JP6013329B2 - 加速された活性の発現を有するテイストマスキング医薬組成物 - Google Patents
加速された活性の発現を有するテイストマスキング医薬組成物 Download PDFInfo
- Publication number
- JP6013329B2 JP6013329B2 JP2013515773A JP2013515773A JP6013329B2 JP 6013329 B2 JP6013329 B2 JP 6013329B2 JP 2013515773 A JP2013515773 A JP 2013515773A JP 2013515773 A JP2013515773 A JP 2013515773A JP 6013329 B2 JP6013329 B2 JP 6013329B2
- Authority
- JP
- Japan
- Prior art keywords
- taste
- sugar alcohol
- pharmaceutical composition
- sodium bicarbonate
- phosphodiesterase inhibitor
- 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.)
- Expired - Fee Related
Links
Classifications
-
- 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
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
-
- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- 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
- A61K47/02—Inorganic compounds
-
- 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
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
- A61K9/0058—Chewing gums
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
-
- 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
- A61K9/14—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
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biophysics (AREA)
- Physiology (AREA)
- Molecular Biology (AREA)
- Nutrition Science (AREA)
- Zoology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Inorganic Chemistry (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Gynecology & Obstetrics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
ホスホジエステラーゼ阻害剤:合計で約10から約150質量部
糖アルコール:合計で約50から約600質量部;及び
炭酸水素ナトリウム:約2から約100質量部
で含む、口内投与のための医薬組成物に関する。
a)約10質量部、より好ましくは約25から約150質量部の量の活性成分;
b)約50から約600質量部、好ましくは約100から約300質量部の量の糖アルコール、特にイソマルト;
c)約2から約100質量部、好ましくは約50質量部の量の炭酸水素ナトリウム;及び任意選択で
d)約2から約50質量部、好ましくは約5から約10質量部又は約10から約50質量部の量のクエン酸。
活性成分: 50mg
イソマルト: 300mg
炭酸水素ナトリウム: 50mg
クエン酸: 12.5mg
及び任意選択で香味料を含む。
R2はメトキシ、エトキシ、プロポキシ、メチル、エチル、又はプロピルであり;
XはO、S、又はNである。
R2はメトキシ、エトキシ、プロポキシ、メチル、エチル、又はプロピルであり;
ヘテロ環は、置換されたヘテロ環である。
クエン酸シルディナフィル 0.05
イソマルト 0.3
クエン酸 0.01
炭酸水素ナトリウム 0.05
香味料 適量
クエン酸シルディナフィル 0.025
イソマルト 0.3
クエン酸 0.01
炭酸水素ナトリウム 0.05
香味料 適量
クエン酸シルディナフィル 0.1
イソマルト 0.3
クエン酸 0.01
炭酸水素ナトリウム 0.05
香味料 適量
タダラフィル 0.05
イソマルト 0.3
クエン酸 0.005
炭酸水素ナトリウム 0.05
香味料 適量
ヒドロキシホモシルディナフィル 0.025
イソマルト 0.3
クエン酸 0.01
炭酸水素ナトリウム 0.05
香味料 適量
クエン酸シルディナフィルの経口吸収に比べてより速い口内吸収を実証するために、クロスオーバーデザイン試験において、本発明の実施例1の処方と、ドイツで一般的に市販されている製品である、クエン酸シルディナフィルの活性成分を含むバイアグラ50mgとを対比して試験する、20人の被験者による実測的調査を行った。結果を表1にまとめた。この結果は、その活性の発現までの時間が予想外にも大幅に短縮したことを実証した。
Claims (4)
- クエン酸シルディナフィルから選択される少なくとも1つのホスホジエステラーゼ阻害剤と、イソマルトから選ばれる少なくとも1つの糖アルコールと、クエン酸と、医薬賦形剤としての炭酸水素ナトリウムとを、以下の質量比:
ホスホジエステラーゼ阻害剤:合計で10から150質量部
糖アルコール:合計で50から600質量部;及び
炭酸水素ナトリウム:2から100質量部
で含み、
前記ホスホジエステラーゼ阻害剤:糖アルコールの質量比が1:3〜1:24であり、
前記糖アルコール:炭酸水素ナトリウムの質量比が1:1〜10:1であり、
前記ホスホジエステラーゼ阻害剤及び前記糖アルコールは粉末混合物又は顆粒として、或いは、圧縮された錠剤中の粉末混合物又は顆粒として存在する、
口内投与のための医薬組成物。 - 糖アルコール:ホスホジエステラーゼ阻害剤の質量比が6:1までであることを特徴とする、請求項1に記載の医薬組成物。
- 前記医薬賦形剤が、流動性添加剤、アラキン酸カルシウム、フマル酸ステアリルナトリウム、及び/若しくはPEG6000から選択される流動促進剤/潤滑剤、崩壊剤、並びに少なくとも1つの香料添加剤をさらに含むことを特徴とする、請求項1又は2に記載の医薬組成物。
- 活性の加速された発現による男性の勃起障害を治療する方法において使用するための、請求項1〜3のいずれか1項に記載の医薬組成物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE102010024866A DE102010024866A1 (de) | 2010-06-24 | 2010-06-24 | Formulierung zur Geschmacksmaskierung |
DE102010024866.5 | 2010-06-24 | ||
PCT/EP2011/003120 WO2011160849A1 (en) | 2010-06-24 | 2011-06-24 | Taste-masked pharmaceutical formulation having accelerated onset of action |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2013529605A JP2013529605A (ja) | 2013-07-22 |
JP6013329B2 true JP6013329B2 (ja) | 2016-10-25 |
Family
ID=44629118
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2013515773A Expired - Fee Related JP6013329B2 (ja) | 2010-06-24 | 2011-06-24 | 加速された活性の発現を有するテイストマスキング医薬組成物 |
Country Status (10)
Country | Link |
---|---|
US (1) | US20130150370A1 (ja) |
EP (1) | EP2585041B1 (ja) |
JP (1) | JP6013329B2 (ja) |
BR (1) | BR112012032463A2 (ja) |
