Comparison with the Base Case

With the same specifications of 99.5 wt% acetic acid in the bottom product and 0.1 wt% acetic acid in the top aqueous product, the acetic acid and water composition profiles of the two base cases are similar. The major difference is the isobutyl acetate composition profiles inside the column. The isobutyl acetate composition inside the top parts of the column is lower than the case with no side-draw and no feed impurity. Also, even with a very small amount of impurity in the feed, the impurity composition inside the column is quite high. 

TABLE 9.19 Comparison of Base-Case Operating Conditions in Sections 9.3 and 9.4. 

ACETIC ACID-WATER (ISOBUTYL ACETATE AS TTHE ENTRAINER) 

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Viracept (nelfinavir, AG-1343) of Agouron (La Jolla/CA, USA) in collaboration with Japan Tobacco (Tokyo, Japan) began only in July 1995 with phase II investigations. Dosages in phase II are set between 770 and 1030 mg daily. The viral count decreased between 15- and 75-fold in comparison with the base case. 

In July 1995, Vertex (Cambridge/MA, USA) presented encouraging preclinical and phase I results for Agenerase (amprenavir,VX-478) the compound demonstrated no toxicity for single doses up to 1200 mg but 70-78% bioavailability in tablet form and a half-life of 8 h in blood plasma, in combination with a 25-fold decrease of viral count in comparison with the base case. Even versus the most resistant HIV strain, VX-478 is only 15-fold less sensitive than against an unmutated virus. 

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