Drug-nutrient cocrystallization-driven strategy towards self-assembly of milrinone and ferulic acid provides an exemplification in perfecting in vitro/vivo characteristics of anti-heart failure drugs

Abstract

A drug-nutrient cocrystallization-driven strategy has been established to highlight the superiority of nutraceutical ferulic acid (FEA) in perfecting the biopharmaceutical peculiarities of anti-heart failure drug milrinone (MLN). Taking the strategy...

First Cocrystallization of Gatifloxacin with Nutraceuticals Displays the Ameliorated In Vitro/Vivo Biopharmaceutical Property and Increased Antibacterial Activity

“…Herein, the diffusion behavior determinations of the samples are performed on the improved Franz diffuser in pH 6.8 phosphate buffers, with the flux and cumulative diffused amounts displayed in Figure . As shown in Figure a, the permeation fluxes of the three samples rise sharply in the first 1 h and then gradually decrease to reach a steady state, which is consistent with the constant, invariant motion of permeation across the membrane . Relative to pure GAT, the peak and steady-state flux values of salts 1 and 2 are increased by approximately quadruple to septuple, respectively.…”

“…As shown in Figure 9a, the permeation fluxes of the three samples rise sharply in the first 1 h and then gradually decrease to reach a steady state, which is consistent with the constant, invariant motion of permeation across the membrane. 55 Relative to pure GAT, the peak and steady-state flux values of salts 1 and 2 are increased by approximately quadruple to septuple, respectively. Additional, as shown in Figure 9b, although the cumulative diffusion of all samples gradually increases within time, the cumulative diffusion amounts of salts 1 and 2 at 8 h are noticed to be 7.87 and 4.62 mg•cm −2 , which are 6.78 and 3.98 times that of parent drug GAT, which is 1.16 mg•cm −2 , respectively, indicating that the current new solid forms possess better membrane diffusion performance.…”

The New Gatifloxacin‐p‐Coumaric Acid Cocrystalline Form for Enhanced In Vitro Pharmaceutical Properties While Improving Oral Bioavailability and Antibacterial Activity

“…Intrinsic Dissolution Rate (IDR) Analysis: IDR analysis was carried out on a RC-6ST intelligent dissolution tester (RC-6, Tianguang Optical Instruments Co., Ltd., China) with a rotating speed of 100 rpm at 37 °C using rotating disk method. [45,46] First, 100 mg of GAT and GAT-CMA were compressed applying DP30A tablet machine, acquiring a tablet (0.5 cm 2 ) with a seal on one side and a flat surface on the other side, and then immersed the obtained tablets into a dissolution cup containing 400 mL buffer at 100 rpm. At regular intervals, took out 5 mL of the separation solution and added the same amount of relevant buffer medium.…”

Copper- or iron-catalyzed stereoselective methylation of enamides using dicumyl peroxide as the methyl source

“…As a common functional group, the methyl group plays a vital role in many pharmaceuticals and biologically active molecules. 1 Although it is small in size and usually considered as chemically inert, the methyl group can induce great changes in the physical, chemical and biological properties of compounds. 2 The introduction of methyl groups into molecules, especially biologically active molecules, can dramatically alter the pharmacokinetic profile and pharmacological properties of molecules for the well-known “magic methyl effect” and has been widely applied in drug discovery (Fig.…”