摘要
目的比较卡铂（ＣＢＰ）瘤内注射（ｉｔ）与静脉注射（ｉｖ）对小鼠Ｓ１８０实体瘤的抑瘤作用、毒性和药代动力学。方法给荷瘤鼠ｉｔ或ｉｖＣＢＰ，用ＨＰＬＣ法测定血药浓度，并测定各组小鼠的瘤重、体重、脾指数和胸腺指数。结果相同剂量下，ｉｔ的血清ＣＢＰ浓度明显低于ｉｖ（Ｐ＜００５），３０和６０ｍｇ·ｋｇ－１ｉｔ与ｉｖ，Ｔ１／２分别为９３３、８８５、８００和８１２ｈ。与生理盐水组比较，ｉｔ与ｉｖＣＢＰ组的抑瘤率分别为２６２６％、４０９５％、２２１５％和３２１８％，脾指数分别减少２７１６％、４８２４％、４０１５％和５４３１％，胸腺指数分别减少８２５％、１５４６％、８２５％和２０６２％。生理盐水组、ｉｔ与ｉｖＣＢＰ组的体重增长率分别为７８％、－０４％、－５０％、－１３％和－９５％。结论ＣＢＰｉｔ有显著抗肿瘤作用，可降低血药浓度，减轻对免疫器官的抑制和毒性反应。
AIM To compare the antitumor effects, toxicity and
pharmacokinetics of carboplatin injected intratumorally and intravenously in mice with solid
S180 tumor. METHODS 30 and 60 mgkg-1 carboplatin were administered intratumorally or
intravenously every three day for 1 wk in mice with transplanted tumor. Serum levels of
carboplatin were determined by reversedphase HPLC. And the weights of tumor, the index of
spleen and thymusgland were measured. RESULTS The serum concentration of carboplatin in
mice treated with intratumoral injection was significantly lower than that in mice receiving
intravenous administration at the same dosage (P<005001). T1/2ke of serum carboplatin was
933(30 mgkg-1,it),885(60 mgkg-1,it), 800(30 mgkg-1,iv) and 812(60 mgkg-1,iv) hours,
respectively. Compared with normal saline (NS) group, the growth of tumor in 30 and 60
mgkg-1(it or iv) carboplatintreated groups was all inhibited, with inhibitory rates of
2626%,4095%,2215% and 3218%,respectively. And the indexes of spleen were decreased by
2716%, 4824%,4015% and 5431%. The reductions of indexes of thymusgland were at rates of
825%,1546%,825% and 2062%,respectively. In addition, the average mouse weight increased
by 78%, while those in carboplatintreated groups decreased by 04%,50%,13% and 95%.
CONCLUSION Carboplatin showed significant antitumor effects when injected intratumorally.
And compared with those in animals receiving intravenous administration, the serum
carboplatin concentrations in mice treated with intratumoral injection were significantly
decreased, while the suppression of immune organs and toxicity was relatively mild.
出处
《中国药理学通报》
CAS
CSCD
北大核心
1999年第2期160-163,共4页
Chinese Pharmacological Bulletin
基金
山东省科委资助
关键词
卡铂
瘤内注射
静脉注射
抗肿瘤作用
毒性
药代动力学
carboplatin
intratumor injection
intravenous injection
antitumor effect
toxicity
pharmacokinetics
