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PubMed1989

Antiinflammatory action of salicylates: aspirin is not a prodrug for salicylate against rat carrageenin pleurisy.

A current hypothesis postulates that the antiinflammatory effect of aspirin (acetylsalicylic acid) is mediated by its metabolite salicylic acid through inhibition of PGE2 synthesis. We tested this hypothesis in rats with carrageenin-induced pleurisy. Aspirin or salicylate, given orally, reduced exudation and cell migration into the pleural cavity, aspirin being more potent than salicylate. The antiinflammatory effect of aspirin cannot be explained only in terms of salicylate formation. Doses of aspirin and salicylate that inhibit inflammation by 50% result in salicylate levels in the exudate of 70 +/- 12 and 323 +/- 17 micrograms/ml, respectively. At a significant antiinflammatory dose (100 mg/kg), salicylate did not reduce the prostaglandin and thromboxane content of the exudate. This indicates that inhibition of cyclooxygenase is not a likely mechanism for the antiinflammatory effect of salicylate. Salicylate only reduced the amount of 6-keto-PGF1 alpha in the exudate at higher doses (200 mg/kg), while aspirin at an equally antiinflammatory dose (50 mg/kg) reduced the content of 6-keto-PGF1 alpha, TXB2, PGD2 but not of PGE2 in the exudate. It therefore seems unlikely that an inhibition of PGE2 synthesis is the common mechanism by which aspirin and salicylate exert their antiinflammatory effects. These results do not supported the hypothesis that aspirin is a prodrug for salicylate but rather indicate that both compounds may exert their antiinflammatory effects partly by different mechanisms.

Animals↗

PubMed2003

Plasma salicylate from methyl salicylate cream compared to oil of wintergreen.

BACKGROUND: Poison Control Centers follow the acetylsalicylic acid (ASA) treatment guideline to manage unintentional ingestions of topical methyl salicylate liniments. For example, one teaspoon of 30% methyl salicylate cream such as Ben Gay provides an "ASA equivalent dose" of 180 mg/kg for a 10 kg child. The ASA treatment guideline advises emesis with syrup of Ipecac and 24 h home followup for this dose. Both the ASA conversion factor to yield the ASA equivalent dose and the treatment guideline assume 100% bioavailability of the salicylate. The nature of this topical dosage product led the investigators to expect less than complete absorption of methyl salicylate. OBJECTIVE: To compare plasma concentrations of salicylate from ingested methyl salicylate cream with plasma concentrations of salicylate from ingested oil of wintergreen. METHODS: Four adult volunteers consented to an open label, four-way crossover design, with randomization to the following treatments: 1 mL Oil of Wintergreen, U.S.P., 6.7 g of Ben Gay 15% and 20 g of Ben Gay 15% and also to hold 5 g of Ben Gay 15% cream in the buccal cavity for 1 minute and then expectorate. Plasma was collected for salicylate determination, and the results analyzed with a noncompartmental pharmacokinetic model. RESULTS: No plasma salicylate was detected after buccal treatment phase. Relative bioavailability for the low-dose treatment was 0.5 compared to oil of wintergreen. CONCLUSION: Plasma salicylate concentrations from methyl salicylate cream are not equal to those achieved after ingestion of oil of wintergreen. Dosage formulation must be considered when predicting toxicity.

Absorption↗

PubMed1991

Symptomatic salicylate ototoxicity: a useful indicator of serum salicylate concentration?

A three phase study was designed to define further the sensitivity and specificity of symptomatic salicylate ototoxicity (primarily tinnitus) for serum salicylate concentrations. In phase one 260 patients with osteoarthritis and 112 with rheumatoid arthritis, none taking salicylates, were interviewed about their ear symptoms. Their responses were not significantly different from those of 134 salicylate treated patients with rheumatoid arthritis previously reported. In the second phase 56 patients who were taking salicylates, and who volunteered the complaint of tinnitus, had serum salicylate concentrations measured while symptomatic, and 30 (54%) had concentrations less than 1.3 mmol/l. Few tolerated an upward salicylate dose adjustment. For phase three, 94 patients were found to have a salicylate concentration above 2.2 mmol/l on one or more occasion, and these subjects were interviewed. Fifty two patients (55%) had no tinnitus, and tinnitus correlated with the blood salicylate concentration in only 28 (30%). Audiological evaluation of most of the symptomatic patients was carried out, and results were abnormal in the majority, even in those patients not reporting tinnitus. Symptomatic salicylate ototoxicity is too nonspecific and too insensitive to be a useful indicator of serum salicylate concentration.

