PARENTERAL PHARMACEUTICAL FORM WHICH RELEASES AROMATASE INHIBITOR AND GESTAGEN, FOR TREATMENT OF ENDOMETRIOSIS

• Main Authors: HEINZ SCHMITZ, RUDOLF KNAUTHE, HENRIIKKA KOROLAINEN, CHRISTINE TALLING, HARRI JUKARAINEN, ARTO PAKKALIN
• Format: Patent
• Language: English; Japanese
• Published: 08.09.2016
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

PROBLEM TO BE SOLVED: To apply active ingredients in a formulation with controlled release avoiding high fluctuations of serum levels which could trigger counterregulation by the pituitary-ovarian-axis in order to avoid counterregulatory effects of the pituitary-ovarian-axis with the highest possible dose of AI on the one hand and to achieve the best contraceptive efficacy with the highest possible dose of gestagen below the ovulation inhibition dose on the other hand.SOLUTION: Provided is a parenteral dosage form releasing an aromatase inhibitor in a daily release rate that does not induce stimulation of the ovaries by negative feed-back of the pituitary-ovarian-axis and a gestagen in a daily release rate below the ovulation inhibition dose but high enough to provide reliable contraceptive protection.SELECTED DRAWING: Figure 1 【課題】一方で最も高い可能性のある用量のＡＩで下垂体−卵巣−軸の対抗制御作用を回避し、他方で排卵阻害用量より少ない最も可能性のある用量のゲスターゲンで最大の避妊効能を達成するために、下垂体−卵巣−軸によって対抗制御をトリガーしうる血清レベルの高い変動を回避する放出を制御する処方にて活性成分を適用すること。【解決手段】アロマターゼ阻害剤を下垂体−卵巣−軸のネガティブフィードバックにより卵巣の刺激を誘発しない一日当たりの放出速度で放出し、かつゲスターゲンを排卵阻害用量よりも低いが、信頼できる避妊的保護を提供するのに十分に高い一日当たりの放出速度で放出する、非経口用剤形。【選択図】図１