FORMULATION AND OPTIMIZATION OF SUSTAINED RELEASE MATRIX TABLET OF NIFEDIPINE USING DIFFERENT GRADES OF HPMC

Authors

  • Shamim Akhtar Mittal Institute of Pharmacy, Bhopal (M.P.)
  • Harish Chandrawanshi Mittal Institute of Pharmacy, Bhopal (M.P.)
  • Mukesh Patel Mittal Institute of Pharmacy, Bhopal (M.P.)
  • Arvind Dangi Mittal Institute of Pharmacy, Bhopal (M.P.)
  • Dr. D. P. Chatterjee Mittal Institute of Pharmacy, Bhopal (M.P.)

Abstract

In the present study nine formulations with variable concentration of polymers (HPMC-K100, HPMC-K4) were prepared by direct compression method and evaluated for physicochemical properties, buoyancy lag time, total floating time, and in-vitro drug release. The results indicated that optimized formulation F 6 on immersion in 0.1N HCl solution at pH 1.2 & 6.8 pH phosphate Buffer at 37±0.50C tablets immediately and remain buoyant up to 12 hrs without disintegration. These two factors are essential for the tablet to acquire bulk densit y < 1, so that it remains buoyant on the gastric fluid. The In vitro drug release data of the optimized formulation was subjected to goodness of fit test by linear regression analysis according to zero order, first order kinetic equation, Higuchi’s and Korsmeyer’s models in order to determine the mechanism of drug release. When the regression coefficient values of were compared, it was observed that ‘r’ values of Higuchi was maximum i.e 0.978 hence indicating drug release from formulations was found to follow Higuchi kinetics. In vitro data obtained for matrix tablet of Nifedipine showed prolonged drug release. Tablets of different release kinetics could be obtained by varying the formulation variables. Thus, Nifedipine is most suitable drug candidate for the Antihypertension. Based on the above considerations, formulation F6 was selected as optimized formula, a perusal of table indicated that the parameters of Matrix Tablet were satisfactory for the intended use.

Key words: Nifedipine, HPMC, Matrix, Sustained Release

References

LECKMAN L, LIBERMAN HA, KANIG JL., THE THEORY AND PRACTICE OF INDUSTRIAL PHARMACY, 3RD ED., VARGHESE PUBLISHING HOUSE, BOMBAY ,1987:430-453

ROBINSON JR, LEE HL, CONTROLLED DRUG DELIVERY : FUNDAMENTALS AND APPLICATION, 2RD EDITION, MARCEL DEKKAR INC., NEW YORK , 1987:4-36

NOTARI. R., BIOPHARMACEUTICS AND CLINICAL PHARMACOKINETICS, AN INTRODUCTION, 3RD, MARCELDEKKER INC. NEW YORK , 1980:152-154.

BROWN MJ, PALMER CR, CASTAIGNE A, ET AL. (2000). "MORBIDITY AND MORTALITY IN PATIENTS RANDOMISED TO DOUBLE-BLIND TREATMENT WITH A LONG-ACTING CALCIUM-CHANNEL BLOCKER OR DIURETIC IN THE INTERNATIONAL NIFEDIPINE GITS INTRSTUDY: INTERVENTION AS A GOAL IN HYPERTENSION TREATMENT (INSIGHT)". LANCET 356 (9227): 366–72. DOI:10.1016/S0140-6736(00)02527-7. PMID 10972368.

POOLE-WILSON PA, KIRWAN BA, VOKÓ Z, DE BROUWER S, VAN DALEN FJ, LUBSEN J (2006). "SAFETY OF NIFEDIPINE GITS IN STABLE ANGINA: THE ACTION TRIAL". CARDIOVAS DRUGS THER 20 (1): 45–54. DOI:10.1007/S10557-006-6312-4. PMID 16552473.

