JP2021536491A - 薬剤放出制御剤形 - Google Patents
薬剤放出制御剤形 Download PDFInfo
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- JP2021536491A JP2021536491A JP2021513266A JP2021513266A JP2021536491A JP 2021536491 A JP2021536491 A JP 2021536491A JP 2021513266 A JP2021513266 A JP 2021513266A JP 2021513266 A JP2021513266 A JP 2021513266A JP 2021536491 A JP2021536491 A JP 2021536491A
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- xyloglucan
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Abstract
Description
1)胞子及び/又は菌株混合物を含む選択された細菌株;
2)発酵基質、窒素源、微量元素(Fe)などの結腸微生物のための栄養素;
3)ビタミン、ホルモン、抗生物質、毒素などを含む細菌増殖の修飾物質;
4)選択された菌株の増殖、生存、又はコロニー形成に有利に及び/又は不利に働くことにより、マイクロバイオームの組成に影響を与える化合物、
が挙げられる。
(A)キシログルカン 25〜90重量%、好ましくは40〜90重量%;
(B)少なくとも1つの医薬品有効成分 10〜60重量%;
(C)希釈剤、結合剤、付着防止剤、潤滑剤、流動促進剤、及びそれらの組合せからなる群から選択される、1種以上の薬学的に許容される賦形剤であって、好ましくは、結合剤又は結合剤及び付着防止剤、特に、PVPとして選択される結合剤及びステアリン酸マグネシウムとしての付着防止剤から本質的になる、薬学的に許容される賦形剤 0〜20重量%、好ましくは5〜10重量%
(A)キシログルカン 25〜90重量%、好ましくは40〜90重量%;
(B)少なくとも1つの医薬品有効成分 10〜60重量%;
(C)希釈剤、結合剤、潤滑剤、流動促進剤、及びそれらの組合せからなる群から選択される、1種以上の薬学的に許容される賦形剤であって、好ましくは、結合剤、特にPVPとして選択される結合剤から本質的になる、薬学的に許容される賦形剤 0〜20重量%、好ましくは5〜10重量%
その顆粒は、前記シェルを適用する前に圧縮されてコアを形成し、好ましくは、圧縮する前に、前記顆粒は、付着防止剤、好ましくはステアリン酸マグネシウムの形態での付着防止剤と混合される。
ガスピクノメーターを使用する方法は、例えば、欧州薬局方Ph.Eur.8(2.9.23、p324)に記載されている。
剤形1は、シェル3内にカプセル化されたコア2を含む。コアは、マトリックス5、この特定の場合にはキシログルカンを含み、その中に医薬品有効成分4(API)が埋め込まれている。
錠剤の製造
3工程プロセスを用いた。
1.造粒
造粒を、流動床造粒機又は高剪断ミキサーのいずれかで実施した。組成は、以下の通りであった:
グリロイド3S (93−X)%
5−ASA(API) X%
ポリビニルピロリドン(Kollidon30) 7%
Xが以下の値である3つの異なる組成、すなわち、33.3%;50%;66.7%、を使用した。
造粒組成物を、Turbulaミキサーで32rpmにて2分間、0.5%ステアリン酸マグネシウムと混合した。12mmの直径、9mmの曲率半径、及び50Nの直径方向破砕力を有する錠剤を、単発式偏心打錠機で毎分20錠の速度で製造した。錠剤重量を、造粒後に決定された組成物のAPI含有量に基づいて600〜630mgの間に調整し、API含有量は1錠あたり200、300及び400mgに達した。上部パンチの圧縮力は10〜13kNの間であった。
錠剤を、600gのバッチサイズのドラム塗工機にてEudragitFS−30−Dでコーティングした。コーティング分散液の組成は以下の通りであった:
Eudragit FS−30−D 43%
クエン酸トリエチル 0.65%
