Solid-phase preparation and characterization of albendazole solid dispersion

Authors

  • R KALAISELVAN Department of Pharmacy Annamalai University, Annamalai Nagar, Tamil Nadu -608.002, India.
  • GP MOHANTA Department of Pharmacy Annamalai University, Annamalai Nagar, Tamil Nadu -608.002, India.
  • PK MANNA Department of Pharmacy Annamalai University, Annamalai Nagar, Tamil Nadu -608.002, India.
  • A MANIMEKALAI Department of Chemistry, Annamalai University, Annamalai Nagar, Tamil Nadu -608.002, India.

Keywords:

Bioavailability, Solid dispersion, Solid-state interaction

Abstract

Solid dispersion of albendazole (ABZ) was prepared by powder mixing method using Eudragit E-100 (EGT) as a carrier.The X-ray diffraction patterns and differential scanning calorimetric thermograms demonstrated that the crystallinity ofthe drug in the physical mixture decreased with the storage time. The higher the storage temperature and the higherthe relative humidity, and the higher the weight ratio of polymer in the mixture, the lower was the heat of fusion of thestored mixture. The specifi c interaction of ABZ with EGT in the solid state was investigated by infrared spectroscopy,and nuclear magnetic resonance. It was understood that EGT undergoes N-protonation, forming hydrogen bond at thetertiary nitrogen, in preference to O-protonation. Phase solubility study showed a linear increase in the solubility withthe polymer concentration. The enhancement of dissolution rate and the dissolution effi ciency depended on the heat offusion value as well as mixing ratio of the polymer. The stored mixture showed a signifi cantly enhanced bioavailabilityin rabbits compared to the freshly prepared one.

Downloads

Download data is not yet available.

References

Wissing S, Craig DQM, Barker SA, Moore WD. The use of stepwise isothermal high sensitivity DSC as a means of detecting drug excipient incompatibility. Int J Pharm 2000; 199: 141–150.

Otsuka M, Matsuda Y. Effect of cogrinding with various kinds of surfactants on the dissolution behavior of phenytoin. J Pharm Sci 1995; 84: 1434–1437.

Shakhtshneider TP, Vasiltchenko MA, Politov AA, Boldyrev VV. The mechanochemical preparation of solid disperse systems of ibuprofen-polyethylene glycol. Int J Pharm 1996; 130: 25–32.

Watanabe T, Ohno I, Wakiyama N, Kusai A, Senna M. Stabilization of amorphous indomethacin by cogrinding in a ternary mixture. Int J Pharm 2002; 241: 103–111.

Sekizaki H, Danjo K, Eguchi H, Yonezawa Y, Sunada H, Otsuka A. Solid-state interaction of ibuprofen with polyvinylpyrrolidone. Chem Pharm Bull 1995; 43: 988–993.

Watanabe T, Wakiyama N, Usui F, Ikeda M, Isobe T, Senna M. Stability of amorphous indomethacin compounded with silica. Int J Pharm 2001; 226: 81–91.

Wen H, New RRC, Craig PS. Diagnosis and treatment of human hydatidosis. Br J Clin Pharmac 1993; 35: 565–574.

Lecuit N, Oksenhendler E, Sarfati C. The use of albendazole for disseminated microsporidian infection in patients with AIDS. Clin Infect Dis 1994; 19: 332–333.

Misra PK, Kumar A, Agarwal U, Jagota SC. A comparative clinical trial of albendazole vs metronidazole in giardiasis. Indian Pediatr 1995; 32: 291–294.

WHO Informal Working Group on Echinococcosis. Guidelines for treatment of Cystic alveolar echinococcosis in humans. Bull WHO 1996; 74: 231–242.

Lopez-Garcia ML, Torrado-Duran S, Torrado-Duran J, Martinez AR, Bolas F. Albendazole versus ricobendazole against enteral and parenteral stages of Trichinella spiralis in mice. Int J Parasitol 1997; 27: 781–785.

Keramidas D, Mavridis G, Soutis M, Passalidis A. Medical treatment of pulmonary hydatidosis: complications and surgical management. Pediatr Surg Int 2004; 19: 774–776.

