Drug administration excipients

Only the first three are discussed in any detail here. Most of these routes of administration place a drug directly or indirectly into systemic circulation. There are a number of these routes, however, by which the drug exerts a local effect, in which case most of the drug does not enter systemic circulation (e.g., intrathecal, intraventricular, intraocular, intraracistemal). Certain routes of administration may exert both local and systemic effects depending on the characteristics of the drug and excipients (e.g., subcutaneous). 

Parenterais The most important criterion for parenterals is that they have to be sterile for injection or infusion administration. Excipients are added to make parenterals isotonic with blood, improve solubility, and control pH of the solution. The solvent vehicles include water-for-injection, sterile sodium chloride, potassium chloride, or calcium chloride solution, and nonaqueous solvents such as alcohol, glycol, and glycerin. Preservatives, antioxidants, and stabilizers are normally added to enhance the properties of the drug product. 

Food and Drug Administration Perspective on Regulation of Pharmaceutical Excipients... 

Osterberg RE, See N. Toxicity of excipients—a Food and Drug Administration perspective. Int J Toxicol 2003 22 377-379. 

Abbreviations. FDA, Food and Drug Administration IPEC, International Pharmaceutical Excipients Council ADME, adsorption, distribution, metabolism, and excretion. 

U.S. Department of Health and Human Services. Guidance for Industry Nonclinical Studies for the Safety Evaluation of Pharmaceutical Excipients. Food and Drug Administration, May 2005. 

Guidance for Industry Nonclinical Studies for Development of Pharmaceutical Excipients. Food and Drug Administration 2005. 

The U.S. Food and Drug Administration (FDA) defines novel (new) pharmaceutical excipients as those substances used in the United States for the first time in a human drug product or by a new route of administration (1). The International Conference on Harmonization of Technical Requirements for Registration of Pharmaceuticals for Human Use (ICH) includes sections in its Common Technical Document (CTD) that details the information required for the approval of novel (new) excipients. Information on the control of excipients is included in Section P.4 of the CTD, and any additional information that may be required should be included in Appendix A.3 of the CTD. 

Pharmaceutical nonactive excipients have long been applied in a variety of pharmaceutical dosage forms to provide a wide range of functional characteristics that facilitate the optimal delivery of a drug to achieve the desired therapeutic effects. Pharmaceutical excipients are inert materials with no adverse effects on the safety and efficacy of therapeutic products. The Food and Drug Administration (FDA) website (1) provides a database listing all the FDA-approved nonactive pharmaceutical excipients. This provides formulation scientists a useful reference for efficient choices of the suitable excipients for the desired formulations of drug. 

The U.S. Food and Drug Administration. 2005. Guidance for industry nonclinical studies for the safety evaluation of pharmaceutical excipients, http //www.fda.gov/cder/ guidance/index.htm. Accessed August 18, 2007. 

One of the goals of the Food and Drug Administration (FDA) and the pharmaceutical industry is to be able to identify the active ingredients in tablets. It has been shown that the Raman spectra of excipients, gel capsules,... 

Powders intended for nasal administration have to be optimized in terms of particle size and morphology as these properties are related to potential irritation in the nasal cavity [23], Certain procedures (e.g., spray drying process) can modify the particle size of the drug powder raw material, but in order to optimize the morphology and flowability properties of some pure drug powders, excipients need to be used. Sacchetti et al. [28] reported that the use of mannitol as a filler and hydroxy-propylmethyl cellulose (HPMC) as a shaper of spray-dried caffeine microparticles modified the typical needle shape of spray-dried caffeine to a more convenient roundish shape. Further addition of polyethylene glycol (PEG) resulted in increased... 

Biopharmaceutic considerations in the design and manufacture of a drug product to deliver the active drug with the desired bioavailability characteristics include 1) the type of drug product (e.g., solution, suspension suppository) 2) the nature of the excipients in the drug product 3) the physicochemical properties of the drug molecule and 4) the route of drug administration. 

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