Acta Scientific Pharmaceutical Sciences (ISSN: 2581-5423)
Volume 5 Issue 4 April 2021
Solubility Enhancement of Azithromycin by Solid Dispersion
Technique Using Mannitol and β-Cyclodextrin
Veer Patel
1
*, Rakesh Patel
2
, Hetansh Shah
1
, Shyam Purohit
1
, Mayur
Pawar
1
and Abuzar Pathan
1
1
Faculty of Pharmacy, Department of Bachelor of Pharmacy (B. Pharm), Parul
Institute of Pharmacy, Parul University, Vadodara, Gujarat, India
2
Faculty of Pharmacy, Department of Pharmaceutics, Parul Institute of Pharmacy,
Parul University, Vadodara, Gujarat, India
*Corresponding Author: Veer Patel, Bachelor of Pharmacy (B. Pharm), Parul
Institute of Pharmacy, Parul University, Vadodara, Gujarat, India.
Research Article
Received: March 02, 2021
Published: March 20, 2021
© All rights are reserved by Veer Patel., et al.
Abstract
Background: Azithromycin is a poorly water soluble drug having low solubility. Dissolution is the rate-limiting step in absorption of
such drugs. Therefore, solubility of such drugs need to be enhanced in order to have a stable and effective dosage form having greater
bioavailability. Solid dispersion technique is one of the effective methods to enhance the solubility of poorly soluble drugs.
Aim and Objectives: The present study aimed at enhancing the solubility of biopharmaceutical classification system Class II Drug,
i.e. Azithromycin using Mannitol and β-Cyclodextrin as a carrier.
Method: Solid dispersions of Azithromycin with Mannitol and β-Cyclodextrin were prepared by Melting, Kneading and Solvent Evap-
oration method. The solubility of these prepared dispersions was evaluated.
Results: Solubility of prepared dispersions of Azithromycin were reported in µg/mL. The solubility of solid dispersion which was
prepared using the Drug: Mannitol mixture in 1:4 ratio was found to be maximum, i.e. reported solubility of 7.8 µg/mL. The solubil-
ity of solid dispersion which was prepared using Drug: β-Cyclodextrin mixture in 1:1.5 ratio was found to be maximum, i.e. reported
solubility of 9.52 µg/mL. The solubility of those dispersions that were prepared using Melting and Kneading Method were found to
be maximum.
Conclusion: Drug having less aqueous solubility can have an enhanced rate of dissolution by using solid dispersion technique.
Keywords: Azithromycin; Solubility; Solid Dispersion; BCS (Biopharmaceutical Classification System); Absorbance
Abbreviations
BCS: Biopharmaceutical Classification System; HCL: Hydrochloric
Acid.
Introduction
Azithromycin, a macrolide antibiotic of the azalide subclass,
exerts its antibacterial action by binding to the 50s ribosomal
subunits of susceptible bacteria and suppressing protein syn-
thesis; however, it differs chemically from erythromycin in that a
methyl-substituted nitrogen atom is incorporated into the lactone
ring. Azithromycin is a white crystalline powder with a molecular
formula of C
38
H
72
N
2
O
12
and a molecular weight of 749.0 gm/mol.
Azithromycin is a broad spectrum antimicrobial agent with oral
Citation: Veer Patel., et al. “Solubility Enhancement of Azithromycin by Solid Dispersion Technique Using Mannitol and β-Cyclodextrin". Acta Scientific
Pharmaceutical Sciences 5.4 (2021): 48-54.