ODOU P, FERRARI N, BARTHÉLÉMY C, ET AL. (2005). "GRAPEFRUIT JUICE-NIFEDIPINE INTERACTION: POSSIBLE INVOLVEMENT OF SEVERAL MECHANISMS". JOURNAL CLINICAL PHARM THER 30 (2): 153–8. DOI:10.1111/J.1365-2710.2004.00618.X. PMID 15811168.

HYPERTENSION: MANAGEMENT OF HYPERTENSION IN ADULTS IN PRIMARY CARE. CLINICAL GUIDELINE CG34. NATIONAL INSTITUTE FOR HEALTH AND CLINICAL EXCELLENCE (NICE), JUNE 2006. FULLTEXT INDEX. ISBN 1-86016-285-1.

GROSSMAN E, MESSERLI FH, GRODZICKI T, KOWEY P (1996). "SHOULD A MORATORIUM BE PLACED ON SUBLINGUAL NIFEDIPINE CAPSULES GIVEN FOR HYPERTENSIVE EMERGENCIES AND PSEUDOEMERGENCIES?". JAMA 276 (16): 1328–31. DOI:10.1001/JAMA.276.16.1328. PMID 8861992.

VARON J, MARIK PE (2003). "CLINICAL REVIEW: THE MANAGEMENT OF HYPERTENSIVE CRISES". CRITICAL CARE (LONDON, ENGLAND) 7 (5): 374–84. DOI:10.1186/CC2351. PMC 270718. PMID 12974970.

CAMPAGNOLO, DI. "AUTONOMIC DYSREFLEXIA IN SPINAL CORD INJURY". EMEDICINE. RETRIEVED 2011-07-14.

KING JF, FLENADY VJ, PAPATSONIS DN, DEKKER GA, CARBONNE B (2003). "CALCIUM CHANNEL BLOCKERS FOR INHIBITING PRETERM LABOUR". IN FLENADY, VICKI. COCHRANE DATABASE OF SYSTEMATIC

Y. RAJAJAYARAO, P. DIVYA, K. DIVYASREE, S. MANOHAR BABU FORMULATION AND EVALUATION OF MATRIX TYPE SUSTAINED RELEASE NIFEDIPINE TABLETS INTERNATIONAL JOURNAL OF RESEARCH IN PHARMACY AND CHEMISTRY 2013, 4(1), 34-45

DEWAN T AKHTER, RIAZ UDDIN, NAZ H HUDA, KUMAR B SUTRADHAR DESIGN AND FORMULATION OF TWICE DAILY NIFEDIPINE SUSTAINED RELEASE TABLET USING METHOCEL K15M CR AND METHOCEL K100LV CR INTERNATIONAL JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES 2012 VOL 4, ISSUE 1,

PRABAKARAN L, VISHALINI M HYDROPHILIC POLYMERS MATRIX SYSTEMS OF NIFEDIPINE SUSTAINED RELEASE MATRIX TABLETS: FORMULATION OPTIMIZATION BY RESPONSE SURFACE METHOD PELAGIA RESEARCH LIBRARY 2010, 1 (1): 147-165

PASUPATHI A, PALANISAMY P, B JAYKAR, R MARGRET CHANDIRA, B.S. VENKATESWARLU FORMULATION, OPTIMIZATION AND IN-VITRO EVALUATION OF NIFEDIPINE SUSTAINED RELEASE TABLET INDIAN JOURNAL OF RESEARCH IN PHARMACY AND BIOTECHNOLOGY2011 VOLUME 1 ISSUE 1 PAGE NO. 90-94

BERTIL ABRAHAMSSONA, MAGNE ALPSTEN, BJORN BAKEC, ULF E. JONSSON, MARIA ERIKSSON-LEPKOWSKA, ANNHILD LARSSON DRUG ABSORPTION FROM NIFEDIPINE HYDROPHILIC MATRIX EXTENDEDRELEASE (ER) TABLET-COMPARISON WITH AN OSMOTIC PUMP TABLET AND EFFECT OF FOOD JOURNAL OF CONTROLLED RELEASE 1998 52 PAGE NO. 301–310

KIBBE AH., HANDBOOK OF PHARMACEUTICAL EXCIPIENTS; AMERICAN PHARMACEUTICAL ASSOCIATION AND PHARMACEUTICAL PRESS, WASHINGTON LONDON; 2000; 3RD ED; 102-106.

