octreotide acetate

物化性质

外观与性状：

无色至灰白色冻干的固体

密度：

1.395 g/cm3

熔点：

153-156ºC

沸点：

1447.228ºC at 760 mmHg

闪点：

829.053ºC

存储条件/存储方法：

库房低温,通风,干燥,与食品原料分开存放

稳定性相关：

是迄今惟一成功地应用于治疗的胃肠激素类似物，是一个含有环状结构的合成八肽，部分氨基酸序列与生长抑素类似，具备生长抑素的几乎全部生物作用，如抑制多种垂体和胃肠胰激素释放，抑制胃酸、胰液和胆汁分泌，抑制胃肠道运动和分泌等，但半衰期为生长抑素的30倍。

安全信息

外观与性状：

无色至灰白色冻干的固体

密度：

1.395 g/cm3

熔点：

153-156ºC

沸点：

1447.228ºC at 760 mmHg

闪点：

829.053ºC

存储条件/存储方法：

库房低温,通风,干燥,与食品原料分开存放

稳定性相关：

是迄今惟一成功地应用于治疗的胃肠激素类似物，是一个含有环状结构的合成八肽，部分氨基酸序列与生长抑素类似，具备生长抑素的几乎全部生物作用，如抑制多种垂体和胃肠胰激素释放，抑制胃酸、胰液和胆汁分泌，抑制胃肠道运动和分泌等，但半衰期为生长抑素的30倍。

毒理性

CHEMICAL IDENTIFICATION

RTECS NUMBER :

HA1000000

CHEMICAL NAME :

L-Cysteinamide, D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophy l-L-lysyl-L-threonyl- N- (2-hydroxy-1-(hydroxymethyl)propyl)-, cyclic(2-7)-disulfide, (R-(R*,R*))-, acetate (salt)

CAS REGISTRY NUMBER :

79517-01-4

LAST UPDATED :

199709

DATA ITEMS CITED :

8

MOLECULAR FORMULA :

C49-H66-N10-O10-S2.2C2-H4-O2

MOLECULAR WEIGHT :

1139.49

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Human - man

DOSE/DURATION :

2587 ug/kg

TOXIC EFFECTS :

Gastrointestinal - changes in structure or function of endocrine pancreas Liver - liver function tests impaired

REFERENCE :

LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 348,1668,1996

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Human - man

DOSE/DURATION :

1429 ug/kg

TOXIC EFFECTS :

Gastrointestinal - changes in structure or function of endocrine pancreas Liver - liver function tests impaired

REFERENCE :

LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 348,1668,1996

TYPE OF TEST :

LD - Lethal dose

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

>50 mg/kg

TOXIC EFFECTS :

Skin and Appendages - dermatitis, allergic (after topical exposure) Skin and Appendages - hair

REFERENCE :

KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 21,5151,1987

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

18100 ug/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 22,967,1991

TYPE OF TEST :

LD - Lethal dose

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

>100 mg/kg

TOXIC EFFECTS :

Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - somnolence (general depressed activity) Behavioral - ataxia

REFERENCE :

KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 21,5151,1987

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

72300 ug/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 22,967,1991

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Mammal - dog

DOSE/DURATION :

>20 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,240,1990 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

18200 ug/kg/13W-C

TOXIC EFFECTS :

Kidney, Ureter, Bladder - other changes Blood - other changes Biochemical - Metabolism (Intermediary) - Plasma proteins not involving coagulation

REFERENCE :

KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 21,5151,1987