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Gemcitabine or gemcitabine salt nano-emulsion injecta and preparation method thereof

A technology of nanoemulsion and gemcitabine, applied in the field of nanoemulsion injection of gemcitabine or its salt and its preparation, can solve the problem of poor stability of gemcitabine liposomes or nano-microspheres, adverse effects of drug stability and bioavailability, stability It can reduce the pain of medication, improve the encapsulation rate and stability, and reduce the effects of toxic and side effects.

Active Publication Date: 2013-06-05
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

CN101444485B discloses a kind of gemcitabine liposome, and this liposome comprises gemcitabine, phospholipid, cholesterol, but the encapsulation efficiency and dispersibility of this liposome all perform poorly, all have unfavorable to the stability of medicine and bioavailability influences
CN101926779A discloses a gemcitabine solid lipid nanoparticle and a preparation method thereof. The preparation still has the problems of low drug encapsulation efficiency and poor stability, and the drug is partially degraded after storage for about 3 months
[0007] Judging from the current research results, gemcitabine liposomes or nanospheres prepared by existing methods have problems such as poor stability, easy aggregation in aqueous solution, overall erosion or surface degradation, and cannot be practically applied in clinical practice.

Method used

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  • Gemcitabine or gemcitabine salt nano-emulsion injecta and preparation method thereof
  • Gemcitabine or gemcitabine salt nano-emulsion injecta and preparation method thereof
  • Gemcitabine or gemcitabine salt nano-emulsion injecta and preparation method thereof

Examples

Experimental program
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Embodiment 1

[0035]

[0036] Preparation method: Under the protection of inert gas, stir 200g soybean oil for injection into the oil phase, and add 200g soybean phospholipid to 500ml water for injection, stir to form the water phase, and mix the oil and water phases evenly under high-speed stirring , And homogenized by a high-pressure homogenizer to make colostrum, add 10g gemcitabine hydrochloride, adjust the pH to 5.0, add water to make the volume to 1000ml, transfer to the high-pressure homogenizer and stir well until the average particle size is below 40nm; Packed and packed with nitrogen.

Embodiment 2

[0038]

[0039] Preparation method: Under the protection of inert gas, stir 200 g of peanut oil for injection into the oil phase, and add 200 g of soybean phospholipid to 500 ml of water for injection, stir to form the water phase, and mix the oil and water phases evenly under high-speed stirring. The colostrum is homogenized by a high-pressure homogenizer, 10g gemcitabine hydrochloride is added, the pH is adjusted to 5.0, and the volume is adjusted to 1000ml with water, and then transferred to the high-pressure homogenizer to fully stir until the average particle size is below 40nm; filling , Nitrogen-filled package.

Embodiment 3

[0041]

[0042] Preparation method: Under the protection of inert gas, stir 200g of sesame oil for injection into the oil phase, and add 200g of soybean phospholipid to 500ml of water for injection, stir to form the water phase, mix the oil phase and the water phase evenly under high-speed stirring. The colostrum is homogenized by a high-pressure homogenizer, 10g gemcitabine hydrochloride is added, the pH is adjusted to 5.0, and the volume is adjusted to 1000ml with water, and then transferred to the high-pressure homogenizer to fully stir until the average particle size is below 40nm; filling , Nitrogen-filled package.

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Abstract

The invention relates to a gemcitabine or gemcitabine salt nano-emulsion injecta and a preparation method of the gemcitabine or gemcitabine salt nano-emulsion injecta. The injecta specifically includes gemcitabine or a gemcitabine salt, oil for injection, a surface active agent and water for injection, wherein the weight ratio of gemcitabine or the gemcitabine salt to the oil for injection to thesurface active agent is 1:(10-100):(10-100), and the average particle size of an emulsion droplet in the emulsion is 1-100nm. The injecta provided by the invention is high in entrapment efficiency and stability and low in side effect.

Description

Technical field [0001] The present invention relates to a novel formulation of gemcitabine or its salt and a preparation method thereof, in particular to a nanoemulsion injection of gemcitabine or its salt and a preparation method thereof. Background technique [0002] Gemcitabine is a difluoronucleoside anti-metabolite anticancer drug that disrupts cell replication. It is a water-soluble analogue of deoxycytidine and is an inhibitory alternative to ribonucleotide reductase. In the process of DNA synthesis and repair, this enzyme is essential for the production of required deoxynucleotides. It has the characteristics of broad anti-tumor spectrum, unique mechanism of action, no cross-resistance with other chemotherapeutics, and no superimposition of toxicity. [0003] As a prodrug, gemcitabine is a good substrate for deoxythymidine kinase phosphorylation in cells, and is converted into the following metabolites under the action of enzymes: gemcitabine monophosphate (dFdCMP), gemcit...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/7068A61K47/44A61P35/00
Inventor 宋阳张春红吕爱锋
Owner JIANGSU HANSOH PHARMA CO LTD