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«Dissertation Zur Erlangung des Doktorgrades der Naturwissenschaften Der Fakultät für Mathematik, Informatik und Naturwissenschaften der ...»

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In Fig. 24 drug release from the liquisolid compacts LS-N and the conventional tablets are shown. It is obvious that the release from the liquisolid compacts LS-N was much faster than that from the conventional tablets. This may be attributed to the above mentioned dissolved state of the drug in these liquisolid compacts. However, in comparison to the liquisolid compacts LS-1 (Fig. 20) containing Avicel® and Aerosil® as carrier and coating materials, respectively, it is interesting, that the release from LS-N compacts was slower than that from LS-1 compacts within the first 10 min, although both formulations contained a 0.9 % drug solution in PEG 300 as liquid portion. The percentage of griseofulvin released from LS-1 compacts reached 95 % already after 5 min, while with LS-N compacts only a release of 82 % was observed within this time period. This initially slower release rate from LS-N compacts may be explained by the slower disintegration of LS-N compacts (Table 11) compared to LS-1 compacts, which disintegrated instantaneously. With LS-N compacts disintegration was the rate-limiting step and thus, drug release may be accelerated by increasing the amount of disintegrant in the formula resulting in faster disintegration.

Fig. 24: Drug release profiles of the liquisolid compacts LS-N and the conventional tablets (means ± SD; n = 3) Drug release enhancement from hydrophilic aerogels and liquisolid compacts 89

5.4 Conclusion Griseofulvin release from silica aerogel tablets and from liquisolid compacts is faster than that from conventional tablets containing the crystalline drug. Moreover, with liquisolid compacts containing the drug suspended in PEG 300 the release rate increases with rising percentage of dissolved drug in the liquid portion. Highest drug release rates are observed with liquisolid compacts containing a drug solution as liquid portion. Therefore, if the desired drug dose is high and/or the drug solubility in the liquid vehicle is low, a high amount of liquid vehicle is needed which in turn requires high amounts of carrier and coating materials. This results in an increase in tablet weight usually leading to an unacceptably large tablet size. Replacement of the commonly used carrier and coating materials Avicel® and Aerosil®, respectively, by the highly adsorptive silicate Neusilin® allows a considerably higher liquid loading capacity ultimately resulting in lower tablet weights.

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