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1. (WO2012124907) I- AND II-TYPE CRYSTALS OF L-Α-GLYCERYL PHOSPHORYL CHOLINE, AND METHOD FOR PREPARING SAME
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2012/124907    International Application No.:    PCT/KR2012/001331
Publication Date: 20.09.2012 International Filing Date: 22.02.2012
IPC:
C07F 9/09 (2006.01), C07C 211/63 (2006.01), C07B 61/00 (2006.01)
Applicants: HANSEOCHEM CO.,LTD. [KR/KR]; 1206-14, Poseung-eup, Pyeongtaek-si Gyeonggi-do 451-820 (KR) (For All Designated States Except US).
OH, Min-Keun [KR/KR]; (KR) (For US Only).
KIM, Ki-Nam [KR/KR]; (KR) (For US Only).
SEO, Ki-Hyeong [KR/KR]; (KR) (For US Only).
KWON, Dae-Gil [KR/KR]; (KR) (For US Only)
Inventors: OH, Min-Keun; (KR).
KIM, Ki-Nam; (KR).
SEO, Ki-Hyeong; (KR).
KWON, Dae-Gil; (KR)
Agent: AJU KIM CHANG&LEE; (Seocho-dong, Saint Hiyan Building) 12-13th Floor, 174 Saimdong-ro, Seocho-gu Seoul 137-860 (KR)
Priority Data:
10-2011-0022392 14.03.2011 KR
10-2011-0022393 14.03.2011 KR
Title (EN) I- AND II-TYPE CRYSTALS OF L-Α-GLYCERYL PHOSPHORYL CHOLINE, AND METHOD FOR PREPARING SAME
(FR) CRISTAUX DE TYPE I ET II DE L-Α-GLYCÉRYL PHOSPHORYL CHOLINE ET LEUR PROCÉDÉ DE PRÉPARATION
(KO) L-α-글리세릴 포스포릴 콜린의 I형 및 II형 결정과 그 제조방법
Abstract: front page image
(EN)The present invention relates to I- and II-type crystals of L-α-glyceryl phosphoryl choline, and to a method for preparing same. More particularly, the present invention relates to noble I- and II-type anhydride crystals of L-α-glyceryl phosphoryl choline, which have a higher purity than conventional liquid L-α-glyceryl phosphoryl choline, and one advantage of which is that formulations and dosages of pharmaceuticals are easily modified, and another advantage of which is that the hygroscopicity of the crystals are much lower than that of conventional polymorphic crystals, providing excellent stability during storage. The present invention also relates to a method for preparing the I- and II-type crystals of L-α-glyceryl phosphoryl choline. The I-type crystal of L-α-glyceryl phosphoryl choline is characterized by having an onset temperature of 147°C and an absorption peak of 150°C based on differential scanning calorimeter (DSC) analysis, and by having diffraction patterns where 2θ-diffraction angles are 9.8±0.2°, 12.0±0.2°, 14.3±0.2°, 15.8±0.2°, and 19.6±0.2° based on X-ray diffraction (XRD) analysis. The II-type crystal of L-α-glyceryl phosphoryl choline is characterized by having an onset temperature of 62°C and an absorption peak of 66°C, and an onset temperature of 141°C and an absorption peak of 145°C based on DSC analysis, and having diffraction patterns where 2θ-diffraction angles are 10.3±0.2°, 12.2±0.2°, 13.4±0.2°, 14.8±0.2°, and 20.6±0.2° based on XRD analysis.
(FR)La présente invention concerne des cristaux de type I et II de L-α-glycéryl phosphoryl choline et leur procédé de préparation. Plus particulièrement, la présente invention concerne des cristaux d'anhydride de type I et II nobles de L-α-glycéryl phosphoryl choline, qui ont une pureté plus élevée que de la L-α-glycéryl phosphoryl choline liquide classique et dont un avantage est que des formulations et formes posologiques de produits pharmaceutiques sont aisément modifiées, et dont un autre avantage est que l'hygroscopicité des cristaux est bien inférieure à celle de cristaux polymorphes classiques, fournissant une excellente stabilité pendant le stockage. La présente invention concerne également un procédé de préparation des cristaux de type I et II de L-α-glycéryl phosphoryl choline. Le cristal de type I de L-α-glycéryl phosphoryl choline est caractérisé en ce qu'il possède une température de début de 147°C et un pic d'absorption de 150°C sur la base d'une analyse au calorimètre différentiel à balayage (DSC), et en ce qu'il possède des motifs de diffraction où des angles de diffraction 2θ sont 9,8±0,2°, 12,0±0,2°, 14,3±0,2°, 15,8±0,2° et 19,6±0,2° sur la base d'une analyse par diffraction des rayons X (XRD). Le cristal de type II de L-α-glycéryl phosphoryl choline est caractérisé en ce qu'il possède une température de début de 62°C et un pic d'absorption de 66°C, et une température de début de 141°C et un pic d'absorption de 145°C sur la base d'une analyse DSC, et en ce qu'il possède des motifs de diffraction où des angles de diffraction 2θ sont 10,3±0,2°, 12,2±0,2°, 13,4±0,2°, 14,8±0,2° et 20,6±0,2° sur la base d'une analyse XRD.
(KO)본 발명은 L-α-글리세릴 포스포릴 콜린의 I형 및 II형 결정과 그 제조방법에 관한 것으로서, 더욱 상세하게는 종래의 액상 L-α-글리세릴 포스포릴 콜린 원료에 비해 순도가 높을 뿐 아니라 제제학적으로 제형 및 용량 변경이 용이한 장점이 있고, 또한 종래의 다형 결정에 비해 흡습성(吸濕性)이 매우 낮기 때문에 저장 안정성이 우수한 장점이 있는 새로운 무수물 형태의 L-α-글리세릴 포스포릴 콜린 I형 및 II형 결정과 그 제조방법에 관한 것이다. 상기 L-α-글리세릴 포스포릴 콜린 I형 결정은 시차주사 열량(DSC) 분석에서 147℃의 개시온도(onset)와 150℃의 흡열피크를 가지며, 분말 X선 회절(XRD) 분석에서 2θ 회절각이 9.8±0.2°, 12.0±0.2°, 14.3±0.2°, 15.8±0.2°, 19.6±0.2°의 회절 패턴을 가지는 것을 특징으로 한다. 상기 L-α-글리세릴 포스포릴 콜린 II형 결정은 시차주사 열량(DSC) 분석에서 62℃의 개시온도(onset) 및 66℃의 흡열피크와, 141℃의 개시온도(onset) 및 145℃의 흡열피크를 가지며, 분말 X선 회절(XRD) 분석에서 2θ 회절각이 10.3±0.2°, 12.2±0.2°, 13.4±0.2°, 14.8±0.2°, 20.6±0.2°의 회절 패턴을 가지는 것을 특징으로 한다.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language: Korean (KO)
Filing Language: Korean (KO)