Effect of ofloxacin on the cartilage of the knee joint of juvenile rats

Ofloxacin is one of fluoroquinolones derivatives, which has a broad spectrum bacterial activity. It is contraindicated in children and adolescents because of its potential chondotoxicity in juveniles. However, fluoroquinolones continue to be prescribed as a drug of choice for treatment of some life threatening diseases in pediatrics. This study was conducted to examine the effect of ofloxacin on cartilage of juvenile rats by light and electron microscopes. Twenty newborn albino rats were treated with an oral dose of 900 mg/kg/day of ofloxacin for 28 days. The animals were sacrificed after the completion of the administration and the knee joints were prepared for light and electron microscopic examination. Morphometric study and statistical analysis of the results were also performed. The lesions were demonstrated in the articular cartilage of all the animals. Fissures, chondrtocyte clusters and wide area of matrix devoid of cells in the intermediate zone were observed. The surface of the premature articular cartilage of the femur was irregular. The matrix of the articular cartilage showed less staining with toluidine blue and masson trichrome. Electron microscopic results showed separation between chondrocyte cell membrane and the matrix. The chondrocytes were necrotic with pyknotic nuclei and vacuolation of their cytoplasm. There were electron dense aggregates on the cell membrane and inside the cells. The thickness of the premature articular cartilage and epiphyseal plate cartilage were significantly decreased. The numbers of chondrocytes of the premature articular cartilage and epiphyseal plate cartilage were significantly decreased. The numbers of chondrocytes of the premature articular cartilage and epiphyseal plate cartilage were significantly decreased

Interaction of rofecoxib with beta-cyclodextrin and hp-beta-cyclodextrin in aquoues solution and in solid state

The interaction between rofecoxib [ROF], an analgesic antiinflammatory drug, with beta-cyclodextrin and HP-beta-cyclodextrin was evaluated in aqueous environment and in solid state. The solubility of ROF with beta-CyD and HP-beta-CyD in aqueous solution was determined and the stability constants were calculated from the phase solubility studies at different temperatures. Binary systems of ROF with the investigated CyDs were prepared by co-grinding and solvent evaporation methods. The formation of inclusion complexes with beta-CyD and HP-beta-CyD in the solid state was investigated by differential scanning calorimetery, infrared spectroscopy and X-ray diffractometry. Dissolution rate of ROF binary systems was determined and compared with those of the physical mixture and the pure drug. It was found that the solubility of ROF increased as a function of both CyDs concentration and temperature showing an AL- type diagram indicating the formation of 1: 1 stoichiometric inclusion complexes. The apparent association constants were found to be 104.45 M-1 and 121.65 M-1 for beta-CyD and HP-beta-CyD; respectively. Co-grinding method led to enhancement of ROF dissolution rate in comparison to the other preparation methods. The in vitro dissolution rate of ROF at pH 7.4 could be ranked in the following order: ground mixture, coevaporate, physical mixture and pure drug. Ground mixture of ROF with HP- beta-CyD and betaCyD has a t50% = 7 min and 50 min, respectively

Formulation and evaluation of rofecoxib tablets in comparison with marketed product

Rofecoxib [ROF] is an analgesic anti-inflammatory drug. It is a selective inhibitor of cyclooxygenase enzyme [Cox-2]. The aim of this work was to prepare and evaluate ROF tablets with higher dissolution rates and higher activity and to compare them with the marketed product. Direct compression technique was adopted for preparation of ROF tablets using different excipients namely; Sta-Rx starch 1500 or mixture of anhydrous lactose and microcrystalline cellulose Avicel pH 101 [1:1 w/w. ratio]. The effect of co-grinding method of ROF with either-polyvinyl pyro-lidone [PVP] 40000 or Avicel pH 101 in a ratio of 1:5 w/w on the drug release from the prepared tablets was also studied. All the tablet quality control tests and the thermal behavior were studied. The anti-inflammatory activity was also studied in rats using paw-edema method and the results were investigated by statistical analysis using ANOVA test at the level of significance [P = 0.05]. All formulations of ROF tablets showed good mechanical properties and complied with the USP XXV pharmacopeial standard requirements for uniformity of dosage units and friability. Differential scanning calorimetry showed transformation of the drug to the amorphous form. Formulae No. 2, 3 [containing co-ground mixture of the drug with either PVP 40000 or Avicel pH 101 and Sta-Rx starch 1500] gave higher percentage of ROF release [t[50%] = 15, 9 min. respectively,] in comparison with the marketed product [t[50%] = 25 min]. It was found also that the prepared ROF tablets show superior anti-inflammatory activity in comparison with the marketed product upon analysis of data using ANOVA test

Comparative study of Inhalational and total intravenous anaesthesia effect on middle ear pressure and postoperative nausea and vomiting

Successful outcome in microsurgery of ENT depends on two important factors. Ther first is prevention of intraopertive and postoperative fluctuation of the middle ear pressure and scond factor is prevention of post operative nausea and vomiting. This study was conducted on 30 patients subjected to elective nasal surgery, the patients were randomly divided into two equal groups each of them 15 patients. Group I receivedd inhalational anaesthetic using halothane and Group II received total intravenous anaesthesia using propofol-Middle ear pressure was measured using tympanometry. The incidence of occurrence of post operative nausea and vomiting was studied in both groups. The blood pressure, heart rate were measured, the dose requirement of nitroglycerine and arterial blood gases [paO2, pacO2pH and Hco3] were assessed. It was found that, the measurements of the middle ear pressure increased in both groups as compared to base line. The inhalational group showed more increase than the propofol group. As regarding the incidence of PONV it was significantly lower after TIVA than after halothane. Arterial blood pressure was significantly lower propofol group than inhalational group and the dose requirment of nitroglycerine was significantly lower in propofol group than inhalational group, there were no significant changes in pH,paO2, pacO2 or Hco3. This work concluded that total intravenous anaesthesia using propofol was superior to inhalational anaesthesia using halothane in this type of surgery regarding to middle ear pressure and postoperative nausea and vomiting [PONV] and controlled hypotensive anaesthesia

Effect of melatonin on analgesic and anti - inflammatory action of indomethacin in rats with induced adjuvant arthritis

This experimental study was carried out to evaluate the possible therapeutic effects of melatonin in rheumatoid arthritis and its interaction with indomethacin. The study was carried out on rats in which rheumatoid-like arthritis were induced experimentally by an intradermal injection of a total volume of 0.1 ml of cold emulsion consisting of native type II collagen and complete Freund's adjuvant. A booster dose was given after three weeks. It could be concluded that melatonin had an immune stimulant effect enhancing the immune system and its use in autoimmune diseases such as rheumatoid arthritis exaggerated arthritic manifestations. Also, a combined administration of melatonin and indomethacin had no therapeutic effect on patients suffering from rheumatoid arthritis