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Objective: The main objective of the present study was to formulate and evaluate a time-controlled single-unit oral pulsatile drug delivery system containing Zafirlukast for the prevention of nocturnal asthma attacks. To provide time-scheduled drug release for Asthma disease. It is used for preventing asthmatic attacks at early morning. Pulsatile release dosage form is increasing patient compliance by reducing the dosing frequency, especially in the early morning. Methods: Core tablets were prepared by incorporating different concentrations of natural and synthetic super disintegrants. Drug-containing core tablets (ZC1-ZC15) with different compositions of natural super disintegrants (Plantago ovata seed powder, Locust bean gum) synthetic super disintegrants (Sodium starch glycolate (SSG), Cross carmellose sodium (CCS), Crospovidone (CP)) were prepared by direct compression technique. The core tablets were subjected to pre-formulation, physicochemical and In vitro drug release studies. The fast disintegrating core tablet formulation was selected and press-coated tablets (P1-P11) were prepared with different compositions of hydrophobic polymers Eudragit RS100, Eudragit RL 100, Ethylcellulose and hydrophilic polymers Hydroxypropyl methylcellulose K4M, K100M. The optimized formulation was selected and quantified based on in vitro drug release profile in simulated gastric and intestinal fluids. Results: The pre and post-compression parameters of tablets were also found to be within limits. Formulation ZC5 with 16 mg of Locust bean gum showed the least disintegrating time, i.e., 22.13 sec, and was selected as the best immediate release core tablet. The press-coated tablet formulation P8 having 62.5 mg Eudragit RS100 and 62.5 mg of HPMC K4M in ratio 1:1 over the core tablet ZC5 showed rapid and drug release nearly after 4 h lag time and 98.86 % up to 12 h. Accelerated stability studies of the optimized formulation P8 indicated no significant difference in release profile after 3 mo. Conclusion: The in vitro dissolution study showed that lag time before drug release was highly affected by the coating amount level and nature of coating polymer used. Time-controlled pulsatile release tablets can be prepared using press-coating techniques.
Objective: The main objective of the present study was to formulate and evaluate a time-controlled single-unit oral pulsatile drug delivery system containing Zafirlukast for the prevention of nocturnal asthma attacks. To provide time-scheduled drug release for Asthma disease. It is used for preventing asthmatic attacks at early morning. Pulsatile release dosage form is increasing patient compliance by reducing the dosing frequency, especially in the early morning. Methods: Core tablets were prepared by incorporating different concentrations of natural and synthetic super disintegrants. Drug-containing core tablets (ZC1-ZC15) with different compositions of natural super disintegrants (Plantago ovata seed powder, Locust bean gum) synthetic super disintegrants (Sodium starch glycolate (SSG), Cross carmellose sodium (CCS), Crospovidone (CP)) were prepared by direct compression technique. The core tablets were subjected to pre-formulation, physicochemical and In vitro drug release studies. The fast disintegrating core tablet formulation was selected and press-coated tablets (P1-P11) were prepared with different compositions of hydrophobic polymers Eudragit RS100, Eudragit RL 100, Ethylcellulose and hydrophilic polymers Hydroxypropyl methylcellulose K4M, K100M. The optimized formulation was selected and quantified based on in vitro drug release profile in simulated gastric and intestinal fluids. Results: The pre and post-compression parameters of tablets were also found to be within limits. Formulation ZC5 with 16 mg of Locust bean gum showed the least disintegrating time, i.e., 22.13 sec, and was selected as the best immediate release core tablet. The press-coated tablet formulation P8 having 62.5 mg Eudragit RS100 and 62.5 mg of HPMC K4M in ratio 1:1 over the core tablet ZC5 showed rapid and drug release nearly after 4 h lag time and 98.86 % up to 12 h. Accelerated stability studies of the optimized formulation P8 indicated no significant difference in release profile after 3 mo. Conclusion: The in vitro dissolution study showed that lag time before drug release was highly affected by the coating amount level and nature of coating polymer used. Time-controlled pulsatile release tablets can be prepared using press-coating techniques.