タルク 6.45%
染料(酸化鉄III) 0.2%
精製水 49.7%
キシログルカン:
商標名:グリロイド3S及びグリロイド2A
(DSP GOKYO FOOD & CHEMICAL Co., Ltd.、Osaka、Japan)
一般名:タマリンド種子多糖又はタマリンドシードガム
化学物質:キシログルカン
FDAによるGrasステータス申告:GRN No.503;物質:タマリンド種子多糖;使用目的:ある特定の食品カテゴリーにおいて、増粘剤、安定剤、乳化剤、及びゲル化剤として使用する;通知人;DSP GOKYO FOOD & CHEMICAL Co., Ltd.;HERBIS OSAKA 20th Floor 2−5−25 Umeda Kita−ku、Osaka、530−0001 Japan;出願日:2014年3月5日
GRAS通知(開示可能な情報):503;終了日:2014年8月12日
薬剤放出は、USP2装置において37℃、パドル回転速度100rpmで測定した。容器ごとに1錠を使用した。以下の培地組成を用いて4段階試験を実施した。
典型的な結果を図3の図に示す。胃及び上部小腸を反映した状態では薬剤は放出されず、これはポリマーコーティングによるものである。これらの環境のそれぞれにおける2時間の滞留時間は、シンチグラフィー及び他の方法によって見出された、軽食後の胃腸管内の固体剤形の通過時間を表すものである。
薬剤放出の速度は、微生物酵素の存在下で濃度依存的に著しく加速し、これにより、開発された送達システムによる、制御された位置誘発薬剤放出の原理が証明された。
上述のYooの刊行物との違いについては、以下の点に注意すべきである:Yooの刊行物における結果は、製造品(ビーズ)が本明細書で提案された錠剤のように作用しないことを証明している。Yooの図5では、活性物質の放出は、pH1.2の人工胃培地内で最初に測定され、次にpH7.4の人工腸培地内で測定されている。Yooのコーティングビーズは、pH1.2での最初の2時間で約10%、pH7.4での次の2時間で約50%の放出を示す。本明細書に記載の製剤は、pH1.2で2時間後に0%の放出、pH6.5で2時間後に0%の放出、及びpH6.8でさらに2時間後に約5%の放出を示す。目的は腸の状態下での放出をできるだけ少なくすることであるため、Yooの製品は本発明者らの要求を満たすには遠く及ばない。
− 2%キシログルカン水溶液(本明細書での試験におけるような3S品質)を、4℃の温度下で、プロペラ撹拌機で24時間撹拌して調製した。
− 植物油を、磁気撹拌下で40℃にて、及び80℃にて加熱した。
− 1mLのキシログルカン溶液を、注射針付き注射器(22Gに対応するID 0.71mm)から油に滴下した。
どちらの温度でも、最初は約2mm〜2.5mmの大きさの滴が形成される。40℃では、数分後に滴が共にウォームに流れる。80℃では、液滴内に気泡が形成され、液滴は表面に上昇し、ろ過中に一緒に流れた。
2 コア
3 シェル
4 医薬品有効成分
5 マトリックス、キシログルカン
6 S−20−50N、総質量631mg、コーティングを含まない
7 S−20−50N、Eudragit FS30、L=2、総質量639mg、コーティングを有する
8 S−20−50N、Eudragit FS30、L=3.5、総質量651mg、コーティングを有する
9 S−19−50N、Eudragit FS30、L=4.9、総質量671mg、コーティングを有する
10 S−20−50N、Eudragit FS30、L=6.8、総質量661mg、コーティングを有する
Claims (15)
- 少なくとも1つのシェル(3)によってカプセル化され、かつ少なくとも1つの医薬品有効成分(4)を含むコア(2)を有する医薬製剤剤形(1)であって、
前記少なくとも1つの医薬品有効成分(4)は、前記医薬製剤剤形(1)の前記コア(2)に埋め込まれているか、又は、前記医薬製剤剤形(1)の前記コア(2)を形成しており、
前記シェル(3)は、pH応答性コーティングを含み、
前記コア(2)及び前記シェル(3)の少なくとも1つは、キシログルカンを基材にしている、前記医薬製剤剤形。 - 前記少なくとも1つの医薬品有効成分(4)が、前記医薬製剤剤形(1)の前記コア(2)に埋め込まれており、前記コア(2)は、前記医薬品有効成分(4)を含有するキシログルカン(5)を基材とするのマトリックスによって形成され、
