JP2010529106A - 微小粒子で構成される徐放性医薬組成物 - Google Patents
微小粒子で構成される徐放性医薬組成物 Download PDFInfo
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- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 20
- 239000010419 fine particle Substances 0.000 title abstract 2
- 238000013268 sustained release Methods 0.000 title 1
- 239000012730 sustained-release form Substances 0.000 title 1
- 239000000203 mixture Substances 0.000 claims abstract description 57
- 239000011859 microparticle Substances 0.000 claims abstract description 33
- 238000002347 injection Methods 0.000 claims abstract description 17
- 239000007924 injection Substances 0.000 claims abstract description 17
- 239000004480 active ingredient Substances 0.000 claims abstract description 12
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims abstract description 12
- 150000003839 salts Chemical class 0.000 claims abstract description 11
- 108090000765 processed proteins & peptides Proteins 0.000 claims abstract description 10
- 229920001577 copolymer Polymers 0.000 claims abstract description 9
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims abstract description 6
- 235000014655 lactic acid Nutrition 0.000 claims abstract description 6
- 239000004310 lactic acid Substances 0.000 claims abstract description 6
- 229920000642 polymer Polymers 0.000 claims abstract description 5
- 239000004005 microsphere Substances 0.000 claims description 16
- 229920001606 poly(lactic acid-co-glycolic acid) Polymers 0.000 claims description 10
- 238000002156 mixing Methods 0.000 claims description 6
- 238000002360 preparation method Methods 0.000 claims description 5
- 206010060862 Prostate cancer Diseases 0.000 claims description 4
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 4
- 238000000034 method Methods 0.000 claims description 4
- 239000004531 microgranule Substances 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 3
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 238000009472 formulation Methods 0.000 description 22
- 108010050144 Triptorelin Pamoate Proteins 0.000 description 11
- VXKHXGOKWPXYNA-PGBVPBMZSA-N triptorelin Chemical compound C([C@@H](C(=O)N[C@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)NCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)C1=CC=C(O)C=C1 VXKHXGOKWPXYNA-PGBVPBMZSA-N 0.000 description 11
- 229960004824 triptorelin Drugs 0.000 description 11
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 9
- 101000904173 Homo sapiens Progonadoliberin-1 Proteins 0.000 description 9
- 102100024028 Progonadoliberin-1 Human genes 0.000 description 9
- 101000996723 Sus scrofa Gonadotropin-releasing hormone receptor Proteins 0.000 description 9
- 239000000556 agonist Substances 0.000 description 9
- XLXSAKCOAKORKW-UHFFFAOYSA-N gonadorelin Chemical compound C1CCC(C(=O)NCC(N)=O)N1C(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)NC(=O)CNC(=O)C(NC(=O)C(CO)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C(CC=1NC=NC=1)NC(=O)C1NC(=O)CC1)CC1=CC=C(O)C=C1 XLXSAKCOAKORKW-UHFFFAOYSA-N 0.000 description 9
- 239000012074 organic phase Substances 0.000 description 8
- 241000700159 Rattus Species 0.000 description 6
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 description 6
- JJTUDXZGHPGLLC-UHFFFAOYSA-N lactide Chemical compound CC1OC(=O)C(C)OC1=O JJTUDXZGHPGLLC-UHFFFAOYSA-N 0.000 description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- 102000007066 Prostate-Specific Antigen Human genes 0.000 description 4
- 108010072866 Prostate-Specific Antigen Proteins 0.000 description 4
- 239000012736 aqueous medium Substances 0.000 description 4
- 239000008346 aqueous phase Substances 0.000 description 4