Adult↗

PubMed2001

Salicylic acid in the serum of subjects not taking aspirin. Comparison of salicylic acid concentrations in the serum of vegetarians, non-vegetarians, and patients taking low dose aspirin.

AIMS: To determine serum salicylic acid concentrations in non-vegetarians and vegetarians not taking salicylate drugs, and to compare these concentrations with those found in patients taking aspirin, 75 mg daily. METHODS: Serum samples were obtained from vegetarians (n = 37) and non-vegetarians (n = 39) not taking salicylate drugs. Non-vegetarians and vegetarians were recruited from the community and from a Buddhist monastery, respectively, in Dumfries and Galloway, Scotland. Patients (n = 14) taking aspirin (75 mg daily) were recruited from the Dumfries diabetic clinic. Serum salicylic acid concentrations were determined using a high performance liquid chromatography method with electrochemical detection. RESULTS: Salicylic acid was detected in every serum sample analysed. Higher serum concentrations of salicylic acid were found in vegetarians than non-vegetarians: median concentrations of 0.11 (range, 0.04-2.47) micromol/litre and 0.07 (range, 0.02-0.20) micromol/litre, respectively; the median of the difference was 0.05 micromol/litre (95% confidence interval for difference, 0.03 to 0.08; p < 0.0001). The median serum concentration of salicylic acid in patients taking aspirin (75 mg daily) was 10.03 (range, 0.23-25.40) micromol/litre, which was significantly higher than that found in non-vegetarians and vegetarians. There was overlap in serum salicylic acid concentrations between the vegetarians and patients taking aspirin. CONCLUSIONS: Salicylic acid, a non-steroidal anti-inflammatory drug, is present in fruits and vegetables and is found in higher concentrations in vegetarians than non-vegetarians. This suggests that a diet rich in fruits and vegetables contributes to the presence of salicylic acid in vivo. There is overlap between the serum concentrations of salicylic acid in vegetarians and patients taking aspirin, 75 mg daily. These findings may explain, in part, the health promoting effects of dietary fruits and vegetables.

Adult↗

PubMed2002

New formulation of chemical peeling agent: 30% salicylic acid in polyethylene glycol. Absorption and distribution of 14C-salicylic acid in polyethylene glycol applied topically to skin of hairless mice.

Salicylic acid is used in chemical peeling procedures. However, they have caused many side effects, even salicylism. To achieve a salicylic acid peeling that would be safer for topical use, we recently developed a new formulation consisting of 30% salicylic acid in polyethylene glycol (PEG) vehicle. In an extension of our previous research, we studied the absorption of 30% salicylic acid labeled with 14C in PEG vehicle applied topically to the intact and damaged skin of male hairless mice. An ointment containing 3 mg salicylic acid in 10 mg vehicle was applied to both groups. In animals with intact skin, 1 h after application the plasma concentration of radioactivity was 1665.1 ng eq/ml, significantly lower than the 21437.6 ng eq/ml observed in mice with damaged skin. Microautoradiograms of intact skin showed that the level of radioactivity in the cornified cell layer was similar at 6 h after application. However, in damaged skin, the overall level of radioactivity showed a decrease by 3 h after application. In the carcasses remaining after the treated intact and damaged skin had been removed, 0.09 and 11.38% of the applied radioactivity remained, respectively. These findings confirm that 30% salicylic acid in PEG vehicle is little absorbed through the intact skin of hairless mice, and suggest that salicylism related to absorption through the skin of quantities of topically applied salicylic acid is not likely to occur in humans with intact skin during chemical peeling with this preparation. This new preparation of 30% salicylic acid in PEG vehicle is believed to be safe for application as a chemical peeling agent.

