Pharmacokinetics of a telmisartan, amlodipine and hydrochlorothiazide fixed-dose combination: A replicate crossover study in healthy Korean male subjects

Purpose: To compare the tolerability and pharmacokinetic profiles of telmisartan, amlodipine, and hydrochlorothiazide (HCTZ) in a fixed-dose combination (FDC, test product) with a co-administered telmisartan/amlodipine FDC and HCTZ in a single-entity tablet (reference product)Methods: This was a single-dose, randomized, open-label, replicate crossover study conducted in healthy male Korean volunteers aged 19 – 50 years. Fasting randomized subjects received a newly developed test product (telmisartan/ amlodipine/HCTZ, 80/10/25 mg) or two tablets of Twynsta® (40/5 mg) and one tablet of HCTZ (25 mg) as reference products. After a washout period, each group replicated the exposure of the other group.Results: The AUClast (h•ng/mL) geometric mean was 3,194.87 and 3,273.77 for the telmisartan test and reference products, respectively; 329.92 and 315.13 for the amlodipine test and reference products; 1,203.98 and 1,150.86 for the HCTZ test and reference products, respectively. The geometric mean of Cmax (ng/mL) was 543.04 and 497.81 for the telmisartan test and reference products, respectively; 7.74 and 7.34 for the amlodipine test and reference products; 218.71 and 184.39 for the HCTZ test and reference products, respectively. For telmisartan, the 90 % CI of GMRs of AUClast (h•ng/mL) and Cmax (ng/mL) were 0.9414 – 1.0496 and 1.0246 – 1.2792, respectively; the coefficient of variation (CV) of telmisartan Cmax was 41.96 %.Conclusion: A formulated FDC tablet containing a telmisartan/amlodipine/HCTZ combination (80/10/25mg) was bioequivalent to a co-administrated commercially available telmisartan/amlodipine combination and HCTZ tablets at equivalent concentrations.Keywords: Fixed-dose combination, Hypertension, Telmisartan, Amlodipine besylate, Hydrochlorothiazide, Pharmacokinetic

Preparation and Characterization of Self-Emulsified Docetaxel

The aim of this paper was to prepare a self-microemulsifying docetaxel (Dtx) using PLGA, Tetraglycol, Labrasol, and Cremophor ELP. The prepared Dtx-loaded self-microemulsifying system (SMES) showed the initial size of the range of 80–100 nm with narrow size distribution and the negative zeta-potential values. Its morphology was a spherical shape by atomic force microscopy. In experiment of stability, Dtx-loaded SMES prepared in DW and BSA condition showed good stability at 37∘C for 7 days. The viability of the B16F10 cells incubated with Dtx-loaded SMES, Dtx-solution, and Taxol were decreased as a function of incubation time. In conclusion, we confirmed that Dtx-loaded SMES showed an inhibitory effect for proliferation of B16F10 melanoma cells

In Vivo Biocompatibility Study of Electrospun Chitosan Microfiber for Tissue Engineering

In this work, we examined the biocompatibility of electrospun chitosan microfibers as a scaffold. The chitosan microfibers showed a three-dimensional pore structure by SEM. The chitosan microfibers supported attachment and viability of rat muscle-derived stem cells (rMDSCs). Subcutaneous implantation of the chitosan microfibers demonstrated that implantation of rMDSCs containing chitosan microfibers induced lower host tissue responses with decreased macrophage accumulation than did the chitosan microfibers alone, probably due to the immunosuppression of the transplanted rMDSCs. Our results collectively show that chitosan microfibers could serve as a biocompatible in vivo scaffold for rMDSCs in rats