Development and characterization of chronotherapeutic tablets of sacubitril-valsartan supramolecular complex using hupu gum and lannea gum by compression coating

Rajeswari Aleti; Kolapalli Venkata Ramana Murthy

doi:10.7324/JAPS.2023.120714

Abstract

Sacubitril-valsartan supramolecular complex (SVSC), a first-in-class Angiotensin Receptor Neprilysin Inhibitor has been approved as a safe and effective treatment for Heart Failure with Reduced Ejection Fraction and reduces the risk of cardiovascular death and re-hospitalization in patients with striking rise in blood pressure during early morning hours. As cardiovascular events are well associated with circadian rhythms, chronotherapeutic drug delivery of SVSC at bedtime (around 10 p.m.) may be a potential approach. The aim and objective of the present investigation is to develop a chronotherapeutic drug delivery system of SVSC using natural gums by compression coating technique that is appropriate in achieving a predetermined lag time of 5-6 hours followed by maximum drug release within 1 hour to attain the required C_maxwhen the disease condition is at peak. Initially the core tablets were optimized which completely released the drug in 25 minutes. The optimized core tablets were subjected to compression coating with different ratios of hupu gum, lannea gum and channelling agent for the preparation of chronotherapeutic tablets. The optimized compression-coated tablets complied with the official and other requirements of tablets. Differential scanning calorimetry and Fourier-transformed infrared spectroscopy studies confirmed the drug and excipient compatibility. Among all formulations, Compression coated Tablets CCT3 met all the objectives of the present investigation and hence, was selected as an optimized compression-coated tablet suitable for chronotherapeutic drug delivery of SVSC in patients with heart failure.

Keyword: Sacubitril-valsartan supramolecular complex heart failure bedtime dosing chronotherapeutic drug delivery systems compression coating technique hupu gum and lannea gum

Citation:

Rajeswari A, Ramana Murthy KV. Development and characterization of chronotherapeutic tablets of sacubitril-valsartan supramolecular complex using hupu gum and lannea gum by compression coating. J Appl Pharm Sci, 2023. https://doi.org/10.7324/JAPS.2023.120714

Copyright: © The Author(s). This is an open-access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Reference

Aleti R, Murthy KVR. Development and validation of UV spectroscopic method for estimation of sacubitril and valsartan combination (LCZ696) in bulk and pharmaceutical tablet dosage forms. Res J Pharm Technol, 2022; 15(11):5232-8. https://doi.org/10.52711/0974-360X.2022.00881

Ayalasomayajula S, Langenickel T, Pal P, Boggarapu S, Sunkara G. Clinical pharmacokinetics of sacubitril/valsartan (LCZ696): a novel angiotensin receptor-neprilysin inhibitor. Clin Pharmacokinet, 2017; 56(12):1461-78. https://doi.org/10.1007/s40262-017-0543-3

Bharathi A, Naik D. Formulation and in vitro evaluation of chronotherapeutic press-coated tablets of valsartan with natural controlled released gums. Eur J Pharm Med Res, 2019; 6(4):480-7.

Chickpetty SM, Basawaraj R, Kulkarni RV. Natural polysaccharides-based compression coated tablets for colon targeted delivery of naproxen for the treatment of colitis. Pharm Lett, 2010; 2(6):114-23.

Dabhi C, Randale S, Belgamwar V, Gattani S, Tekade A. Predictable pulsatile release of tramadol hydrochloride for chronotherapeutics of arthritis. Drug Deliv, 2010; 17(5):273-81. https://doi.org/10.3109/10717541003706240

D'Elia E, Iacovoni A, Vaduganathan M, Lorini FL, Perlini S, Senni M. Neprilysin inhibition in heart failure mechanisms and substrates

beyond modulating natriuretic peptides. Eur J Heart Fail, 2017; 19(6): 710-7. https://doi.org/10.1002/ejhf.799

Dharmarajan K, Hsieh AF, Lin Z, Bueno H, Ross JS, Horwitz LI, Barreto-Filho JA, Kim N, Bernheim SM, Suter LG, Drye EE, Krumholz HM. Diagnoses and timing of 30-day readmissions after hospitalization for heart failure, acute myocardial infarction, or pneumonia. J Am Med Assoc, 2013; 309(4):355-63. https://doi.org/10.1001/jama.2012.216476

Feng L, Godtfredsen SE, Karpinski P, Sutton PA, Prashad M, Girgis MJ, Hu B, Liu Y, Blacklock TJ, Novartis AG. Pharmaceutical combinations of an angiotensin receptor antagonist and a nep inhibitor. Canada Patent CA2590511A1.2007-05-18.

Feng L, Karpinski PH, Sutton P, Liu Y, Hook DF, Hu B, Blacklock TJ, Fanwick PE, Prashad M, Godtfredsen S, Ziltener C. LCZ696: a dual-acting sodium supramolecular complex. Tetrahedron Lett, 2012; 53(3):275-6. https://doi.org/10.1016/j.tetlet.2011.11.029

Gami AS, Howard DE, Olson EJ, Somers VK. Day-night pattern of sudden death in obstructive sleep apnea. N Engl J Med, 2005; 352(12):1206-14. https://doi.org/10.1056/NEJMoa041832

Gunsel WC. Compression-coated and layer tablets, in pharmaceutical dosage forms: tablets. In: Lieberman HA, Lachman L (Eds.). Marcel Dekker, New York, NY, vol. 1, pp 187-224, 1980.

