irThe Effect of WaterSoluble Polymers on Felodipine Aqueous Solubility and Complexing Abilities with Natural and Modified β-Cyclodextrin Icreased aqueous solubility of felodipine by water soluble polymers
Iranian Journal of Pharmaceutical Sciences,
Vol. 3 No. 4 (2007),
1 October 2007
,
Page 197-202
https://doi.org/10.22037/ijps.v3.41021
Abstract
Purpose of this study was to investigate the effect of the presence of the watersoluble polymers viz HPMC, PVPand PEG 6000 on aqueous solubility andcomplexation abilities of felodipine with or without presence of β-cyclodextrin (βCD)and HPβCD by phase solubility studies. The data revealed the initial increase in drugsolubility followed by plateau in the presence of relatively low polymer concentrationi.e. 0.25-0.5 %w/v. Phase solubility diagrams of felodipine in ternary systemshowed similar behaviour to binary system without βCD. Addition of water solublepolymer to βCD solution improved βCD solubilizing efficiency due to increase inβCD complexing power toward felodipine. In binary system solubility was found2.5 to about 10 times higher than in water which was further improved in thepresence of 0.25% w/v water soluble polymer. Ternary systems with βCD showedhighest increments in solubility towards felodipine, with 78.8%, 81.8% and 74%improvement after the addition of 0.25% w/v HPMC, PVPand PEG6000,respectively. Our study confirmed that addition of small amounts of hydrophilicpolymer is useful strategy for improving the solublization and complexing abilitiesof cyclodextrins thus allowing less cyclodextrin to be needed to solubilize givenamount of drug. This offers economic advantage. All the polymers under studyshowed synergistic effect on felodipine cyclodextrin solublization by increasingcomplexation efficiency.The highest solubility improvement up to 81.8% wasobtained for βCD ternary system when 0.25% w/v of PVPwas used.
- Complexation
- Cyclodextrin
- Felodipine
- Water soluble polymers
How to Cite
References
[2]Szejtli J. Cyclodextrin technology. Dorderecht:Kluwer academic publishers, 1988.
[3]Ghorab MK, Adeyeye MC. Enhanced bioavail-ability of process induced fast dissolvingibuprofen cogranulated with βcyclodextrin. JPharm Sci 2003; 92: 1690-7.
[4]Sinha VR, Anitha R, Ghosh S, Nanda A, KumariaR. Complexation of celecoxib with βcyclodextrin:Characterization of interaction in solution andin solid state.J Pharm Sci 2005; 94: 696-87.
[5]Irie T, Uekema K. Pharmaceutical application of cyclodextrin: III- Toxicological issues and safetyevaluations. J Pharm Sci1997; 86: 147-62.
[6]Chowdary KPR, Shrinivas SV. Effect of PVP on complexation and dissolution rate of β and hydroxy propyl βcyclodextrin complexes ofcelecoxib.Indian J Pharm Sci2006; 631-4.
[7]Loftsson T, Hreinsdottir D, Masson M. Evaluationof cyclodextrin solubilisation of drug.Int J Pharm2005; 302: 18-28.
[8]Won DH, Sibeum MS, Sook-Pork LJ, HwangSJ. Improved physicochemical characteristics offelodipine solid dispersion particle by supercriticalantisolvent precipitation process. Int J Pharm2005; 301: 199-208.[9]Kim CK, Park JS. Solubility enhancers for oraldrug delivery; can chemical structuremanipulation be avoided. Am J Drug Del2004;2: 113-30.
[10]Higuchi T, Connors KA. Phase solubilitytechniques. Adv Anal Chem Inst1965; 4: 117-213.
[11]Acarturk F, Kislal O, Celebi N. The effect ofsome natural polymers on solubility anddissolution characteristics of nefedipine.Int JPharm1992; 85: 1-6.
[12]Loftsson T, Fririksdottir H, Gumundsdottir TK.The effect of water-soluble polymers on aqueoussolubility of drugs. Int J Pharm1996; 127:293-7.
[13]Loftsson T, Fririksdottir H, Sigurdardottir AM,Ueda H. Effect of water-soluble polymer on drug-cyclodextrin complexation.Int J Pharm1994;110: 169-77.
[14]Loftson T, Fridrikdottir H, Sigurdardottir AM,Ueda HTH. The effect of polymer on cyclodextrin complexation. Seventh international symposiumon cyclodextrin. Osa T, (ed). Tokiyo: AcademicSocieties Japan, 1994; pp.218-21.
[15]Loftson T, Fridricsdottir F, Gudmundsdottir TK.The influence of water soluble polymer and pHon hydroxy propyl β cyclodextrin complexationof drug. Drug Dev Ind Pharm1996; 22: 401-5.
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