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Paliperidone derivative low-dose tablet and preparation method thereof

A technology of paliperidone and derivatives, applied in the field of low-dose tablets of paliperidone derivatives, to achieve the effect of reducing adverse reactions and side effects, improving therapeutic effect, and reducing irritation and adverse reactions

Inactive Publication Date: 2013-04-24
长春健欣生物医药科技开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the applicable active ingredient drug loading is only 10mg / g or accounts for 4% of the weight of neutral particles, which cannot meet the requirements for lower drug loading; and because the active ingredient needs to be dissolved in a suitable adhesive coating layer Water or other approved liquids are used as solvents, which limits the range of drugs that can be applied; at the same time, because this method requires a coating process, it needs to be operated in a coating pan or an air fluidized bed, and the operation is more cumbersome , requires the drug to remain stable during the process of spraying the coating solution and drying at high temperature, which further limits the drugs that can be applied

Method used

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  • Paliperidone derivative low-dose tablet and preparation method thereof
  • Paliperidone derivative low-dose tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 N-pentoxy paliperidone tablets with a drug loading of 1.5%

[0032] Prescription: n-pentoxy paliperidone 1.5g, spray-dried lactose monohydrate (Flowlac? 100) 83.5g, hydroxypropylmethylcellulose (HPMC K100LV CR) 15g, magnesium stearate 1g, 500 tablets in total.

[0033] Weigh n-pentyloxy paliperidone, Flowlac? 100, HPMC K100LV CR according to the prescription, and use a three-dimensional mixer to mix for 10 minutes to achieve a uniform mixing state; transfer the material mixture to a small mixer at a speed of 25 rpm, and spray the wetting agent for 70 % ethanol 35-40mL can be used to prepare soft materials in a suitable state; use a wet granulator with a 1.6mm sieve to make wet granules, and the speed is 90rpm, until no particles fall from the sieve, and there is no residual unsifted soft material on the sieve. The granulation is completed; dry in a blast drying oven at 45°C for 30 minutes, and keep stirring during the period, until the material is dry, evenly ...

Embodiment 2

[0035] Example 2 Isobutoxy Paliperidone Tablets with 1.5% Drug Loading

[0036] Prescription: Isobutoxy paliperidone 1.5g, spray-dried lactose monohydrate (SuperTab? 11SD) 83.5g, HPMC K100LV CR 15g, magnesium stearate 1g, 500 tablets in total

[0037] Weigh isobutoxy paliperidone, SuperTab? 11SD, HPMC K100LV CR according to the prescription, and use a three-dimensional mixer to mix for 10 minutes to achieve a uniform mixing state; transfer the material mixture to a small mixer at a speed of 25 rpm, and spray the wetting agent for 70 % ethanol 35-40mL can be used to prepare soft materials in a suitable state; use a wet granulator with a 1.6mm sieve to make wet granules, and the rotation speed is 90rpm, until no particles fall from the sieve, and there is no residual soft material that has not been sieved on the sieve. After the granulation is completed, the time required is about 15 minutes; dry in a blast drying oven at 45°C for 30 minutes, and keep stirring during the period,...

Embodiment 3

[0039] Example 3 Isobutoxy Paliperidone Tablets with 0.75% Drug Loading

[0040] Prescription: 3.75g isobutoxy paliperidone, 421.25g spray-dried lactose monohydrate (SuperTab? 11SD), 75g hypromellose, 5g magnesium stearate, 1000 tablets in total

[0041] Weigh isobutoxy paliperidone, SuperTab? 11SD, and HPMC K100LV CR according to the prescription, and mix them with a three-dimensional mixer for 15 minutes to achieve uniform mixing; transfer the material mixture to a small mixer at a speed of 25 rpm, and spray the wetting agent for 70 % ethanol is about 175-200mL to prepare soft materials in a suitable state; use a wet granulator with a 1.0mm sieve to make wet granules at a speed of 90rpm, until no particles fall from the sieve, and there is no remaining unsifted soft material on the sieve. After the granulation is completed, the granulation time is about 20 minutes; dry in a blast drying oven at 45°C for 40 minutes, and keep stirring during the period, until the material is d...

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Abstract

The invention provides a paliperidone derivative low-dose tablet and a preparation method thereof. The paliperidone derivative low-dose tablet is prepared by using spray drying-lactose monohydrate as the diluent and filler by using a wet granulation method. Active components of extreme micro-quantity (can be as low as 0.375% of the weight of the materials) and other auxiliary materials are kept in very good uniform state in the mixing and wet granule preparation process; the defect that the spray drying-lactose monohydrate is poor in compressibility can be greatly overcome in the wet granulation process, so that the prepared granule is good in flowability and can be applied to direct compression so as to obtain the tablet with good content uniformity, hardness and friability results, and the tablet reveals excellent batch repeatability; and meanwhile the wet granulation method can greatly reduce the dust pollution degree in the whole production process, and reduces the influence to the health of operation personnel.

Description

technical field [0001] The invention provides a low-dose paliperidone derivative tablet and a preparation method thereof, belonging to the technical field of medicine. technical background [0002] The paliperidone derivatives involved in the present invention include two kinds of paliperidone derivatives such as n-pentoxy paliperidone and isobutoxy paliperidone. Compared with paliperidone (trade name Invega?), chemically modified paliperidone derivatives have good bioavailability (more than 50%) and longer biological half-life (6-7h) in vivo. It is necessary to have a low-dose tablet that is stable, uniform and released quickly in the body. [0003] The "low-dose preparation" in the present invention refers to a preparation in which the active ingredient accounts for 1% or less of the tablet weight and 2% or less according to the British Pharmacopoeia according to the requirements of the US FDA. Most of the low-dose preparations currently on the market are tablets, and t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/519A61K47/38A61P25/18
Inventor 李又欣黄晚王晨晖于崆峒孙凤英
Owner 长春健欣生物医药科技开发有限公司
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