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Chlorobutanol, or chlorbutol, is an alcohol-based preservative with no surfactant activity . It also elicits sedative-hypnotic and weak local anesthetic actions in addition to antibacterial and antifungal properties. Similar in nature to chloral hydrate, it is formed by the simple nucleophilic addition of chloroform and acetone. As a long-term stabilizer of multi-ingredient preparations, chlorobutanol is normally used at a concentration of 0.5%. At this concentration, it also conserves its antimicrobial activity. Due to the long terminal half-life of 37 days, the use of chlorobutanol as a sedative is limited because of the considerable accumulation which will occur following multiple dosing . Chlorobutanol is a common detergent preservative in eye drops and other ophthalmic therapeutic formulations .
Chlorobutanol, or chlorbutol, is an alcohol-based preservative with no surfactant activity . It also elicits sedative-hypnotic and weak local anesthetic actions in addition to antibacterial and antifungal properties. Similar in nature to chloral hydrate, it is formed by the simple nucleophilic addition of chloroform and acetone. As a long-term stabilizer of multi-ingredient preparations, chlorobutanol is normally used at a concentration of 0.5%. At this concentration, it also conserves its antimicrobial activity. Due to the long terminal half-life of 37 days, the use of chlorobutanol as a sedative is limited because of the considerable accumulation which will occur following multiple dosing . Chlorobutanol is a common detergent preservative in eye drops and other ophthalmic therapeutic formulations .
As a detergent, chlorobutanol disrupts the lipid structure of the cell membrane and increases the cell permeability, leading to cell lysis . It induces conjunctival and corneal cell toxicity via causing cell retraction and cessation of normal cytokines, cell movement, and mitotic activity . It disrupts the barrier and transport properties of the corneal epithelium as well as inhibits the utilization of oxygen by the cornea . Chlorobutanol also inhibits oxygen use by the cornea, which increases susceptibility to infection .
No approved therapeutic indications on its own.
6 associated conditions
One entry per invention. Patent families filed in the US, EP, WO and CN offices.
