Stable phenyl acetic acid ester medicinal fat emulsion

Abstract

The invention provides stable phenyl acetic acid ester medicinal fat emulsion which is a short-acting hypnagogue used for anesthesia and sedation. The stable phenyl acetic acid ester medicinal fat emulsion contains the following components in percentage by weight and volume: 1.0-10.0% of a phenyl acetic acid ester medicine shown in a formula (I), 10.0-30.0% of oil for injection, 0.4-1.6% of phosphatidylcholine, 0.06-0.24% of phosphatidyl ethanolamine and the balance of water for injection.

Description

technical field

[0001] The invention relates to the field of pharmaceutical preparations, in particular to a stable phenylacetate drug fat emulsion and a preparation method thereof. Background technique

[0002] Sedative-hypnotics are widely used to induce and maintain general anesthesia, sedation for surgical or diagnostic procedures, and sedation of patients in intensive care units. An ideal anesthetic drug should have the following characteristics: fast onset, smooth and rapid induction, no excitement; fast metabolism, no accumulation of metabolites in the body, and repeated administration; short recovery period, easy to maintain and control; The function of other organs is less affected, and there are fewer postoperative complications; intravenous injection is less irritating and painless.

[0003] The commonly used anesthetics in clinical practice are propofol and etomidate. Propofol has a quick onset of action, but long-term administration will delay recovery, have o...

Examples

Embodiment 1

[0036]

[0037] The general steps for emulsion preparation are described below:

[0038] (1) Take water for injection, heat it to 65°C, add glycerin to dissolve it, and use it as the water phase;

[0039] (2) Take soybean oil and medium-chain triglycerides, heat to 65°C, add phosphatidylcholine, phosphatidylethanolamine and the compound of formula (1), stir and dissolve, and use it as the oil phase;

[0040] (3) Under high-speed shearing, add the oil phase into the water phase at 65°C, the high-speed shearing speed is 10000rpm, and the time is 10min to form colostrum;

[0041] (4) Adjust the pH value of the colostrum to 7.0-7.5, and add water for injection to the full amount;

[0042] (5) Transfer the colostrum to a high-pressure homogenizer for emulsification, the homogenization pressure is 1000 bar, and 3 cycles;

[0043] (6) Filtration: filter the essence milk through a 0.45 μm microporous membrane, and potting;

[0044] (7) Moist heat sterilization (F0>8), ready to u...

Embodiment 2

[0046]

[0047] The general steps for emulsion preparation are described below:

[0048] (1) Take water for injection, heat it to 65°C, add glycerin to dissolve it, and use it as the water phase;

[0049] (2) Take soybean oil and medium-chain triglycerides, heat to 65°C, add phosphatidylcholine, phosphatidylethanolamine and the compound of formula (1), stir and dissolve, and use it as the oil phase;

[0050] (3) Under high-speed shearing, add the oil phase into the water phase at 65°C, the high-speed shearing speed is 10000rpm, and the time is 10min to form colostrum;

[0051] (4) Adjust the pH value of the colostrum to 7.0-7.5, and add water for injection to the full amount;

[0052] (5) Transfer the colostrum to a high-pressure homogenizer for emulsification, the homogenization pressure is 1000 bar, and 3 cycles;

[0053] (6) Filtration: filter the essence milk through a 0.45 μm microporous membrane, and potting;

[0054] (7) Moist heat sterilization (F0>8), ready to u...

Embodiment 3

[0056]

[0057] The general steps for emulsion preparation are described below:

[0058] (1) Take water for injection, heat it to 65°C, add glycerin to dissolve it, and use it as the water phase;

[0059] (2) Take soybean oil and medium-chain triglycerides, heat to 65°C, add phosphatidylcholine, phosphatidylethanolamine and the compound of formula (1), stir and dissolve, and use it as the oil phase;

[0060] (3) Under high-speed shearing, add the oil phase into the water phase at 65°C, the high-speed shearing speed is 10000rpm, and the time is 10min to form colostrum;

[0061] (4) Adjust the pH value of the colostrum to 7.0-7.5, and add water for injection to the full amount;

