Formulation of orodispersible atenolol-β-cyclodextrin tablets with co-processed crospovidone-croscarmellose sodium and poloxamer 188
DOI:
https://doi.org/10.12928/pharmaciana.v9i2.12841Keywords:
atenolol, orodispersible tablet, β-cyclodextrin, co-processed, Poloxamer 188Abstract
The use of conventional tablets in geriatric patients is currently limited because of a decrease in their physiological functions, such as tremor and difficulty of swallowing pills, which lowers their compliance with drug therapy. Hypertension, one of the degenerative diseases suffered by geriatric patients, is treatable with atenolol tablets or capsules that are less soluble in water or, in other words, has a poor dissolution. This research attempted to improve the dissolution of atenolol by formulating it into orodispersible tablets (ODTs), and as such, the disintegration time was modified by adding co-processed crospovidone-croscarmellose sodium in 1:1 ratio. Moreover, Poloxamer® 188 was added to the formulation of atenolol-β-cyclodextrin inclusion complex. The post-compression test revealed that ODTs disintegrated quickly within 36.67±1.21 seconds (<60 seconds) and had physical characteristics that met the pharmaceutical requirements. The amount of atenolol dissolved within 30 minutes in the dissolution study was 84.39% (%Q30 minutes). The results of the accelerated stability study (at 40 °C and RH 75±5 %) for two weeks proved that the physical and chemical characteristics of the produced orodispersible atenolol tablets were stable.
References
Agoes G, 2012, Sediaan Farmasi Padat 1st edition. Bandung: Penerbit ITB.
Akbari, B. V., Valaki, B.P., Maradiya, V.H., Akbari, A.K., Vidyasagar, G., 2011. Effect of Types of Cyclodextrin on Rosuvastatin Calcium Inclusion Complex, Indian Journal of Pharmacy, 2, 1–8.
Al-Ghabban, F.M., Al-Ani, I.H., Hassan, S.F., Salan, N., 2013, Formulation of Prifinium Bromide and Prifinium Bromide-Diclofenac Sodium combination as orodispersible tablets, International Journal of Pharmacy and Pharmaceutical Sciences, 5: 652–659.
Al Hanbali, O.A., Hamed, R., Arafat, M., Bakkour, Y., Al-Matubsi, H., Mansour, R., Al-Bataineh, Y., Aldhoun, M., Sarfraz, M., Yousef Dardas, A.K., 2018, Formulation and evaluation of diclofenac controlled release matrix tablets made of HPMC and Poloxamer 188 polymer: An assessment on mechanism of drug release., Pakistan Journal of Pharmaceutical Sciences, 31: 345–351.
Allen, L. V, Ansel, H.C., 2014, Ansel’s Pharmaceutical Dosage Forms and Drug Delivery Systems, Philadelphia: Wolters Kluwer Health.
Augsburger, L.L., Hoag, S.W., 2008, Pharmaceutical Dosage Forms-Tablets, in Pharmaceutical Dosage Forms: Tablets. New York: Informa Healthcare.
Aulton M, Summers M, 2013, Aulton’s Pharmaceutics The Design and Manufacture of Medicines. Philadelphia: Churchill Livingstone.
Buha, S.M., Baxi, G.A., Shrivastav, P.S., 2012, Liquid Chromatography Study on Atenolol--Cyclodextrin Inclusion Complex, ISRN Analytical Chemistry, 2012.
Callahan, J.C., Cleary, G.W., Elefant, M., Kaplan, G., Kensler, T., Nash, R.A., 1982, Equilibrium moisture content of pharmaceutical excipients, Drug Development and Industrial Pharmacy, 8: 355–369.
Chandrasekhar, P., Shahid Muhammad, S., Niranjan Babu., M., 2013, Formulation and Evaluation of Oral Dispersible Tablets of Anti Hypertensive Drug Atenolol, International Journal of Pharmacy, 3: 79–84.
Crouter, A., Briens, L., 2013, The Effect of Moisture on the Flowability of Pharmaceutical Excipients, American Association of Pharmaceutical Scientist, 15(1): 65–74.
Dashora, K., 2013, Formulation and Evaluation of Fast Dissolving Tablets Atenolol, Journal of Chemical and Pharmaceutical Sciences, 6(2): 113–119.
Departemen Kesehatan Republik Indonesia, 2014, Farmakope Indonesia Edisi V, Departemen Kesehatan Republik Indonesia, Jakarta.
Desai, P.M., Er, P.X.H., Liew, C.V., Heng, P.W.S., 2014, Functionality of Disintegrants and Their Mixtures in Enabling Fast Disintegration of Tablets by a Quality by Design Approach, American Association of Pharmaceutical Scientist, 15(5): 1093–1104.
Desai, P.M., Liew, C.V., Heng, P.W.S., 2016, Review of Disintegrants and the Disintegration Phenomena, Journal of Chemical and Pharmaceutical Sciences, 105(9): 2545–2555.
Dipiro, E. Al, 2008, Pharmacotherapy: A Pathophysiological Approach. New York: McGraw Hill Medical.
Food and Drug Administration (FDA), 2008, Guidance for industry: orally disintegrating tablets. Cent. Drug Eval. Res. 1–3.