CHOWHAN ZT. ROLE OF BINDERS IN MOISTURE-INDUCED HARDNESS INCREASE IN COMPRESSED TABLETS AND ITS EFFECT ON IN VITRO DISINTEGRATION AND DISSOLUTION. J PHARM SCI 1980; 69: 1–4.

ROWE RC. THE ADHESION OF FILM COATINGS TO TABLET SURFACES – THE EFFECT OF SOME DIRECT COMPRESSION EXCIPIENTS AND LUBRICANTS. J PHARM PHARMACOL 1977; 29: 723–726.

BANKER G, PECK G, JAN S, PIRAKITIKULR P. EVALUATION OF HYDROXYPROPYL CELLULOSE AND HYDROXYPROPYL METHYL CELLULOSE AS AQUEOUS BASED FILM COATINGS. DRUG DEV IND PHARM 1981; 7: 693–716.

OKHAMAFE AO, YORK P. MOISTURE PERMEATION MECHANISM OF SOME AQUEOUS-BASED FILM COATS. J PHARM PHARMACOL 1982; 34 (SUPPL.): 53P.

ALDERMAN DA, SCHULZ GJ. METHOD OF MAKING A GRANULAR, COLD WATER DISPERSIBLE COATING COMPOSITION FOR TABLETS. UNITED STATES PATENT NO. 4,816,298; 1989.

PATELL MK. TASTE MASKING PHARMACEUTICAL AGENTS. UNITED STATES PATENT NO. 4,916,161; 1990.

HARDY JG, KENNERLEY JW, TAYLOR MJ, ET AL. RELEASE RATES FROM SUSTAINED-RELEASE BUCCAL TABLETS IN MAN. J PHARM PHARMACOL 1982; 34 (SUPPL.): 91P.

HOGAN JE. HYDROXYPROPYLMETHYLCELLULOSE SUSTAINED RELEASE TECHNOLOGY. DRUG DEV IND PHARM 1989; 15: 975–999.

SHAH AC, BRITTEN NJ, OLANOFF LS, BADALAMENTI JN. GEL-MATRIX SYSTEMS EXHIBITING BIMODAL CONTROLLED RELEASE FOR ORAL DELIVERY. J CONTROL RELEASE 1989; 9: 169–175.

WILSON HC, CUFF GW. SUSTAINED RELEASE OF ISOMAZOLE FROM MATRIX TABLETS ADMINISTERED TO DOGS. J PHARM SCI 1989; 78: 582–584.

DAHL TC, CALDERWOOD T, BORMETH A, ET AL. INFLUENCE OF PHYSICOCHEMICAL PROPERTIES OF HYDROXYPROPYL METHYLCELLULOSE ON NAPROXEN RELEASE FROM SUSTAINED RELEASE MATRIX TABLETS. J CONTROL RELEASE 1990; 14: 1–10.

VILA JL, REMUNAN C, BRETAL MJ,NUNEZ A. ACCELERATED STABILITY STUDY OF SUSTAINED RELEASE NIFEDIPINE TABLET PREPARE WITH GELUCIRE. INTERNATIONAL JOURNAL OF PHARMACEUTICS VOLUME 80, ISSUES 1–3 PAGES 151-159.

HASIGAVA A,NAKAGAWA H,SUGIMOTO I. APPLICATION OF SOLID DISPERSIONS OF NIFEDIPINE WITH ENTERIC COATING AGENT TO PREPARE A SUSTAIN-RELEASEDOSAGE FORM. CHEMICAL AND CHEMICAL AND PHARMACEUTICAL BULLETIN VOL. 33 (1985) NO. 4 P 1615-1619.

Downloads

Published

2015-09-28

Issue

Section

Original Research Article