Development of Binary and Ternary Complex of Cefuroxime Axetil With Cyclodextrin for Improving Pharmaceutical Characteristics

Abstract

Objective: The current research objective is systematic development and characterization of binary and ternary inclusion complexes of cefuroxime axetil with β-cyclodextrin to improve its pharmaceutical characteristics by using the kneading method.
 Methods: Phase solubility study was carried out using Higuchi and Connors method. Based on its result, binary complexes of cefuroxime axetil with different ratio of β-cyclodextrin were developed and characterized using differential scanning calorimeter (DSC), fourier transform infrared spectroscopy (FT-IR) and X-ray powder diffractometry (XRD). Then, binary complexes were analyzed for in vitro dissolution testing. The ternary complexes were developed using different ratio of PVP K-30 as a ternary component and evaluated for in vitro dissolution testing and in vitro taste masking.
 Results: Binary complex of cefuroxime axetil with β-cyclodextrin (1:1) showed better drug release than pure drug. During the development of the ternary complex, β-cyclodextrin (1:1) and 1% w/v PVP K-30 as a ternary agent resulted in an optimized ternary complex. The DSC, FT-IR and XRD studies clearly revealed the formation of binary and ternary complexes. The ternary complex showed better drug release of>85% within 30 min. in comparison to binary complex. The in vitro taste-masking study revealed the taste masking efficiency of the ternary complex of cefuroxime with β-cyclodextrin.
 Conclusion: The developed binary and ternary complex of cefuroxime axetil based on β-cyclodextrin with PVP K-30 showed improved in vitro dissolution rate and taste masking in comparison to pure drug. The drug release was better in ternary complexes. The present research work successfully shows the utility of binary and ternary complexes for improving pharmaceutical characteristics of cefuroxime axetil.

Review of Applications of Cyclodextrins as Taste-Masking Excipients for Pharmaceutical Purposes

“…PS, FTIR, DSC, PXRD, UV-VIS [50] Cefuroxime axetil HP-β-CD Ten human volunteers were used to assess the oral suspensions' flavors. The study employed the pure medicine cefuroxime axetil as the benchmark, and it also compared the formulations using a market sample.…”

Cyclodextrin Inclusion Complexes with Antibiotics and Antibacterial Agents as Drug-Delivery Systems—A Pharmaceutical Perspective

“…A similar attempt to include cefuroxime axetil in β-CD with and without L-arginine showed that the ternary system performed better than the binary system, offering much better solubility and dissolution rate than cefuroxime axetil alone [ 71 ]. The ternary system was also investigated as a combination of cefuroxime axetil, β-CD, and PVP K-30, and showed the best properties compared to the binary complex and the pure drug substance, with in vitro release tests >85% dissolution within 30 min [ 72 ].…”

Cyclodextrin Multicomponent Complexes: Pharmaceutical Applications

“…Moreover, TA showed that the kneaded product loses less mass, demonstrating that the product obtained by kneading is more stable [75] due to strong electrostatic interactions between PVP-K30 and MβCD, as shown in the IR spectrum. PVP-K30 was also used in a multicomponent complex with βCD and cefuroxime axetil, to improve the latter's pharmaceutical characteristics, via the kneading method [77]. Cefuroxime axetil is a prodrug of cefuroxime cephalosporin, which is used for pharyngitis, respiratory tract infections, acute bacterial otitis, simple skin infections and urinary tract infections.…”

“…It is a BCS class II drug, so it has less aqueous solubility with an oral bioavailability of 37% on an empty stomach, which increases to 52% if taken after meals. In this multicomponent complex of cefuroxime axetil with βCD, PVP-K30 can act as a ternary PVP-K30 was also used in a multicomponent complex with βCD and cefuroxime axetil, to improve the latter's pharmaceutical characteristics, via the kneading method [77]. Cefuroxime axetil is a prodrug of cefuroxime cephalosporin, which is used for pharyngitis, respiratory tract infections, acute bacterial otitis, simple skin infections and urinary tract infections.…”

“…PVP-K30 was also used in a multicomponent complex with βCD and cefuroxime axetil, to improve the latter’s pharmaceutical characteristics, via the kneading method [ 77 ]. Cefuroxime axetil is a prodrug of cefuroxime cephalosporin, which is used for pharyngitis, respiratory tract infections, acute bacterial otitis, simple skin infections and urinary tract infections.…”