Absorption↗

PubMed2006

Comparison of the effects of pulsed dye laser, pulsed dye laser + salicylic acid, and clobetasole propionate + salicylic acid on psoriatic plaques.

BACKGROUND: Studies show that pulsed dye laser (PDL) has some clinical benefits on psoriasis with a low clearance rate. In addition, it has been suggested that applying keratolytics before treatment might be helpful in PDL therapy. Topical corticosteroids remain the most commonly prescribed agents for psoriasis. OBJECTIVE: This study was designed to compare the efficacy of the PDL treatment with that of PDL treatment after salicylic acid on psoriatic plaques. The other goal of this study was to compare the efficacy of the PDL treatment with that of clobetasol propionate treatment. METHODS: Twenty-two patients with chronic, stable psoriatic plaques that involved less than 20% of their body were included in the study. Three similar-appearing psoriasis plaques in these patients were selected. Whereas the first plaque received only PDL, the second plaque received PDL after salicylic acid, and the third plaque received clobetasol propionate ointment and salicylic acid. Evaluation of the study plaques was carried out by the modified Psoriasis Area and Severity Index (mPASI) score and by measuring the area of the plaques. RESULTS: Of the 21 patients, 19 completed the study. Although the decrease in mPASI scores was determined to be maximum for clobetasol propionate + salicylic acid-treated plaques and minimum for only PDL-treated plaques, the decrease was statistically significant in all groups when compared with baseline (p < .003). At the 3- and 6-week evaluations, there was a statistically significant difference between clobetasol propionate + salicylic acid-treated plaques and the two PDL-treated plaques (p < .003); however, the difference observed at the 9-, 12-, and 15-week evaluations was statistically significant only between clobetasol propionate + salicylic acid-treated plaques and PDL-treated plaques (p < .003). When the baseline and 15-week evaluations were compared, there was no statistically significant increase in the mean lesion areas of clobetasol propionate + salicylic acid-treated psoriatic plaques (p > .003), but there was a statistically significant increase in the mean lesion areas of two PDL-treated psoriatic plaques (p < .003). CONCLUSION: The results of this study showed that the effect of PDL could be increased when salicylic acid was added to treatment, although there was no statistically significant difference between both treatment protocols. However, clobetasol propionate + salicylic acid treatment is more effective than both PDL and PDL + salicylic acid treatment.

Adult↗

PubMed1990

Potentiation by salicylate and salicyl alcohol of cadmium toxicity and accumulation in Escherichia coli.

The toxicity of Cd2+ in Escherichia coli K-12 was potentiated by salicylate and several related compounds. The efficiency of plating on Luria broth plates was reduced by more than 10(5)-fold when 10 mM salicylate and 200 microM CdCl2 were present simultaneously but was unaffected when either compound was present by itself. Synergistic effects were found at pH 7.4 with certain other weak acids (acetyl salicylate [aspirin], benzoate, and cinnamate) and with a nonacidic salicylate analog, salicyl alcohol, but not with acetate or p-hydroxy benzoate. Thus, the synergism with Cd2+ is determined by the structure of the compounds and not merely by their acidity. The kinetics of 109Cd2+ uptake by cells grown and assayed in broth indicated the presence of two uptake systems with Kms of 1 and 52 microM Cd2+ and Vmaxs of 0.059 and 1.5 mumol of Cd2+ per min per g of cells, respectively. The kinetics of uptake for cells grown and assayed with 20 mM salicyl alcohol showed 2.5-fold increases in the Vmaxs of both systems but no change in the Kms. Salicylate-grown cells also exhibited increased rates of 109Cd2+ uptake by both systems. Thus, enhanced uptake of Cd2+ may be responsible for the potentiation of Cd2+ toxicity by salicylate and salicyl alcohol.

Acetates↗

PubMed1990

Salicylates and proton transport through lipid bilayer membranes: a model for salicylate-induced uncoupling and swelling in mitochondria.