Ghosh, A., Biswas, S., Ghosh, T., 2011, Preparation and Evaluation of Silymarin β-cyclodextrin Molecular Inclusion Complexes, Journal of Young Pharmacist, 3(3): 205–210.
Gite, S., 2014, Development and Evaluation of Mucoadhesive Tablets of Atenolol and It’s Β-Cyclodextrin Complex, Asian Journal of Biomedical and Pharmaceutical Sciences, 4(37): 25–32.
Hadaruga, D.I., Hadaruga, N.G., Hermenean, A., Rivis, A., Paslaru, V., Codina, G., 2008, Bionanomaterials: Thermal Stability of the Oleic Acid/alpha- and beta-cyclodextrin Complexes, Revista De Chimie, 59(9): 994–998.
Hahm, H.A., Augsburger, L.L., 2008, Orally disintegrating tablets and related tablet formulations, in: Pharmaceutical Dosage Forms: Tablets. New York: Informa Healthcare.
Kabra, A.O., Shah, F.B., Wanare, R.S., April, M., 2011, Formulation and In-Vitro evaluation of rapidly disintegrating tablets using captopril as a model drug, International Journal of Pharmaceutical Sciences Review and Research, 7(2), 206–210.
Kaur, G., Jaiswal, S., Gupta, G.D., 2014, Formulation and Evaluation of Melt in Mouth Tablet by Solid Dispersion Technique, Indo American Journal of Pharmacaeutical Research, 4 (6): 2897-2909.
Kumare, M.M., Marathe, R.P., Kawade, R.M., Ghante, M.H., Shendarkar, G.R., 2013, Design of fast dissolving tablet of Atenolol using novel co-processed superdisintegrant, Asian Journal of Pharmaceutical and Clinical Research, 6(3): 81–85.
Mittapalli, R.K., Sha Qhattal, H.S., Lockman, P.R., Yamsani, M.R., 2010, Varying efficacy of superdisintegrants in orally disintegrating tablets among different manufacturers, Pharmazie, 65(11): 805–810.
Nagar, P., Singh, K., Chauhan, I., Verma, M., Yasir, M., Khan, A., Sharma, R., Gupta, N., 2011, Orally disintegrating tablets: formulation, preparation techniques and evaluation, Journal of Applied Pharmaceutical Science, 1(4): 35–45.
Parfati, N., Rani, K.C., Charles, N., Geovanny, V., Pradnya, D.P., n.d. 2017, Formulasi Orally Disintegrating Tablet Atenolol-β-cyclodextrin Sodium Starch Glycolate, Media Pharmaceutica Indonesiana, 1(4): 197–203.
Parfati, N., Rani, K.C., Meilany, 2018, The effect of coprocessed superdisintegrants ratio (Crospovidone-sodium starch glycolate) to the physicochemical characteristics of atenolol orally disintegrating tablets, Asian Journal of Pharmaceutical and Clinical Research, 11(2): 318-324.
Qiu, Y., Chen, Y., Zhang, G., Liu, L., Porter, W., 2009, Developing solid oral dosage forms. Pharmaceutical theory and practice. New York: Elsevier.
Ramani, R.G., Road, S., Address, C., 2010, Novel Co-Processed Superdisintegrants in The Design of Fast Dissolving Tablets, International Journal of Pharma and Bio Sciences, V1(1), 1-12.
Shahi, S.R., Kanzarkar, M. V., Khadabadi, S.S., Zadbuke, N., 2013, Formulation and evaluation of atenolol orodispersible tablets by phase transition technology, International Journal of Pharmacy and Pharmaceutical Sciences, 5(4): 604–609.
Shankarrao, K.A., Mahadeo, G.D., Balavantrao, K.P., 2010, Formulation and in-vitro evaluation of orally disintegrating tablets of olanzapine-2-hydroxypropyl-β-cyclodextrin inclusion complex. Iranian Journal of Pharmaceutical Research, 9(4): 335-347.
Shargel, L., Yu, A.B.C., n.d, 2015, Applied Biopharmaceutics and Pharmacokinetics seventh edition. New York: McGraw Hill Education.
Sinko, P., 2011, Martin’s Physical Pharmacy And Pharmaceutical Sciences. Philadelphia: Wolters Kluwer Health.
Sun, C.C., 2008, Mechanism of moisture induced variations in true density and compaction properties of microcrystalline cellulose, International Journal of Pharmaceutics, 346(1-2): 93–101.
Türkoǧlu, M., Varol, H., Çelikok, M., 2004, Tableting and stability evaluation of enteric-coated omeprazole pellets, European Journal of Pharmaceutics and Biopharmaceutics, 57(2): 279-286.
United States Pharmacopeial Convention, 2017, U.S. Pharmacopeia National Formulary, The United States Pharmacopeial Convention, Rockville.
Vivek, R., Shailendra, P.S., Sheory, R. V, 2012, Formulation and Evaluation of Orally Disintegrating Tablets of Atenolol with Cyclodextrin Inclusion Complex, International Journal of Drug Discovery and Herbal Research, 2: 461–464.
Downloads
Published
Issue
Section
License
Authors who publish with Pharmaciana agree to the following terms:
- Authors retain copyright and grant the journal the right of first publication with the work simultaneously licensed under a Creative Commons Attribution License (CC BY-SA 4.0) that allows others to share the work with an acknowledgment of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgment of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work.
1.png)
