Excipient, examples

Companies that manufacture food additives will often also produce an excipient grade. Many excipients first found application in processed foods where their demonstrated safety has made them attractive for use as pharmaceutical excipients. Examples of food additives also used in drug products include artificial sweeteners, antioxidants, and inorganic salts. 

Change in the technical grade of an excipient. (Example Avicel PH102 vs. Avicel PH200.)... 

Components and composition—release controlling excipient Example Changes in release controlling ex-... 

The final marketed form of a drug is called a drug product. A drug product includes not only the drug itself but also various components called excipients. Examples of excipients... 

Eorensic science laboratories may have different missions and therefore conduct different types of testing on samples (21,22). Eor example, the United States Department of Justice, Dmg Enforcement Administration (DEA) forensic laboratories assist authorities ia criminal intelligence-gathering efforts. As such, DEA chemists routinely analyze both the iUicit dmg and excipient, the material used ia the cutting or diluting of the pure dmg, ia a given specimen. The excipient may provide information as to where the sample was produced. 

The second example is the SE-HPLC analysis of recombinant hGH. In this example, SE-HPLC is used for both a purity and a protein concentration method for bulk and formulated finished products. This method selectively separates both low molecular weight excipient materials and high molecular weight dimer and aggregate forms of hGH from monomeric hGH, as shown... 

Analytical methods and specifications must be established and validated so as to define and control the quality and purity of the raw materials, intermediates and the finished product. For many standard chemical raw materials, the development of specifications will not be necessary as they are already published in US and European pharmacopoeia (for example, standards for water, organic solvents and various excipients). The ultimate objective of these activities is to be able to manufacture the drugs required for clinical trials in accordance with good manufacturing practice (GMP). 

Regulatory agencies currently set stringent standards on the quantities of nucleic acids allowed in recombinant biological products. In the pharmaceutical industry these requirements necessitate the quantification of trace amounts of nucleic acids in the presence of large quantities of protein and other excipients. Flourescence methods offer advantages for such analyses, but also have limitations. The use of a variety of fluorescent dyes and techniques is described here, and practical examples of such use are presented. 

For thousands of years, nature has provided humankind with a large variety of materials for the most diversified applications for its survival, such as food, energy, medicinal products, protection and defense tools, and others. The pharmaceutical industry has benefitted from such diversity of biomaterials and has exploited the use of natural products as sources of both drugs and excipients. One example of a promising biomaterial for pharmaceutical use is xylan, a hemicellulose largely found in nature, being considered the second most abundant polysaccharide after cellulose. 

Because of the nature of modern pharmaceutical systems, formulators have made more complete investigations of the materials they use. This interest has identified several materials that may have more than one use in tableted systems. The type of effect that an excipient will produce is often dependent upon the concentration in which it is used. For example, Table 5 lists some multiuse excipients and the corresponding concentration ranges required for their various applications. 

Often these design criteria involve competitive requirements. What is best for meeting one criterion may be counterproductive in meeting another. For example, certain excipients such as the hydrophobic stearate lubricants are important for efficient manufacture, yet they have the potential to retard the release of drug from an immediate-release formulation. The design of a dosage form thus frequently requires the optimization of formulation and process variables in a way that best meets all design criteria. 

Some of the most commonly used added substances are listed in Table 2. Pharmacists involved in IV admixture programs must be aware of the types of additives that may be present in the products being combined, since the source of incompatibility between different drugs mixed in solution may be the excipients present. For example, drug formulations containing... 

The incorporation of certain excipients in products is deemed to be undesirable. Examples are the inclusion of mercurial preservatives, the inclusion of benzyl alcohol in parenteral products for use in children, the use of benzoic acid esters in injections, and the inclusion of sulfites and metabisulfites in products in general. If it is intended to use any of these materials, then a full justification will be required. 

A variety of approaches exist for stabilizing proteins, for example, chemical modification, immobilization, and site-directed mutagenesis [95,96], but these techniques are not within the scope of this chapter. The focus here will be on stabilization of proteins via formulation development. The principal formulation strategy is to stabilize the protein using clinically acceptable additives (excipients) or through the use of suitable pharmaceutical-processing technologies. 

Another excipient used in feed additive premixes is a diluent used to dilute or standardize activity. Diluents are similar in composition to grain carriers, except the particle size is generally smaller. No attempt is made to absorb the active drug to the individual particles of the diluents. If a liquid is used it is mainly for dust control. A diluent is considered for use when the level of the active ingredient components in the premix approaches or exceeds 50% of the product or when two or more active components vary greatly from one another in density [13]. Examples of diluent materials are ground limestone, sodium sulfate, kaolin, corn cob flour, and ground oyster shells. 

Absorbents are another class of excipient material used in feed additive premixes. They are used when the drug substance is a liquid or is readily soluble in water, oil, or some other solvent. The liquid is sprayed onto the absorbent in a mixer as the mixer is running. Examples of absorbents are vermiculite, Fullers earth, corn cob fractions, and clay. 

Numerous other examples of the use of solubility to control the delivery profile of drugs from the elementary osmotic pump can be found in the literature, especially the patent literature [35-40], These systems apply to drugs of moderate to high aqueous solubility where either the excipient or the salt form of the drug was used to control the drug solubility within the core formulation. 

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