Hermida RC, Ayala DE, Mojón A, Fernandez JR. Bedtime dosing of antihypertensive medications reduces cardiovascular risk in CKD. J Am Soc Nephrol, 2011; 22(12):2313-21. https://doi.org/10.1681/ASN.2011040361

aIndian Pharmacopoeia, Govt of India, Ministry of Health and Family Welfare, IPC, Ghaziabad, India, 2018a; 2.5.5:309.

Indian Pharmacopoeia, Govt of India. Ministry of Health and Family Welfare, IPC, Ghaziabad, India, vol. 2.5.3, p 308, 2018b.

Indian Pharmacopoeia, Govt of India. Ministry of Health and Family Welfare, IPC, Ghaziabad, India, vol. 2, p 1118, 2018c.

Indian Pharmacopoeia, Govt of India. Ministry of Health and Family Welfare, IPC, Ghaziabad, India, vol. 2.5.1, p 299-302, 2018d.

International Council for Harmonization of Technical Requirements for Pharmaceuticals for Human Use guidelines on "Stability testing of active pharmaceutical ingredients and finished pharmaceutical products" Annex 10. WHO Technical Reports Series, No. 1010, 2018. Available via https://www.fda.gov/regulatory-information/search-fda-guidance-documents/q1ar2-stability-testing-new-drug-substances-and-products (Accessed 24 August 2019)

https://www.who.int/publications/m/item/stability-testing-of-active-pharmaceutical-ingredients-and-finished-pharmaceutical-products-stability-conditions-for-who-member-states-by-region- (Accessed 09 March 2021)

Kobalava Z, Kotovskaya Y, Averkov O, Pavlikova E, Moiseev V, Albrecht D, Chandra P, Ayalasomayajula S, Prescott MF, Pal P, Langenickel TH, Jordaan P, Rajman I. Pharmacodynamic and pharmacokinetic profiles of sacubitril/valsartan (LCZ696) in patients with heart failure and reduced ejection fraction. Cardiovasc Ther, 2016; 34(4):191-8. https://doi.org/10.1111/1755-5922.12183

Koizumi K, Watanabe Y, Monita K, Utosuchi N. New method of preparing high porosity rapidly saliva soluble compressed tablets using mannitol with camphor, a subliming material. Int J Pharm, 1997; 152: 127-31. https://doi.org/10.1016/S0378-5173(97)04924-7

Latha K, Srikanth VV, Sunil SA, Srinivasa NR, Uhumwangho MU, Shaik NB, Ramana Murthy KV. Applicability of gum karaya in the preparation and in vitro evaluation of losartan potassium as chronotherapeutic drug delivery system. J Sci Res, 2015; 7(1-2):65-74. https://doi.org/10.3329/jsr.v7i1-2.21182

Li R, Pan Y, Chen D, Xu X, Yan G, Fan T. Design, preparation and in vitro evaluation of core-shell fused deposition modelling 3D-printed verapamil hydrochloride pulsatile tablets. Pharmaceutics, 2022; 14(2):437. https://doi.org/10.3390/pharmaceutics14020437

Liu XJ, Zhang Y, Wang XZ. Study on co-crystallization of LCZ696 using in situ ATR-FTIR and imaging. Crystals, 2020; 10(10):922. https://doi.org/10.3390/cryst10100922

Lopes CM, Lobo JMS, Pinto JF, Costa P. Compressed mini-tablet as a biphasic drug delivery system. Int J Pharm, 2006; 323(1-2):93-100. https://doi.org/10.1016/j.ijpharm.2006.05.063

Muller JE, Stone H, Turi ZG, Rutherford JD, Czeisler CA, Parker C, Poole WK, Passamani E, Roberts R, Robertson T. Circadian variation in the frequency of onset of acute myocardial infarction. N Engl J Med, 1985; 313(21):1315-22. https://doi.org/10.1056/NEJM198511213132103

Novartis Entresto granted expanded indication in chronic heart failure by FDA. 2021. Available via https://www.novartis.com/news/media-releases/Novartis Entresto granted expanded indication in chronic heart failure by FDA. (Accessed 16 April 2021)

Odeku OA, Fell JT. In-vitro evaluation of khaya and albizia gums as compression coatings for drug targeting to the colon. J Pharm Pharmacol, 2005; 57(2):163-8. https://doi.org/10.1211/0022357055362

Ponikowski P, Voors AA, Anker SD, Bueno H, Cleland JGF, Coats AJS, Falk V, Gonzalez-Juanatey JR, Harjola VP, Jankowska EA, Jessup M, Linde C, Nihoyannopoulos P, Parissis JT, Pieske B, Riley JP, Rosano GMC, Ruilope LM, Ruschitzka F, Rutten FH, van der Meer P, ESC Scientific Document Group. 2016 ESC guidelines for the diagnosis and treatment of acute and chronic heart failure: the task force for the diagnosis and treatment of acute and chronic heart failure of the European society of cardiology (ESC) developed with the special contribution of the heart failure association (HFA) of the ESC. Eur Heart J, 2016; 37(27):2129-200. https://doi.org/10.1093/eurheartj/ehw128

