药科大生物药剂学课件第二三章 药物吸收.ppt

LOGO Polymorphs(多晶型) The drug exists in more than one of the crystalline form. They have identical chemical structure but have different physical properties such as hardness, melting point, solubility, dissolution rate. Crystalline forms (晶型) Polymorphs(多晶型) Amorphous(无定型) Solvates (溶剂化物) Amorphous(无定型) There are no stable appearance and apparent melting points, and a disorder in inner particles. Eg. chloramphenicol palmitate Crystalline forms (晶型) Polymorphs(多晶型) Amorphous(无定型) Solvates (溶剂化物) Solvates (溶剂化物) Some drugs interact with solvent to form a crystal called solvate (药物结晶时与溶媒形成的分子复合物) Hydrous and anhydrous Ionizable salt of drug（盐型） Generally, the ionizable salt of the drug is more water soluble than the free acid or free base. Dosage form Dosage form is a release system of drug. Absorption: for oral dosage form, Solutions Suspensions Powders Capsules Tablets Coated tablets Formulation Ingredients (处方成分) Excipients: the inactive components in a drug product and are often needed to produce a drug product with homogeneity（均一性） and stability（稳定性）。 Questions ? What are the two rate-limiting steps possible in the oral absorption of a solid drug product? Which one would apply to a soluble drug? Which one the pharmacist could alter? Give examples. ? What is the physiologic transport mechanism for the absorption of most drugs from the GI tract? What area of the GI tract is most favorable for the absorption of drugs? Why? ? What type of oral dosage form general yields the greatest amount of systemically available drug in the least amount of time? III. Oral cavity absorption 1. Anatomic and Physiologic Characteristics of oral mucosa Although surface area of oral cavity is limited, oral gingival(牙龈) and sublingual (舌下) mucosa are formed a large capillary network. The oral epithelium is essentially lipophilic, the intercellular space(细胞间隙)which is narrow and tortuous(弯曲的) is relatively hydrophilic