FORMULATION AND EVALUATION OF TELMISARTAN SOLID DISPERSIONS USING ENTADA SCANDENS SEED STARCH AND POLOXAMER-188 AS SUPERDISINTEGRANTS
DOI:
https://doi.org/10.22159/ajpcr.2018.v11i9.28422Keywords:
Entada scandens, Solid dispersions, Telmisartan, Poloxamer-188Abstract
Objective: The current research focuses on solubility enhancement of poorly water-soluble drug telmisartan, using novel superdisintegrants such as Entada scandens seed starch and Poloxamer-188. Starches yielded from plants are pharmaceutically useful as binders, diluents, disintegrants, and lubricants.
Methods: Starches were extracted from E. scandens seed powder using alkali method (sodium hydroxide at 0.1%, 0.25%, and 0.5% concentrations) and water. These starches were subjected for the evaluation of various physicochemical properties and phytochemical tests.
Results: The phytochemical tests revealed the presence of only starch in all the extracts. Of all the starches, the starch prepared from 0.5% sodium hydroxide (ESS4) showed best physicochemical properties. Solid dispersions were prepared using telmisartan, poloxamer-188, and starch (ESS4) in various concentrations using fusion technique. Various pre-formulation parameters were evaluated. From in vitro dissolution studies, it was observed that the solid dispersion formulation TP7 containing telmisartan and poloxamer-188 in 1:4 ratios showed better dissolution rate. Solid dispersion TPS7 containing TP7 formulation and 15% w/w of alkali extracted starch showed faster disintegration and enhanced dissolution rate than the solid dispersions prepared alone with poloxamer-188. Fourier transform infrared spectroscopy and differential scanning calorimetric studies for optimized formulations revealed that there were no major interactions between the drug and excipients. X-ray diffraction studies revealed the crystalline and amorphous nature of formulations.
Conclusion: Thus, the solid dispersions prepared using E. scandens seed starch revealed the superdisintegrant property of starch.
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References
Chiou WL, Riegelman S. Pharmaceutical applications of solid dispersion systems. J Pharm Sci 1971;60:1281-302.
Priya P, Rajendran NN, Lakshmi PK, Umadevi SK, Kaushalya J. A novel captopril hydrochlorthiazide solid dispersion. Int J Pharm Pharm Sci 2010;2:30-2.
Chauhan B, Shimpi S, Paradkar A. Preparation and evaluation of glibenclamide-polyglycolized glycerides solid dispersions with silicon dioxide by spray drying technique. Eur J Pharm Sci 2005;26:219-30.
Bhowmik D, Chiranjib B, Yadav J, Chandira RM, Sampath KP. Emerging trends of disintegrants used in formulation of solid dosage form. Schol Res Lib 2010;2:495-504.
Sunada H, Bi Y. Preparation, evaluation and optimization of rapidly disintegrating tablets. Powder Technol 2002;122:188-98.
Dey SK, Rahman M, Ahmed A, Khatun A, Siraj A. Phytochemical screening and pharmacological activities of Entada scandens seeds. Int J Appl Res Nat Prod 2013;6:34-9.
Benson SC, Pershad SH, Chittiboyina A, Desai P, Pravenec M, Wang J. Identification of telmisartan as a unique angiotensin II receptor antagonist with selective PPAR-modulating activity. Hypertension 2004;43:993-1002.
Fateatun N, Jiaur RM, Sultan MM, Ahmed M. Physicochemical properties of flour and extraction of starch from jack fruit seed. Int J Nut Food Sci 2014;3:347-54.
Menaka T, Nagaraja G, Yogesh DB, Sunil US, Prakash L. Physicochemical properties of flour and isolated starch from jack fruit seeds. Res J Pharm Sci 2011;01:14-8.
Okunlola A, Odeku OA. Comparative evaluation of starches obtained from Dioscorea species as intragranular tablet disintegrants. J Drug Del Sci Technol 2008;18:445-7.
Hetal P, Mukesh G. A review on development of multifunctional co-processed excipient. J Crit Rev 2016;3:48-54.
Ghareeb MM, Abdulrasool AA, Hussein AA, Noordin MI. Kneading technique for preparation of binary solid dispersion of meloxicam with poloxamer 188. AAPS Pharm Sci Tech 2009;10:1206-15.
Quadir A, Kolter K. A comparative study of current superdisintegrants. Pharm Technol 2006;10:1-4.
Shashikumar Y, Veena M, Srinivas M. Solid dispersion technique to enhance the solubility and dissolution rate of aripiprazole by fusion method. Int J Pharm Pharm Sci 2016;8:187-92.
Vidyadhara S, Sasidhar RL, Lakshmi HD, Vijetha P, Vijetha K. Studies on jack fruit seed starch as a novel natural superdisintegrant for the design and evaluation of irbesartan fast dissolving tablets. Int Med Res 2017;6:280-91.
Gubbi S, Jarag R. Liquisolid technique for enhancement of dissolution properties of bromhexine hydrochloride. Res J Pharm Technol 2009;2:382-6.
Anshu S, Chandra PJ, Yuveraj ST. Prepartaion and characterization of solid dispersions of carvedilol with poloxamer-188. J Chil Chem Soc 2013;58:1553-7.
Vipan KK, Prabhakar KV. Preparation and characterization of metformin loaded stearic acid coupled F127 nanoparticles. Asian J Pharm Clin Res 2018;11:212-7.
Isha S, Shailendra B, Alpesh Y. Enhancement of solubility and dissolution of nebivolol by solid dispersion technique. Int J Pharm Pharm Sci 2014;6:566-71.
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