Evaluation of protein undernourishment on the condylar process of the Wistar rat mandible correlation with insulin receptor expression

The mandible condylar process cartilage (CP) of Wistar rats is a secondary cartilage and acts as a mandibular growth site. This phenomenon depends on adequate proteins intake and hormone actions, including insulin. Objectives The present study evaluated the morphological aspects and the expression of the insulin receptor (IR) in the cartilage of the condylar process (CP) of rats subjected to protein undernourishment. Material and Methods The nourished group received a 20% casein diet, while the undernourished group (U) received a 5% casein diet. The re-nourished groups, R and RR, were used to assess the effects of re-nutrition during puberty and adulthood, respectively. CPs were processed and stained with picro-sirius red, safranin-O and azocarmine. Scanning electron microscopy and immunohistochemistry were also performed. Results The area of the CP cartilage and the number of cells in the chondroblastic layer decreased in the U group, as did the thickness of the CP layer in the joint and hypertrophic layer. Renourishment during the pubertal stage, but not during the adult phase, restored these parameters. The cell number was restored when re-nutrition occurred in the pubertal stage, but not in the adult phase. The extracellular matrix also decreased in the U group, but was restored by re-nutrition during the pubertal stage and further increased in the adult phase. IR expression was observed in all CPs, being higher in the chondroblastic and hypertrophic cartilage layers. The lowest expression was found in the U and RR groups. Conclusions Protein malnutrition altered the cellularity, the area, and the fibrous cartilage complex, as well as the expression of the IRs. .

Dissolution rate enhancement of piroxicam by ordered mixing

Micronized piroxicam was mixed with lactose, mannitol, sorbitol, maltitol and sodium chloride to produce ordered mixture in a glass vial by manual hand shaking method. The effect of excipients, surfactant, superdisintegrant, drug concentration and carrier particle size on dissolution rate was investigated. Dissolution rate studies of the prepared ordered mixtures revealed that all water soluble excipients increased the dissolution rate of piroxicam when compared to the dissolution rate of piroxicam or its suspension. Ordered mixture formulation PLF4, consisting of lactose as water soluble excipient, SSG [8% w/s] and SLS [1% w/w], released piroxcam at a very fast rate so much so that about 90% of the composition had passed into solution within 2 min. The order of the dissolution rate enhancement for ordered mixtures of various water soluble excipients was: lactose > mannitol > maltitol > sorbitol > sodium chloride. Carrier granules of size 355-710 micro m were most effective in increasing the dissolution rate of drug from ordered mixtures. Decreasing the carrier particle size reduced drug dissolution from ordered mixtures. The dissolution rate of ordered mixtures consisisting of 1-5% w/w piroxicam was superior to dissolution rate of piroxicam suspension. The dissolution data fitting and the resulting regression parameters indicated Hixson Crowell, cube root law, as the best fit to drug release data of ordered mixtures

In vivo antinociceptive and anti-inflammatory activities of dried and fermented processed virgin coconut oil

The present study was carried out to investigate the antinociceptive and anti-inflammatory activities of virgin coconut oil [VCO] produced by theMalaysian Agriculture Research and Development Institute [MARDI] using various in vivo models. Two types of VCOs, produced via standard drying [VCOA] and fermentation [VCOB] processes were used in this study. Both VCOA and VCOB were serially diluted using 1% Tween 80 to concentrations [v/v] of 10, 50 and 100%. Antinociceptive and anti- inflammatory activities of both VCOs were examined using various in vivomodel systems. The antinociceptive activity of the VCOs were compared to those of 1% Tween 80 [used as a negative control], morphine [5 mg/kg] and/or acetylsalicylic acid [100 mg/kg]. Both VCOA and VCOB exhibited significant [p < 0.05] dose-dependent antinociceptive activity in the acetic acid-induced writhing test. Both VCOs also exerted significant [p < 0.05] antinociceptive activity in both phases of the formalin and hot-plate tests. Interestingly, the VCOs exhibited anti-inflammatory activity in an acute [carrageenan-induced paw edema test], but not in a chronic [cotton-pellet-induced granuloma test] model of inflammation. The MARDI-produced VCOs possessed antinociceptive and anti-inflammatory activities. Further studies are needed to confirm these observations

Synthesis and evaluation of some new 2.4- [1H.3H] -quinazolinedione derivatives as potential analgesic and anti-inflammatory agents

A series of 1-[3-trifluoromethylphenyl]-2, 4-[1H,3H]- quinazolinedione derivatives was synthesized as potential analgesic and anti- inflammatory agents. Structures were confirmed by elemental analysis and spectral data. Five compounds were tested for analgesic and anti- inflammatory activities. Two compounds II and VI exhibited significant analgesic and anti-inflammatory activities compared with flufenamic acid

Evaluation of analgesic, antipyretic and anti-inflammatory activity of spirobarbitunylphenothiazines in rodents.

