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Quetiapine fumarate film-controlled slow-release pellet capsule

A technology of quetiapine fumarate and sustained-release pellets, which can be used in medical preparations with non-active ingredients, organic active ingredients, nervous system diseases, etc., and can solve problems such as decreased release

Inactive Publication Date: 2013-07-24
内蒙古天衡医院管理有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In order to solve the problem of release decline caused by film aging of quetiapine fumarate film-controlled sustained-release pellets prepared by aqueous dispersion coating, the present invention provides a quetiapine fumarate that can maintain stable release performance throughout the validity period. Membrane-controlled quetiapine fumarate sustained-release pellets and capsules are characterized in that the core of the pellets contains low-substituted hydroxypropyl cellulose with high water-swellability, and the sustained-release coating film is deformed by water swelling. thereby counteracting the aging of the membrane

Method used

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  • Quetiapine fumarate film-controlled slow-release pellet capsule
  • Quetiapine fumarate film-controlled slow-release pellet capsule
  • Quetiapine fumarate film-controlled slow-release pellet capsule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] The quetiapine fumarate sustained-release pellet capsule of embodiment 1 common ball core

[0030] 1. Prescription

[0031] 1. Pill core prescription (1000 capsules)

[0032]

[0033] * Calculated as quetiapine is 200g.

[0034] 2. Prescription of sustained-release film coating solution

[0035]

[0036] 3. No. 00 stomach-soluble gelatin capsule shell 1000 capsules

[0037] Second, the preparation process:

[0038] 1. Ball core preparation process:

[0039] (1) quetiapine fumarate is passed through a 60 mesh sieve;

[0040] (2) Take by weighing quetiapine fumarate, microcrystalline cellulose PH101, lactose of recipe quantity, put in the wet granulator and mix uniformly;

[0041] (3) soft material made of 2% sodium carboxymethyl cellulose aqueous solution;

[0042] (4) Extrude on the extruder, the screen aperture is 1.0mm, and the extrusion speed is 20-30rpm;

[0043] (5) spheronization, the spheronization speed is 900~1000rpm, drying in the fluidized bed;

...

Embodiment 2

[0071] Embodiment 2 quetiapine fumarate sustained-release pellet capsule containing 10% low-substituted hydroxypropyl cellulose

[0072] 1. Prescription

[0073] 1. Pill core prescription (1000 capsules)

[0074]

[0075]

[0076] 2. Prescription of sustained-release film coating solution: same as in Example 1

[0077] 3. No. 00 stomach-soluble gelatin capsule shell 1000 capsules

[0078] Second, the preparation process:

[0079] 1. Ball core preparation process:

[0080] (1) quetiapine fumarate is passed through a 60 mesh sieve;

[0081] (2) Take by weighing quetiapine fumarate, microcrystalline cellulose PH101, lactose, low-substituted hydroxypropyl cellulose of prescription quantity, put in wet granulator and mix evenly;

[0082] (3) soft material made of 2% sodium carboxymethyl cellulose aqueous solution;

[0083] (4) Extrude on the extruder, the screen aperture is 1.0mm, and the extrusion speed is 20-30rpm;

[0084] (5) spheronization, the spheronization spee...

Embodiment 3

[0103] Example 3 Quetiapine Fumarate Sustained-release Pellet Capsules Containing 20% ​​Low-Substituted Hyprolose

[0104] 1. Prescription

[0105] 1. Pill core prescription (1000 capsules)

[0106]

[0107] 2. Prescription of sustained-release film coating solution: same as in Example 1

[0108] 3. No. 00 stomach-soluble gelatin capsule shell 1000 capsules

[0109] Second, the preparation process:

[0110] 1. Ball core preparation process: the same as in Example 2

[0111] 2. Preparation process of sustained-release film coating solution:

[0112] Same as Example 1

[0113] 3. Coating (sustained release film):

[0114] The ball core is placed in a fluidized bed for coating, and the weight gain of the coating film is controlled, and the weight gain of the coating is 23.5% and 26.7%.

[0115] 4, heat treatment: with embodiment 1

[0116] 5. Fill capsules

[0117] The coated pellets are filled into capsules to obtain the quetiapine fumarate sustained-release pellets an...

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Abstract

The invention relates to a quetiapine fumarate film-controlled slow-release pellet capsule. A slow-release film of the quetiapine fumarate film-controlled slow-release pellet utilizes Eurdragit RL 30D as a film-formation material. A pellet core of the quetiapine fumarate film-controlled slow-release pellet contains low-substituted hydroxypropyl cellulose having high expansibility, and also contains a pharmaceutically-acceptable common excipient for the slow-release pellet, wherein preferably, the excipient comprises microcrystalline cellulose, and the pellet core comprises 10 to 40wt% of the low-substituted hydroxypropyl cellulose. The slow-release film comprises Eurdragit RL 30D, triethyl citrate as a plasticizer and talcum powder as an antiplastering aid, wherein preferably, a ratio of Eurdragit RS 30D to triethyl citrate to talcum powder is 30: 3: 4 and a film weight increasing ratio is in a range of 19 to 35%. The quetiapine fumarate film-controlled slow-release pellet comprises the pellet core containing low-substituted hydroxypropyl cellulose having high water expansibility and thus after absorbing water, the quetiapine fumarate film-controlled slow-release pellet expands so that the slow-release film is stretched; the thickness of the slow-release film is reduced; the water-permeable micropore size is increased; and permeability is improved and the permeability reduction caused by film aging is counteracted. Therefore, in middle and later stages, the quetiapine fumarate film-controlled slow-release pellet release rate is basically constant; in the last stage, residues are less; and stable release performances can be kept in the period of validity.

Description

technical field [0001] The invention relates to a quetiapine fumarate film-controlled sustained-release pellet capsule, in particular to a quetiapine fumarate film-controlled sustained-release pellet capsule containing low-substituted hydroxypropyl cellulose in the pellet core, It belongs to the field of pharmaceutical preparations. Background technique [0002] Quetiapine fumarate is an atypical antipsychotic drug, which produces anti-schizophrenia effect by antagonizing multiple neurotransmitter receptors, and is used for the treatment of manic episodes in schizophrenia and bipolar disorder. [0003] Quetiapine fumarate is almost insoluble in water, and the earliest common preparation on the market needs to be taken twice a day, the blood concentration fluctuates greatly, the peak concentration is too high, and the adverse reactions are serious. [0004] Quetiapine Fumarate Sustained-release Tablets (trade name: Seroquel) listed by AstraZeneca is a matrix-type sustained-r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/554A61K47/38A61P25/18
Inventor 姜庆伟狄媛吕玉珠唐亚坤刘俊轶
Owner 内蒙古天衡医院管理有限公司
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