JPWO2016163403A1 - 経口フィルム製剤 - Google Patents
経口フィルム製剤 Download PDFInfo
- Publication number
- JPWO2016163403A1 JPWO2016163403A1 JP2017511021A JP2017511021A JPWO2016163403A1 JP WO2016163403 A1 JPWO2016163403 A1 JP WO2016163403A1 JP 2017511021 A JP2017511021 A JP 2017511021A JP 2017511021 A JP2017511021 A JP 2017511021A JP WO2016163403 A1 JPWO2016163403 A1 JP WO2016163403A1
- Authority
- JP
- Japan
- Prior art keywords
- oral film
- film preparation
- drug
- gum
- film
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
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- DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical compound CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 claims description 3
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Abstract
Description
[1]高力価薬物およびフィルム形成ポリマーを含む溶液を展延し、乾燥させることにより得られる経口フィルム製剤、
[2]高力価薬物が、ナルフラフィン塩酸塩、ベラプロストナトリウム、イミダフェナシン、リマプロストアルファデクス、ルビプロストンおよびビタミンD誘導体からなる群より選択される1つである上記[1]記載の経口フィルム製剤、
[3]フィルム形成ポリマーが、セルロース、セルロース誘導体、ポリアルキレングリコール、アクリル酸ポリマー、アクリル酸コポリマー、メタクリル酸ポリマー、メタクリル酸コポリマー、ポリアクリルアミド、ポリビニルピロリドン、ポリビニルアルコール、カルボキシメチルセルロース、デンプン、キサンタンガム、カラヤガム、ローカストビーンガム、トラガントガム、グァーガム、アカシアガム、アラビアガム、カラギーナン、デキストリン、デキストラン、アミロース、アルギン酸、アルギン酸塩、カルボキシビニルポリマー、プルラン、キトサン、カルボキシメチルスターチナトリウム、プランタゴ種皮、ガラクトマンナン、オイドラギット、カゼイン、アルギン酸アルキルエステル、ゼラチン、シクロデキストリン、水溶性プルランエーテル(プルランメチルエーテル、プルランエチルエーテル、プルランプロピルエーテルなど)、水溶性プルランエステル(プルランアセテート、プルランブチレートなど)、寒天、デラカント、キチン、タラガム、および、タマリンドガムからなる群より選択される少なくとも1つである上記[1]または[2]記載の経口フィルム製剤、
[4]グリセリン、プロピレングリコール、ポリエチレングリコール、アルキレングリコール、ポリアルキレングリコール、グリセロール、トリアセチン、脱アセチル化モノグリセリド、およびクエン酸トリエチルからなる群より選択される少なくとも1つの可塑剤をさらに含む上記[1]〜[3]のいずれかに記載の経口フィルム製剤、
[5]抗酸化剤をさらに含む上記[1]〜[4]のいずれかに記載の経口フィルム製剤、
[6]経口フィルム製剤が、口腔内崩壊フィルムである上記[1]〜[5]のいずれかに記載の経口フィルム製剤、
[7]上記[1]〜[6]のいずれかに記載の経口フィルム製剤を含む包装体であって、
(a)包材に入れて窒素置換して封入する、および/または
(b)脱酸素剤と共に包材に封入する
ことにより得られる包装体、
[8]上記[1]〜[6]のいずれかに記載の経口フィルム製剤を、脱酸素機能を有する包材により包装して得られる包装体、
[9]脱湿剤をさらに封入する上記[7]または[8]記載の包装体、および
[10]高力価薬物およびフィルム形成ポリマーを含む溶液を展延し、乾燥する、高力価薬物を含有する経口フィルム製剤の製造方法
に関する。
表1の組成にしたがい、(a)水およびエタノールの混液にヒドロキシプロピルセルロース、ヒプロメロースおよびプロピレングリコールを加え、室温で30分間攪拌して溶解した(溶液A)。(b)適量の水(表1の外)にナルフラフィン塩酸塩を加えて室温で5分間攪拌することにより溶解した(溶液B)。(c)(a)の溶液Aと、(b)の溶液Bとを混合し、スリーワンモーターを用いて室温で30分間練合し、薬液Cを得た。
表2の組成にしたがい、(a)水およびエタノールの混液にヒドロキシプロピルセルロース、ヒプロメロース、プロピレングリコールおよび抗酸化剤(亜硫酸ナトリウム)を加え、室温で30分間攪拌して溶解した(溶液A)。(b)適量の水(表2の外)にナルフラフィン塩酸塩を加えて室温で5分間攪拌することにより溶解した(溶液B)。(c)(a)の溶液Aと、(b)の溶液Bとを混合し、スリーワンモーターを用いて室温で30分間練合し、薬液Cを得た。
実施例1〜4(各実施例でn=3)で得られたフィルム製剤について、各ロット当たり3枚のフィルム製剤の薬物濃度を測定し、平均値および標準偏差を算出した。算出された平均値および標準偏差値より、含量均一性の指標として相対標準偏差を算出し、その結果を表3に示す。
