salicylates and trolamine-salicylate

Radio-epithelitis represents a common problem, for which treatments are characterized by a great heterogeneity. The present review of literature focuses on data referenced in Pubmed((c))/Medline((c)) and published in French/English. Despite a real preclinical rationale, aloe vera and trolamine failed to demonstrate any benefit in the prophylactic settings. In a prospective assessment phase III assessment, Calendula Officinalis was shown to be superior to trolamine for the prevention of radio-epithelitis. In the curative settings, sucrafalte failed to demonstrate any benefit. The benefit of dermocorticoids was suggested in terms of erythema and itching. Promising clinical results are available with hyaluronic acid (MA S065D and Ialugen) and silver leaf may reduce the intensity of cutaneous radio-induced side effects. Data from the literature are conflicting, making real the difficulty to adopt from clinical trials any proof-of-principle strategy. Considering these uncertainties, several strategies are allowed. New topics are under investigation. Present data from the literature highlight the need for further trials, in order to propose evidence-based treatments and to harmonize clinical practice.

Topics: Administration, Topical; Adrenal Cortex Hormones; Aloe; Calendula; Dermatologic Agents; Emulsions; Eosine Yellowish-(YS); Fatty Acids; Humans; Hyaluronic Acid; Lipids; Phytotherapy; Plant Preparations; Radiodermatitis; Radiotherapy; Salicylates; Sesquiterpenes; Sucralfate

To compare the rate and extent of systemic salicylate absorption following single and multiple applications of two topically applied analgesics, one containing methyl salicylate and the other containing trolamine salicylate.. Two-period, two-treatment, randomized, crossover, multiple-dose study in healthy men and women volunteers.. Six men and six women volunteers, 21-44 years of age.. Subjects applied 5 g of an ointment containing 12.5% methyl salicylate twice daily for 4 days (8 doses) or a cream containing trolamine 10% twice daily for two doses, to a 10-cm2 area on the thigh. Treatment order and leg (right or left) were assigned randomly. Subjects were crossed over to the alternate treatment on the other leg after a minimum washout period of 7 days.. The total amount of salicylate recovered in the urine during two dosing intervals (24 hours) on each study day, relative to the applied dose, was used to calculate the bioavailability of each product. Mean standard pharmacokinetic parameters including area under the curve, maximum concentration (Cmax), time to maximum concentration, and minimum concentrations at steady-state were determined from serum concentrations. Serum concentrations were fit to three pharmacokinetic models and the suitability of each model was evaluated. Estimates of absorption rate constant, clearance, volume, and fraction absorbed on day 1 were estimated by using the best-fitting model.. Salicylic acid could not be detected in serum after trolamine application. However, concentrations between 0.31 and 0.91 mg/L were detected within 1 hour of the first application of methyl salicylate and Cmax between 2 and 6 mg/L were observed following the seventh application on day 4. Both the extent and rate of absorption changed after the first 24 hours. The absorption rate constant increased significantly from the first to the seventh dose (first dose absorption rate constant: 0.16 h-1, seventh dose: 0.28 h-1; p < 0.035). Urinary recovery of total salicylate (salicylic acid and principal metabolites of salicylic acid) during the first 24 hours of the methyl salicylate phase averaged 175.2 mg, exceeding the 6.9 mg (p < 0.05) recovered during the trolamine phase. The recovery of salicylate in the urine in the first 24 hours after application of methyl salicylate was significantly greater than the 1.4% recovered after application of trolamine (p < 0.05). Furthermore, the fraction of methyl salicylate recovered in the urine increased significantly from 15.5% on day 1 to approximately 22% on the second, third, and fourth days.. A considerable amount of salicylic acid may be absorbed through the skin after topical application of methyl salicylate products and this may increase with multiple applications. Caution is warranted in patients for whom systemic salicylate may be hazardous or problematic.

Topics: Administration, Cutaneous; Adult; Analysis of Variance; Anti-Inflammatory Agents, Non-Steroidal; Cross-Over Studies; Dosage Forms; Female; Humans; Male; Ointments; Salicylates; Skin Absorption

The purpose of this study was to determine the effects of ultrasound and phonophoresis using an anti-inflammatory-analgesic cream (trolamine salicylate) on delayed-onset muscle soreness (DOMS). Repeated eccentric contractions were used to induce DOMS in the elbow flexors of 40 college-aged women. Subjects were then assigned randomly to one of four groups: (1) group 1 (n = 10) received sham ultrasound using placebo cream, (2) group 2 (n = 10) received sham ultrasound using trolamine salicylate cream, (3) group 3 (n = 10) received ultrasound using placebo cream, and (4) group 4 (n = 10) received ultrasound using trolamine salicylate cream. Subjects were treated on 3 consecutive days. Muscle soreness and active elbow range of motion were assessed daily prior to each treatment. The subjects in group 3 experienced an increase in DOMS, whereas no increase in soreness was observed in the subjects in group 4. The authors concluded that ultrasound enhanced the development of DOMS but that this enhancement was offset by the anti-inflammatory-analgesic action of salicylate phonophoresis. These findings suggest that salicylate phonophoresis may be useful in clinical situations in which it is desirable to administer ultrasound without increasing inflammation.

