Formulation and Evaluation of Hot-melt moulded extended- release tablet of Venlafaxine HCl.
Keywords:
Venlafaxine HCl, Channeling agent, HLB modifier..Abstract
Objective: To prepare and optimize hot melt moulded extended-release of Venlafaxine HCl tablet capable of drug release for 12 hrs using suitable experimental design.
Method: Initially preliminary trial batch was carried out for the selection of hydrophobic base, effect of HLB modifier and channeling agent and also for the selection of their relative quantity for preparation of Venlafaxine HCl extended-release tablet. Stearic acid selected as base, PEG 6000 as HLB modifier, NaCl as channeling agent used with their suitable quantity. For the preparation of Venlafaxine HCl extended-release tablet by hot melt moulding method.
Result and discussion: Identification and compatibility study of drug and excipients were carried out using melting point FTIR and DSC study. Identification proved the drug authentication and compatibility studied proved that Venlafaxine HCl was compatible with selected excipients. Venlafaxine HCl showed λmax 225nm in 0.1N HCl. Hydrophobic base (stearic acid), PEG 6000, NaCl found to be providing the desired result. Result of drug release depend on the concentration of PEG and NaCl % drug release at 15min (Y1) and % drug release at 540 min (Y2) response. Drug release 19.297% at 15 min and drug release 87.526 % at 540 min which was desired for extended-release tablet of venlafaxine HCl.
Downloads
References
[1] Lemke TL., Williams DA., and Roche VF., in FOYE’S Principles of Medicinal Chemistry; 7th Edn; Lippincott Williams & WiIkins, a Wolters Kluwer business, Baltimore, 2012, pp 608.
[2] The National Institute of Mental Health, “Mental health Information”, July 2018, NIMH » anxiety disorders (nih.gov).
[3] Horst WD and Preskorn SH,” Mechanism of action and clinical characteristics of three atypical antidepressant: venlafaxine, nefazodone, bupropion”, J. of affective disorder,1998.
[4] Shargel L., Yu AC., Applied Biopharmaceutics & Pharmacokinetics; 7th Edn 575-577.
[5] “Pharma compass Grow your Pharma Knowledge digitally” venlafaxine HCl https://www.pharmacompass.com/active-pharmaceutical ingredients/venlafaxine- hydrochloride.
[6] Raymond c., poul j Sheskey and Marian E. “handbook of pharmaceutical excipients.” 6th Edn. Pharmaceutical press, 2009
[7] Olver JS and Burrows GD, “The treatment of depression with different formulations of venlafaxine: a comparative analysis” Human psychopharmacology.: Clinical and Experimental;2003.
[8] Saleh AM, and Syed AA, “Utility of novel dual functionalized co-crystallized and ionic based liquid-based drugs for the pain management” International J. pharma. research and bio-science 2016.
[9] Gabe DM, Abdallah OY, “Mini-tablets versus pellets as promising multiparticulate modified release delivery systems for highly soluble drugs” International J. Pharm. 2015.
[10] Yadav K and Srivastava AK, “Evaluation of hydrophilic, hydrophobic and waxy matrix excipients for sustained release tablets of Venlafaxine hydrochloride” Drug Development and Industrial Pharmacy; 2013. 11) Theodoros A and Nikolaos K, “Mechanical properties and drug release of Venlafaxine HCl solid mini matrices prepared by hot-melt extrusion and hot or ambient compression” Drug Development and Industrial Pharmacy;2017.
[11] Jain S and Datta M, “Montmorillonite-alginate microspheres as a delivery vehicle for oral extended release of Venlafaxine hydrochloride” Journal of Drug Delivery Science and Technology,2016.
[12] Dixit M, Cheng X, Nagnia A, and Chen M. Extended-release venlafaxine formulation. United State Patent US 7470435B2, 2005.
[13] Sherman DM, Cark JC, Lamer JU and Steven AW. Extended-release formulation of venlafaxine hydrochloride. United State Patent US 621774171B1, 2001.
[14] Pandita, Bhattacharya S, Kshirsagar S, Joshi R and Joshi M. Venlafaxine HCl in composition of micro tablet. World Intellectual Property Organization WO 2005/074895Al, 2005.
[15] Qingwei J, Quanzhi L, Wenbin Y, Junli Z. Venlafaxine hydrochloride sustained-release pellet capsules. Chinese Patent CN 101987091B, 2015.
[16] Michael R, Angela P, Sims, Edward. Extended-release tablet formulations of venlafaxine. European Patent EP 1 677 776 B1, 2008.
