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目的:考察盐酸齐拉西酮固体分散体胶囊在比格犬体内的药动学过程,评价其生物等效性及吸收是否受食物影响。方法:通过建立盐酸齐拉西酮在比格犬血浆样品的RP-HPLC测定方法,以市售盐酸齐拉西酮胶囊(Zeldox)为参比制剂,对市售胶囊和自研胶囊进行空腹和饱腹下比格犬体内药动学研究。结果:建立了盐酸齐拉西酮比格犬血样测定方法,该方法处理简单,快速,准确。市售Zeldox胶囊和自研胶囊在饱腹Cmax为(243±82)和(124±62)ng·L-1,空腹下为(255±74)和(261±64)ng·L-1,AUC(0-24)分别为(3 798±374),(2 004±254),(3 943±336)和(3 912±331)ng·L-1·h。结论:自研盐酸齐拉西酮固体分散体胶囊空腹和饱腹下吸收均良好,吸收不受食物影响。经生物等效性评价分析可知,自研盐酸齐拉西酮固体分散体胶囊空腹和饱腹下与市售胶囊饱腹下等效。
OBJECTIVE: To investigate the pharmacokinetics of ziprasidone hydrochloride solid dispersions capsules in beagle dogs and to evaluate the bioequivalence and absorption of ziprasidone hydrochloride. Methods: By establishing the ziprasidone hydrochloride in Beagle dog plasma samples by RP-HPLC method, the commercial ziprasidone hydrochloride capsule (Zeldox) as reference preparation, commercially available capsules and self-made capsules for fasting and Pharmacokinetics of beagle dogs under fullness. Results: The determination method of ziprasidone hydrochloride beagle dogs was established. The method was simple, rapid and accurate. The Cmax of commercially available Zeldox capsules and self-made capsules were (243 ± 82) and (124 ± 62) ng · L-1, respectively, and were (255 ± 74) and (261 ± 64) ng · L- AUC (0-24) were (3 798 ± 374), (2 004 ± 254), (3 943 ± 336) and (3912 ± 331) ng · L -1 · h, respectively. CONCLUSIONS: Self-developed ziprasidone solid dispersion capsules are well-absorbed under fasting and fullness, and are not affected by food. Bioequivalence analysis showed that the self-developed ziprasidone solid dispersion capsules under fasting and fullness equivalent to the market under the fullness of the capsule.