Topics: Adult; Anti-Inflammatory Agents, Non-Steroidal; Elbow Joint; Exercise; Female; Humans; Muscular Diseases; Pain Management; Phonophoresis; Range of Motion, Articular; Salicylates; Ultrasonic Therapy

The purpose of this investigation was to determine the effect of ultrasound intensity and mode on serum salicylate levels following phonophoresis. Approximately 12-13 g of a salicylate product (Myoflex) was applied to the right anterior forearm of five males and two females. Randomly ordered ultrasound treatment intensities (0.0 W.cm-2; 1.5 W.cm-2, pulsed 50%; and 1.5 W.cm-2, continuous) were applied through the salicylate-containing product for a 5 min duration. A 7.0 ml blood sample was drawn from the left anterior forearm prior to each treatment and again 2 h after treatment. Analysis of variance indicated that none of the topical salicylate treatments produced an increase in serum salicylate levels. These findings suggest that there is no appreciable absorption of salicylate into the bloodstream following topical application of salicylate with or without the use of ultrasound. Since any penetration of salicylate through the skin would result in an increase in serum salicylate levels, the efficacy of phonophoresis to introduce medication into the subdermal tissue is questionable. These findings suggest that a critical review of phonophoresis in general is indicated.

Topics: Administration, Cutaneous; Adult; Female; Forearm; Gas Chromatography-Mass Spectrometry; Humans; Male; Phonophoresis; Salicylates; Salicylic Acid; Skin Absorption

Twenty-five patients with symptomatic osteoarthritis (OA) of the knee were treated topically for one week with either 10% trolamine salicylate cream or placebo cream in a randomized double-blind crossover study. No significant difference was found in subjective or objective measures of pain relief between the treatment and control groups. Eight patients preferred "active" test cream, six preferred placebo, and 11 had no preference. No side effects were reported. Topically applied 10% trolamine salicylate cream did not relieve the pain of OA of the knee any more than did placebo.

Topics: Administration, Topical; Clinical Trials as Topic; Double-Blind Method; Female; Humans; Knee Joint; Male; Ointments; Osteoarthritis; Random Allocation; Salicylates

Topics: Administration, Topical; Clinical Trials as Topic; Double-Blind Method; Humans; Ointments; Osteoarthritis; Salicylates

Analgesic balms (AB) are widely used in sports medicine. We previously have examined effects of various counterirritant-based AB on pressor responses evoked by muscular contraction (MC), mediated by group III and IV muscle afferents known to produce exercise and nociceptive responses. Our purpose was to examine trolamine salicylate-based analgesic balm (TS) effects.. Ten healthy, adult male and female cats were used. Decerebration under halothane allowed elimination of anesthesia. Electrical stimulation of L7 and S1 ventral roots evoked static MC (30 s). After control runs, commercial TS (10% concentration) was applied to the skin over the contracting muscles of one hind limb (N = 5). MC was evoked every 10 min, alternating between sides. Ipsilateral (T = 0, T + 20, T + 40, T + 60 min) and contralateral (T - 10, T + 10, T + 30, T + 50 min) responses were analyzed. Five additional cats received AB minus TS.. There were significant attenuations in both peak mean arterial pressure (MAP), in the last 12 s and the last 6 s of the 30 s of MC for both contra- and ipsilateral limbs occurring at T + 50 and T + 60 min after TS application, respectively. No significant changes in heart rate (HR) responses were seen for either the ipsi- or contralateral stimulation. There were no changes in MAP or HR in control cats.. These results indicate that TS affects the end of the 30 s of MC, which is thought to be mainly chemically mediated through group IV afferents. TS represents the salicylate class of AB and has no counterirritant properties. TS works as an inhibitor of cyclooxygenase (prostaglandin formation) and is, at least in part, blood borne.

Topics: Administration, Topical; Analgesics; Animals; Blood Pressure; Cats; Electric Stimulation; Female; Heart Rate; Illinois; Male; Muscle Contraction; Muscle, Skeletal; Pressoreceptors; Salicylates

To determine how changes in cutaneous blood flow induced in-vivo by methylsalicylate (MeSA), compared to non-rubefacient triethanolamine salicylate (TSA), affected topical salicylate absorption and distribution, and to assess formulation therapeutic potential by comparing tissue concentrations to published antiinflammatory concentrations.. Flux of salicylate from MeSA and TSA formulations applied to full-thickness rat skin was determined using in vitro diffusion cells. Anaesthetised rats were then used to quantify salicylate concentrations in plasma and tissues underlying the application site for the two formulations over a 6h period. In vitro and in vivo absorption profiles were then compared and the effect of MeSA on cutaneous blood flow assessed.. In vitro flux of salicylate from the MeSA formulation was 40% higher, though after correcting for differences in formulation concentrations the ratio of permeability coefficients was reversed. Contrary to the in vitro predictions, in vivo tissue and plasma concentrations of salicylate in rats rose rapidly in the first 1 hr and were more than the predicted 1.4-fold higher for MeSA. This effect was mirrored by the increase in blood flow induced by MeSA in human cutaneous vessels and that reported in the literature. Potential therapeutic levels were not seen below superficial muscle layers.. Direct tissue penetration of salicylate occurs below application sites from both MeSA and TSA formulations. Tissue concentrations of MeSA were higher than predicted due to its rapid distribution in the blood.

