Asian Journal of Pharmacy and Technology

Open Access Open Access  Restricted Access Subscription Access
Open Access Open Access Open Access  Restricted Access Restricted Access Subscription Access

Preparation and Evaluation of Solid Dispersion of Terbinafine Hydrochloride


Affiliations
1 Seven Hills College of Pharmacy, Tirupati-517561, Andhra Pradesh, India
2 Vikas Institute of Pharmaceutical Sciences, Andhra Pradesh, India
3 Jawaharlal Nehru Technological University, Anantapur, Andhra Pradesh, India
     

   Subscribe/Renew Journal


Terbinafine hydrochloride is a synthetic antifungal drug. It is slightly soluble in water (3mg/ml) and having high permeability through stomach. This results in poor bioavailability after oral administration. Therefore solid dispersion of terbinafine HCl with polyethylene glycol-6000 (PEG 6000) and mannitol were prepared with a view to increase its water solubility. In this study solid dispersion of the drug were prepared by melting method and the drug was taken with carrier in the proportions of (1:1, 1:2 and 1:3). The rate of dissolution of terbinafine HCl was increased with the proportion of (1:3) (Drug: PEG 6000) when compared to the other formulations. In order to predict and correlate the release behavior of the drug from the polymer matrix the dissolution data were fitted in to a suitable model to describe the drug release behavior from polymeric system. The surface morphology of the prepared solid dispersion and drug alone were examined by SEM analysis. The SEM result shows that in the case of solid dispersion of terbinafine HCl, particles were in almost amorphous form, which indicates a reduction in particle size.

Keywords

Antifungal, Bioavailability, Solid Dispersion, Polymer Matrix, SEM
Subscription Login to verify subscription
User
Notifications
Font Size


  • Betageri GV and Makarla KR . Enhancement of dissolution of glyburide by solid dispersion and lyophilization techniques. Int. J. Pharm. 126(1);1995:155-160.

  • Breitenbach J, Schrof W and Neumann J . Confocal Ramanspectroscopy: analytical approach to solid dispersions and mapping of drugs. Pharm. Res.16(7);1999:1109-1113.

  • Chiou WL and Riegelman S. Preparation anddissolution characteristics of several fast-release soliddispersions of griseofulvin. J. Pharm. Sci.58(12);1969:1505-1510.

  • Ho HO, Shu HL, Tsai T and Sheu MT. The preparation and characterization of solid dispersions on pellets using a fluidized bed system. Int. J. Pharm.139;1996: 223-229.

  • Lloyd GR, Craig DQ and Smith A. An investigation into the melting behavior of binary mixes and solid dispersions of paracetamol and PEG 4000. J.Pharm. Sci.86(9);1997: 991-996.

  • Morris KR, Knipp GT and Serajuddin ATM. Structural properties of poly (ethylene glycol)-polysorbate 80 mixture, a solid dispersion vehicle. J.Pharm. Sci.81(2);1992:1185-1188.

  • Moneghini M, Kikic I, Voinovich D and Perissutti B. Processing of carbamazepine-PEG 4000 solid dispersions with supercritical carbon dioxide: preparation, characterization, and in vitro dissolution.Int. J. Pharm.222(1);2001: 129-138.

  • Batra V, Shirolkar V.S, Mahaparaie P.R, Solubility and dissolution enhancement of Glipizide by solid dispersion technique.Int.J.Pharm.42(4); 2008:1:373-378 .

  • Vanshiv S.D, Rao M.R.P, Sonar G.S, Physicochemical characterization and invitro dissolution of Domperidene by solid dispersion technique. Int.J.Pharm.43(1);2009: 1:86-90.

  • Bada pragati kumar, Rama Krishna Reddy M, Enhancing in vitro bioavailability of Nevirapine by employing solid dispersion technique. J.Chem. and Pharm. Sci. 4(1);2011:86-92.

  • Meka lingam, Vobalaboina venkateswarlu, Enhancement of solubility and dissolution rate of poorly water soluble drug using co-solvency and solid dispersion techniques. Int.J. Pharm. Sci and Nano Tech.l.1(1);2009: 349-356.

  • Bhawandeep gill, Tejvir kaur, Sandeep kumar, Formulation and evaluation of Glimepiride solid dispersion tablets. Assn. J. Pharmaceutics.1(4); 2010:212-218.

  • Rajesh Kumar Maheshwari, Arpna Indurkhta, Novel application of mixed hydrotropic solubilization technique in the formulation and evaluation of hydrotropic solid dispersion of Aceclofenac. Assn.J.Pharmaceutics.1(4);2010:235-238.

  • Bourne DWA. Pharmacokinetics. In: Banker GS, Rhodes CT, Modern Pharmaceutics, 4th ed., Marcel Dekker Inc., New York.2002.

  • Lordi NG . Sustained release dosage form. In: The Theory and Practice of Industrial Pharmacy, 3rd Ed., Lea and Febiger, Philadelphia, USA.1986

  • Cox PJ, Khan KA, Munday DL and Sujja-areevath J. Development and evaluation of a multiple-unit oralsustained release dosage form for S (+)-ibuprofen: preparation and release kinetics. Int.J. Pharm.193(2);1999: 73-84.

  • Siepmann J, Kranz H, Peppas NA and Bodmeier R. Calculation of the required size and shape of hydroxypropylmethylcellulose matrices to achieve desired drug release profiles. Int. J. Pharm. 201 (3);2000: 151-164.

  • Siepmann J, Kranz H, Bodmeier R and Peppas NA .HPMCmatrices for controlled drug delivery: a new model combining diffusion, swelling and dissolution mechanisms and predicting the release kinetics. Pharm. Res.16(4);1999: 1748-1756.


Abstract Views: 513

PDF Views: 2




  • Preparation and Evaluation of Solid Dispersion of Terbinafine Hydrochloride

Abstract Views: 513  |  PDF Views: 2

Authors

Subhashis Debnath
Seven Hills College of Pharmacy, Tirupati-517561, Andhra Pradesh, India
Gampa Vijay Kumar
Vikas Institute of Pharmaceutical Sciences, Andhra Pradesh, India
S. V. Satyanarayana
Jawaharlal Nehru Technological University, Anantapur, Andhra Pradesh, India

Abstract


Terbinafine hydrochloride is a synthetic antifungal drug. It is slightly soluble in water (3mg/ml) and having high permeability through stomach. This results in poor bioavailability after oral administration. Therefore solid dispersion of terbinafine HCl with polyethylene glycol-6000 (PEG 6000) and mannitol were prepared with a view to increase its water solubility. In this study solid dispersion of the drug were prepared by melting method and the drug was taken with carrier in the proportions of (1:1, 1:2 and 1:3). The rate of dissolution of terbinafine HCl was increased with the proportion of (1:3) (Drug: PEG 6000) when compared to the other formulations. In order to predict and correlate the release behavior of the drug from the polymer matrix the dissolution data were fitted in to a suitable model to describe the drug release behavior from polymeric system. The surface morphology of the prepared solid dispersion and drug alone were examined by SEM analysis. The SEM result shows that in the case of solid dispersion of terbinafine HCl, particles were in almost amorphous form, which indicates a reduction in particle size.

Keywords


Antifungal, Bioavailability, Solid Dispersion, Polymer Matrix, SEM

References