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1. (WO2018223894) LONG-ACTING SLOW-RELEASE PHARMACEUTICAL PREPARATION AND PREPARATION METHOD THEREFOR
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Pub. No.: WO/2018/223894 International Application No.: PCT/CN2018/089383
Publication Date: 13.12.2018 International Filing Date: 31.05.2018
IPC:
A61K 9/16 (2006.01) ,A61K 47/34 (2017.01) ,A61K 45/00 (2006.01) ,A61K 31/519 (2006.01) ,A61K 31/496 (2006.01) ,A61P 25/18 (2006.01) ,A61P 25/28 (2006.01) ,A61P 31/12 (2006.01) ,A61P 35/00 (2006.01) ,A61P 25/36 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
14
Particulate form, e.g. powders
16
Agglomerates; Granulates; Microbeadlets
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
30
Macromolecular compounds
34
Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45
Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519
ortho- or peri-condensed with heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
496
Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
18
Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
28
for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12
Antivirals
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
30
for treating abuse or dependence
36
Opioid-abuse
Applicants:
广州帝奇医药技术有限公司 AC PHARMACEUTICALS CO., LTD. [CN/CN]; 中国广东省广州市 国际生物岛螺旋三路8号第3层301、302、303单元 Suite 301-303, Building 8, 3rd Luoxuan Road, Guangzhou International Bio-Island, Guangzhou, Guangdong 510300, CN
Inventors:
赖树挺 LAI, Shuting; CN
郑阳 ZHENG, Yang; CN
曹付春 CAO, Fuchun; CN
连远发 LIAN, Yuanfa; CN
刘锋 LIU, Feng; CN
Agent:
广州华进联合专利商标代理有限公司 ADVANCE CHINA IP LAW OFFICE; 中国广东省广州市 天河区花城大道85号3901房 Room 3901, No. 85 Huacheng Avenue, Tianhe District, Guangzhou, Guangdong 510623, CN
Priority Data:
201710425540.807.06.2017CN
Title (EN) LONG-ACTING SLOW-RELEASE PHARMACEUTICAL PREPARATION AND PREPARATION METHOD THEREFOR
(FR) PRÉPARATION PHARMACEUTIQUE À LIBÉRATION LENTE À ACTION PROLONGÉE ET SON PROCÉDÉ DE PRÉPARATION
(ZH) 一种长效缓释药物制剂及其制备方法
Abstract:
(EN) Disclosed is a long-acting slow-release pharmaceutical preparation. The pharmaceutical preparation contains 25%-60% of a water-insoluble or sparingly-soluble drug and 40%-75% of a high-molecular polymer. After the pharmaceutical preparation is subjected to one time of intramuscular injection administration, the ratio of a maximum plasma concentration to a minimum plasma concentration in a main release period is less than 5; the slope of a linear trend line of a cumulative release curve is less than 8 under an in-vitro simulated release condition; the daily release amount is less than 8.5%; and the simulated release condition is a buffer solution with the temperature of 37±0.5°C and the pH of 6.5-8.4. The prepared long-acting slow-release pharmaceutical preparation in the present invention has the beneficial effects that an obvious release delay period or a burst release phenomenon are avoided after administration, a steady state plasma concentration can be quickly achieved, the plasma concentration with a relatively small fluctuation range can be maintained in several weeks or longer after single administration, and the pharmaceutical preparation can take effect quickly and has good compliance with a patient.
(FR) L'invention concerne une préparation pharmaceutique à libération lente à action prolongée. La préparation pharmaceutique contient 25 % à 60 % d'un médicament insoluble dans l'eau ou peu soluble et 40 % à 75 % d'un polymère à poids moléculaire élevé. Après que la préparation pharmaceutique est soumise à un temps d'administration par injection intramusculaire, le rapport d'une concentration plasmatique maximale à une concentration plasmatique minimale dans une période de libération principale est inférieur à 5; la pente d'une ligne de tendance linéaire d'une courbe de libération cumulative est inférieure à 8 dans une condition de libération simulée in vitro; la quantité de libération quotidienne est inférieure à 8,5 %; et la condition de libération simulée est une solution tampon ayant la température de 37±0.5°C et le pH de 6,5 à 8,4. La préparation pharmaceutique à libération lente à action prolongée préparée dans la présente invention a les effets bénéfiques qu'une période de retard de libération évidente ou phénomène de libération initiale rapide à très court terme (également bien connu sous l'anglicisme « burst release ») sont évités après l'administration, une concentration plasmatique à l'état stable peut être obtenue rapidement, la concentration plasmatique avec une plage de fluctuation relativement petite peut être maintenue pendant plusieurs semaines ou plus après une administration unique, et la préparation pharmaceutique peut prendre un effet rapidement et présente une bonne conformité avec un patient.
(ZH) 本发明公开了一种长效缓释药物制剂,所述药物制剂包括25~60%的水难溶性或微溶性药物和40-75%的高分子聚合物,所述药物制剂在单次肌肉注射给药后,主要释放期内的最高血药浓度和最低血药浓度的比值小于5;在体外模拟释放条件下,累计释放曲线的线性趋势线的斜率小于8;日释放量小于8.5%,所述模拟释放条件为37±0.5℃、pH为6.5-8.4的缓冲溶液。本发明制备的长效缓释药物制剂给药后无明显释放延迟期或突释现象、能够快速达到稳态血药浓度、单次给药就能在数周或更长的时间内维持波动幅度较小的血药浓度,起效速度快、患者顺应性好。
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, 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 (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (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, KM, ML, MR, NE, SN, TD, TG)
Publication Language: Chinese (ZH)
Filing Language: Chinese (ZH)