High-amylose sodium carboxymethyl starch matrices: development and characterization of tramadol hydrochloride sustained-release tablets for oral administration.

Teresa Nabais,Grégoire Leclair

doi:10.1155/2014/391523

Abstract

Substituted amylose (SA) polymers were produced from high-amylose corn starch by etherification of its hydroxyl groups with chloroacetate. Amorphous high-amylose sodium carboxymethyl starch (HASCA), the resulting SA polymer, was spray-dried to obtain an excipient (SD HASCA) with optimal binding and sustained-release (SR) properties. Tablets containing different percentages of SD HASCA and tramadol hydrochloride were produced by direct compression and evaluated for dissolution. Once-daily and twice-daily SD HASCA tablets containing two common dosages of tramadol hydrochloride (100 mg and 200 mg), a freely water-soluble drug, were successfully developed. These SR formulations presented high crushing forces, which facilitate further tablet processing and handling. When exposed to both a pH gradient simulating the pH variations through the gastrointestinal tract and a 40% ethanol medium, a very rigid gel formed progressively at the surface of the tablets providing controlled drug-release properties. These properties indicated that SD HASCA was a promising and robust excipient for oral, sustained drug-release, which may possibly minimize the likelihood of dose dumping and consequent adverse effects, even in the case of coadministration with alcohol.

Highlights

Starch is a naturally occurring and a biodegradable polymer that is metabolized by the human body
As non-SD high-amylose sodium carboxymethyl starch (HASCA) particles did not possess any biding properties and the SD procedure resulted in a tablet weight (TW) [T50%, T90%] (h)
SD HASCA is an interesting excipient for sustained drugrelease in solid oral dosage forms

Summary

Introduction

Starch is a naturally occurring and a biodegradable polymer that is metabolized by the human body. Starch is an abundant, cost-effective, and renewable material [1] Due to these advantages, starches and modified starches have been widely and safely used in the food industry as thickeners, enhancers, of organoleptic properties, or texture modifiers and in the pharmaceutical industry as fillers, binders, disintegrants [2], and, more recently, as hydrophilic excipients for controlled drug-release. Starches and modified starches have been widely and safely used in the food industry as thickeners, enhancers, of organoleptic properties, or texture modifiers and in the pharmaceutical industry as fillers, binders, disintegrants [2], and, more recently, as hydrophilic excipients for controlled drug-release Numerous starchmodification methods, such as chemical [3], physical (i.e., gelatinization) [4], enzymatic [5], or a combination thereof, have been employed to produce new starch products with specific properties. Some of the modifications commonly employed to prepare starch derivatives are carboxymethylation, ethoxylation, and oxidation [6]

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