Department of Pharmacy,
Al-Quds University, Jerusalem, Israel
Professor Rafik Karaman is currently a distinguished professor of pharmaceutical sciences, College of Pharmacy, Al-Quds University, Jerusalem, Palestine and adjunct professor at Basilicata University, Italy. He received his Ph.D. degree in pharmaceutical/bioorganic chemistry from the Hebrew University in 1987, his MS degree in Pharmaceutical Sciences from the Hebrew University in 1983, and his bachelor?s degree in Pharmacy from the Hebrew University in 1981. He was an Assistant Professor at the University of Toledo and University of California at Santa Barbara for 5 years where he worked with Professor T.C. Bruice in the bioorganic chemistry field. Professor Karaman is broadly interested in the design and synthesis of prodrug systems to be used for the delivery of certain drugs that have poor water solubility or/and have low bioavailability as well as synthesis of prodrugs for masking the bitter sensation of commonly used drugs. The prodrug design is executed using ab initio, DFT, semiempirical, molecular mechanics as well as molecular dynamics and conformational dynamics methods. The overarching goal of Karaman?s research activities is to establish a method for obtaining prodrugs that their interconversion rates will be controlled or programmed by the chemical features of the linker (promoiety) attached to their active parent drugs. Professor Karaman has more than 160 peer-reviewed manuscripts and book chapters; 120 of them were published in the recent 8 years. He is currently an editor and an editorial board member of 50 international journals in the areas of pharmaceutical sciences.
1. Design, synthesis, characterization and in vitro and in vivo kinetics of pro-prodrug systems to be used for the delivery for certain drugs that have poor water solubility or/and have low bioavailability using ab initio, DFT, semiempirical, molecular mechanics as well as molecular dynamics and conformational dynamics methods. The in-vitro studies will be conducted in media mimics that of stomach (pH 1.2), intestine (pH 6.8) and blood circulation (pH 7.4). The in-vivo studies will be conducted in certain animals and the pharmacokinetic parameters will be determined using advanced technology such as, HPLC and LC-MS.
2. Design and synthesis of linkers to be used for masking bitter taste of drugs that contain a hydroxyl or amine groups (antimalarial, anti-hypertension, anti-bleeding, antibacterial and anticancer drugs) using DFT calculation methods. The synthesis will be carried out using standard organic methods and the kinetic rates of the intramolecular processes will be determined by HPLC monitoring.
3. Design and synthesis of bitter taste antagonists for inactivation of the bitter taste receptor 14.The design will be accomplished using molecular orbital and molecular mechanics methods.
4. Pharmaceuticals removal from wastewater using clay micelle complex, hollow fiber, spiral wounds, charcoal and other adsorbents.
5. Pharmaceuticals removal from wastewater using photodegradation methods such as light/TiO2.
6. Stability of Pharmaceuticals in wastewater and isolation and characterization of degradation products (metabolites). Currently, my group is working on the synthesis of a variety of prodrugs for commonly used drugs. The goal is to enhance the bioavailability and mask the bitterness of those drugs. Among the selected drugs: cephalexin, amoxicillin, azithromycin, aciclovir, dopamine, paracetamol, atenolol, mefenamic acid, diclofenac, naproxen, alendronate, raloxifene, guaifenesin, tranexamic acid and 6-aminocaproic acid. The synthesis of the prodrugs will be followed by in-vitro and in-vivo kinetic studies. The expected time to complete this mission will be about 10 years.