CA (1) | CA2802604C (ja) |
DE (1) | DE102010024866A1 (ja) |
EA (1) | EA031697B1 (ja) |
ES (1) | ES2604484T3 (ja) |
PL (1) | PL2585041T3 (ja) |
WO (1) | WO2011160849A1 (ja) |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2013109221A1 (en) * | 2012-01-18 | 2013-07-25 | Mahmut Bilgic | New effervescent formulations comprising sweetener composition |
WO2014106962A1 (ko) * | 2013-01-07 | 2014-07-10 | 삼아제약 주식회사 | 향상된 용해도를 갖는 신규한 속용성 과립제형 |
US20160317542A1 (en) | 2013-12-09 | 2016-11-03 | Respira Therapeutics, Inc. | Pde5 inhibitor powder formulations and methods relating thereto |
CA3172688A1 (en) | 2020-03-24 | 2021-09-30 | Haifeng Li | Radiating elements having angled feed stalks and base station antennas including same |
Family Cites Families (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IT1217445B (it) * | 1988-04-29 | 1990-03-22 | Altergon Sa | Composizione farmaceutiche orosolubili contenti acetilcisteina |
US4942039A (en) * | 1989-05-09 | 1990-07-17 | Miles Inc. | Effervescent analgesic antacid composition having reduced sodium content |
GT199900061A (es) * | 1998-05-15 | 2000-10-14 | Pfizer | Formulaciones farmaceuticas. |
WO2000057857A1 (en) * | 1999-03-25 | 2000-10-05 | Yuhan Corporation | Rapidly disintegrable tablet for oral administration |
CA2417736A1 (en) * | 2000-07-19 | 2002-01-24 | Lavipharm Laboratories, Inc. | Sildenafil citrate solid dispersions having high water solubility |
SE0202365D0 (sv) * | 2002-08-05 | 2002-08-05 | Pharmacia Ab | New formulation and use thereof |
KR100503949B1 (ko) * | 2003-04-28 | 2005-07-26 | 주식회사유한양행 | 염산 온단세트론의 쓴맛을 효과적으로 은폐한 경구용 구강속붕해정 조성물 |
DE10328180A1 (de) * | 2003-06-16 | 2005-01-13 | Südzucker AG Mannheim/Ochsenfurt | Verwendung von Isomalt als Präbiotikum |
GB0330255D0 (en) * | 2003-12-31 | 2004-02-04 | Vectura Ltd | Multiparticulate formulations for oral delivery |
US20080287456A1 (en) * | 2004-05-28 | 2008-11-20 | Imaginot Pty Ltd | Oral Therapeutic Compound Delivery System |
WO2007060682A1 (en) * | 2005-11-28 | 2007-05-31 | Strides Arcolab Limited | Effervescent granular formulations of antiretroviral drugs |
US8642016B2 (en) * | 2006-07-21 | 2014-02-04 | Jsrnti, Llc | Medicinal delivery system, and related methods |
KR100895942B1 (ko) * | 2007-05-08 | 2009-05-07 | 조선대학교산학협력단 | 생약 추출물을 함유하는 구강 내 속붕해성 제제 조성물 및그의 제조 방법 |
WO2009007768A1 (en) * | 2007-07-06 | 2009-01-15 | Gumlink A/S | Compressed tablet comprising polyol |
WO2009106824A2 (en) * | 2008-02-25 | 2009-09-03 | Cipla Limited | Pharmaceutical formulations |
JP2012505878A (ja) * | 2008-10-14 | 2012-03-08 | マクニール アーベー | 複数部分口内剤形及びその使用 |
-
2010
- 2010-06-24 DE DE102010024866A patent/DE102010024866A1/de not_active Withdrawn
-
2011
- 2011-06-24 WO PCT/EP2011/003120 patent/WO2011160849A1/en active Application Filing
- 2011-06-24 PL PL11736275T patent/PL2585041T3/pl unknown
- 2011-06-24 BR BR112012032463A patent/BR112012032463A2/pt not_active IP Right Cessation
- 2011-06-24 ES ES11736275.6T patent/ES2604484T3/es active Active
- 2011-06-24 CA CA2802604A patent/CA2802604C/en not_active Expired - Fee Related
- 2011-06-24 JP JP2013515773A patent/JP6013329B2/ja not_active Expired - Fee Related
- 2011-06-24 EA EA201390012A patent/EA031697B1/ru not_active IP Right Cessation
- 2011-06-24 US US13/805,587 patent/US20130150370A1/en not_active Abandoned
- 2011-06-24 EP EP11736275.6A patent/EP2585041B1/en not_active Not-in-force
Also Published As
Publication number | Publication date |
---|---|
BR112012032463A2 (pt) | 2016-11-08 |
ES2604484T3 (es) | 2017-03-07 |
CA2802604C (en) | 2018-11-06 |
US20130150370A1 (en) | 2013-06-13 |
PL2585041T3 (pl) | 2017-02-28 |
EP2585041B1 (en) | 2016-08-31 |
EA031697B1 (ru) | 2019-02-28 |
DE102010024866A1 (de) | 2011-12-29 |
EA201390012A1 (ru) | 2013-07-30 |
CA2802604A1 (en) | 2011-12-29 |
WO2011160849A1 (en) | 2011-12-29 |
EP2585041A1 (en) | 2013-05-01 |
JP2013529605A (ja) | 2013-07-22 |
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