In a photochemical chamber, a sample of 27.9 mM indomethacin (IN) in methanol was exposed to a Philips 400-W UV lamp for 5 days in normal atmosphere. Four photoproducts were separated using high-performance liquid chromatography, and their structures were elucidated by various spectroscopic methods, including liquid chromatography–electrospray ionization–mass spectrometry. A reaction scheme of IN in methanol is proposed: The photochemical reaction routes occur mainly via esterification and decarboxylation, followed by oxidation with singlet oxygen to produce an aldehyde. A b-hydroxy-g-lactone was also formed through a photochemical [2 + 2] cycloaddition, and its structure was confirmed by single-crystal X-ray diffraction.

Introduction: Urinary stones are among the most prevalent urological diseases (1-15%). While passing from kidneys to bladder, these stones stay in the lower urethra, causing painful spasms. Watchful waiting method (between 1-6 weeks) is one of the most common remedies in the treatment of lower urethral stones on the other hand, a-receptors, which help with controlling the spasm, exist in the distal urethras, especially in the trigone of the bladder. So, we decided to study the effects of Tamsulosin (a-blockers), as compared to Indomethacin, on patients suffering from distal urethral stones. The objective of this study is to evaluate the effect ofα-blocker (Tamsulosin) on the expulsion of lower urethral stones in the patients who referred to Bahman 22nd and Aria hospitals in one year.materials and methods: 85 patients who were diagnosed as suffering from urethral stones were randomly divided into 2 groups.46 patients who were placed in the first group received Tamsulosin (0.4 mg/daily) with suppository of Indomethacin for 10 days. The other 39 patients in the second group received only Indomethacin. After taking the prescribed medicines, the patients were again examined and controlled by KUB and Ultrasound. Then, the results were compared using statistical analysis.results: 32 of the patients in the first group (the case) who had received Tamsulosin had stone expulsion while the other 14 patients did not. Among the patients in the control group (a total of 39), 22 patients had stone expulsion while 17 patients did not. The result of chi-square test revealed that the 2 groups were not significantly different from each other in terms of stone expulsion and prognosis (P=0.209).There were no statistical differences between the groups of study according to age, gender and the stone size, either.conclusion: According to these findings, we do not suggest the prescription of Tamsulosin as an adjuvant therapy for stone expulsion in patients who have lower ureteral stone without considering their stone size and gender. Instead, just prescribing pain relief (if necessary) and physical activity with large amount of oral liquid intake during the watchful waiting period are enough.

Background and the purpose of the study: During the last two decades one of the most important problems in drug formulations has been low aqueous solubility of new molecules. However, numerous techniques, such as milling, co-solvent solubilization and solid dispersion have been used conventionally for aqueous solubility enhancement and the rate of solubility. Recently, nanoparticle engineering processes have been developed and reported for pharmaceutical applications to increase the dissolution rate of low-soluble drugs which in turn may leads to substantial increases in bioavailability. In this study, a controlled precipitation method was used to produce indomethacin nano-solid suspension in a polymeric matrix (as a model), in order to increase the solubility and rate of the dissolution of poorly soluble model drug.Methods: Nano-solid suspension of indomethacin in polyvinyl pyrrolidine (PVP) was prepared by controlled precipitation technique, characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier Transform Infrared Spectroscopy (FTIR) and evaluated for in vitro solubility and dissolution rate.Results and major conclusion: Absence of thermal and diffractional peaks in DSC and XRD studies indicated that indomethacin interacts with PVP in solid phase. The solubility of indomethacin in nano-solid suspension compared to crystalline form was increased to about four-fold. It was found that particle size distribution depend to the polymer MW and drug: polymer ratios. Spectroscopy methods and Transmission Electron Microscopy (TEM) images showed that indomethacin dispersed as amorphous nanosize particles in freeze dried powder. Enhanced solubility and dissolution rate of indomethacin compared to physical mixtures and crystalline form of indomethacin (polymorph I), demonstrated that it interacts with PVP via hydrogen bond and probably forming eutectic mixture.

We have studied the ulcerogenic effect of indomethacin in stretozocin. Induced diabetic rats. Streptozocin (65 mg kg-1) was injected intraperitoneally to male wistar rats. The blood glucose concentration was determined continuously. Blood glucose level increased significantly (P<0.001) after 30 days. Gastric erosions were induced by intraperitoneal injection of indomethacin (50 mg kg-1) in fasted animals. A significant (P<0.001) increase in ulcer index was found in diabetic rats

Dear editor, The first case of a new severe acute respiratory syndrome was identified in East Asia at the end of 2019, which then spread all over the world. The outbreak of the syndrome was rapid and occurred in all countries. The causative agent of this emerging respiratory disease is betacoronavirus, which is why it is called severe acute respiratory syndrome coronavirus 2 or SARS-CoV2. In addition, the world health organization (WHO) has officially named the disease COVID-19. The disease primarily affects the respiratory tract, but in most cases, it leads to the dysfunction of other organs in the human body, including the gastrointestinal system, cardiovascular system, and central nervous system. Moreover, patients with severe COVID-19 experience cytokine storm syndrome, which is considered the leading cause of death (1, 2)....

