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sodium picosulfate

Names

[ CAS No. ]:
10040-45-6

[ Name ]:
sodium picosulfate

[Synonym ]:
Phenol, 4,4'-(2-pyridinylmethylene)bis-, bis(hydrogen sulfate) (ester), sodium salt (1:2)
sodium picosulfate
Picosulfate Sodium
sodium picosulphate
Phenol, 4,4'-(2-pyridinylmethylene)bis-, 1,1'-bis(hydrogen sulfate), sodium salt (1:2)
Disodium (2-pyridinylmethylene)di-4,1-phenylene disulfate
Sodium picosulfate anhydrous
Disodium (pyridin-2-ylmethylene)di-4,1-phenylene disulfate
4,4’-(2-pyridylmethylene)diphenyl bis(hydrogen sulfate) disodium salt
Picolax
(pyridin-2-ylmethylene)bis(4,1-phenylene) disodium bis(sulfate)
disodium,[4-[pyridin-2-yl-(4-sulfonatooxyphenyl)methyl]phenyl] sulfate
disodium (pyridin-2-ylmethanediyl)dibenzene-4,1-diyl disulfate
EINECS 233-120-9

Biological Activity

[Description]:

Sodium Picosulfate inhibits absorption of water and electrolytes, and increases their secretion.Target: OthersSodium Picosulfate displays cytotoxic effects on cultured liver cells. 800 and 1600 mg/mL induces dose-dependently vacuolic and fatty change as well as necrosis combined with a lowered mitotic activity and a slight increase in LDH values of the rapidly growing cultured liver cells of rabbit. Comparable but less severe effects are observed in 4-day old liver cell cultures of rat, while liver cells cultured for 6 to 11 days tolerate 1600 mg/mL Sodium Picosulfate. In human liver cultures the number of cells is slightly lowered at 800 and 1600 mg/mL and the number of nuclei in division is decreased dependent on dose [1]. Sodium Picosulphate has no major influence on ileal and colonic epithelial cell proliferation. In a 12 weeks study, 10 mg/kg Sodium Picosulphate continuously treatment does not influence the labeling index of Brdu (LI) in the ileum and induces no statistically significant increase of the LI when the treated groups are compared with the control group. The proliferative pattern along the crypts remains unchanged with sodium picosulphate treatment throughout the study [2]. Sodium Picosulphate does not induce chronic changes in colonic motility in rats under long-term treatment. 10mg/kg/day Sodium Picosulphate pretreated for 23 weeks does not induce any significant change in the duration of long spike bursts (LSB) which are associated with phasic contractions, or in LSB frequency in the fasted state or after a 3-gram meal [3].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Metabolic Disease

[References]

[1]. Nishikawa, J. and A. Kast, Toxicity study with sodium picosulfate in cultured liver cells of rabbit, rat and man. Arzneimittelforschung, 1981. 31(2): p. 321-5.

[2]. Geboes, K., et al., Effects of 'contact laxatives' on intestinal and colonic epithelial cell proliferation. Pharmacology, 1993. 47 Suppl 1: p. 187-95.

[3]. Fioramonti, J., C. Dupuy, and L. Bueno, In vivo motility of rat colon chronically pretreated with sennosides. Pharmacology, 1993. 47 Suppl 1: p. 155-61.


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Chemical & Physical Properties

[ Melting Point ]:
272 - 275ºC

[ Molecular Formula ]:
C18H13NNa2O8S2.H2O

[ Molecular Weight ]:
499.42

[ PSA ]:
162.51000

[ LogP ]:
4.10140

[ Storage condition ]:
Hygroscopic, Refrigerator, Under Inert Atmosphere

[ Water Solubility ]:
Freely soluble in water, slightly soluble in ethanol 96 per cent.

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
SM8720000
CHEMICAL NAME :
Phenol, 4,4'-(2-pyridylmethylene)bis-, bis(hydrogen sulfate), disodium salt
CAS REGISTRY NUMBER :
10040-45-6
LAST UPDATED :
199806
DATA ITEMS CITED :
18
MOLECULAR FORMULA :
C18-H13-N-O8-S2.2Na
MOLECULAR WEIGHT :
481.42
WISWESSER LINE NOTATION :
T6NJ BYR DOSWO&R DOSWO &-NA- 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
11300 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: -,993,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
3 gm/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory depression
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: 8,341,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
6980 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation Behavioral - coma Gastrointestinal - hypermotility, diarrhea
REFERENCE :
NAIZAM Nara Igaku Zasshi. Journal of the Nara Medical Association. (Nara Igakkai, c/o Narakenritsu Ika Daigaku, Shijo-cho, Kashihara, Nara-ken, Japan) V.1- 1950- Volume(issue)/page/year: 28,258,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1450 mg/kg
TOXIC EFFECTS :
Behavioral - ataxia
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: 8,341,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
14500 mg/kg
TOXIC EFFECTS :
Behavioral - ataxia Gastrointestinal - hypermotility, diarrhea Skin and Appendages - hair
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: 8,341,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
2900 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory stimulation
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: 8,341,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
6420 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Gastrointestinal - hypermotility, diarrhea
REFERENCE :
NAIZAM Nara Igaku Zasshi. Journal of the Nara Medical Association. (Nara Igakkai, c/o Narakenritsu Ika Daigaku, Shijo-cho, Kashihara, Nara-ken, Japan) V.1- 1950- Volume(issue)/page/year: 28,258,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1600 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory stimulation
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: 8,341,1977 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
3500 mg/kg/5W-I
TOXIC EFFECTS :
Cardiac - changes in heart weight Blood - changes in leukocyte (WBC) count Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
NAIZAM Nara Igaku Zasshi. Journal of the Nara Medical Association. (Nara Igakkai, c/o Narakenritsu Ika Daigaku, Shijo-cho, Kashihara, Nara-ken, Japan) V.1- 1950- Volume(issue)/page/year: 28(2),258,1977
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
225 gm/kg/30D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - other changes in urine composition Nutritional and Gross Metabolic - weight loss or decreased weight gain Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
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: 8,341,1977
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
182 mg/kg/26W-C
TOXIC EFFECTS :
Kidney, Ureter, Bladder - other changes in urine composition Kidney, Ureter, Bladder - changes in bladder weight Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
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: 8,341,1977 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
60 mg/kg
SEX/DURATION :
male 60 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Paternal Effects - other effects on male
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: 8,366,1977
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
6 gm/kg
SEX/DURATION :
female 9-14 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Newborn - stillbirth Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)
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: 8,366,1977
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
60 gm/kg
SEX/DURATION :
female 9-14 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - live birth index (measured after birth)
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: 8,366,1977
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
270 mg/kg
SEX/DURATION :
female 17-22 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
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: 8,366,1977
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
810 mg/kg
SEX/DURATION :
male 8 week(s) pre-mating female 14 day(s) pre-mating - 7 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
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: 8,366,1977
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
900 mg/kg
SEX/DURATION :
female 8-16 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
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: 8,366,1977
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
9 gm/kg
SEX/DURATION :
female 8-16 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 12,67,1976

Safety Information

[ HS Code ]:
2933399090

Customs

[ HS Code ]: 2933399090

[ Summary ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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