论文部分内容阅读
药物以某种方式给药后,其分子能否很好地透过生物膜屏障并及时分布到体内所需作用的部位发挥预期疗效,与其溶解度和溶解速率密切相关。不少药物由于溶解度低于治疗所需浓度而不能制成注射液或由于口服溶解速率低、吸收差而直接影响疗效。因此有的药物即使有较好的生物活性但由于不能获得较好的治疗效果,以至无法应用于临床。如克霉唑虽具有较好的抗霉菌效果,但因不溶于水而无法制成注射剂用于临床。所以增加难溶性药物的溶解度已成为生产和制剂研究中的重要问题。增加溶解度的方法很多,已知的方法有:添加增溶剂和助溶剂、制成复盐或前体药物、改变部分分子结构、复溶媒、溶媒转换、气流粉碎、超声
After the drug is administered in some manner, its molecule can penetrate the biofilm barrier well and distribute to the site of the desired effect in time to exert its expected therapeutic effect, which is closely related to its solubility and dissolution rate. Many drugs because the solubility is lower than the concentration required for treatment can not be made into the injection or oral dissolution rate is low, poor absorption and directly affect the efficacy. Therefore, even if some drugs have good biological activity, they can not be used clinically because of their inability to obtain better therapeutic effects. Such as clotrimazole has a good anti-fungal effect, but can not be made into insoluble in water for clinical use. Therefore, increasing the solubility of poorly soluble drugs has become an important issue in the production and formulation research. There are many ways to increase the solubility, known methods are: adding solubilizers and cosolvents to make double salts or prodrugs, changing some of the molecular structures, complex solvents, solvent conversion, jet milling, sonication