FORMULATION AND EVALUATION OF AN ORAL TIMED PULSATILE DRUG DELIVERY FOR ALLEVIATING PAIN IN RHEUMATOID ARTHRITIS

PASAM JYOTHIRMAYI; ARIGELA BHARATHI; D. RAMA SEKHARA REDDY

doi:10.22159/ijap.2025v17i1.51458

Authors

PASAM JYOTHIRMAYI Krishna University, Krishna District, Andhra Pradesh, India https://orcid.org/0000-0002-4872-330X
ARIGELA BHARATHI K.V. S. R Siddhartha College of Pharmaceutical Sciences, Vijayawada, Andhra Pradesh, India
D. RAMA SEKHARA REDDY Department of Chemistry, Krishna University, Krishna District, Andhra Pradesh, India

DOI:

https://doi.org/10.22159/ijap.2025v17i1.51458

Keywords:

Pulsatile drug delivery system, Chronotherapeutic, Aceclofenac, Rheumatoid arthritis

Abstract

Objective: The present study was aimed to formulate and evaluate an oral timed release pulsatile drug delivery of AcecloFenac (AF) for rheumatoid arthritis pain by the Chronopharmaceutical approach with early morning breakthrough of AF as analgesic and anti-inflammatory agent for the treatment of rheumatoid arthritis.

Methods: AFsolubility was enhanced by formulating it as a self-emulsified system with a suitable oil and surfactant mixture. The interaction between the drug and the excipient was examined using Fourier Transform Infra Red (FTIR) spectroscopy. The prepared formulation consists of 2 different parts: The basic design consists of burst release core tablets with solid self-emulsified AFby using different super disintegrants, and the press-coating of optimised tablets by using different compositions of Ethylcellulose (hydrophobic) and Hydroxy Propyl Methyl Cellulose (HPMC K100) (hydrophilic) polymers.

Results: FTIR studies revealed no interaction between drug and excipients. From the solubility data, suitable oil and surfactants were selected. Pseudo-ternary plots help in finding of suitable surfactant mixtures for solid self-emulsifiedAF. Core tablets were evaluated for precompression characteristics, disintegration time, drug content, weight variation, hardness, friability, thickness, and % drug release. Among all solid self emulsified formulations, S1C6 is successful with 98.88% drug release in 20 min. The compression coat formulations were also evaluated for Hardness, weight variation, thickness, lag time, and in-vitro drug release profile. Among them, F4 was optimised by its suitable lag time and drug release of 97.23% at the end of 6 h.

Conclusion: The system released the drug after a predetermined lag time of 4 h and thus the dosage form can be taken at bedtime so that the drug will be released when the symptoms are prominent. Nine formulations were prepared, of which F4 formulation showed the highest drug release of 97.23 % at the end of 6 h and showed compliance with the chronotherapeutic objective of rheumatoid arthritis

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References

Jain D, Raturi R, Jain V, Bansal P, Singh R. Recent technologies in pulsatile drug delivery systems. Biomatter 2011; 1:57-65. doi: 10.4161/biom.1.1.17717

Deepika Jain, Richa Raturi, Vikas Jain, Praveen Bansal, and Ranjit Singh , recent technologies in pulsatile drug deliverey systems, Biomatter, 2011; 1(1): 57-65. Doi: 10.4161/biom.1.1.17717

Venkataswamy r, Lavanya nallaguntla, review article on pulsatile drug delivery system, Asian J Pharm Clin Res, 2021; 14(6): 48-59. doi: 10.22159/ajpcr.2021.v14i6.41476.

4. Patel HM, Patel UB, Shah C, Bhavesh Akbari. Formulation and development of nanosuspension as an alternative approach for solubility and dissolution enhancement of aceclofenac. International Journal of Advances in Pharmaceutics. 2018;07(05):33-47. doi: https://doi.org/10.7439/ijapR

Santosh Kumar, Sahithi Mulidi. Optimization of statistically designed aceclofenac fast dissolving tablets employing starch glutamate as a novel superdisintegrant. Int J Appl Pharm 2020;12:77-88. doi: http://dx.doi.org/10.22159/ijap.2020v12i1.34987.

