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Register a new userFormulation and evaluation of methyldopa sustained release matrix tablets
صياغة مضغوطات قالبية مديدة التحرر من الميتيل دوبا و تقييمها
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تهدف هذه الدراسة إلى صياغة مضغوطات قالبية مديدة التحرر من الميتيل دوبا باستخدام متماثر محب للماء هو الهيدروكسي بروبيل ميتيل سيللوز (HPMC) لوحده أو بالمشاركة مع متماثر الإيتيل سيللوز (EC) الكاره للماء. حضرت المضغوطات القالبية بطريقة التحثير الرطب wet granulation ، و تم إجراء اختبارات فيزيوكيميائية عديدة على المضغوطات المحضرة. أظهرت الصيغ جميعها مواصفات فيزيوكيميائية متوافقة مع المتطلبات الدستورية. و بينت نتائج دراسات الانحلال في الزجاج أن زيادة تركيز أو درجة لزوجة المتماثر المحب للماء أنقصت معدل تحرر الدواء من المضغوطات، إضافة إلى أن مشاركة المتماثر المحب للماء HPMC K4M مع الإيتيل سيللوز ( EC) أبطأ تحرر الميتيل دوبا أكثر مما لو استخدم المتماثر المحب للماء وحده . كانت حركيات التحرر من معظم الصيغ تتبع نموذج Korsemeyer-Peppas ، و اعتماداً على قيمة أس الانتشار فإن آلية التحرر هي analmous diffusion .
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 prepared 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.
Artificial intelligence review:
Research summary
تهدف هذه الدراسة إلى صياغة وتقييم مضغوطات قالبية مديدة التحرر من الميتيل دوبا باستخدام متماثر محب للماء (HPMC) بمفرده أو بالمشاركة مع متماثر كاره للماء (EC). تم تحضير المضغوطات بطريقة التحثير الرطب وإجراء اختبارات فيزيوكيميائية عليها. أظهرت النتائج أن زيادة تركيز أو درجة لزوجة HPMC تقلل من معدل تحرر الدواء، بينما مشاركة HPMC مع EC تبطئ التحرر أكثر. أظهرت دراسات الانحلال أن الصيغ تتبع نموذج Korsemeyer-Peppas مع آلية تحرر تعتمد على الانتشار غير النظامي. تم تحديد الصيغتين F3 وF7 كأفضل الصيغ لإطالة زمن تحرر الميتيل دوبا حتى 24 ساعة، مما يجعلهما مرشحتين لمزيد من الدراسات الحيوانية.
Critical review
دراسة نقدية: تعتبر هذه الدراسة مهمة في مجال تطوير أنظمة إيصال الدواء مديدة التحرر، حيث تقدم حلاً لزيادة التوافر الحيوي للميثيل دوبا وتقليل عدد الجرعات اليومية. ومع ذلك، كان من الممكن تحسين الدراسة بإجراء تجارب إضافية على نماذج حيوانية لتأكيد النتائج المخبرية. كما أن الدراسة لم تتطرق إلى تأثير العوامل البيئية مثل درجة الحرارة والرطوبة على استقرار المضغوطات، وهو جانب مهم لضمان فعالية الدواء على المدى الطويل. بالإضافة إلى ذلك، كان من الممكن تقديم تحليل اقتصادي لتكلفة الإنتاج مقارنة بالفوائد العلاجية.
Questions related to the research
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ما الهدف الرئيسي من هذه الدراسة؟
الهدف الرئيسي هو صياغة وتقييم مضغوطات قالبية مديدة التحرر من الميتيل دوبا باستخدام متماثر محب للماء (HPMC) بمفرده أو بالمشاركة مع متماثر كاره للماء (EC).
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ما هي الطريقة المستخدمة لتحضير المضغوطات في هذه الدراسة؟
تم تحضير المضغوطات باستخدام طريقة التحثير الرطب.
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ما هو تأثير زيادة تركيز HPMC على معدل تحرر الدواء؟
زيادة تركيز HPMC تؤدي إلى تقليل معدل تحرر الدواء من المضغوطات.
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ما هي الصيغتان اللتان تم تحديدهما كأفضل صيغ لإطالة زمن تحرر الميتيل دوبا؟
الصيغتان F3 وF7 تم تحديدهما كأفضل صيغ لإطالة زمن تحرر الميتيل دوبا حتى 24 ساعة.
References used
KUSHAL, M.; MONALI, M.; DURGAVATI, M.; MITTAL, P.; UMESH, S. & PRAGNA, S. Oral Controlled Release Drug Delivery System: An Overview . International Research Journal of Pharmacy. Vol.4,No.3,2013,70-76
MAHAJAN, P.; MAHAJAN, S. & MISHRA, D. Valsartan Release From Sustained Release Matrix Tablet and Effect Of Cellulose Derivatives. International Journal Of Pharmacy & Life Sciences. Vol.2, NO.1,2011,521-530
KHANADI, M.; CHAKRABORTY, S.; SHARMA, A.; PANDA, D.; KHANAM,N. & PANDA, S.K. Development of Propranolol Hydrochloride Matrix Tablets: An Investigation on Effects of Combination of Hydrophilic and Hydrophobic Matrix Formers Using Multiple Comparison Analysis . International Journal of Pharmaceutical Sciences Review and Research . Vol.1,No.2,2010,1-7
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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.
Methyldopa, an anti-hypertensive drug having a half life of less than 2 hours, and given with a dose of 250 mg 3-4
times daily.
Objective: The present study was for objective of developing a sustained release (SR) matrix tablets of methyldopa
usin
g hydroxypropyl methylcellulose(HPMC) as release controlling factor, and to study the effect of some formulation
factors on drug release from tablets.
Methods: Hydrophilic SR matrix tablets containing 250 mg of methyldopa were prepared using wet granulation
method. Granules were evaluated for moisture content, loose bulk density, tapped bulk density, compressibility index
and hausner’s ratio. Tablets were subjected to physiochemical studies and in vitro dissolution study. Effect of
concentration and viscosity grade of HPMC, both binder and lubricant concentration on drug release from matrix
tablets was evaluated .
Results: All formulations showed physiochemical properties which appear to be in compliance with pharmacopeial
standards. From the in vitro dissolution studies, it was clear that as the concentration or viscosity of polymer increased,
the rate of drug release was found to be decreased. Higher concentration of binder (PVP K30) showed slower release
of drug, while the level of lubricant(magnesium stearate and talc) appeared to insignificantly affect release rates. Drug
release kinetics of about all formulations correspond best to Korsemeyer-Peppas model and drug release mechanism
was found to be anomalous (non-Fickian) diffusion based on release exponent value. The formulation F6 (containing
15% HPMC K100M ) was selected as the optimized formulation as it sustained the release over 24 hrs.
Conclusion: The results of this study showed that the drug release from HPMC based matrix tablets using methyldopa
as a drug model could be modulated by varying the polymer concentration, the polymer viscosity and the binder
concentration with no significant effect of varying the lubricant concentration.
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 formula
tions 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
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.
For controlling the release of Ketoprofen from matrix tablets, combinations
between different polymers in different ratio were formulated.
Aim: The aim of this study is to investigate the applicability of HPMC combination with
Polymethacrylates (Eُudragit RS, RL & L100) for controlling the release of ketoprofen from matrix
tablets. Four types of HPMC with different viscosities were tested in the study.
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