Enhancement of water solubility of felodipine by preparing solid dispersion using poly-ethylene glycol 6000 and poly-vinyl alcohol

P G Bhole, V R Patil


In the present study, solid dispersion (SD) of felodipine was prepared to enhance its water solubility.The SD was prepared by using polyethylene glycol (PEG 6000) and polyvinyl alcohol (PVA) as a carrier with different drug polymer ratios
using different techniques (physical mixing and solvent evaporation).The product was characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD) and in vitro dissolution rate studies. Phase solubility analysis was performed in aqueous solution for drug polymer interactions. DSC and XRD analysis demonstrated the conversion of felodipine to amorphous form with both physical mixture (PM) and SD. SD with PVA released 95% of the drug in 85 min as compared with 89% of drug released in 90 min by SD with PEG 6000.Thus, SD with both polymers increased drug release, particularly greater in the case of PVA than PEG 6000.

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Dollery C. editor. In: Therapeutic drugs. 2nd ed. New York: Churchill

Livingstone; 1999.

Abernethy DR, Schwartz JB. Calcium-Antagonist Drugs. N Engl J Med


Blychert E, Edgar B, Elmfeldt D, Hedner T. A Population Pharmacokinetics

of Felodipine. Br J Clin Pharmacol 1997;31:15-24.

Budavari S. et al. editors. In: The Merck Index, Merck Research

Laboratories. 12th ed. INC, White House, N.J: Division of Merck and

company; 1996. p. 670.

Moffat AC, Osselton MD, Widdop B. Clarke’s Analysis of drugs. Vol. 2.

rd ed. Pharmaceutical Press; 2002. p. 1018-9.

Anzai K, Mizoguchi J, Yanagi T, Hirayama F, Arima H, Uekama K.

Improvement of dissolution properties of a new helicobacter

pylori eradicating agent (tg44) by inclusion complexation with

beta- yclodextrin. Chem Pharm Bull (Tokyo) 2007;55:1466-70.

Ki HM, Choi HK. The effect of meloxicam/ethanolamine salt

formation on percutaneous absorption of meloxicam. Arch Pharm Res


Barzegar-Jalali M, Nayebi AM, Valizadeh H, Hanaee J, Barzegar- alali

J A, Adibkia K, et al. Evaluation of in vitro-in vivo correlation and

anticonvulsive effect of carbamazepine after cogrinding with

microcrystalline cellulose. J Pharm Pharm Sci 2006;9:307-16.

Wang L, Cui FD, Hayase T, Sunada H. Preparation and evaluation of

solid dispersion for nitrendipine-carbopol and nitrendipine-hpmcp

systems using a twin screw extruder. Chem Pharm Bull (Tokyo)


Kim EJ, Chun MK, Jang JS, Lee IH, Lee KR, Choi HK. Preparation of a

solid dispersion of felodipine using a solvent wetting method. Eur J

Pharm Biopharm 2006;64:200-5.

Leonardi D, Barrera MG, Lamas MC, Saloman CJ. Development of

prednisolone: Polyehylene glycol 6000 Fast-release Tablets From

Solid Dispersions: Solid-State Characterization, Dissolution Behavior,

and Formulation Parameters. AAPS PharmSciTech 2007;8:E108.

Sammour OA, Hammad MA, Megrab NA, Zidan AS. Formulation and

optimization of mouth dissolve tablets containing rofecoxib solid

dispersion. AAPS PharmSciTech 2006;7:E55.

Vijaya Kumar SG, Mishra DN. Preparation, characterization and in vitro

dissolution studies of solid dispersion of meloxicam with peg 6000.

Yakugaku Zasshi 2006;126:657-64.

Serajjudin AT. Solid dispersion of poorly water soluble drugs: early

promises, subsequent problems and recent breakthroughs. J Pharm

Sci 1999;88:1058-66.

Chawala G, Bansal AK. Improved dissolution of a poorly water soluble

drug in solid dispersions with polymeric and non-polymeric hydrophilic

additives. Acta Pharm 2008;58:257-74.

DOI: http://dx.doi.org/10.22377/ajp.v3i3.273


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