrate to room temperature and put it in the refrigerator to freeze. White crystals are precipitated, filtered, and dried under reduced pressure to obtain 43.8 g of limoraban lactate product, with a yield of 79.7%. The reaction process is shown in the following formula:

[0028]

Embodiment 3～5

[0029] Examples 3-5 Preparation of Limoraban Citrate Orally Disintegrating Tablets

[0030] Drug A: Limoraban Citrate 5.0g

[0031] 70g microcrystalline cellulose

[0032] Low-substituted hydroxypropyl cellulose 5g

[0033] Micronized silica gel 2g

[0034] Magnesium stearate 1 g

[0035] 2 grams protein sugar

[0036] Starch 15g

[0037] Drug B: Limoraban citrate 10.0 g

[0038] 65g microcrystalline cellulose

[0039] Low-substituted hydroxypropyl cellulose 5g

[0040] Micronized silica gel 2g

[0041] Magnesium stearate 1 g

[0042] 2 grams protein sugar

[0043] Starch 15g

[0044] Drug C: Limoraban Citrate 20.0g

[0045] Microcrystalline Cellulose 55g

[0046] Low-substituted hydroxypropyl cellulose 5g

[0047] Micronized silica gel 2g

[0048] Magnesium stearate 1 g

[...

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PUM

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Abstract

The invention relates to an oral rapidl disintegrating tablet medicament and a process for preparation, which is constituted by organic acid salt of liimola class mixture of a pattern (I) structure which is used as available medicament composition and findings components, wherein the weight ratio of the available medicament composition is 5 to 20%, and the others are findings components. The oral rapidl disintegrating tablet medicament is put into an oral cavity without needing drinking, which can be collapsed in 25 seconds, and no foreign matter and gritty feelings can be felt when the medicament is put into the oral cavity, and the oral rapidl disintegrating tablet medicament gets into a stomach through natural swallowing action, which is convenient for patients whose swallowing is difficult and who have no water and are inconvenient to drink water. The oral rapid disintegrating tablet medicament is collapsed to be turbid liquor in an oral cavity, and the turbid liquor takes a highly decentralized state, and the medicament is quickly dissolved out, which is beneficial for gastric mucosa to absorb, digestion time of the medicament is shortened as the medicament is convenient to be given, which is beneficial for the medicament to rapidly take effect. The medicament can be economically and conveniently produced in large scale through common apparatus, and medicaments which are gotten can keep excellent appearance and considerable mechanical strength, which has excellent abradability.

Description

technical field [0001] The invention relates to an orally rapidly disintegrating tablet medicament and a preparation method thereof, in particular to an orally rapidly disintegrating tablet medicament with an organic acid salt of a rimoraban compound as an effective pharmaceutical ingredient and a preparation method thereof. Background technique [0002] The organic acid salt of the rimonabant compound with the structure of formula (I) is an active ingredient of a new weight-loss drug, and is a selective type 1 cannabinoid receptor antagonist. [0003] [0004] The drug acts on the body's endogenous cannabinoid system, which is involved in the regulation of body weight and metabolism. Preliminary test results have shown that it can not only reduce body weight and narrow waist circumference, but also reduce body mass index (BMI) greater than 27kg / m 2 Obese people can also improve blood lipid status. At the same time, the number of patients with metabolic syndrome in the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/415A61P3/04
Inventor 雍智全韩为跃闻亚磊谭培何凯张仁怀林吉侃
Owner DONGGUAN TAILI BIOTECH
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