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A double-blind study of the effectiveness of betamethasone-17-benzoate in the treatment of recurrent aphothous ulcers (RAU) was concucted. The drug was found to be effective in reducing symptoms and shortening healing time but not in preventing recurrences. Evaluation of the medical histories and laboratory studies suggests that multiple factors may be involved in the etiology of RAU, as reported by others.
We present a case of persistent vulvar vestibulitis treated for several years unsuccessfully that has come to an end using a six week course of submucous infiltration of betamethasone and lidocaine in the vestibular area.
We compared the phospholipid profile in tracheal aspirates from surfactant-treated preterm neonates with and without prenatal betamethasone administration. We found higher phosphatidylglycerol concentrations and lower phosphatidylinositol and sphingomyelin concentrations in corticosteroid-treated preterms ( P < 0.01). We speculate that prenatal corticosteroids enhance biochemical surfactant phospholipid maturation.
Micro-liquid chromatography-mass spectrometry (micro-LC-MS) was utilized to quantitatively determine betamethasone and its major unconjugated metabolite, 6 beta-hydroxybetamethasone, in equine plasma and urine. The advantage of micro-LC-MS over conventional gas chromatography-mass spectrometry in corticosteroid determination is illustrated and the reliable, steadfast nature of micro-LC-MS is demonstrated through example.
The physicochemical stability and the compatibility between N-acetylcysteine (1 g/5 ml), betamethasone (4 mg/1 ml) and netilmicin (100 mg/1 ml) were studied at room temperature (25+/-2 degrees C) over 1 h. During this study, drug concentrations were measured using three separate HPLC methods with UV detection at t=0, 5, 10, 20, 30, and 60 min. The pH of the mixture was determined. Degradation products of the drugs were assayed using HPLC. This study demonstrates the stability and compatibility of the mixture over 1 h at room temperature. The pinkish non-remnant coloration observed when pouring N-acetylcysteine into a recipient has no effect on the stability of the drug.
The complete separation of a composite mixture that consisted of Betamethasone Dipropionate (BMD), Clotrimazole and their derivatives in a pharmaceutical dosage form was achieved within 15 min using sodium dodecyl sulfate (SDS) micellar electrokinetic chromatography (MEKC). For the MEKC separations, electrophoretic media consisting of SDS-phosphate buffer and various concentrations of alcohols or acetonitrile were used. The optimal condition for separating BMD, Clotrimazole and their analogues was found to be 50 mM SDS-15% acetonitrile-5% butanol at pH 7.2. The results demonstrated that the method was valid for the quantitation of BMD, Clotrimazole and analogues with selectivity and precision comparable to that of High-Performance Liquid Chromatography (HPLC).
The aim of this work was to develop an analytical method for a simultaneous determination of cyanocobalamin (Vitamin B12), betamethasone, and diclofenac, present in pharmaceutical formulations, by high performance liquid chromatography, assuring rapidity, accuracy, precision, and selectivity. The working conditions were as follows: RP18 column of 125 mm x 4 mm ID and a particle size of 5 microm; mobile phase acetonitrile-water (40:60; v/v) (pH* 3.45) adjusted with acetic acidl flow gradient from 0.8 to 1.9 ml/min.; injection volume of 20 microl; temperature 34 degrees C and detection at 240 nm. The method was adequately validated, and linearity, accuracy, as well as the system, method and interday precision, for each active principle, were determined.
