Betamethasone dipropionate ointment

The betamethasone dipropionate and citric acid are dissolved in the triacetin with mixing and heat to 35°C if needed. 

The microcrystalline wax, propylene glycol stearate, and mineral oil are melted together by heating to 75°-85°C while stirring to make the oleaginous phase. 

After cooling the oleaginous phase to about 55°C, the tiacetin solution is added while mixing to make a homogenous dispersion. Mixing should be of sufficient intensity to disperse the triacetin solution finely and uniformly. 

Mixing is continued while cooling at room temperature. 

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Betamethasone dipropionate cream, ointment 0.05% Clobetasol propionate cream, ointment 0.05% Diflorasone diacetate 0.05%... 

Experimental studies on the percutaneous absorption of hydrocortisone fail to reveal a significant increase in absorption when applied on a repetitive basis and a single daily application may be effective in most conditions. Ointment bases tend to give better activity to the corticosteroid than do cream or lotion vehicles. Increasing the concentration of a corticosteroid increases the penetration but not proportionately. For example, approximately 1% of a 0.25% hydrocortisone solution is absorbed from the forearm. A 10-fold increase in concentration causes only a fourfold increase in absorption. Solubility of the corticosteroid in the vehicle is a significant determinant of the percutaneous absorption of a topical steroid. Marked increases in efficacy are noted when optimized vehicles are used, as demonstrated by newer formulations of betamethasone dipropionate and diflorasone diacetate. 

Simonsen L, Hoy G, Didriksen E et al, (2004) Development of a new formulation combining calcipotriol and betamethasone dipropionate in an ointment vehicle. Drug Development and Industrial Pharmacy 30 1095-1102. 

The therapeutic effectiveness of topically applied corticosteroids is attributed primarily to their antiinflammatory activity. The relative efficacy of topical corticosteroids appears to be in the following order hydrocortisone, prednisolone, betamethasone < hydrocortisone valerate or butyrate, betamethasone valerate, triamcinolone acetonide, flucinolone acetonide < betamethasone dipropionate, fluocino-nide. In addition to the nature of the corticosteroid, its solubility, and, to a lesser extent, the concentration used, clinical efficacy is influenced by the formulation of the preparation. Glucocorticoids appear to have greater efficacy when formulated in ointment bases than in cream or lotion vehicles. This could be attributed to the occlusive effect provided by ointments. The application of an occlusive dressing further enhances penetration and persistence of the steroid (reservoir effect) in the stratum corneum. " ... 

The percutaneous absorption of high-potency topical glucocorticoids has been documented, but hypothalamic-pituitary-adrenal axis suppression, leading to clinically significant adrenal insufficiency or Cushing s syndrome, is infrequent. Two patients developed adrenal suppression after the unregulated use of betamethasone dipropionate 0.05% ointment (about 80 g/week) or clobetasol 0.05% ointment (up to 100 g/week), obtained without prescription to treat psoriasis (362). 

Betamethasone dipropionate 0.05% (Diprosone) Cream, ointment, lotion... 

Figure 14.10 Release rates of betamethasone dipropionate from ointments into various receptor fluids. 0), 5% hexane in acetonitrile (2), octanol (3), acetonitrile (4), 60°/o acetonitrile in water (5), 95% ethanol Cdata from Zatz et al. 1996).

Zatz, J. L., J. Varsano, and V. P. Shah. 1996. In vitro release of betamethasone dipropionate from petrolatum-based ointments. Pharm. Dev. Technol. 1 293-298. 

This particular study was a single-centre, investigator-blinded, within-subject randomised, active and vehicle-controlled, intraindividual comparison of six topical products in patients with psoriasis vulgaris. The products evaluated were caldpotriol ointment (50 jig/g), calcipotriol cream (50 jig/g), two-compoxmd ointment (calcipotriol 50 jig/g and betamethasone dipropionate 0.5 mg/g), two-compound gel (calcipotriol 50 jig/g betamethasone dipropionate 0.5 mg/g), an investigational ointment (calcipotriol 25 gg/g hydrocortisone lOmg/g), and a vehicle control. 

Betamethasone valerate is analysed in a sample of ointment used for treating haemorrhoids, the related steroid beclomethasone dipropionate is used as an internal standard. The following data were produced ... 

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