Transdermal drug delivery is an alternative route for systemic drug delivery which minimizes the absorption and increases the bioavailability. The main objective of the present work was to develop a suitable matrix type transdermal drug delivery system of Clopidogrel bisulphate using different polymers HPMC E15, Eudragit L100 and to compare the drug release through physical method and chemical method. Matrix type transdermal patches containing Clopidogrel Bisulfate were prepared by solvent evaporation technique. The prepared transdermal patches were evaluated for Thickness, folding endurance, tensile strength and in vitro studies. The prepared transdermal drug delivery system of Clopidogrel bisulphate using different polymers such as HPMC E15 and Eudragit L 100 had shown good promising results for all the evaluated parameters. Based on the In-vitro drug release, drug content and folding endurance results formulation F4 was concluded as an optimized formulation which shows its higher percentage of drug release. Keywords: Transdermal drug delivery, Clopidogrel bisulphate, HPMC E15, Eudragit L100
Adilakshmi, D. et al. Simultaneous Formulation, Estimation and Evaluation of Allopurinol Sustained Release Tablets using various suitable Excipients. Asian Journal of Pharmaceutical Analysis. 2016; 6(3), 155-166. DOI: 10.5958/2231-5675.2016.00025.9 James, H. P. et al. Smart polymers for the controlled delivery of drugs–a concise overview. Acta Pharmaceutica Sinica B. 2014; 4(2), 120-127. doi: 10.1016/j.apsb.2014.02.005 Salve, P. et al. Development and Evaluation of Sustained Release Dosage Form using Hydrophilic and Hydrophobic Materials. Research Journal of Pharmacy and Technology. 2016; 9(5), 481-489. DOI: 10.5958/0974-360X.2016.00089.5 Ismail, R. et al. Formulation and in vitro evaluation of once-daily methyldopa sustained release matrix tablets. Research Journal of Pharmacy and Technology. 2015; 8(2), 161-166. DOI: 10.5958/0974-360X.2015.00029.3 Madhukar, G. A. et al. Optimization of Various Grades of HPMC for Development of Sustained Release Matrix Tablets of Theophylline. Asian Journal of Pharmacy and Technology. 2017; 7(1), 19-26. DOI: 10.5958/2231-5713.2017.00004.6 Qi, X. et al. Floating tablets for controlled release of ofloxacin via compression coating of hydroxypropyl cellulose combined with effervescent agent. International Journal of Pharmaceutics. 2015; 489(1-2), 210-217. doi: 10.1016/j.ijpharm.2015.05.007 Abdulhameed, K. A. A., & Salih, N. A. Controlled Release of Cefixime using Sodium Carboxymethyl Cellulose Polymer. Research Journal of Pharmacy and Technology. 2019; 12(9), 4073-4079. DOI: 10.5958/0974-360X.2019.00701.7 Perez-Marcos, B. et al. Mechanical and drug-release properties of atenolol-carbomer hydrophilic matrix tablets. Journal of Controlled Release. 1991; 17(3), 267-276. doi: 10.1016/0168-3659(91)90145-4 World health organization (WHO). Musculoskeletal conditions. Available at: https://www.who.int/news-room/fact-sheets/detail/musculoskeletal-conditions (дата обращения – 08.02.2021) Thimmasetty, J. et al. Solubility parameter estimation of celecoxib by current methods. Asian Journal of Research in Chemistry. 2009; 2(2), 188-195. Terse, P., and Mallya, R. Formulation and Evaluation of Celecoxib loaded colon Targeted Microsponges. Asian Journal of Research in Pharmaceutical Science. 2020; 10(2), 73-78. DOI: 10.5958/2231-5659.2020.00014.4 Paulson, S. K. et al. Pharmacokinetics of celecoxib after oral administration in dogs and humans: effect of food and site of absorption. Journal of Pharmacology and Experimental Therapeutics. 