ENHANCEMENT OF THE SOLUBILITY AND THE DISSOLUTION RATE OF TAMOXIFEN CITRATE SOLID DISPERSION USING SOLUPLUS BY SOLVENT EVAPORATION TECHNIQUE

Hayder Hussein Abduljabbar; Shaimaa Nazar Abd Alhammid

doi:10.22159/ajpcr.2019.v12i1.28933

Authors

Hayder Hussein Abduljabbar Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Baghdad, Iraq.
Shaimaa Nazar Abd Alhammid Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Baghdad, Iraq.

DOI:

https://doi.org/10.22159/ajpcr.2019.v12i1.28933

Keywords:

Tamoxifen citrate, Solid dispersion, Nil, Orodispersible tablet, Superdisintegrants

Abstract

Objective: The aim of the present study was the enhancement in the solubility of tamoxifen citrate using solid dispersion which is considered as a great solution to overcome the poor water solubility behavior of tamoxifen citrate (TMX) by solvent evaporation technique using SoluplusÂ® as a novel carrier then formulate it as an orodispersible tablet.

Method: A total of 24 formulas were prepared as a solid dispersion by solvent evaporation method using SoluplusÂ® as a polymeric solubilizer in the ratio of 1:1, 1:3, 1:5, 1:7, and 1:10 then formulated as orodispersible tablets by incorporating three types of superdisintegrants; croscarmellose, crospovidone, and sodium starch glycolate (SSG) with the solid dispersion. Characterization of the formulation was done using differential scanning colorimetry, Fourier transforms infrared spectroscopy, X-ray diffraction, and scanning electron microscope and the best formula was selected according to the disintegration and dissolution tests.

Results and Discussion: Formula 22 were selected as the best formula which contains mixed types of superdisintegrants; croscarmellose and SSG with the fastest complete disintegration of 6.5 s and complete dissolution with <2 min.

Conclusion: Accordingly, TMX was successfully enhanced its water solubility by converting its crystalline structure into the amorphous state through solid dispersion with SoluplusÂ® and formulated as an orodispersible tablet to improve its oral absorption.

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Author Biographies

Hayder Hussein Abduljabbar, Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Baghdad, Iraq.

College of Pharmacy University of Baghdad Iraq

Shaimaa Nazar Abd Alhammid, Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Baghdad, Iraq.

College of Pharmacy University of Baghdad Iraq

References

Hortobagyi GN, de la Garza Salazar J, Pritchard K, Amadori D, Haidinger R, Hudis CA, et al. The global breast cancer burden: Variations in epidemiology and survival. Clin Breast Cancer 2005;6:391-401.

Ravikumara NR, Bharadwaj M, Madhusudhan B. Tamoxifen citrate-loaded poly(d,l) lactic acid nanoparticles: Evaluation for their anticancer activity in vitro and in vivo. J Biomater Appl 2016;31:1-18.

Beale, JM, Block JH. Wilson and Gisvoldâ€™s Textbook of Organic Medicinal and Pharmaceutical Chemistry. 12th ed. Philadelphia, PA, USA: Lippincott, Williams and Wilkins; 2011. p. 834.

Elnaggar YS, El-Massik MA, Abdallah OY. Self-nanoemulsifying drug delivery systems of tamoxifen citrate: Design and optimization. Int J Pharm 2009;380:133-41.

El-Leithy ES, Abdel-Rashid RS. Lipid nanocarriers for tamoxifen citrate/coenzyme Q10 dual delivery. J Drug Deliv Sci Technol 2017;41:239-50.

Meng F, Gala U, Chauhan H. Classification of solid dispersions: Correlation to (I) stability and solubility (II) preparation and characterization techniques. Drug Dev Ind Pharm 2015;41:1401-15.

Baghel S, Cathcart H, Oâ€™Reilly NJ. Polymeric amorphous solid dispersions: A review of amorphization, crystallization, stabilization, solid-state characterization, and aqueous solubilization of biopharmaceutical classification system class II drugs. J Pharm Sci 2016;105:2527-44.

Yadav Sh K, Veena M, Srinivas M. Solid dispersion techneque to enhance the solubility and dissolution rate of aripiprazole by fusion method. Int J Pharm Pharm Sci 2016;8:187-192.

Reginald-Opara JN, Attama A, Ofokansi K, Umeyor C, Kenechukwu F. Molecular interaction between glimepiride and soluplus-PEG 4000 hybrid based solid dispersions: Characterisation and anti-diabetic studies. Int J Pharm 2015;496:741-50.

Mohammadi G, Hemati V, Nikbakht MR, Mirzaee S, Fattahi A, Ghanbari K, et al. In vitro and in vivo evaluation of clarithromycin-urea solid dispersions prepared by solvent evaporation, electrospraying and freeze drying methods. Powder Technol 2014;257:168-74.

Fule R, Amin P. Development and evaluation of lafutidine solid dispersion via hot melt extrusion: Investigating drug-polymer miscibility with advanced characterisation. Asian J Pharm Sci 2014;9:92-106.

Khan AW, Kotta S, Ansari SH, Sharma RK, Ali J. Enhanced dissolution and bioavailability of grapefruit flavonoid naringenin by solid dispersion utilizing fourth generation carrier. Drug Dev Ind Pharm 2015;41:772-9.

Huang Y, Dai WG. Fundamental aspects of solid dispersion technology for poorly soluble drugs. Acta Pharm Sin B 2014;4:18-25.

Shamma RN, Basha M. SoluplusÂ®: A novel polymeric solubilizer for optimization of carvedilol solid dispersions: Formulation design and effect of method of preparation. Powder Technol 2013;237:406-14.

Dave V, Yadav RB, Ahuja R, Sahu AK. Formulation and evaluation of orally dispersible tablets of chlorpheniramine maleate by fusion method. Marmara Pharm J 2017;21:67-77.

Shankarrao KA, Mahadeo GD, Balavantrao KP. Formulation and in vitro evaluation of orally disintegrating tablets of olanzapine-2- hydroxypropyl-beta-cyclodextrin inclusion complex. Iran J Pharm Res 2010;9:335-47.

Ge Z, Yang M, Wang Y, Shan L, Gao C. Preparation and evaluation of orally disintegrating tablets of taste masked phencynonate HCl using ion-exchange resin. Drug Dev Ind Pharm 2015;41:934-41.

Kimura SI, Uchida S, Kanada K, Namiki N. Effect of granule properties on rough mouth feel and palatability of orally disintegrating tablets. Int J Pharm 2015;484:156-62.

Homayouni A, Sadeghi F, Nokhodchi A. Preparation and characterization of celecoxib dispersions in soluplus Â® : Comparison of spray drying and conventional methods. Iran J Pharm Res 2015;14:35 50.

Shuai S, Yue S, Huang Q, Wang W, Yang J, Lan K, et al. Preparation, characterization and in vitro/vivo evaluation of tectorigenin solid dispersion with improved dissolution and bioavailability. Eur J Drug Metab Pharmacokinet 2016;41:413-22.

Rao NR, Patel T, Gandhi S. Development and evaluation of carbamazepine fast dissolving tablets prepared with a complex by direct compression technique. Asian J Pharm 2009;3:97-105.

Khairnar DA, Anantwar SP, Chaudhari CS, Shelke PA. Superdisintegrants: An emerging paradigm in orodispersible tablets. Int J Biopharm 2014;5:119-28.

Egla M, Abd Al hammid Sh N. Design zolmitryptan liquisolid orodispersible tablets and their in vitro evaluation. Int J Pharm Pharm Sci 2017;9:297-303.