Practicum 1: Effect Of Formulation On Tablet Dissolution And Auc Value Of Drug

PRACTICUM 1: EFFECT OF FORMULATION ON TABLET DISSOLUTION AND AUC VALUE OF DRUG Description of Theory Drugs can be administered in various ways and through several routes which aim to produce therapeutic effects, both locally and systemically. Drugs that reach systemic circulation in solid form and are administered orally will undergo several processes, namely, disintegration, dissolution and absorption through the cell membranes of the digestive tract. Drug dissolution is the kinetic process of drug molecules being released from the solid phase and entering the solution phase. Generally, drugs are only in solution form that can be absorbed, distributed, metabolized, excreted, or even exert pharmacological action.Dissolution is a determining stage in this process, especially for active substances that have poor solubility in water. The drug will reach the systemic circulation starting with the slowest stage. If the dissolution process of a particular drug particle is fast or if the drug is given in a solution.Several factors that can influence dissolution include the physicochemical properties of the drug, formulation factors, anatomy and physiology of the gastrointestinal tract and others. Implementation of Practicum a. Tools and materials Ingredients: 500 mg paracetamol tablets (generic tablets and branded tabletstrade), phosphate buffer solution pH 5.8. Tool:Dissolution tester,UV-VIS spectrophotometer, measuring pipettes and equipment glass b. Work procedures 1) Each group uses one test sample with a predetermined dissolution medium. 2) Determination of the wavelength of the active substance solution; make a standard solution of 100 µg/mL concentration and measure the absorbance at a wavelength of 200 800 nm. 3) Making a calibration curve; make a standard solution of the active substance with several concentrations and measure the absorption at the maximum wavelength (measurement results in no. 2). The results obtained were then plotted in a graph of the relationship between concentration and absorbance so that the linear regression equation y = a ± bx was obtained. 4) Determination of dissolution profile; dissolution container (chamber) filled with water and set the temperature at 37ºC, then chamber filled with 900 mL of dissolution medium. Tablet samples are included inchamber which has been filled with dissolution medium, then the dissolution tool is set at a speed of 50 rpm. 5 mL of solution is taken at 0, 5, 10, 15, 20 and 30 minutes. Each time taken must be replaced with the same amount of medium again. Then take 1 mL of the solution, then put it in a 100 mL measuring flask and fill the volume with phosphate buffer pH 5.8 to 100 mL. The absorption of each solution at the maximum wavelength was measured using a UV - Vis spectrophotometer, then determined the level of active substance dissolved per unit time using a calibration curve. Dissolved levels of active substances can be calculated by: - Calculate the x value (ppm) using the linear regression equation: y = ± a ± bx x = (y ± a)/ ±b→y = sample absorbance - Calculate the C value (mg) at the minute of sampling C = (X * Medium volume * FP)/1000 - Calculating Correction Factor (FK) FK = (sampling volume/medium volume) * C minutes before Calculating dissolved drug levels (mg) Dissolved drug levels (mg) = C + cumulative FK - Calculate the % dissolution content % dissolution content = (mg dissolved/mg active substance) * 100 Evaluation a. Experiment Results 1) Medicinal substance calibration curve 2) Tablet dissolution profile 3) AUC graph b. Discussion From the data and experimental results, analyze and discuss the influence of formulation factors on the dissolution profile and AUC values of tablet samples from two different manufacturers, and write down the conclusions obtained from this CF experiment. c. Report (see Practical Results Report Guidelines)