Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – 9,10-seco- cyclopentanohydrophenanthrene ring system doai
Patent
1995-04-28
1997-03-18
Cook, Rebecca
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
9,10-seco- cyclopentanohydrophenanthrene ring system doai
A61K 4744
Patent
active
056123272
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This is a 371 of PCT/JP94/01443 filed Sep. 1, 1994.
The present invention relates to a novel 1.alpha.,24-(OH).sub.2 --V.D.sub.3 cream composition. More specifically, the present invention relates to a 1.alpha.,24-(OH).sub.2 --V.D.sub.3 cream composition having a good skin permeability of the active ingredient 1.alpha.,24-(OH).sub.2 --V.D.sub.3. Still more specifically, the present invention relates to a 1.alpha.,24-(OH).sub.2 --V.D.sub.3 cream composition having a good skin permeability of the active ingredient 1.alpha.,24-(OH).sub.2 --V.D.sub.3, having an improved chemical stability of the active ingredient 1 .alpha.,24-(OH).sub.2 --V.D.sub.3, superior in physical stability as a cream composition, and superior in feeling at the time of application to the skin.
BACKGROUND ART
1.alpha.,25-(OH).sub.2 --V.D.sub.3 (1.alpha.,25-dihydroxylcholecalciferol), 1.alpha.,24-(OH).sub.2 --V.D.sub.3 (1.alpha.,24-dihydroxylcholecalciferol), etc. exhibit a Ca-homeostasis regulating action, which is known as a biological action of V.D.sub.3, and therefore, are called active-type V.D.sub.3 s. The biological actions of active type V.D.sub.3 s are diverse. In addition to the above-mentioned Ca-homeostasis regulating action, mention may be made of an action of bone formation, an action of inducing cell differentiation, an action of suppressing the secretion of the para-thyroid hormone, etc. Among these, regarding the Ca-homeostasis regulating action, the above substances are already being clinically administered as oral formulations for treatment of osteoporosis, osteomalacia, and other so-called osteopenia and are recognized to have superior therapeutic effect. On the other hand, clinical application has been studied for the action in inducing cell differentiation, though later than with the Ca-homeostasis regulating action. In particular, since the hard-to-cure skin disease of psoriasis is considered to be caused by the incomplete undifferentiation and accelerated proliferation of epidermic cells, application of active-type V.D.sub.3 s has been studied. As psoriasis is a disease of the epidermis, the outer layer of the skin, local administration to the affected location of the skin is more advantageous over oral administration, injection, and other general administration in terms of bioavailability and also enables prevention of general side effects, and is therefore considered as a best method of administration.
Dosage forms for local skin administration include ointments, creams, and other semisolid agents, tape agents, cataplasms, powder agents, etc., but when considering the symptoms of psoriasis, semisolid agents are best. As a 1.alpha.,24-(OH).sub.2 --V.D.sub.3 ointment, the present inventors have already disclosed a formula for an water-free ointment (see the specification of Japanese Examined Patent Publication (Kokoku) No. 3-68009). Good therapeutic effects have been reported by this water-free ointment, but since the base of the ointment is white petrolatum, it is not possible to avoid an oily, sticky feeling after application. Therefore, there has been a need for an external formulations improved in the feeling when applied onto the face etc.
Cream compositions include large amounts of water, and therefore, are not sticky as with ointments and have been used for a long time as external agents. They are classified by composition into two types of emulsion type cream compositions, that is, oil-in-water types (O/W) or water-in-oil types (W/O), as well as aqueous gel type cream compositions. A comparison of these three types by the state when rubbed on the skin shows that the aqueous gel type cream compositions suffer from the problem of the gel base polymer precipitating on the skin, while the water-in-oil type (W/O) emulsion cream compositions suffer from the problem that the white color and other external colors do not easily vanish. As opposed to this, oil-in-water type (O/W) emulsion cream compositions are advantageous in that the white color and other external colors easily vanish.
However, in
REFERENCES:
patent: 4871723 (1989-10-01), Makino et al.
CA 105: 30074, Makino, 1986.
Makino Yuji
Matugi Hideo
Suzuki Yoshiki
Cook Rebecca
Teijin Limited
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