Unit galenical form for local hormonotherapy of vaginal dryness

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/565 (2006.01) A61K 9/00 (2006.01) A61K 9/06 (2006.01) A61K 9/51 (2006.01)

Patent

CA 2233919

This galenical form in intended to a local treatment, essentially non systemic, of the vaginal dryness, particularly in menopaused women. It comprises a free natural oestrogen, particularly in micronized or vectorized, selected amongst 17.beta.-estradiol and its salts in solution or in suspension in a lipophilic agent, with an oestrogen contents corresponding to a unit dose equivalent to 15 µg at the most, preferably less than 10 µg of 17.beta. estradiol, a bioadhesive gelifying hydrophilic agent, a gelifying agent of the lipophilic agent and a hydrodispersible agent. It comprises on the one hand, in the form of a soft capsule, an external solid hard or soft envelope containing gelatine and glycerin and, on the other hand, a liquid or semi-liquid internal phase containing the lipophilic agent with the oestrogen in solution or in suspension, the bioadhesion agent and the gelifying hydrophilic agent of the lipophilic agent. In a sustained release ovule form, it comprises a solid hard or semi-soft non aqueous homogeneous phase containing the lipophilic agent with the oestrogen in solution or in suspension, the hydrophilic bioadhesive gelifying agent, the gelifying agent of the lipophilic agent and the hydrodispersible agent.

Cette forme galénique est destinée à un traitement local, essentiellement non systémique, de la sécheresse vaginale, notamment chez la femme ménopausée. Elle comprend un estrogène naturel libre, notamment micronisé, ou bien vectorisé, choisi parmi le 17.beta.-estradiol et ses sels en solution ou en suspension dans un agent lipophile, avec une teneur en estrogène correspondant à une dose unitaire équivalente d'au plus 15 µg, de préférence moins de 10 µg, de 17.beta.-estradiol, un agent hydrophile gélifiant bioadhésif, un agent gélifiant de l'agent lipophile et un agent hydrodispersible. Sous forme de capsule molle, elle comprend, d'une part, une enveloppe externe solide dure ou molle contenant de la gélatine et de la glycérine et, d'autre part, une phase interne liquide ou semi-liquide non aqueuse contenant l'agent lipophile avec l'estrogène en solution ou en suspension, l'agent de bioadhésion et l'agent hydrophile gélifiant de l'agent lipophile. Sous forme d'ovule à libération prolongée, elle comprend une phase homogène solide dure ou semi- molle non aqueuse contenant l'agent lipophile avec l'estrogène en solution ou en suspension, l'agent hydrophile gélifiant bioadhésif, l'agent gélifiant de l'agent lipophile et l'agent hydrodispersible.

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