[17] Butreddy A, Sarabu S, Dumpa N, Bandari S and Repka MA, “Extended release pellets prepared by hot melt extrusion technique for abuse deterrent potential: Category-1 in-vitro evaluation”, International Journal of Pharmaceutics, 2020;587:119624. doi:10.1016/j.ijpharm.2020.119624.
[18] Nashed N, Lam M and Nokhodchi A, “A comprehensive overview of extended release oral dosage forms manufactured through hot melt extrusion and its combination with 3D printing”, International Journal of Pharmaceutics, 2021;596:120237. doi:10.1016/j.ijpharm.2021.120237.
[19] Tort S, Kodan Akça E, Olğaç S, Saar S, Yıldız A, Ünal İS, et al., “Development and evaluation of sustained release tablet formulations of venlafaxine hydrochloride”, Sağlık Bilimlerinde Değer (Online), 2022;12(1):28-35. doi:10.33631/sabd.1055227.
[20] Devhadrao A, Devhadrao N, Sable V, Tare M, et al., “Formulation and evaluation of venlafaxine hydrochloride osmotic tablets”, International Journal of Pharmaceutical Quality Assurance, 2023;14(1):81-86. doi:10.25258/ijpqa.14.1.14.
[21] Khute S and Jangde RK, “Optimization of nasal liposome formulation of venlafaxine hydrochloride using a Box-Behnken experimental design”, Current Therapeutic Research, 2023;99:100714. doi:10.1016/j.curtheres.2023.100714.
[22] Maniruzzaman M, Boateng JS, Snowden MJ and Douroumis D, “A review of hot-melt extrusion: Process technology to pharmaceutical products”, ISRN Pharmaceutics, 2012;2012:436763. doi:10.5402/2012/436763.
[23] Patil H, Tiwari RV and Repka MA, “Hot-melt extrusion: From theory to application in pharmaceutical formulation”, AAPS PharmSciTech, 2016;17(1):20-42. doi:10.1208/s12249-015-0360-7.
[24] Repka MA, Shah S, Lu J, Maddineni S, Morott J, Patwardhan K and Mohammed NN, “Melt extrusion: Process to product”, Expert Opinion on Drug Delivery, 2012;9(1):105- 125. doi:10.1517/17425247.2012.638218.
[25] Crowley MM, Zhang F, Repka MA, Thumma S, Upadhye SB, Battu SK, et al., “Pharmaceutical applications of hot-melt extrusion: Part I”, Drug Development and Industrial Pharmacy, 2007;33(9):909-926. doi:10.1080/03639040701498791.
[26] Bruce C, Chowdary KPR and Suryadevara V, “Formulation and evaluation of sustained release matrix tablets using hot melt granulation technique”, International Journal of Pharmaceutical Sciences and Research, 2021;12:xxxx-xxxx.
[27] “Development and characterization of sustained-release solid dispersions using hot-melt extrusion technology”, Pharmaceutics, 2021;13:xxxx-xxxx.
[28] Bounartzi M, Panagopoulou A, Kantiranis N, Malamataris S and Nikolakakis I, “Effect of plasticiser type on the hot melt extrusion of venlafaxine hydrochloride”, Journal of Pharmacy and Pharmacology, 2014;66(2):297-308. doi:10.1111/jphp.12117.
[29] Yadav K and Srivastava AK, “Evaluation of hydrophilic, hydrophobic and waxy matrix excipients for sustained release tablets of venlafaxine hydrochloride”, Drug Development and Industrial Pharmacy, 2013;39(7):1062-1070.
[30] Theodoros A and Nikolaos K, “Mechanical properties and drug release of venlafaxine HCl solid mini matrices prepared by hot-melt extrusion and hot or ambient compression”, Drug Development and Industrial Pharmacy, 2017.
[31] Li Y, Liu L, Wang X, et al., “Preparation and in vitro/in vivo evaluation of sustained-release venlafaxine hydrochloride pellets”, International Journal of Pharmaceutics, 2012;426(1- 2):107-115
Downloads
Published
How to Cite
Issue
Section
License
This work is licensed under a Creative Commons Attribution 4.0 International License.
You are free to:
- Share — copy and redistribute the material in any medium or format
- Adapt — remix, transform, and build upon the material for any purpose, even commercially.
Terms:
- Attribution — You must give appropriate credit, provide a link to the license, and indicate if changes were made. You may do so in any reasonable manner, but not in any way that suggests the licensor endorses you or your use.
- No additional restrictions — You may not apply legal terms or technological measures that legally restrict others from doing anything the license permits.
