Microencapsulation of a Slightly Soluble Drug by Surface Neutralization Method Using an Enteric Polymer

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Succeeding our previous study on enteric microencapsulation by surface neutralization method for acidic drugs, a new means of application was developed for the encapsulation of non-acidic drugs. Indomethacin was chosen as a model drug in this study because of its low solubility in water and non-acidicity. Carboxymethylethylcellulose (CMEC) was used as enteric polymer as previously.Indomethacin was not encapsulated as it was, but the encapsulation could be done using its core granules added with an organic acid. Thus, the influences of preparation temperature, species of organic acid and its concentration in the cores as well as the species of binder on the properties of resultant microcapsules (MCs) were examined.CMEC content in MCs increased as the temperature increased. The CMEC content prepared using maleic acid was higher than that prepared using fumaric acid. These phenomena were correlated with the dissolution rate of organic acid from the cores during the manufacturing process and the phase separation of CMEC determined at various temperatures and pH.MCs having thick films prepared at high temperatures did not always have high resistance to the dissolution of indomethacin in the 1st fluid. The most effective membrane was obtained when MCs were prepared at around 20℃.Binders used in the cores affected the CMEC content in MCs and the dissolution rate of indomethacin. Hydrophobic ethylcellulose (EC) depressed the dissolution more strongly than did hydrophilic polyvinylalcohol (PVA).
公益社団法人日本薬学会の論文
1990-09-25

Microencapsulation of a Slightly Soluble Drug by Surface Neutralization Method Using an Enteric Polymer

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