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丁吡卡因

丁吡卡因用途

【用途一】
该品是一种安全有效的局部麻醉药，日本、英国、美国、德国均有生产。丁吡卡因盐酸对小白鼠（皮下给药）LD50为82±6mg/kg。家免持续静脉给药所致痉挛量（CD50）为0.18±0.02mg/kg/min。

丁吡卡因名称

[ CAS 号 ]:
2180-92-9

[ 中文名 ]:
丁吡卡因

[ 英文名 ]:
Bupivacaine

[中文别名 ]:

布比卡因

[英文别名 ]:

Bupivacaine
L-(-)-Bupivacaine
(-)-Bupivacaine
Levobupivacaine
MFCD00243007
EINECS 218-553-3
(S)-(-)-Bupivacaine
(S)-Bupivacaine
(RS)-bupivacaine

丁吡卡因物理化学性质

[ 密度 ]:
1.0±0.1 g/cm3

[ 沸点 ]:
423.4±45.0 °C at 760 mmHg

[ 分子式 ]:
C₁₈H₂₈N₂O

[ 分子量 ]:
288.428

[ 闪点 ]:
209.9±28.7 °C

[ 精确质量 ]:
288.220154

[ PSA ]:
32.34000

[ LogP ]:
3.64

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.547

[ 储存条件 ]:
库房通风低温干燥,与食品原料分开存放

丁吡卡因MSDS

详细MSDS(安全技术说明书)

丁吡卡因毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TK6060000

CHEMICAL NAME :: 2',6'-Pipecoloxylidide, 1-butyl-

CAS REGISTRY NUMBER :: 2180-92-9

LAST UPDATED :: 199612

DATA ITEMS CITED :: 11

MOLECULAR FORMULA :: C18-H28-N2-O

MOLECULAR WEIGHT :: 288.48

WISWESSER LINE NOTATION :: T6NTJ A4 BVMR B1 F1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human

DOSE/DURATION :: 4300 ug/kg

TOXIC EFFECTS :: Vascular - measurement of regional blood flow Behavioral - euphoria

REFERENCE :: AANEAB Acta Anaesthesiologica Scandinavica. (Munksgaard International Pub., POB 2148, DK-1016 Copenhagen K, Denmark) V.1- 1957- Volume(issue)/page/year: 21,521,1977

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 47 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #3632766

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 5600 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: APTOA6 Acta Pharmacologica et Toxicologica. (Copenhagen, Denmark) V.1-59, 1945-86. For publisher information, see PHTOEH Volume(issue)/page/year: 31,273,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 35 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #3632766

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 7100 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #3632766

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 1620 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: AACRAT Anesthesia and Analgesia (New York). (Elsevier Science Pub. Co., Inc., 52 Vanderbilt Ave., New York, NY 10017) V.36- 1957- Volume(issue)/page/year: 64,209,1985

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Parenteral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 64 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 26,78,1976

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intratracheal

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 12500 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 26,78,1976

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 36600 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #3632766 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intracervical

DOSE :: 500 ug/kg

SEX/DURATION :: female 39 week(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system

REFERENCE :: JPEMAO Journal of Perinatal Medicine. (Walter de Gruyter, Inc., 200 Saw Mill River Rd., Hawthorne, NY 10532) V.1- 1973- Volume(issue)/page/year: 12,75,1984

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraspinal

DOSE :: 2396 mg/kg

SEX/DURATION :: female 39 week(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - behavioral Reproductive - Effects on Newborn - other postnatal measures or effects

REFERENCE :: BJOGAS British Journal of Obstetrics and Gynaecology. (Blackwell Scientific Pub. Ltd., POB 88, Oxford, UK) V.82- 1975- Volume(issue)/page/year: 88,407,1981

丁吡卡因安全信息

[ 危害码 (欧洲) ]:
T+:Verytoxic;

[ 风险声明 (欧洲) ]:
R26/27/28;R38;R41

[ 安全声明 (欧洲) ]:
S22-S26-S36/37/39-S45

[ 危险品运输编码 ]:
2811

丁吡卡因制备

左布比卡因的制备：消旋的布比卡因和L-(+)-酒石酸溶于丙酮，在室温搅拌至固体全溶，加入右布比卡因酒石酸盐，搅拌至右布比卡因酒石酸盐完全沉淀出。过滤出固体，在滤液中加入左布比卡因酒石酸盐，搅拌使左布比卡因酒石酸盐沉淀析出。过滤出固体，往滤液中加入消旋的布比卡因，加入丙酮，搅拌至固体全
溶。加入右布比卡因酒石酸盐晶种，搅拌约7h，如此不断进行下去。每次得右布比卡因酒石酸盐和左布比卡因酒石酸盐。在搅拌下，将左布比卡因酒石酸盐溶于水，用浓氨水调节pH值。过滤、水洗、干燥至恒重，得粗左布比卡因，用热异丙醇重结晶，得纯左布比卡因。