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A kind of sirolimus nano drug composition and preparation method thereof

A nano-drug, sirolimus technology, which is applied in the directions of drug combinations, pharmaceutical formulations, and non-active components of medical preparations, can solve the problems of unsuitable large-scale industrialized continuous production, complex preparation processes, and high production costs, and achieves Easy to scale up and large-scale production, uniform particle size distribution, convenient transportation and storage

Active Publication Date: 2020-11-03
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, these methods have disadvantages such as complex preparation process and high production cost, or the obtained particle size is relatively large, so they are not suitable for large-scale industrialized continuous production.

Method used

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  • A kind of sirolimus nano drug composition and preparation method thereof
  • A kind of sirolimus nano drug composition and preparation method thereof
  • A kind of sirolimus nano drug composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] A preparation method of sirolimus nano drug composition, comprising the steps of:

[0050] S01. Sirolimus bulk drug (scanning electron microscope picture shown in Figure 1) and ethanol were prepared into 10 mL of sirolimus ethanol solution with a concentration of 10 mg / mL; polyvinylpyrrolidone and deionized water were prepared into 0.5 mg / mL mL of auxiliary material aqueous solution 200mL, at the same time add 5mg sodium lauryl sulfate to the auxiliary material aqueous solution;

[0051] S02. Turn on the external circulation supergravity rotating packed bed, adjust the speed to 2272rpm; turn on the feed pump, and simultaneously transport sirolimus ethanol solution and auxiliary material aqueous solution into the supergravity rotating packed bed for recrystallization reaction, and control the sirolimus The feeding rate of the ethanol solution is 2mL / min, the feeding rate of the aqueous solution of the drug excipient is 40mL / min, and the temperature of the control system ...

Embodiment 2

[0060] A preparation method of sirolimus nano drug composition, comprising the steps of:

[0061] S01. Sirolimus bulk drug and methanol were prepared into 10 mL of sirolimus ethanol solution with a concentration of 10 mg / mL; polyvinylpyrrolidone and deionized water were prepared into 200 mL of 0.5 mg / mL excipient aqueous solution;

[0062] S02. Turn on the external circulation supergravity rotating packed bed, adjust the speed to 2840rpm; turn on the feed pump, and simultaneously transport sirolimus ethanol solution and auxiliary material aqueous solution into the supergravity rotating packed bed for recrystallization reaction, and control the sirolimus The feed rate of ethanol solution is 5mL / min, the feed rate of pharmaceutical excipient aqueous solution is 50mL / min, and the temperature of the control system is 20°C to obtain the nano-suspension;

[0063] S03. Add mannitol and polyvinylpyrrolidone to the obtained nano-suspension, and then spray-dry to obtain a sirolimus nano...

Embodiment 3

[0066] A preparation method of sirolimus nano drug composition, comprising the steps of:

[0067] S01, sirolimus raw material drug and dimethyl sulfoxide are made into 10 mL of sirolimus dimethyl sulfoxide solution with a concentration of 50 mg / mL; polyvinylpyrrolidone and deionized water are made into 8 mg / mL excipients 200mL aqueous solution;

[0068] S02. Turn on the external circulation supergravity rotating packed bed, adjust the rotating speed to 2250rpm; turn on the feed pump, and simultaneously transport sirolimus ethanol solution and auxiliary material aqueous solution into the supergravity rotating packed bed for recrystallization reaction, and control the sirolimus The feed rate of ethanol solution is 10mL / min, the feed rate of pharmaceutical excipient aqueous solution is 200mL / min, and the temperature of the control system is 20°C to obtain the nano-suspension;

[0069] S03. Add mannitol and polyvinylpyrrolidone to the obtained nano-suspension, and then spray-dry ...

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Abstract

The invention discloses a sirolimus nano-drug composition. The composition is prepared from, by weight, 10-30wt% of sirolimus, 10-50wt% of an auxiliary material and 20-80% of a protective agent. The invention further discloses a preparation method of the sirolimus nano-drug composition. The particle size of the nano-drug composition is small, the nano-drug composition is narrow in distribution, the particle size is 50-400 nm, the dispersity is good, the application range is wide, and the sirolimus nano-drug composition can be applied to the preparation of tablets, capsules and oral solutions; the drug dissolution rate in 5 min is larger than or equal to 85%.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a sirolimus nano-preparation and a preparation method thereof. Background technique [0002] Sirolimus, chemical name: (3S, 6R,7E, 9R, 10R, 12R, 14S, 15E,17E,19E, 21S, 23S, 26R, 27R, 34aS)-9, 10, 12, 13 , 14, 21, 22, 23, 24, 25, 26,27, 32, 33, 34, 34a-hexadecahydro-9, 27-dihydroxy-3-[(1R)-2-[(1S, 3R , 4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethyl]-10, 21-dimethoxy-6,8,12,14, 20, 26-hexamethyl-23, 27-Epoxy-3H-pyrido[2,1-c][1,4]oxaazepine-1,5,11,28,29(4H, 6H, 31H)-pentanone . Molecular formula is C 51 h 79 NO 13 , the relative molecular mass is 914.19, the melting point is between 183-185°C, and its molecular structure is as follows: [0003] [0004] Sirolimus (SRL) is a new type of potent macrolide immunosuppressant, mainly used for the treatment of anti-rejection after organ transplantation, and its trade name is Rapamycin. As the third-generati...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K47/32A61K47/26A61K47/36A61K31/436A61P37/06
CPCA61K9/1623A61K9/1635A61K9/1652A61K31/436
Inventor 乐园沈煜栋陈鹏林谡轩
Owner BEIJING UNIV OF CHEM TECH