及び/又は、前記コアは、少なくとも0.7、好ましくは少なくとも0.75若しくは少なくとも0.8の相対密度を有する単一の固体圧縮成形コアであり;
及び/又は、前記コア及び/又は前記医薬製剤剤形全体の、最小直径の方向での平均直径が、少なくとも3mm、好ましくは少なくとも4mm、より好ましくは少なくとも4.5mm又は5mmであり、;
及び/又は、前記コア及び/又は前記医薬製剤剤形全体は、少なくとも25N、好ましくは少なくとも40N、より好ましくは少なくとも100Nの破砕力を有する、請求項1に記載の医薬製剤剤形(1)。 - 前記シェル(3)が、キシログルカン(5)を基材にしているか又はキシログルカン(5)を含まない、pH応答性コーティングの形態の少なくとも1つの外層と、並びに、前記外層がキシログルカン(5)を含まない場合は、キシログルカン(5)を基材とする少なくとも1つの内層とを含む、請求項1又は2に記載の医薬製剤剤形(1)。
- 前記医薬製剤剤形が、経口投与及び結腸における前記医薬品有効成分の標的放出に適合され、前記シェル(3)が、6.5を超えるpH、好ましくは少なくとも6.7のpH、より好ましくは少なくとも6.8のpHでのみ溶解するpH応答性コーティングを少なくとも1つ含むか、又は、当該pH応答性コーティングからなる、請求項1〜3のいずれかに記載の医薬製剤剤形(1)。
- 前記シェル(3)、特にその前記少なくとも1つのpH応答性コーティングが、合成ポリマー及び/又は生体高分子、又はそれらの混合物を基材にしており、好ましくはアニオン性アクリレートコポリマーを基材にしており、好ましくはアクリル酸メチル、メタクリル酸メチル、及びメタクリル酸を基材とするアニオン性コポリマーを基材にしており、好ましくは、遊離カルボキシル基のエステル基に対する比率が1:5〜1:10であり、好ましくは前記比率が1:10であり、好ましくは、前記アニオン性アクリレートコポリマーの重量平均モル質量(Mw)が200,000〜400,000g/mol、好ましくは250,000〜300,000g/molである、請求項1〜4のいずれかに記載の医薬製剤剤形(1)。
- 前記シェル(3)、特にその前記少なくとも1つのpH応答性コーティングが、アニオン性アクリレートコポリマーの混合物、好ましくはアクリル酸メチル、メタクリル酸メチル、及びメタクリル酸を基材とするアニオン性コポリマーの混合物からなり、好ましくは、遊離カルボキシル基のエステル基に対する比率が1:5〜1:10であり、好ましくは前記比率が1:10であり、好ましくは、前記アニオン性アクリレートコポリマーの重量平均モル質量(Mw)が、200,000〜400,000g/mol、好ましくは250,000〜300,000g/molであり、25%未満の割合のさらなる添加剤を含み、前記さらなる添加剤が、好ましくは、ポリオキシエチレン及びその誘導体、アニオン性界面活性剤、特にラウリル硫酸ナトリウム、タルク、染料、特に酸化鉄(III)、安定剤、特にクエン酸トリエチルからなる群から選択される、請求項1〜5のいずれかに記載の医薬製剤剤形(1)。
- 前記少なくとも1つのpH応答性コーティング又は前記シェル(3)全体の乾燥コーティングの量が、1〜10mg/cm2、好ましくは2.5〜6mg/cm2である、請求項1〜6のいずれかに記載の医薬製剤剤形(1)。
- 前記シェル(3)を形成する1つだけの単一のカプセル化pH応答性コーティング(3)が供される、請求項1〜7のいずれかに記載の医薬製剤剤形(1)。
- 前記コア(2)の前記マトリックスが、本質的又は完全にキシログルカン(5)からなり、好ましくは、前記キシログルカン(5)が、タマリンドゥス・インディカ種子から得られ、及び/又は、冷水可溶性であり、及び/又は、非晶質であり、
及び/又は、出発物質として使用される前記キシログルカンが、少なくとも70μm、好ましくは70〜150μm、より好ましくは80〜110μmの粒径(d50%)を有し、
及び/又は、前記キシログルカンが、400,000〜500,000g/molの重量平均モル質量(Mw)を有し、
