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Amrubicin liposome and preparation method thereof

A technology of amrubicin hydrochloride liposome and blank liposome, which is applied in liposome delivery, pharmaceutical formula, medical preparations containing active ingredients, etc., can solve the problems of poor patient compliance and many adverse reactions, and achieve dissolution High degree of survival, increase survival days and survival rate, and reduce drug toxicity

Active Publication Date: 2016-06-01
CHONGQING SHENGHUAXI PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] However, at present, there are many adverse reactions after amrubicin is taken, and there are few research reports on the poor compliance of patients. Bixing liposome was used as the research object, and combined with dissolution test and toxicity test, it was initially shown that the liposome freeze-dried preparation can reduce the toxicity of the drug to a certain extent under the premise of ensuring a high dissolution rate of the drug in vitro

Method used

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  • Amrubicin liposome and preparation method thereof
  • Amrubicin liposome and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0032]Dipalmitoylphosphatidylcholine (DPPC):cholesterol:DSPE-PEG2000 was dissolved in 1000mL ethanol and isopropanol mixed solvent (1:6) at a ratio of 1:0.05:0.01, and freeze-dried to obtain a lipid phase mixture. Dissolve ammonium sulfate in pH 3 phosphate buffer solution to obtain a concentration of 0.05M·L -1 The ammonium sulfate solution was added to the above-mentioned freeze-dried lipid phase mixture, heated and stirred in a water bath at 55° C. for 1.5 hours to obtain blank liposome intermediate I. Blank liposome intermediate Ⅰ was sized three times by micro jetting, and the pressure was set at 11000 psi to obtain blank liposome intermediate Ⅱ with uniform particle size. Using column chromatography, the blank liposome intermediate II was treated with 0.5M·L of pH 3 -1 The trehalose phosphate solution replaced the ammonium sulfate in the external phase to obtain a blank liposome solution. Prepare a 5% amrubicin hydrochloride solution with water for injection, and the a...

Embodiment 2

[0034] Dissolve dipalmitoylphosphatidylcholine (DPPC): distearoylphosphatidylcholine (DSPC): cholesterol: DSPE-PEG2000 in 1000mL ethanol and tert-butanol mixed solvent at a ratio of 0.7:0.3:0.5:0.2 ( 1:6), freeze-dried to obtain a lipid phase mixture. Dissolve ammonium sulfate in pH 3 phosphate buffer solution to obtain a concentration of 0.5M·L -1 The ammonium sulfate solution was added to the above-mentioned freeze-dried lipid mixture, heated and stirred in a water bath at 55° C. for 1.5 hours to obtain blank liposome intermediate I. Blank liposome intermediate Ⅰ was sized three times by micro jetting, and the pressure was set at 11000 psi to obtain blank liposome intermediate Ⅱ with uniform particle size. Using column chromatography, the blank liposome intermediate II was treated with 1M·L of pH 3 -1 The trehalose phosphate solution replaced the ammonium sulfate in the external phase to obtain a blank liposome solution. A 5% amrubicin hydrochloride solution was prepared ...

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Abstract

The invention relates to amrubicin liposome and a preparation process thereof. The liposome contains therapeutic dose of amrubicin, and appropriate amount of phospholipid, cholesterol and the like. At the same time, the invention provides a preparation method of the liposome-preparable dosage form-lyophilized preparation. The dosage form is suitable for the treatment of malignant tumors, and reduces the toxic and side effects of the anticancer drug amrubicin to a certain extent.

Description

technical field [0001] The invention relates to an amrubicin liposome freeze-dried preparation and a preparation method thereof. Background technique [0002] Amrubicin (amrubicin), the chemical name is (7S,9S)-9-acetyl-9-amino-7-[(2-deoxy-B-D-erythro-pentopyranosyl)oxy]-7 ,8,9,10-tetrahydro-6,11-dihydroxy-5,12-tetracenedione, this product is a fully synthetic third-generation anthracycline antibiotic and a powerful DNA topoisomerase II inhibitor, used for the treatment of non-small cell lung cancer and small cell lung cancer, was registered and marketed in Japan in 2002. The clinical dose is calculated as amrubicin hydrochloride, once a day for adults, 45mg / m each time 2 (Body surface area), dissolved in 20ml of normal saline or 5% glucose injection, injected intravenously for 3 consecutive days, then stopped the drug for 3 to 4 weeks, and then proceeded to the next course of treatment (Yuan Yongrong, Chang Ping. Ammonium hydrochloride for lung cancer Rubicin [J]. Qilu P...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/704A61P35/00
Inventor 胡洁何亮贾春荣
Owner CHONGQING SHENGHUAXI PHARMA CO LTD