Introduction:Solubility and dissolution of a poor water-soluble drug are the two major barriers for formulation scientists in development of drug delivery. Many of the potent drugs do not show the therapeutic effects due to solubility issues but may show toxicity issues when used in high doses. Solid dispersion (SD) technology is an excellent tool for enhancing the solubility and dissolution and hence related bioavailability.Materials and Methods:SD of spironolactone (SPL) was developed using an inert carrier polyethylene glycol 4000 (PEG 4000) by the conventional fusion method and characterized for various characterization parameters.Results:Solubility of pure drug and SD of SPL in water was found to be 23.54 ± 1.75 μg/mL and 61.73 ± 1.26 μg/mL, respectively. The maximum cumulative percentage release from pure drug, SPL marketed product (tablet), physical mixture, and SPL SD at 60 min was 27.25 ± 1.83%, 35.64 ± 3.65%, 47.72 ± 2.45%, and 74.24 ± 3.25%, respectively in 0.1 N HCl.Conclusions:SD of SPL was developed successfully. The solubility of SPL SD was found to be significantly increased (P < 0.05) as compared to SPL active pharmaceutical ingredient (API) and physical mixture of PEG 4000 and SPL. The current study indicated that SD of SPL was a better option for enhancing solubility of a poorly soluble therapeutic agent.
Introduction: Upper gastrointestinal (UGI) endoscopy includes visualization of the oropharynx, esophagus, stomach, and proximal duodenum, with real time assessment and interpretation of the findings encountered. An upper endoscopy is indicated in the diagnostic evaluation of signs and symptoms of a wide variety of gastrointestinal disorders. Besides there are some therapeutic implication of the endoscopy. This study was conducted to study the spectrum of diseases found during the upper gastrointestinal endoscopy in patient presenting in Lumbini Medical College and Teaching Hospital (LMCTH). Methods: This was a retrospective observational study carried out in LMCTH. The endoscopic record book of the patients who underwent UGI endoscopy for various reasons from February 2011 to 2013 was analysed. The risk factor of smoking and alcohol was also included and analysed in the study. Results: All together 550 upper GI endoscopy was performed in the two years. There were 290 males (52.72%) and females were 260 (47.38%). The mean age was 45.7 years (SD=17.9). Most of the patient belonged to the age group 41 to 80 years (71%). Among total patients, 209 (38%) of them were found to be macroscopically normal. Of those who had positive endoscopic findings; 165 (48.4%) had gastritis and 36 (10.6%) had duodenal ulcer, esophageal varices was in 30 (8.8%), gastric carcinoma in nine (2.6%) of cases. Cigarette smoking was significantly associated with the presence of peptic ulcer disease (p=0.01) and malignancy of gastrointestinal tract (p=0.03). Alcohol intake was non-significantly related to peptic ulceration (p=0.07) and malignancy of gastrointestinal tract (p=0.09). Conclusion: Upper gastrointestinal endoscopy is a safe and useful procedure for investigating patients with gastrointestinal complains. Gastritis was the most common finding among the patients who had abnormal endoscopy followed by duodenal ulcer and esophageal varices.
Atorvastatin calcium is a lipid-lowering agent. It has approximately 15% of bioavailability, remaining amount of drug showed adverse effect which is undesirable for patients. The objective of the study was to enhance the solubility and a dissolution profile of the atorvastatin (AT) calcium. Solid dispersion (SD) is a technique which enhances the solubility and a dissolution profile of poorly soluble drug. Various methods are being used for SDs such as microwave irradiation fusion, kneading, solvent evaporation, fusion, and dropping method. The authors have used here conventional fusion method using PEG 4000 as a hydrophilic carrier. The solubility of pure drug, physical mixture using PEG 4000 (1:3), and SD in phosphate buffer solutions (pH 6.8) was found to be 55.33 ± 0.66, 81.89 ± 2.35, and 93.66 ± 1.35, respectively. Fourier transform infrared and differential scanning calorimetry study showed the significant peak shift of drug in SD. It indicated that the nature of drug had been changed from crystalline form to amorphous form due to conversion into SD formulation. The dissolution rate was significantly increased when the drug polyethylene glycol 4000 ratio was 1:3. The mean cumulative percentage drugs release from pure drug, physical mixture, marketed tablet, and SD at 1 h was 28.92 ± 1.66%, 55.26 ± 0.95%, 72.16 ± 1.33%, and 91.66 ± 1.65%, respectively. It was concluded that the solubility and dissolution profile of SD of AT calcium showed the enhancement of solubility and dissolution when compared with marketed preparations.
The thermodynamic properties of dilute solutions of hydrogen and deuterium in palladium-copper alloys with copper contents of 10, 25, and 40 at.% have been determined by a calorimetric-equilibrium method at 555 K. The results are compared (a) with corresponding data for hydrogen in palladium–silver at the same temperature and (b) with equilibrium data for palladium–copper measured near room temperature. (1) The partial excess entropies of hydrogen in dilute solutions in palladium–copper alloys are reduced significantly compared to pure palladium. In palladium–copper this effect is only about one-half that in palladium-silver. Even so, it is believed to reflect in both systems a nonrandom distribution of the hydrogen atoms among the available interstitial sites. (2) It is shown that to a first approximation the dissolved hydrogen atoms may be considered to be isotropic, three-dimensional Einstein oscillators. In this approximation the observed differences between hydrogen and deuterium may be used to calculate the vibrational frequency of hydrogen. For palladium–copper these differences do not vary with copper content within experimental error. This points towards ?H being essentially independent of alloy composition. This behavior contrasts with that of hydrogen in palladium–silver, for which Picard et al. [J. Chem. Phys. 70, 2710 (1979)] recently found increasing values of ?H with increasing silver content. It is suggested that the different behavior of ?H in large measure may account for the observed difference between the concentration dependence of the excess entropy of hydrogen in palladium–copper and in palladium–silver.
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