ENZYMATIC DEGRADATION OF CROSS-LINKED EXCIPIENT MATRIX OF CO-PROCESSED XANTHAN GUM-AMYLOSE AND DISSOLUTION PROFILE OF DICLOFENAC SODIUM TABLET
DOI:
https://doi.org/10.22159/ijap.2017.v9s1.42_48Keywords:
Cross-linked of excipient co-processed xanthan gum-amylose, Alpha-amylase, Dissolution profile, Enzymatic degradation, Sustained-release tabletAbstract
Objectives: This study aims to determine the amount of excipient that is degraded by alpha-amylase and the influence of alpha-amylase to the
dissolution profile of sustained-release tablets that use matrix CL-Co-A-XG.
Methods: Excipient is cross-linked with two concentrations of sodium trimetaphospate, which are 6% (CL6-Co-A-XG) and 12% (CL12-Co-A-XG).
Each excipient is made with the ratios 1:1, 1:2, and 2:1 amylose-xanthan gum. Enzymatic degradation tests are performed on excipient powders for
60 minutes. Sustained-release tablet with CL-Co-A-XG excipient as a matrix is formulated through direct compression method. Then, drug dissolution
tests are performed in a phosphate buffer with a pH of 7.4 both using and without using alpha-amylase as a medium for 8 hrs.
Results: The results of this study show that CL6-Co-A-XG and CL12-Co-A-XG degraded 20% at 10 and 30 minutes, respectively. In addition, the release
profile of F1-F6 tablets show the sustained-release profile that follows zero-order and Korsmeyer–Peppas kinetics and is unaffected by the presence
of alpha-amylase.
Conclusions: From this study, it can be concluded that the CL-Ko-A-XG excipients are more resistant to enzymatic degradation than amylose. Therefore,
this excipient shows potential as a single matrix sustained-release tablet.
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References
Ratnaparkhi MP, Jyoti PG. Sustained release oral drug delivery systeman
overview. Int J Pharm Res Rev 2013;2(3):11-21.
Ariani L, Surini S. Eksipien Koproses Xanthan Gum-Amilosa
Tersambung Silang Sebagai Matriksdalam Formulasi Tablet Lepas
Lambat Natrium Diklofenak [Tesis]. Depok: Universitas Indonesia;
Hung PV, Morita N. Effects of granule sizes on physicochemical
properties of cross-linked and acetaylated wheat starches. Starch Stärke
;57(9):413-20.
Rudnic E, Schwartz J. Oral solid dosage form. In: Remington JP,
Gennaro AR, editors. The Science and Practice of Pharmacy. Vol. I.
Philadelphia, PA: Lippincott Williams & Willkins; 1995. p. 654-7.
Indonesian Ministry of Health. Farmakope Indonesia. 3rd ed. Jakarta:
Indonesian Ministry of Health; 1979. p. 639.
United States Pharmacopeial Convention. United States
Pharmacopoeia 32: National Formulary 27. Washington DC: United
States Pharmacopeial Convention; 2009.
Cury BS, Klein SI, Evangelista RC. Modeling a system of phosphated
cross-linked high amylose for controlled drug release. Part 1: Synthesis
and polymer characterization. J React Funct Polym 2008;68(8):1200-6.
Bejenariu AC, Popa M, Dulong V, Picton L, Cerf DL. Trisodium
trimetaphosphate crosslinked xanthan networks: Synthesis, swelling,
loading, and releasing behavior. Polym Bull 2009;62(4):525-38.
Wurzburg OB, editor. Cross-linked starches. In: Modified Starches:
Properties and Uses. Florida: CRC Press; 1989.
Mathur A. Studies on Phosphorylation Status of Starch in Potato Tubers
(Solanum tuberosum L.) [Dissertation]. Patiala: Thapar Institute of
Engineering and Technology Patiala; 2003.
Rowe RC, Sheskey PJ, Owen SC. Handbook of Pharmaceutical
Excipients. 6th ed. London: Pharmaceutical Press; 2009. p. 564-5.
Lieberman HA, Lachman L, Schwartz JB. Pharmaceutical Dosage
Forms Tablet. 2nd ed. Vol. 3. New York: Bassel, Marcel Dekker; 1990.
Martin A, Bustamante P, Chun A. Physical Pharmacy: Physical
Chemical Principles in the Pharmaceutical Science. 4th ed. Philadelphia,
PA: Lea & Febiger; 1993. p. 447-52.
Lachman L, Lieberman HA, Kanig J. Teori dan Praktek Farmasi Industri. 3rd ed. Jakarta: UI Press; 1994.
Dumoulin Y, Alex S, Szabo P, Cartilier L, Mateescu MA. Cross-linked amylose as matrix for drug controlled release. X-Ray and FT-IR
structural analysis. Carbohydr Polym 1998;37(4):361-70.
Kinci M, Meleh M, Veber M, Vrecer F. Study of physicochemical parametes affecting the release of diclofenac sodium from liphopilic matrix tablet. Acta Chim Slov 2004;51(3):409-25.
Chen H, Wang Y, Leng Y, Zhao Y, Zhao X. Effect of NaCl and sugar on physicochemical properties of flaxseed polysaccharide-potato starch complexes. Sci Asia 2014;40:60-8.
Shoaib HM, Merchant HA, Tazeen J, Yousuf RI. Once-daily tablet formulation and in vitro release evaluation of cefpodoxime using hydroxylpropyl methylcellulose: A technical note. AAPS Pharm Sci Technol 2006;7(3):E178-83.