The potential of liquisolid systems to improve the dissolution properties of a water-insoluble agent (indomethacin) was the purpose of this survey. In this study, different formulations of liquisolid tablets using different co-solvents (non-volatile solvents) were prepared and the effect of several amounts of them on the dissolution behaviour of indomethacin was investigated. It is worth mentioning that the ratio of microcrystalline cellulose (carrier) to silica (coating powder material) was 20 in all formulations. To evaluate any interaction between indomethacin and the other components in liquisolid formulations, the differential scanning calorimeter (DSC) was used. The results showed that the liquisolid formulations exhibited significantly higher drug dissolution rates in comparison with directly compressed tablet. The enhanced rate of indomethacin dissolution derived from liquisolid tablets was probably due to an increase in wetting properties and surface area of drug particles available for dissolution. Moreover, it was indicated that the fraction of molecularly dispersed drug (FM) in the liquid medication of liquisolid systems was directly proportional to their indomethacin dissolution rate (DR). An attempt was made to correlate the percentage drug dissolved in 10 min with the solubility of indomethacin in PEG 200 and glycerin. In conclusion, the liquisolid compacts technique can be a promising alternative for the formulation of water insoluble drugs, such as indomethacin into rapid release tablets.

The role of inflammation has been shown in the pathogenesis of epilepsy, while glucocorticoids and adrenaline have anti-inflammatory effects. The aim of the present study was to investigate the effects of adrenaline, prednisolone, and indomethacin on caffeine-induced epilepsy (epileptiform activity) in rats and to examine the mechanism of the pro-epileptic effect of indomethacin. The adrenalectomized rats that had been given only adrenaline (the control group) did not die; however, adrenaline did not prevent the adrenalectomized rats which were given prazosin, phenoxybenzamine, yohimbine, metoprolol, and propranolol from dying. In the rats given propranolol+adrenaline, the rate of death was 100%, while this rate was 50% in the groups receiving prazosin+adrenaline, phenoxybenzamine+adrenaline, and metoprolol+adrenaline. The rate was 75% in the group given yohimbine+adrenaline. Prednisolone increased the degree of convulsion in adrenalectomized rats. Over-reduction in the blood catecholamine level made epileptogenesis more severe. It was observed that adrenaline pressed epileptogenesis via its own receptors (a- 1, a- 2, b- 1, b- 2). It was also revealed that all of the adrenergic receptors were responsible due to antiepileptic activity; b- 2 receptors played the most important role. It was observed that both acute and chronic indomethacin administration reduced the catecholamine levels. The situation in which acute administration of indomethacin did not affect epileptogenesis might originate from the fact that the structure of indomethacin did not significantly increase the corticosterone level.

OBJECTIVES: For poorly soluble, highly permeable (Class II) drugs, such as indomethacin, the rate of GI absorption is often controlled by the dissolution rate in the gastrointestinal tract. There are several techniques to enhance the dissolution of poorly soluble substances. Among them, the technique of liquisolid compact is a promising technique to increase dissolution rate of poorly soluble drugs. The aim of this study was to asses the use of liquisolid technique in enhancing dissolution rate of indomethacin and evaluation of effect of various carriers and solvents on drug release from its liquisolid 'tablets. METHODS: In this study, the dissolution behaviors of indomethacin from liquisolid compacts were investigated at two different media Simulated Gastric Fluid (SGF, pH=1.2) and Simulated Intestinal Fluid (SIF, pH=7.2). To this end, several formulations of liquisolid compacts containing variety of carriers (microcrystalline cellulose, lactose, starch, sorbitol and manitol) and nonvolatile solvents in various ratios of drug: solvent (polyethylene glycol 400) were prepared and dissolution profile of them were studied, Results: The results showed that liquisolid compacts demonstrated a considerably higher drug dissolution rates than those of conventionally made capsules and directly compressed tablets. This was due to the increased wetting properties and surface of drug available for dissolution. The results showed that the dissolution rate of the drug in SIF is better than SGF medium. In the evaluation of the kind of solvents, there were not any significant differences between solvents in SIF medium but in SGF, the formulation containing propylene glycol as solvent had a better dissolution profile. Among the carriers, also microcrystalline cellulose had better liquid retention potential, but in both SGF and SIF media, there was no significant difference between the dissolution rates of formulations. CONCLUSION: It can be concluded that the liquisolid technique can be used to increase the dissolution rate of poorly water soluble drugs.