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Register a new userPreparation of prolonged release matrix tablets of verapamil and comparaison with coated ones
تحضير مضغوطات قالبية مطولة التأثير للفيراباميل ومقارنتها بالمحضرة بطريقة التلبيس
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إن هدف هذه الدراسة هو تحضير مضغوطات مطولة التأثير للفيراباميل قالبية وأخرى محضرة بطريقة التلبيس وذلك نظراً لأهمية هذه الأنظمة في إيتاء الأدوية وتحسين مطاوعة المرضى واستجابتهم للعلاج. حضرت عدة صيغ باستخدام بلمرات مختلفة معدلة للتحرر(EURS وEURL) واستخدمت طريقة الضغط المباشر للمضغوطات المعدة للتلبيس,وطريقتا التحثير الرطب والضغط المباشر للمضغوطات القالبية. وتم تقييم الصيغ المحضرة في مرحلة ما قبل الضغط كما درست الخواص الفيزيائية للمضغوطات الناتجة, وأجري فحص الانحلال, ودرست نماذج حركيات التحرر في الزجاج. أظهرت النتائج أن المضغوطات القالبية الحاوية على 7.5أو10% من الإيدراجيت RSوRL على الترتيب, وتلك الملبسة باستخدام محلول التلبيس (15%) المطبق 120في حالة (EuRS100) أو 200مرة في حالة (EURL100) كانت الأفضل حيث حررت حوالي 90-95% من محتواها من الفيراباميل خلال 24 ساعة
The purpose of this study was to prepare prolonged release tablets of verapamil: matrix and coated tablets, because of the importance of these systems in drug delivery and improving the patient compliance and therapeutic efficacy .Different formulations were prepared by using different release-modifiers polymers (EURL100 and EURS100). Direct compression technique was used to prepare coated tablets while matrix tablets were prepared by wet granulation and direct compression methods. The prepared formulations were evaluated in terms of their precompression parameters, physical characteristics, dissolution test and in vitro drug release kinetic studies. The results showed that matrix tablets containing 7.5or10% of EuRS100 and EuRL100 respectively and that coated tablets prepared by using coating solution (15%) which was applied about 120(in case of EuRS100) or 280 (in case of EuRL100) times were the best. These tablets released about 90-95% of verapamil within 24h
References used
KHACHANE, K. N.; BANKAR, V. H.; GAIKWAD, P. D.; PAWAR, S. P. Novel Sustained Release Drug Delivery System: Review. International Journal of Pharmaceutical Research and Development. 3(12), 2012, 1-14
ANCSEL, H. C.; ALLEN, L. V.; POPOVICH, N. G. Modified release dosage forms and drug delivery systems In: Pharmaceutical dosage forms and drug delivery systems, 7th Edn, Lippincott, Williams C Wilkins, Philadelphia. 1997, 229-243
MODI, Sh. A.; GAIKWAD, P. D.; BANKAR, V. H.; PAWAR, S. P. Sustained Release Drug Delivery System : A Review. International Journal of Pharma.Research and Development. 2(12), 2011, 147-160
Kabir et al.,2009
Bhagwat DA, Kawtikwar PS, Sakarkar DM. Sustained release matrices of verapamil HCl using glyceryl monosterate and stearic acid. Res J Pharm Tech 2008;1:405-09
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Nifedipine is one of the most used calcium channel blocking agents. Due to its low aqueous solubility, it often shows low and irregular bioavailability after oral administration. Nifedipine has short half-life so it has to be administered many times
a day. Immediate-release formulations increase the risk of myocardial infarction and mortality. This research aims to prepare dual-function drug delivery system to enhance nifedipine solubility using solid dispersion technique, and extend its release by incorporating these dispersions in matrix tablets. 32 Factorial design was employed; two independent variables, Poloxamer 188 and Ethyl cellulose, to improve solubility and extend release respectively, were used in 3 levels. The prepared tablets were examined, and succeeded in extending nifedipine release up to 12 hrs. The equations that link the dependent and independent variables were obtained, through which tablet hardness and the released amount after 1, 4 and 6 hours could be predicted.
The objective of the present study was to formulate methyldopa sustained release
matrix tablets using hydrophilic hydroxypropyl methylcellulose (HPMC) alone or in
combination with hydrophobic ethyl cellulose polymer(EC). Matrix tablets were prepare
d
by wet granulation method, and subjected to physiochemical studies. All formulations
showed physiochemical properties which appear to be in compliance with pharmacopeial
standards. The in-vitro dissolution studies showed that increase in concentration or
viscosity of HPMC polymer led to decrease in the rate of drug release decreased. The
results also revealed that Combination of HPMC K4M and EC slower drug release more
than using HPMC K4M alone. Drug release kinetics of about all formulations correspond
best to Korsemeyer-Peppas model and drug release mechanism was anomalous diffusion
based on release exponent value.
The present study aims to develop sustained release (SR) matrix tablets of methyldopa using
hydrophilic hydroxypropyl methylcellulose (HPMC), and to study the effect of some formulation
variables (HPMC concentration and viscosity grade, combination
with hydrophobic Ethylcellulose
(EC) in different ratio, binder and lubricants concentrations) on the properties of prepared tablets.
Matrix tablets were prepared by wet granulation method, and prepared granules and tablets were
subjected to suitable physiochemical studies. Drug release kinetics showed that drug release
mechanism for about all formulations was found to fit best to Higuchi model and drug release
mechanism was anomalous diffusion based on release exponent value. The in-vitro dissolution
studies showed that formulation F6 containing 15% of HPMC K100M and formulation F11
containing EC:HPMC K4M (5%:10%) were able to sustain the release of methyldopa up to 24 hours
so these two formulations were selected as suitable formulations.
تلبي الأشكال الصيدلية ذات التحرر المعدل مطالب عدة لا يمكن تحقيقها عادة بالأشكال التقليدية . من هذه المطالب اراحة المريض وتحسين مطاوعته للعلاج
تلبي الأشكال الصيدلية ذات التحرر المعدل مطالب عدة لا يمكن تحقيقها عادة بالأشكال التقليدية . من هذه المطالب اراحة المريض وتحسين مطاوعته للعلاج
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