Author(s): K.V.R.N.S. Ramesh, Nameh Yousef Ower, Omar Sarheed, Quamrul Islam

Email(s): venkatramesh@rakmhsu.ac.ae

DOI: 10.52711/0974-360X.2022.00933   

Address: K.V.R.N.S. Ramesh*, Nameh Yousef Ower, Omar Sarheed, Quamrul Islam
Department of Pharmaceutics, RAK College of Pharmacy, RAK Medical and Health Sciences University, Ras Al Khaimah, United Arab Emirates.
*Corresponding Author

Published In:   Volume - 15,      Issue - 12,     Year - 2022


ABSTRACT:
Dissolution of drugs is a prerequisite in the development of their oral dosage forms with satisfactory bioavailability. In this investigation, solid dispersion of the model drug indomethacin in gelucire (50/13) and inclusion complexation in sulfobutyl ether beta cyclodextrin are employed to enhance the dissolution. Fast dissolving products (F1-F8) of indomethacin are prepared by different methods such as solvent evaporation, freeze drying and kneading and comparatively evaluated. The ternary and binary systems of the products are prepared and evaluated for their efficiency in increasing the dissolution. The dissolution efficiency values (DE30) were found to be higher for solid dispersions (73.34%) and inclusion complexes (53.12%) than the pure drug indomethacin (3.32%). The x ray diffraction and differential scanning calorimetry studies revealed that the crystalline drug is converted into an amorphous form in the dispersions and inclusion complexes. Soluplus and gelucire are employed as ternary components in the solid dispersions and inclusion complexes respectively and are found to be resulting in ternary systems which were found to be superior to the binary systems. A 22 full factorial experimental design in order to investigate the combined influence of method of preparation and nature of the product. It was observed that the method of preparation and nature of the product (a ternary system or a binary system) will influence the extent of improvement of dissolution of the drug.


Cite this article:
K.V.R.N.S. Ramesh, Nameh Yousef Ower, Omar Sarheed, Quamrul Islam. Dissolution Enhancement of Indomethacin through Binary and Ternary Solid dispersions and Inclusion Complexes – A Comparative Evaluation. Research Journal of Pharmacy and Technology 2022; 15(12):5529-6. doi: 10.52711/0974-360X.2022.00933

Cite(Electronic):
K.V.R.N.S. Ramesh, Nameh Yousef Ower, Omar Sarheed, Quamrul Islam. Dissolution Enhancement of Indomethacin through Binary and Ternary Solid dispersions and Inclusion Complexes – A Comparative Evaluation. Research Journal of Pharmacy and Technology 2022; 15(12):5529-6. doi: 10.52711/0974-360X.2022.00933   Available on: https://rjptonline.org/AbstractView.aspx?PID=2022-15-12-27