[0062] (5) Transfer the colostrum to a high-pressure homogenizer for emulsification, the homogenization pressure is 1000 bar, and 3 cycles;

[0063] (6) Filtration: filter the essence milk through a 0.45 μm microporous membrane, and potting;

[0064] (7) Moist heat sterilization (F0>8), ready to use...

technical field

[0001] The invention relates to the field of pharmaceutical preparations, in particular to a stable phenylacetate drug fat emulsion and a preparation method thereof. Background technique

[0002] Sedative-hypnotics are widely used to induce and maintain general anesthesia, sedation for surgical or diagnostic procedures, and sedation of patients in intensive care units. An ideal anesthetic drug should have the following characteristics: fast onset, smooth and rapid induction, no excitement; fast metabolism, no accumulation of metabolites in the body, and repeated administration; short recovery period, easy to maintain and control; The function of other organs is less affected, and there are fewer postoperative complications; intravenous injection is less irritating and painless.

[0003] The commonly used anesthetics in clinical practice are propofol and etomidate. Propofol has a quick onset of action, but long-term administration will delay recovery, have o...

Examples

Embodiment 1

[0036]

[0037] The general steps for emulsion preparation are described below:

[0038] (1) Take water for injection, heat it to 65°C, add glycerin to dissolve it, and use it as the water phase;

[0039] (2) Take soybean oil and medium-chain triglycerides, heat to 65°C, add phosphatidylcholine, phosphatidylethanolamine and the compound of formula (1), stir and dissolve, and use it as the oil phase;

[0040] (3) Under high-speed shearing, add the oil phase into the water phase at 65°C, the high-speed shearing speed is 10000rpm, and the time is 10min to form colostrum;

[0041] (4) Adjust the pH value of the colostrum to 7.0-7.5, and add water for injection to the full amount;

[0042] (5) Transfer the colostrum to a high-pressure homogenizer for emulsification, the homogenization pressure is 1000 bar, and 3 cycles;

[0043] (6) Filtration: filter the essence milk through a 0.45 μm microporous membrane, and potting;

[0044] (7) Moist heat sterilization (F0>8), ready to u...

Embodiment 2

[0046]

[0047] The general steps for emulsion preparation are described below:

[0048] (1) Take water for injection, heat it to 65°C, add glycerin to dissolve it, and use it as the water phase;

[0049] (2) Take soybean oil and medium-chain triglycerides, heat to 65°C, add phosphatidylcholine, phosphatidylethanolamine and the compound of formula (1), stir and dissolve, and use it as the oil phase;

[0050] (3) Under high-speed shearing, add the oil phase into the water phase at 65°C, the high-speed shearing speed is 10000rpm, and the time is 10min to form colostrum;

[0051] (4) Adjust the pH value of the colostrum to 7.0-7.5, and add water for injection to the full amount;

[0052] (5) Transfer the colostrum to a high-pressure homogenizer for emulsification, the homogenization pressure is 1000 bar, and 3 cycles;

[0053] (6) Filtration: filter the essence milk through a 0.45 μm microporous membrane, and potting;

[0054] (7) Moist heat sterilization (F0>8), ready to u...

Embodiment 3

[0056]

[0057] The general steps for emulsion preparation are described below:

[0058] (1) Take water for injection, heat it to 65°C, add glycerin to dissolve it, and use it as the water phase;

[0059] (2) Take soybean oil and medium-chain triglycerides, heat to 65°C, add phosphatidylcholine, phosphatidylethanolamine and the compound of formula (1), stir and dissolve, and use it as the oil phase;

[0060] (3) Under high-speed shearing, add the oil phase into the water phase at 65°C, the high-speed shearing speed is 10000rpm, and the time is 10min to form colostrum;

[0061] (4) Adjust the pH value of the colostrum to 7.0-7.5, and add water for injection to the full amount;

[0062] (5) Transfer the colostrum to a high-pressure homogenizer for emulsification, the homogenization pressure is 1000 bar, and 3 cycles;

[0063] (6) Filtration: filter the essence milk through a 0.45 μm microporous membrane, and potting;

[0064] (7) Moist heat sterilization (F0>8), ready to use...

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