Study design: Single centre, single ascending dose study. Objectives: To compare the pharmacokinetics and assess the safety of capromorelin, a compound that has potential to treat constipation following spinal cord injury (SCI), in groups of able-bodied and SCI volunteers. Setting: Local population from Victoria, Australia. Methods: Following initial screening and baseline blood collections, participants received ascending oral doses (20, 50 and then 100 mg at least 1-week apart) of capromorelin after pre-dose blood collection, followed by blood collections over the following 12 h for pharmacokinetic analysis and 1-week and 4-week follow-up blood collections for safety evaluations. Blood pressure and heart rate were monitored. Results: No serious adverse events were recorded following any dose in either the able-bodied group or the SCI group. There were no abnormal blood pressure or heart rate changes. Minor adverse events resolved quickly without the need for treatment. Pharmacokinetic behaviour was broadly similar between groups, with both exhibiting dose-dependent increases in C max and AUC 0-∞ . The SCI participants showed greater variance in pharmacokinetic parameters and had a slightly delayed T max and half-life. Conclusion: Capromorelin at the doses tested was safe and well tolerated in both SCI and able-bodied participants and also showed similar pharmacokinetics with dose-dependent increases in concentration and drug exposure.
Background: Metaraminol 10 mg/mL injection is often diluted with sodium chloride 0.9% and pre-drawn into syringes by anaesthetists for use in the management of intraoperative hypotensive crisis. The 10 mg/mL ampoule presentation poses a significant safety hazard since the entire content needs to be drawn into a syringe and then diluted so that 0.5 mg doses may be administered. There have been incidents where 10 mg rather than the intended 0.5 mg have been administered to the patient. Additionally the pre-drawn metaraminol is discarded at the end of the case if not used, which results in significant wastage. A pre-filled syringe presentation of metaraminol will improve patient safety and reduce wastage. Aim: To determine the feasibility and stability of metaraminol 3 mg/6 mL pre-filled syringes. Method: Metaraminol 10 mg/mL injections were diluted with sodium chloride 0.9% and repacked into 3 mg/6 mL syringes. Syringes were stored at three different conditions: room temperature, refrigerated and frozen. Metaraminol syringes from each storage condition were analysed in triplicate, using a validated high performance liquid chromatography assay on Days 0,1,7,14, 28, 58, 91, 126, 161, 189, 252, 315 and 378. A 5% change limit was used to assess stability. Results: Metaraminol 3 mg/6 mL syringes were stable when analysed up to Day 378 with levels remaining at 95.4 +/− 0.4% of initial concentration for both room temperature and refrigerated storage. In the frozen storage arm, samples that were defrosted immediately and 7 days prior to sampling exceeded the 5% limit by day 315 and day 378, respectively. Conclusion: Metaraminol 3 mg/6 mL pre-filled syringes are stable for up to 378 days when stored at room temperature, or refrigerated and this presentation is feasible for use in the operating theatre.
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