Synthesis, Characterization and in Vitro Kinetics of Novel Atenolol Prodrugs

الموضوعات

علوم تطبيقية وتكنولوجية

الملخص

Prodrugs are substances administered inaninactive form that is then metabolized in the body into the corresponding active drug. The rationale behind administering prodrugs is to optimize the drug absorption, distribution, metabolism, and excretion. Since first described in the 1950s, prodrugs continue to be a fertile area of research. There are a number of small pharmaceutical/biotech companies dedicated to use prodrugs for the delivery of older but problematic drugs as well as to develop broad-based prodrug technologies for application to new and future drugsRecently Drug design become increasingly relies on computer modelingtechniques. In the past few decades computational chemistry methods have been utilizedin 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 three different atenolol prodrugs were designed, synthesized and characterized using FT-IR, 1H-NMR LC-MS and their in vitrointra-conversion to their parent drug, atenolol, revealed that the t1/2was largely affected by the pH of the medium. For atenolol ProD1in vitrokinetic study demonstrated that thet1/2was largely affected by the pH of the medium. The determined t1/2values in 1N HCl, buffer pH 3, and buffer pH 5 were 1.66, 3.73, and 168 hours, respectively. Andat pH 7.4 no intraconversionwas observed. On the other hand,atenolol ProD 2 was found to be readily intraconverted, but In the case of atenolol ProD 3no reaction was observed.

روابط وملفات

التعريف والنوع

رقم الوثيقة

0dd7881b-3eb8-419e-bc34-742078f7ba60

رقم العقد

0

نوع الوسائط

Crawler

نوع المحتوى

الرسائل العلمية

صيغة المصدر

رسائل ماجيستير

نوع الملف

pdf text

أسماء الملفات

1696432_1.pdf

بيانات النشر

ترجمة العنوان

تصنيع ودراسة المواصفات والحركية لدواء مساعد مصمم للأتنولول

ألقاب المؤلفين

[{"name_ar":"الاء احمد محمد قطيط","title_ar":"اعداد","title_en":"Preparation"},{"name_ar":"رفيق قرمان","title_ar":"اشراف","title_en":"Supervision"}]

اللغة

English

المصدر والدورية

اسم المصدر

Synthesis, Characterization and in Vitro Kinetics of Novel Atenolol Prodrugs

المحتوى والصفحات

عدد الصفحات

0

إشراف وإعداد

الإشراف

رفيق قرمان

الإعداد

الاء احمد محمد قطيط

الاقتباسات الببليوغرافية