Preparation method and application of four-arm polyethylene glycol succinic acid florfenicol compound

Abstract

The invention provides a preparation method and application of a four-arm polyethylene glycol succinic acid florfenicol compound. The compound is generated by reacting four-arm PEG succinic acid with florfenicol under the action of a catalyst and a dehydrating agent. The compound is used for preparing four-arm polyethylene glycol succinic acid florfenicol particles, and the preparation method comprises the following steps: (1) sieving sucrose, and uniformly mixing the sieved sucrose with the four-arm polyethylene glycol succinic acid florfenicol compound to obtain powder; (2) uniformly mixing 95v% medicinal ethanol, povidone and Tween 80 to prepare a wetting agent; and (3) uniformly mixing the wetting agent and the powder, and conducting granulating, drying and sieving. The four-arm polyethylene glycol succinic acid florfenicol granular preparation is good in taste masking effect, slow in release, safe and efficient. The granular preparation has the unique advantages that the solubility is increased, and the treatment effect is remarkably improved.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, and in particular relates to a preparation method and application of a four-arm polyethylene glycol succinate florfenicol compound. Background technique [0002] Florfenicol, also known as florfenicol, is an animal-specific antibiotic developed by Schering-Plough in the late 1970s in search of better chloramphenicol derivative antibacterial drugs. Because of its broad antibacterial spectrum, good antibacterial effect, fast absorption, and no cross-resistance with other commonly used drugs, it is widely used in veterinary clinical prevention and treatment of bacterial infectious diseases in pigs, chickens, fish, cattle and other animals. Because florfenicol has many practical values, such as broad antibacterial spectrum, no aplastic anemia, etc., it has been widely used in aquaculture and animal husbandry in recent years. [0003] Dosage forms such as powders, injections, solutions, ...

AI Technical Summary

Problems solved by technology

However, whether it is the old formulation of Florfenicol or the newly developed formulation, there are more or less problems, such as: the taste-masking effect of soluble powder and solution is poor, while the general premix and powder have poor fluidity and dispersibility It is relatively low, and it is not easy to mix evenly with the feed; the injection form belongs to individual administration, not through oral administration. Although there is no problem of poor palatability, the clinical application of the injection form is relatively cumbersome, and its applicability in intensive large-scale breeding production is poor. , once the disease breaks out on a large scale, it is impossible to make the maximum effect of florfenicol realistically

Florfenicol liposomes are prone to hydrolysis and oxidation reactions, so they need to be stored at low temperature, and the encapsulation efficiency of liposomes is low, and the drug is easy to leak out during storage

Florfenicol microspheres have many problems such as small drug loading, unstable shape, easy aggregation and blockage of microspheres, uneven drug release, etc.

The florfenicol solid has poor drug stability, is prone to aging during storage, and is easily affected by the properties of the carrier material

β-cyclodextrin is often used as an inclusion agent for florfenicol inclusion complexes. β-cyclodextrin is unstable to acids and is limited by the size and shape of drug molecules, so its solubility in water is low

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