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New precursor medicinal preparation

A preparation and liquid medicine technology, which is applied in the field of freeze-dried preparations and preparations of propofol water-soluble precursor compounds, can solve instability and other problems, and achieve long-term stable storage and high safety effects

Active Publication Date: 2010-06-02
YICHANG HUMANWELL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0022] The purpose of the present invention is to solve the problem that the water-soluble precursor compound of propofol is unstable in an aqueous medium, and to provide a kind of propofol water-soluble prodrug (that is, 1-hydroxyl group replace) safe and stable preparations available for clinical use, which overcomes the deficiencies in the prior art

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Example 1 Freeze-dried powder injection of compound of formula I (Z is sodium)

[0058] Prescription: single dose

[0059] Formula I compound (Z is sodium) 0.1g

[0060] Mannitol 0.025g

[0061] Appropriate amount of water for injection

[0062] The preparation method is as follows: weighing according to the formula, dissolving the compound of formula I (Z is sodium) in water for injection, adding mannitol, and stirring until completely dissolved. The amount of activated carbon added is 0.05-1.0% (w / v), stirred for 30 minutes, and filtered. The filtrate is sterilized by filtration through a 0.22um microporous membrane, filled in vials or vials, half-stoppered, placed on the shelf of a freeze dryer, pre-frozen at -30~-50°C for 1 to 4 hours, and then set the temperature Dry once at -10-0°C for 8-24 hours, and continue drying at 20-30°C for 2-12 hours until the moisture reaches the requirement. Vacuum or nitrogen-filled pressure plug is enough, the sample is redissolv...

Embodiment 2

[0063] Example 2 Freeze-dried powder injection of the compound of formula I (Z is sodium) without excipients

[0064] Prescription: single dose

[0065] Formula I compound (Z is sodium) 0.1g

[0066] Appropriate amount of water for injection

[0067] The preparation method is: weighing according to the formula, dissolving the compound of formula I (Z is sodium) in water for injection, and stirring until completely dissolved. The amount of activated carbon added is 0.05-1.0% (w / v), stirred for 30 minutes, and filtered. The filtrate is sterilized by filtration through a 0.22um microporous membrane, filled in vials or vials, half-stoppered, placed on the shelf of a freeze dryer, pre-frozen at -30~-50°C for 1 to 4 hours, and then set the temperature Dry once at -10-0°C for 8-24 hours, and continue drying at 20-30°C for 2-12 hours until the moisture reaches the requirement. Vacuum or nitrogen-filled pressure plug is enough, the sample is redissolved quickly and the solution is ...

Embodiment 3

[0068] Example 3 Compatibility test of compound of formula I (Z is sodium) and common lyophilized excipients

[0069] With reference to the "Technical Guidelines for the Research of Chemical Drug Preparations" and the "Chinese Pharmacopoeia" 2005 edition two appendix stability inspection methods, the phase of the formula I compound (Z is sodium) and the common lyophilized excipients was determined by high performance liquid phase method. Capacitance.

[0070] The following table is the measurement result of formula I compound (Z is sodium) and sodium chloride, mannitol under different conditions

[0071]

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Abstract

The invention discloses a freeze-drying preparation of a water-solubility propofol precursor compound and a preparation method thereof. The freeze-drying preparation of the propofol precursor compound, prepared in the method of the invention, has the advantages of favorable water solubility, stability and safety.

Description

technical field [0001] The invention relates to pharmaceutical preparation technology, in particular to a freeze-dried preparation of a water-soluble precursor compound of propofol and a preparation method thereof. Background technique [0002] Successfully delivering drugs to patients is extremely important for treating diseases, however, many clinically active drugs are limited in application due to their extremely low water solubility. Due to poor water solubility, many drugs are usually formulated in the presence of co-solvents or solubilizers, which brings inconvenience to clinical use. [0003] Propofol (2,6-diisopropylphenol) is a low-molecular-weight phenol derivative, which is used as a hypnotic or sedative, and has been widely used in the induction and maintenance of anesthesia or sedation through intravenous injection. The advantages of its use as an anesthetic include: intravenous administration, rapid onset and elimination of anesthesia, and fewer side effects ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/05A61P23/00A61P25/20
Inventor 李莉娥李杰陈顺符义刚
Owner YICHANG HUMANWELL PHARMA
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