Search In this Thesis
   Search In this Thesis  
العنوان
Formulation and evaluation of some self-emulsifying drug delivery systems containing certain drugs /
المؤلف
Eltobshi, Amal Ahmed Gamal.
هيئة الاعداد
باحث / أمل أحمد جمال الطوبشى
مشرف / أحمد طلعت إبراهيم نوح
مشرف / جلال محمود عبد الغنى السيد
مشرف / إلهام عبد المنعم السعيد محمد
الموضوع
Osteoarthritis. Diacerein. Self-nanoemulsifying.
تاريخ النشر
2019.
عدد الصفحات
online resource (150 pages) :
اللغة
الإنجليزية
الدرجة
ماجستير
التخصص
الصيدلة ، علم السموم والصيدلانيات
تاريخ الإجازة
1/1/2019
مكان الإجازة
جامعة المنصورة - كلية الصيدلة - الصيدلانيات
الفهرس
Only 14 pages are availabe for public view

from 191

from 191

Abstract

Background: Effective treatment of osteoarthritis necessitates symptomatic relief and hindrance of joint degeneration progression. Non-steroidal anti-inflammatory drugs permit symptomatic relief only and can cause mucosal injury in the gut. Before absorption, diacerein (DCN) is converted into rhein that counteracts cartilage degeneration without affecting prostaglandin production. Yet, low DCN solubility and laxative action of unabsorbed rhein in the colon hindered its use. Thus, enhanced DCN dissolution would allow absorption at the upper gut improving its bioavailability and possibly abolishing the laxative action. Objectives: Enhance dissolution and possibly therapeutic efficacy of DCN by preparing SNEDDS using different carriers, gelucire 44/14 (GLC) and D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), at different drug:carrier weight ratios of 1:1, 1:2, 1:4, 1:6, 1:8 and 1:10. Methods: Preparing SNEDDS using different carriers, gelucire 44/14 (GLC) and D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), at different drug:carrier weight ratios of 1:1, 1:2, 1:4, 1:6, 1:8 and 1:10. The prepared SNEDDS and their corresponding physical mixtures (PMs) were evaluated for their solid state characterization, employing Fourier transform infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC), x-ray diffractometry (XRD) and scanning electron microscopy (SEM). In addition, drug content, and in-vitro dissolution were studied. The results of in-vitro dissolution were analyzed applying different kinetic models. The optimized systems were further examined with respect to their morphology, size distribution and zeta potential. study the anti-inflammatory action of DCN optimized SNEDDS formulae 1:10 DCN:GLC and 1:8 DCN:TPGS was carried out in comparison with free drug against carrageenan-induced hind paw edema in rats Results: All soild state characterization results indicated complete conversion of DCN into the amorphous form or homogeneous dispersion of the partially crystalline drug into the molten carrier. Formulation of DCN as SNEDDSs with GLC or TPGS resulted in a significantly (p < 0.05) higher drug release than that seen in case of the drug alone and the corresponding PMs. Kinetic analysis of the biphasic release pattern of DCN from all prepared binary systems indicated that the release mechanism of DCN from these systems varied between first and zero order kinetics. Korsemeyer-Peppas model application suggested supercase II transport that refers to the erosion of the polymer chain that could explain the initial burst drug release. Collectively, solid state characterization, SEM examination results and in vitro release studies revealed that the optimized systems were, 1:8 DCN:TPGS and 1:10 DCN:GLC SNEDDSs. Conclusion: Finally, we concluded that Formulation of DCN as SNEDDSs with GLC or TPGS was succeed to enhance DCN dissolution and efficacy in the treatment of osteoarthritis.