Puri V, Sharma A, Kumar P, Singh I, Huanbutta K. Synthesis and characterization of Thiolated Gum Ghatti as a novel excipient: development of compression-coated mucoadhesive tablets of domperidone. ACS Omega, 2021; 6(24):15844-54. https://doi.org/10.1021/acsomega.1c01328

Ross AC, Macrae RJ, Walther M, Stevens HN. Chronopharmaceutical drug delivery from a pulsatile capsule device based on programmable erosion. JPP, 2000; 52(8):903-9. https://doi.org/10.1211/0022357001774787

Shim CY. Heart failure with preserved ejection fraction: the major unmet need in cardiology. Korean Circ J, 2020; 50(12):1051-61. https://doi.org/10.4070/kcj.2020.0338

Smolensky MH, Portaluppi F. Chronopharmacology and chronotherapy of cardiovascular medications: relevance to prevention and treatment of coronary heart disease. Am Heart J, 1999; 137(42):S14-24. https://doi.org/10.1016/S0002-8703(99)70392-3

Solomon SD, McMurray JV, Anand I, Ge J, Lam P, Maggioni AP, Martinez F, Packer M, Pfeffer MA, Pieske B, Redfield MM, Rouleau JL, van Veldhuisen DJ, Zannad F, Zile MR, Desai AS, Claggett B, Jhund PS, Boytsov SA, Comin-Colet J, Cleland J, Düngen D, Goncalvesova E, Katova T, Kerr Saraiva JF, Lelonek M, Merkely B, Senni M, Shah SJ, Zou J, Rizkala R, Gong J, Shi C, Lefkowitz MP, PARAGON-HF Investigators and Committees. Angiotensin-Neprilysin inhibition in heart failure with preserved ejection fraction. N Engl J Med, 2019; 381(17):1609-20. https://doi.org/10.1056/NEJMoa1908655

Songa AS, Meka VS, Nali SR, Kolapalli VR. An in vitro and in vivo investigation into the suitability of compression coated tablets of indomethacin for the treatment of rheumatoid arthritis which follow circadian rhythms. Drug Dev Ind Pharm, 2013; 39(3):447-56 https://doi.org/10.3109/03639045.2012.662509

Singh S, Shyale SS, Karade P. Formulation and evaluation of orally disintegrating tablets of lamotrigine. Int J Pharm Sci Nanotechnol, 2015; 8(2):2881-8. https://doi.org/10.37285/ijpsn.2015.8.2.11

Stevens H, MacDougal F. Controlled onset oral drug delivery: an opportunity for innovative life cycle management. American Pharmaceutical Review, 2014. Available via https://www.americanpharmaceuticalreview. com/Featured-Articles/163671-Controlled-Onset-Oral-Drug-Delivery-An- Opportunity-for-Innovative-Life-Cycle-Management/ (Accessed 19 June 2019)

Sunil SA, Srikanth MV, Rao NS, Murthy KV. Chronotherapeutic drug delivery from indomethacin compression coated tablets for early morning pain associated rheumatoid arthritis. Curr Drug Deliv, 2013; 10(1):109-21. https://doi.org/10.2174/1567201811310010017

USFDA Dissolution testing methods. Available via https://www. accessdata.fda.gov/scripts/cder/dissolution/dsp_getalldata.cfm (Accessed 24 October 2019)

Vemula SK, Bontha VK. Colon targeted guar gum compression coated tablets of flurbiprofen: formulation, development and pharmacokinetics. Biomed Res Int, 2013; 2013(6):287919; https://doi. org/10.1155/2013/287919 https://doi.org/10.1155/2013/287919

Virani SS, Alonso A, Benjamin EJ, Bittencourt MS, Callaway W, Carson AP, Chamberlain AM, Chang R, Cheng S, Delling FN, Djousse L, Elkind MSV, Ferguson JF, Fornage M, Khan S, Kissela BM, Knutson L, Kwan TW, Lackland T, Lewis TT, Lichtman JH, Longenecker CT, Loop MS, Lutsey PL, Martin SS, Matsushita K, Moran E, Mussolino ME, Perak AM, Rosamond D, Roth GA, ampson KA, Satou GM, Schroeder EB, Shah SH, Shay M, Spartano NL, Stokes A, Tirschwell L, VanWagner LB and Tsao CW. American Heart Association Council on Epidemiology and Prevention Statistics Committee and Stroke Statistics Subcommittee. Heart disease and stroke statistics-2020 update: a report from the American heart association. Circulation, 2020; 141(9):e139-596. https://doi.org/10.1161/CIR.0000000000000757

Volpe M, Gallo G. Sacubitril/valsartan for heart failure with preserved ejection fraction and resistant hypertension: one shot for a double strike? Eur Heart J, 2021; 42(36):3753-5. https://doi.org/10.1093/eurheartj/ehab489

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