Preparation and application of polymer composition loaded with sirolimus compound or its derivative
A technology of sirolimus and polymers, which is applied in the field of nano-medicine preparation, can solve problems such as disapproval of using the human body, inability to release smoothly, and increased side effects
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[0045] Example 1
[0046] 100mg of methoxy polyethylene glycol-poly(ε-caprolactone) copolymer (MPEG 2000 -PCL 2000 ) And 15mg of sirolimus were dissolved in 3ml of absolute ethanol, the organic solvent was quickly removed under reduced pressure, and then 5ml of preheated water for injection was added, and under stirring conditions, the bundle was formed at 60°C and passed through a 0.22μm filter membrane. The filtrate was lyophilized to obtain a sample.
Example Embodiment
[0047] Example 2
[0048] 100mg of methoxy polyethylene glycol-polylactic acid copolymer (MPEG 2000 -PLA 1700 ) And 15mg of sirolimus were dissolved in 3ml of absolute ethanol, the organic solvent was quickly removed under reduced pressure, and then 5ml of preheated water for injection was added, and under stirring conditions, the bundle was formed at 60°C and passed through a 0.22μm filter membrane. The filtrate is lyophilized to obtain a sample, see figure 1 , See the transmission electron microscope map of nanomicelle solution figure 2 .
[0049] Twelve SD rats were randomly divided into two groups, each with 6 rats, namely Temsirolimus micelle sirolimus nanomicelle group and Temsirolimus injection Sirolimus injection group. The two groups of experimental animals were injected with sirolimus nanomicelles and sirolimus injection via tail veins respectively, and blood was collected at 0.083, 0.5, 1, 2, 4, 6, 8, 10, 12, 24 h after administration. , The blood sample was centrifug...
Example Embodiment
[0057] Example 3
[0058] 100mg of polycaprolactone-polyethylene glycol-polycaprolactone copolymer (PCL 800 -PEG 2000 -PCL 800 ) And 15mg of sirolimus were dissolved in 3ml of absolute ethanol, the organic solvent was quickly removed under reduced pressure, and then 5ml of preheated water for injection was added, and under stirring conditions, the bundle was formed at 60°C and passed through a 0.22μm filter membrane. The filtrate was lyophilized to obtain a sample.
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