Kharwade R, Nair H, Masurkar D, Pise A, More S, Pise S. Formulation and evaluation of chronomodulated pulsatile drug delivery system for nocturnal hyperacidity. Res J Pharm Technol. 2022; 15(4): 1449-54. doi: 10.52711/0974-360X.2022.00240

Parekh, K., Thakkar, V., Joshi, A. et al. Optimizing pulsatile release of febuxostat for managing gout flares: a chronotherapeutic approach. Futur J Pharm Sci 9, 89 (2023). https://doi.org/10.1186/s43094-023-00542-9

Tekade, A. R., & Gattani, S. G. (2009). Development and evaluation of pulsatile drug delivery system using novel polymer. Pharmaceutical Development and Technology, 14(4), 380–387. https://doi.org/10.1080/10837450802712625 .

Mangesh A. Bhutkar , Somnath D. Bhinge. Formulation and Evaluation of Valsartan Pulsincap Drug Delivery System for Treatment of Hypertension. Asian J. Pharm. Tech. 2018; 8 (2):65-70 . doi: 10.5958/2231-5713.2018.00010.7

Maroni A, Zema L, Loreti G, Palugan L, Gazzaniga A. Film coatings for oral pulsatile release. Int J Pharm 2013; 457:362-71. doi: 10.1016/j.ijpharm.2013.03.010

PashamS,Venkatesh DP,SujitN.Pulsatiledrugdeliverysystem:aformulationapproach for the treatment of diseases. Int J Curr Pharm Res 2020; 14:16-21. doi: http://dx.doi.org/10.22159/ijcpr.2020v12i3.38328.

Chaudhari S, Chaudhari P, Narawane S. Development and Optimization of chronopharmaceutical drug delivery system for asthma. JDDT, 2016;6(1):25-3. doi: https://doi.org/10.22270/jddt.v6i1.1178

Rashid, R., Zaman, M., Ahmad, M., Khan, M.A., Butt, M.H., SalawiSalawi, A., Almoshari, Y., Alshamrani, M., & Sarfraz, R.M., Press-Coated Aceclofenac Tablets for Pulsatile Drug Delivery: Formulation and In Vitro Evaluations. Pharmaceuticals, 2022;15(1):303-326. oi:10.3390/ph15030326

Rompicharla B, Prabha KS, TabasumMd, “A Comprehensive Review of Pulsatile Drug Delivery System”. Int Res J Pharm 2012; 3:106-8. doi:10.22159/ijcpr.2021v13i2.41543

Kamisetti, Formulation and evaluation of pulsatile drug delivery system of lovastatin, International Journal of Biology Pharmacy and Allied Sciences, 2024; 13(5): 2287-2299 doi:10.31032/IJBPAS/2024/13.5.8015

Reddy Dumpa, Nagi, Suresh Bandari, and Michael A. Repka. 2020. "Novel Gastroretentive Floating Pulsatile Drug Delivery System Produced via Hot-Melt Extrusion and Fused Deposition Modeling 3D Printing" Pharmaceutics 12, no. 1: 52. https://doi.org/10.3390/pharmaceutics12010052

HoareT, TimkoBP, SantamariaJ,GoyaGF, IrustaS, LauS,etal. Magnetically triggered nanocomposite membranes: a versatile platform for triggered drug release. Nano Lett 2011; 11(1):1395-400. doi: 10.1021/nl200494t

N Vishal, Gupta H G. Shivakumar. Preparation and characterization of superporous hydrogels as gastroretentive drug delivery system for rosiglitazone maleate. Daru journal of pharmaceutical sciences. 2010; 18(3): 200–210.