及び/又は、前記キシログルカンが、脱ガラクトシル化されていない及び/又は、天然であり、好ましくは、前記キシログルカンが、天然の高度に精製されたキシログルカンであり、より好ましくは、冷水可溶性型のものである、請求項1〜8のいずれかに記載の医薬製剤剤形(1)。 - 前記コア(2)が、下記(A)〜(C):
(A)キシログルカン 25〜90重量%、好ましくは40〜90重量%;
(B)少なくとも1つの医薬品有効成分 10〜60重量%;
(C)希釈剤、結合剤、付着防止剤、潤滑剤、流動促進剤、及びそれらの組合せからなる群から選択される、1種以上の薬学的に許容される賦形剤であって、好ましくは、結合剤又は結合剤及び付着防止剤、特に、PVPとして選択される結合剤及びステアリン酸マグネシウムとしての付着防止剤から本質的になる、薬学的に許容される賦形剤 0〜20重量%、好ましくは5〜10重量%;からなり、
又は、前記コア(2)が、下記(A)〜(C):
(A)キシログルカン 25〜90重量%、好ましくは40〜90重量%;
(B)少なくとも1つの医薬品有効成分 10〜60重量%;
(C)希釈剤、結合剤、潤滑剤、流動促進剤、及びそれらの組合せからなる群から選択される、1種以上の薬学的に許容される賦形剤であって、好ましくは、結合剤、特にPVPとして選択される結合剤から本質的になる、薬学的に許容される賦形剤 0〜20重量%、好ましくは5〜10重量%;からなる顆粒からなり、
前記顆粒は、前記シェルを適用する前に圧縮されてコア(2)を形成し、好ましくは、圧縮する前に、前記顆粒は、付着防止剤、好ましくはステアリン酸マグネシウムの形態での付着防止剤と混合される、請求項1〜9のいずれかに記載の医薬製剤剤形(1)。 - 前記コア(2)の前記マトリックスの、前記少なくとも1つの医薬品有効成分に対する重量比が、少なくとも1:2、好ましくは少なくとも1:1、より好ましくは少なくとも2:1である、請求項1〜10のいずれかに記載の医薬製剤剤形(1)。
- 結腸内のマイクロバイオーム集団の均衡若しくは下部消化管の生理機能を確立、再確立、及び/又は、改変させる目的のための、又は免疫調節若しくは免疫抑制のための、又は以下の状態、すなわち炎症性腸疾患、特に潰瘍性大腸炎及び/又はクローン病、クロストリジウム・ディフィシル感染症、結腸がん、結腸外科処置後のうちの少なくとも1つの状態の処置のための、請求項1〜11のいずれかに記載の医薬製剤剤形(1)。
- 前記医薬品有効成分が、メサラジン、ブデソニド、カペシタビン、フルオロウラシル、イリノテカン、オキサリプラチン、UFT、セツキシマブ、パニツムマブ、免疫調節性若しくは免疫抑制性成分であって、免疫抑制性グルココルチコイド、免疫抑制性細胞増殖抑制剤、免疫抑制性(ポリ又はモノクローナル)抗体、イムノフィリンに作用する免疫抑制剤、インターロイキン、サイトカイン、ケモカイン、若しくは免疫調節性イミド薬を含み、特にタクロリムス、シクロスポリンを含むもの、又は結腸内のマイクロバイオーム集団の平衡を確立、再確立、及び/又は、改変することを目的とする材料、又は下部消化管の生理機能に有益な効果をもたらす化合物又はそれらの組合せ、からなる群から選択される、請求項1〜12のいずれかに記載の医薬製剤剤形(1)。
- 少なくとも1週間、好ましくは少なくとも2週間、又は少なくとも2か月若しくは少なくとも1年、又はさらには生涯の期間にわたって、少なくとも1日1回、好ましくは1日2回、経口投与される、請求項1〜13のいずれかに記載の医薬製剤剤形(1)。
- 請求項1〜14のいずれかに記載の医薬製剤剤形を製造する方法であって、第1のステップでは、キシログルカン、少なくとも1つの医薬品有効成分、及び必要に応じて1種以上の薬学的に許容される賦形剤を、混合しその後圧縮して前記コアを形成するか、又は、これらを混合し処理して顆粒を形成し、好ましくは圧縮成形して、少なくとも0.7、好ましくは少なくとも0.75若しくは少なくとも0.8の相対密度を有し、及び/又は、最小直径の方向での平均直径が、少なくとも3mm、好ましくは少なくとも4mm、より好ましくは少なくとも4.5mm又は5mmである単一のコアを形成し、続いて、必要に応じて最初に前記顆粒をさらなる処理剤と混合し、圧縮して前記コアを形成し、ここで、両方の場合における混合は、好ましくは流動床造粒機又は高剪断ミキサーを使用して行うことができ、
