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A kind of sirolimus nano-suspension and preparation method thereof

A technology of nanosuspension and sirolimus, which is applied in the field of medicine, can solve the problems of high cost, debris pollution of grinding machines, and restrictions on the popularization and use of sirolimus, and achieves low preparation cost and mild preparation method conditions Effect

Active Publication Date: 2016-06-29
SHANDONG XINRUI BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Sirolimus tablets currently on the market use grinding technology to reduce the particle size of sirolimus raw materials to the nanometer level and prepare them into nanosuspensions, which improves the oral absorption of sirolimus, but the cost of this technology Very high, and there will be debris contamination from the grinder, which limits the promotion and use of sirolimus

Method used

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  • A kind of sirolimus nano-suspension and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0019] Dissolve 0.1 g of sirolimus and 0.01 g of copovidone PVPS6300 in 50 mL of absolute ethanol, slowly add 0.01 g of PVPK-90 into 1000 mL of water, evaporate at 40°C, and evaporate the ethanol to obtain sirolimus The concentration of sirolimus is 0.1mg / ml for the nanosuspension. The average particle size of the sirolimus nanosuspension was measured, and the result was 490nm, and the suspension remained stable within 48h.

Embodiment 2

[0021] Dissolve sirolimus 0.1g and copovidone PVPS6300.05g in 50mL of 95% ethanol, slowly add 0.05g of PVPK-90 into 400mL of water, evaporate at 40°C, and evaporate the ethanol to obtain sirolimus The concentration of sirolimus is 0.3mg / ml for the nanosuspension. Measure the average particle diameter of sirolimus nanosuspension, the result is 105nm (the transmission electron microscope picture of sirolimus nanosuspension is shown in figure 1 ), the suspension remained stable within 48h.

Embodiment 3

[0023] Dissolve 0.1 g of sirolimus and 0.02 g of copovidone PVPS6300 in 20 mL of absolute ethanol, slowly add 0.02 g of PVPK-90 into 200 mL of water, evaporate at 40°C, and evaporate the ethanol to obtain sirolimus The concentration of sirolimus is 0.5mg / ml for the nanosuspension. The average particle size of the sirolimus nanosuspension was measured, and the result was 368nm, and the suspension remained stable within 48h.

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Abstract

The invention belongs to the technical field of medicines, and discloses a sirolimus nanoparticle suspension agent and a preparation method thereof. The sirolimus is poor in stability, small in solubility, and low in oral bioavailability, so that promotion and use of the sirolimus are restricted. The sirolimus nanoparticle suspension agent disclosed by the invention is characterized by containing sirolimus, copovidone PVPS630 and povidone PVPK-90; and the mass ratio of the sirolimus to the copovidone PVPS630 to the povidone PVPK-90 is (4-10) to (1-2) to (1-2). The sirolimus nanoparticle suspension agent disclosed by the invention is mild in preparation method, simple and controllable; and the sirolimus achieves high oral bioavailability.

Description

technical field [0001] The invention relates to a sirolimus nano-suspension and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Sirolimus, also known as rapamycin, is a macrolide antibiotic immunosuppressant with good antitumor effect. The solubility of sirolimus in water is very small, and the oral bioavailability is very low, which limits the efficacy of sirolimus. Therefore, it is very necessary to study effective dosage forms and techniques to improve the oral absorption of sirolimus. [0003] Nanosuspension refers to a dosage form in which drug particles are dispersed in an aqueous solution containing a stabilizer with a nanoscale particle size. And it can be solidified by post-treatment processes such as spray drying and freeze drying, and further prepared into various dosage forms according to different administration routes, such as tablets, pills, capsules, etc. Since the drug in the nanosuspension is in a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K31/436A61K47/32A61P37/06A61P35/00
Inventor 刘明录吴东颖冯建海张传鹏金海峰马洪华
Owner SHANDONG XINRUI BIOTECH CO LTD
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