JP2021098694A - フィナステリドを含む徐放性注射用組成物 - Google Patents
フィナステリドを含む徐放性注射用組成物 Download PDFInfo
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- JP2021098694A JP2021098694A JP2020213698A JP2020213698A JP2021098694A JP 2021098694 A JP2021098694 A JP 2021098694A JP 2020213698 A JP2020213698 A JP 2020213698A JP 2020213698 A JP2020213698 A JP 2020213698A JP 2021098694 A JP2021098694 A JP 2021098694A
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Abstract
Description
AUC=投与量(dose)/クリアランス(clearance)
CLs=V×K
薬物の清掃率(drug clearance)=投与量(dose)/AUC
AUC=最初濃度(Co)/消失速度定数(K)
台形公式でAUCを求めるとき、血中濃度は自然対数の値で置換しない。
1)第1混合物を調製する段階(S100)と、
2)第2混合物を調製する段階(S200)と、
3)第1混合物を直線方向のマイクロチャネルに注入する段階(S300)と、
4)第2混合物を両側面または一側面のマイクロチャネルに注入する段階(S400)と、
5)徐放性粒子を収集する段階(S500)と、
6)収集した徐放性粒子を撹拌する段階(S600)と、
7)徐放性粒子を洗浄および乾燥する段階(S700)との順に行われる。
[フィナステリドを含む徐放性粒子を含有した皮下注射用組成物の調製]
1.フィナステリドを含む徐放性粒子の調製
ポリ(ラクチド-コ-グリコライド)コポリマー(PLGA)およびフィナステリドをジクロロメタン(dichloromethane)に溶解して、第1混合物を調製した。この際、第1混合物内のポリ(ラクチド-コ-グリコライド)コポリマーは15重量%の比で含まれ、ポリ(ラクチド-コ-グリコライド)コポリマーおよびフィナステリドの重量比は2:1である。
ポリ(ラクチド-コ-グリコライド)コポリマーおよびフィナステリドの重量比を9:1で含むことを除いて、実施例1と同様に調製した。
ポリ(ラクチド-コ-グリコライド)コポリマーおよびフィナステリドの重量比を12:1で含むことを除いて、実施例1と同様に調製した。
前記実施例1〜3により調製された徐放性粒子は、1バイアルを基準に2.0mlの懸濁溶剤に加えた後、均一に懸濁させて皮下注射用組成物として調製した。
前記懸濁溶剤は、下記表1のような組成で構成した。
[徐放性粒子の性状検討]
本発明の一実施例による徐放性粒子の性状を検討するために、調製済みの徐放性粒子の性状をSEM写真により確認した。
実施例1〜3の3回測定した結果は、下記表2の通りである。
[薬物動態特性評価]
本発明のフィナステリドを含む徐放性粒子およびこれを含有した注射剤形に対する薬物動態評価を確認した。
・マイクロ天秤(Micro balance):SI-234、DENVER INSTRUMENT社
・遠心機(Centrifuge):Centrifuge 5424、Eppendorf社
・ボルテックス・ミキサー(Vortex mixer):Model Genie-2、Scientific Industries社
・ピペット(Auto pipette):Research plus 20μL、100μL、200μL、1000μL、Eppendorf社
・ネジキャップ(Screw caps)、Microsolve社
・バイアル(Vials):Screw top 300μL、Microsolve社
・シリンジ式ディスペンサ(Syringe dispenser):PB-600、HAMILTON社
・超音波洗浄機(Ultrasonic cleaner):3510E-DTH、BRANSONIC(登録商標)
・HPLC:1290 InfinityII、Agilent Technologies社
・質量分析計(Mass spectrometer):6490 Triple Quad LC/MS、Agilent Technologies社
・データ処理システム(Data processing system):Masshunter Workstation Ver B.07(Agilent)
LC−MS/MS条件は下記の通りである。
・HPLC:1290 InfinityII、Agilent Technologies社
・カラム:Phenomenex Kinetex C18、1.7μm(100mm×2.1mm、I.D.)
