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sn38 lipid composition, its preparation method and use

A lipid composition and phospholipid technology, applied in the directions of drug combination, liposome delivery, drug delivery, etc., can solve the problems of difficult industrialized large-scale production, complex preparation process, low drug encapsulation rate, etc. The effect of curative effect and improvement of encapsulation rate

Active Publication Date: 2021-05-18
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because SN38 has poor affinity with lipids such as phospholipids, it is difficult to stabilize in the membrane, so the liposome preparations disclosed in the above patents all have low drug encapsulation efficiency, large particle size, poor stability, easy drug leakage, and complicated preparation process Problems such as difficulty in industrialized mass production

Method used

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  • sn38 lipid composition, its preparation method and use
  • sn38 lipid composition, its preparation method and use
  • sn38 lipid composition, its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1 Preparation of SN38 lipid composition freeze-dried powder injection

[0049] Weigh 30mg of SN38, 600mg of soybean lecithin, 60mg of soybean oil, 150mg of cholesterol and 60mg of PEG-DSPE into a 250mL round-bottomed flask, dissolve in 30mL of chloroform:methanol (1:1, v / v), and store at 60-70°C Evaporate under reduced pressure to form a lipid film on the wall of the bottle. Add 30 mL of PBS solution (pH=5) containing 10 wt% sucrose and 0.1 wt% poloxamer 188 to hydrate for 1 hour to fully hydrate the film, and then homogenize under high pressure ( Homogenize at a pressure of 20000 psi) 5 times to obtain a lipid composition suspension, which is divided into vials and lyophilized to obtain SN38 lipid composition lyophilized powder. The freeze-dried SN38 lipid composition freeze-dried powder injection after freeze-drying adds water reconstitution, measures its particle size, electric potential and encapsulation efficiency, its particle size (see figure 1 ), potent...

Embodiment 2

[0050] Example 2 Preparation of SN38 Lipid Composition Freeze-dried Powder

[0051] Weigh 30 mg of SN38, 1200 mg of hydrogenated soybean lecithin, 100 mg of MCT, 200 mg of cholesterol, 50 mg of DSPG, 50 mg of PEG-DSPE, and 50 mg of HS15 in a 100 mL round bottom flask, and dissolve them in a mixed solvent of 50 mL of chloroform / methanol (9:1, v / v), Evaporate under reduced pressure at 60°C to form a lipid film on the bottle wall, add 30mL sodium acetate buffer (pH=3) containing 15wt% sucrose and 0.5wt% PVP-K30 to hydrate for 2 hours, and then homogenize under high pressure to obtain lipid The substance composition suspension is divided into vials and freeze-dried to obtain the product. The freeze-dried phospholipid composition freeze-dried powder was reconstituted with water, and its particle size and encapsulation efficiency were measured. As a result, the particle size and encapsulation efficiency were 178.2nm and 86.7% respectively.

Embodiment 3

[0052] The preparation of embodiment 3 SN38 lipid composition

[0053] Weigh 30mg of SN38, 335mg of egg yolk lecithin, 10mg of camellia oil, 30mg of TPGS, 50mg of cholesterol and 15mg of PEG-DSPE into a 100mL round bottom flask, and dissolve in 50mL of dichloromethane / methanol (1:1, v / v) mixed solvent Afterwards, spray-dry (inlet temperature: 60°C) to obtain white granules, add 60mL of 10wt% trehalose, 0.5wt% chitosan sodium succinate buffer (pH=4) for hydration for 2 hours, and then homogenize under high pressure A lipid composition suspension is obtained. The particle size and encapsulation efficiency were determined to be 120.8nm and 85.4%, respectively.

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Abstract

The present invention relates to a kind of SN38 lipid composition and its preparation method and application, described SN38 lipid composition comprises SN38, phospholipid, oil for injection, cholesterol, long cycle membrane material, and can form protective layer on lipid surface Functional materials, functional excipients that can reverse drug resistance. The SN38 lipid composition solves the problems of poor drug solubility, difficulty in making preparations, low encapsulation efficiency of existing lipid preparations, poor stability in vivo and in vitro, and easy and rapid leakage of drugs, and improves the circulation time of drugs in the body. Function, so that the drug is enriched in the tumor site, reducing side effects, greatly improving the efficacy, and to a certain extent, can overcome the multidrug resistance of the tumor.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a SN38 lipid composition, a preparation method and its use in the preparation of pharmaceutical preparations for treating tumors, especially drug-resistant tumors. Background technique [0002] 7-Ethyl-10-hydroxycamptothecin (SN38) is an active metabolite of irinotecan (CPT-11), a derivative of camptothecin obtained through chemical structure modification. It has the characteristics of strong anti-cancer effect and high anti-cancer activity. The in vitro cytotoxicity test shows that for some tumor cell lines, the anti-tumor activity of SN38 is 100-1000 times that of irinotecan. Its mechanism of action is selective inhibition of DNA topoisomerase I (TOPO I). During the action, the camptothecin-like drug lactone ring opens, the acyl group interacts with the nucleophilic part of TOPO I, and forms a camptothecin-like drug-TOPO I- DNA ternary complex,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K9/19A61K47/14A61K31/4745A61P35/00
CPCA61K9/0019A61K9/127A61K9/19A61K31/4745A61K47/14A61K47/44
Inventor 李亚平陈伶俐罗肖张丽
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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