TEROXIRONE

NSC - 296934

SMILES: O=C1N(CC2CO2)C(=O)N(CC3CO3)C(=O)N1CC4CO4

Chemical Name: 1,3,5-Tris(oxiranylmethyl)-1,3,5-triazine-2, 4, 6(1H,3H,5H)-trione

Other Names: Henkel's Compound; Triazinetrione triepoxide;
a-Triglycodyl isocyanurate; a-TGI, Teroxirone (USAN)

CAS Registry Number: 2451-62-9

Molecular Formula: C12H15N3O6     M.W.: 297.3

How Supplied: For injection, 100 mg, vial: supplied as a white
lyophilized powder with 200 mg of mannitol, USP, in a 20 mL
flint vial.

Solution Preparation: 100 mg/vial: When constituted with
10 mL of Sterile Water for Injection, USP, each milliliter contains
10 mg of teroxirone and 20 mg of mannitol, USP, at pH 6.0 to
8.0.

Storage: Store the intact vials under refrigeration.

Stability: Shelf-life surveillance of the intact vials is ongoing.
Intact vials are stable for at least 3 years at refrigeration
temperature (2-8 °C). Intact vials are unstable when stored at
elevated temperature (50 °C).

Solutions of teroxirone are most stable at around pH 6. A study
of teroxirone 5 mg/mL in various buffer systems over a pH range
of 3 to 9.7 at 25 °C yielded the following data at 4 and 24 hours:


Percent Of Teroxirone Remaining

ph 4 Hrs.† 24 Hrs.
---------------------------
3  89  49
5.5 †† 97  76
6.4 †† 97  79
7.5 †† 91  57
9.7 †† 92  49

The constituted solution of teroxirone exhibits approximately 2 to
5% decomposition in 4 hours at room temperature (22-25 °C).

Further dilution to a concentration of 0.1 mg/mL in 0.9% Sodium
Chloride Injection, USP, results in a solution exhibiting about 2%
decomposition in 2 hours and 8 to 10% in 4 hours at room
temperature (22-25 °C) or under refrigeration (2-8 °C).
Teroxirone is much less stable in 5% Dextrose Injection, USP,
exhibiting approximately 12% decomposition in 2 hours and 17%
in 4 hours.

At concentrations of 0.19, 1.0 and 2.4 mg/mL in 0.9% Sodium
Chloride Injection, USP, at 37 °C, teroxirone decomposes 10%
in 111, 126, and 162 minutes, respectively. After 4 hours at 37
°C, teroxirone losses of 21, 16, and 15% were observed at the
three concentrations, respectively.

Route of Administration: Intravenous