Topics: Administration, Topical; Animals; Anti-Inflammatory Agents, Non-Steroidal; Laser-Doppler Flowmetry; Male; Rats; Rats, Wistar; Regional Blood Flow; Salicylates; Skin Absorption; Tissue Distribution

The penetration of active ingredients from topically applied anti-inflammatory pharmaceutical products into tissues below the skin is the basis of their therapeutic efficacy. There is still controversy as to whether these agents are capable of direct penetration by diffusion through the tissues or whether redistribution in the systemic circulation is responsible for their tissue deposition below the application site.. The extent of direct penetration of salicylate from commercial ester and salt formulations into the dermal and subcutaneous tissue of human volunteers was determined using the technique of cutaneous microdialysis. We also examined differences in the extent of hydrolysis of the methylester of salicylate applied topically in human volunteers and in vitro skin diffusion cells using full-thickness skin and epidermal membranes.. The present study showed that whilst significant levels of salicylate could be detected in the dermis and subcutaneous tissue of volunteers treated with the methylsalicylate formulation, negligible levels of salicylate were seen following application of the triethanolamine salicylate formulation. The tissue levels ofsalicylate from the methylsalicylate formulation were approx. 30-fold higher than the plasma concentrations.. The absorption and tissue concentration profiles for the commercial methylsalicylate formulation are indicative of direct tissue penetration and not solely redistribution by the systemic blood supply.

Topics: Administration, Topical; Adult; Cells, Cultured; Diffusion; Female; Humans; Hydrolysis; In Vitro Techniques; Male; Microdialysis; Salicylates; Skin; Skin Absorption

Recently, triethanolamine salicylate (TEAS) is frequently being incorporated in several over-the-counter topical analgesic pharmaceutical products. Since the clinical efficacy of such dosage form depends upon the release of the active ingredient at the site of application, the present study was undertaken to study the in vitro release of the (TEAS) from commonly used ointment bases and two most popular commercial products in the U.S. market. Also, the effects of various penetration enhancers, such as, ethanol, propylene glycol, polyethylene glycol-400, dimethyl-sulfoxide (DMSO), polysorbate-80 and urea were evaluated. In general, the drug release from the experimental formulations was higher than the commercial products studied. The inclusion of the penetration enhancing ingredients increased the drug release from some of the formulations evaluated. The hydrophilic emulsion base with 10% ethanol exhibited the best in vitro drug release. The apparent viscosity profiles of the formulations showed no definite relationship with the amounts of drug release. However, significant differences in the (TEAS) release from the experimental formulations were observed.

Topics: Administration, Topical; Chemistry, Pharmaceutical; Ointments; Salicylates

Studies to determine the extent of local tissue penetration of topically applied trolamine [14C]salicylate were conducted in domestic pigs. The preparation was applied onto a 100-cm2 shaved area of skin overlying the biceps femoris at a concentration of 0.7 mg of salicylate/cm2 to closely approximate the actual use in humans. At least 82% of the topically applied trolamine salicylate was absorbed over a 2-h period. Based on blood and muscle salicylate levels, a localization of the absorbed drug occurred in muscle underlying the treated area within 120 min. Muscle from the treated area had a concentration of salicylate that was 13 times that of blood and 49 times that of muscle taken from untreated areas. Blood samples taken from the treated area at 10, 20, and 30 min showed that salicylate levels ranged from 15.8 to 5.3 micrograms/g. Less than 0.5% of the applied drug was excreted in the urine during the 2-h period.

Topics: Administration, Topical; Animals; Female; Kinetics; Muscles; Salicylates; Skin Absorption; Swine

The local, articular, and systemic absorption of oral and topical salicylates was studied in dogs and humans using radioisotope techniques. Topical triethanolamine 14C-salicylate was found capable of percutaneous absorption into the knee joint and surrounding tissues. In dogs, topical salicylate application resulted in higher salicylate concentrations than oral aspirin in a number of tissues, despite lower blood levels. In patients with rheumatoid arthritis, intraarticular 14C-salicylate levels after triethanolamine 14C-salicylate cream were 60 per cent of those obtained with oral aspirin. Four of six patients reported equal improvement in local discomfort after oral and topical salicylates. A potential role for topical salicylate cream in the treatment of localized rheumatic disorders is suggested.

Topics: Absorption; Administration, Oral; Administration, Topical; Animals; Anti-Inflammatory Agents, Non-Steroidal; Aspirin; Dogs; Humans; Knee Joint; Male; Middle Aged; Salicylates; Synovial Fluid; Time Factors; Tissue Distribution

Topics: Amino Alcohols; Chemistry, Pharmaceutical; Ointments; Pharmacy; Research; Salicylates; Spectrum Analysis