・カラム温度:40±0.5℃
・移動相(Mobile phase):(A)0.1%ギ酸−蒸留水(Formic acid in DW)
(B)100%メタノール
・アイソクラティック溶出移動相(Isocratic elution mobile phase):
A:B(40:60、v/v)
・流速:0.2mL/min
・注入量:5μl
・サンプルトレイ温度:10±5℃
・インジェクター洗浄液(強):70%メタノール
・インジェクター洗浄液(弱):30%メタノール
・捕捉時間(Acquisition time):8分
・オートサンプラの実行時間(Autosampler run time):8分
・質量分析計(Mass spectrometer):6490 Triple Quad LC/MS、Agilent Technologies社
・イオン化(Ionization):陽イオン電子スプレー(ESI+)
・モード:MRM
・ガス温度:200℃
・ガスフロー(Gas flow):14L/min
・吸入器(Nebulizer):20psi
・キャピラリー:3000V
詳細なPKプロファイルは、下記の表5の通りである。
[フィナステリドを含む徐放性粒子を含有した皮下注射用組成物の調製]
前記調製例1と同様の方法により徐放性粒子を調製した後、皮下注射用組成物として調製した。
[調製例2で調製された徐放性粒子を用いた薬物動態特性評価]
調製例2で調製された実施例1〜3は、先般の薬物動態評価実験と同じものであり、実施例4および5に対する結果が追加された結果は、下記表6の通りである。
Claims (7)
- フィナステリドを含む徐放性注射用組成物であり、
体内に注入された徐放性注射用組成物はフィナステリドを持続的に放出し、
前記放出されたフィナステリドは、最大血中濃度(Cmax)に対する最初血中濃度(Cint)の比が2〜11である、
フィナステリドを含む徐放性注射用組成物。 - 前記フィナステリドの最大血中濃度(Cmax)は、投与されたフィナステリド1mgに対して0.3μg/L〜0.5μg/Lである、
請求項1に記載のフィナステリドを含む徐放性注射用組成物。 - 前記フィナステリドの薬物濃度曲線下面積(The area under the concentration、AUC0−t)は、投与されたフィナステリド1mgに対して70(μg*h/L)〜100(μg*h/L)である、
請求項1に記載のフィナステリドを含む徐放性注射用組成物。 - 前記徐放性注射用組成物は薬物の放出速度が調節され、初期過放出の問題がなく、
1ヶ月〜3ヶ月間持続的な放出パターンを形成し、
DHTおよびテストステロン(Testosterone)の生成を抑制する、
請求項1に記載のフィナステリドを含む徐放性注射用組成物。 - 前記注射用組成物は懸濁溶剤を含み、
前記懸濁溶剤は、等張剤、懸濁剤、および溶剤を含む、
請求項1に記載のフィナステリドを含む徐放性注射用組成物。 - 前記等張剤は、D−マンニトール(D-Mannitol)、マルチトール(Maltitol)、ソルビトール(Sorbitol)、ラクチトール(Lactitol)、キシリトール(Xylitol)、塩化ナトリウム(Sodium chloride)、およびその混合からなる群より選択される、
請求項5に記載のフィナステリドを含む徐放性注射用組成物。 - 前記懸濁剤は、カルボキシメチルセルロースナトリウム(Sodium Carboxymethylcellulose)、ポリソルベート80(Polysorbate 80)、でんぷん(starch)、でんぷん誘導体、多価アルコール類、キトサン(chitosan)、キトサン誘導体、セルロース(cellulose)、セルロース誘導体、コラーゲン(collagen)、ゼラチン(gelatin)、ヒアルロン酸(hyaluronic acid、HA)、アルギン酸(alginic acid)、アルジン(algin)、ペクチン(pectin)、カラギーナン(carrageenan)、コンドロイチン(chondroitin)、コンドロイチン硫酸(chondroitin sulfate) 、デキストラン(dextran)、デキストラン硫酸(dextran sulfate)、ポリリジン(polylysine)、チチン(titin)、フィブリン(fibrin)、アガロース(agarose)、フルラン(fluran)、キサンタンガム(xanthan gum)、およびその混合からなる群より選択される、
請求項5に記載のフィナステリドを含む徐放性注射用組成物。
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