Formulation and evaluation of glimepiride solid dispersion tablets

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Published: Aug 23, 2014
DOI: https://doi.org/10.22377/ajp.v4i3.221

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Bhawandeep Gill
Tejvir Kaur
Sandeep Kumar
G D Gupta

Abstract

Glimepiride (GMP) is poorly water soluble drug, so solubility is the main constraint for oral its bioavailability. An attempt has been made to increase the solubility of this model drug by formulating solid dispersion (SD) using Poloxamer 188(PXM 188) as polymer and then formulating SDs tablets of the best formulation of SDs. Tablet formulations were prepared by direct compression technique using superdisintegrant croscarmellose sodium in different concentrations. SDs were evaluated for XRD, SEM, in vitro dissolution profiles, and dissolution efficiency, and developed tablet formulations were
evaluated for various pharmaceutical characteristics viz. hardness, % friability, weight variation, drug content, disintegration time, in vitro dissolution profiles, and dissolution efficiency. Among different formulations of SDs, SD containing drug is to polymer ratio 1 : 4 gives best dissolution profile and dissolution efficiency and among tablet formulations, formulations containing 5% croscarmellose sodium gives best disintegration and dissolution profiles compared with other formulations. Results showed that poloxamer is a promising polymer for enhancing the solubility of GMP.

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How to Cite
Gill, B., Kaur, T., Kumar, S., & Gupta, G. D. (2014). Formulation and evaluation of glimepiride solid dispersion tablets. Asian Journal of Pharmaceutics (AJP), 4(3). https://doi.org/10.22377/ajp.v4i3.221
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Vol. 4 No. 3 (2010): Jul-Sep
Section
Articles

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References

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:

-20.

Nokhodchi A, Javadzadeh Y, Reza M, Barzegar JM. The effect of type

and concentration of vehicles on the dissolution rates of a poorly

water soluble drug (indomethacin) from liquisolid compacts. J Pharm

Pharm Sci 2005;8:18-25.

Chiou WL, Rigelman S. Pharmaceutical application of solid dispersion

system. J Pharm Sci 1971;60:1281-302.

Serajuddin A. Solid dispersion of poorly water soluble drugs: early

promises, subsequent problems and recent breakthroughs. J Pharm

Sci 1999;88:1058-66.

Leuner C, Dressman J. Improving drug solubility for oral delivery using

solid dispersions. Eur J Pharm Biopharm 2000;50:47-60.

Sekiguchi K, Obi N. Studies on absorption of eutectic mixture-I. Chem

Pharm Bull 1961;9:866-72.

Liu C, Liu C, Desai KGH. Enhancement of dissolution rate of valdecoxib

using solid dispersions with polyethylene glycol 4000. Drug Dev Ind

Pharm 2005;31:1-10.

Verheyen S, Blaton N, Kinget R, Van den Mooter G. Mechanism of

increased dissolution of diazepam and temazepam from polyethylene

glycol 6000 solid dispersions. Int J Pharm 2002;249:45-58.

Hirasawa N, Ishise S, Miyata H. An attempt to stabilize nivaldipine

solid dispersion by the use of ternary systems. Drug Dev Ind Pharm

;29:997-04.

Karavas E, Ktistis G, Xenakis A, Georgarakis E. Miscibility behavior and

formation mechanism of stabilized felodipine-polyvinylpyrrolidone

amorphous solid dispersions. Drug Dev Ind Pharm 2005;31:473-89.

Hirasawa N, Danij K, Haruna M, Otsuka A. Physicochemical

characterization and drug release studies of naproxen solid dispersions

using lactose as a carrier. Chem Pharm Bull (Tokyo) 1998;46:1027-30.

Zheng Y, Haworth IS, Zuo Z, Chow MS, Chow AH. Physicochemical and

structural characterization of Quercetin-β-Cyclodextrin complexes. J

Pharm Sci 2005;94:1079-89.

Rawat S, Jain SK. Rofecoxib-beta-cyclodextrin inclusion complex for

solubility enhancement. Pharmazie 2003;58:639-41.

Okimoto K, Miyake M, Ibuki R, Yasumura M, Ohnishi N, Nakai

T. Dissolution mechanism and rate of solid dispersion particles

of nivaldipine with hydroxypropylmethylcellulose. Int J Pharm

;159:85-93.

Chutimaworapan S, Ritthidej GC, Yonemochi E, Oguchi T, Yamamoto

K. Effect of water soluble carriers on dissolution characteristics of

nifedipine solid dispersions. Drug Dev Ind Pharm 2000;26:1141-50.

Chen Y, Zhang G, Neilly J, Marsh K, Mawhinney D, Sanzgiri Y. Enhancing the bioavailability of ABT-963 using solid dispersion containing Pluronic F-68. Int J Pharm 2004;286:69-80.

Mehta K, Kislalioglu S, Phuapradit W, Malick W, Shah N. Multi-unit

controlled release systems of Nifedipine and Nifedipine:Pluronic F-68

solid dispersions: characterization of release mechanisms. Drug Dev

Ind Pharm 2002;28:275-85.

Schmolks IR. Poloxamers in controlled drug delivery. In: Tarcha PJ,

ed. Polymers for Controlled Drug Delivery. Boca Raton, FL: CRC Press;

P. 189-14.

Seo A, Holm P, Kristensen HG, Schaefer T. The preparation of

agglomerates containing solid dispersions of diazepam by melt

agglomeration in a high shear mixer. Int J Pharm 2003;259:161-71.

Saettone MF, Giannacini B, Delmonte G, Campigli V, Tota G, LaMarca

F. Solubilization of tropicamide by poloxamers:physicochemical data

and activity data in rabbits and humans. Int JPharm 1988;43:67-76.

Passerini N, Albertini B, GonzalezRodriguez ML, Cavallari C, Rodriguez

L. Preparation on and characterization of ibuprofen-poloxamer 188

granules obtained by melt granulation. Eur J Pharm Sci 2002;15:71-78.

Kwon GS. Polymeric micelles for delivery of poorly water-soluble

compounds. Crit Rev Ther Drug Carrier Syst 2003;20:357-03.

Yong CS, Yang CH, Rhee JD, Lee BJ, Kim DC, Kim DD, et al. Enhanced

rectal bioavailability of ibuprofen in rats by poloxamer 188 and menthol.

Int J Pharm 2004;269:169-76.

Kabanov KV, Batrakova EV, AlakhovVY. Pluronic block copolymers as

novel polymer therapeutics for drug and gene delivery. J Control

Release 2002;82:189-12.

Jones MC, Leroux JC. Polymeric micelles-a new generation of colloidal

drug carriers. Eur J Pharm Biopharm 1999;48:101-11.

Chen Y, Zhang GGZ, Neilly J, Marsh K, Mawhinney D, Sanzgiri YD.

Enhancing the bioavailability of ABT-963 using solid dispersion

containing pluronic F-68. Int J Pharm 2004;286:69–80

Frick A, Moller H, Wirbitzki E. In vitro/in vivo biopharmaceutical

characterization of oral immediate release drug products. Comparison

of phenoxymethylpenicillin potassium, glimepiride and levofloxacin.

Eur J Pharm Biopharm 1998;46:305-11.

Davis SN. The role of glimepiride in the effective management of type 2 diabetes. J Diabetes Complications 2004;18:367-76.