Experimental investigation of ternary mixture of diclofenac sodium with pharmaceutical excipients

The goal of this work was the study of drug-excipient interactions of ternary mixtures between diclofenac sodium when introduced with excipients commonly explored in solid dosage formulas such as microcrystalline cellulose and stearic acid obtained by three methods. Differential scanning calorimetry (DSC) (DSC), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), and the structural characterization technique of diffraction (XRPD) were used to investigate the characterization and potential physical and chemical interactions of solid products of diclofenac sodium with excipients prepared by different methods. This work revealed a possible interaction between diclofenac sodium, microcrystalline cellulose, and stearic acid in mixture prepared by microwave irradiation also; it was found compatibility for ternary mixtures prepared by physical mixture and co evaporation methods. Results of this study can be useful in the development of the method of preparation and select adequate excipients with suitable compatibility.

Formulation and Evaluation of Levocetirizine Dihydrochloride and Ambroxol Hydrochloride Lozenges

The present work aims to formulate and evaluate levocetirizine dihydrochloride and ambroxol hydrochloride hard candy lozenges to produce a slow-release of drugs for the management of cold and cough. The lozenges were prepared using sucrose, liquid glucose, hydroxyethylcellulose, and hydroxypropyl methylcellulose K4M by heating and congealing method. Sweetener with flavors was utilized to facade the bitter taste of the drug. The developed lozenges were exposed to various physical and chemical characters, and in vitro disintegration and dissolution. The developed formulations include hardness of 8 to 11 kg/cm², non-gritty, and agreeable mouthfeel. The optimized formula was examined for drug excipient interactions subjecting to Fourier transform infrared (FTIR) spectral analysis. Drug release for lozenges was highest in formulation FL8. The hard candy lozenges can present an attractive substitute formulation in allergic conditions.

Excipient Interactions in Glucagon Dry Powder Inhaler Formulation for Pulmonary Delivery

Purpose: This study describes the development and characterization of glucagon dry powder inhaler (DPI) formulation for pulmonary delivery. Lactose monohydrate, as a carrier, and L-leucine and magnesium stearate (MgSt) were used as dispersibility enhancers for this formulation. Methods: Using Fourier-transform infrared (FTIR) spectroscopy, Differential Scanning Calorimetry (DSC), and Raman confocal microscopy, the interactions between glucagon and all excipients were characterized. The fine particle fractions (FPFs) of glucagon in different formulations were determined by a twin stage impinger (TSI) using a 2.5% glucagon mixture, and the glucagon concentration was measured by a validated LC-MS/MS method. Results: The FPF of the glucagon was 6.4%, which increased six-fold from the formulations with excipients. The highest FPF (36%) was observed for the formulation containing MgSt and large carrier lactose. The FTIR, Raman, and DSC data showed remarkable physical interactions of glucagon with leucine and a minor interaction with lactose; however, there were no interactions with MgSt alone or mixed with lactose. Conclusion: Due to the interaction between L-leucine and glucagon, leucine was not a suitable excipient for glucagon formulation. In contrast, the use of lactose and MgSt could be considered to prepare an efficient DPI formulation for the pulmonary delivery of glucagon.