DILTIAZEM HCL MICROCAPSULES USING ETHYL CELLULOSE ETHER DERIVATIVE POLYMER AS RELEASE RETARDING AGENT: IN-VITRO CHAPTER
DOI:
https://doi.org/10.29121/granthaalayah.v3.i8.2015.2961Keywords:
Diltiazemhcl, Microencapsulation, Kinetic Models, Drug Release RateAbstract [English]
This study presents sustained releasemicroencapsulation of Diltiazem HCL.
Its in-vitro dissolution study in phosphate buffer pH 7.4 as dissolution medium and in vivo behaviour in animal subjects. The microcapsules were prepared using polymers Ethocel 7P and Ethocel 7FP at two different drug to polymer (D: P) ratios i.e. 1:5 and 1:10 and the effect of concentration was observed on drug release behaviour. The prepared microcapsules were evaluated for different physical characteristics i.e. Bulk density, Tap density, Compressibility index, Hausner’s ratio and Angle of repose. Characterization of the developed microcapsules was carried out using Differential Scanning Calorimetery and Fourier Transform Infrared Spectroscopy while Scanning Electron Microscopy was performed to observe the morphology of the microcapsules. Model dependent and in dependent approaches were used to find out the drug transport mechanism and to compare the drug release profiles with standard formulation respectively.
All the formulations show anomalous, non-Fickian diffusion mechanism and the data was best fitted in Korsmeyer’sPeppas equation.
While carrying out in vivo studies, simple and rapid HPLC methods were developed which revealed optimum serum concentration (Cmax) levels for the developed microcapsules predicting least chances of side or adverse effects.
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References
YAMUDA T, OHNISHI H AND MACHIDA Y (2001). Sustained release ketoprofenmicroparticles with ethylcellulose and carboxymethylethylcellulose. J. Control. Release,75: 271-282.
MURTAZA G, AHAMD M, AKHTAR N AND RASOOL F (2009). A comparative study of various microencapsulation techniques: effect of polymer viscosity on microcapsule characteristics. Pak. J. Pharm. Sci., vol.22, no.3, pp.291-300.
NOKHODCHI A AND FARID D (2002). Microencapsulation of paracetamol by various emulsion techniques using cellulose acetate phthalate.Pharmaceutical technology, 54-60.
OZYAZICI M, SEVGI F AND ERTAN G. (1996). “micromeritic studies on nicardipine hydrochloride microcapsules,” int. J. Pharm. 138 (1), 25–35.
KADAM M, HASHMI S I, AND KALE R.V (2011).Studies on extraction of ginger oil and its microencapsulation.Ejeafche, 10(6), [2382-2390].
YEO Y, PARK K (2004). A new microencapsulation method using an ultrasonic atomizer based on interfacial solvent exchange. Journal of controlled release 100, 379–388. DOI: https://doi.org/10.1016/j.jconrel.2004.09.012
REDDY K, MUTALIK S. & REDDY S. (2003). Once-daily sustained-release matrix tablets of nicorandil: Formulation and in vitro evaluation. AAPS PharmSciTech, 4, 480-488. DOI: https://doi.org/10.1208/pt040461
LACHMAN L, LIEBERMAN H. A. & KANIG J. L. (1987). The Theory and Practice of Induatrial Pharmacy. Philadelphia, PA: Lea and Fabiger;. 317-318.
ABDELKADER H, ABDALLA Y O & SALEM H (2008b). Formulation of Controlled-Release Baclofen Matrix Tablets II: Influence of Some Hydrophobic Excipients on the Release Rate and In Vitro Evaluation. AAPS PharmSciTech, 9, 675-683. DOI: https://doi.org/10.1208/s12249-008-9094-0
LEE J. & HERMAN J. H. (1993). Angle of Repose and Angle of Marginal Satbility: molecular dynamics of granular particles. Journal of Physics A: Mathematical and General, 26, 373-383.
KORSMEYER R., GURNY R., DEOLKER E., BURI P. & PEPPAS N. (1983). Mechanism of solute release from porous hydrophillic polymers. Ind J Pharm, 15, 25-35. DOI: https://doi.org/10.1016/0378-5173(83)90064-9
SHAH S U, SHAH K U, JAN S U, KAMRAN A, REHMAN A U, HUSSAIN A AND KHAN G M (2011). Formulation and in vitro evaluation of ofloxacin-ethocel controlled release matrix tablets prepared by wetgranulation method: influence of co-excipientson drug release rates. Pak. J. Pharm. Sci., vol.24, no.3, pp.255-261.
KHAN, G. M. & JIABI, A. 1998. Formulation and in vitro evaluation of ibuprofen-carbopol® 974P-NF controlled release matrix tablets III: influence of co-excipients on release rate of the drug. Journal of Controlled Release, 54, 185-190. DOI: https://doi.org/10.1016/S0168-3659(97)00225-3
BHARAT K R (2005). Studies on microencapsulation of diltiazemHCl. Rajiv Gandhi University of Health Sciences, Karnataka, Bangalore.
PRABU S. L, SHIRWAIKAR AA, SHIRWAIKAR A, RAVIKUMAR G, KUMAR A, JACOB A (2009). Formulation and evaluation of oral sustained release of Diltiazem Hydrochloride using rosin as matrix forming material, Ars Pharm, Vol.50 nº1; 32-42.
SHARIFF, A., MANNA, P., PARANJOTHY, K. & MANJULA, M. 2007. Entrapment of andrographolide on cross linked alginate pellets: II Phaysicochemical characterization to studaythe pelletization of andrographolide. Pak. J. Pharm. Sci., , 2, 1-9.
SAJEEV C, VINAY G, ARCHNA R AND SAHA RN (2002). Oral controlled release formulation of diclofenac sodium by microencapsulation with ethylcellulose. J. Microencapsul.,19: 753-760.
SHAH S U, SHAH K U, REHMAN A U AND KHAN G M (2011). Investigating the in vitro drugrelease kinetics fromcontrolled release diclofenac potassium-ethocel matrix tablets and the influence of co-excipientson drug release patterns.Pak. J. Pharm. Sci., vol.24, no.2, april 2011, pp.183-192.
BADSHAH, A., SUBHAN, F. & RAUF, K. 2010. Controlled Release Matrix Tablets of Olanzapine: Influence of Polymers on the In vitro Release and Bioavailability. AAPS PharmSciTech, Vol. 11, No. 3.pp 1397-1404.
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