Analgesic, antipyretic and anti-inflammatory activities of newly synthesized spirobarbitunylphenothiazines viz 10-[7, 11-Di(4-4' dimethoxphenyl)-3-oxo-9-methylaminoimino-2, 4-diazaspiro [5.5] undecane 1, 5 dione] acetylphenothiazine (test drug A) and 10-[7, 11-Di (N.N-dimethylaminophenyl)-3-oxo-9-methylaminoimino-2, 4-diazaspiro [5, 5] undecane-1, 5 dione] acetylphenothiazine (test drug B) have been screened in Swiss mice and Wistar rats. The peripheral analgesic activity of test drugs A and B was investigated by acetic acid induced writhing test in Swiss mice while the central analgesic action was assessed by hot-wire (tail flick test) of the analgesiometer and tail-clip test in Wistar rats. Antipyretic activity was assessed on Brewer's yeast induced pyrexic model while antiinflammatory activity was seen on carrageenan induced hind paw oedema. Analgesic activity was found to be only of peripheral type as there was reduction of 66% in writhing responses by test drugs A and B in dose of 80 mg/kg in mice. No change in the tail flick responses was observed on analgesiometer or by tail clip by both the test drugs. Reduction of 1.5 to 2.0 degrees C in rectal temperature was observed in pyretic rats by test drugs A and B in dose of 80 mg/kg. 80% reduction in paw volume was noted in 80 mg/kg dose of both the test drugs which was comparable to the anti-inflammatory activity of 300 mg/kg, p.o. of phenylbutazone.

Utility of potassium iodate for the estimation of lornoxicam, meloxicam and sulbutiamine in pharmaceutical formulations

In this study, a simple and accurate method was described for the determination of lornoxicam, meloxicam and salbutiamine. The method involved the oxidation of drugs with potassium iodate in acidic medium with the liberation of iodine. The liberated iodine was extracted into cyclohexane and the absorbance was measured at 520 nm. The effect of different experimental parameters on the development of the color was studied [the concentration of the reagent, temperature and reaction time]. The method was applicable over a concentration range of 0.10-0.50, 0.05-0.30 and 0.05-0.40 mg ml-1 for lornoxicam, meloxicam and salbutiamine, respectively. The proposed method was successfully applied to the determination of the studied drugs in bulk powder and in the pharmaceutical dosage forms. The validity of the method was assessed by applying the standard addition technique

Bases farmacológicas del uso de antiinflamatorios no esteroidales en caballos / Proper use of non-steroidal anti-inflammatory agents in the horse. A review

El uso de antiinflamatorios no esteroidales en la clínica de equinos es una práctica común. En este ensayo se resume la información clínico-farmacológica más relevante en cuanto al uso de estos fármacos. En este sentido, los datos vertidos no resultan de la extrapolación en otras especies. Se pretende que la información compilada permita dar un uso más racional a dichos medicamentos, estrechando la brecha que se genera entre el cínico sujeto a una enorme carga de trabajo y la información creciente sobre el particular. Se destacan únicamente aspectos básicos de la fisiopatología de la inflamación y se hace mención de los antiinflamatorios no esteroidales más utilizados en equinos; por ejemplo, fenilbutazona, flunixina meglumina, así como de los que se encuentran en fase experimental en esta especie (piroxicam, eltanaco, ácido tolfenámico). A pesar de su baja toxicidad, se destacan los signos clínicos y hallazgos de necropsia generados por el mal uso de aqellos fármacos y con base en sus rasgos farmacocinéticos y farmacodinámicos se presentan las dosis y los usos de los medicamentos aceptados por la comunidad

In-vitro evaluation of sustained release ibuprofen microspheres

Microspheres for oral use have been employed to target and to sustain the release of the drug. The objective of this study was to use the melt dispersion technique and aqueous vehicle to entrap ibuprofen into wax carrier (carnauba wax) with the aid of surfactant (Pluronic L-62). The effects of different levels of Pluronic L-62, stirring speed, and ibuprofen levels, as well as the in-vitro release rate of ibuprofen were evaluated. The in-vitro dissolution of ibuprofen in phosphate buffer pH 7.2 showed that microspheres prepared with low amount of drug (1.5 g) released 58.1 percent of ibuprofen after 6 hours, while microspheres prepared with high amount of drug (6.0 g) released only 38.9 percent of ibuprofen. Microsphere formulations prepared by using aqueous vehicle were spherical and of smooth surface. In general the melt dispersion technique was a successful method for preparing sustained release ibuprofen microspheres