その後、第2のステップで、前記コアを、シェルを形成する少なくとも1つのコーティングによりコーティングし、ここで好ましくは、前記コーティングの形成には、分散液が供され、さらに好ましくはドラム塗工機内で施される、方法。
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- 2019-09-03 JP JP2021513266A patent/JP2021536491A/ja active Pending
- 2019-09-03 CA CA3111353A patent/CA3111353A1/en active Pending
- 2019-09-03 US US17/272,512 patent/US20210322325A1/en not_active Abandoned
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Patent Citations (1)
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US20180000740A1 (en) * | 2016-03-11 | 2018-01-04 | Gateway Pharmaceutical LLC | Pharmaceutical compositions for colon-specific delivery |
Non-Patent Citations (3)
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ARUN R. RAJ: "Formulation and evaluation of prednisolone tablets using biodegradable natural polysaccharid", INTERNATIONAL JOURNAL OF PHARMACEUTICALSCIENCES AND RESEARCH, JPN6023011311, 2013, pages 26, ISSN: 0005022528 * |
DEEPALI GAWALE: "Formulation and in-vitro characterization of multiple unit sustained release matrix pellets", INDIAN JOURNAL OF NOVEL DRUG DELIVERY, vol. 5(4), JPN6023011310, 2013, pages 208 - 220, ISSN: 0005022529 * |
MI KYONG YOO; ET AL: "DRUG RELEASE FROM XYLOGLUCAN BEADS COATED WITH EUDRAGIT FOR ORAL DRUG DELIVERY", ARCHIVES OF PHARMACAL RESEARCH, vol. VOL:28,NR:6, JPN5021012594, June 2005 (2005-06-01), pages 736 - 742, XP055558934, ISSN: 0005022527, DOI: 10.1007/BF02969366 * |
Also Published As
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US20240082168A1 (en) | 2024-03-14 |
US20210322325A1 (en) | 2021-10-21 |
AU2019334434A1 (en) | 2021-03-18 |
KR20210054521A (ko) | 2021-05-13 |
MX2021002686A (es) | 2021-08-11 |
CA3111353A1 (en) | 2020-03-12 |
WO2020048979A1 (en) | 2020-03-12 |
BR112021004213A2 (pt) | 2021-05-25 |
EP3846784A1 (en) | 2021-07-14 |
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