We tested the hypotheses that (1) maternal betamethasone (betaM) treatment over the range of clinical doses for prevention of prematurity-related pathologies from day 15 to 21 of rat gestation would produce growth retardation, and (2) the lowest betaM dose to produce growth retardation would result in hypertension in adult offspring. In experiment 1, pregnant Sprague-Dawley rats were administered betaM (0, 50, 100, 200, 400, or 600 microg/kg per day, subcutaneously) on days 15-21 of pregnancy and necropsied on day 21.5, with fetal lung and placental weights recorded. In experiment 2, two more groups of rats (0 or 100 microg/kg per day, subcutaneously) were allowed to deliver, and offspring were instrumented at 100 +/- 4 days of postnatal life with indwelling left carotid arterial catheters. After 48 hours of recovery, blood pressure was recorded continuously for 24 hours. In experiment 1, all newborn rats treated with betaM, and their placentas, except those receiving 50 microg/kg per day, were growth retarded in comparison with controls (P <.05). All treated lungs were smaller than those of controls (P <.05). In experiment 2, no differences were found in the mean arterial blood pressure of adult offspring given the lowest effective dose of betaM (100 microg/kg per day) compared with controls (114.2 +/- 5.3 mmHg versus 114.6 +/- 3.4 mmHg, respectively). These data suggest that glucocorticoids given in the last week of rat pregnancy in the lowest human clinical dose do not cause hypertension and somatic growth retardation. However, the presence of lung growth restriction at this dose argues for more studies on the efficacy of even lower concentrations for their ability to improve lung and other organ and tissue function while avoiding unwanted side effects.
Glucocorticoids (GCs) are the most effective drugs for anti-inflammatory diseases. A number of adverse side effects, however, limit chronic treatment with GCs. To improve their therapeutic usefulness, attempts have been made to dissociate the two main actions of the glucocorticoid receptor (GR), transactivation and transrepression, which are believed to be responsible for the side effects and anti-inflammatory effects, respectively. We report here species-specific differences in the transactivation response mediated by GR. Dexamethasone (DEX), betamethasone (BM), and their esterified-derivatives had full transrepression agonistic activity in a reporter assay using CV-1 cells transfected with either human or rat GR. These GCs also had full transactivation agonistic activity in CV-1 cells transfected with human GR. The esterified-BM, however, had only partial transactivation agonistic activity in cells transfected with rat GR, whereas BM and esterified-DEX had full transactivation agonistic activity. Moreover, in rat hepatoma H4-II-E cells, the esterified-BM failed to induce tyrosine aminotransferase, which is regulated by GR-mediated transactivation activity. There were no significant differences between the binding affinity of these GCs to human and rat GR. Consistent with the weak transactivation activity of esterified-BM mediated by rat GR, there were few side effects, evaluated by thymus involution and body weight loss, in an antigen-induced asthmatic model in rats. These results suggest that the potency of esterified-BM to induce transactivation activity is different between species and that this difference is not due to differences in receptor binding.
The biomechanical repercussion of the corticoid-induced osteopenia (a severe consequence of long-term glucocorticoid therapy) was studied in cortical bone of small rodents. Growing rats receiving 12.5-3200 micrograms/kg/d of betamethasone (BMS) s.c. for 20 days suffered a log-dose related impairment in body weight gain and in mechanical (fracture load, bending stiffness) and cross-sectional properties (area, moment of inertia) of femur diaphyses. No changes in bone material properties (ability to stand stress, elastic modulus, energy absorption per unit volume) were observed. At variance with the biphasic dose-response curves (positive effects at low-medium doses, negative at high doses) previously obtained with cortisol in a similar model, only negative effects on every variable studied were observed in this experiment. Results suggest that BMS effects on cortical bone biomechanics derived mainly or completely from those induced on bone geometry (biomechanical correlate of corticoid-induced osteopenia) in the assayed conditions. Data are compatible with a BMS-induced change in the setpoint of bone mechanostat. Correlation of bone geometric and biomechanical data with body weight gain showed that the anti-anabolic effects of BMS on bone were proportionally less intense than those exerted on the whole biomass.
Cushing's syndrome due to the abuse of Betamethasone nasal drops has not been described before. This report presents such a case and emphasises the care which one must take in prescribing topical steroids.
