Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ketone doai
Patent
1986-09-25
1987-10-13
Goldberg, Jerome D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ketone doai
514274, 514454, 514560, 514732, 514789, 424DIG5, A61K 3112, A61K 31505, A61K 3135, A61K 3120
Patent
active
046999299
DESCRIPTION:
BRIEF SUMMARY
The present invention is concerned with new paraffin-based pharmaceutical compositions to be applied to the skin. The invention is particularly concerned with compositions containing readily oxidizable drugs such as dithranol and its derivatives.
One of the drawbacks of the ointment bases used in the treatment of skin diseases is a tendency to spread from the affected skin to the surrounding healthy skin and to clothes. This is particularly detrimental when poorly penetrating ointments are used which contain vaseline, paraffin oil, and soft waxes and which mainly affect the horny layer and the epidermis. It is almost impossible to direct such ointments to the affected skin areas only, and dosage is difficult and extremely variable. This causes problems, especially if the ointment includes agents which irritate the skin or which colour the skin and clothes. One substance that affects the colours healthy skin is dithranol, or anthranil, still the most commonly used pharmaceutical for the topical treatment of psoriasis.
P. G. Unna was the first scientist to develop ointment sticks containing dermatological agents in an attempt to reduce the above drawbacks /Monatschefte fur Praktische Dermatologi 1886:5 157-167/. According to Unna, dry, localised, spot-like skin diseases, such as psoriasis, dry eczemas, and spotty fungal skin diseases are best suited for treatment with ointment sticks. He suggests that the consistency of the ointment stick be sufficiently soft so that little force is needed to apply a stripe of ointment to the skin but, on the other hand, sufficiently hard so that the stick is not deformed when used or when exposed to high temperatures. According to him, these requirements, though dependent on the pharmaceutical used, could be satisfied by mixtures of olive oil and wax. Unna used colophonium as a hardening agent in addition to wax. Unna used yellow beeswax (cera flava). Of the ointment stick formulae suggested by Unna, almost all of which had stick bases of similar compositions, the following two deserve mention: "Stilus acid. salicyl. unguens 10%" (Acid. salicyl. praec. 10.0, Colophoni 5.0, Cerae flavae 45.0, Ol. oliv. prov. 40.0) and "Stilus Chrysarobini unguens 30%" (Chrysarobini 30.0, Colophoni 5.0, Cerae flavae 35.0, Ol. oliv. prov. 30.0).
Unna also developed a paraffin ointment stick (Paraffini solid. 50.0, Paraffini liquid. 50.0), but, owing to the softness of the stick he did not mix any pharmaceutical into the stick, but used the stick for oiling dry, horny skin in the way a lip pomada is used.
Since Unna's pioneering work, there have been very few papers on ointment sticks in the treatment of skin diseases.
In 1941, F. Dietel mentioned the chrysarobin ointment stick for the treatment of psoriasis /Deutsche medizinische Wochenschrift 1941:9 237-9/. The composition of the stick was: Chrysarobin 30.0, Cerae flav. 20.0, Adipis lanae 50.0.
In 1962 and 1966, there were two papers in which a close relative of chrysarobin, cignolin (or dithranol) was used in ointment sticks/Weber, G., Medizinische Welt 1962:35 1839-40 and Schafe, M. K., Zeitschrift fur Hautund Geschlechtskrankheiten 1966 XL 347-51/. In both papers, the same commercial preparation "Psoriacid" was used. The exact composition of the ointment base was not given, but it included Vaselinium album, Adeps lanae, Paraff. solidum suffanita and Cera alba.
In 1970, F. Novotny used the following ointment stick base in his study: Oleum ricini 1.0, Paraffinum liquidum 4.0, Cera flava 43.0, Oleum cacao 52.0, /Cs. Derm. 45 (1970):1 20-22/.
At present, only one ointment stick is available as a commercial preparation in the Nordic countries. This is an "Anthraderm" stick containing 0.5, 1.0 or 2.0% dithranol (Pharma-medica). The composition of the ointment base has not been given as a percentage, but the base contains wool alcohols, cocoa oil, white beeswax, whale wax (cetaceum), and peanut oil (oleum arachidis) as well as 0.5% salicylic acid and 0.02% butylated hydroxytoluene as stabilizers.
Even though stick-shaped preparations would be a g
REFERENCES:
patent: 3957969 (1976-05-01), Fujiyama et al.
patent: 4327114 (1982-04-01), Brickl et al.
Heikinheimo Hanna-Maija
Mustakallio Kimmo K.
Sothmann Gunnar A.
Goldberg Jerome D.
Kilcoyne John M.
Orion-yhtyma Oy
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