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Register a new userFormulation of methyldopa sustained release matrix tablets using hydrophilic polymers
صياغة مضغوطات قالبية مديدة التحرر من الميتيل دوبا باستخدام متماثرات محبة للماء
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Added by
Tishreen University رسالة ماجستير
Publication date
2015
fields
Pharmacy
and research's language is
العربية
Created by
ربا اسماعيل
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تهدف هذه الدراسة إلى صیاغة مضغوطات قالبیة مدیدة التحرر من المیتیل دوبا باستخدام متماثر الهیدروكسي بروبيل ميتيل سيللوز (HPMC) المحب للماء و دراسة تأثیر عوامل الصیاغة المختلفة (تركیز المتماثر المحب للماء ودرجة لزوجته، المشاركة مع متماثر الإیتیل سیللوز الكاره للماء بنسب مختلفة ، تركیز كل من العامل الرابط والمزلقات المستخدمة) على خواص المضغوطات الناتجة.
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.
Artificial intelligence review:
Research summary
تهدف هذه الدراسة إلى تطوير مضغوطات قالبية مديدة التحرر من الميتيل دوبا باستخدام متماثرات محبة للماء مثل هيدروكسي بروبيل ميتيل سيللوز (HPMC). تم دراسة تأثير عدة عوامل صياغة مثل تركيز المتماثر، درجة لزوجته، المشاركة مع متماثر كاره للماء (إيتيل سيللوز) بنسب مختلفة، وتركيز كل من العامل الرابط والمزلقات المستخدمة على خصائص المضغوطات الناتجة. تم تحضير المضغوطات القالبية بطريقة التحثير الرطب، وأجريت الاختبارات الفيزيائية والكيميائية المناسبة على الحثيرات والمضغوطات المحضرة. أظهرت نتائج دراسة الانحلال في الزجاج أن الصيغتين F6 (الحاوية على 15% من HPMC K100M) وF11 (الحاوية على مشاركة بين EC:HPMC K4M بنسبة 10%:5%) كانتا قادرتين على إطالة زمن تحرر الميتيل دوبا حتى 24 ساعة. بناءً على ذلك، تم اعتبار هاتين الصيغتين مناسبتين لتحقيق الهدف المرجو من هذه الدراسة. تم تحليل حركيات التحرر باستخدام نماذج مختلفة مثل نموذج Higuchi ونموذج Korsmeyer-Peppas، وأظهرت النتائج أن آلية التحرر هي انتشار غير طبيعي (anomalous diffusion).
Critical review
دراسة نقدية: تعتبر هذه الدراسة شاملة ومفصلة في تحليل تأثير عوامل الصياغة المختلفة على تحرر الميتيل دوبا من المضغوطات القالبية. ومع ذلك، يمكن تحسين الدراسة من خلال تضمين تجارب إضافية لدراسة تأثير عوامل أخرى مثل نوع الممدد والعامل الرابط والمزلقات. كما أن الدراسة تفتقر إلى البيانات الحيوية في الجسم الحي، والتي يمكن أن تعزز من موثوقية النتائج وتطبيقاتها العملية. بالإضافة إلى ذلك، يمكن أن تكون الدراسة أكثر شمولية إذا تم تطبيق الصيغتين الفضلئين على مواد فعالة أخرى ودراسة خواص المضغوطات الناتجة. بشكل عام، تعتبر هذه الدراسة خطوة مهمة نحو تطوير أنظمة إيصال دواء مديدة التحرر، ولكن هناك مجال للتحسين والتوسع في البحث.
Questions related to the research
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ما هي الأهداف الرئيسية لهذه الدراسة؟
تهدف الدراسة إلى تطوير مضغوطات قالبية مديدة التحرر من الميتيل دوبا باستخدام متماثرات محبة للماء ودراسة تأثير عوامل الصياغة المختلفة على خصائص المضغوطات الناتجة.
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ما هي الصيغتين اللتين تم اعتبرهما مناسبتين لتحقيق الهدف المرجو من الدراسة؟
الصيغتين F6 (الحاوية على 15% من HPMC K100M) وF11 (الحاوية على مشاركة بين EC:HPMC K4M بنسبة 10%:5%) كانتا قادرتين على إطالة زمن تحرر الميتيل دوبا حتى 24 ساعة.
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ما هي آلية التحرر التي تم تحديدها لمعظم الصيغ المحضرة؟
تم تحديد أن آلية التحرر هي انتشار غير طبيعي (anomalous diffusion) بناءً على قيمة أس الانتشار.
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ما هي التوصيات المستقبلية التي قدمتها الدراسة؟
توصي الدراسة بإجراء دراسات التحرر في الجسم الحي للمضغوطات المحضرة، ودراسة تأثير عوامل صياغة أخرى مثل استخدام متماثرات طبيعية محبة للماء، وتطبيق الصيغتين الفضلئين على مواد فعالة أخرى.
References used
.QAZI, F.; SHOAIB, M. H.; YOUSUF , R. I.; QAZI, T. M.; MEHMOOD, Z. A. and HASAN, S. M. F. Formulation development and evaluation of Diltiazem HCl sustained release matrix tablets using HPMC K4M and K100M. Pakistan Journal of Pharmaceutical Sciences. 26(4), 2013, 653-66
PATEL, H.; PANCHAL, D. R.; PATEL, U.; BRAHMBHATT, T. and SUTHAR, M. Matrix Type Drug Delivery System: A Review. Journal of Pharmaceutical Science and Bioscientific Research. 1(3), 2011, 143-151
AKBARI, J.;ENAYATIFARD, R.;SAEADI, M and SAGHAFI, M. Influence of Hydroxypropyl Methylcellulose Molecular Weight Grade on Water Uptake, Erosion and Drug Release Properties of Diclofenac Sodium Matrix Tablets. Tropical Journal of Pharmaceutical Research. 10(5), 2011, 535-541
SHARMA, V. J. & AMIN P.D. Design and Optimization of Metoprolol Succinate Formulation Using Melt Granulation Technique. International Journal of Pharmaceutical Sciences. 5(3), 2013, 230-238
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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.
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
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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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