Preparation and In vitro characterization of a novel self-nano emulsifying drug delivery system for a fixed-dose combination of candesartan cilexetil and hydrochlorothiazide was written by Zewail, Moataz B.;El-Gizawy, Sanaa A.;Osman, Mohamed A.;Haggag, Yusuf A.. And the article was included in Journal of Drug Delivery Science and Technology in 2021.Electric Literature of C33H34N6O6 This article mentions the following:
A fixed-dose combination of Candesartan cilexetil (CAN) and Hydrochlorothiazide (HCTZ) is commonly used for the management of hypertension. CAN (BCS class II) and HCTZ (BCS class IV) suffer from inadequate oral bioavailability. Herein, the study aims to design a self-nano emulsifying drug delivery system (SNEDDS) containing a fixed-dose combination of both drugs to enhance their dissolution rate and hence oral bioavailability. Formulation of fixed-dose combination-loaded SNEDDS was carried out using various oils, surfactants, and co-surfactants, and phase diagrams were plotted using different ratios. In vitro characterizations of drug-loaded SNEDDS were achieved through optical clarity, emulsification efficiency, globule size, morphol., viscosity, drug-excipient interactions, and thermodn. stability. The in vitro release profiles of both drugs from optimized SNEDDS and their in vivo biol. activity compared to free drugs and a marketed product were studied. Optimized formulas showed a percentage transmittance greater than 90%, emulsification time less than 1 min, globule size in the nanometric range of (27-69 nm), and superior thermodn. stability after dilution and at different pH values. Fourier Transform Infra-Red (FTIR) studies demonstrated the absence of physicochem. interactions between drugs and additives. Transmission electron microscopy (TEM) images revealed spherical, non-aggregated globules that were consistent with the results of size anal. Optimized SNEDDS showed a better release profile for both drugs than those of pure drugs and marketed products and therefore, higher biol. activity was observed in hypertensive rats. SNEDDS can be used as a promising drug delivery carrier for improvement of the dissolution rate and the pharmacodynamic activity of the antihypertensive fixed-dose combination of CAN/HCTZ. In the experiment, the researchers used many compounds, for example, 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5Electric Literature of C33H34N6O6).
1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5) belongs to imidazole derivatives. The solubility of imidazoles in ethers is lower than that in alcohols and decreases with increasing chain length of the ethers . In contrast, the solubility of benzimidazoles in alcohols (C3–C6) is higher than in water and generally decreases with a Imidazole based anticancer drug find applications in cancer chemotherapy. It is used as buffer component for purification of the histidine tagged recombinant proteins in immobilized metal-affinity chromatography (IMAC).Electric Literature of C33H34N6O6
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem