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Vulnerability of Hydro-Alcoholic Media on In Vitro Drug Release from Galantamine HBr Pellets Comprising of Compritol 888 ATO and Ethocel
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Objective: The objective of the present study was to assess the interaction between the Galantamine HBr pellets and alcohol. Concomitant administration of alcohol and formulation can affect the plasma concentration of drug or give dose dumping effect or failure of the dosage form as the number of excipients especially polymers used in the modified dosage form cannot withstand in the presence of alcohol. Materials and Methods: The modified release pellets of galantamine hydrobromide were formulated incorporating a waxy polymer – Compritol 888 ATO and a hydrophobic polymer – Ethocel using extrusion spheronization technique. In vitro drug release of galntamine pellets was performed in distilled water and 10-40% ethanol containing distilled water. The saturated solubility of galantamine was measured in different dissolution media and pure ethanol. Results and Discussion: In vitro drug release study showed similarity at all the levels of alcohol (10-40%) as f2 value was found to be more than 50. In vitro drug release was slightly reduced in the presence of alcohol as the galantamine is slightly less soluble in ethanol compared to distilled water. There was change observed in drug release kinetics and mechanism but no significant change was observed in drug release. Conclusion: The suitability of Compritol 888 ATO and Ethocel as a matrix forming excipient in the formulation of pellets can resist the effect of alcohol makes it suitable for the alternative polymer in the wider application for designing of modified release dosage form.
Keywords
Hydroalcoholic Media, Compritol 888 ATO, Ethocel, Sustained Release Pellets, Galantamine HBr
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- Lazzari A, Kleinebudde P, Knop K. Xanthan gum as a rate-controlling polymer for the development of alcohol resistant matrix tablets and mini-tablets. Int J Pharm [Internet]. 2018;536(1):440–9. Available from: http://dx.doi.org/10.1016/j.ijpharm.2017.12.014
- Nep EI, Mahdi MH, Adebisi AO, Ngwuluka NC, Conway BR, Smith AM, et al. Hydro-alcoholic media effects on theophylline release from sesamum polysaccharide gum matrices. Drug Dev Ind Pharm [Internet]. 2018;44(2):251–60. Available from: https://doi.org/10.1080/03639045.2017.1386209
- World Health Organization. Global status report on alcohol and health 2018 [Internet]. 2018. Available from: http://www.who.int/substance_abuse/publications/global_alcohol_report/en/
- Robert J., Meyer M., Hussain A. FDA ’ s ACPS Meeting , Awareness Topic : Mitigating the Risks of Ethanol Induced Dose Dumping from Oral Sustained / Controlled Release Dosage Forms Ph . D . Office of New Drugs and Office of P. Center for Drug Evaluation and Research, FDA. 2005.
- USFDA. FDA’s alert for healthcare professionals. Hydromorphone hydrochloride extended-release capsules (marketed as PalladoneTM), Alcohol- PalladoneTM interaction. [Internet]. Available from: http://www.fda.gov/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProviders/ucm129288.htm
- Nep EI, Mahdi MH, Adebisi AO, Dawson C, Walton K, Bills PJ, et al. The influence of hydroalcoholic media on the performance of Grewia polysaccharide in sustained release tablets. Int J Pharm [Internet]. 2017;532(1):352–64. Available from: http://dx.doi.org/10.1016/j.ijpharm.2017.09.022
- Missaghi S, Fegely KA, Rajabi-Siahboomi AR. Investigation of the effects of hydroalcoholic solutions on textural and rheological properties of various controlled release grades of hypromellose. AAPS PharmSciTech [Internet]. 2009;10(1):77–80. Available from: http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=2663671&tool=pmcentrez&rendertype=abstract
- Levina M, Vuong H, Rajabi-Siahboomi AR. The influence of hydro-alcoholic media on hypromellose matrix systems. Drug Dev Ind Pharm. 2007;33(10):1125–34.