Amidon GL, Lennernas H, Shah VP, Crison JR. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 1995; 12: 413–420.

Jung H, Medina L, Garcia L, Fuentes I, Esparza RM. Absorption studies of albendazole and some physicochemical properties of the drug and its metabolite, albendazole sulphoxide. J Pharm Pharmacol 1998; 50: 43–48.

Lipinski CA, Lombardo F, Dominy BW, Feeney PJ. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev 1997; 23: 3–25.

Malan CEP, Villiers MM, Lotter AP. Evaluation of compatibility of tablet excipients with albendazole and closantel using DSC and HPLC. Drug Dev Ind Pharm 1997; 23: 533–537.

Higuchi, T. and Connors, K.A. Phase solubility techniques. Adv. Anal. Chem. Instr 1965; 4: 117-212.

Joshi BV, Patil VB, Pokharkar VB. Compatibility studies between carbamazepine and tablet excipients using thermal and non thermal methods. Drug Dev Ind Pharm 2002; 28: 687–694.

Sertsou G, Butler J, Hempenstall J, Rades T. Physical stability and enthalpy relaxation of rug-hydroxypropyl methylcellulose

phthalate solvent change co-precipitates. J Pharm Pharmacol 2003; 55: 35–41.

Miyazaki T, Yoshioka S, Aso Y, Kojima S. Ability of polyvinylpyrrolidone and polyacrylic acid to inhibit the crystallization of amorphous acetaminophen. J Pharm Sci 2004; 93: 2710–2717.

Silverstein RM, Bassler GC, Morrill TC. Spectrometric identification of organic compounds, 4th ed., John Wiley and Sons, New York, 1981; pp. 127–129.

El-Hinnawi MA, Najib NM. Ibuprofen-polyvinylpyrrolidone dispersions. Proton nuclear magnetic resonance and infrared

studies. Int J Pharm 1987; 37: 175–177.

Mura P, Manderioli A, Bramanti G, Ceccarelli L. Properties of solid dispersions of naproxen in various polyethylene glycols. Drug Dev Ind Pharm 1996; 22: 909–916.

Guyot M, Fawaz F, Bildet J, Bonini F, Langueny AM. Physicochemical characterization and dissolution of norfloxacin/

cyclodextrin inclusion compounds and PEG solid dispersions. Int J Pharm 1995; 123: 53–63.

Zingone G, Rubessa F. Release of carbamazepine from solid dispersions with polyvinylpyrrolidone/vinylacetate copolymer

(PVP/PA). STP Pharm Sc 1994; 4: 122–127.

Torre PDL, Torrado S, Torrado S. Preparation, dissolution and characterization of praziquantel solid dispersions. Chem Pharm Bull 1999; 47: 1629–1633.

Khan KA. The concept of dissolution efficiency. J. Pharm. Pharmacol. 1975; 27: 48–49.

Sertsou G, Butler J, Hempenstall J, Rades T. Solvent change co-precipitation with hydroxypropyl methylcellulose phthalate to improve dissolution characteristics of a poorly water-soluble drug. J Pharm Pharmacol 2002; 54: 1041–1047.

McKellar QA, Scott EW. The benzimidazole anthelmintic agent - A review. J Vet Pharmacol Therap 1990; 13: 223–247.

Delatour P, Benoit E, Besse S. Comparative enantioselectivity in the sulphoxidation of albendazole in man, dogs and rats. Xenobiotica 1991; 21: 217–221.

Lopez-Garcia ML, Torrado S, Torrado S, Martinez AR, Bolas F. Methimazole-mediated enhancement of albendazole oral bioavailability and anthelmintic effects against parenteral stages of Trichinella spiralis in mice: the influence of the dose-regime. Vet Parasitol 1998; 75: 209–219.

Published

2006-03-20

How to Cite

1.
KALAISELVAN R, MOHANTA G, MANNA P, MANIMEKALAI A. Solid-phase preparation and characterization of albendazole solid dispersion. Ars Pharm [Internet]. 2006 Mar. 20 [cited 2024 May 18];47(1):91-107. Available from: https://revistaseug.ugr.es/index.php/ars/article/view/5019

Issue

Section

Original Articles