Sustained-release Theophylline Matrix Tablet Using Hydrophilic Polymers: Effects of Agitation Rates and pH on Release Kinetics

Main Article Content

E. I. Akpabio
D. E. Effiong
T. O. Uwah
N. I. Sunday
G. Jacob
U. Isong

Abstract

Background and Objective: Modified-release tablet of theophylline that can increase its usefulness despite narrow therapeutic index and short half-life, is being formulated. However, the rate and extent of release of a sustained-release delivery system can be affected by some factors. This work is aimed at investigating the effect of agitation rates and pH of dissolution medium on release kinetics of sustained-release theophylline tablet formulated using hydrophilic polymers.

Materials and Methods: Theophylline granules was formulated using 3 polymers (HPMC, SCMC and Sodium alginate) to form 3 batches of granule by wet granulation method, using 95% ethanol. The granules compacted to batches of sustained-release matrix tablets. The tablet batches were characterized for tablet properties, and dissolution studies carried out using simulated gastric and intestinal fluid separately at different agitation rates. The data from dissolution studies were subsequently fitted into 4 drug release kinetics models.

Results: The swelling of the 3 polymers over time was noteworthy, although there was no significant difference between them. The release kinetic followed the Higuchi model and zero-order releasing more than 90% over 8 hours period, with t10 and t90 released at 14 minutes and 6.8 hours respectively. The mechanical properties of the tablets were within the acceptable limit.

Conclusion: The agitation rate and pH of the medium had no significant effect on the release of the theophylline from the batches of matrix tablets except in the case of F1 which showed a marginally significant effect.

Keywords:
Theophylline, sustained-release, agitation rate, pH effect, release kinetics, hydrophilic polymer, matrix tablet.

Article Details

How to Cite
Akpabio, E. I., Effiong, D. E., Uwah, T. O., Sunday, N. I., Jacob, G., & Isong, U. (2020). Sustained-release Theophylline Matrix Tablet Using Hydrophilic Polymers: Effects of Agitation Rates and pH on Release Kinetics. Journal of Advances in Medical and Pharmaceutical Sciences, 22(5), 36-50. https://doi.org/10.9734/jamps/2020/v22i530173
Section
Original Research Article

References

Karna S, Chaturvedi S, Agrawal V, Alim M. Formulation approaches for sustained release dosage forms: a review”. Asian Journal of Pharmaceutical and Clinical Research. 2015;8:34-41.

Available:https://innovareacademics.in/journals/index.php/ajpcr/article/view/7185

Mayur Karvekar, Arshad Bashir Khan. A brief review on sustained-release matrix type drug delivery system. Journal of Pharmaceutical Research. 2017;16:282.

DOI: 10.18579/jpcrkc/2017/16/3/118769s

Raslan H, Maswadeh H. In vitro dissolution Kinetic Study of Theophylline from mixed controlled release matrix tablets containing hydroxy propyl methylcellulose and Glycerylbehenate. Indian Journal of Pharmaceutical Sciences. 2006;68:308-312.

DOI: 10.4103/0250-474X.26658

Kendre PN, Lateef SN, Godge RK, Chaudhari PD, Fernandes SL, Vibhute SK. Oral sustained delivery of theophylline floating matrix tablets- formulation and In-vitro evaluation. International Journal of PharmTech Research. 2010;2:130-139.

Available:https//:www.researchgate.net› publication › 285940418

Nagaswamy VD, Sangeetha S, Samantha MK, Sanka S, Suresh B. Design and evaluation of Ethyl cellulose Sustained release matrix tablet of theophylline International journal of Pharmaceutical Science and Nanotechnology. 2008;1:60-63.

Available:https//:www.ijpsnonline.com

El-Bagory I, Barakat N, Ibrahim MA, El-Enazi F. Formulation and in vitro evaluation of theophylline matrix tablets prepared by direct compression: Effect of polymer blends. Saudi Pharmaceutical Journal. 2012;20:229-238.

DOI: 10.1016/j.jsps.2011.11.007

Deshmukh K, Chidambaram K, Sadasivuni KK, Ponnamma D, AlMaadeed MA. Biopolymer composites with high dielectric performance: Interface engineering in electronics in: Biopolymer Composites in Electronics. 2017;27-128.

Available:https://doi.org/10.1016/B978-0-12-809261-3.00003-6

Maiti S, Dey P, Kaity S, Ray S, Maiji S, Sa B. Investigation on processing variables for the preparation of fluconazole-loaded ethyl cellulose microspheres by modified multiple emulsion technique. AAPS Pharm SciTech. 2009;1(10):703-715.

DOI: 10.1208/s12249-009-9257-7

Kuen Yong Leea, David J. Mooneyd. Alginate: Properties and biomedical applications. Progress in Polymer Science. 2012;37:106–126.

