• Journal of Pharmaceutical Investigation
• /
• 제27권3호
• /
• pp.213-217
• /
• 1997

The present sustained-release terfenadine-pseudoephedrine HCl dosage form was the core tablet composed of outer (fast-release) layer containing 60 mg of terfenadine and l0mg of pseudoephedrine HCl, and inner (sustained-release) layer containing 110 mg of pseudoephedrine HCl. The purpose of this study was to investigate the possibility of formulating the terfenadine-pseudoephedrine HCl double-layered tablet which was bioequivalent to the core tablet. Its sustained-release and fast-release layer were formulated with disintegrating agents and polymers, respectively, varying with their kinds and amounts. The comparative dissolution test of double-layered and core tablet was carried out at pH 1.2, 4.0 and 6.8, leading to select composite of double-layered tablet whose dissolution pattern was similar to that of core tablet. It was composed of fast-release layer containing 60mg of terfenadine. 10 mg of pseudoephedrine HCl, sodium bicarbonate, microcrystalline cellulose and sodium starch glycolate, and sustained-release layer containing 110 mg of pseudoephedrine HCl and ethylcellulose/hydroxypropyl methylcellulose) (110/30 mg/tablet).

• 약학회지
• /
• 제32권4호
• /
• pp.251-257
• /
• 1988

A simple and sensitive HPLC method was developed for the simultaneous determination of ten kinds of active ingredients formulated in commercial cough-cold mixtures. A group of Pseudoephedrine HCl, dl-Methylephedrine HCl, Noscapine, Chlorophenylamine maleate, Dextromethorphan HBr and Phenylpropanolamine HCl were determined at 254nm using a Novapak $C_{18}$ column with mobile phase consisting of a mixture of methanol-acetonitrile-1, 4dioxane-tetrahydrofuran-water(12 : 20 : 20 : 5 : 43, pH4.7) containing 0.013M-dioctyl sodium sulfosuccinate. The another group of Acetoaminophen, Caffeine, Guaifenesin and Ethenzamide were also determined at 254nm using a Novapak $C_{18}$ column as the stationary phase, and a mixture of methanol-1% aqueous acetic acid (3 : 7). The results indicate that these methods are accurate and precise with relative standard deviation of not more than 1% (n=5) for the above active ingredients.

• 약학회지
• /
• 제41권3호
• /
• pp.305-311
• /
• 1997

Sustained release-microspheres and immediate release-pellets were prepared to develop a controlled release multiparticulate system containing both water soluble and insoluble dr ug. Pseudoephedrin.HCl (EPD) and terfenadine (TRF) were used as model drugs, respectively. Sustained release-EPD microspheres were prepared by solvent evaporation method using Eudragit RL or RS as a matrix combined with pH-insensitive film coating. Smaller EPD microspheres were obtained when smaller amount of Eudragit as a matrix material or larger amount of magnesium stearate as a dispersing agent was used. However the obtained microspheres did not show syfficient sustained release characteristics. About 97% of EPD was released after 1 hr irrespective of matrix material used. Subsequent coating of the microspheres with pH-insensitive polymer such as Eudragit RS or ethylcelulose (EC) resulted good sustained in 37.5, 73.3 and 92.0% release of encapsulated EPD in distilled water after 1, 3 abd 7 hr, respectively. It corresponds to mean dissolution time (MDT) of 2.3 hr, which is much larger than that of un-coated EPD microspheres (0.0048 hr). Immediate release TRF pellets were prepared by spherically agglomerated crystallization using Eudragit E as an inert matrix and methylene chloride as a liquid binder. Using Eudragit E alone as a matrix resulted in satisfactory physical properties of the pellets such as sphericity, surface texture and flowability, but led to slower release of TRF from pellets than un-modified TRF powder (MDT of 1.70 vs 1.43 hr in pH 1.2 dissolution medium). Introducing propylene glycol or sodium lauryl sulfate as an emulsifier brought about faster release of TRF from pellets (MDT of 1.14 and 0.95 hr, respectively). In conclusion, microencapsulation by solvent evaporation combined with film coating and spherically agglomerated crystallization were successfully utilized to prepare controlled release multiparticulate system composed of sustained release EPD-microspheres and immediate release TRF pellets.