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据统计,1987～1994年合成的2 246种药物中,有31.2%的溶解度不超过20μg·ml~(-1);有人估计,近年合成的药物,有约1/3的溶解度不足10μg·ml~(-1),有1/3溶解度为10～100μg·ml~(-1)(均属于《中国药典》规定的几乎不溶或不溶范围)。20世纪80年代以前,溶解度不超过20g·ml~(-1)的药物还是闻所未闻,因其溶解度达不到治疗浓度。目前,特性溶解度低至1μg·ml~(-1)的候选药物也还不少。通过多种提高溶解度的途径,这些药物都可能获得满意的药效。
According to statistics, 31.2% of the 2 246 medicines synthesized in 1987-1994 do not exceed 20μg · ml -1. Some people estimate that about 1/3 of the drugs synthesized in recent years have a solubility of less than 10μg · ml ~ (-1), 1/3 of the solubility was 10 ~ 100μg · ml ~ (-1) (all belong to the “Chinese Pharmacopoeia” almost insoluble or insoluble range). Before the 1980s, the solubility of no more than 20g · ml ~ (1) of the drug is still unheard of because of its solubility does not reach the therapeutic concentration. At present, there are not many candidate drugs with characteristic solubility as low as 1 μg · ml -1. Through a variety of ways to increase solubility, these drugs are likely to obtain satisfactory efficacy.