A kind of galantamine nano-brain targeted drug for nasal administration and preparation method thereof
A galantamine and brain-targeting technology, which is applied in the field of medicine, can solve problems such as inaccessibility of drugs, achieve protection and promote regeneration, have good biosorption, and improve brain-targeting effects
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Embodiment 1
[0043] Preparation of nano-brain-targeted drug for intranasal administration of galantamine
[0044]The present embodiment provides a preparation method for the nasal administration of the anti-senile dementia targeted drug of the present invention, which specifically includes the following steps:
[0045] 1) Under a nitrogen atmosphere, the acetic acid-sodium acetate buffer solution of 10 mol of chitosan and 1 mol of potassium periodate were stirred and reacted at 4 °C for 48 h, and then 1 mol of ethylene glycol solution was added to the solution to stop the reaction, and the product was concentrated by rotary evaporation. Dialyzed in 1mol / L NaCl aqueous solution and deionized water for 48h to remove impurities, and the final product was freeze-dried to obtain hydroformyl chitosan (CS-CHO);
[0046] 2) Dissolve 1 mol of hydroformyl chitosan (CS-CHO) in 3 mol of DMSO, then add 1 mol of sodium chlorite, stir and react for 24 h, the product is concentrated by rotary evaporation ...
Embodiment 2
[0049] In vitro drug release study of galantamine loaded with chitosan
[0050] The drug was placed in a dialysis bag, and samples were periodically taken from the release medium for analysis of drug content. The specific process is as follows: freeze-dry the obtained drug solution, accurately weigh a certain amount, and then disperse it in 10ml of artificial cerebrospinal fluid by ultrasonic, put it in a dialysis bag (MWCO=12,000), put it in a 100ml conical flask, and add 40ml of artificial cerebrospinal fluid at a constant temperature In the shaker (set temperature 37°C, rotating speed 60r / min), sample 2ml at intervals, and add the same amount of release medium. This method can ensure that the polymer micelles remain in the dialysis bag, making the determination of the drug content more accurate.
[0051] The result is as figure 1 As shown, the release rate of galantamine hydrobromide solution is relatively fast, and it is basically released within 12 hours, and the cumula...
Embodiment 3
[0052] Example 3 Brain targeting evaluation
[0053] Healthy rats were taken and randomly divided into 4 groups, namely galantamine original drug group (original drug group); nano drug-loaded micelle group (experimental group); blank carrier micelle (blank group); normal saline (negative group) control group). 24h before the experiment, fasting but not water.
[0054] The rats were anesthetized by intraperitoneal injection of 2% pentobarbital sodium solution (40m / kg), supine and fixed on the rat board, the neck skin and muscles were incised, the trachea, esophagus, esophagus and trachea were separated, and tracheal intubation was performed. The upper segment is ligated to avoid the loss of the drug solution to the gastrointestinal tract after nasal administration. During the whole experiment, the anesthesia was supplemented timely to ensure that the rats were always under anesthesia.
[0055] Thirty minutes after the operation, the rats in the nasal administration group wer...
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