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Physicochemical Parameters Impact on Analgesic Activity of Acetylsalicylic Acid and Salicylamide

This study explores the influence of lipophilic, electronic, and steric properties on the analgesic activities of Acetylsalicylic Acid (Aspirin) and Salicylamide. Experimental parameters of pKa (Electronic), Rm (Lipophilic), and RM (Steric) were investigated. Results indicated Aspirin's higher lipophilicity, acidity, and smaller size compared to Salicylamide. Analgesic activity tests on mice showed Aspirin's higher efficacy. Physicochemical properties of Rm, pKa, and RM play significant roles in determining analgesic activity.

sumayah-buthainah
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Physicochemical Parameters Impact on Analgesic Activity of Acetylsalicylic Acid and Salicylamide

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  1. ABSTRACT Study of Lipophilic (Rm), Electronic (pKa) and Steric (RM) Parameter of Acetylsalycylic acid and Salicylamide and Their Analgesic Activities. Research was aim to study the influence of Lipophilic, Electronic and Steric properties of Acetylsalicylic acid (Aspirin) and Salicylamide on the analgesic activities of the compounds. The physicochemical parameters used in the experiment were pKa (Electronic), Rm (Lipophilic) and RM (Steric). Rm (Retention modified) was determined by Reverse Phase Thin Layer Chromatography. pKa was determined by spectrophotometry and RM (molar refractivity) was determined by measuring the refractive index and density of the solution of the compounds. The analgesic activities of the compounds were tested on mice using writhing test and were represented in ED50. Rm of acetylsalicylic acid was 0.13 and salicylamide was 0.05. The results showed that the acetylsalicylic acid was more lipophilic than salicylamide. pKa of acetylsalicylic acid was 3.24 and pKa of salicylamide was 8.74. The results showed that acetylsalicylic acid was more acid than salicylamide. RM of acetylsalicylic acid was 38.29 and salicylamide was 58.61. The results showed that the acetylsalicylic acid was smaller in size than salicylamide. ED50 of acetylsalicylic acid was 129.96 mg/kg BB and salicylamide was 182.28 mg/kg BB. The results showed that acetylsalicylic acid had higher analgesic activity than salicylamide. It can be concluded that the physicochemical properties which influence the analgesic activity was Rm, pKa and RM. Keyword: Acetylsalicylic acid, Salicylamide, pKa (negative log Ka), RM (molar refraction), Rm (retention modified), analgesic activity.

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