Mechanisms of proton transport were investigated in phospholipid bilayer membranes exposed to salicylates and benzoates. Membranes were formed from diphytanoyl phosphatidylcholine in decane plus chlorodecane (50% vol/vol). Proton and anion conductances (GH and GA) were calculated from the total conductances and the H+ or A diffusion potentials produced by transmembrane H+ or A gradients. At low pH salicylate caused a GH which was proportional to the square of the total weak acid concentration, and GH was maximum when pH = pK. At neutral to alkaline pH salicylate caused a GA which was proportional to the first power of the salicylate concentration, and GA was independent of pH. Both GH and GA were inhibited by phloretin. The results suggest that salicylate acts as an HA2-type proton carrier at low pH and as a lipid-soluble anion at neutral pH. Salicylate has been implicated as a causal factor in Reye's syndrome, as well as in aspirin poisoning, and salicylate has been reported to increase the proton conductance of inner mitochondrial membranes. The present results suggest that in mitochondria salicylate increases passive proton uptake by a combination of HA influx (driven by the concentration gradient) and A efflux (driven by the voltage and concentration gradients). Model calculations suggest that over the range of therapeutic to toxic concentrations, salicylate causes net H+ influx sufficient to explain the reported "loose coupling," uncoupling and swelling of mitochondria. The relative ineffectiveness of aspirin and benzoate can be explained by their low A permeabilities, whereas the ineffectiveness of 2,6-dihydroxybenzoate can be explained by its low pK.

Anions↗

PubMed1991

Preparation and evaluation of Eudragit gels. II: In vitro release of salicylic acid, sodium salicylate, and ketoprofen from Eudragit L and S organogels.

The in vitro dissolution characteristic of salicylic acid, sodium salicylate, and ketoprofen from Eudragit L and S organogels was investigated by the rotation disk method. The dissolution pattern of salicylic acid and erosion of Eudragit L polymer from the organogels followed apparent zero-order kinetics, providing strong evidence for a surface erosion mechanism and negligible diffusional release of salicylic acid. On the other hand, the dissolution of salicylic acid from Eudragit S organogels was a linear function of the square root of time. The apparent dissolution rate of salicylic acid from Eudragit S organogels increased with increasing temperature from 32 to 42 degrees C and agitation rate from 50 to 200 rpm. A linear relationship was obtained between the logarithm of apparent dissolution rate constants and the reciprocal of absolute temperatures. The activation energy for release of salicylic acid from Eudragit S organogels was in the range of 2.99 to 5.57 kcal/mol. From various experimental results, it was concluded that the release process of salicylic acid from Eudragit S organogels was diffusion controlled through the organogels matrix.

Acrylic Resins↗

PubMed1996

Urinary salicylate excretion in subjects eating a variety of diets shows that amounts of bioavailable salicylates in foods are low.

Intake of acetylsalicylic acid reduces the risk of cardiovascular disease and is associated with a decreased risk for colorectal cancer. Amounts of salicylates in foods are thus of interest, but data are scarce and controversial. We gave 58 mumol (10.5 mg) pure acetylsalicylic acid or 66 mumol (9.1 mg) salicylic acid to six volunteers and recovered 77-80% in 24-h urine samples. Thus, urinary excretion is a valid indicator for intake of free forms of (acetyl)salicylic acid. To estimate the bioavailable salicylate contents of diets, we subsequently studied salicylate excretion in 17 volunteers from 14 countries and four continents who ate a wide variety of self-selected diets. Median 24-h urinary salicylate excretion was 10 mumol (range: 6-12 mumol). Values increased with the fiber content of the diet (r = 0.73), suggesting that vegetable foods are the main sources of salicylates. However, amounts of salicylates in a variety of diets are evidently low and probably insufficient to affect disease risk.

Adult↗

PubMed1988

The effects of salicylate concentration on the uptake of salicylate and cefmetazole into rat isolated small intestinal epithelial cells.

