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PubMedDate not supplied

Combination of calcipotriol and clobetasol propionate as a premixed ointment for the treatment of psoriasis.

The treatment of psoriasis requires good compliance, efficacy and low toxicity because of its long-term course and wide distribution. The aim of the study was to compare the efficacy of a once daily application of calcipotriol alone or calcipotriol and a superpotent steroid in a premixed form in patients with psoriasis. The monotherapy group of 32 patients with stable plaque psoriasis received 0.005% calcipotriol alone once daily. The combination group of 29 patients was treated once per day with 0.004% calcipotriol/0.01% clobetasol propionate as a premixed ointment. Eruption score of truncal involvement was evaluated. The combination regimen was more efficacious than the monotherapy as evidenced by (1) more patients with at least 50% reduction in the eruption score after 2 weeks, (2) lower eruption score after 6 weeks and later, and (3) less adverse effects. The combined once-per-day application of 0.004% calcipotriol/0.01% clobetasol propionate as a premixed ointment is a promising regimen for psoriasis.

Administration, Cutaneous↗
PubMed2001

[In situ IR study of the reaction behavior of transition metal oxides-propionic acid system, Fe2Cr(mu 3-O) (mu-O2CC2H5)6(H2O)3Cl.xH2O and Cr3 (mu 3-O) (mu-O2CC2H5)6(H2O)3NO3.xH2O].

The reaction behavior of the title complexes have been investigated by means of in situ IR in nitrogen atmosphere. It has been found that they enabled the propionic acid to convert to acetaldehyde and pentanone in different temperature. The sequence of the ketonization reaction activity for metal oxides Fe3O4 > MnO2 > Cr2O3 > Co2O3 > Ni2O3 has analogy to that for metal clusters [Fe2MnOPH] > [Fe3OPH] > [Fe2CrOPH] > [Fe2CoOPH] > [Fe2NiOPH] > [Cr3OPH][OPH = (mu 3-O)(mu-O2CC2H5)6(H2O)3]. For the ketonization reactions, the reaction temperatures of transition-metal oxides were much higher than that of corresponding metal clusters [Fe2MOPH]. It has been verified that the active component of metal cluster [Fe2MOPH] is not the corresponding transition-metal oxides. The difference between Fe3O4 and Fe2O3 which catalyze the conversion of propionic acid to acetaldehyde and pentanone respectively were demonstrated.

English Abstract↗
PubMedDate not supplied

Treatment of Hailey-Hailey disease with tacrolimus ointment and clobetasol propionate foam.

Hailey-Hailey disease, or familial benign chronic pemphigus, is a chronic disease without a known cure. Current therapeutic strategies attempt to suppress Hailey-Hailey outbreaks and allow the patient to live comfortably with this condition. We have found that applying topical tacrolimus 0.1% ointment (Protopic) twice a day to affected areas is an excellent way to control Hailey-Hailey disease. In addition to effectively controlling Hailey-Hailey outbreaks, tacrolimus is a relatively safe and noninvasive mode of treatment, without significant side effects. We recommend intermittent therapy with clobetasol propionate 0.05% foam (Olux Foam) for patients who break through suppressive therapy with tacrolimus a few times per year. In patients with frequent outbreaks of Hailey-Hailey disease despite suppressive therapy with tacrolimus, we recommend alternating the tacrolimus with clobetasol propionate 0.05% foam every 6 weeks.

Clobetasol↗
PubMed2001

Use of lactic and propionic acid bacteria in the production of fermented parsley juice.

Taking into consideration the proliferation rate of Propionibacterium sp. cells, pH changes and sensory properties of the fermented product obtained, selection of propionic acid bacteria (PAB) was made in order to determine their usefulness for the production of fermented parsley juice. The analysis included 12 strains, belonging to the following species: P. thoenii (4 strains), P. jensenii (6 strains), P. freudenreichii (1 strain) and P. acidipropionici (1 strain). The experiments show that many strains of propionic acid rods develop well in parsley juice, allowing to achieve the desired taste qualities of the product. The Propionibacterium strains selected by elimination were used as components of vaccine containing: Lactobacillus plantarum, Lactococcus lactis ssp. lactis, Saccharomyces cerevisiae.

