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Prostaglandin E1 lipid microsphere injection with charge effect and preparation method thereof

A technology of prostaglandins and lipid microspheres, which is applied in the field of medicine, can solve the problems of not giving full play to the advantages of lipid microspheres, and achieve the effects of improving the body's tolerance, solving large doses, and ensuring safety

Inactive Publication Date: 2011-01-26
李淑斌
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Problems existing in existing injections: At present, there are many dosage forms of alprostadil preparations in China, such as freeze-dried powder injections, cyclodextrin-included freeze-dried powder injections, fat emulsion injections, etc.
Minakuchi et al. reported that when PGE 1 After diluting with 10 times the amount of saline or buffer salt (pH 5.6), most of the PGE 1 was directly released into the aqueous medium, based on this result, they believed that the PGE1 emulsion did not exert its advantages as lipid microspheres in clinical therapeutic applications

Method used

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  • Prostaglandin E1 lipid microsphere injection with charge effect and preparation method thereof
  • Prostaglandin E1 lipid microsphere injection with charge effect and preparation method thereof
  • Prostaglandin E1 lipid microsphere injection with charge effect and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0071] Prescription: prostaglandin 0.5mg, egg yolk lecithin 1.5g, medium chain oil for injection 8g, sodium hydroxide appropriate amount, glycerin 2.5g, the rest is water for injection, 100ml in total.

[0072] Process:

[0073] (1) Preparation of oil phase: Add medium chain oil for injection into the preparation tank, control the temperature of medium chain oil for injection at 40°C, add egg yolk lecithin, stir vigorously until dissolved, cool down to 30°C, add medicine, stir to mix uniform;

[0074] (2) Preparation of water phase: Stir water and glycerin at 40°C for 5 minutes to make them completely miscible;

[0075] (3) At 30°C, add the oil phase to the water phase and stir vigorously to form colostrum;

[0076] (4) adjust the pH value to 5 with sodium hydroxide;

[0077] (5) Homogenizer: adjust the homogenization pressure to 500bar in the first step, and then adjust it to 1000bar in the second step, and homogenize the solution repeatedly;

[0078] (6) The emulsion obt...

Embodiment 2

[0080] Prescription: prostaglandin 0.5mg, soybean lecithin 1.5g, soybean oil for injection 10g, glucose 5g, appropriate amount of sodium citrate, and the rest water for injection, 100ml in total.

[0081] Process:

[0082] (1) Preparation of oil phase: add soybean oil for injection into the preparation tank, control the temperature of soybean oil for injection at 60°C, add soybean lecithin, and stir vigorously until dissolved;

[0083] (2) Preparation of water phase: Stir water and glucose at 55°C for 5 minutes to make them completely miscible;

[0084] (3) At 60°C, add the oil phase to the water phase and stir vigorously to form colostrum;

[0085] (4) adjust the pH value to 5.8 with sodium hydroxide;

[0086] (5) Homogenizer: adjust the homogenization pressure to 600bar in the first step, and then adjust it to 1500bar in the second step, and homogenize the solution repeatedly;

[0087] (6) The emulsion obtained above is sterilized by filtration with a 0.22um microporous m...

Embodiment 3

[0089] Prescription: prostaglandin 0.5mg, egg yolk lecithin 1.2g, soybean oil for injection 6g, glyceryl caprylate 4g, mannitol 5g, oleic acid 0.01g, appropriate amount of sodium hydroxide, the rest is water for injection, a total of 100ml. (attached Figure 23 )

[0090] Process: Under nitrogen protection throughout the process

[0091] (1) Preparation of the oil phase: Add soybean oil for injection, glyceryl caprylate and oleic acid into the preparation tank, control the temperature at 60°C, add egg yolk lecithin, stir vigorously until dissolved, cool down to 50°C and add the drug, Mix vigorously;

[0092] (2) Preparation of water phase: Stir water and mannitol at 50°C for 5 minutes to make them completely miscible;

[0093] (3) At 30°C, add the water phase to the oil phase, stir vigorously to form colostrum;

[0094] (4) adjust the pH value to 6 with sodium hydroxide;

[0095] (5) Homogenizer: adjust the homogenization pressure to 400bar in the first step, and then adj...

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Abstract

The invention relates to a method for preparing a prostaglandin E1 lipid microsphere injection of a charging non-homogeneous phase (comprising a water phase, an oil / water interfacial film phase and an oil phase) dispersion system, of which the surface of the lipid microsphere can be charged with positive electricity or negative electricity. The prostaglandin E1 is alprostadil, of which the chemical structure comprises a basic skeleton of 20-carbon fatty acid with a 5-carbon ring and two side chains, wherein one side chain is provided with a hydrophilic carboxylic acid group, so that the prostaglandin E1 has the characteristic of light surface activity action. By utilizing the characteristic, and according to the formula and the preparation process provided in the invention, the prostaglandin E1 has an unique drug-carrying mode in a solution of lipid microsphere with the non-homogeneous phase dispersion system, and the prepared lipid microsphere injection is fundamentally different from an alprostadil injection(Kaishi<TM>, and is prepared by adopting the technology of the Japanese business corporation LTT Bio-Pharma Co., Ltd. already sold in markets, and the difference lies in thatthe drug-carrying mode is completely different, the content of degradation products in the preparation such as impurities is more than 50 percent lower than that of in the Kaishi, so that the prostaglandin E1 lipid microsphere injection and the alprostadil injection are fundamentally different. The invention relates to a method for preparing the prostaglandin E1 lipid microsphere injection and the drug-carrying characteristics thereof in a three-phase system; in the formula, 0.0001 to 0.1 weight portion of prostaglandin E1 is used as a drug, the prostaglandin E1 is added with auxiliary materials for medical purpose to prepare the prostaglandin E1 lipid microsphere injection, and the auxiliary materials for medical purpose comprises the following materials in portion by weight: 5 to 20.

Description

Technical field: [0001] The present invention relates to the technical field of medicine, precisely, it is a kind of prostaglandin E that is distributed inwardly (oil phase, oil / water interface membrane phase) 1 Lipid microsphere injection and its preparation method, and the preparation method of liposphere preparation suitable for prostaglandin drugs. Background technique: [0002] Prostaglandin (PNstaglandinum, PG) is a kind of unsaturated fatty acid with 20 carbon atoms, which contains different subtypes and has a wide range of biological effects. Prostaglandin E 1 (Alprostadil, PGE 1 ) is one of the extremely active physiologically active substances, which can inhibit platelet aggregation, thromboxane A 2 generation, atherosclerosis, lipid plaque formation, and the role of immune complexes. The main component of alprostadil lipid microsphere injection is prostaglandin E 1 , and its chemical name is: (1R, 2R, 3R)-3-hydroxy-2[(E)-(3S)-3-hydroxy-1-octenyl]-5-oxocyclope...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K31/5575A61P1/16A61P7/02A61P9/00A61P9/10
Inventor 李淑斌宋健
Owner 李淑斌
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