A stimuli-responsive amphiphilic cyclodextrin polymer carrier, its preparation and its application in the preparation of sustained and controlled release drugs
A cyclodextrin polymer, stimuli-responsive technology, which can be used in drug combinations, inactive components of polymer compounds, microcapsules, etc. Issues such as drug release
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Embodiment 1
[0113] (1) Protection of the 6-hydroxyl group of cyclodextrin
[0114] In DMF, 14.5g of tert-butyldimethylchlorosilane, 9g of cyclodextrin and 5mL of triethylamine were reacted at 30°C for 96 hours to protect the 6-position primary alcohol of cyclodextrin, and then the solvent was distilled off under reduced pressure, and the silica gel column layer The product was purified by gradient elution with methanol and dichloromethane, and dried in vacuum to obtain tert-butyldimethylsiloxycyclodextrin a;
[0115] (2) Alkylation of 2 and 3 hydroxyl groups of cyclodextrin
[0116] Take 2 g of a and react with 0.5 g of sodium hydride in anhydrous DMF for 24 hours, then add 0.21 mL of dodecane bromide, and react for 3 days at 30 ° C; then add 0.5 g of sodium hydride in anhydrous DMF, and react After 24 hours, 0.21 mL of dodecane bromide was added and reacted at 30° C. for 2 days. Quenching with methanol, distilling off the solvent under reduced pressure, purifying the product by gel chr...
Embodiment 2
[0136] Compared with Example 1, the main difference is that the hydrophobic segment is an ethyl group, and the specific operations are as follows:
[0137] (1) Protection of the 6-hydroxyl group of cyclodextrin
[0138] In DMF, 9g of triphenylchloromethane, 5g of cyclodextrin and 5mL of triethylamine were reacted at 70°C for 96 hours to protect the 6-position primary alcohol of cyclodextrin, and then the solvent was distilled off under reduced pressure, and methanol was used for silica gel column chromatography. The product was purified by gradient elution with dichloromethane, and dried in vacuo to obtain triphenylmethyl ether-cyclodextrin a;
[0139] (2) Alkylation of 2 and 3 hydroxyl groups of cyclodextrin
[0140] Take 2g of a and react with 0.5g sodium hydride in anhydrous DMF for 24 hours, then add bromoethane 0.15mL, and react at 30°C for 3d; then add 0.5g sodium hydride in anhydrous DMF, react for 24h, After that, 0.15 mL of ethyl bromide was added, and the reaction ...
Embodiment 3
[0147] Compared with Example 1, the main difference is that some 2,3-positions modify the hydrophobic segment, and the specific operations are as follows:
[0148] (1) Protection of the 6-hydroxyl group of cyclodextrin
[0149] In DMF, 14.5g of tert-butyldimethylchlorosilane, 9g of cyclodextrin and 5mL of triethylamine were reacted at 70°C for 96 hours to protect the 6-position primary alcohol of cyclodextrin, and then the solvent was distilled off under reduced pressure, and the silica gel column layer The product was purified by gradient elution with methanol and dichloromethane, and dried in vacuum to obtain tert-butyldimethylsiloxycyclodextrin a;
[0150] (2) Alkylation of 2 and 3 hydroxyl groups of cyclodextrin
[0151] Take 2 g of a and react fully with 0.5 g of sodium hydride in anhydrous DMF, then add 0.21 mL of bromododecane, react at 30 ° C for 24 h, quench with methanol, remove the solvent by distillation under reduced pressure, and use gel chromatography Purify t...
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