Excipients Used in Pharmaceutical Formulations

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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
[1]. 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..
[1]. 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
[2]. 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
[2]. 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
[3].

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
[4].

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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Author: Ayman Waddad

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