C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 5/075 (2006.01) C07K 1/02 (2006.01) C07K 5/072 (2006.01)
Patent
CA 2331819
A methyl ester of N-[N-(3,3-dimethylbutyl)-L-.alpha.-aspartyl]-L-phenylalanine (A-form crystals) having characteristic X-ray diffraction peaks, e.g., at diffraction angles of at least 6.0~, 24.8~, 8.2~, and 16.5~ (2.theta., CuK.alpha. line) is dried to a water content below 3 wt.%. The thus-dried crystals are novel crystals (C-form crystals) of the methyl ester of N-[N-(3,3- dimethylbutyl)-L-.alpha.-aspartyl]-L-phenylalanine which have an excellent rate of dissolution. These crystals, when examined by X-ray powder diffractometry, have characteristic X-ray diffraction peaks at least at diffraction angles of 7.1~, 19.8~, 17.3~, and 17.7~ (2.theta., CuK.alpha. line). When the C-form crystals are in the form of granules, they have further improved solubility.
L'invention concerne un éther méthylique de N-[N-(3,3-diméthylbutyl)-L-.alpha.-aspartyl]-L-.alpha.-phénylalanine (cristaux de forme A) présentant des pics de diffraction aux rayons X caractéristiques, par exemple selon des angles de diffraction d'au moins 6,0·, 24,8·, 8,2·, et 16,5· (2.theta., ligne CuK¿.alpha.?), séché jusqu'à obtenir un contenu en eau inférieur à 3 % en poids. Les cristaux séchés ainsi obtenus sont de nouveaux cristaux (cristaux de forme C) de l'éther méthylique de N-[N-(3,3-diméthylbutyl)-L-.alpha.-aspartyl]-L-.alpha.-phénylalanine, présentant une excellente vitesse de dissolution. Ces cristaux, lorsqu'ils sont examinés par diffraction aux rayons X, présentent des pics de diffraction aux rayons X caractéristiques, selon au moins des angles de diffraction de 7,1·, 19,8·, 17,3· (2.theta., ligne CuK¿.alpha.?). Lorsque les cristaux de forme C se présentent sous forme de granulés, ils améliorent leur solubilité.
Ishida Hirotoshi
Kishishita Akihiro
Nagai Takeshi
Nagashima Kazutaka
Ajinomoto Co. Inc.
Ogilvy Renault Llp/s.e.n.c.r.l.,s.r.l.
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