The uptake of salicylate into rat isolated small intestinal epithelial cells reached an equilibrium within 15 min, but that of cefmetazole alone did not. The presence of salicylate at concentrations greater than 50 mM accelerated the uptake of cefmetazole, which reached equilibrium within 5 min. At equilibrium, the uptake clearance of salicylate (mumol (g protein)-1 M-1 initial salicylate concn) was greater than that of cefmetazole. The uptake clearance of salicylate during the first several minutes was concentration-dependent, and a 'super-uptake' clearance of salicylate, greater than equilibrium values, was observed when 100 mM salicylate was present. This indicates that some mechanism, other than a simple diffusion process, may be involved in salicylate uptake into these cells.

Animals↗

PubMed1980

Comparative plasma salicylate and urine salicylurate levels following administration of aspirin, magnesium salicylate, and choline magnesium trisalicylate.

Eighteen healthy volunteers were administered single doses of commercially available solid dosage forms of aspirin, magnesium salicylate (I), and choline magnesium trisalicylate (II), equivalent to approximately 500 mg of salicylic acid, in a randomized, complete crossover design. Plasma salicylate and urine salicylurate levels were measured by high-pressure liquid chromatography at frequent intervals following dosing; the resultant profiles, areas under the curve (AUC), and percentages of dose excreted as salicylurate were statistically analyzed by an analysis of variance. The plasma salicylate levels following the two dosage forms containing I and II were virtually identical when corrected for small differences in the dose. The plasma salicylic acid level following aspirin was approximately 10% lower during the 1.5--3.0-hr interval due to a portion of unhydrolyzed aspirin, but the dose-corrected AUC for the products tested did not differ significantly (p < 0.05). During the 24 hr following dosing, 66.5 +/- 12.1 68.4 +/- 7.1, and 60.9 +/- 14.1% of the salicylic acid were excreted as urine salicylurate for aspirin, I, and II, respectively, with no significant difference (p < 0.05). Based on this study, there are no significant differences in the rate and extent of absorption of salicylate following the three dosage forms tested, and the elimination kinetics of salicylic acid are not altered by these dosage forms.

Adolescent↗

PubMedDate not supplied

Liquid chromatographic determination of salicylate and methyl salicylate in blood and application to a postmortem case.

A liquid chromatographic method is presented for the quantitation of salicylate and methyl salicylate in blood. It employs an initial alkaline extraction to separate methyl salicylate from salicylate. Methyl salicylate is then hydrolyzed to salicylate, extracted under acidic conditions and chromatographed. This method was used in an attempt to identify methyl salicylate and salicylate in a postmortem case.

Chromatography, Liquid↗

PubMed1977

Blood and saliva salicylate measurement in the monitoring of salicylate therapy.

Total and free plasma salicylate as well as saliva salicylate was measured in 13 patients with rheumatoid arthritis treated with different doses of acetylsalicylic acid alone. Although the clinical response was judged moderately effective to effective in all cases, total and free plasma salicylate varied markedly. Saliva salicylate correlated well with both total plasma salicylate and fre plasma salicylate. Determination of saliva salicylate may be a simple and useful technique for the monitoring of salicylate therapy.

Adult↗

PubMed1996

Medicated oils and severe salicylate poisoning: quantifying the risk based on methyl salicylate content and bottle size.

In Hong Kong, medicated oils containing methyl salicylate account for 48% of acute salicylate poisoning cases treated in the general medical ward of the Prince of Wales Hospital. To quantify better the risk to average persons who have intentionally ingested these medicated oils, the methyl salicylate content and bottle size of 7 commonly available formulations were examined. Koong Yick Hung Far Oil had the highest methyl salicylate content (67%) and was available only in 60-ml bottles. If the entire bottle of this product were ingested, the equivalent of 184 adult 300-mg aspirin tablets would have been swallowed. Accidental ingestions of as little as 6 ml of Koong Yick Hung Far Oil by a child can be fatal. Six other products contained 15-40% methyl salicylate and their biggest bottle sizes range from 28-57 ml. Among medicated oils commonly found in Hong Kong, Koong Yick Hung Far Oil poses the greatest threat for severe salicylate poisoning if swallowed because of its high salicylate content and its availability in 60-ml bottles. The threat from medicated oils can probably be reduced by restricting their bottle size and methyl salicylate concentration. Physicians and clinical toxicologists should appreciate the toxic potential of these products.

