Formulation, Physical Stability, and the Clinical Effectiveness of Extemporaneous Ivermectin Oral Solution.

Ivermectin is a gamma amino butyric acid (GABA)-gated-Cl-channels modulator, which has been used orally in the treatment of numerous parasitic infections. The study target was to set up a stable, efficient 0.2% w/v ivermectin solution, which would be achieved from pure ivermectin powder as a source of the active pharmaceutical ingredient. Several trial solutions were prepared. The most fitting solution, with respect to its organoleptic properties, was chosen for additional investigation, including the solution's physical stability. Two storage conditions, room temperature (25°C, 60% relative humidity) and accelerated stability chambers (40°C, 75% relative humidity) were subjected to guarantee the physical stability of the solution through the 3-month study period. Furthermore, other quality tests were assessed, (e.g., pH, assay, organoleptic properties, microbial contamination) for the same latter period. Quantification of ivermectin was validated utilizing a high-performance liquid chromatography analytical method. The adopted solution showed accepted organoleptic properties. The pH of the solutions was approximately 5 and remained unchanged during the stability study. The mean percent of remained ivermectin solution was close to 97% ± 0.2 at room temperature. Ivermectin solution was additionally tested for microbial contamination, and it was free from any microbial contamination (E. coli bacteria: Negative/mL, yeast and molds count: <10 cfu/mL and aerobic microbial count results in <10 cfu/mL). The adopted formula showed the best physical stability within at least the three months of storage at both room and accelerated conditions. Ivermectin solution was successfully prepared from its pure powder. This formula provides a stable, efficient oral solution for those who suffer from swallowing difficulties or patients in the intensive care unit who cannot receive the medication in a solid dosage form. Using the suggested formula, community and hospital pharmacists could prepare an effective, high quality ivermectin oral solution using pure ivermectin powder.

Weight and content uniformity of lorazepam half-tablets: A study of correlation of a low drug content product.

The aim of this study was to investigate the degree of correlation between the weight and the content of spilt-halves of lorazepam 2.5 mg tablets. Weight variation and drug content of lorazepam half-tablets were evaluated according to the European Pharmacopoeia tests. Only one individual mass of the 30 half tablets was outside the limits of 85-115% of the average mass, but since it was within 75-125% of the average mass, the product passed the test. Each individual content was between 85% and 115% of the average content (99.8% expressed as a percent to label claim) and within the limits of 75-125%, so the product passed the uniformity of content test. The correlation coefficient (r) between the weight and the content of split halves was found to be 0.994. The weights of split tablet halves appear to be directly correlated with their drug content even for a medication with a low drug content, thus it is recommended that pharmacists who split tablets into two halves, assure the weight uniformity of the resultant halves. Manufacturers should develop formulation and manufacturing procedures that ensure high degree of correlation between weight and content not only among the whole tablet but also among the obtained tablet halves.