Wang A Y, Peura. "The prevalence and incidence of Helicobacter pylori associated peptic ulcer disease and upper gastrointestinal bleeding throughout the world". Gastrointestinal endoscopy clinics of North America October 2011;21(4):613–35. doi: 10.14740/jocmr4348

BonthagaralaB, VadrevuS, NamaS, SudarshanD, NuthakkiS. Formulation and evaluation of pulsatile drug delivery system of atenolol. American journal of biological and pharmaceutical research. 2014;1(1):28-33. doi: 10.13040/IJPSR.0975-8232.11(7).3229-42

Garg AK, Kumar A, Rani S, Singh M, Sharma A, Kumar R. Formulation and Evaluation of Chronotherapeutic Pulsatile Drug Delivery System Containing Rabeprazole Sodium. Journal of Applied Pharmaceutical Science. 2017;7(02):093-100. doi: 10.7324/JAPS.2017.70211

AgamTushar, Yadav Gangotri, Jain Ashish, Ware Pallavi and Kamble Srushti, Formulation and Evaluation of Pulsatile Drug Delivery System of Dexlansoprazole Running title- Dexlansopra-zole Pulsincap System, International Journal of Pharmaceutical Sciences and Nanotechnology. 2023, 16(5):6976-6988. doi: https://doi.org/10.37285/ijpsn.2023.16.5.6

Jagdale SC, Suryawanshi VM, Pandya SV, Kuchekar BS, Chabukswar AR. Development of press- coated, floating-pulsatile drug delivery of lisinopril. Scientia pharmaceutica. 2014;82(2):423-440. doi: 10.3797/scipharm.1301-27

GargBK, GnanarajanG, KothiyalP. Formulation and evaluation of pulsatile drug delivery system of rosuvastatin calcium using different swelling polymers. The pharma innovation. 2012;1(7):61-67. doi: https://www.thepharmajournal.com/archives/2012/vol1issue7/PartA/7.7.pdf

AmitADhengale, AvinashBDarekar, RavindraBSaudagar. Development and Evaluation of Pulsatile Drug Delivery System Containing Etodolac. International journal of pharmacy and pharmaceutical research. 2016; 8 (1): 312-325. doi: https://ijppr.humanjournals.com/wp-content/uploads/2017/01/28.Amit-A.-Dhengale-Avinash-B.-Darekar-Ravindra-B.-Saudagar.pdf

Lakshmi Prasanna, JayachandraReddy, Umasankar,JyosthanaDevi, Rajitha. Formulation and evaluation of pulsatile drug delivery system of zafirlukast. International journal of pharmacy.2017;7(3):147-154. doi:10.37118/ijdr.26634.04.202

Muhammed, R. A., Mohammed, S., Visht, S., & Yassen, A. O. A Review On Development Of Colon Targeted Drug Delivery System. International Journal of Applied Pharmaceutics, 2024; 16(2); 12–27. doi: 10.22159/ijap.2024v16i2.49293

DN, C. P., and S. A. “A solubility enhancement of aceclofenac by new crystallization technique”. Asian Journal of Pharmaceutical and Clinical Research, Feb. 2022; 15(2): 113-8, doi:10.22159/ajpcr.2022.v15i2.43134.

Zhang, L., Zhang, lanying, zhang, M., Y., Li, Z., Zhao, A., & Feng, J. (2013). Self-emulsifying drug delivery system and the applications in herbal drugs. Drug Delivery , 2013;22( 4): 475 -486. doi:10.3109/10717544.2013.861659

Bijapuri Srivastava, Palla Sneha, Ragineedi Gnana Kumar, Dharani Sobha N, & Shanigaram Aashritha. Development of Aceclofenac Solid Self-Emulsifying Drug Delivery Systems. International Journal of Clinical Pharmacokinetics and Medical Sciences, 2022; 2(2): 47–53. doi: 10.26452/ijcpms.v2i2.269

Rashid R, Zaman M, Ahmad M, Khan MA, Butt MH, Salawi A, Almoshari Y, Alshamrani M, Sarfraz RM. Press-Coated Aceclofenac Tablets for Pulsatile Drug Delivery: Formulation and In Vitro Evaluations. Pharmaceuticals (Basel). 2022;15(3):326-335. doi: 10.3390/ph15030326. doi: 10.3390/ph15030326