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Arginine ibuprofen composition for injection

A technology of arginine ibuprofen and composition, applied in the direction of drug combination, medical preparations containing active ingredients, organic active ingredients, etc., can solve the problem of low absolute bioavailability, short maintenance time in vivo, and strong first-pass effect and other problems, to achieve good synergy, reduce the first-pass effect, and improve the effect of treatment

Inactive Publication Date: 2013-09-18
HAINAN WEI KANG PHARMA QIANSHAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although MT has a variety of physiological functions and pharmacological effects, it has unstable oral absorption kinetics, rapid distribution and clearance, and t 1 / 2 Short (30-50min), large individual differences, strong first-pass effect, low absolute bioavailability (1%-37%), and short maintenance time in vivo (1-3h)

Method used

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  • Arginine ibuprofen composition for injection
  • Arginine ibuprofen composition for injection
  • Arginine ibuprofen composition for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1, the preparation of the freeze-dried powder injection of arginine ibuprofen composition for injection, in 1000 pieces.

[0021] prescription

[0022]

[0023]

[0024] 2. Preparation process

[0025] a) Add 70g of mannitol to 1500ml of water for injection, stir and add 30g of arginine ibuprofen to dissolve, then add 0.6g of melatonin and stir evenly;

[0026] b) Add 1.8g of melatonin and 16.59g of medium-substituted hydroxypropyl-β-cyclodextrin into 500ml of water for injection, stir at 50°C for 6 hours, and detect that the encapsulation rate of melatonin is greater than 90%;

[0027] c) After mixing the solutions of groups a and b above, add HCL solution to adjust the pH value to 6.7, add 0.1% activated carbon and stir for 30 minutes to filter out the activated carbon, and then filter the liquid through 0.45 μm and 0.22 μm microporous membranes to detect the content of intermediates , according to arginine ibuprofen, 30mg per bottle;

[0028] d) F...

Embodiment 2

[0029] Embodiment 2, the preparation of the freeze-dried powder injection of arginine ibuprofen composition for injection, in 1000 pieces.

[0030] 1. Prescription

[0031]

[0032] 2. Preparation process

[0033] a) Add 70g of mannitol to 1500ml of water for injection, stir and add 30g of arginine ibuprofen to dissolve, then add 1g of melatonin and stir evenly;

[0034] b) Add 3g of melatonin and 21.38g of medium-substituted hydroxypropyl-β-cyclodextrin into 500ml of water for injection, stir at 50°C for 6 hours, and detect that the encapsulation rate of melatonin is greater than 90%;

[0035] c) After mixing the solutions of groups a and b above, add HCL solution to adjust the pH value to 6.7, add 0.1% activated carbon and stir for 30 minutes to filter out the activated carbon, and then filter the liquid through 0.45 μm and 0.22 μm microporous membranes to detect the content of intermediates , according to arginine ibuprofen, 30mg per bottle;

[0036] d) Fill according...

Embodiment 3

[0037] Embodiment 3, the preparation of the freeze-dried powder injection of arginine ibuprofen composition for injection, in 1000 pieces.

[0038] 1. Prescription

[0039]

[0040] 2. Preparation process

[0041] a) Add 70g of mannitol to 1500ml of water for injection, stir and add 30g of arginine ibuprofen to dissolve, then add 1.3g of melatonin and stir evenly;

[0042] b) Add 3.9g of melatonin and 16.92g of moderately substituted hydroxypropyl-β-cyclodextrin into 500ml of water for injection, stir at 50°C for 5 hours, and detect that the encapsulation rate of melatonin is greater than 90%;

[0043] c) After mixing the solutions of groups a and b above, add HCL solution to adjust the pH value to 6.7, add 0.1% activated carbon and stir for 30 minutes, filter out the activated carbon, and filter the liquid through 0.45 μm and 0.22 μm microporous membranes to detect intermediates Content, according to arginine ibuprofen, 30mg per bottle;

[0044] d) Fill according to the...

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Abstract

The invention provides an arginine ibuprofen composition for injection, and relates to the technical field of medicine manufacturing. The main medicine of the composition comprises arginine ibuprofen and melatonin, wherein the melatonin comprises a quick release part and a cyclodextrin-included slow release part. According to the arginine ibuprofen composition for injection provided by the invention, the therapeutic effect of the arginine ibuprofen is improved, instability caused by oral administration of MT (Melatonin) is avoided and MT is quick to distribute and eliminate and the like, and the first pass effect of MT is reduced. The dosage of MT is reduced. The design of dosage combining quick release and slow release is in accordance with secretion characteristic of MT, so that the problem of half-life period of MT is solved and the bioavailability of a product is improved. Melatonin combined with arginine ibuprofen has a good synergistic effect for treating arthritis.

Description

Technical field: [0001] The present invention relates to the technical field of medicine and medicine manufacture, in particular to a composition of arginine ibuprofen for injection, more specifically, to a freeze-dried composition for injection containing ibuprofen arginine and melatonin . Background technique: [0002] The chemical name of arginine ibuprofen is: trans-4-[(2-amino 3,5-dibromobenzyl) amino] cyclohexanol, molecular formula: C19H32O4N4 molecular weight 380.47. Its structural formula is as follows: [0003] [0004] Ibuprofen arginine (ibuprofen) is a nonsteroidal anti-inflammatory drug (NSAID). Like other 2-aryl propionate derivatives, there is a chiral center at the α position of the propionate group, so ibuprofen has two enantiomers, and it will have physiological and metabolic effects. produce different effects. The fact is that (S)-(+)-ibuprofen (i.e. Dexibuprofen) has significant activity no matter in laboratory testing or clinical trials. The ibup...

Claims

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Application Information

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IPC IPC(8): A61K31/4045A61K9/19A61P29/00A61P19/02A61K31/192
Inventor 汪六一汪金灿郝结兵李彪吴函峰
Owner HAINAN WEI KANG PHARMA QIANSHAN
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