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Rubescensin preparation and preparation method and use of same

A pharmaceutical preparation and solvent technology, applied in the field of oridonin A preparation and its preparation and application, can solve the problems of low drug loading efficiency, affecting the safety of injection preparations, etc.

Inactive Publication Date: 2009-09-23
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These carriers avoid the use of irritating solvents for solubilization, but these carriers generally have the problem of low drug loading efficiency, and a large number of surface-active excipients are required to disperse, emulsify or stabilize Oridonin. At the same time, A large amount of oil and lipid components are used in the process of preparation, sterilization and storage, which are prone to produce harmful substances due to oxidation, hydrolysis, etc., especially lysophospholipids, which significantly affect the safety of injection preparations

Method used

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  • Rubescensin preparation and preparation method and use of same

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preparation example Construction

[0036] In a preferred embodiment, the preparation method according to the diterpene drug preparation of the present invention comprises the following steps:

[0037] Use organic solutions containing diterpenoids and aqueous solutions containing surface active substances to prepare oil-in-water emulsions;

[0038] The organic solvent is removed, the diterpene drug and the surface active substance are self-assembled to form a micelle-like self-assembled structure, and the diterpene drug injection is prepared.

[0039] Optionally, in the above method, some surface active substances may also be added to the organic solution of the diterpene drug, so as to enhance the dissolution of the diterpene drug.

[0040] In some embodiments, the organic solvent can be selected from water immiscible or low miscible organic solvents or mixtures thereof, preferably selected from one or more of the following: chloroform, diethyl ether, dichloromethane, ethyl acetate Esters and their mixtures. ...

Embodiment 1

[0070] Embodiment 1 Oridonin A Injection

[0071] The concentration of oridonin was 1 mg / ml, polysorbate and pluronic F68 were selected as surface active substances, the total concentration was 4 mg / ml, and normal saline was used as solvent. The specific preparation method is as follows: dissolve 100 mg oridonin and 100 mg dehydrated polysorbate in 30 ml chloroform as the oil phase; dissolve 300 mg pluronic F68 in deionized water, and dilute to 100 ml as the water phase. Mix the two phases of oil and water isothermally at 40°C, use a tissue homogenizer with a rotation speed of 10,000rpm to mix for 3 minutes, and quickly remove chloroform by rotary evaporation in a water bath at 40°C, and then you can obtain a clear and clear Oryx chinensis with a concentration of 1mg / ml A drug injection, the average particle size of drug-loaded micellar particles is 150nm.

[0072] Take 2ml of the prepared 1mg / ml Oridonin A injection, put it into a dialysis bag with a molecular weight cut-off...

Embodiment 2

[0074] Embodiment 2 Rubescensine A Injection

[0075] The concentration of oridonin was 0.5 mg / ml, Pluronic F68 and polyoxyethylene hydrogenated castor oil were selected as surface active substances, the total concentration was 8 mg / ml, and deionized water was used as solvent. The specific preparation method is as follows: dissolve 50 mg oridonin and 2 mg polyoxyethylene hydrogenated castor oil in 40 ml chloroform as the oil phase; dissolve 6 mg Pluronic F68 in deionized water, and make it to 100 ml as the water phase Mutually. The two phases of oil and water were mixed isothermally at 40° C., and mixed for 3 minutes using a tissue homogenizer with a rotating speed of 10,000 rpm. In a water bath at 50°C, the chloroform was quickly removed with nitrogen gas. A clear oridonin injection with a concentration of 0.5 mg / ml and an average diameter of 120 nm can be obtained.

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Abstract

The invention generally relates to a diterpene pharmaceutical preparation and preparation method and use of the same. Particularly, the invention discloses a pharmaceutical preparation, which comprises diterpenes such as the rubescensin and amphiphilic surfactants, and any other pharmaceutically acceptable carriers and / or excipients. In addition, the invention also relates to the preparation method and the use of the pharmaceutical preparation in disease treatment.

Description

technical field [0001] The present invention generally relates to diterpene pharmaceutical preparations and their preparation methods and uses. More specifically, the present invention discloses a pharmaceutical preparation, which contains diterpene drugs and amphiphilic surface active substances, and optionally other pharmaceutically acceptable carriers and / or excipients. The invention furthermore relates to a process for the preparation of said pharmaceutical preparation and its use in the treatment of diseases. Background technique [0002] Oridonin is a natural organic compound of kaurene diterpenoids isolated from the Lamiaceae plant, which has strong anti-tumor activity and is effective for a variety of metastatic tumors. It is used for the treatment of liver cancer, esophageal cancer, pancreatic cancer, etc. A new study found that Rubescensine A also has a good effect on the treatment of acute leukemia (a drug for the treatment of M2 type acute myeloid leukemia and ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/35A61P35/00
Inventor 徐宇虹魏晓慧
Owner SHANGHAI JIAO TONG UNIV
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