PREPARATION AND CHARACTERIZATION OF CHITOSAN SUCCINATE AS COATING POLYMER FOR ENTERIC-COATED TABLET
DOI:
https://doi.org/10.22159/ijap.2018.v10s1.76Keywords:
Enteric-coated tablet, Chitosan succinate, N-acylation chitosan, Sodium diclofenacAbstract
Objective: This present study was aimed to evaluate the potential of chitosan succinate as a coating polymer.
Methods: In this study, chemical modification of chitosan was performed by substituting a succinate group into chitosan's amine group. This reaction
used a water-solvent method to obtain chitosan succinate. Chitosan succinate was characterized and used as a coating agent in enteric-coated tablet
dosage forms containing sodium diclofenac as the drug model at concentrations of 3% and 4% and combined it with hydroxypropyl methylcellulose
phthalate (HPMCP) in ratios of 3:1 and 2:1 (3%). The obtained tablets were evaluated based on their physical appearance, uniformity of weight and
size, thickness film, disintegration time for an hour in acid, and dissolution profile.
Results: Although the enteric-coated tablets with 3% and 4% chitosan succinate dissolved after 1 h in acid, they could not hold drug release in the
acid medium under 10%. The enteric-coated tablet combined with chitosan succinate and HPMCP (3:1 and 2:1) at 3% did not dissolve after 1 h in the
acid medium and could hold drug release up to 8.53% in acid.
Conclusion: A combination of chitosan succinate and HPMCP (3:1 and 2:1) at 3% has a better ability to hold drug release in acid medium and met the
requirement as a coating in enteric-coated tablet dosage forms.
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References
Porter SC, Bruno CH. Coating of pharmaceutical solid dosage forms.
In: Lieberman HA, Lachman L, Schwartz JB, editors. Pharmaceutical
Dosage Forms: Tablets. 2nd ed., Vol. 3. USA: Marcel Dekker; 1990.
p. 93-113.
Leon L, Lieberman, Herbert A, Joseph BS, editors. Pharmaceutical
Dosage Forms: Tablets. 2nd ed., Vol. 3. USA: Marcel Dekker; 1990.
p. 123-38, 592, 784.
Rowe RC, Sheskey PJ, Owen SC. Handbook of Pharmaceutic
Excipients. 5th ed. London: Pharmaceutical Press and American
Pharmacists Association; 2006.
Champagne LM. The Synthesis of Water Soluble N-Acyl Chitosan
Derivatives for Characterization as Antibacterial Agents. Academic
Dissertation. The Department of Chemistry, B.S. Xavier University of
Louisiana; 2008.
Aiedeh K, Taha MO. Synthesis of chitosan succinate and chitosan
phthalate and their evaluation as suggested matrices in orally
administered, colon-specific drug delivery systems. Arch Pharm
(Weinheim) 1999;332:103-7.
Radiman CL, Achmad S, Ariwahjoedi B. Synthesis of water soluble
succinate chitosan (Sintesis kitosan suksinat larut air). Akta Kimindo
;2:113-6.
Verma N, Chattopadhiyay P. In-vitro and in-vivo evaluation of
mucoadhesive patches containing metropolol succinate. Asian J Pharm
Clin Res 2012;5:168-71.
Yadav U, Chowdhuri AR, Sahu SK, Husain N, Rehman Q. Formulation
of nanoparticles of terlmisartan incorporated in carboxymethyl chitosan
for the better drug delivery and enhanced bioavailability. Asian J Pharm
Clin Res 2017;10:236-41.
Aiping Z, Tian C, Lanhua Y, Hao W, Ping L. Synthesis and
characterization of N-succinyl-chitosan and its self-assembly of
nanospheres. Carbohydr Polym 2006;66:274-9.
Dutta PK, Dutta J, Tripathi VS. Chitin and chitosan: Chemistry,
properties, and applications. J Sci Ind Res 2004;63:20-31.
Al-Najjar BY, Hussain SA. Chitosan microspheres for the delivery of
chemotherapeutic agents: Paclitaxel as a model. Asian J Pharm Clin
Res 2017;10:15-9.
Anthony CM, Osselton D, Widdop B. Clarke’s Analysis of Drugs and
Poisons. 3rd ed. London: Pharmaceutical Press; 2005.
Ying GQ, Yang H, Yi Y, Xu F. Relationships between the molecular
structure and moisture-absorption and moisture-retention abilities of
succinyl chitosan. Polymer Bull 2007;59:509-16.
Yan C, Chen D, Gu J, Hu H, Zhao X, Qiao M. Preparation of N-succinylchitosan
and its physical-chemical properties as a novel excipient.
Yakugaku Zasshi 2006;126:789-93.
Lima IS, Airoldi C. Interaction of copper with chitosan and succinic
anhydride derivative-a factorial design evaluation of the chemisorption
process. Colloids Surf A Physicochem Eng Asp 2003;229:129-36.
Shigemasa Y, Matsura H, Sashiwa H, Saimoto H. Evaluation of
different absorbance ratios from IR spectroscopy for analyzing the
degree of deacetylation in chitin. Int J Biol Macromol 1996;18:237-42.
Martin A, Swarbrick J, Cammarata A. Pharmaceutical Physics: The
Basic of Physical Chemistry in Pharmaceutical Science (Farmasi
fisika: Dasar-dasar kimia fisik dalam ilmu farmasetik). 3rd ed. Jakarta:
UI Press; 1990. p. 859.
Guillory KJ. Developing Solid Oral Dosage Forms: Pharmaceutical
Theory and Practice. USA: Charon Tech; 2009.
Brady JE, Dürig T, Shang SS. Polymer properties and characterization.
In: Yihong Q, Chen Y, Zhang GZ, editors. Developing Solid Oral
Dosage Forms (211). New York: Academic Press; 2009.