A series of 9 alpha-halo-12 beta-hydroxy and 12 beta-acyloxy analogues of betamethasone 17,21-dipropionate were synthesized and tested for topical antiinflammatory potency in the croton oil ear assay. The compounds were assayed for systemic absorption in the contralateral ear assay, in which it was found that 12 beta-hydroxy analogues 9, 13, and 15 were all absorbed but the corresponding 12 beta-esters 11a-e, 14, and 16 were not. On repeated high-dose applications to the mouse ear, there was no evidence of systemic absorption of any 12 beta-propionate ester as gauged by thymus weights (thymic involution) and plasma cortisol levels (adrenal suppression). Results of limited SAR studies showed that topical antiinflammatory activity and systemic absorption were not greatly influenced by the 9 alpha-halogen but were largely dependent on the polarity and size of the 12 substituent. While the optimal compounds 14 and 16 were less topically active than the controls beta- and beclomethasone dipropionate, unlike the controls, they displayed no systemic effects, even after repeated high-dose applications. Surprisingly, propionate 14 was devoid of atrophogenic activity.
The use of polymer latexes as vehicles for drug transport and controlled delivery in the body is a very active research field in applied colloid science. In this work, the polymer chosen is a commercially available ethylcellulose-based material, Aquacoat. We report electrokinetic (electrophoresis) data on this polymer in the presence of the soluble glucocorticoid betamethasone disodium phosphate (BMP). The electrophoretic mobility of the particles becomes more negative as the concentration of BMP in the medium is increased between 10(-5) and 10(-3) M, this demonstrating that the negative species produced upon dissolution of BMP adsorb on the particles; this trend is reversed for higher concentrations due to the phenomenon of double layer thickness. When pH is increased at constant BMP concentration, the negative mobility increases in absolute value, but it reaches lower values than attained in the absence of BMP. This is interpreted as another consequence of adsorption, since the ionization constants of the phosphate and sulfate groups are different. Such adsorption is confirmed and measured by spectrophotometric analysis of the supernatants after centrifugation of the suspensions; it is found that the adsorption density increases with the initial concentration of BMP in the medium, an almost vertical isotherm being obtained for concentrations above 5 x 10(-3) M, possibly due to bidimensional aggregation of the adsorbed molecules and multilayer adsorption at higher concentrations. It is found that the adsorbed amount increases with the ionic strength of the medium as a consequence of screening of the particle and BMP charges, whereas these electrostatic contributions to adsorption manifest also in the pH dependence of adsorption. IR analysis of the particles after equilibration with BMP solutions of increasing concentration agrees well with adsorption data.
PURPOSE: The objective of the present study was to develop prolonged anti-inflammatory action of DL-lactide/glycolide copolymer (PLGA) nanosphere incorporating a water-soluble corticosteroid (betamethasone sodium phosphate; BSP). Another aim was to demonstrate the biocompatibility and biologic efficacy of these BSP-loaded nanospheres directly administered into ovalbumin-induced chronic synovitis in the rabbit. METHODS: BSP-loaded nanospheres were prepared by an emulsion solvent diffusion method in oil (caprylate and caprate triglyceride). The drug releasing properties of the nanospheres were measured in vitro in phosphate buffer saline (PBS: pH7.4), and in vivo in rat air-pouch (pseudo synovial fluid). The BSP-loaded nanosphere suspensions were administered into the joint cavity in a model of antigen-induced arthritic rabbit and evaluated by measuring the joint swelling, and the biocompatibility was appraised by histologic microscopy. RESULTS: The BSP-nanospheres were a unimodally-dispersed particulate system with a mean diameter ranging from 300 to 490 nm, and BSP was efficiently entrapped in the lipophilic copolymer (PLGA), although its hydrophilic properties. The drug release-rate from the nanospheres in PBS was controlled by the molecular weight and the lactic/glycolic acid (LA/GA) ratio of the polymers. The in vitro releasing study demonstrated that sustained drug release occurred for over three weeks. In the antigen-induced arthritic rabbit, the joint swelling decreased significantly by administering BSP-loaded nanospheres during a 21-day period after intra-articular challenge. With regards to the prolonged anti-inflammatory efficacy, serum antibody to ovalbumin showed a sustained reduction during the period, and the steroidal effect appeared by the degradation of the polymer in the synovium. The BSP-nanosphere administered was phagocytosed by the synovial activated-cells and the cartilage degradation was almost prevented. CONCLUSIONS: Direct intra-articular injection of a PLGA nanosphere system with a water-soluble steroid provided a prolonged pharmacological efficacy in the joints of arthritic rabbits. The local anesthetic in the knee-joints was evaluated to be safe and without biologic damage.
