Preparation and Characterization of Solid Dispersion of Tinidazole with Benzoic Acid and Tartaric Acid
Keywords:
Solid dispersion, tinidazole, saturation aqueous solubility, humectability, intrinsic dissolution rateAbstract
Two solid dispersions (SDs) were prepared in order to increase the dissolution rate of tinidazole (TND) by applying the method of grinding and moisturizing with drops of ethanol, using tartaric acid (TTA) and benzoic acid (BZA) as carrier agents. These carrier agents showed complete miscibility with TND, according to the DSC results. The two SDs were characterized and compared with pure TND through XRPD, DSC, FT-IR, particle size, water saturation solubility, equivalent specific surface, wettability and intrinsic dissolution rate tests. All samples were evaluated in the same particle range, and it was found that the increase in the dissolution of the two SDs in comparison to the pure drug was not a result of the reduced particle size but of the partial amorphization of the TND. The carrier-drug ratio makes the TND dosage in these two dispersions a promising alternative for the tablet form.References
Yanbin Huang, Wei-Guo Dai.Fundamental aspects of solid dispersion technology for poorly soluble drugs. Review.Acta PharmaceuticaSinicaB;4(1):18–25, 2014.
Chau Le-Ngoc Vo, Chulhun Park, Beom-Jin Lee.Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs.European Journal of Pharmaceutics and Biopharmaceutics 85. 799–813, 2013.
Yanbin Huang, Wei-Guo Dai. Fundamental aspects of solid dispersion technology for poorly soluble drugs. Acta Pharmaceutica Sinica B;4(1):18–25, 2014.
Dumbre K.A, Gadhave M.V, Gaikwad D.D. Development, evaluation and characterization of surface solid dispersion for solubility and dissolution enhancement of nifedipine. Asian Journal of Pharmaceutical Research and Development Vol. 2 (3) May–June 70-77, 2014.
Iswarya Sridhar, Abha Doshi, Bhagyashri Joshi, Vandana Wankhede, Jesal Doshi. Solid Dispersions: an Approach to Enhance Solubility of poorly Water Soluble Drug.Journal of Scientific and Innovative Research 2 (3): 685-694, 2013.
RodrıÌguez-Spong B, Price CP, Jayasankar A, Matzger AJ, RodrıÌguez-Hornedo Nr. General principles of pharmaceutical solid polymorphism: A supramolecular perspective. Advanced Drug Delivery Reviews. 56(3):241-74, 2004.
Vishweshwar P, McMahon JA, Bis JA, Zaworotko MJ. Pharmaceutical co-crystals. Journal of Pharmaceutical Sciences 95(3):499-516, 2006.
Stahly GP. A Survey of Cocrystals Reported Prior to 2000. Crystal Growth & Design 9(10):4212-29, 2009.
Manes G, Balzano A. Tinidazole: from protozoa to Helicobacter pylori--the past, present and future of a nitroimidazole with peculiarities.Expert Rev Anti Infect Ther. 2004 Oct; 2(5):695-705
EP. European Pharmacopoeia. 5 ed 2004.Council of Europe, V2. pg 2585. 2727, 2004.
Paun Jalpa S., Chapla Vishal K., Raval Mihir K., Tank Hemraj M Improvement of Physicochemical properties of tinidazole cocrystals: An Influence Of Additives. Indo American Journal of Pharm Research,3(5). p3680-3688, 2013.
Puckhraj Chhaprel, Amit Talesara, Amit K Jain. Solubility enhancement of poorly water soluble drug using spray drying technique. International Journal of Pharmaceutical Studies and Research, 3(2):01-5, 2012.
P. Sabitha Reddy, S. Sujani and K. Ravindra Reddy. Microcrystals: For Improvement of Solubility and Dissolution of Tinidazole. Asian J. Pharm. Tech, Vol. 1: Issue 3, Pg 64-69, 2011.
Agarwal V. Dissolution and powder flow characterization of solid self-emulsified drug delivery system (SEDDS).International Journal of Pharmaceutics 366, 44–5 , 2009.
Paun J. CV, Raval M., Tank H M. Improvement Of Physicochemical Properties Of Tinidazole Cocrystals: An Influence Of Additives. Indo American Journal of Pharmaceutical Research, 3(5):3680, 2013.
Stamboliadis ET. The energy distribution theory of comminution specific surface energy, mill efficiency and distribution mode. Minerals Engineering, 20(2):140-5, 2007.
Wells JI. Pharmaceutical preformulation: the physicochemical properties of drug substances. 227 p, United Kingdom, 1988.
Maheshwari R, Chaturvedi S, Jain N. Novel spectrophotometric estimation of some poorly water soluble drugs using hydrotropic solubilizing agents, march 1, 2006. 195-8 p, 2006.
National Institutes of Health. ImageJ,Bethedsa, Maryland, USA, [revised 2014 November 26; cited 2016 Frebruary 26]. Available from: http://rsbweb. nih.gov/ij/;
Kwok DY, Neumann AW. Contact angle interpretation in terms of solid surface tension. Colloids and Surfaces A: Physicochemical and Engineering Aspects, 161(1):31-48, 2000.
Joshi SS, hilegaonkar SB. Verification of official Dissolution Media for Tinidazole. Journal of Pharmacy Research, 3(7), 2010.
Zakeri-Milani P, Barzegar-Jalali M, Azimi M, Valizadeh H. Biopharmaceutical classification of drugs using intrinsic dissolution rate (IDR) and rat intestinal permeability. European Journal of Pharmaceutics and Biopharmaceutics;73(1):102, 2009.
Hendriksen BA, Williams JD. Characterization of calcium fenoprofen 2. Dissolution from formulated tablets and compressed rotating discs. International Journal of Pharmaceutics, 69(2):175-80, 1991.
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