Abstract
Bisantrene solubility and skin toxicity were studied in mice given intraperitoneal (IP) and intradermal (ID) drug respectively. Bisantrene (1 mg/ml) in 5% dextrose readily precipitated in the mouse peritoneum. The admixture of bisantrene into various lipophilic solvents did not reduce drug precipitation in vivo in the mouse or in vitro in human plasma at 37°C. Drug stability studies using high performance liquid chromatography (HPLC) showed markedly reduced bisantrene stability at alkaline pH. Bisantrene skin toxicity in BALB/c mice was characterized by ulceration which persisted for up to four months after ID injection. Skin toxicity was consistently reduced by dilute sodium bicarbonate injection into the bisantrene extravasation site. Three clinical extravasation cases treated with sodium bicarbonate showed no bisantrene ulceration. Ineffective local antidotes included sodium cromolyn, N-acetylcysteine, hydrocortisone, and heat (which appeared to increase toxicity).
| Original language | English (US) |
|---|---|
| Pages (from-to) | 351-357 |
| Number of pages | 7 |
| Journal | Investigational New Drugs |
| Volume | 2 |
| Issue number | 4 |
| DOIs | |
| State | Published - Dec 1984 |
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Keywords
- bisantrene solvability
- skin toxicity
ASJC Scopus subject areas
- Pharmacology
- Molecular Medicine
Cite this
Bisantrene solubility and skin toxicity studies : Efficacy of sodium bicarbonate as a local ulceration antidote. / Dorr, Robert T; Peng, Yei Mei; Alberts, David S.
In: Investigational New Drugs, Vol. 2, No. 4, 12.1984, p. 351-357.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Bisantrene solubility and skin toxicity studies
T2 - Efficacy of sodium bicarbonate as a local ulceration antidote
AU - Dorr, Robert T
AU - Peng, Yei Mei
AU - Alberts, David S
PY - 1984/12
Y1 - 1984/12
N2 - Bisantrene solubility and skin toxicity were studied in mice given intraperitoneal (IP) and intradermal (ID) drug respectively. Bisantrene (1 mg/ml) in 5% dextrose readily precipitated in the mouse peritoneum. The admixture of bisantrene into various lipophilic solvents did not reduce drug precipitation in vivo in the mouse or in vitro in human plasma at 37°C. Drug stability studies using high performance liquid chromatography (HPLC) showed markedly reduced bisantrene stability at alkaline pH. Bisantrene skin toxicity in BALB/c mice was characterized by ulceration which persisted for up to four months after ID injection. Skin toxicity was consistently reduced by dilute sodium bicarbonate injection into the bisantrene extravasation site. Three clinical extravasation cases treated with sodium bicarbonate showed no bisantrene ulceration. Ineffective local antidotes included sodium cromolyn, N-acetylcysteine, hydrocortisone, and heat (which appeared to increase toxicity).
AB - Bisantrene solubility and skin toxicity were studied in mice given intraperitoneal (IP) and intradermal (ID) drug respectively. Bisantrene (1 mg/ml) in 5% dextrose readily precipitated in the mouse peritoneum. The admixture of bisantrene into various lipophilic solvents did not reduce drug precipitation in vivo in the mouse or in vitro in human plasma at 37°C. Drug stability studies using high performance liquid chromatography (HPLC) showed markedly reduced bisantrene stability at alkaline pH. Bisantrene skin toxicity in BALB/c mice was characterized by ulceration which persisted for up to four months after ID injection. Skin toxicity was consistently reduced by dilute sodium bicarbonate injection into the bisantrene extravasation site. Three clinical extravasation cases treated with sodium bicarbonate showed no bisantrene ulceration. Ineffective local antidotes included sodium cromolyn, N-acetylcysteine, hydrocortisone, and heat (which appeared to increase toxicity).
KW - bisantrene solvability
KW - skin toxicity
UR - http://www.scopus.com/inward/record.url?scp=0021749290&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0021749290&partnerID=8YFLogxK
U2 - 10.1007/BF00171585
DO - 10.1007/BF00171585
M3 - Article
C2 - 6096286
AN - SCOPUS:0021749290
VL - 2
SP - 351
EP - 357
JO - Investigational New Drugs
JF - Investigational New Drugs
SN - 0167-6997
IS - 4
ER -