Soluble cyclodextrin inclusion compound of Florfenicol

Appearance

White to off-white powder

Grade

Pharmaceutical grade

Standard

In‑house (enterprise) standard

Description

The inclusion complex is formed by encapsulating florfenicol (FF) molecules into the hydrophobic cavity of cyclodextrin (e.g., β-cyclodextrin, hydroxypropyl-β-cyclodextrin, or dimethyl-β-cyclodextrin) via host–guest inclusion complexation. Florfenicol is a novel animal-specific amphenicol broad-spectrum antibiotic. However, its aqueous solubility is extremely poor, far below the effective dose required for veterinary clinic. Thus, FF is often used in large doses, which significantly limits its preparation and application. Complexation with cyclodextrin significantly improves aqueous solubility, dissolution rate, and bioavailability. The inclusion complex is typically formed at a 1:1 molar ratio.

CAS Number

Component CAS numbers: florfenicol 76639-94-6; β-cyclodextrin 7585-39-9; hydroxypropyl-β-cyclodextrin 128446-35-5; 2,6-dimethyl-β-cyclodextrin 51146-08-8.

Storage

Store in tightly sealed containers, protected from light, in a cool, dry place.

Applications

Widely used in veterinary medicine for: treatment of bacterial infections in food-producing animals (poultry, swine, cattle, and fish); respiratory diseases; as a broad-spectrum antibiotic in drinking water formulations; injectable formulations.

Safety

The inclusion complex reduces muscle irritation compared to commercial florfenicol injections. Well tolerated in target animals.

Stability

Stable under recommended storage conditions. FF-DM-β-CD solutions showed no significant change in FF content over 7 days. Products show good quality stability.