An oral scabicide, STROMECTOL ® Tablets (ivermectin) is often administered to patients as a simple suspension by feeding tube. However, it was reported that the administration by this method was less effective than oral administration of tablets. One reason for this lower efficacy might be that the devices and technique for this method of administration are not appropriate. The aim of this study is to propose an appropriate technique. In this report, we compare the recovery ratio when a simple suspension is pushed through a syringe under various conditions. As a result of washing the syringe with distilled water after the first use, the recovery of ivermectin was higher than that without washing. The recovery of ivermectin from syringes set at an angle of 90° and 45° to the horizon was significantly higher than that at 0° and-45°. And recovery from previously used syringes was about 10% higher than that from new syringes (p<0.05). Furthermore, after having orally administered STROMECTOL ® Tablets and gavaged its suspension with an appropriate delivery technique to rabbits, we measured the ivermectin concentrations in plasma by LC-MS/MS. The AUC0-192h of ivermectin was almost equivalent for both methods of administration. In conclusion, to secure the same dosage of administration with a simple suspension as that of tablets, it is highly recommended to employ a previously used syringe at an angle of over 45°, and to inject by a technique that washes out the entire residue in the syringe after first injection.
Fixed dose combination tablets consisting of mirabegron (MB) and solifenacin succinate (SS) were developed and formulated into bilayer tablets in the current study. The results of a chemical stability study showed that the original formulation for the tablets led to a significant increase of unknown degradants in the SS layer. Two compatibility studies were conducted to simulate the interface between the MB and SS layers, and the results revealed that the degradants only formed in the presence of both active pharmaceutical ingredients (APIs), and that the presence of maltose in the SS layer was critical to inducing degradation. High resolution mass spectroscopy coupled with high performance liquid chromatography was used to determine the chemical structures of the degradants, which were identified to MB derivatives bearing one or two sugar units. These findings therefore suggested that the degradation of the API could be attributed to the addition of sugar units from maltose to MB under the acidic conditions caused by SS. With this in mind, we developed a new formulation by replacing maltose with hydroxypropyl cellulose as a polymer-type binder. The results showed that this formulation suppressed the formation of the degradants. The results of this study have shown that chemical degradation can occur at the interface of bilayer tablets and that an alternative strategy is available to formulate more stable MB/SS bilayer tablets.
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