実施例3と同様にして作製されたフィルム製剤を、イージーピール(凸版印刷(株)製)に、そのまま、あるいは脱酸素・脱湿剤(三菱瓦斯化学(株)製のファーマキープ(KD−20))と共に封入し、または脱湿機能を有する包材(東洋製罐(株)製のモイスチャーガード(MG))に封入し、80℃の恒温器に入れて保存した。保存開始時、および保存中(3日後、7日後)の製剤について、薬物(ナルフラフィン塩酸塩)含量を測定した。結果を図1に、保存開始時を100とする薬物含量(%)として示す。
保存温度を60℃とし、保存中の測定時期を0.5ヵ月後と1ヵ月後とした以外は試験例2と同様にして、薬物(ナルフラフィン塩酸塩)含量を測定した。結果を図2に、保存開始時を100とする薬物含量(%)として示す。
フィルム製剤を表4に示す包装に封入し、60℃の恒温器に入れて保存した。試料1〜4には実施例3と同様にして作製されたフィルム製剤を用い、試料5には実施例5で得られたフィルム製剤を用いた。保存開始時、および保存中(0.5ヵ月後、1ヵ月後)の製剤について、薬物(ナルフラフィン塩酸塩)含量を測定した。結果を図3に、保存開始時を100とする薬物含量(%)として示す。
Claims (10)
- 高力価薬物およびフィルム形成ポリマーを含む溶液を展延し、乾燥させることにより得られる経口フィルム製剤。
- 高力価薬物が、ナルフラフィン塩酸塩、ベラプロストナトリウム、イミダフェナシン、リマプロストアルファデクス、ルビプロストンおよびビタミンD誘導体からなる群より選択される1つである請求項1記載の経口フィルム製剤。
- フィルム形成ポリマーが、セルロース、セルロース誘導体、ポリアルキレングリコール、アクリル酸ポリマー、アクリル酸コポリマー、メタクリル酸ポリマー、メタクリル酸コポリマー、ポリアクリルアミド、ポリビニルピロリドン、ポリビニルアルコール、カルボキシメチルセルロース、デンプン、キサンタンガム、カラヤガム、ローカストビーンガム、トラガントガム、グァーガム、アカシアガム、アラビアガム、カラギーナン、デキストリン、デキストラン、アミロース、アルギン酸、アルギン酸塩、カルボキシビニルポリマー、プルラン、キトサン、カルボキシメチルスターチナトリウム、プランタゴ種皮、ガラクトマンナン、オイドラギット、カゼイン、アルギン酸アルキルエステル、ゼラチン、シクロデキストリン、水溶性プルランエーテル、水溶性プルランエステル、寒天、デラカント、キチン、タラガム、およびタマリンドガムからなる群より選択される少なくとも1つである請求項1または2記載の経口フィルム製剤。
- グリセリン、プロピレングリコール、ポリエチレングリコール、アルキレングリコール、ポリアルキレングリコール、グリセロール、トリアセチン、脱アセチル化モノグリセリド、およびクエン酸トリエチルからなる群より選択される少なくとも1つの可塑剤をさらに含む請求項1〜3のいずれか1項に記載の経口フィルム製剤。
- 抗酸化剤をさらに含む請求項1〜4のいずれか1項に記載の経口フィルム製剤。
- 経口フィルム製剤が、口腔内崩壊フィルムである請求項1〜5のいずれか1項に記載の経口フィルム製剤。
- 請求項1〜6のいずれか1項に記載の経口フィルム製剤を含む包装体であって、
(a)包材に入れて窒素置換して封入する、および/または
(b)脱酸素剤と共に包材に封入する
ことにより得られる包装体。 - 請求項1〜6のいずれか1項に記載の経口フィルム製剤を、脱酸素機能を有する包材により包装して得られる包装体。
- 脱湿剤をさらに封入する請求項7または8記載の包装体。
- 高力価薬物およびフィルム形成ポリマーを含む溶液を展延し、乾燥する、高力価薬物を含有する経口フィルム製剤の製造方法。
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KR20190107481A (ko) * | 2018-03-12 | 2019-09-20 | 충북대학교 산학협력단 | 멜록시캄을 포함하는 구강붕해필름 제조방법 및 이에 의해 제조된 멜록시캄을 포함하는 구강붕해필름 |
FR3087125B1 (fr) | 2018-10-11 | 2021-07-02 | Ferring Bv | Procede de fabrication d'une formulation solide pour administration orale, installation et formulation solide associees |
JP2020075874A (ja) * | 2018-11-06 | 2020-05-21 | ニプロ株式会社 | ルビプロストン含有フィルム状医薬組成物 |
US11857557B2 (en) | 2019-09-30 | 2024-01-02 | Cure Pharmaceutical, Inc. | Oral dissolvable film containing vitamin D3 |
MX2022011527A (es) * | 2020-03-18 | 2022-11-10 | Cara Therapeutics Inc | Formulaciones de oligosacaridos de agonistas del receptor opioide kappa. |
CN113476427B (zh) * | 2021-07-26 | 2022-11-25 | 北京丰科睿泰医药科技有限公司 | 一种伏硫西汀口腔膜剂及其制备方法 |
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EP3281625A4 (en) | 2018-08-29 |
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EP3281625A1 (en) | 2018-02-14 |
WO2016163403A1 (ja) | 2016-10-13 |
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JP7347474B2 (ja) | 2023-09-20 |
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