Microsphere-gel slow-release preparation for treating malignant tumor and thoracic-celiac metastasis

A technology for malignant tumors and sustained-release preparations, which is applied in the directions of antitumor drugs, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. It can prolong the survival time and reduce the systemic toxicity and side effects.

Inactive Publication Date: 2019-07-26
THE AFFILIATED HOSPITAL OF SOUTHWEST MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, along with the wide application of chemotherapeutic drugs and more and more studies, there are some defects in chemotherapeutic drugs: poor water solubility; Higher concentrations are formed locally in the tumor, which affects the therapeutic effect
Therefore, in order to solve the problem of short effective

Method used

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  • Microsphere-gel slow-release preparation for treating malignant tumor and thoracic-celiac metastasis
  • Microsphere-gel slow-release preparation for treating malignant tumor and thoracic-celiac metastasis
  • Microsphere-gel slow-release preparation for treating malignant tumor and thoracic-celiac metastasis

Examples

Experimental program
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Effect test

Embodiment 1

[0019] Example 1: Preparation and application of PCL-PEG-PCL microsphere sodium hyaluronate gel sustained release preparation loaded with fluorouracil, paclitaxel and cisplatin

[0020] Prepared by emulsified solvent evaporation method: Weigh 15 mg of paclitaxel and 85 mg of polycaprolactone-polyethylene glycol-polycaprolactone (PCL-PEG-PCL) polymer and dissolve it in 1 ml of dichloromethane, PCL-PEG -The number-average molecular weight of the PCL segment in the PCL polymer is about 500,000, and the number-average molecular weight of the PEG segment is about 10,000; the above solution is added dropwise to 20 ml of PVA (2.5% w / v) under stirring at 3400 rpm aqueous solution. After stirring for 10 minutes, the organic solvent was removed by rotary evaporation at room temperature for 10 minutes to form microspheres; the obtained microspheres were collected by centrifugation at 5000 rpm, washed and centrifuged three times with distilled water, and the drug-loaded microspheres prepa...

Embodiment 2

[0022] Implementation example two: preparation and application of Pluronic-PLGA microsphere chitosan gel sustained-release preparation loaded with cisplatin and fluorouracil

[0023] Prepare by emulsifying solvent evaporation method: weigh 15 mg of cisplatin and 85 mg of poloxamer-polylactic acid-glycolic acid (Pluronic-PLGA) polymer and dissolve in 1 ml of dichloromethane, the number average molecular weight of the PLGA polymer is About 100000; the above solution was added dropwise to 20ml of an aqueous solution containing PVA (2.5% w / v) under stirring at 3400rpm. After stirring for 10 minutes, the organic solvent was removed by rotary evaporation under reduced pressure for 10 minutes at room temperature to form microspheres. The obtained microspheres were collected by centrifugation at 5000 rpm, washed and centrifuged three times with distilled water, and the drug-loaded microspheres prepared above were freeze-dried and preserved. Then the above-mentioned lyophilized drug-l...

Embodiment 3

[0025] Implementation example three: preparation and application of PEG-PCL microsphere hyaluronic acid gel sustained-release preparation loaded with epirubicin, cisplatin and fluorouracil

[0026] Prepared by emulsified solvent evaporation method: Weigh 15 mg of fluorouracil and dissolve it in tetrahydrofuran and acetone, and dissolve 85 mg of PEG-PCL polymer in 1 ml of dichloromethane. The number average molecular weight of the PEG segment in the PEG-PCL polymer is About 200, the number average molecular weight of the PCL chain segment is about 10000; the above solution is mixed, and under stirring at 3400rpm, is added dropwise to 20ml of aqueous solution containing PVA (2.5% w / v). After stirring for 10 minutes, the organic solvent was removed by rotary evaporation under reduced pressure for 10 minutes at room temperature to form microspheres. The obtained microspheres were collected by centrifugation at 5000 rpm, washed and centrifuged three times with distilled water, and ...

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Abstract

The invention discloses a microsphere-gel slow-release preparation for treating malignant tumor and thoracic-celiac metastasis. The preparation comprises a microsphere base, antitumor drug and a gel carrier for dispersing the microsphere base and the antitumor drug, the antitumor active drug is loaded on the microsphere base, loading amount of the antitumor active drug on the microsphere base is 1-50%, and a mass ratio of the microsphere base to the gel carrier is 1:3-5. The microsphere base can be segmented copolymer or homopolymer, and when the microsphere base is the segment copolymer, number-average molecular weight ratio of a hydrophobic chain segment to a hydrophilic chain segment is 1-2500. The microsphere-gel slow-release preparation which is chemotherapy drug is formed by loadingchemotherapy drug on high molecular polymer, and the preparation can generate slow-release and antitumor effects when being in-situ injected into a body; the preparation has relatively little whole-body toxic and side effect, so that better continuous treatment effect is realized.

Description

technical field [0001] The invention belongs to the technical field of sustained-release preparations, and in particular relates to a microsphere-gel sustained-release preparation for treating malignant tumors and thoracoabdominal metastasis. Background technique [0002] In recent years, the incidence and mortality of malignant tumors in my country are on the rise, and the situation is becoming more and more severe. For the treatment of malignant tumors, there are mainly surgery, chemotherapy, radiotherapy, immunotherapy and so on. Among them, chemotherapy is one of the most commonly used clinical treatment methods. However, along with the wide application of chemotherapeutic drugs and more and more studies, there are some defects in chemotherapeutic drugs: poor water solubility; A higher concentration is formed locally in the tumor, thereby affecting the therapeutic effect. Therefore, in order to solve the problem of short effective drug action time and severe side effe...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K47/34A61K47/36A61K45/00A61K31/513A61K31/337A61K33/243A61P35/00A61P35/04
CPCA61K9/06A61K9/0024A61K47/34A61K47/36A61K45/00A61K31/513A61K31/337A61K33/243A61P35/00A61P35/04
Inventor 傅少志罗佳
Owner THE AFFILIATED HOSPITAL OF SOUTHWEST MEDICAL UNIV
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