Beverages↗
PubMed2005

An open label study of clobetasol propionate 0.05% and betamethasone valerate 0.12% foams in the treatment of mild to moderate acne keloidalis.

Acne keloidalis (AK) is a disease affecting primarily African American men. Topical steroids are a widely accepted treatment of AK; however, no studies have been published investigating their effectiveness. The purpose of this open-label study was to assess the efficacy and tolerability of clobetasol propionate 0.05% and betamethasone valerate 0.12% foams in the treatment of AK in 20 African American patients. These patients were treated for 8 to 12 weeks using a pulsed-dose regimen. We found topical clobetasol propionate foam to be effective in improving AK, and our patients found the foam vehicle to be cosmetically acceptable.

Acne Keloid↗
PubMedDate not supplied

Anti-inflammatory properties of tixocortol 17-butyrate,21-propionate (JO 1222), a novel, locally acting corticosteroid.

Tixocortol 17-butyrate,21-propionate (JO 1222) is a novel, locally acting, C-21 thioester-linked corticosteroid with significant activity in a number of models of inflammation. In models of acute inflammation, JO 1222 had an ED30 of 3 micrograms in carrageenan-induced oedema, an ED50 of 5 ng in croton oil-induced inflammation, and 4 micrograms and 2 micrograms/pleural cavity in carrageenin-induced pleurisy in the rat and mouse respectively. In a model of subchronic inflammation JO 1222 had an ED50 of 39 micrograms/pellet (cotton pellet-induced granuloma) and an ED50 of 13 ng in oxazolone-induced hypersensitivity. The overall relative potency was found to be beclomethasone DP greater than betamethasone DP = JO 1222 greater than hydrocortisone 17-butyrate,21-propionate greater than hydrocortisone acetate. In contrast to any of the other corticosteroids, including beclomethasone DP, JO 1222 did not have any marked systemic effects in any of the above models following oral or local administration. Furthermore, in contrast to other locally acting corticosteroids such as beclomethasone DP, JO 1222 had little or no effect on the thymus or body weight. These findings suggest that JO 1222 is a novel, potent, locally acting corticosteroid with little or no systemic effects and thus has therapeutical potential in diseases such as asthma, arthritis, ulcerative colitis and rhinitis.

Adrenal Cortex Hormones↗
PubMed1990

[Antiproliferative activity of a highly purified coal tar preparation in comparison with clobetasol-17-propionate].

Coal tar and glucocorticosteroids are among the preparations used for the treatment of hyperproliferative inflammatory dermatosis. Coal tar generally seems to have a better effect on psoriasis capillitii than betamethasone-17-valerate. This finding is confirmed by investigations with human skin fibroblasts. The coal tar preparation Berniter has a strongly inhibitory effect on cell proliferation. The action of the preparation with tar can be clearly distinguished from the effect of the vehicle. At the ED50 concentration of the substance with tar, the vehicle without tar causes no inhibition. Based on weight equivalents Berniter has a greater inhibitory effect on proliferation of human skin fibroblasts than clobetasol-17-propionate. In the case of both substances protein biosynthesis is only affected at concentrations higher than those needed for the inhibition of proliferation. Berniter and the vehicle without tar have an equally strong effect on protein synthesis. Berniter affects the nucleoside triphosphatase bound to the nuclear membrane, and thus influences the nucleocytoplasmic transport of mRNA. The effect of the vehicle and the preparation containing tar on this parameter are very similar. Berniter has a positive effect on cell mobility. In preconfluent cultures the mobility of the cell is slightly increased and in confluent cultures significantly. Our results show that Berniter inhibits proliferation in cell cultures of human skin fibroblasts to a higher degree than clobetasol-17-propionate. It is to be assumed that neither the inhibition of protein synthesis nor the inhibition of mRNA transport play a causal role in the antiproliferative effect of coal tar. Inhibition of proliferation as a result of general damage to the cell can also be practically ruled out.

