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العنوان
Effect of some pharmaceutical excipients and neutriceuticals on oral absorption of acyclovir in rabbits /
المؤلف
Shatla, Ali Ali Ali.
هيئة الاعداد
باحث / Ali Ali Shatla
مشرف / Omar Y. Mady,
مشرف / Yusuf Ahmed Haggag
مشرف / لايوجد
الموضوع
Pharmaceutical Science.
تاريخ النشر
2023.
عدد الصفحات
194 p. :
اللغة
الإنجليزية
الدرجة
الدكتوراه
التخصص
الصيدلة ، علم السموم والصيدلانيات
تاريخ الإجازة
13/8/2023
مكان الإجازة
جامعة طنطا - كلية الصيدلة - التكنولوجيا الصيدلية
الفهرس
Only 14 pages are availabe for public view

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from 211

Abstract

Acyclovir is a BCS class III drug that has high solubility and low permeability. Acyclovir is an antiviral drug used for the treatment of herpes simplex and varicose zoster. D-glucose is reported as a permeation enhancer for BCS class III drugs. It is the most commonly occurring isomer of glucose in nature. Honey is one of the public foods. Therefore, it was tried to study the enhancement of honey on the absorption of acyclovir in vivo in comparison with pure D-glucose. The effect was studied in albino rabbits using a 2-way parallel pharmacokinetic study from a hypo-osmotic solution containing the drug with different additives. The order of bioavailability enhancement of the additives to the drug can be arranged according to the following: honey (10.09 folds) > D- glucose-NaCl (8.33 folds)> honey-NaCl (7.77folds) > D-glucose (5.63 folds). D-glucose has been transported actively through the transcellular pathway (SGLT1) producing energy that led to a contraction of the prejunctional actomyosin ring resulting in the widening of the paracellular pathway. More widening of the paracellular pathway could be expected by using honey as a result of its content of glucose, fructose, and sucrose. The winding effect of the additives was histologically studied using light staining and a transmission microscope. D-glucose showed very thin tight junctions between closely adjacent enterocytes while D-glucose with NaCl revealed several enterocytes with one widely dilated tight junction and loosening and thinning of the others. Honey treated group demonstrated loosening and wide dilatation of the tight junctions. The analytical and histological evidence support the bioavailability enhancement of D-glucose to the drug which will be more pronounced from food sources. D-glucose and honey proved as permeation enhancers for acyclovir. Therefore, a pharmaceutical technology process of the drug with its permeation enhancers was carried out and the actual drug contents were determined using validated HPLC method. The drug bioavailability from its spray dried products was studied in rabbits compared to the pure drug. The drug bioavailability from its sprayed products was increased by 9.15, 7.54, 7.10 and 5.09 folds on using honey, D-glucose-NaCl, honey-NaCl or D-glucose respectively. The histological study at the end of the experiment of the rabbit small intestine showed a widening of the drug absorption pathway (paracellular pathway) which is consent with the order of the drug permeability enhancement by its permeation enhancer. The drug spray dried products were pulverized, and the micromeritics properties were studied and then compressed into tablets. The pharmacopeial and non- pharmacopeial quality control tests of the tablets were carried out indicating the complying of the tablets with required standard limits. The drug release showed complete drug release with the absence of burst effect.