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Pharmaceutical composition, pharmaceutical preparation, application and preparation method thereof for treating cancer

A technology of pharmaceutical preparations and traditional Chinese medicines, applied in the field of medicine, can solve the problems of not achieving the best therapeutic effect, rapid death of animals, vasodilation, etc., and achieve the effects of reducing gastrointestinal toxicity, uniform particle size and high encapsulation rate.

Active Publication Date: 2022-06-07
スゾウユタイファーマシューティカルテクノロジーカンパニーリミテッド
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  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

[0007] However, intravenous injection or infusion of berberine solution can cause vasodilation, blood pressure drop, heart depression and other reactions, and animal experiments have also shown that intravenous administration of berberine solution can lead to rapid death of animals
Moreover, many literatures have reported that if the in vivo pharmacokinetic behavior of the two drugs is inconsistent, after in vivo administration, the two drugs will not circulate in the body with the optimal synergistic ratio, so that the optimal therapeutic effect will not be achieved.

Method used

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  • Pharmaceutical composition, pharmaceutical preparation, application and preparation method thereof for treating cancer
  • Pharmaceutical composition, pharmaceutical preparation, application and preparation method thereof for treating cancer
  • Pharmaceutical composition, pharmaceutical preparation, application and preparation method thereof for treating cancer

Examples

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Effect test

Embodiment 1

[0044] Example 1: Weigh HSPC (150 mg), cholesterol (60 mg), DSPE-MPEG2000 (1.2 mg), dissolve them in 15 mL of chloroform, evaporate under reduced pressure at 39° C. to form a film, and place under vacuum for 12 hours to remove residual solvent. At 65°C, 10 mL of 600 mM sucrose octasulfate triethylamine salt solution was added for hydration for 30 min to form multilamellar vesicle liposomes (MLV). The MLVs were then gradually extruded through polycarbonate membranes of 0.4 μm, 0.2 μm and 0.1 μm to obtain unilamellar blank liposomes. Pass the extruded liposome sample through a Sepharose CL-4B gel column pre-equilibrated with the outer aqueous phase (20mM HEPES+150mMNaCl) to obtain a blank liposome suspension; mix 10.6 mg of irinotecan with blank The liposomes were incubated at 60 °C for 60 min, and then 5.3 mg of berberine was added. After incubation for 30 min, the drug loading was terminated in an ice-water bath. The co-loaded liposomes of irinotecan and berberine were obtain...

Embodiment 2

[0045] Example 2: This example is the same as Example 1, the difference is: 30mM sucrose+20mM histidine was used to replace 20mM HEPES+150mMNaCl, the obtained liposome irinotecan encapsulation rate was 90%, and the Alkali is 43%.

Embodiment 3

[0046] Example 3: This example is the same as Example 1, except that 20 mM HEPES+150 mM NaCl was replaced with a pH 7.0 phosphate buffer, the obtained liposome irinotecan had an encapsulation efficiency of 85%, and the Alkali is 76.4%.

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Abstract

The invention discloses a pharmaceutical composition for treating cancer, a pharmaceutical preparation and its application and preparation method. The pharmaceutical composition comprises: irinotecan and berberine. In the nano liposome preparation of the drug combination, the mass ratio of irinotecan and berberine is 1-10:1-10; the mass ratio of irinotecan and phospholipid is 1:5-15; the mass ratio of phospholipid and cholesterol The mass ratio is 1‑10:1. The pharmaceutical preparation provided by the present invention is a co-loaded liposome, which has a high encapsulation efficiency and a high drug loading capacity, and can deliver two drugs synchronously, ensuring that the synergistic ratio can still be maintained when the drugs reach the tumor site. The invention has good application potential in the treatment of cancer.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a pharmaceutical composition for treating cancer, a pharmaceutical preparation and an application and preparation method thereof. Background technique [0002] Liposomes have been used as drug carriers in the treatment of various diseases, especially in the treatment of cancer, showing obvious advantages. Encapsulating anticancer drugs in liposomes can significantly improve the metabolic kinetics of drugs in vivo, increase the accumulation of drugs in tumor tissue, reduce the toxic and side effects of drugs, and improve therapeutic effects. [0003] Irinotecan (IRI), a topoisomerase I inhibitor, is indicated for the treatment of various solid tumors including lung, colorectal, ovarian, breast and pancreatic cancers. However, IRI has serious side effects (such as myelosuppression and gastrointestinal toxicity), which limit its clinical application. Highly encapsulated irinotecan ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7048A61K9/127A61K47/24A61K47/28A61K31/352A61K31/4375A61K31/4745A61P35/00
CPCA61K9/127A61K31/4745A61K31/352A61K31/4375A61K31/7048A61K47/24A61K47/28A61P35/00A61K2300/00
Inventor 邱诗王永军何仲贵
Owner スゾウユタイファーマシューティカルテクノロジーカンパニーリミテッド
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