REFERENCES:
1.    Williams HD, Trevaskis NL, Charman SA, Shanker RM, Charman WN, Pouton CW et al. Strategies to address low drug solubility in discovery and development. Pharmacol Rev. 2013; 65(1): 315-499. https://doi.org/10.1124/pr.112.005660
2.    Miller JM, Beig A, Carr RA, Spence JK, Dahan A. A win – win solution in oral delivery of lipophilic drugs: supersaturation via amorphous solid dispersions increases apparent solubility without sacrifice of intestinal membrane permeability. Mol Pharm. 2012; 9(7): 2009-2016. https://doi.org/10.1021/mp300104s
3.    Amidon GL, Lennemas 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: 413-420. https://doi.org/10.1208/s12248-014-9620-9
4.    Singh A, Mooter VG. Spray drying formulation of amorphous solid dispersions. Adv Drug Deliv Rev. 2016; 100: 27-50. https://doi.org/10.1016/j.addr.2015.12.010
5.    Elaine KS. AHFS Drug Information:  American Society of Health System Pharmacists, Maryland, Bethesda. 2020; 2204-2214. https://doi.org/10.1007/978-1-349-80162-6
6.    Thorat VP, MahaparalePR, Gonjari ID.  Fast Dissolving Drug Delivery System of Cilnidipine using Gelucire. 50/13. Res J. Pharm Technol. 2019; 12 (5); 2185. https://doi.org/10.5958/0974-360x.2019.00364.0
7.    Harikrishnan V, Sreejith M, Elthose MJ, Akash M. Gelucire: an optional innovative tool for both sustained and fast release of drugs in treating diabetes mellitus type ii disease. Asian J. Res. Pharm. Sci. 2017; 7(1): 33-37. https://doi.org/10.5958/2231-5659.2017.00006.6
8.    Suchetana D, Kulkarni PK, Shailesh T. Dissolution behavior of olmesartan medoxomil drug in polymeric micelles of soluplus and pluronic f127. Res J Pharm Technol. 2021; 14(4): 2200-4. https://doi.org/10.52711/0974-360x.2021.00390
9.    Mai K, Bashar AT, Motasem A, Aref Z. Enhancement of the dissolution and bioavailability from freeze-dried powder of a hypocholesterolemic drug in the presence of soluplus. Powder Technol. 2018; 329: 25–32. https://doi.org/10.1016/j.powtec.2018.01.068
10.    Lust A, Strachan CJ, Veski P, Aaltonen J, Heinamaki J, Yliruusi, J. et al. Amorphous solid dispersions of piroxicam and soluplus((R)): qualitative and quantitative analysis of piroxicam recrystallization during storage. Int. J. Pharm. 2015; 486 (1-2): 306–314. https://doi.org/10.1016/j.ijpharm.2015.03.079
11.    Deepak S, Subhashree M, Anjum A, Sanjeeb KS, Rabinarayan R. An Assessment of Olmesartan Medoxomil Tablet by Inclusion Complex Technique. Res J Pharma Dosage Forms and Tech. 2021; 13 (3):193-197. https://doi.org/10.52711/0975-4377.2021.00034
12.    Farhatjahan IS, Meenakshi BP , Naazneen IS , Vandana BP. Preparation and Characterization of Lercanidipine Hydrochloride Inclusion complex with β-cyclodextrin and effect of Complexation on Solubility and Dissolution.2017 ; 10 (4): 1041. https://doi.org/10.5958/0974-360x.2017.00189.5
13.    Jain AS, Date AA, Nagarsenker MS, Pissurlunkar RR, Coutinho EC. Sulfobutyl ether β-cyclodextrin (SBE7 β-CD) carbamazepine complex: preparation, characterization, molecular modeling, and evaluation of in vivo anti-epileptic activity. AAPS Pharm Sci Tech. 2011; 12:1163-75. https://doi.org/10.1208/s12249-011-9685-z
14.    Lockwood SF, O’Malley S, Mosher GL. Improved aqueous solubility of crystalline astaxanthin (3, 3’-dihydroxy-β, β-carotene-4, 4’-dione) by captisol (sulfobutyl ether β-cyclodextrin). J Pharm Sci. 2003; 92:922-6. https://doi.org/10.1002/jps.10359
15.    Rajewski RA, Traiger G, Bresnahan J, Jaberaboansar P, Stella VJ, Thompson DO. Preliminary safety evaluation of parenterally administered sulfoalkyl ether β-cyclodextrin derivatives. J Pharm Sci. 1995; 84: 927-32. https://doi.org/10.1002/jps.2600840805
16.    Higuchi T, Connors KA. “Phase-solubility techniques,” In: Reilly CN, Ed., Advances in analytical chemistry and instrumentation, Wiley-Interscience, New York; 1965. p. 117-211.
17.    Loftsson T, Marcus EB. Cyclodextrins as functional excipients: methods to enhance complexation efficiency. J Pharm Sci. 2012; 101:3019-32. https://doi.org/10.1002/jps.23077
18.    Mohammad A. Investigations of polyethylene glycol mediated ternary molecular inclusion complexes of silymarin with beta cyclodextrins. J Appl Pharm Sci. 2015; 5:26-31. https://doi.org/10.7324/japs.2015.50905
19.    Loftsson T, Fridriksdottir H, Sigurdardottir AM, Ueda H. The effect of water-soluble polymers on drug cyclodextrin complexation. Int J Pharm. 1994; 110:169-77. https://doi.org/10.1016/0378-5173(94)90155-4
20.    Ngiik T, Amal AE. Effects of liquisolid formulations on dissolution of naproxen. Eur J Pharm Biopharm. 2009; 73 (3):  373–384. https://doi.org/10.1016/j.ejpb.2009.08.002
21.    Craig DQM The mechanisms of drug release from solid dispersions in water-soluble polymers. Int J Pharm. 2002; 231 (2): 131–144. https://doi.org/10.1016/s0378-5173(01)00891-2
22.    Shailesh B, Aparna P, Gudithi S, Varsha  P, A comparative study of approaches used to improve solubility of roxithromycin. Powder Technol. 2006;169 (2): 22–32.  https://doi.org/10.1016/j.powtec.2006.07.016
23.    Bankar PV, Mahatma OP. Improved dissolution rate of leflunomide using hydroxypropyl-β-cyclodextrin inclusion complexation by freeze-drying method. Int J Drug Deliv. 2012; 4(4):498-506.
24.    Sultan A, Syed SI, Mohammad AA, Afzal H, Faiyaz S, Abdulhakeem A. Stimulatory effects of soluplus on flufenamic acid β-cyclodextrin supramolecular complex: physicochemical characterization and pre-clinical anti-inflammatory assessment.  AAPS PharmSciTech. 2020; 21 (5) :145. https://doi.org/10.1208/s12249-020-01684-2
25.    Khan KA The concept of dissolution efficiency. J Pharm Pharmacol. 1975; 27(1):48-9. https://doi.org/10.1111/j.2042-7158.1975.tb09378.x
26.    Mathew OB, James M, Edward C.  In Florey K, Ed., Analytical profiles of drug substances. Academic Press New York 1984; 13: 211-238. https://doi.org/10.1016/s0099-5428(08)60192-6
27.    Wang X, Dearmas H, Blaton N, Michoel A, Vandenmooter, G Phase characterization of indomethacin in binary solid dispersions with PVP VA64 or Myrj 52. Int J Pharm. 2007; 345 (1-2): 95-100. https://doi.org/10.1016/j.ijpharm.2007.05.046




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