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The Pharma Innovation Journal 2016; 5(6): 05-13
ISSN: 2277- 7695
TPI 2016; 5(6): 05-13
© 2016 TPI
www.thepharmajournal.com
Received: 02-04-2016
Accepted: 03-05-2016
Pinki Rajbhar
Shambhunath Institute of
Pharmacy, Jhalwa, Allahabad,
U. P, India.
Atul K. Sahu
Shambhunath Institute of
Pharmacy, Jhalwa, Allahabad,
U. P, India.
S. S. Gautam
Shambhunath Institute of
Pharmacy, Jhalwa, Allahabad,
U. P, India.
Raj K. Prasad
Shambhunath Institute of
Pharmacy, Jhalwa, Allahabad,
U. P, India.
V. Singh
Shambhunath Institute of
Pharmacy, Jhalwa, Allahabad,
U. P, India.
S. K. Nair
Shambhunath Institute of
Pharmacy, Jhalwa, Allahabad,
U. P, India.
Correspondence
Pinki Rajbhar
Shambhunath Institute of
Pharmacy, Jhalwa, Allahabad,
U. P, India.
Formulation and Evaluation of Clarithromycin Co-
Crystals Tablets Dosage Forms to Enhance the
Bioavailability
Pinki Rajbhar, Atul K. Sahu, S. S. Gautam, Raj K. Prasad, V. Singh, S. K.
Nair
Abstract
Clarithromycin is a semi-synthetic macrolide antibiotic which inhibits bacterial protein synthesis by
binding to the bacterial 50S ribosomal subunit. In this work BCS Class II drug Clarithromycin is used as
a model drug, which is having poor solubility but high permeability. A pharmaceutical co-crystal is a
single crystalline solid that incorporates two neutral molecules, one being an active pharmaceutical
ingredient (API) and the other a co-crystal former. Co-crystals of Clarithromycin were prepared using co-
crystal former (urea), with method of preparation (solvent evaporation). In the present study,
Clarithromycin co-crystals tablets were prepared and evaluated in order to improve the dissolution by
enhancing the solubility of Clarithromycin using urea co crystals to improve the bioavailability. In this
work, the wet granulation method was attempted for formulation of conventional tablets of
Clarithromycin. The Clarithromycin tablets are available in 250mg- 500mg, doses in market. Dose of
250mg was selected for the present research work.
Keywords: Clarithromycin, Poor solubility, co-crystal, Tablet, Bioavailability etc.
Introduction
The poor solubility of drug is a major problem which limits the development of highly potent
pharmaceutics. The drugs with low solubility lead to low oral bioavailability and erratic
absorption which is particularly pertinent to drugs within class II of the Biopharmaceutical
Classification System (BCS). BCS Class II drug Clarithromycin is having poor solubility but
high permeability
1-4
. Therefore, one of the most challenging tasks in drug development is to
improve the drug solubility in order to enhance the bioavailability of these drugs. Several
strategies have been employed to overcome these limitations. The approaches to increase the
solubility and the available surface area for dissolution are classified as physical and chemical
modifications. Clarithromycin, Fig. 1, is a semi-synthetic macrolide antibiotic which inhibits
bacterial protein synthesis by binding to the bacterial 50s ribosomal subunit. In this work, the
wet granulation method was attempted for formulation and evaluation of conventional tablets
of Clarithromycin to improve the bioavailability
5-9
.
O
HO
H
3
C
CH
3
O
H
3
C
OH
OCH
3
CH
3
O
CH
3
CH
3
O
H
3
C O
O
O
CH
3
HO
H
3
CO
CH
3
H
3
C
OH
N(CH
3
)
2
Clarithromycin
Fig 1: Structure of Clarithromycin