- Emeje M, Nwabunike P, Isimi C, Kunle O, Ofoefule S. Hydro-Alcoholic Media: An Emerging in vitro Tool for Predicting Dose Dumping from Controlled Release Matrices. J Pharmacol Toxicol. 2008;3(2):84–92.
- Larsson M, Hjärtstam J, Berndtsson J, Stading M, Larsson A. Effect of ethanol on the water permeability of controlled release films composed of ethyl cellulose and hydroxypropyl cellulose. Eur J Pharm Biopharm [Internet]. 2010;76(3):428–32. Available from: http://dx.doi.org/10.1016/j.ejpb.2010.09.007
- Muley S, Nandgude T, Poddar S. Extrusion – spheronization a promising pelletization technique : In-depth review. Asian J Pharm Sci [Internet]. 2016;11(6):684–99. Available from: http://dx.doi.org/10.1016/j.ajps.2016.08.001
- Roy P, Shahiwala A. Multiparticulate formulation approach to pulsatile drug delivery : Current perspectives. J Control Release [Internet]. 2009;134(2):74–80. Available from: http://dx.doi.org/10.1016/j.jconrel.2008.11.011
- Fakult M, Petrovick GF. Orodispersible Tablets Containing Taste- Masked Lipid Pellets with Metformin Hydrochloride for Use by Elderly Patients [Internet]. Heinrich-Heine-Universität Düsseldorf; 2015. Available from: https://docserv.uni-duesseldorf.de/servlets/DerivateServlet/Derivate-36734/Doctoral Thesis Petrovick.pdf
- Patere SN, Kapadia CJ, Nagarsenker MS. Influence of Formulation Factors and Compression Force on Release Profile of Sustained Release Metoprolol Tablets using Compritol(®) 888ATO as Lipid Excipient. Indian J Pharm Sci [Internet]. 2015;77(5):620–5. Available from: http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=4700717&tool=pmcentrez&rendertype=abstract
- Marchaud D, Cuppok Y, Arcuri K, Girard JM, Miolane C. Improving drug safety : Compritol ® 888 ATO matrix tablets deliver consistent sustained drug release in hydro-alcoholic media and when broken . :1–2.
- Crowley MM, Schroeder B, Fredersdorf A, Obara S, Talarico M, Kucera S, et al. Physicochemical properties and mechanism of drug release from ethyl cellulose matrix tablets prepared by direct compression and hot-melt extrusion. Int J Pharm. 2004;269(2):509–22.
- Singh G, Pai RS, Devi VK. Optimization of Pellets Containing Solid Dispersion Prepared by Extrusion / Spheronization Using Central Composite Design and Desirability Function. J Young Pharm [Internet]. 2012;4(3):146–56. Available from: http://dx.doi.org/10.4103/0975-1483.100020
- Wang J, Kan S, Chen T, Liu J. Application of quality by design (QbD) to formulation and processing of naproxen pellets by extrusion-spheronization. Pharm Dev Technol [Internet]. 2015;20(2):246–56. Available from: http://dx.doi.org/10.3109/10837450.2014.908300
- Rana HB, Gohel MC, Dholakia MS, Gandhi TR, Omri A, Thakkar VT. Development of Sustained Release Pellets of Galantamine HBr by Extrusion Spheronization Technique Incorporating Risk based QbD Approach. Res J Pharm Technol. 2018;11.
- Zhang L, Huang Z, Wan X, Li J, Liu J. Measurement and Correlation of the Solubility of Febuxostat in Four Organic Solvents at Various Temperatures. J Chem Eng Data. 2012;57:3149–52.
- Patel A V, Patel VJ, Patel A V, Dave JB, Patel CN. Determination of galantamine hydrobromide in bulk drug and pharmaceutical dosage form by spectrofluorimetry. J Pharm Bioallied Sci. 2013;5(4):314–7.
