Slow-release, controlled-release prepn. contg. chlortenozicam

A technology of lornoxicam and controlled-release preparations, which is applied in the direction of anti-inflammatory agents, non-central analgesics, and medical preparations of non-active ingredients. To avoid the peak and valley phenomenon, reduce the toxic and side effects, and achieve the effect of long-lasting curative effect

Inactive Publication Date: 2007-04-18
何岩
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the common oral preparations of lornoxicam have large fluctuations in blood concentration and unst

Method used

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  • Slow-release, controlled-release prepn. contg. chlortenozicam
  • Slow-release, controlled-release prepn. contg. chlortenozicam
  • Slow-release, controlled-release prepn. contg. chlortenozicam

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1: Preparation of Lornoxicam Tablets

[0036] 1000 pieces

[0037] Lornoxicam 8g

[0038] Poloxamer 40g

[0039] Microcrystalline Cellulose 52g

[0040] Preparation process: Lornoxicam and poloxamer are made into solid dispersion by flux method, crushed through a 100-mesh sieve, added microcrystalline cellulose, mixed evenly, and compressed into tablets.

[0041] Determination of dissolution rate:

[0042] According to the dissolution determination method (Chinese Pharmacopoeia version two appendices X C third method in 2005), the phosphate buffer 250ml with PH=7.4 is the dissolution medium, and the rotating speed is 50 revolutions per minute, operated according to law, respectively in 5 minutes, 10 minutes, At 15 minutes, 20 minutes, 30 minutes, and 45 minutes, 5 ml of samples were taken, and at the same time, dissolution medium of the same temperature and volume was added, the samples were filtered, and the filtrate was taken fo...

Embodiment 2

[0043] Embodiment 2: Preparation of Lornoxicam Sustained-release Tablets

[0044] 1000 pieces

[0045] Lornoxicam 8g

[0046] Poloxamer 32g

[0047] Ethylcellulose (45cps) 10g

[0048] Microcrystalline Cellulose 44g

[0049] Preparation process: Lornoxicam and poloxamer are made into solid dispersion by solvent method, crushed through a 100-mesh sieve, mixed with ethyl cellulose and microcrystalline cellulose, and pressed into tablets. Lornoxicam: ethyl cellulose = 1: 1.25, can effectively sustained release.

[0050] Determination of release rate of sustained-release tablets:

[0051]According to the dissolution assay method (Chinese Pharmacopoeia version two appendix X C third method in 2005), the phosphate buffer 250ml with PH=7.4 is the dissolution medium, and the rotating speed is 50 revolutions per minute, operated according to law, respectively at 1, 2, 4, Take 5ml of the solution at 6, 8, and 12 hours, add the dissolution medium at the sam...

Embodiment 3

[0052] The preparation of embodiment 3 lornoxicam sustained-release tablets

[0053] 1000 pieces

[0054] Lornoxicam 8g

[0055] Poloxamer 32g

[0056] Hypromellose K4M 20g

[0057] Microcrystalline Cellulose 44g

[0058] Preparation process: Lornoxicam and poloxamer are made into solid dispersion by flux method, crushed through a 100-mesh sieve, mixed with ethyl cellulose and microcrystalline cellulose, and pressed into tablets. When lornoxicam:hypromellose=1:1.25, it can be effectively sustained release.

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Abstract

A slow-release or release-controllable lornoxicam with durable antalgic and anti-inflammation effect is disclosed. The povidone, polyethanediol and poloxamer are used to prepare the dispersing substance of lornoxicam or the beta-cyclodextrin or its derivative is used for preparing its inclusion substance. The slow-releasing material is used for controlling its release.

Description

technical field [0001] The invention relates to a non-steroidal anti-inflammatory drug Lornoxicam sustained and controlled release preparation and a preparation method thereof. technical background [0002] Lornoxicam (Lornoxicam) its chemical name is 6-chloro-4-hydroxy-2-methyl-N-2-pyridyl-2H-thiophene-[2,3-e]-1,2-thiazine- 3-Carbonoxalylethylenediamine-1,1-dioxide, molecular formula C 13 h 10 C 2 N 3 o 4 S 2 , the molecular weight is 371.82. Lornoxicam belongs to the non-steroidal anti-inflammatory analgesics, which is a thiazide derivative and has strong analgesic and anti-inflammatory effects. Its mechanism of action includes: (1) inhibiting the synthesis of prostaglandins by inhibiting the activity of cyclooxygenase (COX); however, lornoxicam does not inhibit the activity of 5-lipid oxidase, so it does not inhibit the synthesis of leukotrienes , nor shunt arachidonic acid to the 5-lipid oxidase pathway. (2) Activate the opioid ne...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K9/52A61K31/542A61K47/32A61K47/34A61K47/38A61K47/40A61K47/24A61P29/00A61P25/04A61P19/02A61K47/10
Inventor 何岩
Owner 何岩
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