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药品中口服剂所占的比例最大,因为许多药物可以通过简便的口服给药取得充分疗效。另外,由于胃酸等消化液导致分解,胃肠粘膜或肝脏的第一关卡效应所致非活化等原因,使经口给药发生困难的药物及从制剂上想办法或应用某些措施后经口给药的也不少。另外,最近人们注意利“给药部位”的研究,即不需经过复杂的过程,直接把药物送入体循环的方法。并且,正集中精力研究经皮肤或消化道以外的各种粘膜给药的吸收机理。由于经口腔粘膜吸收的药物,不经过肝脏,而直接进入体循环,对易受第一关卡效应影响的药物,口腔粘膜被视为有效的给药途径。尽管舌下给药是经口腔粘膜的主要方法,但使用的药物仅有硝酸甘油等少数药,因为口腔粘膜的主要功能是“屏障”作用,并不是易于通透的组织请参看表1。
Oral drugs account for the largest proportion of drugs, because many drugs can be easily obtained by oral administration to achieve full effect. In addition, due to gastric acid and other digestive juices lead to decomposition, gastrointestinal mucosa or liver caused by the first hurdle due to non-activation and other reasons, to make oral administration difficult drugs and from the formulations to find ways or after the application of certain measures by mouth A lot of medication. In addition, attention has recently been paid to the study of “drug delivery sites,” a method of directly delivering drugs into the systemic circulation without going through a complicated process. In addition, attention is being focused on the absorption mechanism of various mucosal administrations beyond the skin or the digestive tract. Due to oral mucosal absorption of drugs, without the liver, and directly into the systemic circulation, susceptible to the first barrier effect of drugs, oral mucosa is considered an effective route of administration. Although sublingual administration is the primary method of oral mucosa, the drug used is only a small number of drugs such as nitroglycerin, because the main function of the oral mucosa is a “barrier” and not easily permeable tissue see Table 1.