Oral tablet containing iloperidone, and its preparation method

A technology for oral tablets of iloperidone and iloperidone, which is applied in the field of pharmaceutical preparations and can solve problems such as complex processes

Active Publication Date: 2012-11-21
ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
View PDF6 Cites 6 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The process is relatively complex

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Oral tablet containing iloperidone, and its preparation method
  • Oral tablet containing iloperidone, and its preparation method
  • Oral tablet containing iloperidone, and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

Appropriate amount

[0047] Preparation process: Weigh a certain amount of purified water as a wetting agent; (V，0.9) =9μm iloperidone, lactose, microcrystalline cellulose, hypromellose, and internally added crospovidone were placed in a wet granulator and mixed uniformly to obtain mixture A; an appropriate amount of purified water was added to mixture A to prepare granules to obtain wet granules; the wet granules were sized and dried to obtain dry granules; the dry granules were evenly mixed with crospovidone, silicon dioxide, and magnesium stearate and then pressed into tablets; tablet weight 370mg, compressed into tablets Hardness 3-8kp.

[0048] Measure the iloperidone tablets prepared in Comparative Example 1 of the present invention, Comparative Example 2, Comparative Example 3, Comparative Example 4, Example 1 according to the disintegration time limit inspection method (two appendices of Chinese Pharmacopoeia version in 2010) The disintegration time in water, t...

Embodiment 2

[0057] components

[0058] Preparation process: Weigh a certain amount of purified water as a wetting agent; (V，0.9) = 4.5μm Iloperidone, lactose, microcrystalline cellulose, hypromellose, and internally added crospovidone are placed in a wet granulator and mixed uniformly to obtain mixture A; add an appropriate amount of purified water to mixture A Granulate to obtain wet granules; granulate and dry the wet granules to obtain dry granules; mix the dry granules with external crospovidone, silicon dioxide, and magnesium stearate evenly and then press into tablets; tablet weight 90mg, press Tablet hardness 1-4kp.

Embodiment 3

[0060] components

[0061] Crospovidone (additional)

[0062] Preparation process: Weigh a certain amount of purified water as a wetting agent; (V，0.9) =9μm iloperidone, lactose, microcrystalline cellulose, hypromellose, and internally added crospovidone were placed in a wet granulator and mixed uniformly to obtain mixture A; an appropriate amount of purified water was added to mixture A to prepare granules to obtain wet granules; the wet granules were sized and dried to obtain dry granules; the dry granules were evenly mixed with crospovidone, silicon dioxide, and magnesium stearate and then pressed into tablets; tablet weight 140mg, compressed into tablets Hardness 2-5kp.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
particle diameteraaaaaaaaaa
Login to view more

Abstract

The invention discloses an oral tablet containing iloperidone, and its preparation method. The oral tablet is characterized in that the oral tablet contains iloperidone, hydroxypropyl methylcellulose, lactose, microcrystalline cellulose, a disintegrating agent, a lubricant, and a flow aid, wherein the application amount of the hydroxypropyl methylcellulose is 4.0-6.0%. The iloperidone tablet prepared according to the preparation method in the invention has good in-vitro dissolution to guarantee the iloperidone tablet has a good in-vivo biological utilization degree. Simultaneously the invention also provides the preparation method of the oral tablet, and the preparation method has the advantages of simple technology, low cost, and suitableness for commercial production.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to an iloperidone oral tablet and a preparation method thereof. Background technique [0002] Iloperidone is an antagonist of 5-hydroxytryptamine and dopamine D2 receptors, and is mainly used for the treatment of schizophrenia. Its chemical name is 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy]-3-methoxy Phenyl] ethyl ketone, the structural formula is as follows: [0003] [0004] CN101822673A and CN101822674A disclose a pharmaceutical composition of iloperidone containing a surfactant. The surfactant in the composition is selected from sodium lauryl sulfate and sodium dodecyl sulfate. Although the use of surfactants can increase the solubility of the drug, thereby promoting the dissolution of the drug, common surfactants such as sodium lauryl sulfate have certain toxicity and irritation, and can produce acute toxic reactions on the skin...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/454A61K47/38A61P25/18
Inventor 屠后为舒佳妮胡李斌施祥杰彭俊清陈浩李巧霞胡功允
Owner ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap