Application of Amphiphilic Polymers in the Preparation of Oral Drugs
An amphiphilic polymer and pharmaceutical preparation technology, which is applied in the directions of pharmaceutical formulations, medical preparations of inactive ingredients, and emulsion delivery, etc., can solve the problem of not mentioning the oral absorption effect of nanomicelles, the complex synthesis process, and the increased process difficulty. and other problems, to achieve the effect of improving transmembrane transport efficiency, simple preparation process, and promoting oral absorption.
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preparation example Construction
[0061]
[0062] The pharmaceutical preparation of the present invention is a peptide transporter PepT1 targeting pharmaceutical preparation of intestinal epithelial cells, and its preparation method comprises the following steps: (1) preparation of amphiphilic polymer; (2) preparation of nano micelles.
[0063] In step (1), vitamin E-succinate VES is esterified with polyethylene glycol PEG to obtain polyethylene glycol ester TPGS with an ester group at one end; the polyethylene glycol ester TPGS with amino The protected amino acid undergoes a condensation reaction; then the protecting group is deprotected to obtain the amphiphilic polymer; wherein, the amino acid is selected from one or both of valine and phenylalanine.
[0064]The esterification reaction can be carried out in an organic solvent such as dichloromethane. The catalyst for the esterification reaction can be selected from one or both of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride EDCl or 4-dimeth...
preparation example 1-L
[0078] Preparation example 1-L-valine-polyethylene glycol vitamin E succinate
[0079]
[0080] Vitamin E succinate (VES, 3 mmol) was dissolved in 30 mL of dichloromethane (DCM), then 1-ethyl-3(3-dimethylpropylamine) carbodiimide (EDCl, 6 mmol) and 4-di Dimethylaminopyridine (DMAP, 3 mmol), magnetically stirred for 1 h in an ice bath. Then a DCM solution (5 mL) of PEG (n is 44, molecular weight 2000, 3 mmol) was added, reacted for 24 h at 30° C. under nitrogen protection, and the sample was purified by column chromatography to obtain the intermediate product TPGS. Under the catalysis of EDCl (4mmol) and DMAP (2mmol), TPGS (2mmol) and benzyloxycarbonyl valine (Cbz-valine, 2mmol) were reacted at 30°C for 12h, and purified by column chromatography to obtain benzyloxycarbonyl valine Acid-PEG-VES, followed by palladium carbon / H 2 Under the action, the benzyloxycarbonyl group is removed to obtain the target product L-valine-polyethylene glycol vitamin E succinate (Val-TPGS). ...
preparation example 2-L
[0081] Preparation example 2-L-phenylalanine-polyethylene glycol vitamin E succinate
[0082]
[0083] Vitamin E succinate (VES, 3 mmol) was dissolved in 30 mL of dichloromethane (DCM), then 1-ethyl-3(3-dimethylpropylamine) carbodiimide (EDCl, 6 mmol) and 4-di Dimethylaminopyridine (DMAP, 3 mmol), magnetically stirred for 1 h in an ice bath. Then a DCM solution (5 mL) of PEG (n is 44, molecular weight 2000, 3 mmol) was added, reacted for 24 h at 30° C. under nitrogen protection, and the sample was purified by column chromatography to obtain the intermediate product TPGS. Under the catalysis of EDCl (4mmol) and DMAP (2mmol), TPGS (2mmol) and benzyloxycarbonylphenylalanine (Cbz-phenylalanien, 2mmol) were reacted at 30°C for 12h, and purified by column chromatography to obtain benzyloxycarbonylbenzene Alanine-PEG-VES, followed by palladium carbon / H 2 Under the action, the benzyloxycarbonyl group is removed to obtain the target product L-phenylalanine-polyethylene glycol vi...
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