Excipients Used in Pharmaceutical Formulations
Dear readers I am back again and I do apology about my late posting due to my busy timetable in the lab. This time we will talk about pharmaceutical excipients, with special emphasis on its safety, as one of the major components in drug formulation. As we need to add many additives to have nice cooked meal with enjoyable taste reflecting the harmonization of our different components; it will be the same situation in drug formulation as we also need to add a lot of additive to enhance the performance of our dosage forms. Food poisoning could result from improper mixing or using of invalid components, and so the case in pharmaceutical formulation, using the wrong excipients in the wrong place may lead to serious pharmaceutical, pharmacological and toxicological problems.
Excipients defined as inert, safe and nontoxic compound could be added to the drug formula so as to enhance the pharmaceutical and pharmacological properties of our dosage form. Excipients can be classified either according to their function or according to the dosage forms had been added to. In general context with regard to solid dosage forms: diluents, fillers, disintegrating agents, lubricants, glidants, sweetening agent, coloring agent, flavoring agent, solubility enhancer, emulsifying agent, suspending agent, surface active agent, plasticizer, etc... The fact that excipients are inert substances have been changed with time since now some excipients have direct influence in dissolution rate and drug absorption. Furthermore some excipients had been found to encounter some activity regarding the facilitation of penetration inside the tumor cell. On the other hand some studies confirmed the doubts on presence of some side effects associated with presence of certain types of excipients, e.g. the presence of sucrose, lactose, parabens, and menthol are associated with diabetes mellitus, stomach cramps, hypersensitivity reaction, spasms of the larynx in infants, respectively. An important consideration on drug-excipients compatibility should be put in mind, since M. DouVsa, P. Gibala, J. Havl'iVcek, L. PlaVcek, M. Tkadlecov'a,J. BVrich'aVc they discovered that the phenylephrine in common cold formula had been subjected to degradation during pharmaceutical processes and only associated with those formulas containing saccharose.
The use of excipients in pediatric formulations is one of the most important challenges face the formulators. We can't consider children as the adults because they have special and unique needs. On the other hand the different anatomical and physiological features should be considered in formulating pediatric dosage forms which make the formulators puzzled between compatibility, stability and palatability of the formula. Cardiovascular, hepatotoxicity, respiratory and central nervous system toxic effects found to be associated with the use of a general solvent propylene glycol. Sucrose as sweetening agent in higher concentration can cause dental caries.
Hereby, we conclude that excipients should not consider any longer as inert compounds, but we should do an extra effort to investigate the possible hazardous effect of the excipients in order to have safe formulation practice.
1. Aulton, M.E. and J.W. Cooper, Pharmaceutics : the science of dosage form design. 2ed ed. 2003, Edinburgh ; New York: Churchill Livingstone. xv, 734 p.
2. Ursino, M.G., et al., Excipients in medicinal products used in gastroenterology as a possible cause of side effects. Regul Toxicol Pharmacol, 2011.
3. M. DouVsa, P., et al., Drug-excipient compatibility testing - identification and characterization of degradation products of phenylephrine in several pharmaceutical formulations against the common cold,. Drug-excipient compatibility testing - identification and characterization of degradation products of phenylephrine in several pharmaceutical formulations against the common cold,, 2011. In Press.
4. Fabiano, V., ChiaraMameli, and GianVincenzoZuccotti, Paediatric pharmacology:Remembertheexcipients. Pharmacol Res, 2011. In Press.
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