- 238000000338 in vitro Methods 0.000 description 4
- 239000008363 phosphate buffer Substances 0.000 description 4
- 210000002966 serum Anatomy 0.000 description 4
- 238000010171 animal model Methods 0.000 description 3
- 238000001125 extrusion Methods 0.000 description 3
- 238000001727 in vivo Methods 0.000 description 3
- 229960003604 testosterone Drugs 0.000 description 3
- 239000008215 water for injection Substances 0.000 description 3
- RKDVKSZUMVYZHH-UHFFFAOYSA-N 1,4-dioxane-2,5-dione Chemical compound O=C1COC(=O)CO1 RKDVKSZUMVYZHH-UHFFFAOYSA-N 0.000 description 2
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 description 2
- 239000004372 Polyvinyl alcohol Substances 0.000 description 2
- 238000007906 compression Methods 0.000 description 2
- 230000006835 compression Effects 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 239000000839 emulsion Substances 0.000 description 2
- 238000001914 filtration Methods 0.000 description 2
- 238000000227 grinding Methods 0.000 description 2
- 238000010438 heat treatment Methods 0.000 description 2
- 238000000265 homogenisation Methods 0.000 description 2
- 239000008188 pellet Substances 0.000 description 2
- 239000012071 phase Substances 0.000 description 2
- 229920002451 polyvinyl alcohol Polymers 0.000 description 2
- 239000008213 purified water Substances 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 206010060800 Hot flush Diseases 0.000 description 1
- 101000857870 Squalus acanthias Gonadoliberin Proteins 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- JMMWKPVZQRWMSS-UHFFFAOYSA-N isopropanol acetate Natural products CC(C)OC(C)=O JMMWKPVZQRWMSS-UHFFFAOYSA-N 0.000 description 1
- 229940011051 isopropyl acetate Drugs 0.000 description 1
- GWYFCOCPABKNJV-UHFFFAOYSA-N isovaleric acid Chemical compound CC(C)CC(O)=O GWYFCOCPABKNJV-UHFFFAOYSA-N 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/08—Peptides having 5 to 11 amino acids
- A61K38/09—Luteinising hormone-releasing hormone [LHRH], i.e. Gonadotropin-releasing hormone [GnRH]; Related peptides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
- A61K9/1647—Polyesters, e.g. poly(lactide-co-glycolide)
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- A61P35/00—Antineoplastic agents
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
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Abstract
Description
-D(v,0.1)が、10〜30マイクロメートル、
-D(v,0.5)が、30〜70マイクロメートル、
-D(v,0.9)が、50〜110マイクロメートル
として定義されるサイズ分布を有する。
トリプトレリンパモ酸塩の製剤は、以下のプロセスを用いて調製される。
D(v,0.1)=23マイクロメートル
D(v,0.5)=55マイクロメートル
D(v,0.9)=99マイクロメートル
として定義される。
D(v,0.1)=15.6マイクロメートル
D(v,0.5)=33.4マイクロメートル
D(v,0.9)=60.8マイクロメートル
として定義されるサイズ分布を有する。
トリプトレリンパモ酸塩の微小顆粒の製剤は、実施例1に記載されているようにして調製される。
D(v,0.1)=17.6マイクロメートル
D(v,0.5)=39.9マイクロメートル
D(v,0.9)=84.2マイクロメートル
として定義される。
トリプトレリンパモ酸塩の微小粒子の製剤は、実施例1に記載されるようにして調製される。
D(v,0.1)=20.5マイクロメートル
D(v,0.5)=51.7マイクロメートル
D(v,0.9)=96.9マイクロメートル
として定義される。
トリプトレリンパモ酸塩と0.18dl/gの固有粘度を有するPLGA95/5とのミクロスフェアの製剤は、以下の如く調製される:
D(v,0.1)=17.8マイクロメートル
D(v,0.5)=37.1マイクロメートル
D(v,0.9)=74.8マイクロメートル
として定義されるサイズ分布を有する。
患者の服薬遵守及び便宜を増進させるべく、発明者らは、6ヶ月(24週)置きの注射を可能とする先述の実施例3に定義される製剤をも開発した。この実施例において考察される研究は、進行性前立腺癌の患者120人に22.5mgのトリプトレリンパモ酸塩を2回連続で筋肉内投与した後の、この製剤の有効性及び安全性を調査した。4週間のテストステロン評価が、48週間に渡り遂行された。
Claims (15)
- 少なくとも注射後6ヶ月目を含む一定期間の間有効成分を緩慢に放出する微小粒子(microparticle)で構成される医薬組成物であり、前記組成物が、非水溶性ペプチド塩の形態の有効成分を包摂するPLGA型のコポリマーで構成される微小粒子の群を含み;前記コポリマーが更に、少なくとも75%の乳酸を含み、及び25℃のクロロホルム中で、かつポリマー濃度が0.5g/dLで測定された固有粘度(inherent viscosity)が0.1〜0.9dl/gであり;前記微小粒子が更に、以下:
-D(v,0.1)が、10〜30マイクロメートル、
-D(v,0.5)が、30〜70マイクロメートル、
-D(v,0.9)が、50〜110マイクロメートル
と定義されるサイズ分布を有する、前記組成物。 - 乳酸の量が少なくとも85%である、請求項1に記載の医薬組成物。
- 前記固有粘度が0.1〜0.4dl/gである、請求項2に記載の医薬組成物。
