Rapamycin nano slow-release agent and preparation method thereof

A technology of rapamycin and sustained release agent, applied in the field of rapamycin nano sustained release agent and its preparation, which can solve the problems of insufficient targeting, fast natural degradation rate, and low concentration of rapamycin at the site of action , to achieve the effect of small blood vessel risk, good tumor targeting effect, stable encapsulation efficiency and drug loading

Active Publication Date: 2019-12-31
严鹏科
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Rapamycin is a hydrophobic drug and cannot be directly used for injection. It needs to be dissolved in a certain organic solvent before it can be injected, which is likely to cause adverse effects on the human body; the bioavailability of rapamycin in the body is very low, and it is easy to cause it to fail to reach the disease site. problem that has expired
[0007] Currently on the market, phospholipids or cholesterolones are used as the nano sustained-release carrier of rapamycin. Fast, so that rapamycin reaches the site of action with low concentration and insufficient targeting

Method used

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  • Rapamycin nano slow-release agent and preparation method thereof
  • Rapamycin nano slow-release agent and preparation method thereof
  • Rapamycin nano slow-release agent and preparation method thereof

Examples

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preparation example Construction

[0043] The preparation method of this rapamycin nano-sustained release agent, comprises the following steps:

[0044] 1) adding the rapamycin bulk drug and the soluble polymer carrier to the organic solvent to form an organic phase;

[0045] 2) Inhale the organic phase into the syringe, drop it into the aqueous phase liquid at a rate of 1-10 drops per minute, and stir at room temperature for 30min-3h;

[0046] 3) reclaiming the organic solvent under reduced pressure;

[0047] 4) Centrifuge for 5-120min, take the supernatant, and filter through a 0.22-0.45μm filter membrane to obtain a micellar solution;

[0048] 5) Freeze-drying the micellar solution to obtain the rapamycin nano-sustained release agent.

[0049] During the preparation process of the rapamycin nano-sustained-release agent, through the mutual dissolution process of the organic phase and the aqueous phase liquid, by stirring and dispersing, the micelles with small particle sizes are formed by physical force; R...

Embodiment 1

[0053] A rapamycin nano-sustained-release agent, made of the following components: 5mg rapamycin, 10mg mPEG-PLA block polymer, 1mL acetone and 50mL PBS buffer;

[0054] Its preparation method comprises the following steps:

[0055] 1) adding rapamycin bulk drug and mPEG-PLA block polymer into acetone to form an organic phase;

[0056] 2) Inhale the organic phase into the syringe, add dropwise at a rate of 5 drops per minute to the stirring PBS buffer at 500 rpm, and stir at room temperature at 600 rpm for 60 min;

[0057] 3) Recover the organic solvent under reduced pressure at 40°C;

[0058] 4) Centrifuge at 4000r / min for 30min, take the supernatant, filter and sterilize through a microporous membrane with a pore size of 0.22μm to obtain a micellar solution;

[0059] 5) Freeze-drying the micellar solution to obtain the rapamycin nano-sustained release agent.

Embodiment 2

[0061] A rapamycin nano-sustained-release agent, made of the following components: 5mg rapamycin, 20mg mPEG-PLA block polymer, 1mL acetone and 50mL PBS buffer;

[0062] Its preparation method comprises the following steps:

[0063] 1) adding rapamycin bulk drug and mPEG-PLA block polymer into acetone to form an organic phase;

[0064] 2) Inhale the organic phase into the syringe, add dropwise at a rate of 5 drops per minute to the stirring PBS buffer at 500 rpm, and stir at room temperature at 600 rpm for 60 min;

[0065] 3) Recover the organic solvent under reduced pressure at 40°C;

[0066] 4) Centrifuge at 5000r / min for 30min, take the supernatant, filter and sterilize through a microporous membrane with a pore size of 0.22μm to obtain a micellar solution;

[0067] 5) Freeze-drying the micellar solution to obtain the rapamycin nano-sustained release agent.

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Abstract

The present invention discloses a rapamycin nano slow-release agent. The rapamycin nano slow-release agent is made of the following raw materials in parts by weight: 1 part of rapamycin, 0.5-20 partsof a soluble high molecular polymer carrier, 40-200 parts of an organic solvent and 400-20,000 parts of an aqueous phase solution. The present invention also provides a preparation method of the rapamycin nano slow-release agent. The rapamycin nano slow-release agent has a nano micellar structure and particle size between 10-200 nm, and is low in risks to blood vessels. The half-life of the rapamycin nano slow-release agent in blood can be as high as 50 hours or more, the rapamycin nano slow-release agent can directly reach affected areas of tumors, is subjected to continuous administration and has a tumor regression rate of 50%.

Description

technical field [0001] The invention relates to the technical field of rapamycin preparations, in particular to a rapamycin nano sustained-release agent and a preparation method thereof. Background technique [0002] Tumor Cancer has become the number one killer that endangers human health. Although there are endless ways to treat tumors, the living conditions of most patients have not been greatly improved. Among the various treatment methods for tumors, chemotherapy is still the most commonly used option. Although chemotherapeutic drugs are widely used, their therapeutic effect on solid tumors is uncertain. The fundamental problem is that traditional chemotherapeutic drugs cannot reach an effective therapeutic concentration in the tumor site or cannot maintain a sufficient duration of action. Moreover, traditional chemotherapeutic drugs indiscriminately kill normal cells, resulting in a variety of toxic and side effects. The effect of chemotherapy drugs depends not only ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/19A61K31/436A61K47/10A61K47/32A61K47/34A61P35/00A61P37/06
CPCA61K9/1075A61K9/19A61K31/436A61K47/10A61K47/32A61K47/34A61P35/00A61P37/06
Inventor 严鹏科
Owner 严鹏科
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