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Lenalidomide gastric retention sustained release tablet and preparation method thereof

A technology for lenalidomide and sustained-release tablets, which is applied in the field of lenalidomide gastroretentive sustained-release tablets and the preparation thereof, can solve the problems of unfavorable formulation stability, unfavorable production, poor stability and the like, and achieves high drug bioavailability , Small side effects, high compliance effect

Active Publication Date: 2018-09-11
AC PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Commonly used bleaching aids include stearyl alcohol, stearic acid, glyceryl monostearate, glyceryl behenate, carnauba wax, white wax, hydrogenated vegetable oil, etc. These substances have poor stability, low melting point, and are not It is beneficial to the stability of the preparation and is not conducive to production
Commonly used foaming agents are alkaline carbonates or bicarbonates, which are not suitable for drugs that are unstable to alkalis

Method used

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  • Lenalidomide gastric retention sustained release tablet and preparation method thereof
  • Lenalidomide gastric retention sustained release tablet and preparation method thereof
  • Lenalidomide gastric retention sustained release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049]

[0050] Information on Accelerated Release Agents and Sustained Release Materials:

[0051] product name

[0052] Lenalidomide is crystal form B, and the weight-average molecular weight of hydroxypropylmethylcellulose K200M is about 1,200,000. Tablet preparation method: Weigh the above-mentioned raw and auxiliary materials except magnesium stearate, pass through a 60-mesh sieve, and mix well , plus magnesium stearate, mixed properly and pressed into tablets, tablet hardness 9-10kg / cm 2 , tablet density 0.991g / cm 3 .

[0053] Example 1 Floatability of gastric-floating sustained-release tablets: the tablet floats rapidly after being put into the dissolution vessel, and continues to float in the dissolution medium for at least 24 hours.

[0054] The release measurement result of the lenalidomide gastric retention sustained-release tablet prepared according to Example 1:

[0055] time (h)

[0056] The test results showed that the lenalidomide gast...

Embodiment 2

[0058]

[0059]

[0060] Information on Accelerated Release Agents and Sustained Release Materials:

[0061] product name

[0062] Lenalidomide is crystal form A, and the weight-average molecular weight of hydroxypropyl methylcellulose K250 is about 200,000. Preparation method: Weigh the above-mentioned raw and auxiliary materials except sodium stearyl fumarate, pass through a 60-mesh sieve and mix well , plus sodium stearyl fumarate, mixed properly and pressed into tablets, tablet hardness 3-4kg / cm 2 , tablet density

[0063] 0.755g / cm 3 .

[0064] Example 2 Floatability of gastric-floating sustained-release tablets: the tablet floats rapidly after being put into the dissolution vessel, and continues to float in the dissolution medium for at least 24 hours.

[0065] The release measurement result of the lenalidomide gastric retention sustained-release tablet prepared according to Example 2:

[0066] time (h)

[0067] The test results show that th...

Embodiment 3

[0069]

[0070] Information on Accelerated Release Agents and Sustained Release Materials:

[0071]

[0072]

[0073] Lenalidomide is crystal form II, and the weight-average molecular weight of hydroxypropyl methylcellulose K750 is about 250,000. Preparation method: Weigh the above-mentioned raw and auxiliary materials except talc powder, pass through a 60-mesh sieve and mix evenly, then add talc The powder is properly mixed and pressed into tablets, the hardness of the tablet is 5-6kg / cm 2 , tablet density 0.949g / cm 3 .

[0074] Example 3 Floatability of gastric-floating sustained-release tablets: the tablet floats quickly after being put into the dissolution vessel, and continues to float in the dissolution medium for at least 24 hours.

[0075] The release measurement result of the lenalidomide gastric retention sustained-release tablet prepared according to Example 3:

[0076] time (h)

[0077] The test results showed that the lenalidomide gastric ret...

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Abstract

The invention discloses a lenalidomide gastric retention sustained release tablet and a preparation method thereof. The sustained release tablet comprises 3-14 wt% of lenalidomide, 14-68 wt% of a low-bulk density release promoter, 23-70 wt% of a low-bulk density sustained release material, and the balance of other pharmaceutically acceptable auxiliary materials, wherein the bulk density of the release promoter is 0.24-0.52 g / cm<3>; and the bulk density of the sustained release material is 0.29-0.51 g / cm<3>. The sustained-release tablet is in a floating state in the stomach environment, is notdirectly excluded from the stomach due to gastric emptying, has a gastric retention effect, is not easily discharged with the stomach content, and has high drug bioavailability and small side effects.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a lenalidomide gastric retention sustained-release tablet and a preparation method thereof. Background technique [0002] Lenalidomide is an anti-tumor immunomodulator, which has been widely used clinically in multiple myeloma (MM). It was developed by Celgene and marketed in capsule form. [0003] Commercially available lenalidomide capsules are rapidly absorbed in the gastrointestinal tract after oral administration, the peak blood drug time is 0.5-1.5 hours, and the half-life is about 3 hours. When the dose is 5-50 mg, the maximum plasma concentration (Cmax) and the area under the plasma concentration-time curve (AUC) can increase proportionally with the increase of the dose. However, its blood concentration fluctuates greatly, and its toxic and side effects are obvious, which significantly reduces the number of neutrophils and platelets. Therefore, it is necess...

Claims

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Application Information

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IPC IPC(8): A61K31/454A61K9/22A61K47/38A61P35/00
CPCA61P35/00A61K9/0065A61K9/2054A61K31/454A61K9/2095
Inventor 罗华锋何静瑜谭晓峰赖树挺刘锋
Owner AC PHARMA
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