New non-symmetrical dimers which contain respective side units of azobenzene and 1,2,3-triazole-choloesteral have been synthesised from the reaction between 6-azido-[4-(4-acetylphenylazo)phenoxy]alkane and cholesteryl-4-(prop-2-ynyloxy)benzoate. The results show that the derivatives of 6-bromo[4-(4-acetylphenylazo)phenoxy]alkanes which possess the odd alkyl spacers exhibit dimesomorphism of N and SmA phases whilst the members with even numbers are non-mesogenic. However, the 6-azido-[4-(4-acetylphenylazo)phenoxy]-alkanes show N and SmA phases in a wide temperature range. On heating and cooling the target compounds cholesteryl 4-[(1-(6-(4-(4ʹ-acetylphenylazo)phenoxy)alkyl)-1H-1,2,3-triazol-4-yl)methoxy]benzoate show chiral nematic (oily streak and fan-shaped texture) and focal conic texture characteristics of smectic A phases with high thermal stability. Present investigation also reveals the effect of the spacer length upon the phase transition temperature. Intercalated arrangement is favoured by the molecules in the smectic phase. The observation is well established by XRD measurement wherein the actual molecular length is smaller than the theoretical value.

Nausea and vomiting are symptoms associated with a lot of diseases and oral tablets may be unprofitable for patients especially those suffering from nausea and vomiting. Therefore, this study aimed to formulate a new meclizine and pyridoxine combination formula for chewable tablets and provide rapid drug absorption and decrease motion sickness. The new chewable formulation has been prepared to provide fast action, is more acceptable, and could be used for all age categories. Seven trials haves been carried out to prepare to find the suitable one where formula 7 of the chewable gum preparation exhibited good taste and hardness, while the gelatin formulation give an accepted formula after four trials with better taste and good acceptance. The prepared formulations give a dissolution profile of meclizine (95.53–102.8%) and pyridoxine (99.25 ± 115%) and assay (98 + 0.05–99.3 ± 0.8%) for meclizine and (97 ± 0.9–100.0 ± 0.08%) for the pyridoxine in three prepared formulations of chewable tablets. Followed by the evaluation, the formulation and testing them on human volunteers are carried out to confirm their effect to ensure acceptance and fast actions. The finding is promising for preparing a new route of administration of meclizine and pyridoxine combination to be used in the market.

Background and Objectives Hemorrhoids are defined as swollen veins in the anus and lower rectum. Hemorrhoids are a common medical problem and have a negative impact on people’s lives. The drugs that are available on the market are limited, and therefore, the objective of the present research is to develop and evaluate a lidocaine and nitroglycerin ointment combination for enhanced external hemorrhoid treatment. Materials and Methods Five formulations of 0.1% lidocaine and 0.1% nitroglycerin ointments (F1-F5) were developed using hydrocarbon bases (B1 and B2), hydrophilic petrolatum B3, hydrophilic B4, and emulsifying base B5. Different physicochemical parameters were conducted to evaluate the quality of the studied formulations. Results Cracking was observed for F1 and F2 and phase transitions were noticed for F4 and F5. While, the hydrophilic petrolatum base formulation F3 showed the best physical stability up to one month with high uniformity with a drug content of 107.5% and a calibration curve R=0.9999. Docking study confirmed the activity of lidocaine and nitroglycerin towards hemorrhoids through conventional hydrogen bonds with target proteins 6s3a and 6t3w, respectively. F3 was tested by nine patients who suffered from external hemorrhoids for seven days. Patients reported a decrease in hemorrhoid grain sizes with excellent tolerability. Conclusion The developed single formulation of two different drugs, lidocaine and nitroglycerin, has synergistic action and is well-tolerated treatment option for external hemorrhoids, as it not only decreases the hemorrhoid symptoms (pain and itchy) but also eliminates the side effects like headache that arise when the drugs are administered alone.

Cephalosporin is one of the antibiotics that are widely used because of its broad spectrum and high effectiveness. The aim of the present research was to formulate and evaluate the antimicrobial effect of meclizine (ME) alone and in combination with cefixime (CFM) and cefuroxime (CXM). Evaluation of antibacterial activities was determined by using Klebsiella (sensitive and ESBL), Escherichia coli, Staphylococcus aureus (sensitive and MRSA), and Pseudomonas aeruginosa. The molecular docking was conducted for ME and CFM with the crystal structure of beta‐ketoacyl‐acp synthase III + malonyl/CoA. The results show that ME has the highest minimum inhibitory concentrations (MICs) activity against sensitive Klebsiella spp., followed by sensitive S. aureus . The combination of ME and CXM demonstrated a synergistic activity against both sensitive and resistant S. aureus and sensitive Klebsiella with an interpretation of minimum bactericidal concentration (MBC) of < 0.06, 0.1875, and 0.33, respectively. Meanwhile, partial synergism activity is observed against E. coli , and indifference activity against P. aeruginosa and Klebsiella ESBL with an interpretation FBC of 0.75, 1.2, and 1.25, respectively. The ME and CFM combination showed partial synergism activity against sensitive Klebsiella, E. coli, and P. aeruginosa with an interpretation FBC of 0.625, 0.75, and 0.75, respectively. While indifference activity was recorded against both sensitive and MRSA S. aureus and Klebsiella ESBL with interpretation FBC of 4, 1.25, and 1.5, respectively. The ME and CXM combination showed the highest activity against Gram‐positive bacteria and sensitive Klebsiella , while the ME and CFM combination showed the highest activity against Gram‐negative bacteria. This combination may consider be a promising formula as an antimicrobial drug.