Preparation Of Lidocaine Hydrochloride Transdermal Film-forming Spray

Objective:The amide local anesthetics Lidocaine Hydrochloride belongs to middle-effectlocal anesthetics and the water solution was stable. It has a wide range of safety, quick effect and it can penetrate mucous membrane, but the half-life is relatively short.This paper intends to combine the characteristics of transdermal drug delivery systems to develop a new sustained release formulation of lidocaine hydrochloride named transdermal film-forming spray. From the drug solution was spread on the application site immediately after the dry film forming agent volatile solvent. To facilitate the application of the various parts of the affected area, especially the elbow, knee and other parts is not flat. At the same time, it has the characteristics of slow release and long effect. Is expected to provide a new type of long-term pain for long-term pain medication, reduce the pain of patients. Methods:Establish one method to screen the membrane materials based on the spray width. The single factor test method was used to study the dosage of the auxiliary materials by spray width and film formation time. Used spray width, transparency of film, uniformity of film and toughness of film as index to optimize the prescription byorthogonal test. Investigate the spray performance and general character by Chinese Pharmacopoeia 2015 edition rules of spray preparation standards. The drug content was determined by ultra performance liquid chromatography(UPLC), and the quality standard of the preparation was studied. In vitro diffusion test was performed by using Franze diffusion instrument and isolated rat skin. At the same time, the accumulation of the drug and the volume of the skin were measured. Skin irritation and allergy tests were carried out in nude mice. The preliminary stability of the preparation was investigated by influencing factors. Results:1. The materials used in this study waspreliminary determinedthrough the establishment of the film material screening method, including the dispersion of NE30 D, P407, PVA-1788, silicone defoaming agent and glycerol.2. Under the conditions established by liquid chromatography, accessories do not interfere with the determination of LID, and the method has high accuracy. Single factor and orthogonal experiments were designed to investigate the optimal prescription.3. Quality research shows that the spray effect of the preparation is better. The liquid and membrane properties have good stability and strong applicability. The in vitro transdermal test of the preparation can be seen that the function of LID quick acting was retained, and the film could be released at the same time, the release process was consistent with the Higuchi drug release model. By nude skin irritation and sensitization test, it was concluded that the spray of lidocaine hydrochloride in this study had no irritation and sensitization to the skin.4. The influence factors test can be seen, the preparation of the initial stability was better, need to avoid high temperature storage. Conclusions:The transdermal film-forming spray made of this research was good in all aspects. The prescription composition was appropriate and the film was stable. In vitro transdermal results showed that the preparation has certain sustained-release ability, and lied the foundation for the development of the LID.