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A kind of alprostadil freeze-dried microemulsion composition and preparation method thereof

A technology of alprostadil and freeze-dried microemulsion, which is applied in the field of alprostadil freeze-dried microemulsion composition and its preparation, can solve the problems of high content of degraded impurities, vascular stimulation, etc., achieve encapsulation efficiency and stability improvement, Avoid drug degradation and reduce the effect of vascular irritation

Active Publication Date: 2019-05-07
SHANGHAI FANGYU HEALTH PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In view of the above problems, the present invention provides a safer, more stable alprostadil freeze-dried microemulsion composition, to solve its stimulation of blood vessels, the problem of high content of degradation impurities

Method used

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  • A kind of alprostadil freeze-dried microemulsion composition and preparation method thereof
  • A kind of alprostadil freeze-dried microemulsion composition and preparation method thereof
  • A kind of alprostadil freeze-dried microemulsion composition and preparation method thereof

Examples

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Effect test

Embodiment 1

[0042] Embodiment 1: the preparation of composition of the present invention

[0043] Weigh 26g of polyethylene glycol 15-hydroxystearate, 2g of phosphatidylglycerol, 25g of medium-chain triglycerides, and 4g of phosphatidylcholine, stir at about 60°C to dissolve and mix evenly, then lower the temperature to 25°C Add 5 mg of alprostadil, stir to dissolve and mix evenly to obtain a mixed oil phase; weigh 75 g of glucose, add it to 600 ml of water, stir to dissolve, and control the temperature at about 25°C to obtain a water phase; Mix with mixed oil, control the temperature at about 25°C; adjust the pH to 5.2 with 0.5M hydrochloric acid and 0.5M sodium hydroxide, add water to the full amount (1L); homogenize 3 times under the pressure of 400bar through a high-pressure homogenizer, Control the temperature at about 8°C; filter aseptically, fill in vials, freeze-dry, cap, and package.

Embodiment 2

[0044] Embodiment 2: the preparation of composition of the present invention

[0045] Weigh 20g polysorbate 80, 3g phosphatidylserine, 20g medium chain triglycerides, 5g phosphatidylcholine, stir at about 50°C to dissolve and mix evenly, lower the temperature to about 29°C, add 5mg of alprostadil, Stir to dissolve and mix evenly to obtain a mixed oil phase; weigh 75g of sucrose, add it to 800ml of water, stir to dissolve, and control the temperature at about 29°C to obtain a water phase; under stirring, mix the water phase with the mixed oil phase, and control the temperature 29°C or so; use 0.5M hydrochloric acid and 0.5M sodium hydroxide to adjust the pH to 4.0, add water to the full amount (1L); use a high-pressure homogenizer to homogenize twice under a pressure of 400bar, and control the temperature at about 10°C; Bacterial filtration, filled in vials, freeze-dried, capped, packaged, ready to be obtained.

Embodiment 3

[0046] Embodiment 3: the preparation of composition of the present invention

[0047] Weigh 15g of polyethylene glycol 15-hydroxystearate, 1g of phosphatidylinositol, 10g of medium-chain triglycerides, and 5g of phosphatidylcholine, stir at about 65°C to dissolve and mix evenly, and lower the temperature to 22°C Add 5 mg of alprostadil, stir to dissolve and mix evenly to obtain a mixed oil phase; weigh 50 g of mannitol, add it to 500 ml of water, stir to dissolve, and control the temperature at about 22°C to obtain a water phase; Mix the phase with the mixed oil phase, control the temperature at about 20°C; adjust the pH to 5.0 with 0.5M hydrochloric acid and 0.5M sodium hydroxide, add water to the full amount (1L); homogenize 6 times under the pressure of 100bar through a high-pressure homogenizer , temperature controlled at about 8°C; after aseptic filtration, filled in vials, freeze-dried, capped, and packaged, ready to be obtained.

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Abstract

The invention provides PGE1 (prostaglandin E1) freeze-dried microemulsion composition. The composition is prepared from PGE1, a non-ionic emulsifier, chondroitin sulfate, anionic phospholipid and a freeze-drying protective agent, and raw materials and components comprise, in percentage by mass, 0.001%-0.04% of PGE1, 1%-55% of the non-ionic emulsifier, 0.1%-20% of anionic phospholipid, 0.6%-28% of an oil phase and 5%-98% of the freeze-drying protective agent. The encapsulation efficiency and the stability of the composition are significantly improved, reduction of free drug concentration is facilitated, vascular irritation of a preparation is reduced, and the composition is safer and more stable.

Description

technical field [0001] The invention relates to a composition, in particular to an alprostadil freeze-dried microemulsion composition and a preparation method thereof. Background technique [0002] Alprostadil (PGE 1 ) is a 20-carbon unsaturated fatty acid, widely present in tissues and body fluids of different species of mammals, and is one of its own active substances. Exogenous alprostadil, as a vasodilator and platelet aggregation agent, has a wide range of pharmacological activities. At present, there are multiple dosage forms on the market, including injections (alprostadil powder for injection, alprostadil fat emulsion, injection Alprostadil dry emulsion), external agents (alprostadil urethral suppository, alprostadil cream), can be used for: treatment of extremities caused by chronic arterial occlusive disease (thromboangiitis obliterans, arteriosclerosis obliterans, etc.) Resting pain in limbs caused by ulcers and microvascular circulation disorders; treatment of ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/5575A61K47/24A23L33/12A61P9/14A61P9/10A61P17/02A61P29/00A61P7/02A61P9/00A61P1/16
CPCA23V2002/00A61K9/19A61K31/5575A61K47/24A23V2200/326A23V2200/30A23V2250/186
Inventor 蔡伟惠金方
Owner SHANGHAI FANGYU HEALTH PHARMA TECH CO LTD
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