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Pharmaceutical Technology: Controlled Drug Release, Volume 2

Pharmaceutical Technology: Controlled Drug Release, Volume 2

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18 MATRIX FORMULATIONS [CH. 1<br />

Fig. 3—Effect of grain size for drug A.<br />

with the Moritz TS10 are 166 µm (formula 6) and 152 µm (formula 7). For the granulate prepared<br />

with a planetary mixer, the mean diameter is 326 µm and the distribution is wider (80% between<br />

180 and 500 µm).<br />

If calcium hydrogen phosphate is the only diluent, the dissolution rate is more dependent on pH<br />

variations (Fig. 4) than with lactose: t 50 increases from 8.0 h (pH 2.0) to 22.1 h (pH 7.4) with<br />

calcium hydrogen phosphate, and from 9.7 h (pH 2.0) to 13.7 h (pH 7.4) with lactose.<br />

Fig. 4—Effect of pH for drug A.<br />

<strong>Drug</strong> B<br />

The dissolution rate does not exhibit significant differences between Methocel E4M CR,<br />

Methocel K4M and Metolose 60SH4000 (formula 8): the respective t 50 values are 1.78 h, 1.86 h<br />

and 1.75 h. Dissolution speed is higher with Metolose 90SH4000 (t 50 =1.06 h) (Fig. 5) and

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