JPWO2019214726A5 - - Google Patents

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JPWO2019214726A5
JPWO2019214726A5 JP2020561817A JP2020561817A JPWO2019214726A5 JP WO2019214726 A5 JPWO2019214726 A5 JP WO2019214726A5 JP 2020561817 A JP2020561817 A JP 2020561817A JP 2020561817 A JP2020561817 A JP 2020561817A JP WO2019214726 A5 JPWO2019214726 A5 JP WO2019214726A5
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buprenorphine
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diffraction pattern
ray powder
powder diffraction
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JP2021522306A (en
JP7421804B2 (en
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Claims (8)

式ＩＩで表される３－アシル－ブプレノルフィンの結晶形。
Figure 2019214726000001
ここで、Ｒは炭素原子数１～１７の直鎖または分岐鎖アルキル部分を有するアシル基であり、
当該結晶形は、４．７０、８．４４、９．３８、２０．５６度２θ±０．２度２θのピーク、６．０３、９．０８、９．５８、９．６８度２θ±０．２度２θのピーク、５．９８、９．４３、１１．８３、１１．９３度２θ±０．２度２θのピーク、７．５３、８．１３、１３．４８、１６．０３度２θ±０．２度２θのピーク、５．８０、８．００、１１．５０、１７．３４度２θ±０．２度２θのピーク、または５．６８、８．０３、１１．３８、１７．２３度２θ±０．２度２θのピークを含むＸ線粉末回折パターンを特徴とする。 Crystal form of 3-acyl-buprenorphine represented by formula II.
Figure 2019214726000001
Here, R is an acyl group having a linear or branched-chain alkyl moiety having 1 to 17 carbon atoms.
The crystal forms are 4.70, 8.44, 9.38, 20.56 degrees 2θ ± 0.2 degrees 2θ peaks, 6.03, 9.08, 9.58, 9.68 degrees 2θ ± 0. .2 degree 2θ peak, 5.98, 9.43, 11.83, 11.93 degree 2θ ± 0.2 degree 2θ peak, 7.53, 8.13, 13.48, 16.03 degree 2θ ± 0.2 degree 2θ peak, 5.80, 8.00, 11.50, 17.34 degree 2θ ± 0.2 degree 2θ peak, or 5.68, 8.03, 11.38, 17. It features an X-ray powder diffraction pattern containing a peak of 23 degrees 2θ ± 0.2 degrees 2θ. 前記の３－アシル－ブプレノルフィンは、
下記図１に示されるものと一致するＸ線粉末回折パターンを有する酢酸ブプレノルフィン、
Figure 2019214726000002

下記図５に示されるものと一致するＸ線粉末回折パターンを有するピプレン酸ブプレノルフィン、
Figure 2019214726000003

下記図９に示されるものと一致するＸ線粉末回折パターンを有するペンタン酸ブプレノルフィン、
Figure 2019214726000004

下記図１３に示されるものと一致するＸ線粉末回折パターンを有するヘキサン酸ブプレノルフィン、

Figure 2019214726000005

下記図１７に示されるものと一致するＸ線粉末回折パターンを有するデカン酸ブプレノルフィン、
Figure 2019214726000006

または、
下記図２１に示されるものと一致するＸ線粉末回折パターンを有するドデカン酸ブプレノルフィン
Figure 2019214726000007

である、請求項１に記載の結晶形。 The above-mentioned 3-acyl-buprenorphine is
Buprenorphine acetate, which has an X-ray powder diffraction pattern consistent with that shown in FIG. 1 below .
Figure 2019214726000002

Buprenorphine piprenate, which has an X-ray powder diffraction pattern consistent with that shown in FIG. 5 below .
Figure 2019214726000003

Buprenorphine pentanate having an X-ray powder diffraction pattern consistent with that shown in FIG. 9 below ,
Figure 2019214726000004

Buprenorphine hexane acid, having an X-ray powder diffraction pattern consistent with that shown in FIG. 13 below .

