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Water-insoluble medicine sustained-release pellet, sustained-release orally disintegrating tablet thereof and preparation method thereof

A technology of orally disintegrating tablets and sustained-release pellets, applied in the field of sustained-release pellets, can solve the problems of inability to achieve long-acting release, short slow release time, incomplete coating, etc., to maintain blood drug concentration, production steps Simple, selective effects

Inactive Publication Date: 2010-10-20
SHANGHAI INST OF PHARMA IND +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] The slow release time of the existing sustained-release preparations of water-insoluble drugs is short, and long-acting release cannot be achieved, and the longest is only 6 hours
For example, ibuprofen sustained-release and fast-disintegrating tablets use phospholipids as blockers and Kollicoat SR 30D as coating material. The slow-release and fast-disintegrating tablets are prepared by granulation and coating process, but due to the limitation of granulation process, the coating is not complete. So that the slow release time is only 1.5 hours (Fast dispersible / slow releasing ibuprofen tablets.Adamo Fini, Valentina Bergamante, Gian Carlo Ceschel, A.Fini et al. / European Journal of Pharmaceutics and Biopharmaceutics 69(2008)335-341)
And the medicine that releases medicine slowly in the body reaches more than 8 hours, can keep stable blood drug concentration, reduce side effect, and can reduce the frequency of taking, greatly facilitates the taking of medicine, especially brings convenience for the crowd of taking medicine for a long time, but has not been can achieve

Method used

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  • Water-insoluble medicine sustained-release pellet, sustained-release orally disintegrating tablet thereof and preparation method thereof
  • Water-insoluble medicine sustained-release pellet, sustained-release orally disintegrating tablet thereof and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1 prepares acetaminophen sustained-release pellets

[0031] 1. pill heart medicine

[0032] Add 17g of polyvinylpyrrolidone PVP S630 and 100g of paracetamol to 560ml of 75% (v / v) ethanol to make a medicinal solution, wherein the concentration of paracetamol is 15g / 100ml, and the concentration of binder PVPS630 is 2.5% (wt) . Put the sucrose ball core with an average particle size of 0.15 mm in a fluidized bed for 10 minutes, and slowly spray the drug solution on the surface of the ball core. Weight gain after taking medicine: 45.0-50.0%. The operating conditions of the tangential jet fluidized bed are: the fan frequency is 20-23Hz; the material temperature is 33-35°C; the rotation frequency of the turntable is 100-150rpm; the atomization pressure of the atomizing spray gun is 0.10-0.15MPa; The liquid spray speed is 12~15g / min.

[0033] 2. Package isolation layer

[0034] Dissolve 15 g of hydroxypropyl methylcellulose (HPMC) in 300 ml of pure water, and s...

Embodiment 2

[0037] Example 2 Preparation of acetaminophen sustained-release pellets orally disintegrating tablets

[0038] Tablet preparation orally disintegrating tablet, one piece (mg)

[0039] Acetaminophen extended-release pellets 225

[0040] Mannitol 178

[0041] Microcrystalline Cellulose 87

[0042] Cross-linked polyvinylpyrrolidone 22

[0043] Hypromellose 11

[0044] aspartame 2

[0045] Magnesium Stearate 1

[0046] Microsilica 1

[0047] Talc 15

[0048] The preparation method is as follows:

[0049] Pass the acetaminophen sustained-release pellets obtained in Example 1 through a 60-mesh sieve, and the auxiliary materials that can be directly compressed: mannitol, microcrystalline cellulose, cross-linked polyvinylpyrrolidone, hydroxypropyl cellulose, magnesium stearate , talcum powder, micro-silica gel and aspartame are directly compressed with a tablet machine, and the hardness of the tablet is 3kg.

[0050] Get this sustained-release pellet orally disintegrating ta...

Embodiment 3

[0051] Embodiment 3 prepares diclofenac sodium sustained-release pellets

[0052] 1. Pills and medicines

[0053] Add 17g of polyvinylpyrrolidone PVP VA64 and 100g of diclofenac sodium to 560ml of 75% (v / v) ethanol, wherein the concentration of diclofenac sodium: 15g / 100ml, the concentration of binder: 2.5% (wt). Put the sucrose ball core with an average particle size of 0.10 mm in a fluidized bed for 10 minutes, and slowly spray the above-mentioned medicinal solution on the surface of the core. Weight gain after taking medicine: 45.0-50.0%. The operating conditions of the tangential jet fluidized bed are: the fan frequency is 20-23Hz; the material temperature is 33-35°C; the rotation frequency of the turntable is 100-150rpm; the atomization pressure of the atomizing spray gun is 0.10-0.15MPa; The liquid spray speed is 12~15g / min.

[0054] 2. Package isolation layer

[0055] Dissolve 13 g of hydroxypropyl methylcellulose in 300 ml of pure water, and slowly spray it on the ...

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Abstract

The invention discloses a water-insoluble medicine sustained-release pellet, a sustained-release orally disintegrating tablet thereof and a preparation method thereof. The water-insoluble medicine sustained-release pellet comprises a hollow pellet core, a medicine layer, an insulation layer and a sustained-release layer, wherein the sustained-release layer comprises the following ingredients: 54 to 88 percent of sustained-release materials, 2 to 30 percent of antitackiness agents and 1 to 30 percent of pore-foaming agents, wherein the percentage is the mass percentage in the sustained-release layer, wherein the sustained-release materials are one kind or several kinds of materials selected from ethyl acrylate and methyl methacrylate copolymers, polyvinyl acetate and ethyl cellulose. Through regulating the coating combinations and filling auxiliary materials to be pressed into orally disintegrating tablets, the medicine can be slowly released for more than 8 to 13 hours, so the stable blood medicine concentration can be maintained, the side effect is reduced, the medicine taking times can be reduced, and the medicine taking is convenient. The invention conforms to zero-grade release, has the advantages of high final accumulated medicine release amount, high efficacy, strong selectivity, good mouth feeling, simple production steps and high efficiency, and can be applied to large-scale production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a water-insoluble sustained-release pellet, its sustained-release orally disintegrating tablet and a preparation method thereof. Background technique [0002] The existing sustained-release preparations of water-insoluble drugs have a short slow-release time and cannot achieve long-acting release, the longest being only 6 hours. For example, ibuprofen sustained-release and fast-disintegrating tablets use phospholipids as blockers and Kollicoat SR 30D as coating material. The slow-release and fast-disintegrating tablets are prepared by granulation and coating process, but due to the limitation of granulation process, the coating is not complete. The sustained release time is only 1.5 hours (Fast dispersible / slow releasing ibuprofen tablets. Adamo Fini, Valentina Bergamante, Gian Carlo Ceschel, A. Fini et al. / European Journal of Pharmaceutics and Biopharmaceutics 69 (2008...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/22A61K47/32A61K47/34A61K47/38A61K31/167A61K31/196A61K31/192A61K31/549A61P29/00A61K47/10A61K47/14A61K47/26
Inventor 任麒孙冠男李杰吴梦菲任瑶刘丽媛
Owner SHANGHAI INST OF PHARMA IND
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