Stability of amorphous azithromycin in a tablet formulation

MSc (Pharmaceutics), North-West University, Potchefstroom Campus, 2015It is a well-known fact that drugs can exist in different solid-state forms. These solid-state forms can be either crystalline or amorphous. Furthermore, significant differences are identified between the different solid-state forms of the same drug. Physico-chemical properties that are affected by the solid-state include: melting point, solubility, dissolution rate, stability, compressibility, processability, to name but a few. During the last two decades a significant amount of attention was directed towards the amorphous solid-state forms of drugs. The amorphous form is the direct opposite of the crystalline solid-state. While crystalline forms are constituted by unit cells arranged in a repetitive and structured nature, amorphous forms do not have a long-range order. This lack of order leads to an increase in the Gibbs free energy of such compounds which in turn leads to increased dissolution and solubility. The advantage of improved aqueous solubility and dissolution is a sought after characteristic within the pharmaceutical industry. Improved solubility ultimately could lead to improved bio-availability of a drug. In this study the amorphous nature and stability of amorphous azithromycin was studied. Although previous studies reported that amorphous azithromycin can be easily prepared, there is not a significant amount of data available on the stability of the amorphous form. Furthermore, the effect of milling, mixing, compression, handling and storage on the amorphous form was also investigated. This study showed that amorphous azithromycin remains stable during milling, mixing and compression. A compatibility study on azithromycin when mixed with tableting excipients showed some incompatibilities and this was helpful information to assist with the choice of excipients to be included in the tablet formulation. During the formulation study it became evident that good formulation strategies can greatly improve the flow properties of a drug. The stability of amorphous azithromycin was also studied. During this phase of the study an atypical stability indicating method was used in order to determine and demonstrate the stability of amorphous azithromycin. Dissolution studies were used to illustrate the stability of amorphous azithromycin due to the fact that dissolution is the only method that indicates the phenomena of solution-mediated phase transformation of an amorphous form to a stable crystalline form. During the stability study of six months at 40°C ± 75% RH no recrystallisation of the amorphous form to the crystalline form occurred. It was concluded that amorphous azithromycin will remain stable during processing steps, product formulation and manufacturing as well as during storage for a period of six months at elevated temperature and humidity.Master

Adsorption, Equilibrium Isotherm, and Thermodynamic Studies towards the Removal of Reactive Orange 16 Dye Using Cu(I)-Polyaninile Composite

To overcome some of the limitations of activated carbon like efficiency, cost-effectiveness, and reusability, the present work deals with Cu(I)-based polyaniline (PANI) composite for the removal of reactive orange 16 (RO16) dye. Following the synthesis and characterization of formed Cu(I)-PANI composite, the batch experiments performed for the removal of RO16 dye indicated that the composite has the capacity to reduce the coloring from RO16. The experiments were conducted for the study of effects against changes in pH, time, and dose at room temperature, where we observed for a pH impact on the dye adsorption capacity in the range of 2–12. Among all, the optimal RO16 removal was found to be 94.77% at a pH of 4 and in addition, the adsorption kinetics confirmed to be pseudo-second-order with more suitability towards the Langmuir isotherm, where it is presumed to be the formation of a monolayer of dye molecule at the homogeneous absorbent surface. The calculated maximum capacity, qm, determined from the Langmuir model was 392.156 mg/g. Further application of isotherms to attain thermodynamic parameters, a slight positive value of ΔS° for RO16 adsorption was observed, meaning that there is an increased randomness in the irregular pattern at the specific Cu(I)-PANI interface for an adsorption process. This mechanism plays an essential role in maintaining the effects of water pollution; and, based on the analysis therefore, it is prominent that the Cu(I)-PANI composite can be employed as a promising and economical adsorbent for the treatment of RO16 and other dye molecules from the sewage in wastewater

Exploration of the antibacterial capacity and ethanol sensing ability of Cu-TiO2 nanoparticles

Titanium oxide (TiO2) is one of the most scrutinized material because of its in-built fundamental properties and has been developed as an outstanding photo-catalytic material intended for many different industrial applications. In order to further explore the properties of TiO2, we prepared Copper-loaded TiO2 (Cu-TiO2) nanoparticles (NPs) for inhibiting the growth of bacterial cells and also to serve as a chemical sensor. The physico-chemical characteristics of the synthesized Cu-TiO2 NPs were characterized by many different techniques for the crystallinity, bonding and functionality, morphology, elemental composition, and absorption characteristics. From the results, we confirm for the formation of anatase phase of TiO2 having a tetragonal crystal system, while the morphology studies indicated that the Cu dope TiO2 has spherical morphology. The elemental analysis confirmed for the inclusion of Cu into TiO2 crystal lattice and the absorption spectroscopic analysis helped for the bandgap calculation and visible light absorption property of Cu-TiO2 NPs. The metal nanoclusters of Cu are observed to be deposited on different phases and sites of TiO2 resulting in the inter-band transitions. Further, the sensitivity of Cu-TiO2 as a chemical sensor is determined by fabricating the electrode at the FTO glass substrate where the ethanol sensitivity was found to be little increased/enhanced with Cu loading. Finally, the antibacterial activity of Cu-TiO2 NPs was confirmed by its activity against various bacterial cultures and are found to be efficient