Adult↗

PubMed1976

Effect of nonionic surfactants on percutaneous absorption of salicylic acid and sodium salicylate in the presence of dimethyl sulfoxide.

Fifteen nonionic surfactants, 10% (w/w), were each incorporated into white petrolatum USP ointment base containing 10% (w/w) salicylic acid or 11.6% (w/w) sodium salicylate with 10% (w/w) dimethyl sulfoxide. Percutaneous absorption was determined from blood salicylate levels in New Zealand white rabbits at regular intervals for 8 hr following application of the ointment. Percutaneous absorption of salicylic acid was increased significantly when sorbitan monopalmitate, sorbitan trioleate, poloxamer 231, poloxamer 182, polyoxyethylene 4 lauryl ether, polyoxyethylene 2 oleyl ether, or polyoxyl 8 stearate was added to the ointment containing dimethyl sulfoxide, salicylic acid, and white petrolatum. Percutaneous absorption of sodium salicylate was increased significantly when sorbitan monolaurate, sorbitan monopalmitate, or poloxamer 182 was added to the ointment containing dimethyl sulfoxide, sodium salicylate, and white petrolatum.

Animals↗

PubMed1981

Salicylate-aspirin interaction in the rat. Evidence that salicylate accumulating during aspirin administration may protect vascular prostacyclin from aspirin-induced inhibition.

Aspirin inhibits cyclooxygenase, thus preventing thromboxane A2 production in blood platelets and prostacyclin in vascular cells. Aspirin is rapidly hydrolyzed to salicylate in the circulation. The objectives of this study were (a) to evaluate whether administration of salicylate, though ineffective by itself, prevents the inhibitory effect of aspirin on platelet and/or vascular cyclooxygenase activity; (b) to verify whether salicylate accumulating in blood after aspirin administration interferes with the pharmacological activity of further doses of aspirin. Pretreatment of rats with sodium salicylate (25-100 mg/kg i.p.) resulted in dose-related prevention of the effect of a subsequent dose of aspirin (2.5-10 mg/kg i.v.) on both platelet and vascular cells. Sodium salicylate appeared to amplify the greater response of platelets to aspirin compared with vessel wall. Pretreatment of rats with repeated high doses of aspirin (200 mg/kg) resulted after 24 h in blood salicylate levels (150-200 microgram/ml) that significantly prevented the inhibitory effect of a subsequent dose of aspirin on newly synthesized vascular prostacyclin. Blood salicylate levels obtained after 36 or 48 h (less than 50 microgram/ml) were too low to blunt aspirin's effect. The interference with aspirin of its major endogenous metabolite should be borne in mind when interpreting results obtained with high dose aspirin or during repeated administration of this drug.

Animals↗

PubMedDate not supplied

Salicylic acid and PEG-contained polyanhydrides: synthesis, characterization, and in vitro salicylic acid release.

Poly [bi(o-carboxyphenyl)adipate-polyethylene glycol] anhydrides--P(BOCA-PEG)--polymeric drugs were synthesized and characterized by Fourier transformed infrared spectroscopy, NMR, DSC, gel permeation chromatography, etc. Salicylic acid loading efficiency of these polymers ranged from 43.5% to 71.3%, which was much higher than that of other polymeric drugs with salicylic acid. The in vitro release of salicylic acid from the polymers was carried out in buffer conditions with different pH values and and rat gastrointestinal contents. The results showed the release rate of salicylic acid increased with the increase of PEG content in the polymers and the increase of pH value of degradation buffer solution. The rat cecal contents also greatly promoted the release of salicylic acid. In 0.1M phosphate buffer solution at pH8.0, 37 degrees C containing 5% rat cecal contents, P(BOCA-PEG200)(80:20) had 15% salicylic acid released in 21 hr, indicating its potential use in colon-specific salicylic acid delivery.

Animals↗