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Tumor-targeting albumin nano-lyophilized powder injection preparation and preparation method thereof

A nano-albumin and tumor-targeting technology, which is applied in the field of albumin nano-lyophilized powder injection preparations and its preparation, can solve the problems of staying in the research stage and achieve the goal of improving drug efficacy, water solubility, and stability Effect

Inactive Publication Date: 2011-11-09
TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, the use of advanced drug delivery systems to improve the solubility and targeting of such drugs is the main research direction at present, such as making emulsions, liposomes, microspheres, micelles, solid lipid nanoparticles, etc., although all Some progress has been made, but there are limitations, and most remain at the research stage

Method used

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  • Tumor-targeting albumin nano-lyophilized powder injection preparation and preparation method thereof
  • Tumor-targeting albumin nano-lyophilized powder injection preparation and preparation method thereof
  • Tumor-targeting albumin nano-lyophilized powder injection preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1, Preparation and Quality Evaluation of Paclitaxel Albumin Nano-lyophilized Powder Injection

[0037] Prescription composition:

[0038]

[0039]

[0040] Preparation Process:

[0041] (1) Weigh the insoluble antineoplastic drug according to the prescription amount, add latent solvent for ultrasonic dissolution, mix with soybean lecithin, glyceryl tricaprylate, glyceryl tributyrate and polyethylene glycol-lauryl hydroxystearate, and stir Evenly, solution A is obtained;

[0042] (2) Weigh albumin and freeze-dried excipients according to the prescription amount, add them to water for injection, and obtain solution B after dissolving;

[0043] (3) Mix solutions A and B, stir evenly, and filter through a microporous membrane (0.22 μm);

[0044] (4) Place the solution obtained in step 3 in a freeze-drying apparatus, and set the freeze-drying parameters as follows: the pre-freezing temperature is -50°C, and the pre-freezing time is 2.5 hours; the total numbe...

Embodiment 2

[0046] Example 2, Preparation and Quality Evaluation of Paclitaxel Albumin Nano-lyophilized Powder Injection

[0047] Prescription composition:

[0048]

[0049] Preparation Process:

[0050] (1) Take the insoluble antineoplastic drug according to the prescription amount and add it into a latent solvent for ultrasonic dissolution, mix it with phospholipids, glyceryl tricaprylate, glyceryl tributyrate and polyethylene glycol-lauryl hydroxystearate, stir evenly, Obtain solution A;

[0051] (2) Weigh albumin and freeze-dried excipients according to the prescription amount, add them to water for injection, and obtain solution B after dissolving;

[0052] (3) Mix solutions A and B, stir evenly, and filter through a microporous membrane (0.22 μm);

[0053] (4) Place the solution obtained in step 3 in a freeze-drying apparatus, and set the freeze-drying parameters as follows: the pre-freezing temperature is -50°C, and the pre-freezing time is 2.5 hours; the total number of subl...

Embodiment 3

[0055] Example 3, Preparation and quality evaluation of paclitaxel albumin nano freeze-dried powder preparation

[0056] Prescription composition:

[0057]

[0058] Preparation Process:

[0059] (1) Take the insoluble antineoplastic drug according to the prescription amount and add it into a latent solvent for ultrasonic dissolution, mix it with phospholipids, glyceryl tricaprylate, glyceryl tributyrate and polyethylene glycol-lauryl hydroxystearate, stir evenly, Obtain solution A;

[0060] (2) Weigh albumin and freeze-dried excipients according to the prescription amount, add them to water for injection, and obtain solution B after dissolving;

[0061] (3) Mix solutions A and B, stir evenly, and filter through a microporous membrane (0.22 μm);

[0062] (4) Place the solution obtained in step 3 in a freeze-drying apparatus, and set the freeze-drying parameters as follows: the pre-freezing temperature is -50°C, and the pre-freezing time is 2.5 hours; the total number of s...

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Abstract

The invention discloses a tumor-targeting albumin nano-lyophilized powder injection preparation and a preparation method thereof. The preparation comprises the following components: an insoluble antitumor drug (for example, taxol), albumin, tricaprylin, tributyrin, polyethylene glycol-12-hydroxy stearate and phospholipid. The tumor-targeting albumin nano-lyophilized powder injection preparation provided by the invention can spontaneously form a nanoemulsion with the particle size of about 100nm after being diluted by normal saline, and the drug can target the tumor tissues after intravenous injection, thus improving the effectiveness and safety. In addition, the tumor-targeting albumin nano-lyophilized powder injection preparation provided by the invention is simple in preparation process and suitable for industrialized production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an albumin nano freeze-dried powder preparation with tumor targeting and a preparation method thereof. Background technique [0002] There are many anti-tumor drugs from natural sources, such as taxanes, camptothecins, podophyllotoxins, harringtonines, etc., which have high anti-tumor activity in vitro, but due to their low water solubility, there is a lack of suitable preparations, thereby limiting the clinical application of these drugs. At present, insoluble antineoplastic drug injections commonly used in clinic are usually made of compound solvents, solubilizers, etc. Although the problem of drug administration is solved, the irritation or toxicity of the prescription is increased, and clinical application may cause allergic reactions. Medicinal properties, etc. [0003] For example, Paclitaxel is a natural product extracted from the bark of Taxus brevifolia, w...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K47/42A61P35/00
Inventor 张小宁郝艳丽孙敏敏
Owner TSINGHUA UNIV
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