Lysine-ketoprofen and its production

A technology of lysine ketone and lysine, which is applied in the field of amino acid ketoprofen, can solve the problems such as the inability to know the efficacy of arginine ketoprofen ketoprofen, the inability to know the stability, and the like, and achieve increased stability. Sex, improve antipyretic, improve the effect of safety

Inactive Publication Date: 2007-04-04
BEIJING SAISHENG PHARMA
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  • Claims
  • Application Information

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Problems solved by technology

In this patent application, only arginine ketoprofen is compared with 10% gum arabic for pharmacodynamics, and it is proved that it has analgesic and anti-inflammat...

Method used

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  • Lysine-ketoprofen and its production
  • Lysine-ketoprofen and its production

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] First add 73.06 grams (0.4mol) of L-lysine and 1000ml of distilled water in the reaction vessel, then add 101.7g (0.4mol) of racemic ketoprofen after dissolving, stir until the solution is clear, freeze-dry to obtain 171.2 grams of white Block or powder is ketoprofen lysine, the yield is 98.0%, and the purity is 99.2%.

[0029] The freeze-drying conditions are: 20℃~-45℃, pre-freezing for 2.5 hours; -45℃~-40℃, sublimation for 3 hours; -40℃~0℃, sublimation for 8 hours; 0℃~30℃, drying for 8 hours; 30℃~35℃, dry for 2.5 hours; vacuum is less than 0.2Mbar, control the maximum product temperature not to exceed 35℃, and the shelf temperature not to exceed 40℃.

[0030] Pharmacodynamic test of lysine ketoprofen

Embodiment 2

[0031] [Example 2] Antipyretic test

[0032] Take 50 ground rabbits weighing 1.6-2.0 kg, half male and half male, and divide them into random groups, 10 rabbits in each group, and administer them by intragastric administration (ig). Negative control group (normal saline 1ml / kg), positive control group (ketoprofen 20mg / kg)), lysine ketoprofen low dose group (3.0mg / kg)), middle dose group (20mg / kg)) , high dose group (80mg / kg)). After measuring the normal body temperature of the rabbit, intravenous injection of inactivated Escherichia coli liquid (about 1106 / kg bacteria, calculated by turbidimetric method) caused fever. After 3 to 4 hours, body temperature was measured as a fever indicator. When the body temperature rose above 1°C, the rabbits in each group were given ig respectively according to the above dosage. Body temperature was measured at 1, 1.5, 2, and 2.5 hours after administration. The degree of body temperature drop at each time point after administration was use...

Embodiment 3

[0035] [Example 3] Analgesic test - hot plate method

[0036] Fifty female mice weighing 19-21 g were taken and divided into random groups, 10 in each group. Divided into 10% gum arabic group (blank group), ketoprofen group (30mg / kg), lysine ketoprofen was divided into 10mg / kg group, 30mg / kg group, 80mg / kg group, ig administration. Adjust the constant temperature water bath hot plate to 55±0.5°C, place the mouse on the hot plate, measure once every 5 minutes, and calculate the average value for 2 consecutive times. The normal pain response latency of each mouse was tested, and the mice licked their hind feet and kicked their legs as pain response indicators. The pain response latency was measured again at 0.5, 1, 1.5, 2, 2.5 hours after ig administration. Those who exceed 60s are counted as 60s.

[0037] The results are shown in Table 2. The results showed that, compared with the blank group, the lysine ketoprofen group had significant differences in the pain thresholds of...

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Abstract

A lysine ketoprofen with antipyretic, analgesia and anti-inflammatory functions and its production are disclosed. The process is carried out by proportioning lysine with ketoprofen in 1:1mol to obtain the final product. Its advantages include higher pharmacodynamic strength, better solubility, safety and stability and low side effect.

Description

technical field [0001] The invention relates to an amino acid ketoprofen, in particular to a lysine ketoprofen and a preparation method thereof. [0002] The present invention also relates to pharmaceutical compositions comprising lysine ketoprofen. Background technique [0003] Ketoprofen and its chiral enantiomers are a class of 2-aryl propionic acid non-steroidal anti-inflammatory drugs, the main mechanism of action is reversible inhibition of cyclooxygenase and lipoxygenase, thereby inhibiting the Biosynthesis of alkenes, exert antipyretic, analgesic and anti-inflammatory effects and central analgesic effect. It is mainly used clinically to treat various arthritis, postoperative pain and chronic cancer pain, etc., and its curative effect is better than that of ibuprofen. [0004] Ketoprofen is an organic acid drug, insoluble in water, with a half-life of only 1.6 to 1.9 hours in the body. After gastrointestinal administration, it is mainly distributed in the stomach, s...

Claims

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Application Information

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IPC IPC(8): C07C229/26C07C227/14A61K31/198A61P29/00
Inventor 马骉孔双泉姜桂荣宋梦薇张宁
Owner BEIJING SAISHENG PHARMA
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