Universitas Indonesia Conferences, Asian Federation for Pharmaceutical Sciences (AFPS) 2019

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The effect of Excipients on Physicochemical Properties of Telmisartan and Telmisartan-Oxalic Acid Hydrate Salt Co-Crystal
Hestiary Ratih, Jessie Sofia Pamudji, Fikri Alatas, Sundani Nurono Soewandhi

Last modified: 2019-07-18


Telmisartan (TMS) belongs to class II drugs in Biopharmaceutical Classification System (BCS), a drug that has low solubility and high permeability. TMS also has  poor flow rate so that it can cause problems in the manufacturing process of pharmaceutical preparations. Based on previous research, TMS with oxalic acid coformers (OXA) formed multicomponent crystals namely hydrate salt co-crystal (HSC) TMS:OXA:H2O (2:1,5:3) and with the formation of HSC there was an increase in solubility, dissolution and tabletability compared with the TMS.  The dissolution test of HSC and TMS tablet with various compression strengths showed that all tablets were not disintegrated in a pH 7.5 phosphate buffer media.  The purpose of this study was to determine the effect of several disintegrants on dissolution and multicomponent crystal tabletability formed with subsequent treatments compared to pure TMS and innovator products.  Disintegrants used were Starch 1500 (S1500) and croscarmellose sodium (CCS) with a ratio of TMS/HSC: disintegrant (1: 9) and (3: 7) b/b.  Evaluation on the mixture of TMS:disintegrant and HSC:disintegrant were carried out in a physical mixture, the milled mixture, the mixture compressed into tablet, and the powder tablets. Characterization includes PXRD and SEM and a dissolution test was carried out and the tensile strength of the mixture of TMS/HSC:disintegrant was determined. The dissolution rate and tabletability of the mixture of HSC:disintegrant (1:9) and (3:7) are higher compared to the mixture of TMS:disintegrant (1:9) and (3:7). The combination of HSC:CCS (1:9) produced the highest dissolution rate and tabletability compared with other disintegrants in all treatments. The milled mixture treatment produced the highest dissolution with DP60 minutes which was 105.90±0.17% and 60 minutes dissolution efficiency (ED60), which was 101.09±0.48%.  For the treatment of the mixture compressed into tablet and the powder tablets, the dissolution rate of HSC:CCS (1: 9) compared with innovator tablet. HSC:CCS (1:9) produces better dissolution results than innovator tablets.

Keywords: telmisartan, oxalic acid, hydrate salt co-crystal, dissolution, tabletability