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Tacrolimus lipid emulsion for injection and preparation method thereof

A crolimus fat emulsion and tacrolimus technology, applied in the field of medicine, can solve the problems of lack of relevant research data on efficacy and safety, decreased pharmaceutical stability, and drug precipitation, etc., so as to reduce local and vascular irritation. , Improve physical stability, increase the effect of chemical stability

Active Publication Date: 2015-01-14
西安远大德天药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

From the perspective of pharmacy, the inventions using a combination of various surfactants in the above public information are not the best inventions, and there are no relevant research data on the efficacy and safety of their clinical applications, and their safety is questionable
[0012] In addition, there are some problems in the existing solution composition. The drug will precipitate during the storage during the delivery period, and its pharmaceutical stability will decrease as the content of the drug decreases.
Therefore, traditional solution compositions are not suitable for human injection formulations

Method used

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  • Tacrolimus lipid emulsion for injection and preparation method thereof
  • Tacrolimus lipid emulsion for injection and preparation method thereof
  • Tacrolimus lipid emulsion for injection and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0041] The tacrolimus fat emulsion for injection of this embodiment contains 0.2 g of tacrolimus, 10 g of soybean oil, 10 g of medium-chain fatty acid triglycerides, and lecithin (egg yolk lecithin) in every 100 mL of tacrolimus fat emulsion for injection. ) 2g, oleic acid 0.05g, L-poly(lactic acid) poly(ethylene glycol) block copolymer (provided by Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, wherein the viscosity-average molecular weight of polyethylene glycol is 2000, and the viscosity-average molecular weight of L-poly(lactic acid) is 14000) 1.4g, glycerol 2.5g, vitamin E 1.5g, cholesterol 0.8g, edetate disodium 0.02g, hydrochloric acid (the amount is such that the pH of the tacrolimus fat emulsion for injection is 6.0), and the balance is water for injection.

[0042] The preparation method of the tacrolimus fat emulsion for injection of the present embodiment is:

[0043] Step 1, adding tacrolimus, vitamin E and cholesterol into a mixed solvent ...

Embodiment 2

[0049] This embodiment is the same as Example 1, wherein the difference is: the oily solvent for injection is castor oil, corn oil, soybean oil, sesame oil, cottonseed oil, peanut oil, safflower oil, medium chain fatty acid triglyceride, crow One or more of gall oil, palm oil, sunflower oil, seabuckthorn seed oil, angelica oil, pepper oil, garlic oil, zedoary oil and Chuanqiong oil, or castor oil, corn oil, sesame oil, cottonseed oil , peanut oil, safflower oil, medium-chain fatty acid triglycerides, javanica javanica oil, palm oil, sunflower oil, sea buckthorn seed oil, angelica oil, pepper oil, garlic oil, zedoary oil, and chuanqiong oil, or For castor oil, corn oil, sesame oil, cottonseed oil, peanut oil, safflower oil, javanica oil, palm oil, sunflower oil, seabuckthorn seed oil, angelica oil, pepper oil, garlic oil, zedoary oil and Chuanqiong oil A mixture with soybean oil; the surfactant is one or more than three of lecithin, Span, Tween, Pluronic, sodium oleate, oleic a...

Embodiment 3

[0051] The tacrolimus fat emulsion for injection of this embodiment contains 0.01 g of tacrolimus, 10 g of javanica javanica oil, 0.5 g of lecithin (egg yolk lecithin) in every 100 mL of tacrolimus fat emulsion for injection, and sodium oleate 0.1g, Tween 800.4g, D-polylactic acid polyethylene glycol block copolymer (Changchun Institute of Applied Chemistry, Chinese Academy of Sciences provides, wherein the viscosity-average molecular weight of polyethylene glycol is 5000, and the viscosity-average molecular weight of L-polylactic acid is 8000 ) 1g, glycerol 1g, ascorbic acid 1g, cholesteryl sulfate sodium 0.5g, edetate sodium calcium 0.01g, sodium hydroxide (the amount is to make the pH value of the tacrolimus fat emulsion for injection be 9.0), and the balance is the injection use water.

[0052] The preparation method of the tacrolimus fat emulsion for injection of the present embodiment is:

[0053] Step 1, adding tacrolimus and sodium cholesteryl sulfate into Brucea java...

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Abstract

The invention discloses a tacrolimus lipid emulsion for injection, and the tacrolimus lipid emulsion contains tacrolimus, an oily solvent for injection, a surfactant, amphiphilic block copolymers, an osmotic pressure regulator for injection, an antioxidant and a stabilizer. In addition, the invention also discloses a preparation method of the lipid emulsion. The tacrolimus lipid emulsion is capable of effectively increasing the chemical stability of the medicines; most of medicines in the tacrolimus lipid emulsion are distributed in an oil phase or an oil-water interface; and the medicines are prevented from directly contacting water, are solubilized into the oil phase, and are isolated, so that the medicine dosage of the water phase is reduced, the hydrolysis amount of the medicines is greatly reduced, and the stability on the medicines is greatly improved. The tacrolimus lipid emulsion for injection disclosed by the invention can be used for wrapping a part of medicines into the oil phase or an interfacial film, and preventing the medicines from directly contacting body fluid, so that the local and vascular stimulation which can be generated by the medicines is reduced.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a tacrolimus fat emulsion for injection and a preparation method thereof. Background technique [0002] Organ transplantation is known as one of the three major advances in human medicine in the 20th century. Organ transplantation, as the last effective means of organ failure treatment, is in great demand in China. Now there are more than 100 hospitals and more than 200 experts across the country who can perform 25 kinds of transplantation including kidney, liver, heart, pancreas, lung, bone marrow and cornea. For allogeneic organ transplantation, organ transplant patients need to take immunosuppressants for life after transplantation. Immunosuppressants play an important role in the survival time of organ transplant patients and maintaining the good function of transplanted organs. Therefore, the development of immunosuppressants as drugs for organ transplantation ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/436A61K47/44A61K47/34A61K47/28A61P37/06A61P31/10
Inventor 王亚轩唐星
Owner 西安远大德天药业股份有限公司
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