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compression of matrices prepared by using the melt granulation technique. The effect of different concentrations of PREC
on the in-vitro drug release of VPH was studied by comparing it with the marketed formulation and percent release given
in USP for VPH extended release tablets. Effect of release enhancers such as microcrystalline cellulose (MCC) and lactose
on in-vitro drug release was also studied. Biopharmaceutical evaluation of the satisfactory formulation was also performed
in order to estimate the maximum concentration of drug in plasma (Cmax), time required to reach maximum concentration
(tmax), elimination rate constant (k), elimination rate constant (t1/2), area under curve (AUC(0-t) and AUC(02a), apparent
volume of distribution (Vd) and mean residence time. The results showed that PREC can be utilized as the matrix forming
agent to sustain the release of VPH. The results of biopharmaceutical evaluation showed that the rate of absorption appeared
to be more sustained, resulting in a more uniform plasma concentration profile of VPH. More bioavailability was noted with
the sustained release formulation even though the drug has substantial first pass metabolism. The results indicated that it is
possible to make once-a-day sustained-release tablet of VPH by using the melt granulation technique.
Key words: Biopharmaceutical evaluation, melt granulation, precirol ATO 5, sustained release, verapamil hydrochloride
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Tripathi K D. Essentials of Medical Pharmacology. 5th ed. New Delhi:
Jaypee Brothers Medical Publishers; 2003. p. 495-8.
Indian Pharmacopoeia Government of India. Ministry of Health and
Family Welfare. Vol. 2. New Delhi: The controller of publications; 1996.
Passerini N, Apertini B. Preparation and characterization of
ibuprofen- poloxamer 188 granules obtained by melt granulation. Eur
J Pharm Sci 2002;15:71-8.
Saraiya D, Bolton S. The use of precirol to prepare sustained release
tablet of theophylline and quinidine gluconate. Drug Dev Ind Pharm
Sprockel OL, Sen M, Shivanand P, Prapaitrakul W. Melt extrusion
processes for manufacturing matrix drug delivery systems. Int J Pharm
Bansal P, Haribhakti K, Subramanian V, Plako Giannis F. Effect of
formulation and process variables on dissolution profile of Naproxen
sodium from tablets. Drug Dev Ind Pharm 1994;20:2151-6.
Taggart CM, Ganley JA, Sickmulller A, Walker SE. The evaluation of
formulation and processing conditions of a melt granulation process.
Int J Pharm 1984;19:139-48.
Royce A, Suryvanshi J, Shah U, Vishnupad K. Alternative granulation
technique: Melt granulation. Drug Devl Ind Pharm 1996;22:917-24.
Rowe RC, Sheskey PJ, Weller PJ. A Handbook of Pharmaceutical
excipients. 4th ed. Pharmaceutical Press, American Pharmaceutical
Association; 2003. p. 267-8, 260-1, 106-7, 669-71.
Paradkar AR, Maheshwari M, Chauhan MB. Sustained release matrices
of metformin hydrochloride and glyceryl behenate. Indian Drugs
Aulton ME. Pharmaceutics: The Science of Dosage Form Design. 2nd ed.
Livingstone C: Elsevier Science Ltd; 2002. p. 315-20.
More HN, Hazare AA. Practical Pharmaceutics (Physical pharmacy).
st ed. Kolhapur: Manas Prakashan; 2004. p. 86-105.
Hausner HH. Friction conditions in a mass of metal powder. Int J of
Pow Metall 1967;3:7-13.
Clark. Clarkâ€™s Analysis of Drugs and Poisons. 2nd ed. Pharmaceutical
Press, American Pharmaceutical Association; 2004.
Chatwal GR, Anand SK. Instrumental methods of chemical analysis.
th ed. Himalaya Publishing House; 2002. p. 2.55, 2.318-31, 2.747-8.
Indian Pharmacopoeia Government of India, Ministry of Health and
Family Welfare. Vol. 2. New Delhi: The controller of publications; 1996. p.
The United State Pharmacopoeia, United State Pharmacopoeial
Covenction. Asian ed. Rockville, MD:2000; p. 1741-2.
Paulo C, Jose M, Sousa L. Modeling and comparison of dissolution
profiles. Eur J Pharm Sci 2001;13:123-33.
Brahmankar DM, Jaiswal SB. Textbook of Biopharmaceutics and
Pharmacokinetics, 1st ed. Delhi: Vallabh Prakashan; 1995. p. 212-27.
Mallick S, Gupta BK, Ghosal SK. Biopharmaceutical evaluation of oral
controlled release verapamil hydrochloride microcapsules. I J Pharm
Mallick S, Gupta BK, Ghosal SK. Extractive spectrophotometric
determination of nifedipine and verapamil hydrochloride. Eastern
Dhumal R, Shimpi S, Chauhan B, Mahadik K, Paradkar A. Evaluation
of a drug with wax-like properties as a melt binder. Acta Pharm
Sadeghi F, Garekani HA, Sadeghi R. Composition of ethylcellulose matrix
characteristics prepared by solid dispersion technique or physical
mixing. DARU 2003;11:7-13.
Hamdani J, Moes AJ, Amighi K. Physical and thermal characterization of
precirol and compritol as lipophilic glycerides used for the preparation
of controlled release matrix tablets. Int J Pharm 2003;260:47-57.
Reza MS, Quadir MA, Haider SS. Comparative evaluation of plastic,
hydrophobic and hydrophilic polymers as matrices for controlled
release drug delivery. J Pharm Pharmac Sci 2003;6:282-91.
Jordhan T, Mandal TK. Effect of lactose on drug release from plastic
matrix system. Pharm Res 1995;12:170.