Bioinfo Publications 217
DEVELOPMENT AND VALIDATION OF A STABILITY-INDICATIVE AGAR DIFFUSION ASSAY TO
DETERMINE THE POTENCY OF FLUCLOXACILLIN SODIUM IN CAPSULES
International Journal of Microbiology Research
ISSN: 0975-5276 & E-ISSN:0975-9174, Volume 4, Issue 4, 2012, pp.-217-222.
Available online at http://www.bioinfo.in/contents.php?id=27
FLÁVIA A.M. FIORENTINO* AND HÉRIDA R.N. SALGADO
Post Graduation Program in Pharmaceutical Sciences, School of Pharmaceutical Sciences, Univ. Estadual Paulista, Araraquara, SP, Brazil.
*Corresponding Author: Email- flafiorentino@ig.com.br
Received: May 17, 2012; Accepted: May 24, 2012
Abstract- Flucloxacillin sodium (FLU) is a semi-synthetic penicillin active against many gram-positive bacteria such as streptococci and
penicilinase-producing staphylococci, including methicillin-susceptible S. aureus. This study describes the development and validation of a
microbiological assay, applying the diffusion agar method for the determination of FLU, as well as the evaluation of the ability of the method
in determining the stability of FLU in capsules against acidic and basic hydrolysis, photolytic and oxidative degradations, using S. aureus
ATCC 25923 as micro-organism test and 3 x 3 parallel line assay design (three doses of the standard and three doses of the sample in each
plate), with six plates for each assay, according to the Brazilian Pharmacopoeia. The validation method showed good results including line-
arity, precision, accuracy, robustness and selectivity. The assay is based on the inhibitory effect of FLU using Staphylococcus aureus ATCC
25923. The results of the assay were treated by analysis of variance (ANOVA) and were found to be linear (r = 0.9997) in the range from 1.5
to 6.0 μg/mL, precise (repeatability: R.S.D. = 1.63 and intermediate precision: R.S.D. = 1.64) and accurate (98.96%). FLU solution (from the
capsules) exposed to direct UVC light (254 nm), alkaline and acid hydrolysis and hydrogen peroxide causing oxidation were used to evalu-
ate the specificity of the bioassay. Comparison of bioassay and liquid chromatography by ANOVA showed no difference between methodol-
ogies. The results demonstrated the validity of the proposed bioassay, which is a simple and useful alternative methodology for FLU deter-
mination in routine quality control.
Key words- Flucloxacillin, Bioassay, Penicillin, Pharmaceutical formulation, Quality control, Validation.
International Journal of Microbiology Research
ISSN: 0975-5276 & E-ISSN:0975-9174, Volume 4, Issue 4, 2012
Introduction
Flucloxacillin (FLU) is a semi-synthetic and penicillinase-stable
isoxazolyl penicillin active against many Gram-positive bacteria
such as hemolytic streptococci and penicillinase-producing staph-
ylococci, including methicillin-susceptible S. aureus (MSSA), but
not active against methicillin-resistant S. aureus. It acts by the
inhibition of transpeptidation, thus leading to the formation of a
weakened peptidoglycan. As autolysins continue to act, the cell
walls of Gram-positive organisms become progressively weaker,
and osmotic lysis takes place [1,2]. FLU is chemically known as
sodium (2S,5R,6R)-6-[[[3-(chloro-6-fluorophenyl)-5-methylisoxazol
-4-yl]carbonyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo
[3.2.0]hepatane - 2 carboxylate monohydrate [3-5]. FLU is used
for the treatment of skin, soft tissue and respiratory tract infections
as well as endocarditis and osteomyelitis caused by methicillin-
susceptible S. aureus [2]. The chemical structure of FLU sodium
is presented in (Fig. 1).
Fig. 1- Chemical structure of flucloxacillin sodium (CAS 1847-24-
1).
Citation: Flávia A.M. Fiorentino and Hérida R.N. Salgado (2012) Development and Validation of a Stability-Indicative Agar Diffusion Assay
to Determine the Potency of Flucloxacillin Sodium in Capsules. International Journal of Microbiology Research, ISSN: 0975-5276 & E-
ISSN:0975-9174, Volume 4, Issue 4, pp.-217-222.
Copyright: Copyright©2012 Flávia A.M. Fiorentino and Hérida R.N. Salgado. This is an open-access article distributed under the terms of
the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the origi-
nal author and source are credited.