Solubility and Dissolution Rate Enhancement of Poorly Soluble Telmisartan using Hydrotropy Method

Abstract

Objectives: Drugs given by oral route will undergo dissolution followed by permeation then it reaches to blood.
Low water solubility is the foremost issue that comes upon with the development of dosage forms for newly
discovered drugs as well as old drugs. Telmisartan is a class II category drug under the biopharmaceutical
classification system, which limits its bioavailability to about 40%. Hydrotropy method has several advantages
compared to other methods such as cost-effectiveness, ease of process, compatibility, scalable, and flexibility
to varieties of dosage forms. Henceforth, an attempt has been made to improve the solubility of telmisartan
using the hydrotropy method. Materials and Methods: Three different hydrotropic agents (urea, mannitol,
and lactose) in different concentrations (10–50%) were used to find the solubility of the drug. The design
of an expert statistical tool was utilized to optimize the best concentration of hydrotropic agent for having
maximum solubility of the drug. Results: In a 40% urea blend, the solubility was obtained approximately
25.87 times more than pure drug (0.003 mg/mL) which showed the potential of the hydrotropic agent. This
obtained optimized batch was further characterized for drug release profile and other related parameters. The
optimized concentration of urea showed 87.46 ± 0.17% of drug release in 8 h which is relatively higher than
the plain drug release. Conclusion: Therefore, it can be concluded that the 40% concentration of urea as a
hydrotropic agent showed to be a key factor for enhancement of solubility followed by dissolution of poorly
soluble telmisartan drug.