ENZYMATIC DEGRADATION OF CROSS-LINKED EXCIPIENT MATRIX OF CO-PROCESSED XANTHAN GUM-AMYLOSE AND DISSOLUTION PROFILE OF DICLOFENAC SODIUM TABLET

Silvia Surini,Azizahwati Azizahwati,Nurul Nizma

doi:10.22159/ijap.2017.v9s1.42_48

Silvia Surini, Azizahwati Azizahwati + Show 1 more

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https://doi.org/10.22159/ijap.2017.v9s1.42_48

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Abstract

Objectives: This study aims to determine the amount of excipient that is degraded by alpha-amylase and the influence of alpha-amylase to thedissolution 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 for60 minutes. Sustained-release tablet with CL-Co-A-XG excipient as a matrix is formulated through direct compression method. Then, drug dissolutiontests 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 releaseprofile of F1-F6 tablets show the sustained-release profile that follows zero-order and Korsmeyer–Peppas kinetics and is unaffected by the presenceof 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.

Highlights

Oral administration of drugs is a frequently used route of administration
Sustained-release tablet preparations contain two or more doses of a drug, which are released over time
Materials The materials used for this study were: Diclofenac sodium (Yung Zip Chemical, Taiwan); Amylose (Shangqiu Kangmedia Bio Tech, China); Xanthan gum (CV, Tristars Chemicals, Indonesia); sodium trimetaphosphate (STMP) (Shangqiu Kangmedia Bio-Tech, China); Alpha-amylase porcine (Sigma, Missouri, United States); Avicel PH 102, sodium hydroxide, hydrochloric acid, sulfuric acid, nitric acid, ammonium molybdate tetrahydrate, sodium hydroxide, sodium chloride, sodium bicarbonate, aqua destillata (Merck, Darmstadt, Germany); potassium dihydrogen phosphate, 96% ethanol (Brataco, Jakarta, Indonesia); ascorbic acid (Takeda, Tokyo, Japan); and iodine and potassium iodide (Mallinckrodt, Surrey, London)

Summary

Introduction

Oral administration of drugs is a frequently used route of administration. Various forms of pharmaceutical preparations are developed around it. One of the fastest growing oral preparations today is the sustainedrelease tablet. Sustained-release tablet preparations contain two or more doses of a drug, which are released over time. The sustained-release preparation aims to decrease the frequency of drug administration for drugs with short half-lives. Reduced frequency of drug delivery will improve patient compliance and reduce the risk of fluctuations in blood levels when using the drug. The popular system used in sustained -release drugs is the matrix system. The polymers used in the preparation of the sustained-release preparation matrix should have characteristics that allow it to regulate its release of the drug and keep the form of the matrix during the drug’s release [1]

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