NOVEL AMORPHOUS FORMS OF PITAVASTATIN CALCIUM

• Main Authors: SCHOENING KAI-UWE, SZELAGIEWICZ MARTIN, BLATTER FRITZ, VAN DER SCHAAF PAUL ADRIAAN
• Format: Patent
• Language: English; Japanese
• Published: 22.03.2018
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

PROBLEM TO BE SOLVED: To provide methods of producing novel amorphous forms of pitavastatin calcium, the novel amorphous forms, and pharmaceutical compositions containing the amorphous forms.SOLUTION: Novel amorphous forms having characteristic peaks in X-ray powder diffraction patterns are produced by adding a non-solvent to an organic solvent solution of (3R,5S)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxy-6(E)-heptanoic acid hemicalcium salt or lyophilizing an aqueous solution of the salt.SELECTED DRAWING: None 【課題】ピタバスタチンカルシウムの新規なアモルファス形態の製造方法、新規なアモルファス形態、及び該アモルファス形態を含む医薬組成物を提供する。【解決手段】（３Ｒ，５Ｓ）−７−［２−シクロプロピル−４−（４−フルオロフェニル）キノリン−３−イル］−３，５−ジヒドロキシ−６（Ｅ）−ヘプテン酸ヘミカルシウム塩の有機溶剤溶液に非溶剤を加えるか、又は上記塩の水溶液を凍結乾燥することにより、Ｘ線粉末回折図形において特徴的なピークを有する新規なアモルファス形態を製造する。【選択図】なし