Lidokainin biyoadhesiv ilaç şeklinin geliştirilmesi
Bioadhesive systems have been used for many years in dentistry and orthopedics well as in opthalmology and for surgical applications. Controlled release polymeric systems for drug delivery are often designed in order to target drugs in specific areas of the body. Biodahesive controlled release systems ar a new type of preparation that can render treatment more effective and safe, not only for topical diseases, but also for systemic ones. In the study we developed a bioadhesive disc using lidocaine as an active ingredient. Discs were prepared at various ratious of polyacrylic acid (Carbopol 934) (CP) adhesive component, hydroxypropyl cellulose (HPC) and hydroxypropyl methyl cellulose (HPMC-TC, HPMC-SH) matrix component. There were 6 types of formulations. The formulation codes were A, B, C, D, E, F). Firstly, bioadhesive strength and swelling properties of discs were examined. The purpose of this study was to develop a bioadhesive disc exhibiting sufficient adhesive properties and minimal swelling. The bioadhesive bond strength of the discs was examined in a modified tensile strength apparatus using bovine oral mucosa as the biological matrix. The swelling properties of the discs were examined in an isotonic saline solution. The increase in the lateral thickness of the bioadhesive discs against time was used as an index of swelling. The adhesive bond strength of the all 2:1 mixtures were intermediate (12 kPa) and the swelling was minimal. It was suggested that 2:1 miwtures of CP and cellulosic polymers may be most suitable for oral applications. Lidocaine as a local anaesthetic agent used in dental analgesia. This study was designed to establish the safety of an adhesive disc (lidocaine) for dental analgesia. These also include improved patient compliance. The adhesive discs were designed to adhere to the gingival mucosa, releasing lidocaine from their occlusive surface. Lidocaine disc was placed on the gingival mucosa centred around the first upper premolar tooth. The results obtained from electrical stimulation were expressed.211 Mucosal anaesthesia of the pulp was achieved in clinically. The formulations F which was contaning CP:HPMC-SH (1:2) as a matrix component was the best one for achieving mucosal anaesthesia of the pulp. The dissolution profile of lidocaine was investigated and the absorption when this dosage form was applied. Lidocaine amount measured by high performance liguid chromatography (HPLC). The results indicate that the absorption of lidocaine from the oral mucosa following the gingival administration is approximately 70 % of the administred dose with formulation F. The results also indicates, the absorption of lidocaine is higher that of the formulations D, E, F, in the first 1 hr period after gingival administration due to the addition of Na lauryl sulphate into the formulations. When the Makoid-Banakar function was employed to evaluate the in-vitro, in-vivo correlation and the test goodness of fit at 95 % confidence. The data provided did fit the model well. And also overall the in-vitro, in-vivo correlations were poor. But there were two set of formulations namely, formulations A-C and D-F. The correlation for the former class is better than the latter. The relations of the outputs of dissolution test with kinetic equations (first order, zero order, Higuchi, Hixson-Crowell) have been analyzed. A good linear relationship has also been established between all of the formulations and Higuchi equation. In the study once adhesion of the discs had occured (after approximately 30 s). They were self-retaining and well -tolerated. Mucosal anaesthesia was achieved desired the first 1 hr period in clinically. Adhesive disc has several potential advantages over conventional delivery techniques, these include improved patient compliance, disk can be removed easily, the adhesive disc of lidocaine is capable of by-passing the hepatic "first-pass" metabolism.