Karim A
Angiology. 1983 Jan;34(1):11-22. doi: 10.1177/000331978303400102.
A recent important advance in biopharmaceutics has been the utilization of controlled delivery of drugs to the systemic circulation through the intact skin. With the conventional tablet and capsule dosage forms, the amount of drug absorbed through the gastrointestinal (GI) tract varies depending on the quantity and types of food in the stomach, on the GI motility and transit time. Acid and/or alkaline labile drugs may be deactivated prior to absorption from the GI tract while some drugs also get deactivated by GI microbial flora. In the case of drugs with a high hepatic extraction ratio, the absorbed drug may be largely deactivated by first-pass metabolism before reaching the systemic circulation. Drug absorption through the GI tract can therefore result in variable and/or unpredictable blood levels. Some of this variability can be minimized by administering controlled-release tablet or capsule formulations. However, these dosage forms cannot eliminate the inherent variability associated with first-pass metabolism.
生物制药学领域最近一项重要进展是通过完整皮肤实现药物向体循环的控释给药。对于传统的片剂和胶囊剂型,经胃肠道(GI)吸收的药物量会因胃内食物的量和类型、胃肠道蠕动及转运时间而有所不同。酸和/或碱敏感药物在从胃肠道吸收前可能会失活,而一些药物也会被胃肠道微生物菌群灭活。对于肝提取率高的药物,吸收的药物在到达体循环之前可能会因首过代谢而大量失活。因此,药物经胃肠道吸收会导致血药浓度变化不定和/或不可预测。通过服用控释片剂或胶囊制剂,可将其中一些变异性降至最低。然而,这些剂型无法消除与首过代谢相关的固有变异性。