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Clarified propofol injection and preparation method thereof

A technology of injection and propofol, which is applied in the field of medicine, can solve the problems of long preparation time, high concentration of free propofol, and ineffective pain effect, and can reduce the risk of injection pain, small hemolysis, and The effect of low dosage of excipients

Inactive Publication Date: 2020-05-15
BIKA BIOTECH GUANGZHOU CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] From 1993 to now, more than ten international patents such as PCT / GB / 00737, WO / 2003 / 06324, W / O / 2004 / 108113, WO / 2007 / 052295, WO / 2012 / 104730 and US patents 7138387, 7034013, 9006215, etc. The patent documents of cyclodextrin used to clarify the preparation of propofol injection are disclosed, but these patents have defects such as high cyclodextrin dosage, difficulty in filtration, long preparation time, easy contamination of bacteria, high pH, ​​and difficult storage.
[0005] A clinical study in 2011 showed (Anesthesia & Analgesia 2011; 113:738-41, CrystalB.Wallentine et al.) that when sulfobutyl ether-β-cyclodextrin was applied to propofol injection, the concentration of free propofol was too high , the pain reduction effect is not obvious
So far, no clarified propofol injection with low free propofol concentration has been successfully developed

Method used

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  • Clarified propofol injection and preparation method thereof
  • Clarified propofol injection and preparation method thereof
  • Clarified propofol injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～8

[0067] At room temperature, take the prescribed amount of sulfobutyl ether-β-cyclodextrin and the corresponding prescribed amount of sodium bicarbonate, add 50 mL of water for injection, stir and dissolve, pass nitrogen through the solution to remove dissolved oxygen, and add 1000mg of propofol, stir for 2-6 hours, adjust the pH value to 6-9, add water to 100mL, stir evenly, sterilize by 0.22μm filter, put it into a transparent sterile ampoule bottle, and seal it with sterile nitrogen to exhaust the air. Store at 25°C. Wherein in each embodiment the consumption of raw material and the outward appearance of the injection that obtains and the concentration of free propofol are shown in Table 1.

[0068] figure 1 The magnified figure of the proton nuclear magnetic resonance spectrum of the sample prepared according to Example 2 is listed.

Embodiment 9～10

[0070] Examples 9-10 were prepared with reference to the patents of Cydex Corporation, specifically referring to Examples 1 and 2 of US7034013. figure 2 The magnified figure of the proton nuclear magnetic resonance spectrum of the sample prepared according to Example 9 is listed.

[0071] Wherein in each embodiment the consumption of raw material and the outward appearance of the injection that obtains and the concentration of free propofol are shown in Table 1.

[0072] Table 1

[0073]

[0074]

[0075] From Examples 1 to 10, it can be seen that when sodium bicarbonate is higher than 1% (w / v), the preparation is slightly yellow and has poor stability, and when sodium bicarbonate is lower than 0.01% (w / v), the preparation is milky. Comparing Example 9 and Example 10, increasing the concentration of sulfobutyl ether-β-cyclodextrin cannot significantly reduce the concentration of free propofol.

[0076] In Examples 8-10 that do not contain sodium bicarbonate, when the ...

Embodiment 11

[0078] At room temperature, take 18.0g of sulfobutyl ether-β-cyclodextrin, 100mg of sodium citrate, add 50mL of water for injection, stir and dissolve, pass nitrogen through the solution to exclude dissolved oxygen, and add 1000mg of propofol under nitrogen atmosphere Phenol, stir for 2-6 hours, adjust the pH value to 6-9, add water to 100mL, stir evenly, sterilize by 0.22μm filter, put it into a transparent sterile ampoule, seal it with sterile nitrogen to exhaust the air, and store it at 25°C After storage, the measured free propofol concentration was 37.3 μg / mL.

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Abstract

The invention relates to clarified propofol injection and a preparation method thereof. The injection includes propofol, cyclodextrin, a stabilizing agent, a pH regulating agent and injection water; the pH value of the injection is 6-9, and preferably is 7-8.5. The injection can be filtered online, and is few in ingredient kinds, low in using amount, low in free propofol concentration, convenientin storage and good in stability.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a clarified propofol injection and a preparation method thereof. Background technique [0002] Propofol, as a commonly used clinical intravenous anesthetic, has been widely used for its fast onset, short duration of action, fast metabolism and high safety. Commercially available propofol emulsions include injection emulsions, medium- and long-chain fat emulsions, and long-chain fat emulsion preparations. This type of preparation has defects such as complex ingredients, easy to be contaminated with bacteria, high probability of injection pain, and excipients such as soybean oil and peanut oil that are easy to cause allergies, which have seriously affected the patient's body. Developing a propofol injection that does not use emulsion as an excipient can reduce the risk of medication for patients. [0003] There are many kinds of pharmaceutical excipients in the prior...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K47/40A61K47/02A61K31/05A61P23/00
CPCA61K9/0019A61K9/08A61K47/02A61K31/05A61P23/00A61K47/6951Y02A50/30
Inventor 许英挺
Owner BIKA BIOTECH GUANGZHOU CO LTD
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