DOI:10.1016/j.progpolymsci.2011.06.003

Thomas Dürig Kapish Karan. Binders in wet granulation in: Handbook of pharmaceutical wet granulation theory and Practice in a Quality by Design Paradigm. 2019;317-349.

DOI:10.1016/B978-0-12-810460-6.00010-5

Banes PJ. Theophylline. American Journal of Respiratory and Critical Care Medicine. 2013;188(8):901–906.

DOI: 10.1164/rccm.201302-0388PP

Akpabio EI, Effiong DE, Uwah TO, Sunday NI. Formulation and in-vitro evaluation of theophylline hydrochloride effervescent floating tablets: Effect of polymer concentration on tablet buoyancy. International J of Pharm. Pharm. Sci. 2020;12(1):59-65.

DOI: 10.22159/ijpps.2020v12i1.35055

Okunlola A, Adewusi SA. Development of Theophylline microbeads using pregelatinized breadfruit starch (Artocarpus altilis) as a novel co-polymer for controlled release. Advanced Pharmaceutical Bulletin. 2019;9(1).

DOI: 10.15171/apb.2019.0

Aulton ME. Powder flow in: Aulton ME, Taylor KMG, Aulton’s Pharmaceutics: The design and manufacture of medicines (5th ed.). Churchill Livingstone Elsevier. 2018; 189-198.

Available:https://www.inkling.com/store/book/aulton-aultons-pharmaceutics-5e/

Akpabio EI, Effiong DE, Uwah TO, Godwin J. Evaluating Hydrocolloids of Sida acuta in sustained-release matrix tablet of Ibuprofen. Global Journal of Medical research. 2020;20(1):1-8

Available:https://globaljournals.org/GJMR_Volume20/3-Evaluating-Hydrocolloids-of-Sida-Acuta.pdf

Ofori-Kwakye K, Mfoafo KA, Kipo SL, Kuntworbe N, El Boakye-Gyasi M. Development and evaluation of natural gum-based extended release matrix tablets of two model drugs of different water solubilities by direct compression. Saudi Pharmaceutical Journal. 2006;24: 82-91

Available:http://dx.doi.org/10.1016/j.jsps.2015.03.005

Uwah Timma O, Akpabio EI, Effiong DE, Akpabio AE, Jacob G. Preliminary Investigations into The Physicochemical and Compaction Characteristics of Modified Starch of Discorea alata Using Diclofenac sodium tablet. International Journal of Pharmacy and Pharmaceutical Sciences. 2018;10(7):66-74.

DOI: 10.22159/ijpps.2018v10i7.23730

Thoorens G, Krier F, Leclercq B, Carlin B, Evrard B. Microcrystalline cellulose, a direct compression binder in a quality by design environment – A review. Int. J. Pharm. 2014;473(1-2):64–72.

DOI: 10.1016/j.ijpharm.2014.06.055

International Pharmacopoeia. WHO Department of Essential Medicines and Health Products; 2019.

Available:https://apps.who.int/phint/pdf/b/7.5.3.5.2-Uniformity-of-mass-for-single-dose-preparations.pdf

Pharmacopeia, United States. The United States Pharmacopeia 29, The National Formulary 24. United States Pharmacopeial Convention. 2006;2110.

Available:http://ftp.uspbpep.com/v29240/usp29nf24s0_m82190.html

Ahmad M, Akhtar N, Murtaza G, Hussain SW. Formulation development and in-vitro evaluation of theophylline microcapsules Pak. J. Pharm. Sci. 2012;5(1):15-19.

Available:https://www.ncbi.nlm.nih.gov/pubmed/22186304

Obeidat WM, Price JC. Viscosity of polymer solution phase and other factors controlling the dissolution of theophylline microspheres prepared by the emulsion solvent evaporation method. J. Microencapsul. 2003;20:57-65.

Available:https://www.ncbi.nlm.nih.gov/pubmed/12519702

Chakraborty S, Khandai M, Sharma A, Niranjan Patra CH, Jagannath Patro V, Kumar Sen K. Effects of drug solubility on the release kinetics of water soluble and insoluble drugs from HPMC based matrix formulations. Acta Pharm. 2009;59:313–323.

Available:http://dx.doi.org/10.2478/v10007-009-0025-8

Ali Nokhodchi, Shaista Raja, Pryia Patel, and Kofi Asare-Addo. The role of oral controlled release matrix tablets in drug delivery systems. Bioimpacts. 2012;2(4): 175–187.

DOI: 10.5681/bi.2012.027

Evelyn Ojoe; Edna Mitie Miyauchi; Tais Cobo Viviani; Vladi Olga Consiglieri. Formulation and in vitro evaluation of theophylline-Eudragit® sustained-release tablets. Rev. Bras. Cienc. Farm. 2005;41 (3).

DOI: 10.1590/S1516-93322005000300011