Adenosine Triphosphatases↗
PubMedDate not supplied

The metabolism of alpha-aminobenzo(b)thiophene-3-propionic acid (the sulfur analog of tryptophan) in the rat.

The biotransformation of 3H-labeled alpha-aminobenzo[b]thiophene-3-propionic acid (the sulfur analog of tryptophan) was investigated in rats. Forty-eight hours after ip administration, 80% of the radioactive dose was recovered in the urine and 5% in the feces; tissue levels of radioactivity accounted for the remainder of the administered dose. The urinary metabolites were identified by a combination of thin-layer chromatography, gas chromatography, and gas chromatography-mass spectrometry, and were quantitated by thin-layer chromatography and liquid-scintillation counting to give, as percentages of the administered dose, unchanged alpha-aminobenzo[b]thiophene-3-propionic acid (20.6%), benzo[b]thiophene-3-acetic acid (1.3%), benzo[b]thiophene-3-pyruvic acid (14.2%), benzo[b]thiophene-3-lactic acid (4.9%), and N-(benzo[b]thiophene-3-acetyl)glycine (46.2%).

Animals↗
PubMed1986

Hydrolysis of hydrocortisone 17-butyrate 21-propionate by cultured human keratinocytes.

Hydrolysis of 17-butyrate 21-propionate (HBP) by human keratinocytes was studied using an in vitro system. In the culture of human keratinocytes 1.308 nmole/ml of hydrocortisone 17-butyrate (de-esterified HBP at the position of 21) was found at 1 h after the addition of 10 nmole/ml HBP. At 6 h most of HBP was de-esterified to become HB17 and a small amount of hydrocortisone 21-propionate (de-esterified HBP at the position of 17) was detected. Hydrocortisone (HC) was not detectable. These results indicate that when HBP is applied on the skin, it is hydrolyzed at the position of 21, and reaches the dermis where it finds the way to get into the systemic circulation. The intracellular concentration of HBP was estimated to be more than 5 times its extracellular concentration and its accumulation was higher than HC. These results were discussed in relation to the potentiation of local antiinflammatory action and the reduction of systemic effects of topical glucocorticoid.

Administration, Topical↗
PubMed1989

Intrinsic potencies of novel thiol ester corticosteroids RS-85095 and RS-21314 as compared with clobetasol 17-propionate and fluocinonide.

The intrinsic potencies of two novel topical thiol ester corticosteroids, RS-85095 and RS-21314, were compared with the high potency corticosteroids clobetasol 17-propionate and fluocinonide, using human vasoconstriction assays. In these assays, four or five concentrations (0.03 to 3 mg/L) of the corticosteroids in 95% ethanol (alcohol, USP) were applied to predetermined sites on the forearm of volunteers and were occluded following evaporation of the alcohol. The responses were scored in terms of the presence or absence of vasoconstriction and the degree of vasoconstrictive intensity. No statistically significant difference was found in the intrinsic potencies of RS-85095, RS-21314, and clobetasol 17-propionate, and all three corticosteroids were significantly more potent than fluocinonide.

Administration, Topical↗
PubMed1989

Hindering of tumor lung metastasizing with alpha-(4-cyclohexylphenyl)propionic acid in mice.

Alpha-(4-cyclohexylphenyl)propionic acid, a potent inhibitor of platelet aggregation, has appeared to reduce the quantity and size of Lewis lung carcinoma (LLC) tumor nodules in the lungs. The number of animals developing the tumor colonies in the lungs was decreased by 34% to 49% either when the tumor cells were injected i.v. and alpha-(4-cyclohexylphenyl)propionic acid was administered during 3 days, or when the tumor cells were transplanted i.m. The primary tumor was removed 6 days later and the drug administered during 8 or 21 days.

