Excipients in pharmaceuticals

In addition to the information relating to excipients in the development pharmaceutics guidelines there are two guidelines that specifically address excipients in pharmaceutical products—3AQ9a (adopted February 1994) and EMEA/CVMP/004/98 Final (adopted February 1999). These expand on the information in the development pharmaceutics guidelines. 

Te Wierik, G. H. P, Bergsma, J., Arends, A. W., Boersma, T., Eissens, A. C., Lerk, C. F. (1996). A new generation of starch products as excipient in pharmaceutical tablets. I. Preparation and binding properties of high surface area potato starch products. Int. J. Pharm., 134,27-36. 

Kalinkova GN. Studies of beneficial interactions between active medicaments and excipients in pharmaceutical formulations. Int J Pharm 1999 187 1. 

Lucas P, Clarke MJ, Anderson K, Tobyn MJ, Staniforth JN. The role of fine particle excipients in pharmaceutical dry powder aerosols. Paper presented at Respiratory Drug Delivery VI, 1998. 

Pharmaceuticals. Lecithin and especially purified phosphatidylcholine can act as excipients in pharmaceutical (drug) formulation to enhance and control the Unavailability of the active component. Moreover, phosphatidylcholine can be utilized as a diedelic source, as it involved in the cholesterol metabolism and the metabolism of fats in the liver also, it can be utilized as a precursor of brain acetylcholine, as neurotransmiticr. 

For a very long time, scientists generally underestimated the importance of excipients in pharmaceutical dosage forms. Excipients were cheap ingredients viewed solely as inert supports for medicaments. Today, with modern pharmaceutical excipients on the shelf, development of various novel drug delivery systems, and production with high-speed tablet/capsule machines, excipients are rather more than the sugar in the pill.9,10... 

Research on nasal powder drug delivery has employed polymers such as starch, dextrans, polyacrylic acid derivatives (e.g., carbopol, polycarbophil), cellulose derivatives (microcrystalline cellulose, semicrystalline cellulose, hydroxypropylmethyl cellulose, hydroxypropyl cellulose, carboxymethyl cellulose), chitosan, sodium alginate, hyaluronans, and polyanhydrides such as poly(methyl vinyl ether-co-maleic anhydride) (PVM/MA). Many of these polymers have already been used as excipients in pharmaceutical formulations and are often referred to as first-generation bioadhesives [38-45], In nasal dry powder a single bioadhesive polymer or a... 

SEPIFILM 003 and 752 The association of cellulose with a film coating agent was originally patented by SEPPIC. Microcrystalline cellulose is probably one of the most extensively used excipients in pharmaceutical and nutritional products. Unlike other fillers, such as lactose, cellulose is inert, vegetable derived, and accepted worldwide and its shelf life is unlimited. Figure 31 shows the advantage of cellulose microcrystalline in film coating. 

When compressible and non-compressible excipients are mixed together, the adsorption of the non-compressible excipients onto the surface of the compressible excipients will reduce mixed powder compressibility. Lerk et al. and te Wierik et al. studied a new generation of starch products, which have a high surface area as excipients in pharmaceutical tablets, and confirmed that there is a positive relationship between the specific surface area and the binding capacity (i.e., compactibility). The surface area that takes part in the interparticle attraction is small, and only a minor fraction of the... 

Hypersensitivity reactions can occur due to the presence of contaminants or excipients in pharmaceutical dosage forms (e.g., outbreaks of eosinophilia-myalgia syndrome associated with oral tryptophan contaminants in various drugs). Another example is the anaphylactoid reactions to the surfactant Cremaophor EL, which is used in paclitaxel (Taxol). 

In the last 10 years, there has been great concern regarding the use of animal-derived excipients in pharmaceutical formulations. There is a possibility of contamination of an excipient by either an undetected virus [e.g., hepatitis C, human immunodeficiency virus (HIV)] or prion that may cause transmissible... 

Excipients in Pharmaceutical Dosage Forms The Challenge of the 21st Century Conference Proceedings Nice France, May 14—15, 1998. 

Altimaras, J. Nieto-Hernandez, T. Buitrago, F. Presence of excipients in pharmaceutical products in three sources of therapeutic information. Aten. Primaris. 1996, 18 (4), 190-193. 

Sulfobutylether-p-cyclodextiin (Captisol ) is one of newest excipients in pharmaceutical commercial formulations, is very safe, chemically stable, water-soluble, and is an excellent solubilizing drug delivery technology for molecules in which it forms an inclusion complex. An aqueous solution with 12%wt/v Captisol is isotonic, but formulations can contain as much as 30%wt/v Captisol. Ziprasidone mesylate, a rapid... 

Solubilization of Drugs in Aqueous Media / 3311 Solubilizing Excipients in Pharmaceutical Formulations / 3334 Spectroscopic Methods of Analysis Atomic Absorption and Emission Spectrophotometry / 3367... 

Chitosan is a polymer of glucosamine and A-acetyl-glucosamine, obtained from crustacean shells. It has been used to lower blood lipid concentrations, for body weight reduction (26), and as an excipient in pharmaceutical formulations. 

Mannitol is an osmotic diuretic that has been used in acute oliguric renal insufficiency, acute cerebral edema, and the short-term management of glaucoma, especially to reduce intraocular pressure before ophthalmic surgery. Other indications include promotion of the excretion of toxic substances by forced diuresis, bladder irrigation during transurethral resection of the prostate, and oral administration as an osmotic laxative for bowel preparation. Mannitol is used as a diluent and excipient in pharmaceutical formulations and as a bulk sweetener. 

Microcrystalline cellulose is not absorbed systemically following oral administration and thus has little toxic potential. Consumption of large quantities of cellulose may have a laxative effect, although this is unlikely to be a problem when cellulose is used as an excipient in pharmaceutical formulations. 

Disodium edetate is used widely in topical, oral, and parenteral pharmaceutical formulations it is used extensively in cosmetic and food products. Disodium edetate and edetate calcium disodium are used in a greater number and variety of pharmaceutical formulations than is edetic acid. Both disodium edetate and edetate calcium disodium are poorly absorbed from the gastrointestinal tract and are associated with few adverse effects when used as excipients in pharmaceutical formulations. 

Muldering KB. Placebo evaluation of selected sugar-based excipients in pharmaceutical and nutraceutical tableting. Pharm Technol 2000 24(5) 34, 36, 38, 40, 42, 44. 

Weiner AL. Lipid excipients in pharmaceutical dosage forms. In Swarbrick J, Boylan JC, eds. Encyclopaedia of Pharmaceutical Technology, 2nd edn, vol. 2. New York Marcel Dekker, 2002 1659-1673. 

Peanut oil is used as an excipient in pharmaceutical formulations primarily as a solvent for sustained-release intramuscular injections. It is also used as a vehicle for topical preparations and as a solvent for vitamins and hormones. In addition, it has been part of sustained-release bead formulations, nasal drug delivery systems, and controlled-release injectables. ... 

D Arcy PF. Adverse reactions to excipients in pharmaceutical formulations. In Florence AT, Salole EG, eds. Formulation Factors in Adverse Reactions. London Wright, 1990 1-22. 

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