A rapid, simple and single stereo selective high-performance liquid chromatographic (HPLC) method was developed and validated for enantiomers of palonosetron hydrochloride (PALO) and its process related chiral impurit...A rapid, simple and single stereo selective high-performance liquid chromatographic (HPLC) method was developed and validated for enantiomers of palonosetron hydrochloride (PALO) and its process related chiral impurities. A computer simulating software was used for the development of chiral method. The developed method was able to separate not only the enantiomers of palonosetron hydrochloride but also its process related chiral impurities within 12 min. The chromatographic separation was carried out by normal phase chromatography using a 3 μm column of cellulose based chiral stationary phase (Chiralcel-OD 250mm × 4.6mm) with a mobile phase comprised of n-hexane: ethanol: methanol: heptafluoro butyric acid: diethyl amine (70:15:15:0.05:0.1, v/v) at a flow rate of 1.0 mL/min. The effects of additive concentration as well as nature of polar organic modifier, flow rate, and temperature on enantioselectivity were investigated. The limit of detection (LOD) and limit of quantification (LOQ) of the palonosetron isomers and its related chiral impurities were found to be in the range 0.06-0.10 μg/mL and 0.14 - 0.24 μg/mL respectively. The method showed excellent linearity (R2 > 0.998) over a range of 0.14 to 1.125 μg/mL. The percentage recovery of the isomers in bulk drug samples ranged from 87.0 to 116.0.展开更多
Objective The aim of this study was to explore the clinical efficacy and toxicity of a combination aprepitant and palonosetron hydrochloride therapy in preventing chemotherapy-induced nausea and vomiting associated wi...Objective The aim of this study was to explore the clinical efficacy and toxicity of a combination aprepitant and palonosetron hydrochloride therapy in preventing chemotherapy-induced nausea and vomiting associated with a cisplatinum-based regimen in patients with lung cancer. Methods Sixty-eight patients with lung cancer were randomly assigned to receive either aprepitant plus palonosetron hydrochloride(group A, n = 38) or tropisetron(group B, n = 30). Acute(0–24 h) and delayed(2–5 d) emetic episodes, nausea, vomiting, constipation, and dizziness were compared between the two groups in the five days following cisplatinum-based chemotherapy.Results Group A had a higher complete control rate for both acute and delayed emetic episodes than Group B(36.8% vs. 13.3% and 31.6% vs. 13.3%, respectively; P < 0.05 for both). There was no significant difference in the constipation rate between the two groups. Conclusion Aprepitant combined with palonosetron hydrochloride is active and well tolerated in both acute and delayed emetic episodes in patients with lung cancer treated by a cisplatinum-based regimen.展开更多
文摘A rapid, simple and single stereo selective high-performance liquid chromatographic (HPLC) method was developed and validated for enantiomers of palonosetron hydrochloride (PALO) and its process related chiral impurities. A computer simulating software was used for the development of chiral method. The developed method was able to separate not only the enantiomers of palonosetron hydrochloride but also its process related chiral impurities within 12 min. The chromatographic separation was carried out by normal phase chromatography using a 3 μm column of cellulose based chiral stationary phase (Chiralcel-OD 250mm × 4.6mm) with a mobile phase comprised of n-hexane: ethanol: methanol: heptafluoro butyric acid: diethyl amine (70:15:15:0.05:0.1, v/v) at a flow rate of 1.0 mL/min. The effects of additive concentration as well as nature of polar organic modifier, flow rate, and temperature on enantioselectivity were investigated. The limit of detection (LOD) and limit of quantification (LOQ) of the palonosetron isomers and its related chiral impurities were found to be in the range 0.06-0.10 μg/mL and 0.14 - 0.24 μg/mL respectively. The method showed excellent linearity (R2 > 0.998) over a range of 0.14 to 1.125 μg/mL. The percentage recovery of the isomers in bulk drug samples ranged from 87.0 to 116.0.
文摘Objective The aim of this study was to explore the clinical efficacy and toxicity of a combination aprepitant and palonosetron hydrochloride therapy in preventing chemotherapy-induced nausea and vomiting associated with a cisplatinum-based regimen in patients with lung cancer. Methods Sixty-eight patients with lung cancer were randomly assigned to receive either aprepitant plus palonosetron hydrochloride(group A, n = 38) or tropisetron(group B, n = 30). Acute(0–24 h) and delayed(2–5 d) emetic episodes, nausea, vomiting, constipation, and dizziness were compared between the two groups in the five days following cisplatinum-based chemotherapy.Results Group A had a higher complete control rate for both acute and delayed emetic episodes than Group B(36.8% vs. 13.3% and 31.6% vs. 13.3%, respectively; P < 0.05 for both). There was no significant difference in the constipation rate between the two groups. Conclusion Aprepitant combined with palonosetron hydrochloride is active and well tolerated in both acute and delayed emetic episodes in patients with lung cancer treated by a cisplatinum-based regimen.
