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Preparation and Evaluation of Atenolol Floating Beads as a Controlled Delivery SystemPreparation and Evaluation of Atenolol Floating Beads as a Controlled Delivery System

Authors: Yehia I. Khalil يحيى اسماعيل خليل --- Lena M. Thomas
Journal: Iraqi Journal of Pharmaceutical Sciences المجلة العراقية للعلوم الصيدلانية ISSN: 16833597 Year: 2011 Volume: 20 Issue: 1 Pages: 70-80
Publisher: Baghdad University جامعة بغداد

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Abstract

This study aims to encapsulate atenolol within floating alginate-ethylcellulose beads as an oral controlled-release delivery system using aqueous colloidal polymer dispersion (ACPD) method.To optimize drug entrapment efficiency and dissolution behavior of the prepared beads, different parameters of drug: polymer ratio, polymer mixture ratio, and gelling agent concentration were involved.The prepared beads were investigated with respect to their buoyancy, encapsulation efficiency, and dissolution behavior in the media: 0.1 N HCl (pH 1.2), acetate buffer (pH 4.6) and phosphate buffer (pH 6.8). The release kinetics and mechanism of the drug from the prepared beads was investigated.All prepared atenolol beads remained floating on 0.1 N HCl (pH 1.2) medium over 24 hours. Besides, high yield beads of 73.07- 84.31% was obtained. Encapsulation efficiencies were in the range of 33.10 % -79.04 %, and were found to increase as a function of increasing drug: polymer mixture ratio and the gelling agent concentrations.Moreover, atenolol release profile from the beads was affected by the pH of the dissolution medium. It was found to be slowest in 0.1 N HCl (pH 1.2) and fastest in phosphate buffer (pH 6.8).The obtained results suggest that atenolol could be formulated as a controlled release beads, using ethylcellulose and alginate as polymers, using ACPD method.

تهدف هذه الدراسة لتغليف الاتينولول في كريات طافية من الاثيل سليلوزالجيناتالصوديوم كنظام تحررمسيطر عليه باستعمالطريقة الانتشار المائي.لتحسين كفاءة التحميل الدوائي و سلوك تحرر العقار من الكريات المحضرة ٬ فان عدة عوامل مثل نسبة العقارالمكوثرات٬ نسبة مزيج المكوثرات اضافة الى تركيز المادة المهلمنة قد تضمنت في هذه الدراسة. لقد تم التحري عن الكرياتالمحضرة بالنسبة الى قابليتها على الطفو ٬ كفاءة التحميل الدوائي وسلوك التحررالدوائي في الاوساط: 0.1 مولاري لحامض٬ محلول الاسيتات المائي (الاس الهيدروجيني 4.6 ) ومحلول الفوسفات المائي (الاس ( الهيدروكلوريك (الاس الهيدروجيني 1.2٬ كما تمت محاولة التوصل الى معرفة آلية التحررالحركي للدواء من الكريات المحضرة.لقد وجد ان جميع الكريات ( الهيدروجيني 6.8المحضرة بقيت طافية في وسط حامضي 0.1 مولاري لحامض الهيدروكلوريك (الاس الهيدروجيني 1.2 ) لفترة زادت عن 24 ساعة ٬٬ % 79.04 84.31% وبقابلية تحميل دوائي بنسبة 3٫10 اضافةالى ان تلك الكريات كانت بكمية ناتج نهائي يتراوح بين 73.07كما وجد ان قابلية التحميل الدوائي تزداد كدالة لزيادة نسبة العقار:المكوثرات وتركيز المادة المهلمنة . لقد وجد ان الشكل البياني لتحررالاتينولول من كريات الجينات الصوديومالاثيلسليلوز تتأثر بالاس الهيدروجيني لوسط التحرر الدوائي وان ابطأ تحرر يتم في وسط.( 0.1 مولاري لحامض الهيدروكلوريك (الاس الهيدروجيني 1.2 ) واسرعها في محلول الفوسفات المائي (الاس الهيدروجيني 6.8ان النتائج المستحصلة من الدراسة تقترح بان الاتينولول يمكن تصييغه على شكل كريات محورة التحرر باستعمال الاثيل سليلوزوالجينات الصوديوم كمكوثرات باستعمال طريقة الانتشار المائي.


Article
Preparation and Evaluation of Physical and, Rheological Properties of Clotrimazole Emulgel

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Abstract

Recently, emulgel has emerged as one of the most interesting topical preparations in the field of pharmaceutics. In this research clotrimazole was formulated as topically applied emulgel ; different formulas were prepared. The prepared emulgels were evaluated for their physical appearance , rheological behaviour , and in vitro drug release . The influence of the type of gelling agent (carbopol 934 and methyl cellulose), the concentration of both the emulsifying agent (2% and 4% w/w of mixture of span 20 and tween 20) and the oil phase (5% and 7.5% w/w of liquid paraffin) and the type of oil phase (liquid paraffin and cetyl alcohol), on the drug release from the prepared emulgels was investigated. Commercially available topical canestin® cream was used for comparison. All the prepared emulgels showed acceptable physical properties concerning colour, homogeneity, consistency, and pH value. Rheological studies revealed that all emulgels formulations exhibited a shear – thinning behaviour with thixotropy, indicating structural break down of intermolecular interaction between polymeric chains. Clotrimazole emulgels exhibited higher drug release than canestin® cream. The results of in vitro release showed that methyl cellulose – based emulgel gave better release than carbopol 934 – based one. Also it was found that the emulsifying agent concentration had the most pronounced effect on the drug release from the emulgels, followed by the oil phase concentration, which has a retardation effect, and finally the type of the gelling agent. It was suggested that the clotrimazole emulgel formulation prepared with methyl cellulose, with low concentration of oil phase (5%w/w liquid paraffin) and high concentration of emulsifying agent (4%w/w), showed an optimum formula for highest drug release (74.4% after three hours), which followed higuchi diffusion model with a diffusion-controlled mechanism.

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