Excipient definition

Excipients also meet the definition of component in the Good Manufacturing Practice (GMP) regulations in 21 CFR Section 210.3(b)(3) Component means any ingredient intended for use in the manufacture of a drug product, including those that may not appear in such drug product. ... 

Most drugs that are prescribed to us are formulated with active pharmaceutical ingredients and excipients. The formulations of selected drugs are presented in Exhibit 5.11. According to the US Pharmacopoeia and National Formulary definition, excipients are any component, other than the active substance(s), intentionally added to the formulation of a dosage form. There are many reasons for the addition of excipients ... 

In most instances the specimens will be self-evident (e.g., samples of blood, plasma, serum, urine, spinal fluid, aqueous humor, organs, tissues, and tissue fractions that are taken from a test system with the intention of performing an examination or analysis). In other instances the definition may not be as clear. For example, the assay plates used in the mammalian cell transformation assay and the mammalian point mutation assay are considered specimens even though they bear many of the attributes of a test system. For these assays, the originally plated cells plus media and excipients are the test system. After treatment with the test or... 

Thus, the impressive size of BASF s Fine Chemical Division is due to a BASF-specific definition of the term fine chemicals. In fact, the division, which is part of the business segment Agricultural Products Nutrition produces large volume aroma chemicals (a.o. 40,000 metric tons/year of citral) and vitamins (A, B2, C and E), as well as several lines of specialty chemicals (a.o. excipients and personal care products). Fine chemicals as defined in Section 1.1 account for about 150 million ( 190 million) in 2006, after full consolidation of the Swiss Fine Chemical company Orgamol, acquired in 2005. BASF holds a leading position in ibuprofen (made in USA), coffein and pseudoephedrin (made in Germany). BASF forecasts a further increase to 500 million ( 625 million) within 10 years which should make it the third largest fine-chemical company. 

The inactive ingredients are updated quarterly, by the fifth working day of April, July, October, and January. To search for the excipient, one can enter any portion of the name of an excipient, of at least three characters. Search results are displayed alphabetically, sorted first by ingredient, then by the route of administration and dosage form. Routes of administration and dosage forms are derived from current approved labeling. Refer to the IIG query search results column headers for data field definitions. 

This definition begins to capture the wide potential range of excipient usage in modern pharmaceutical products. It is, however, a long distance from recognizing the many potential uses of excipients to the development of a rational regulatory scheme that can facilitate market and regulatory acceptance of nontraditional... 

From 1975 to 1990, scientists at the University of Kansas utilized a rational synthetic design for the definition of a new excipient, the SBE derivative of P-CD (SBE7-P-CD CAPTISOL ). Designing renal safety into the CD was approached by introducing anionic substituents onto the CD structure. This approach capitalized on the increased water solubility that would be realized with the introduction of an ionic substituent. Higher intrinsic water solubility was expected to help minimize the potential precipitation of the CD, if concentrated in the kidney cell, and the charged substituent was expected to capitalize on the ability of the kidney to efficiently excrete ionic compounds into the urine, thus reducing residence time and exposure of the kidney cells to the CD. 

Currently, 29 excipient monographs have reached Stage 6 in the process and have been signed-off and accepted by the three pharmacopeias (Stage 6). To proceed to the next stage in the process, it was necessary for USP to create a new general chapter. The new chapter (1196), Pharmacopeial Harmonization, explains the role of the PDG, defines the PDG process, elaborates on the definitions of harmonized,... 

Excipients are those other materials used in formulation science. In short, excipients comprise everything in the formulation other than the API (1). IPEC-Americas and IPEC-Europe have developed a more detailed definition ... 

There are two main approaches to excipient compatibility screening isothermal studies at an elevated temperature and variable temperature studies in which the temperature is steadily increased, as in DSC. Both approaches are valid, but it is important to note, as has been stated above, that excipient compatibility testing is not a definitive test. We cannot state that an interaction will not take place, even though one may not have been found. We can only state which excipients to avoid because there is a very obvious interaction. A typical scheme is given in Figure 1 for a DSC-based excipient compatibility study. (There are other schemes that are used successfully.)... 

Figure 1 Increasingly complex drug-delivery systems erode definitive differentiation between drug and excipient. ...

When an excipient distributor is sourcing a material for a user for the first time or even for subsequent orders on a nonstock item, a key element of information that must be communicated to the user is the availability of the excipient and the time it will take between when an order is placed and when the excipient is actually delivered to the user site. The definition of availability can be variable, especially if the distributor happens to represent international excipient makers, who may have the material in stock overseas, requiring additional lead times of anywhere from two to eight weeks, depending on the service of the supplier and customs, and, now as a result of the Bioterrorism Act, FDA intervention with entry into the United States. 

One of the major obstacles to definitively examining the role of formulation components on enterocyte-based processes is the possible effect of excipient inclusion on other complicating factors. For example, the inclusion of lipids or surfactants in in vitro metabolic or transport screens runs the risk of affecting the thermodynamic activity of the drug in solution, thereby obscuring the role of metabolic and transport processes. Similarly, some surfactants and lipid-surfactant conjugates may cause transient increases in intestinal permeability as... 

Formulation Optimization. Formula optimization follows the selection of a formulation composition from the preliminary screening work. Formulation optimization focuses on determining the optimal level of each excipient to enable definition of a design space for each individual excipient. A proper DOE study is an effective and efficient way of defining the excipient levels and aiding in the selection of the optimal formulation. Factors in an optimization DOE study may include ... 

The hygroscopicity of a drug and pharmaceutical substances is a potential parameter to be considered in tablet formulation. The moisture uptake rate is quite variable depending on the type of drug and excipients as well as the environmental conditions. So, a concise definition of hygroscopicity is not possible. Powders can absorb moisture by both capillary imbibition and swelling. The instantaneous water absorption prosperties of pharmaceutical excipients correlate with total surface area while the total absorption capacity correlates with powder porosity [22],... 

According to this definition, impurities also include all excipients used to form the dmg formulation, giving it adequate consistency, stability, solubility, taste, and other factors. This brings us to an apparent contradiction with the existing definition of chemical impurity in pharmaceutical analysis and analysis of dmgs, all excipients are treated the same as the active substance. This means that they have to meet the same standards in terms of their purity, cannot contain impurities in quantities larger than that of the active substance, and have to meet other standards referring to the chemical structure, properties, and so on. 

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