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Oral disintegrating tablets of microcrystallites of aripiprazole composition and preparation method thereof

A technology of orally disintegrating tablets and aripiprazole, which is applied in the field of orally disintegrating tablets containing aripiprazole composition microcrystals and its preparation, can solve the problems that cannot reflect the advantages of fast dissolution of orally disintegrating tablets, Achieve the effect of good taste, convenient taking, and improved taste

Inactive Publication Date: 2011-10-19
QILU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The aripiprazole orally disintegrating tablet involved in this invention uses a large amount of microcrystalline cellulose and micropowder silica gel, and the use of insoluble excipients causes discomfort in the oral cavity after disintegration; at the same time, because aripiprazole is insoluble Drug, the dissolution rate of the orally disintegrating tablet obtained in CN1709256A is lower than that of the original drug aripiprazole ordinary tablet (trade name: Anlufan), which cannot reflect the advantage of fast dissolution of the orally disintegrating tablet

Method used

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  • Oral disintegrating tablets of microcrystallites of aripiprazole composition and preparation method thereof
  • Oral disintegrating tablets of microcrystallites of aripiprazole composition and preparation method thereof
  • Oral disintegrating tablets of microcrystallites of aripiprazole composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1. The orally disintegrating tablet of microcrystalline aripiprazole composition consists of:

[0053] Aripiprazole composition microcrystalline (2.5 parts of aripiprazole + 5 parts of lactose) 7.5 parts

[0054] 15 parts lactose (filler)

[0055] Mannitol 59.4 parts (filler)

[0056] Optimized microcrystalline cellulose 10 parts (filler)

[0057]6 parts of crospovidone (disintegrant)

[0058] Sweet orange essence 0.5 parts (flavoring agent)

[0059] 0.6 parts of aspartame (flavoring agent)

[0060] 1.0 parts of magnesium stearate (lubricant);

[0061] Preparation:

[0062] Mix the microcrystalline aripiprazole composition with lactose passed through a 40-mesh sieve to prepare mixture A; mannitol, optimized microcrystalline cellulose, crospovidone, sweet orange essence, and aspartame were passed through a 40-mesh sieve respectively After sieving, mix uniformly to obtain mixture B, mix mixture A and mixture B uniformly in equal increments, add magnesium st...

Embodiment 2

[0063] Example 2. The orally disintegrating tablet of microcrystalline aripiprazole composition consists of:

[0064] Microcrystalline Aripiprazole Composition

[0065] (5 parts of aripiprazole + 5 parts of lactose) 10 parts

[0066] Mannitol 72.9 parts (filler)

[0067] 5 parts microcrystalline cellulose (filler)

[0068] Low-substituted hydroxypropyl cellulose 6 parts (disintegrant)

[0069] 3 parts of croscarmellose sodium (disintegrant)

[0070] Micropowder silica gel 0.5 part (lubricant)

[0071] Strawberry essence 0.5 parts (flavoring agent)

[0072] 0.6 parts of aspartame (flavoring agent)

[0073] 1.5 parts of magnesium stearate (lubricant);

[0074] Preparation:

[0075] Mix the microcrystalline aripiprazole composition with mannitol passing through a 40-mesh sieve to prepare mixture A; microcrystalline cellulose, low-substituted hydroxypropyl cellulose, croscarmellose sodium, micropowder silica gel, strawberry essence and aspartame were respectively passed t...

Embodiment 3

[0076] Example 3. Aripiprazole composition The composition of microcrystalline orally disintegrating tablets by mass is:

[0077] Microcrystalline Aripiprazole Composition

[0078] (2 parts of aripiprazole + 2 parts of lactose) 4 parts

[0079] Mannitol 75 parts (filler)

[0080] Optimized microcrystalline cellulose 10 parts (filler)

[0081] 8 parts of crospovidone (disintegrant)

[0082] Sweet orange essence 1.5 parts (flavoring agent)

[0083] Aspartame 0.5 parts (flavoring agent)

[0084] Micropowder silica gel 0.5 part (lubricant)

[0085] 0.5 parts of magnesium stearate (lubricant);

[0086] Preparation:

[0087] Mix the microcrystalline aripiprazole composition with mannitol passing through a 40-mesh sieve to prepare mixture A; optimize microcrystalline cellulose, crospovidone, sweet orange essence, and aspartame after passing through a 40-mesh sieve Mix uniformly to prepare mixture B, mix mixture A and mixture B uniformly by adding equal amounts, add micropowde...

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Abstract

The invention relates to orally disintegrating tablets of microcrystallites of an aripiprazole composition and a preparation method thereof, and the orally disintegrating tablets mainly compose the microcrystallites of the aripiprazole lactose composition, a filling agent, a disintegrating agent, a flavor correction agent and a lubricating agent, wherein the particle size of the microcrystallites of the aripiprazole lactose composition is less than 30 mu m. The preparation method comprises the following steps: uniformly mixing all components of the aripiprazole orally disintegrating tablets and then directly tabletting or performing wet-granulation tabletting. The microcrystallites obtained by common micronization of the aripiprazole lactose composition are higher in dissolution rate in comparison with those by independent micronization of aripiprazole; simultaneously, the crystal form of the aripiprazole in the microcrystallites of the composition is not transformed and the uniformity of content of the orally disintegrating tablets is higher; and the hardness of the aripiprazole orally disintegrating tablets is 5-8kg, the disintegration time limit is less than 30 seconds, not only the tablets can be prevented from breaking during transportation, but also the tablets are convenient to take.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an orally disintegrating tablet containing aripiprazole composition microcrystals and a preparation method thereof. Background technique [0002] Schizophrenia is a severely disabling mental illness. Its symptoms are mainly positive symptoms (such as delusions, hallucinations, thinking disorders, hostility and suspicion) and weird behaviors, negative symptoms (such as slow response, apathy, poor speech, etc.) Cognitive symptoms caused by damage to reasoning ability, and some patients may also have affective symptoms (especially depression). [0003] Aripiprazole is a poorly soluble drug with a solubility of about 7.8g / L in water and its chemical name is 7-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy Base]-3,4-dihydroquinolinone, which is a quinolone derivative, its mechanism of action is not yet clear, but it is currently considered to be through the do...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/496A61K47/26A61K47/38A61P25/18
Inventor 王晶翼李长军王婧璨杨清敏李颖张明会
Owner QILU PHARMA
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