Synalar
Solid-state investigation of fluocinolone acetonide.

Bartolomei M, Ramusino MC, Ghetti P.

Laboratorio di Chimica del Farmaco, Istituto Superiore di Sanita, Rome, Italy.

Three crystalline modifications of fluocinolone acetonide, A, B and C, were characterized by means of FTIR, DSC, TG-FTIR, MICRO-FTIR and X-ray diffractometry. They were easily differentiated by their IR absorption bands in the 3600-3400 cm-1 range. The thermal behavior was also elucidated using combined techniques; thermomicroscopy and thermogravimetry coupled with Fourier transform infrared spectroscopy were found to be very useful tools for a better understanding of thermal events. On heating, form A and C were fully converted into form B. Polymorph A was found to be enantiotropically related to B, while form C was monotropically related to B. The existence of three polymorphs was confirmed by means of their different X-ray diffraction patterns. Detailed methods of preparation of the three modifications are also described.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9278884&dopt=Abstract fluocinolone Synalar



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Effect of percutaneous absorption of fluocinolone acetonide on the activity of superoxide dismutase and total antioxidant status in patients with psoriasis.

Gavan N, Popa R, Orasan R, Maibach H.

Department of Dermatology, Cluj Napoca, Romania.

This study defines a modification of antioxidant systems by percutaneous absorption of fluocinolone acetonide. Total antioxidant status (TAS) provides an overall indication of antioxidant status. Superoxide dismutase (SOD), a primary antioxidant, accelerates the dismutation of the toxic superoxide radical produced during the oxidative energy processes into the less harmful molecules, hydrogen peroxide and molecular oxygen. We monitored the level of SOD and TAS in 7 males with psoriasis and 6 control subjects before and after a single application of fluocinolone acetonide 0.025% ointment to 90% of the body. The results showed that the plasma level of TAS was significantly increased (p < 0.02) at 24 h posttreatment. The erythrocytic level of SOD was significantly decreased (p < 0.01) only at 12 h after glucocorticosteroid application. The level of TAS and SOD in patients with psoriasis was also significantly increased (p < 0.01 for both situations) as compared to healthy controls. Our study suggests that fluocinolone acetonide as a therapeutic agent may play a role in the oxidative stress in skin diseases.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9413891&dopt=Abstract fluocinolone Synalar



Synalar
Corticosteroid contact hypersensitivity screening in Singapore.

Khoo BP, Leow YH, Ng SK, Goh CL.

National Skin Centre, Singapore.

BACKGROUND: Topical corticosteroids have been in use since 1957. Two percent to 5% of patients attending patch test (PT) clinics have problems with corticosteroid contact hypersensitivity. Controversies abound with regard to the choice of steroids in the standard battery, the method of patch testing and reading, and the ideal concentration and vehicle. OBJECTIVE: To assess betamethasone 17-valerate (1% pet.), fluocinolone acetonide (0.25% petrolatum [pet.]), and tixocortol pivalate (1% pet.) used in the authors' standard battery. METHODS: Data were analyzed for patients seen between January 1994 and December 1996 who had positive PT reactions to one or more of these steroids. RESULTS: 3,603 patients had standard PTs, of which 20 had positive reactions to one or more of these steroids. There were three positive reactions to betamethasone 17-valerate, 17 to tixocortol, and none to fluocinolone. On further patch testing to the authors' steroid battery, only one tixocortol-positive patient had a positive reaction to hydrocortisone (1% ethanol/ dimethyl sulfoxide [DMSO]). CONCLUSIONS: Corticosteroid allergy is found to be relatively uncommon in Singapore on the basis of this screening series. The frequency of negative reactions to fluocinolone acetonide is sufficiently low for this corticosteroid to be excluded from the authors standard series. The significance of positive tixocortol reactions remains unknown. From the review of other relevant literature, the authors recommend that budesonide be added to their present series. Testing betamethasone 17-valerate in 1% ethanol may yield more positive allergic reactions. Individuals with a positive allergic PT reaction to one corticosteroid should subsequently be tested to a full corticosteroid series.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9601908&dopt=Abstract fluocinolone Synalar



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[Comparative studies in man on the percutaneous absorption of diflucortolone valerate, betamethasone-17-valerate, beclomethasone dipropionate and fluocinolone acetonide]

[Article in German]

Tauber VU, Amin M, Fuchs P, Speck U.

Percutaneous absorption of 6alpha,9-difluor-11beta-hydroxy-16alpha-methyl-21-valeryloxy-1,4-pregnadience-3,20-dione (diflucortolone valerate, DFV, Nerisona), betamethasone 17-valerate (BV), beclomethasone dipropionate (BDP) and fluocinolone acetonide (FA) by damaged skin was examined on the backs of 4 healthy males from whom the stratum corneum had been removed by "stripping". The determination of percutaneous absorption was performed on the one hand by a method employing radioactive labelled compounds (DFV, BV) and measuring the elimination with the urine and faeces and on the other hand by photometric determination (DFV, BV, BD, fa) of the corticoid remaining on the skin immediately following application and at the end of a 24-h period of exposure. Direct measurement of the radioactivity in the urine and faeces revealed that percutaneous absorption from a new W/O emulsion takes place up to 2.2+/-0.8% in the case of DFV (0.1%) and to at least 12.2+/-3.3% in the case of BV (0.12%) within 24 h. The determination of percutaneous absorption via recovery from the skin produced the following results for the 4 corticoid preparations examined: DFV (14.8+/-4.2%) and BDP (14.0+/-4.3%) approximately equal, BV (23.5+/-4.1%) a marked increase and FA (39.2+/-2.4%) the highest level of absorption. This order for percutaneous absorption appears to correlate to the frequency of systemic side effects.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1036945&dopt=Abstract fluocinolone Synalar



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Effect of fluocinolone acetonide cream on human skin blood flow.

Chimoskey JE, Holloway GA Jr, Flanagan WJ.

Blood flow rate was measured in the forearm skin of human subjects exposed to ultraviolet irradiation. Blood flow was determined by the 133Xe disappearance technique 18 hr after ultraviolet (UV) irradiation with a Westinghouse RS sunlamp held 10 inches from the skin for 10 min. Ultraviolet irradiation caused skin blood flow to increase. Application of fluocinolone acetonide cream, 0.025%, 4 times in the 16 hr following UV irradiation had no effect on either control skin blood flow or the UV-induced hyperemia.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1151118&dopt=Abstract fluocinolone Synalar