Nanosuspensi Parasetamol tanpa Surfaktan yang Dibuat Menggunakan Metode Dry-Milling: Formulasi, Uji In Vitro dan Uji Efek Antipiretik dan Analgetik

Abstract

Background: Paracetamol is a drug with poor water solubility. Therefore, the preparation of paracetamol nanosuspension was carried out. However, in previous studies, the results of testing the pharmacological effects in vivo were low. This is thought to be due to the use of surfactants where surfactants can form micelles and at high doses can cause various side effects and toxic so that in nanosuspensions it can reduce the drug effectiveness. Therefore, paracetamol nanosuspension without surfactant was prepared. Objective: To make paracetamol nanosuspensions without surfactants by dry-milling, evaluate, and compare the antipyretic-analgesic effects in vivo using paracetamol nanosuspension preparations with surfactants and paracetamol suspensions as comparators. Method: Identification of raw materials, preparation of paracetamol nanosuspension without surfactant by dry-milling method, evaluation of preparations, and stability test for 3 months. Then, antipyretic effect was tested using 2,4-dinitrophenol induction and analgesic effect was tested using hot plate method in vivo. Results: The level in the paracetamol preparation has met the requirements. In nanosuspension dissolution with surfactant is faster compared to nanosuspension without surfactant and suspension. Dissolution in phosphate buffer at pH 5,8 is faster than in gastric medium at pH 1,2. Stability testing shows the preparation to be stable for 3 months. Antipyretic-analgesic testing shows that nanosuspensions without surfactants have a better effect than nanosuspensions with surfactants but do not have a significant difference, while suspensions have a significant difference. Conclusion: Nanosuspensions without surfactants can be made by the dry-milling method. Nanosuspensions with surfactants dissolve faster, but the therapeutic effect of nanosuspensions without surfactants is better than that of nanosuspensions with surfactants and suspensions