Supersaturable self-microemulsifying drug delivery system enhances dissolution and bioavailability of telmisartan

To enhance the dissolution and oral bioavailability of telmisartan (TMS), a poorly water-soluble anti-hypertensive drug, a supersaturable self-microemulsifying drug delivery system (SuSMEDDS) was developed. Amorphous alkalinized TMS (AAT) was formulated into a SMEDDS, composed of Capmul® MCM (oil), Cremophor^® RH40 (surfactant), and tetraglycol (co-surfactant).

Although the SMEDDS was rapidly dissolved (> 80% within 5 min) in a limited condition (500 mL, pH 6.8), drug precipitation was observed over time, resulting in a decrease in dissolution levels. The precipitation was due to drug recrystallization, as determined by differential scanning calorimetry and powder X-ray diffraction analyses. Several polymers, including Soluplus^® (SOL), were screened as precipitation inhibitors; ultimately, SuSMEDDS-SOL was prepared by admixing SOL and the SMEDDS at a 5:100 (w/w) ratio. SuSMEDDS-SOL was superior in terms of dissolution efficiency (> 90% over 2 h) and dissolution-retaining time (no precipitation over 2 h).

An in vivo pharmacokinetic study in rats revealed that the oral bioavailability of SuSMEDDS-SOL was 4.8-, 1.3-, and 1.2-fold greater than those of the TMS suspension, AAT solution, and SMEDDS, respectively. Therefore, SuSMEDDS-SOL is a promising candidate to enhance the dissolution and oral bioavailability of TMS.

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Article Information: Sun Young Park, Chang Hwa Jin, Yoon Tae Goo, Bo Ram Chae, Ho Yub Yoon, Chang Hyun Kim, Seh Hyon Song, Sang Beom Han & Young Wook Choi (2020). Supersaturable self-microemulsifying drug delivery system enhances dissolution and bioavailability of telmisartan. Pharmaceutical Development and Technology, DOI: 10.1080/10837450.2020.1834580