Development and optimization of inclusion complexation of ternary system of Candesartan cilexetil using design of experiment was written by Vinchure, Bhagyashree D.;Shaikh, Amir A.;Pawar, Yogesh D.. And the article was included in European Journal of Biomedical and Pharmaceutical Sciences in 2018.Formula: C33H34N6O6 This article mentions the following:
Background: Now a day some new chem. entities suffer from poor aqueous solubility The biopharmaceutical classification system (BCS) classifies them as class II substances. Different carriers were used to increase solubility of these class II drugs. Objective:The objective of the present investigation was to study the effect of Phys. mixing and High speed homogenization method on drug release of Candesartan (CAND) using polyvinyl pyrrolidone K30 (PVP K30) and β-cyclodextrin (β-CD) to enhance the solubility and bioavailability. Methods: β-CD and PVP K-30 was used to prepare ternary system of Candesartan cilexetil. Central composite design (CCD) was used for preparation and optimization of ternary system. Effect of Phys. mixing method and High speed homogenization method was investigated by evaluating Drug release (% R), dissolution efficiency (DE), mean dissolution time (MDT). Characterization of drug and polymer interactions were done using differential scanning calorimetry (DSC), X ray diffraction (XRD) and Fourier transform IR spectroscopy (FT-IR) study. Results: Results of in vitro drug release showed that various combinations of PVP K-30 and β-CD prepared using CCD approach by both the methods showed greater dissolution rate of Candesartan Cilexetil than pure Candesartan Cilexetil (*p< 0.05). Optimized formulation (Run 8) of Phys. mixing method and (Run 8) High speed homogenization method gave 67.64% and 92.56% drug release in 60 min, resp. Results of DSC, XRD and FTIR revealed the interaction of drug with carriers and formation of amorphous ternary system of Candesartan cilexetil. Conclusion: Data obtained by comparing both methods suggest that High speed homogenization method is superior in increasing dissolution of candesartan than phys. mixing method. Use of central composite design in preparation of ternary system of Candesartan cilexetil was an effective approach for dissolution enhancement of Candesartan cilexetil. 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: 145040-37-5Formula: 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. Imidazole is the basic core of some natural products such as histidine, purine, histamine and DNA based structures, etc. Among the different heterocyclic compounds, imidazole is better known due to its broad range of chemical and biological properties. Imidazole also acts as a microtubule destabilizing agents and inhibits topoisomerase and Cytochrome P450 Family 26 Subfamily A Member 1 (CYP26A1) enzymes.Formula: C33H34N6O6
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem