The preparation method of albendazole thermosensitive liposome

A technology of albendazole heat-sensitive lipid and albendazole heat-sensitive lipid, which can be used in liposome delivery, medical preparations containing non-active ingredients, medical preparations containing active ingredients, etc., and can solve head hooks Problems such as shedding, structure disappearance, and cortex destruction, to achieve the effects of slowing down drug release, improving solubility, and high ABZ drug loading

Inactive Publication Date: 2018-05-01
CHONGQING MEDICAL UNIVERSITY
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Problems solved by technology

The results showed that after the combined use of albendazole thermosensitive liposomes and high-intensity focused ultrasound, the morphological observation showed that the cortex was severely damaged, calcium particles disappeared, vacuolation was obvious, the head hooks fell off, and some structures even disappeared, and the mortality rate was high

Method used

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  • The preparation method of albendazole thermosensitive liposome
  • The preparation method of albendazole thermosensitive liposome
  • The preparation method of albendazole thermosensitive liposome

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Embodiment Construction

[0025] The present invention will be further described below in conjunction with embodiment.

[0026] A kind of albendazole thermosensitive liposome is made up of the raw material of following mass parts, as shown in table 1:

[0027] Table 1, albendazole thermosensitive liposome raw material composition (unit: parts by mass)

[0028]

[0029] A kind of preparation method of albendazole thermosensitive liposome, carries out according to the following steps:

[0030] Step 1. Put the dipalmitoylphosphatidylcholine, monopalmitoylphosphatidylcholine, distearoylphosphatidylglycerol and albendazole into the round-bottomed flask successively according to the proportion, and then add the Add the chloroform-methanol mixture, avoid light and fully dissolve;

[0031] Step 2, the round-bottomed flask is placed on a rotary evaporator, the chloroform-methanol mixture is removed, and a white film is obtained on the inner wall of the round-bottomed flask;

[0032] Step 3, adding a phosp...

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Abstract

The invention discloses an albendazole thermosensitive liposome, which consists of dipalmitoylphosphatidylcholine, monopalmitoylphosphatidylcholine, distearoylphosphatidylglycerol and albendazole. The preparation process is as follows: first put the above four raw materials into a round-bottomed flask in proportion, then add the chloroform-methanol mixed solution, remove the chloroform-methanol mixed solution on a rotary evaporator after dissolving; continue to add phosphate buffer solution, and hydrate to obtain Milky white liquid; then transfer the milky white liquid to a centrifuge tube, and use an ultrasonic cell disruptor to process it for 150 seconds; finally filter, and freeze-dry the filtrate to obtain a finished product. The remarkable effect of the present invention is that ABZ is encapsulated in the heat-sensitive liposome carrier to improve the solubility of the drug, slow down the release of the drug, enhance the liver targeting, and finally achieve the purpose of improving bioavailability; in addition, the present invention The obtained albendazole thermosensitive liposome (TSL‑ABZ) has a high significant encapsulation efficiency and ABZ drug loading.

Description

technical field [0001] The invention relates to a preparation method of a new dosage form of albendazole, in particular to a preparation method of albendazole thermosensitive liposome. Background technique [0002] Albendazole (ABZ), also known as Changchongqing, chemical name 5-propylthio-1H-benzimidazole-2-carbamate methyl ester, is a broad-spectrum antiparasitic drug of benzimidazoles, But because it is insoluble in water, the intestinal absorption rate and bioavailability are very low. Traditionally, albendazole is in the form of powder or tablet. The cure rate of this common dosage form for non-intestinal parasitic diseases is only about 30%, and the concentration of liver drugs is relatively low. Someone proposed a kind of albendazole liposome afterwards, but adopt lecithin as raw material in its scheme, the albendazole liposome that prepares does not have heat sensitivity. [0003] Later, the researchers conducted a study on high-intensity focused ultrasound-induced...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/4184A61K47/24A61P33/00
Inventor 张静叶彬王梦莹
Owner CHONGQING MEDICAL UNIVERSITY
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