تصنيع ودراسة المواصفات ل الأدوية المساعده المصممة ل حمض ترانزاميك و براسيتامول

هبه نعيم خميس غريب; hiba naeem khamees ghareeb

تصنيع ودراسة المواصفات ل الأدوية المساعده المصممة ل حمض ترانزاميك و براسيتامول

dc.contributor.advisor	رفيق قرمان
dc.contributor.author	هبه نعيم خميس غريب	ar
dc.contributor.author	hiba naeem khamees ghareeb	en
dc.contributor.examiner	د. صالح أبو لافي
dc.contributor.examiner	د. وليد صويلح
dc.date.accessioned	2018-10-07T11:30:51Z
dc.date.available	2018-10-07T11:30:51Z
dc.date.issued	2014-02-22
dc.description.abstract	Prodrug is a chemical devise in which the drug is covalently linked to a chemical moiety; this linked moiety will temporarily affect the physicochemical properties of the drug for increasing their usefulness or decreasing their toxicity. The prodrug should be converted to its active form by metabolic or/and chemical processes, conversion process involves metabolism by enzymes distributed throughout the body. These enzymes might either decrease the drug’s bioavailability, or a genetic polymorphisms might lead to variability in prodrug activation and thus affect the efficacy and safety of designed prodrug. In the past few decades computational chemistry methods have been utilized in calculating physicochemical and molecular properties of compounds. This tool can be used to design prodrugs that chemically (intramolecular processes) interconvert to their parent drugs without any involvement of enzyme catalysis. The release of the active drug is solely dependent on the rate limiting step of the intramolecular process. Based on DFT calculations four different tranexamic acid prodrugs and three different bitter less paracetamol prodrugs were designed, synthesized and characterized using FT-IR, 1H-NMR LCMS and their in vitro intra-conversion to their parent drugs revealed that the t1/2 was largely affected by the pH of the medium. For tranexamic acid ProD 1 the experimental t1/2 values in 1N HCl, buffer pH 2 and buffer pH 5 were 54 minutes, 23.9 hours and 270 hours, respectively. Tranexamic acid ProD 2 was readily converted in 1 N HCl and pH 2 while it was entirely stable at pH 5 and pH 7.4. On the other hand, tranexamic acid ProD 3 and Prod 4 were stable in all media studied. The experimental t1/2 values for paracetamol ProD 2 in pH 3 and pH 7.4 were 3 hours and 18 minutes respectively and for paracetamol ProD 3 it was 27 hours in pH 3 and 12 hours in pH 7.4. In vitro binding for paracetamol ProD 2 to bitter taste receptors revealed that this prodrug lacks any binding affinity and it was found not to have any bitter sensation. This suggests, that paracetamol ProD 2 can replace its parent drug, paracetamol, for the use asbitterless antipyretic drug for geriatrics and pediatrics.	en
dc.identifier.other	21112813
dc.identifier.uri	https://dspace.alquds.edu/handle/20.500.12213/1317
dc.language.iso	en_US
dc.publisher	AL-Quds University	en
dc.publisher	جامعة القدس	ar
dc.subject	العلوم الصيدلانية	ar
dc.subject	Pharmaceutical Sciences	en
dc.subject.other	رسالة ماجستير	ar
dc.subject.other	دراسات عليا	ar
dc.subject.other	Higher Studies	en
dc.subject.other	Master Thesis	en
dc.title	تصنيع ودراسة المواصفات ل الأدوية المساعده المصممة ل حمض ترانزاميك و براسيتامول	ar
dc.title	Synthesis and Characterization of Designed Tranexamic Acid and Paracetamol Prodrugs	en
dc.type	Thesis

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