Animals↗
PubMed1988

Contact allergy to clobetasol propionate.

Two cases of contact allergy to clobetasol propionate are described. Neither patient had positive epicutaneous tests to other structurally similar fluorinated steroids or to other steroids with the propionate ester, but both had multiple positive tests within the European standard battery. Comparison with previously reported cases reveals that multiple contact allergies are a frequent finding in patients with allergy to this topical steroid.

Administration, Topical↗
PubMed1988

Human pharmacokinetics of erythromycin propionate-N-acetylcysteinate: comparative evaluation with erythromycin stearate and N-acetylcysteine.

The pharmacokinetic pattern of erythromycin propionate-N-acetylcysteinate (EPAC) (erythromycin stinoprate I.N.N.), a new derivative, was studied on 12 healthy volunteers after single and multiple oral treatments. Microbiological and/or HPLC analytical methods were used to titer either erythromycin as base, propionate and total or N-acetylcysteine (NAC). In the acute experiment, a comparative evaluation was performed with erythromycin stearate (ES) and with N-acetylcysteine, according to a randomized-multi-crossover design. EPAC showed a better bioavailability than ES with longer-lasting serum levels of active antibiotic. NAC concentrations in the serum after EPAC were practically identical to those found after an oral administration of NAC alone. The multiple treatment study, performed in the same 12 volunteers with only EPAC, indicated that the pharmacokinetic pattern is somewhat different from that observed after a single dose, since higher concentrations were present at the steady state conditions.

Acetylcysteine↗
PubMed1987

Optical resolution and configuration of 2-(4-dimethylvinylphenyl)propionic acid.

Optical resolution of (+/-)-2-(4-dimethylvinylphenyl)propionic acid (I) was performed through fractional crystallization of its salts with (S)-(-)- and (R)-(+)-alpha-phenylethylamine. 2-(4-Dimethylvinylphenyl)propionic acid, in comparison to ibuprofen, has greater antiinflammatory, analgesic and antipyretic activities, as well as a higher therapeutic index. Absolute configuration was determined by comparison of the (S)-(-)-alpha-phenylethylamide 1H-N.M.R. spectra of the enantiomers of (I) and of the enantiomers of ibuprofen whose configuration was already known. Thus, the absolute configuration (S) was assigned to (+)-(I).

Chromatography, High Pressure Liquid↗
PubMed1986

Comparative toxicity study of hydrocortisone 17-butyrate 21-propionate (HBP) ointment and other topical corticosteroids in rats.

Comparative systemic and topical toxicity in male rats treated on the dorsal skin for 14 consecutive days with a volume of 0.15 g/100 g (body weight) of 0.1% hydrocortisone 17-butyrate 21-propionate (HBP) ointment, 0.05% clobetasol propionate (CP) ointment, 0.1% predonisolone 17-valerate 21-acetate (PVA) ointment and 0.1% diflucortolone valerate (DV) ointment was studied. In all the treated groups body weight gain was suppressed, serum concentration of total cholesterol and triglycerides increased and the lymphatic tissues and skin were atrophic. The DV and CP groups had adrenal atrophy and renal lesions, and the DV group also had gastric and hepatic lesions. The systemic effect of HBP ointment was weaker than that of the other drugs (DV greater than CP much greater than PVA greater than HBP). All the drugs significantly reduced the skin fold thickness in treated areas throughout the application period. The dermal atrophic effect of HBP ointment was also relatively weaker than that of the other drugs. From the above evidence, it was concluded that HBP ointment was less toxic than the other topical corticosteroids.

Administration, Topical↗
PubMed1985

The molecular morphology of bovine heart mitochondrial NADH-ubiquinone reductase. Cross-linking with dithiobis(succinimidyl propionate).