- Roberts M, Cespi M, Ford JL, Dyas AM, Downing J, Martini LG, et al. Influence of ethanol on aspirin release from hypromellose matrices. Int J Pharm [Internet]. 2007;332(1–2):31–7. Available from: http://linkinghub.elsevier.com/retrieve/pii/S0378517306007903
- Yan H, Zhang S, He J, Liu J. Application of ethyl cellulose, microcrystalline cellulose and octadecanol for wax based floating solid dispersion pellets. Carbohydr Polym [Internet]. 2016;148:143–52. Available from: http://dx.doi.org/10.1016/j.carbpol.2016.04.050
- Galantamine Extended-Release Capsules, USP Revision Bulletin Official. 2016.
- Dash S, Murthy PN, Nath L, Chowdhury P. Kinetic modeling on drug release from controlled drug delivery systems. Acta Pol Pharm [Internet]. 2010;67(3):217–23. Available from: http://www.ncbi.nlm.nih.gov/pubmed/20524422
- Yang S. Preparation and evaluation of novel galantamine hydrobromide sustained-release capsule. Bangladesh J Pharmacol. 2016;11:82–91.
- Gohel MC, Sarvaiya KG, Mehta NR, Soni CD, Vyas VU, Dave RK. Assessment of similarity factor using different weighting approaches. Dissolution Technol. 2005;12(4):22–7.
- Singhvi G, Singh M. Review : in-Vitro Drug Release Characterization Models. Int J Pharm Stud Res. 2011;II(I):77–84.
- Siepmann J, Peppas NA. Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose ( HPMC ). Adv Drug Deliv Rev [Internet]. 2012;64:163–74. Available from: http://dx.doi.org/10.1016/j.addr.2012.09.028
- Korsmayer RW, Gumy R, Doelker E, Buri P, Peppas NA. Mechanisms of solute release from porous hydrophilic polymers. interantional jouranl Pharm. 1983;15:25–35.
- Zhang Y, Huo M, Zhou J, Zou A, Li W, Yao C, et al. DDSolver: An Add-In Program for Modeling and Comparison of Drug Dissolution Profiles. AAPS J [Internet]. 2010;12(3):263–71. Available from: http://www.springerlink.com/index/10.1208/s12248-010-9185-1
- Jedinger N, Schrank S, Mohr S, Feichtinger A, Khinast J, Roblegg E. Alcohol dose dumping: The influence of ethanol on hot-melt extruded pellets comprising solid lipids. Eur J Pharm Biopharm [Internet]. 2015;92:83–95. Available from: http://www.scopus.com/inward/record.url?eid=2-s2.0-84924764680&partnerID=tZOtx3y1
- Fadda HM, Mohamed MAM, Basit AW. Impairment of the in vitro drug release behaviour of oral modified release preparations in the presence of alcohol. Int J Pharm [Internet]. 2008;360(1–2):171–6. Available from: http://linkinghub.elsevier.com/retrieve/pii/S0378517308003426
- Levina M, Rajabi-siahboomi AR. The influence of concomitant use of alcoholic beverages on hypromellose matrix tablets. Pharm Technol [Internet]. 2008;20(12):1–4. Available from: http://www.pharmtech.com/influence-concomitant-use-alcoholic-beverages-hypromellose-matrix-tablets
- Palmer D, Levina M, Farrell TP, Rajabi-siahboomi A. The Influence of Hydro-Alcoholic Media on Drug Release from Polyethylene Oxide Extended Release Matrix Tablets. Pharm Technol. 2011;35(7):1–8.
- Dhameliya P. Preparation and evaluation of sustained release tablet of eperisone hydrochloride by Compritol ATO 888 as a matrix forming agent. J Drug Deliv Ther. 2014;4(3):132–7.
- Angadi SC, Manjeshwar LS, Aminabhavi TM. Stearic acid-coated chitosan-based interpenetrating polymer network microspheres: Controlled release characteristics. Ind Eng Chem Res. 2011;50(8):4504–14.
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