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Nimesulide temperature sensitive hydrogel and preparation method thereof

A gel and water-phase technology, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, non-central analgesics, etc., can solve problems such as leakage, foreign body sensation, and inability to adjust dosage, and achieve stable and easy-to-control quality, The effect of increasing the absorption area and shortening the onset time

Inactive Publication Date: 2011-05-25
LOGISTICS UNIV OF CAPF
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, ordinary suppositories are mostly semi-solid, which will cause obvious foreign body sensation and a certain degree of leakage when used, and the dosage cannot be adjusted

Method used

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  • Nimesulide temperature sensitive hydrogel and preparation method thereof
  • Nimesulide temperature sensitive hydrogel and preparation method thereof
  • Nimesulide temperature sensitive hydrogel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1: Mix Poloxamer 407, Poloxamer 188, and 5% (w / w / ) NaOH evenly, then add nimesulide powder, and finally add distilled water to the full amount, and stir evenly.

Embodiment 2

[0039] Example 2: Pass nimesulide through a 200-mesh sieve, mix it with Poloxamer 188 and 5% (w / w / ) NaOH, stir evenly, add Poloxamer 407 particles, and continue stirring until the solution is uniform .

Embodiment 3

[0040] Example 3: Nimesulide was passed through a 200 mesh sieve, mixed with Poloxamer 188 and 5% (w / w / ) NaOH, stirred evenly and then added into the concentrated solution of Poloxamer 407, and continued to stir until the solution was dissolved uniform.

[0041] Table 1

[0042]

Exterior

phase transition temperature

Example 1

homogeneous solution

34±0.79℃

Example 2

homogeneous solution

34±0.79℃

Example 3

homogeneous solution

34±0.79℃

[0043] The influence of different components of embodiment 4~10 on phase transition temperature

[0044] The phase transition temperature measurement method is the same as in Examples 1-3. The preparation method is the same as in Example 3.

[0045] Table 2

[0046]

[0047] Examples 11-16 The influence of other ingredients on gel properties

[0048] The phase transition temperature measurement method is the same as in Examples 1-3. The preparation method is th...

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PUM

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Abstract

The invention provides Nimesulide temperature sensitive gel and a preparation method thereof. The Nimesulide temperature sensitive gel comprises Nimesulide, a temperature sensitive gel material, a pH regulator, a preservative and the like and is characterized in that: the temperature sensitive gel material is poloxamer, and the weight ratio of the poloxamer to the Nimesulide is 9:1; and the optimized temperature sensitive gel material is poloxamer 407. The temperature sensitive gel is sensitive to temperature changes, and rabbit rectum experimental results show that the temperature sensitive gel has higher medicament release rate and higher bioavailability which are obviously better than those of the conventional Nimesulide common suppositories. The Nimesulide temperature sensitive gel reserves the advantages of the conventional suppositories, overcomes the defects of the conventional suppositories to a certain extent and has a wide clinical application prospect. The Nimesulide temperature sensitive gel uses common safe pharmaceutical excipients, has a simple production process, stable and easily-controlled quality and high process reproducibility, and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a nimesulide temperature-sensitive hydrogel and a preparation method thereof. Background technique [0002] Nimesulide (NIM) is a new third-generation non-steroidal anti-inflammatory drug, administered orally or rectally, twice a day, for the treatment of various inflammations and pains. The results of clinical research show that nimesulide can effectively relieve the pain caused by diseases such as arthritis, cancer, embolism, oral surgery, and dysmenorrhea, and can relieve the pain caused by adults or children during surgical operations, as well as adults or children suffering from respiratory tract infection, nasal Pain, fever and inflammation caused by pharyngeal diseases and trauma. Nimesulide has a better curative effect than other NSAIDs, and its gastrointestinal side effects are less than similar drugs. Oral administration is easy to absorb, the plasma protein b...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/18A61K47/34A61K47/36A61K47/38A61P29/00A61K47/10
Inventor 张莉袁园刘晓辉陈莉申去非仲博胡霞
Owner LOGISTICS UNIV OF CAPF
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