| Apatinib is a new oral micromolecular tyrosine kinase inhibitor,which is mainly used as the third-line treatment for chemotherapy-refractory advanced metastatic gastric cancer patients.However,apatinib has relatively serious side effects,and it is difficult to balance the clinical efficacy and adverse reactions,and off-label drug use often occurs in practical clinical application.The main contents of this paper are as follows:1.Quantification of the plasma concentration of apatinib may be an effective method to balance the clinical efficacy and adverse reactions.We conducted a study on the plasma concentration of apatinib and clinical practice.In this study,a simple,convenient,accurate and durable 2D-LC method was established and adequately verified as per the U.S.Food and Drug Administration(FDA)guidelines.Validation indicators and results include: selectivity,standard curve(15.27-1491.48 ng/mL),accuracy(Intra-day: 0.07%-2.23%;Inter-day: 0.19%-1.20%),precision(Intra-day: 1.97%-4.79%;Inter-day: 2.25%-10.22%),sensitivity(accuracy: 2.53%-4.14%;precision: 9.71%-11.51%),recovery(97.45%-108.92%),reproducibility(Intra-day: 0.11%-0.18%;Inter-day: 0.23%-0.46%),stability(Freeze/thaw: 0.72%-8.72%;short-term: 0.45%-4.61%;long-term: 0.59%-4.25%).The above data indicate that this method can be used in clinical pharmacokinetics and plasma concentration monitoring of apatinib.Blood concentrations were monitored in 19 patients taking apatinib using this method.The results showed that the blood concentration of apatinib had no correlation with patients' gender,age and BMI.The average blood concentration of 250 mg/qd,425 mg/qd and 500 mg/qd groups were 120.96 ng /mL,272.7ng /mL and 321.94 ng /mL,respectively.The blood concentration of apatinib varied greatly among patients,and the relationship between blood concentration and efficacy and adverse reactions should be further studied.2.The use of apatinib mesylate tablets in a third-class A oncology hospital from January 2017 to January 2019 was analyzed.The use of hospitalized patients could be divided into four aspects: basic conditions of patients,cancer types,drug regimens and dosage.The actual use of Apatinib will provide ideas and guidance for standardizing clinical rational drug use and prospective research.A total of 450 patients were enrolled by reviewing the medical records.The number of male patients(305 cases)was about twice that of female patients(145 cases).Age: the number of patients under 45 years old was 57,between 45 and 59 years old was 167,between 60 and 74 years old was 205,over 75 years old was 21.BMI: 51 patients were mild,247 patients were normal,116 patients were overweight,34 patients were obese,2 patients were very obese.KPS: 411 patients were non-dependence,37 were semi-dependent and 2 patients were dependent.The number of patients receiving surgical treatment was 219,but 231 patients were not.The number of patients receiving at least two kinds of systemic chemotherapy was 307,but 143 patients were not.Apatinib mesylate tablets are involved in the treatment of 35 types of cancers,including gastric cancer(164 cases)which is the most widely used it,followed by lung cancer,liver cancer and other cancers.There were 41 kinds of treatment schemes,including 284 cases of single drug targeting therapy and 102 cases of combination of two drugs,22 cases of combination of three drugs and 5 cases of combination of four drugs.The combination use of paclitaxel was the most frequent in 49 cases.There are 9 dosage forms of Apatinib Mesylate Tablets.The daily dosage ranges from 125 mg to 1500 mg.The results obtained from the above data are objective and true,which can be used for reference in prospective research and clinical practice. |
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