Novel hydrochloric acid topotecan intratumor injection preparation composition and preparation method thereof

A technology for intratumoral injection of topotecan hydrochloride, applied in the field of intratumoral injection preparations and its preparation, new topotecan hydrochloride intratumoral injection preparation composition and its preparation fields, to achieve improved stability, reduced side effects, and easy infusion The effect of pretending

Inactive Publication Date: 2014-01-01
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main toxic reaction of topotecan is bone marrow suppression, which is a dose-limiting toxic reaction, but its occurrence can be predicted, and it is

Method used

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  • Novel hydrochloric acid topotecan intratumor injection preparation composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

specific Embodiment 1

[0032] Weigh 0.8g of soybean lecithin and 0.08g of cholesterol, add 10mL of dichloromethane to dissolve. Dichloromethane was removed by rotary evaporation at 35°C, and dried in vacuum for 2 hours to remove residual organic solvent. Add 20mL of 0.3mol / L ammonium sulfate solution and hydrate at 35°C for 30min. High-pressure homogeneous treatment, granulation through 0.22μm microporous membrane. Add 80mg of topotecan hydrochloride powder, stir to dissolve, incubate at 65°C for 20min, pass through a 0.22μm microporous membrane to obtain the finished liposome. 5% lactose and 5% sucrose were selected as freeze-drying protective agents, and the liposomes were freeze-dried. The liposome encapsulation efficiency was 86.9%.

[0033] Add chitosan (0.05g) to acetic acid solution (0.1M), stir evenly, add 3 mg of the prepared topotecan hydrochloride liposome lyophilized powder, stir evenly, place in ice water bath and continue stirring for 15min, and β-glycerophosphate Sodium (48%, 0.8 ...

specific Embodiment 2

[0034] Weigh 0.8g of soybean lecithin and 0.18g of cholesterol, add 10mL of dichloromethane to dissolve. Dichloromethane was removed by rotary evaporation at 35°C, and dried in vacuum for 2 hours to remove residual organic solvent. Add 20mL of 0.3mol / L ammonium sulfate solution and hydrate at 35°C for 30min. High-pressure homogenization treatment, passing through a 0.22 μm microporous membrane for sizing. Add 80mg of topotecan hydrochloride powder, stir to dissolve, incubate at 65°C for 20min, pass through a 0.22μm microporous membrane to obtain the finished liposome. 5% lactose and 5% sucrose were selected as freeze-drying protective agents, and the liposomes were freeze-dried. The liposome encapsulation efficiency was 90.6%.

[0035] Add chitosan (0.05g) to acetic acid solution (0.1M), stir evenly, add 3 mg of the prepared topotecan hydrochloride liposome lyophilized powder, stir evenly, place in ice water bath and continue stirring for 15min, and β-glycerophosphate Sodi...

specific Embodiment 3

[0036] Weigh 0.9 g of soybean lecithin and 0.225 g of cholesterol, add 10 mL of dichloromethane to dissolve. Dichloromethane was removed by rotary evaporation at 35°C, and dried in vacuum for 2 hours to remove residual organic solvent. Add 20mL of 0.25mol / L ammonium sulfate solution and hydrate at 35°C for 30min. High-pressure homogeneous treatment, granulation through 0.22μm microporous membrane. Add 80mg of topotecan hydrochloride powder, stir to dissolve, incubate at 65°C for 20min, pass through a 0.22μm microporous membrane to obtain the finished liposome. 5% lactose and 5% sucrose were selected as freeze-drying protective agents, and the liposomes were freeze-dried. The liposome encapsulation efficiency was 93.6%.

[0037] Add chitosan (0.05g) to acetic acid solution (0.1M), stir evenly, add 3 mg of the prepared topotecan hydrochloride liposome lyophilized powder, stir evenly, place in ice water bath and continue stirring for 15min, and β-glycerophosphate Sodium (48%,...

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Abstract

The invention relates to a novel hydrochloric acid topotecan intratumor injection preparation composition and a preparation method thereof, belonging to the field of medicament preparations. According to the composition, a lipidosome technique and an in-situ gel technique are combined and used, the main medicine component, namely, hydrochloric acid topotecan, is carried into a lipid bilayer film through an active medicine carrying method; and the temperature sensitive gel of chitosan/sodium beta-glycerophosphate is used as a gel material which can be kept be liquid at a low temperature, and is converted into solid when the temperature is risen to the body temperature. The invention discloses the preparation method of the composition. The method comprises the following steps of preparing the hydrochloric acid topotecan lipidosome by using an ammonium sulfate gradient method, selecting a freeze-drying protecting agent, determining the concentration of the chitosan and the sodium beta-glycerophosphate, and preparing the composition. Due to the composition and the preparation method, on the basis that active components are protected and the stability of the preparation is improved, the release of the medicine is controlled, and the biological utilization degree of the main medicine is improved; due to adoption of an intratumor injection mode, the side effect of the main medicine component is reduced, and the compliance of a patient is improved; and the composition is easy to fill, and the industrial production is facilitated.

Description

technical field [0001] The invention relates to an intratumoral injection preparation and a preparation method thereof, in particular to a novel topotecan hydrochloride intratumoral injection preparation composition and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] The main modes of current tumor treatment are: surgical resection, radiotherapy and chemotherapy. During cancer treatment, almost all cancer patients will undergo surgery to remove as much tumor tissue as possible. However, residual tumor cells after surgical resection of tumor tissue are highly likely to cause metastasis during the administration of postoperative radiation therapy or systemic chemotherapy. Changing the administration method of systemic chemotherapy and injecting drugs directly into the tumor site by intratumoral injection has gradually attracted people's attention. And this will also become an effective way to improve the bioa...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K31/4745A61K47/36A61P35/00
Inventor 吴正红邢嘉玉祁小乐主雪华张子崴
Owner CHINA PHARM UNIV
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