“These new compounds, like rocks, never dissolve in water.” It sounds so familiar to you, does it not Product development scientists often encounter signi cant dif culties in solving the problem
of poor water solubility of drug candidates in the development of pharmaceutical dosage forms
(Sweetana and Akers, 1996; Yamashita and Furubayashi, 1998; Willmann et al., 2004; Di et al.,
2006). As a matter of fact, more than one-third of the drugs listed in the U.S. Pharmacopeia fall into
the poorly water-soluble or water-insoluble categories (Pace et al., 1999). It was reported a couple of
decades ago that more than 41% of the failures in new drug development have been attributed to poor
biopharmaceutical properties, including water insolubility (Lipper, 1999; Prentis et al., 1988), while
it was still indicated recently that about 50% failure of drug candidates was due to poor “drug-like”
properties (Hartmann et al., 2006). It is commonly recognized in the pharmaceutical industry that on
average more than 40% of newly discovered drug candidates are poorly water soluble. Poor “druglike”
properties of lead compounds led to ineffective absorption in the site of administration, which
has been designated as an important part of the high clinical failure due to poor pharmacokinetics.
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