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Profarmaco: un approccio strategico in continua crescita in campo farmaceutico

Magliocca, Salvatore (2015) Profarmaco: un approccio strategico in continua crescita in campo farmaceutico. Doctoral Thesis.

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Abstract

During my PhD course I synthesized galactosylated prodrugs of indomethacin, flurbiprofen, ketoprofen, mefenamic acid, diclofenac and ibuprofen. In the synthesis of these prodrugs, when possible, was used a ionic liquid exactly 1-butyl-3-methylimidazolium hexafluorophosphate ([bmim][PF6]) in order to reduce pollutants and improve the yields. Then for each prodrug were studied chemical and enzymatic stability (human plasma) in vitro, in order to perform pharmacological experiments in vivo. All the prodrugs showed pharmacological and toxicological profile better than parent drugs, indeed a remarkable reduction of ulcerogenicity was found. I worked also at another project aiming to enhance concentration of mycophenolic acid, an immunosuppressant, in lymphatic vessels. In this case was used 1,3-dipalmitoil diglyceride as vector linked, via different spacers, to parent drug. Lymphatic transport studies were performed on synthesized prodrugs evaluating the lymphatic concentration of parent drug; the experimental results showed that the amount of mycophenolic acid released in the lymphatic vessels by prodrugs is higher than the immunosuppressant itself.

Item Type:Doctoral Thesis
ID Code:10498
Contributors:Boatto, Gianpiero
Publisher:Università degli studi di Sassari
Uncontrolled Keywords:Galactose, prodrug, ionic liquids, controlled release, ulcerogenicity
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01-a Nuovi Dipartimenti dal 2012 > Chimica e Farmacia
Cicli, scuole e corsi:Ciclo 27 > Scienze e Tecnologie chimiche > Scienze farmaceutiche
Deposited On:18 Mar 2015 10:06

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