Rapamycin slow-release dosage form as well as preparation method, rapamycin slow-release injection and application

A slow-release injection, rapamycin technology, applied in the field of medicine, can solve the problems of unmet medical needs in the treatment of OA, short drug retention time, repeated injections, etc., to achieve long retention time in the body, reduce adverse reactions and safety Effects of Accident, Relief and Treatment of Osteoarthritis

Inactive Publication Date: 2018-11-09
白晓春
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, there is a high unmet medical need for the treatment of OA
For the treatment of OA drugs, such as rapamycin, it is a hydrophobic drug and cannot be injected directly. It needs to be dissolved in an organic solvent such as DMSO before injection. However, organic solvents are toxic and will bring inevitable side effects to patients.
In addition, there is also the problem that the drug retention time is short and multiple repeated injections are required

Method used

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  • Rapamycin slow-release dosage form as well as preparation method, rapamycin slow-release injection and application
  • Rapamycin slow-release dosage form as well as preparation method, rapamycin slow-release injection and application
  • Rapamycin slow-release dosage form as well as preparation method, rapamycin slow-release injection and application

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preparation example Construction

[0071] The present invention also provides the preparation method of the above-mentioned sustained-release dosage form of rapamycin, comprising:

[0072] The formulation amount of rapamycin and organic solution of slow-release material is provided, mixed evenly with emulsifier, and the organic solvent is removed to obtain the rapamycin sustained-release dosage form.

[0073] The preparation method of the above-mentioned rapamycin sustained-release dosage form provided by the present invention is simple, convenient and fast, and the prepared rapamycin sustained-release dosage form has good stability, long residence time in the body, good drug release, and high bioavailability. It is beneficial to popularization and application of industrialized production.

[0074] In some preferred embodiments, the boiling point of the organic solvent is no higher than 50°C.

[0075] The boiling point of the organic solvent is not higher than 50°C, which can ensure that in the subsequent remo...

Embodiment 1

[0098] This embodiment provides a sustained-release dosage form of rapamycin, including rapamycin and poly(lactic-co-glycolic acid) (PLGA 50 / 50) at a mass ratio of 1:20. It is prepared by the following method to obtain microspheres:

[0099] (1) Dissolve 20mg PLGA and 1mg rapamycin in 1mL dichloromethane (DCM);

[0100] (2) Prepare 6mL of 1% polyvinyl alcohol (PVA) solution and dissolve it in ultrapure water;

[0101] (3) Pour (1) into (2), and stir magnetically for 30 minutes;

[0102] (4) Sonicate (3) for 4 minutes;

[0103] (5) under magnetic stirring, naturally evaporate the organic solvent in (4);

[0104] (6) centrifuge (5) at room temperature for 20min, 12000g;

[0105] (7) Collect the microspheres, wash them twice with ultrapure water, and freeze-dry them for storage;

[0106] (8) Prepare a 10 mg / mL injectable PLGA-coated rapamycin dosage form, wherein the rapamycin content is 450 μg / mL.

Embodiment 2

[0108] This embodiment provides a sustained-release dosage form of rapamycin, comprising rapamycin and poly(lactic-co-glycolic acid) (PLGA 50 / 50) at a mass ratio of 1:10. It is prepared by the following method to obtain microspheres:

[0109] (1) Dissolve 10 mg PLGA and 1 mg rapamycin in 1 mL dichloromethane (DCM);

[0110] (2) Prepare 6mL of 1% polyvinyl alcohol (PVA) solution and dissolve it in ultrapure water;

[0111] (3) Pour (1) into (2), and stir magnetically for 30 minutes;

[0112] (4) Sonicate (3) for 4 minutes;

[0113] (5) under magnetic stirring, naturally evaporate the organic solvent in (4);

[0114] (6) centrifuge (5) at room temperature for 20min, 12000g;

[0115] (7) Collect the microspheres, wash them twice with ultrapure water, and freeze-dry them for storage;

[0116] (8) Prepare a 10 mg / mL injectable PLGA-coated rapamycin dosage form, wherein the rapamycin content is 600 μg / mL.

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Abstract

The invention provides a rapamycin slow-release dosage form as well as a preparation method, a rapamycin slow-release injection and application, which relate to the technical field of medicines. The rapamycin slow-release dosage form comprises rapamycin and a slow-release material in a mass ratio of 1: (10 to 50). The rapamycin slow-release dosage form is high in drug content, capable of realizinga slow-release and controlled-release effect of a drug, and capable of effectively alleviating and treating osteoarthritis. The preparation method of the rapamycin slow-release dosage form provided by the invention is simple to operate, and the prepared rapamycin slow-release dosage form is good in stability, long in retention time in a human body, high in bioavailability, and favorable for the popularization and application of industrialized production. The rapamycin slow-release injection can be directly injected without using an organic solvent, can reduce the adverse reaction and safety accidents caused by the organic solvent, is long in retention time in the human body, does not need to be repeatedly injected for multiple times, can reduce the cost of administrating the drug for multiple times, and can alleviate the pain of a patient and the irritation.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a rapamycin sustained-release dosage form and a preparation method, a rapamycin sustained-release injection and its application. Background technique [0002] Osteoarthritis (OA), also known as degenerative arthritis, is the most prevalent disease among the elderly and the obese. OA is a disease of the joints, but unlike rheumatoid arthritis (RA), the disease is not systemic and usually affects only one or a few joints. This disease results in total destruction of the articular cartilage, hardening of the underlying bone and formation of osteophytes, resulting in loss of movement and pain. The end result is often the need for total joint replacement. [0003] The World Health Organization survey found that 10% of men and 18% of women in the world suffer from OA to varying degrees. In Asia, 1 out of every 6 people suffers from OA. At present, there are more than 100 million OA ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/10A61K31/436A61K47/32A61K47/34A61K47/36A61P19/02A61P29/00
CPCA61K9/0019A61K9/08A61K9/10A61K31/436A61K47/32A61K47/34A61K47/36A61P19/02A61P29/00
Inventor 白晓春崔忠凯杨潇李凯张海严
Owner 白晓春
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