addedsubstance教程.pptVIP

* Added substances and vehicles in parenteral formulations 1.Active Drug Substance (Active pharmaceutical ingredient - API) Chemical compound with pharmacological effect (or other direct effect ) intended for use in diagnosis, treatment or prophylaxis of diseases. International non-proprietary names (INN, generic names) Direct clinical use of the active drug substances as they are is rare due to a number of good reasons: API handling can be difficult or impossible (e.g., low mg and ?g doses) Accurate drug dosing can be difficult or impossible API administration can be impractical, unfeasible or not according to the therapeutic aims Some API can benefit from reducing the exposure to the environmental factors (light, moisture…), or they need to be chemically stabilized due to the inherent chemical instability API can be degraded at the site of administration (e.g., low pH in stomach) API may cause local irritations or injury when they are present at high concentrations at the site of administration or absorption API can have unpleasant organoleptic qualities (taste, smell – compliance!) Administration of active substance would mean to have no chance for modification (improvement) of its PK profile 2.Excipients An excipient is an inactive substance used as a carrier for the active ingredients of a medication. The selection of suitable excipients and the proportions used will be determined on the basis of the desired route of administration, the dose, the physicochemical property of the active and the proposed method of manufacture for the product. 3. Excipients in parenteral formulations antioxidants(抗氧化剂) these antioxidants maintain product stability by being preferentially oxidized and gradually consumed over the shelf life of the products ascorbic acid(抗坏血酸)，cysteine(半胱氨酸),sodium sulfite(亚硫酸钠)，monothioglycerol(硫代甘油) antimicrobial agents(抗菌剂) to prevent growth of any microorganisms。 A suitable preservative system is required in all