Polyoxyl 35 Castor Oil

Category

Emulsifier; Solubilizer; Humectants

Grade

Pharmceutical Excipients

Description

Polyoxyl 35 castor oil occurs as a pale yellow, oily liquid that is clear at temperatures above 26℃. It has a faint but characteristic odor and can be completely liquefied by heating to 26℃. Polyoxyl 40 hydrogenated castor oil occurs as a white to yellowish, semisolid paste at 20℃ that liquefies at 30℃. It has a very faint characteristic odor and is almost tasteless in aqueous solution. Polyoxyl 60 hydrogenated castor oil occurs as a white paste at room temperature. It has little taste or odor in aqueous solution.

UNII

6D4M1DAL6O

Chemical Name

Polyethoxylated castor oil

CAS Number

61791-12-6

Synonyms

Acconon; Arlatone; Cremophor; Etocas; Eumulgin; Jeechem; Lipocol; macrogolglyceroli hydroxystearas; macrogolglyceroli ricinoleas; Mapeg; Marlowet; Nikkol; Protachem; Simulsol

Administration route

Intramuscular; Intravenous; Intravesical; Ophthalmic; Oral; Topical

Dosage Form

Injection, emulsion, Soultion, drops, capsule, suspension, tablet, cream

Stability and Storage Conditions

Polyoxyethylene 35 castor oil can form a stable solution in various organic solvents such as chloroform, ethanol, and propylene glycol; it can also form a clear and stable solution in water. Polyoxyethylene 35 castor oil and other polyoxyethylene castor oil derivatives are miscible, and can be mixed with fatty acids, fatty alcohols, and some animal and vegetable oils under heating conditions. Polyoxyethylene 40 hydrogenated castor oil is also stable in hydroalcoholic solutions. When the aqueous solution of polyoxyethylene 35 castor oil is heated, its solubility decreases and becomes turbid. Polyoxyethylene 40 hydrogenated castor oil aqueous solution is heated for a long time, and the solid phase and liquid phase can be separated after cooling. However, the sample can be restored to its original state by homogenization. Polyoxyethylene 35 castor oil is stable in low concentrations of electrolytes such as acids or salt solutions, with the exception of mercuric dichloride. Polyoxyethylene 35 castor oil aqueous solution can be sterilized by hot-pressed steam at 121°C for 20 minutes. The product darkens during this process, but this does not speak to the stability of the product. Polyoxyethylene hydrogenated castor oil aqueous solution can also be sterilized by autoclaved steam at 121°C, but it can cause a slight decrease in pH value. Although polyoxyethylene castor oil derivatives are nearly sterilized during manufacture, microbial contamination may still occur during storage. Polyoxyethylene castor oil derivatives should be filled in airtight containers and stored in a cool, dry place away from light.

Source and Preparation

Polyoxyethylene castor oil derivatives are prepared by reacting ethylene oxide with castor oil or hydrogenated castor oil under certain conditions. Polyoxyethylene 35 castor oil is produced by reacting 1 moL castor oil with 35-40 moL ethylene oxide. Polyoxyethylene 40 hydrogenated castor oil is prepared by reacting 1moL of hydrogenated castor oil with 40-45 moL of ethylene oxide. Polyoxyethylene 60 hydrogenated castor oil is prepared by reacting 1moL hydrogenated castor oil with 60 moL ethylene oxide.

Applications

Polyoxyethylene castor oil derivatives are nonionic surfactants used in oral, topical and injectable dosage forms, they are also used in cosmetics and animal food. Polyoxyethylene 35.castor oil is mainly used as an emulsifier and solubilizer, especially suitable for the preparation of aqueous solutions containing volatile oils, fat-soluble vitamins, and other hydrophobic substances. 1.mL of an aqueous solution of 25% (v/v) polyoxyethylene 35.castor oil can solubilize about 10 mg vitamin A palmitate; about 10 mg vitamin D; about 120 mg vitamin E; about 120 mg vitamin K1. When solubilizing fat-soluble vitamins, the drug or components should first be dissolved in polyoxyethylene 35.castor oil (Cremopbor EL), then slowly add water and stir vigorously. When water is added, the viscosity increases, and when the water content reaches about 40% (v/v), there is a maximum viscosity. For a short time, heating to about 60°C or adding polyethylene glycol and/or propylene glycol can increase the solubilizing power. In oral formulations, polyoxyethylene 35.castor oil tastes banana. Polyoxyethylene 35.castor oil has been used as a solvent for patented injections such as diazepam, propanidine, and alfaxalon containing alfadolone acetate; see item 14. Polyoxyl 35.castor oil is also used in glycerin suppositories. Veterinary polyoxyethylene 35.castor oil emulsifies cod liver oil, oil and fat, mixed into animal food. In cosmetics, polyoxyethylene 35.castor oil is mainly used as a solubilizer for fragrances and volatile oils in a medium containing 30~50% v/v alcohol (ethanol or propylene glycol). It can be used in place of castor oil in hand washes. Polyoxyethylene 40 hydrogenated castor oil is preferred in oral formulations compared to polyoxyethylene 35.castor oil because the former is almost odorless. Polyoxyethylene 40 hydrogenated castor oil is used to increase the solubility of vitamins, essential oils, and certain pharmaceuticals in hydroalcoholic or total aqueous solutions. Using 1.mL of 25% (v/v) polyoxyethylene 40 hydrogenated castor oil in water, approximately 88 mg of vitamin A palmitate, or approximately 160 mg of vitamin A propionate, can be solubilized. It can also increase the solubility of other drugs, such as alfadolone, alfaxalon, hexachlorophene, hexetidine, levomepromazine, miconazole, propanidine, thiopental, etc. In the aerosol medium containing water, adding polyoxyethylene 40 hydrogenated castor oil can improve the solubility of the propellant in the water phase. Suitable for increasing the solubility of mixtures of dichlorodifluoromethane and propane/butane. When there are bubbles in the hydroalcoholic solution containing polyoxyethylene 40 hydrogenated castor oil, adding a small amount of polypropylene glycol 2000 can eliminate the bubbles. Polyoxyl 40 hydrogenated castor oil is also used to emulsify fatty acids and fatty alcohols.

Safety

Polyoxyethylene castor oil derivatives are used in a variety of oral, topical, and parenteral pharmaceutical formulations.Acute and chronic toxicity tests in animals have shown polyoxyethylene castor oil derivatives to be essentially nontoxic and nonirritant materials; see Table VI.However, there are reports of cardiovascular changes and nephrotoxicity in various species of animals.Several serious anaphylactic reactions, cardiotoxicity, nephrotoxicity, neurotoxicity, and pulmonary toxicity have also been observed in humans and animals following parenteral administration of formulations containing polyoxyethylene castor oil derivatives. The precise mechanism of the reaction is not known.

Incompatibilities

Various ester components in polyoxyethylene hydrogenated castor oil are easy to saponify in strong acid and strong alkali solution. In aqueous solution, polyoxyethylene 35 castor oil is stable to most electrolytes at certain concentrations. However, precipitation may occur when it is compatible with mercury dichloride. Precipitation can occur with some organic substances at a certain concentration, especially those containing phenolic hydroxyl groups, such as: phenol, resorcinol, tannic acid. Polyoxyl 40 Hydrogenated Castor Oil and Polyoxyl 60 Hydrogenated Castor Oil are generally not affected by salts in hard water.