*Corresponding Author Address: Ana Carolina Kogawa, Faculdade de Ciências Farmacêuticas de Araraquara, UNESP, Rodovia
Araraquara-Jaú, km 1, CEP 14801-902, Araraquara, SP, Brazil.E-mail: ac_kogawa@yahoo.com.br
Journal of Pharmaceutical and Biological Sciences
ISSN: 2320-1924; CODEN: JPBSEV
Published by Atom and Cell Publishers © All Rights Reserved
Available online at: http://www.jpabs.org/
Original Article
Impact of rifaximin potency after treatment with different solvents
Ana Carolina Kogawa* and Hérida Regina Nunes Salgado
Department of Pharmaceutics, School of Pharmaceutical Sciences of Araraquara, Univ Estadual Paulista -
UNESP, Araraquara, São Paulo, Brazil
Received: 23-03-2017 / Revised Accepted: 24-04-2017 / Published: 26-04-2017
ABSTRACT
Rifaximin is an oral antibiotic used for the treatment of hepatic encephalopathy, ulcerative colitis, irritable
bowel syndrome, Clostridium difficile, travelers' diarrhea and acute diarrhea. Production of rifaximin involves
the use of different solvents. The performance of these solvents can affect the activity of this antimicrobial. The
general objective of this work is to show the importance in the rigorous production of rifaximin raw material.
The specific objectives of this work are to show that the use of different solvents or even a modification in the
process of obtaining the raw material can lead to different activities of powder. A purposeful change in the
process of obtaining the rifaximin raw material by recrystallization, using different solvents, resulted in
significant changes in antimicrobial activity. This is an alert to the production of pharmaceutical inputs. The
process of obtaining raw material must be standardized, aiming not only the quality of the medicine, but also,
aiming the consequences of the use of non-quality medicines that generate a vicious cycle in the public health
system.
Keywords: rifaximin, antibiotic, raw material, antimicrobial activity, quality.
INTRODUCTION
Rifaximin (Fig. 1) is a antimicrobial used for
thetreatment of hepatic encephalopathy, ulcerative
colitis, irritable bowel syndrome, Clostridium
difficile, travelers' diarrhea and acute diarrhea [1-
3].
Figure 1. Chemical structure of rifaximin (CAS
80621-81-4).
On the market, tablets of rifaximin in crystalline
form α are found, its systemic bioavailability is
limited and this is one of the advantages of the use
of this antimicrobial, which acts locally. The
amorphous form showed significantly higher
bioavailability and therefore lower tolerability [4].
The production of rifaximin involves the use of the
following solvents: purified water, ethyl alcohol,
chloroform, dichloromethane and ethyl acetate [5-
8].
Does the change in any of these solvents, the time
of exposure to them during the production of this
raw material or a small change in the process of
obtaining it can lead to differences in the activity of
this antimicrobial? This work shows the
importance of the rigorous production of the raw
material of rifaximin against the results of
antimicrobial activity obtained.
EXPERIMENTAL
Material: Rifaximin, form α, acquired of the
company NutraTech Development Limited
(China), was used.
Method: Rifaximin was solubilized in purified
water, ethyl alcohol, acetone, chloroform,
dichloromethane and ethyl acetate and re-obtained
by recrystallization. The materials obtained are
described in Table 1 [9].