Figure 2019214726000005

Buprenorphine decanoate, which has an X-ray powder diffraction pattern consistent with that shown in FIG. 17 below .
Figure 2019214726000006

or,
Buprenorphine dodecanoate with an X-ray powder diffraction pattern consistent with that shown in FIG. 21 below .
Figure 2019214726000007

The crystalline form according to claim 1. 請求項１または２に記載の結晶形およびその薬学的に許容される担体を含む持効性医薬組成物。 A long-acting pharmaceutical composition comprising the crystalline form according to claim 1 or 2 and a pharmaceutically acceptable carrier thereof. 懸濁水性希釈剤に、請求項１または２に記載の結晶形またはその薬学的に許容される塩を含み、有機溶媒、ポリ乳酸ポリマー、ポリグリコリドポリマー、またはポリ乳酸とポリグリコリドのコポリマーを含まず、患者または動物に注射されたときに少なくとも１週間続く安定した放出プロファイルを示す、水性注射可能な医薬懸濁液。 The suspension aqueous diluent contains the crystalline form according to claim 1 or 2 or a pharmaceutically acceptable salt thereof, and contains an organic solvent, a polylactic acid polymer, a polyglycolide polymer, or a copolymer of polylactic acid and polyglycolide. An aqueous injectable pharmaceutical suspension that exhibits a stable release profile that lasts at least 1 week when injected into a patient or animal. ８０μｍ未満の平均粒径を有する、請求項４に記載の注射可能な医薬懸濁液。 The injectable pharmaceutical suspension according to claim 4, which has an average particle size of less than 80 μm. 前記の懸濁水性希釈剤は、リン酸緩衝生理食塩水におけるポリエチレングリコールポリマーおよびポリソルベートを含む、請求項４に記載の注射可能な医薬懸濁液。 The injectable pharmaceutical suspension of claim 4, wherein the suspended aqueous diluent comprises a polyethylene glycol polymer and polysorbate in phosphate buffered saline. 前記の３－アシル－ブプレノルフィンまたはその薬学的に許容される塩は５％～３０％ｗ／ｗの濃度で存在する、請求項４に記載の注射可能な医薬懸濁液。 The injectable pharmaceutical suspension according to claim 4, wherein the 3-acyl-buprenorphine or a pharmaceutically acceptable salt thereof is present at a concentration of 5% to 30% w / w. 請求項４に記載の水性注射可能な医薬懸濁液であって、前記の水性注射可能な医薬懸濁液を必要とする対象の皮下または筋肉内に少なくとも１週間の治療上有効な期間で投与される、オピオイド中毒、疼痛またはうつ病を治療するための水性注射可能な医薬懸濁液。 The aqueous injectable pharmaceutical suspension according to claim 4, which is administered subcutaneously or intramuscularly to a subject in need of the aqueous injectable pharmaceutical suspension for a therapeutically effective period of at least 1 week . An aqueous injectable pharmaceutical suspension for the treatment of opioid addiction, pain or depression.
JP2020561817A 2018-05-11 2019-05-10 Long-acting injectable formulations and crystalline forms of buprenorphine derivatives Active JP7421804B2 (en)

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GB202019594D0 (en) * 2020-12-11 2021-01-27 Univ London Queen Mary Sustained release formulations of crystalline drugs
WO2023020608A1 (en) * 2021-08-20 2023-02-23 苏州恩华生物医药科技有限公司 Pharmaceutical composition containing dinalbuphine sebacate
WO2023246865A1 (en) * 2022-06-24 2023-12-28 Alar Pharmaceuticals Inc. Stable pharmaceutical composition of buprenorphine and preparation method and use thereof
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CN1263760C (en) * 2002-11-12 2006-07-12 财团法人奇美医院 Novel buprenorphine ester derivatives and process for preparing the same and medical compounds with long-acting analgesic effect
JP2004175706A (en) 2002-11-26 2004-06-24 Chi Mei Foundation Medical Center New buprenorphine ester derivative, method for preparing the same and analgesic composition having persistency of validity for many hours
GB2481017B (en) * 2010-06-08 2015-01-07 Rb Pharmaceuticals Ltd Microparticle buprenorphine suspension
US9272044B2 (en) * 2010-06-08 2016-03-01 Indivior Uk Limited Injectable flowable composition buprenorphine
FR2975912B1 (en) * 2011-05-30 2013-06-14 Flamel Tech Sa CONTROLLED RELEASE COMPOSITION OF BUPRENORPHINE
JP6471089B2 (en) 2012-03-19 2019-02-13 アルカームス ファーマ アイルランド リミテッド Pharmaceutical composition comprising fatty acid ester
US9393211B2 (en) * 2013-03-15 2016-07-19 Oakwood Laboratories LLC High drug load buprenorphine microspheres and method of producing same
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