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To establish a method for the quantification of aripiprazole in male SD rats muscle, and apply it to the research of drug residue at injection site in rats after administration of long-acting aripiprazole injection (LAI), and to compare the pharmacodynamics in mice.
An ultra-high performance liquid chromatography tandem mass spectroscopy (UPLC-MS/MS) assay was used to determine the concentration of aripiprazole in rats muscle. Sample pre-treatment: Muscle tissue was homogenized in a 30% acetonitrile solution containing 5% acetic acid, and then precipitated with 0.1% formic acid in acetonitrile for detection. Chromatography column: Waters HSS T3TM C18 column (2.1 mm×50.0 mm, 1.8 μm). Mobile phase: 5% acetonitrile and 95% acetonitrile both containing 0.1% formic acid. Flow rate: 0.6 mL·min-1. Injection volume: 5 μL. Mass spectrometry conditions: electrospray ion-source positive ions mode, multiple reaction monitor (MRM) scanning mode. After intramuscular administration of 25 mg·mL-1 aripiprazole microspheres for injection (MS) or long-acting aripiprazole for injection (brand name: Abilify Maintena®, AM), the drug residue in male SD rats was determined using an UPLC-MS/MS method. The hyperlocomotion model was established by acute administration of phencyclidine (PCP). And a comparative study was conducted on the efficacy of MS (40, 80, 240 mg·kg-1) and AM (80 mg·kg-1).
After 28 days of administration, the drug residue ratio of MS group was 6.27%-12.38%, while that of AM group was 23.31%. After 35 days of administration, the average drug residue ratios were 0.58%-2.94% and 10.28%-18.87%, respectively. Both the AM group and each dose (40, 80, 240 mg·kg-1) of MS group could inhibit the spontaneous movement of mice induced by PCP.
The inhibitory effect of Aripiprazole Microsphere for injection is comparable to that of Abilify Maintena on the spontaneous movement of mice caused by PCP. And there is a certain dose-response relationship for MS, while the drug residue at the injection site of MS is much lower than that of Abilify Maintena.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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