- 前記固有粘度が、0.55〜0.75dl/g、より好ましくは0.63〜0.67dl/gである、請求項2に記載の医薬組成物。
- 前記微小粒子がミクロスフェア(microsphere)である、請求項1〜4のいずれか1項に記載の医薬組成物。
- 前記微小粒子が微小顆粒(microgranule)である、請求項1〜4のいずれか1項に記載の医薬組成物。
- 前記有効成分を包摂し、70%〜80%の量の乳酸を含むPLGA型のコポリマーで構成される微小粒子のもう一つの群を更に含む、請求項1〜6のいずれか1項に記載の医薬組成物。
- 前記他の群の固有粘度が0.60〜0.7dl/gである、請求項7に記載の医薬組成物。
- 前記他の群の微小粒子が微小顆粒である、請求項8に記載の医薬組成物。
- 両群の用量比が50:50である、請求項7〜9のいずれか1項に記載の医薬組成物。
- 前記微小粒子群の少なくとも1つが、無溶媒プロセスにおいて、前記PLGAと、前記非水溶性ペプチド塩とを混合することにより収得される、請求項1〜10のいずれか1項に記載の医薬組成物。
- 前記組成物の注射後少なくとも4ヶ月目から6ヶ月目まで(6ヶ月目を含む)の期間、非水溶性ペプチド塩を緩慢に放出するための、請求項1〜6のいずれか1項に定義される医薬組成物の使用。
- 前記組成物の注射の1ヶ月後から前記期間が開始される、請求項12に記載の使用。
- 請求項7〜11のいずれか1項に定義される他の微小粒子の群の使用を含み、前記他の群が、前記組成物の注射後少なくとも最初の3ヶ月の間、前記非水溶性ペプチド塩を放出するように設計されている、請求項12又は13のいずれかに記載の使用。
- 前記請求項1〜11のいずれか1項に記載の組成物が6ヶ月置きに投与されることを特徴とする、前立線癌治療剤の調製のための、前記組成物の使用。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
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EP07109767 | 2007-06-06 | ||
EP07109767.9 | 2007-06-06 | ||
IB2007054372 | 2007-10-27 | ||
IBPCT/IB2007/054372 | 2007-10-27 | ||
PCT/IB2008/052241 WO2008149320A2 (en) | 2007-06-06 | 2008-06-06 | Slow release pharmaceutical composition made of microparticles |
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JP2010529106A true JP2010529106A (ja) | 2010-08-26 |
JP5419169B2 JP5419169B2 (ja) | 2014-02-19 |
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US (3) | US10166181B2 (ja) |
EP (3) | EP2500014B1 (ja) |
JP (1) | JP5419169B2 (ja) |
KR (1) | KR101631475B1 (ja) |
CN (1) | CN101677959B (ja) |
AP (1) | AP3000A (ja) |
AU (1) | AU2008259411B2 (ja) |
BR (1) | BRPI0812250B8 (ja) |
CA (1) | CA2688478C (ja) |
CO (1) | CO6251234A2 (ja) |
CY (2) | CY1118434T1 (ja) |
DK (2) | DK2164467T3 (ja) |
EA (1) | EA019284B1 (ja) |
ES (2) | ES2694401T3 (ja) |
HK (1) | HK1141737A1 (ja) |
HR (2) | HRP20161785T1 (ja) |
HU (2) | HUE040391T2 (ja) |
IL (1) | IL202501A (ja) |
LT (2) | LT2164467T (ja) |
MA (1) | MA31422B1 (ja) |
ME (1) | ME00959B (ja) |
MX (1) | MX2009012856A (ja) |
MY (1) | MY150450A (ja) |
NZ (1) | NZ582423A (ja) |
PL (2) | PL2164467T3 (ja) |
PT (2) | PT2500014T (ja) |
RS (2) | RS55591B1 (ja) |
SI (2) | SI2164467T1 (ja) |
TN (1) | TN2009000476A1 (ja) |
UA (1) | UA99830C2 (ja) |
WO (1) | WO2008149320A2 (ja) |
ZA (1) | ZA200907940B (ja) |
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UA99830C2 (uk) | 2007-06-06 | 2012-10-10 | Дебио Ресшерчи Фармасютикю С.А. | Фармацевтична композиція з пролонгованим вивільненням, виготовлена з мікрочастинок |
PT105270B (pt) | 2010-08-26 | 2012-05-31 | Domino Ind Ceramicas S A | Camada de sílica com libertação lenta de fragrância, telha cerâmica e respectivo processo de produção |
CN105267153B (zh) * | 2015-11-27 | 2018-05-11 | 上海苏豪逸明制药有限公司 | 一种曲普瑞林缓释微粒及其制备方法 |
CN105797134B (zh) * | 2016-03-29 | 2019-06-14 | 浙江圣兆药物科技股份有限公司 | 一种难溶亮丙瑞林缓释制剂 |
EP3535297B1 (en) | 2016-11-02 | 2022-08-10 | Debiopharm International, S.A. | Methods for improving anti-cd37 immunoconjugate therapy |
KR102402639B1 (ko) | 2017-11-24 | 2022-05-26 | 삼성전자주식회사 | 전자 장치 및 그의 통신 방법 |
CN111000798B (zh) * | 2019-12-26 | 2021-11-23 | 四川恒博生物科技有限公司 | 一种采用原位凝胶技术的犬用非手术去势注射液 |
IT202000017191A1 (it) | 2020-07-15 | 2022-01-15 | Xbrane Biopharma Ab | Procedimento senza acqua per preparare una composizione farmaceutica per un rilascio più prolungato e controllato di triptorelina o di un suo sale |
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JPH0687758A (ja) * | 1992-07-27 | 1994-03-29 | Rhone Merieux | Lhrhホルモンおよびその類似体を徐々に放出する微小球体の製造方法と、その微小球体と、それを含む製剤 |
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JP2005509611A (ja) * | 2001-10-10 | 2005-04-14 | ピエール、ファーブル、メディカマン | 徐放型生物分解性微小球およびその製造方法 |
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