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Entecavir high-density lipoprotein enveloping preparation, and preparation method and use thereof

A technology of high-density lipoprotein and entecavir, which is applied in the field of entecavir high-density lipoprotein encapsulation preparation and preparation thereof

Active Publication Date: 2014-03-26
唐为钢
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] However, 60%-70% of the currently marketed oral anti-hepatitis B drug entecavir is excreted by the kidneys in the human body, resulting in side effects of entecavir nephrotoxicity. Less than 1% of entecavir is absorbed by the liver of the organ infected with hepatitis B virus. Therefore, about 99% The entecavir reaches the human organs that should not go

Method used

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  • Entecavir high-density lipoprotein enveloping preparation, and preparation method and use thereof
  • Entecavir high-density lipoprotein enveloping preparation, and preparation method and use thereof
  • Entecavir high-density lipoprotein enveloping preparation, and preparation method and use thereof

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preparation example Construction

[0051] The invention provides a preparation method of entecavir high-density lipoprotein encapsulation preparation, said method comprising the following steps:

[0052] The first step is to obtain the high-density lipoprotein particle precursor loaded with the internal phase buffer through supercritical fluid technology: mix cholesterol, hydrogenated soybean phospholipid and ammonium salt buffer, and obtain the loaded internal phase buffer through a supercritical fluid reactor. High-density lipoprotein particle precursors;

[0053] The second step is to make the particle size of high-density lipoprotein particle precursor to nanometer level: mix the high-density lipoprotein particle precursor and apolipoprotein A1 loaded with internal phase buffer, and ultrasonically treat the particle size of high-density lipoprotein particle to be 30-50nm, preferably 30-40nm;

[0054] The third step is to replace the external phase buffer with phosphate buffer by molecular sieve, and the pH...

preparation Embodiment 1

[0088] Preparation of Entecavir HDL Encapsulation Preparation 1

[0089] 1. Utilize supercritical fluid technology (putting into the reaction raw material is 50 grams of 0.3M (NH 4 ) 2EDTA (pH=5.0) buffer, 5.5 grams of hydrogenated soybean lecithin HSPC and 2.4 grams of cholesterol, the reaction kettle temperature is 60 ° C, the reaction kettle pressure is 200 bar) preparation loading 0.3M (NH 4 ) 2 High-density lipoprotein particle precursor in EDTA buffer, reacted and equilibrated for 40 minutes;

[0090] 2. Add 9.5 grams of ApoAI polypeptide and ultrasonic treatment (80KHZ, 0.07-0.14W / cm2, 10 minutes) to the prepared high-density lipoprotein particle precursor to reduce the particle size of the high-density lipoprotein particle precursor to about 30-50nm (nano), to obtain high-density lipoprotein particles, the G-50 molecular sieve column replacement high-density lipoprotein particle external phase buffer is phosphate buffer saline (PBS) with pH=8.5, after replacing the ...

preparation Embodiment 2

[0094] Preparation of entecavir encapsulated in liposomes

[0095] The preparation of entecavir encapsulated in liposomes is the same as the process of preparing entecavir encapsulated in high-density lipoprotein, except that ApoA I protein is not added.

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Abstract

The invention discloses an entecavir high-density lipoprotein enveloping preparation, and a preparation method and a use thereof. The entecavir high-density lipoprotein enveloping preparation contains entecavir, phospholipid, cholesterol and ApoAl in the weight ratio of 5: 7: 3: (5-20).

Description

technical field [0001] The invention relates to the field of pharmaceutical liposomes, in particular to an entecavir high-density lipoprotein encapsulation preparation and its preparation method and application. Background technique [0002] At present, more than 12 nanoparticle drug delivery systems have been approved by the FDA for clinical application, and all of these nanoparticle drug delivery systems that have been marketed do not have organ-specific targeting. . [0003] There are 7 anti-hepatitis B drugs that have been marketed (FDA) in the world, two of which are interferon and PEGylated interferon, and the other 5 are nucleotide analogues, of which PEGylated interferon, tenofovir, entecavir (entecavir) ) These three drugs will play a dominant role in the future. The sales of entecavir in China's anti-hepatitis B drug market are increasing every year. In 2008, the annual sales of entecavir (entecavir) sales in my country reached 856 million yuan, an increase of 19...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/522A61K47/42A61P1/16A61P31/20
Inventor 唐为钢
Owner 唐为钢
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