Macrogol 15 Hydroxystearate

Category

Nonionic Surfactant; Solubilizing Agents; Stabilizing Agents

Molecular Formula

C20H40O4

Molecular Weight

344.53

Grade

Pharmceutical Excipients

Description

Macrogol 15 hydroxystearate is a yellowish-white, almost odorless waxy mass or paste at room temperature, which becomes liquid at approximately 30℃.

UNII

NA

Chemical Name

2-Hydroxyethyl-12-hydroxyoctadecanoate

CAS Number

70142-34-6

Synonyms

12-Hydroxyoctadecanoic acid polymer with a-hydro-o-hydroxypoly( oxy-1, 2-ethanediyl); 12-hydroxystearic acid polyethylene glycol copolymer; macrogoli 15 hydroxystearas; polyethylene glycol- 15-hydroxystearate; polyethylene glycol 660 12-hydroxystearate; Solutol HS 15

Stability and Storage Conditions

Macrogol 15 hydroxystearate has a high chemical stability. The prolonged action of heat may induce physical separation into a liquid and a solid phase after cooling, which can be reversed by subsequent homogenization. Macrogol 15 hydroxystearate is stable for at least 24 months if stored in unopened airtight containers at room temperature (maximum 25℃). Aqueous solutions of macrogol 15 hydroxystearate can be heat-sterilized (121℃, 0.21 MPa).The pH may drop slightly during heating, which should be taken into account. Separation into phases may also occur, but agitating the hot solution can reverse this. Aqueous solutions can be stabilized with the standard preservatives used in pharmaceuticals. Macrogol 15 hydroxystearate should be stored in tightly sealed containers in a dry place.

Source and Preparation

Macrogol 15 hydroxystearate is produced by reacting 15 moles of ethylene oxide with 1 mole of 12-hydroxystearic acid.

Applications

Macrogol 15 hydroxystearate is frequently used in preclinical testing of drugs, mainly for IV and other parenteral applications.

Safety

Macrogol 15 hydroxystearate is used in parenteral pharmaceutical preparations in concentrations up to 50% to solubilize diclofenac, propanidid, and vitamin K1. It has also been used in preclinical formulations in preparing supersaturated injectable formulations of water-insoluble molecules. It is generally regarded as a relatively nontoxic and nonirritant excipient. Macrogol 15 hydroxystearate is reported not to be mutagenic in bacteria, mammalian cell cultures and mammals. LD50 (dog, IV): >3.10 g/kg LD50 (mouse, IP): >0.0085 g/kg LD50 (mouse, IV): >3.16 g/kg LD50 (rabbit, IV): 1.0-1.4 g/kg LD50 (rat, oral): >20 g/kg LD50 (rat, IV): 1.0-1.47 g/kg