2001; 297(2), 638-645. Gong, L. et al. Celecoxib pathways: pharmacokinetics and pharmacodynamics. Pharmacogenetics and Genomics. 2012; 22(4), 310-318. doi: 10.1097/FPC.0b013e32834f94cb USP 41- NF36 (2018) The United States Pharmacopeial Convention, USA. Mathur N. et al. Evaluation of quality control parameters on various brands of paracetamol tablet formulation. World J Pharm Pharmaceut Sci. 2015; 4(7):976–984. Ravi, G. et al. Development and Evaluation of oral controlled release tablets of oxybutynin using various polymers. Research Journal of Pharmacy and Technology. 2020; 13(8), 3854-3860. DOI: 10.5958/0974-360X.2020.00682.4 Saha, R. N. et al. Determination of celecoxib in pharmaceutical formulations using UV spectrophotometry and liquid chromatography. Journal of Pharmaceutical and Biomedical Analysis. 2002; 28(3-4), 741-751. doi: 10.1016/S0731-7085(01)00678-1 Mandale, T. R. et al Development and validation of analytical method for simultaneous estimation of amlodipine besylate and celecoxib in pure and combined dosage form. Research Journal of Pharmacy and Technology. 2020; 13(9), 4280-4284. DOI: 10.5958/0974-360X.2020.00756.8 Hamed, R., and Omran, H. Development of dual–release pellets of the non-steroidal anti–inflammatory drug celecoxib. Journal of Drug Delivery Science and Technology. 2020; 55. doi: 10.1016/j.jddst.2019.101419 Biswas, B. K. et al. In vitro release kinetic study of esomeprazole magnesium from methocel K15M and methocel K100 LVCR matrix tablets. Dhaka University Journal of Pharmaceutical Sciences. 2008; 7(1), 39-45. doi.org/10.3329/dujps.v7i1.1216 Wise DL. Handbook of Pharmaceutical Controlled Release Technology. UK: CRC press, (2000). 902 P. ISBN 9780824703691 Tiwari, S.B. et al. Controlled release formulation of tramadol hydrochloride using hydrophilic and hydrophobic matrix system. AAPS PharmSciTech. 2003; 4, 18–23. doi: 10.1208/pt040331 Sawant, V. A. et al. In-Vitro Release Kinetic Study of Mosapride Citrate Dihydrate from Sustained Release Matrix Tablet Containing Two Different Viscosity Grades of HPMC. Research Journal of Pharmaceutical Dosage Forms and Technology. 2009; 1(3), 207-212. Iwata, M., & Ueda, H. Dissolution properties of glibenclamide in combinations with polyvinylpyrrolidone. Drug Development and Industrial Pharmacy. 1996; 22(11), 1161-1165. doi: 10.3109/03639049609065953 Ejikeme, P.M. Investigation of the physicochemical properties of microcrystalline cellulose from agricultural wastes I: orange mesocarp. Cellulose. 2008; 15, 141–147. doi: 10.1007/s10570-007-9147-7 Saeio, K. et al. Factors influencing drug dissolution characteristic from hydrophilic polymer matrix tablet. Scientia Pharmaceutica. 2007; 75(4), 147-164. doi: 10.3797/scipharm.2007.75.147 Maharjan, S. et al. Formulation and Evaluation of sustained release Sodium Alginate beads of Indomethacin. Asian Journal of Pharmacy and Technology. 2019; 9(3), 165-172. DOI: 10.5958/2231-5713.2019.00028.X Sareen, R. et al. Meloxicam carbopol-based gels: characterization and evaluation. Current Drug Delivery. 2011; 8(4), 407-415. Mostafavi, A. et al. Development of a prolonged-release gastroretentive tablet formulation of ciprofloxacin hydrochloride: Pharmacokinetic characterization in healthy human volunteers. International Journal of Pharmaceutics. 2011; 409(1-2), 128-136. doi: 10.1016/j.ijpharm. 2011.02. 035
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