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众所周知大多数药物制成口服剂型,在胃肠道内的溶出均为一级动力学过程,不能维持恒定的血药水平。注射剂和滴眼液也如此,首先迅速释药到周围组织,而后速度不断下降,持续数小时之久。这些剂型多剂量给药后虽能达到稳态血药浓度,但仍呈锯齿形变化。大多数药物的药理作用均与血药浓度有关,表示受体效应随药物浓度的增加而增强。如果血中药物浓度维持在治疗有效范围(C_(min)到C_(max))内,则治疗作用将能维持不变,是最为理想的给药方法。
As we all know, most of the drugs made into oral dosage forms, dissolution in the gastrointestinal tract are a first-order kinetic process, can not maintain a constant blood drug levels. The same is true for injectables and eye drops, which first release rapidly to the surrounding tissue and then decrease in speed for several hours. Although these dosage forms can reach steady-state plasma concentration after multiple-dose administration, they still show zigzag changes. Pharmacological effects of most drugs are related to plasma concentration, indicating that the receptor effect increases with increasing drug concentration. If the blood drug concentrations remain within the therapeutic range (C min min to C max), then the treatment will be able to maintain the same, is the most ideal method of administration.