The molecular morphology of NADH-ubiquinone reductase (complex I) was investigated by cross-linking with the cleavable bifunctional reagent, dithiobis(succinimidyl propionate). Cross-linking inhibits the following activities of the complex--NADH----3-acetylpyridine adenine dinucleotide (oxidized), NADH----2,6-dichloroindophenol, NADH----ferricyanide, and NADH----menadione--to different degrees with the greatest inhibition occurring with either ferricyanide or 3-acetylpyridine adenine dinucleotide as electron acceptor. Addition of 150 microM NADH affords partial protection from inhibition. Cross-linking quenches the FMN fluorescence of complex I (288 nm excitation/515 nm emission), and addition of 150 microM NADH greatly reduces the quenching. Treatment of complex I (1 mg/ml) for 2 min with dithiobis(succinimidyl propionate) (0.2 mg/ml) at 4 degrees C revealed a cross-linked product consisting of the following seven subunits: 75-80, 53-57, 42, 33-35, 24-27, 17-18, and 12.5-15.5 kDa. Five minutes of treatment cross-linked the unidentified polypeptides of 69 and 51 kDa to six of the seven complex I subunits, but the 12.5-15.5-kDa subunit may be missing from this cross-linked product, while 15 min of treatment cross-linked additional unidentified polypeptides of 177, 107, 72, and 63 kDa. Since longer times of cross-linking result in a larger number of unidentifiable polypeptide spots, the shorter cross-linking time results are taken as a more accurate picture of the native enzyme conformation. This would indicate that within complex I the following subunits are within 12 A of each other at one or more points in space: 75-80, 53-57, 42-45, 33-35, 24-27, 17-18, and, perhaps, 12.5-15.5 kDa. These subunits represent portions of all three fractions of the enzyme, i.e. flavoprotein, iron-protein, and insoluble or hydrophobic fractions.

Animals↗
PubMed1985

Neighboring proteins in rat liver 60 S ribosomal subunits disulfide-linked by hydrogen peroxide oxidation or cross-linked with dithiobis(succinimidyl propionate).

Neighboring proteins in rat liver 60 S ribosomal subunits were investigated by two kinds of cross-linking techniques: treatment of 60 S subunits with 1) hydrogen peroxide, which promotes the formation of protein-protein disulfide linkages and 2) a disulfide-bridged bifunctional reagent dithiobis(succinimidyl propionate). The cross-linked protein complexes formed were separated by two-dimensional polyacrylamide gel electrophoresis in a basic-sodium dodecyl sulfate gel system under nonreducing conditions. Each complex in the gel was labeled with 125I and extracted under reducing conditions. The protein components of the complex were analyzed by two kinds of two-dimensional polyacrylamide gel electrophoresis, followed by autoradiography. Closely neighboring pairs disulfide-linked by hydrogen peroxide were identified as L4-L6, L4-L29, L6-L29, L18a-L29, and L29-L32; more distant pairs cross-linked with dithiobis(succinimidyl propionate) were identified as L3-L5, L3-L24, L3-L37a, L4-L14, L4-L18a, L5-L10, L5-L11, L7/L7a-L27, L7/L7a-L36, L13-L35, and L13a-L14.

Animals↗
PubMedDate not supplied

[Effectiveness of using Maliutka and Malysh adapted propionic-acidophilus mixtures in the combined treatment of congenital hypotrophy].

The physical and psychomotor development, immune responsiveness, and intestinal microflora were studied in 82 infants with congenital hypotrophy depending on the nutrition pattern. It was shown that children who received the propionic-acidophilic mixtures Malyutka and Malush manifested the highest daily weight gain, the most rapid disappearance on the manifestations of food allergy, an increase in immune responsiveness. A decrease in the cultivation rate of Proteus vulgaris and pathogenic staphylococcus, as well as an increase in the cultivation of bifidobacteria. The data obtained permit recommending the use of the propionic-acidophilic mixtures Malyutka and Malysh in combined treatment of children with congenital hypotrophy.

Body Weight↗