Cultures of human astrocytoma have been derived by collagenase digestion and are presumed, from their aneuploid karyotypes, to be predominantly neoplastic. Early passage cultures in proliferative phase have been cloned in the presence of dexamethasone and betamethasone, both commonly used in management of patients with brain tumours. These steroids raise both the cloning efficiency and the proliferative capacity of cells within each clone. Inhibition was detected only in very high steroid concentrations (25-50 microng/ml). Since these concentrations are unlikely to be attained in vivo it is concluded that anticipated physiological levels of these steroids enhance cell survival at low densities in culture. The significance of this in vivo is discussed.
Eighty patients were randomised in a single-masked parallel-group study to receive topically either the test drug, a diclofenac and gentamicin combination, or a betamethasone and neomycin combination after routine cataract extraction and intraocular lens implantation. Each group was assessed over a 6 week period for post-operative inflammation. The two drug combinations were equally effective in suppressing inflammation in the early post-operative stages and the diclofenac-gentamicin combination was slightly more effective in the later stages. The test drug was well tolerated and showed no adverse effects. We feel it is an effective and relatively safe drug which has a role as an anti-inflammatory agent after cataract extraction and has potential advantages in certain circumstances.
OBJECTIVE: To examine the consequences of antenatal betamethasone (AB) exposure on postnatal stress regulation. STUDY DESIGN: Fourteen AB exposed infants born at 28-30 weeks' gestation were assessed in the NICU during postnatal week 1 and at 34 weeks postconception. Nine infants born at 34 weeks gestation without AB treatment were evaluated as a postconceptional age comparison group. Salivary cortisol, heart rate, and behavior were measured at baseline and in response to a heelstick blood draw. RESULTS: Repeated measures ANOVAs revealed that both groups displayed an increase in heart rate and behavioral distress in response to the stressor. The cortisol response, however, was blunted in AB-treated infants at both assessments. CONCLUSION: AB treatment has consequences for hypothalamic-pituitary-adrenal (HPA) axis regulation that persist for at least four to six weeks after birth, indicating that studies of long-term effects are warranted.
A clinical study was conducted to determine whether, in the topical treatment of psoriasis, a combination of calcipotriol and betamethasone valerate after previous treatment with calcipotriol alone was more effective than the continuation of the monotherapy with calcipotriol, especially in 'low responders'. Patients (n = 169) with the clinical diagnosis 'chronic plaque-type psoriasis' were treated twice daily for 2 weeks with calcipotriol, followed by a 4-week treatment with calcipotriol monotherapy in 87 patients or combined calcipotriol/betamethasone valerate in 82 patients; all patients were followed for 8 weeks. The psoriasis area and severity index (PASI) was used to compare the two treatment groups. The overall therapeutic result was also assessed by the investigators and patients. The combination therapy was more effective, as assessed by all evaluated variables; moreover, patients showing insufficient response to calcipotriol alone after 2 weeks showed a regression of psoriatic lesions using the combination regimen. Thus, the combination of calcipotriol and topical steroids is recommended as the therapy of first choice for patients who do not respond well to treatment with 2 weeks of calcipotriol alone. Furthermore, this combination reduces the hazards associated with the long-term use of topical corticosteroids (atrophy and rebound) as well as the irritation associated with calcipotriol.