WO2004096229A1 - Composition medicamenteuse en solution - Google Patents

Composition medicamenteuse en solution Download PDF

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Publication number
WO2004096229A1
WO2004096229A1 PCT/JP2004/006159 JP2004006159W WO2004096229A1 WO 2004096229 A1 WO2004096229 A1 WO 2004096229A1 JP 2004006159 W JP2004006159 W JP 2004006159W WO 2004096229 A1 WO2004096229 A1 WO 2004096229A1
Authority
WO
WIPO (PCT)
Prior art keywords
compound
pharmaceutical composition
solution
solution pharmaceutical
amount
Prior art date
Application number
PCT/JP2004/006159
Other languages
English (en)
Japanese (ja)
Inventor
Masaru Higaki
Takayuki Murakami
Original Assignee
Dainippon Sumitomo Pharma Co., Ltd.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Dainippon Sumitomo Pharma Co., Ltd. filed Critical Dainippon Sumitomo Pharma Co., Ltd.
Priority to JP2005505932A priority Critical patent/JP4607761B2/ja
Priority to CN2004800179834A priority patent/CN1812794B/zh
Priority to KR1020057020365A priority patent/KR101169478B1/ko
Publication of WO2004096229A1 publication Critical patent/WO2004096229A1/fr
Priority to HK07101101.7A priority patent/HK1095737A1/xx

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

  • the present invention provides a solution pharmaceutical composition containing mosapride, which is useful as an injection or an oral preparation, that is, a solution composition having both solubility and pH within a desired range and having high stability. Make it an issue.
  • the amount of water in the composition, compound A, propylene glycol, and the remainder except for the oxidizing substances themselves and the additives themselves, which are added as necessary, are water, the amount of which is necessary to complete the solution pharmaceutical composition. It is. With respect to this amount of water, “the amount necessary to complete the solution pharmaceutical composition” means the total amount of water used in the process of preparing the desired solution pharmaceutical composition, and dissolves Compound A in propylene dalicol When propylene glycol is used as an aqueous solution at the time, the amount of water is used when adjusting the amount of water, when adding an acidic substance, the amount of water to be used as the aqueous solution, and finally when adjusting the total amount of the solution pharmaceutical composition. It is the total amount, such as the amount of residual water added.
  • Compound A or a physiologically acceptable salt thereof is added to a Zl solution obtained by adding a predetermined amount of propylene glycol to a certain amount of water and mixing, followed by stirring and dissolving.
  • the pH is adjusted to a desired pH by adding an appropriate amount of the above-mentioned acidic substance. Dissolve the physiologically acceptable salt.
  • the pH can be adjusted to an appropriate pH by adding the acidic substance as necessary. Coordination is encouraged.
  • water is added to adjust the volume of the composition to prepare the solution pharmaceutical composition of the present invention. That is, in preparing the above composition, it is preferable to use a slightly smaller amount of water to be mixed with propylene glycol, and to adjust the volume to a certain volume by finally adding water.
  • the drug-containing powder or granule contains Compound A or a physiologically acceptable salt thereof, and contains various additives used in the above solution injection or oral solution. Fill in a suitable container.
  • the required amount of the above-mentioned drug solution is added to the drug-containing powdery or granular substance, and the compound A is sufficiently mixed and dissolved to thereby provide the compound of the present invention.
  • Solution compositions can be prepared and used.
  • Test Example 2 The test performed in Test Example 2 below, that is, the stability test under the conditions of “storage at 60 ° C. for one month” was performed to show that the composition of the present invention was extremely stable. This is a stability test under severe conditions. Accelerated stability test, usually performed to estimate the storage stability of a drug at room temperature, from "40 ° C, 6 months storage” Is also a severe test.
  • Test example 2 60 ° C, 1 month stability test
  • Example 13 (Injection containing compound A_a 1.72 mg gm1) (no acidic substance added) According to the formulation (production amount) shown in Formulation Example 7 (Table 11), an injection of compound A-a was produced. That is, 2 liters of water for injection was placed in a stainless steel container, 2.5 kg of propylene glycol was added, and the mixture was stirred for 5 minutes with a stirrer (FBL 1200 MM, manufactured by Fine) to mix uniformly. Next, 13.225 g of compound A-b was added and stirred for 15 minutes. The H of the resulting solution was 4.5. Thereafter, an appropriate amount of water for injection was added to make the total amount 5 liters.
  • a stirrer FBL 1200 MM, manufactured by Fine
  • Example 15 (Compound A-a 3.43 mg / m1 containing injection)

Landscapes

  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

La présente invention a trait à une composition médicamenteuse en solution comprenant (a) un composé 4-amino-5-chloro-2-éthoxy-N-[4-(4-fluorobenzyl)-2-morpholinyl]méthyl]benzamide (composé A) ou un de ses sels pharmaceutiquement acceptables, (b) du propylène glycol, et (c) de l'eau. La composition médicamenteuse en solution contenant le composé (A) est utile sous forme d'injection ou de médicament peroral. En d'autres mots, la composition médicamenteuse en solution présente une solubilité et un pH dans des plages souhaitées et présente une grande stabilité.
PCT/JP2004/006159 2003-04-30 2004-04-28 Composition medicamenteuse en solution WO2004096229A1 (fr)

Priority Applications (4)

Application Number Priority Date Filing Date Title
JP2005505932A JP4607761B2 (ja) 2003-04-30 2004-04-28 溶液医薬組成物
CN2004800179834A CN1812794B (zh) 2003-04-30 2004-04-28 溶液药用组合物
KR1020057020365A KR101169478B1 (ko) 2003-04-30 2004-04-28 용액 의약조성물
HK07101101.7A HK1095737A1 (en) 2003-04-30 2007-01-31 Medicinal composition in solution form

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2003-124694 2003-04-30
JP2003124694 2003-04-30

Publications (1)

Publication Number Publication Date
WO2004096229A1 true WO2004096229A1 (fr) 2004-11-11

Family

ID=33410196

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2004/006159 WO2004096229A1 (fr) 2003-04-30 2004-04-28 Composition medicamenteuse en solution

Country Status (6)

Country Link
JP (1) JP4607761B2 (fr)
KR (1) KR101169478B1 (fr)
CN (1) CN1812794B (fr)
HK (1) HK1095737A1 (fr)
TW (1) TW200509941A (fr)
WO (1) WO2004096229A1 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007083679A1 (fr) * 2006-01-20 2007-07-26 Dainippon Sumitomo Pharma Co., Ltd. Nouveau comprimé pelliculé
JP2010515740A (ja) * 2007-01-10 2010-05-13 ノバルティス アーゲー デアセチラーゼインヒビター製剤
JP2013522320A (ja) * 2010-03-18 2013-06-13 イノファーマ，インコーポレイテッド 安定なボルテゾミブ製剤

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101405615B1 (ko) * 2007-08-27 2014-06-12 (주)아모레퍼시픽 조성물 내 ｐＨ 조절을 통해 안정화된 벤즈아미드 화합물을함유하는 피부 외용제 조성물, 및 그 벤즈아미드 화합물안정화 방법

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS63264467A (ja) * 1986-04-30 1988-11-01 Dainippon Pharmaceut Co Ltd ベンズアミド誘導体
JP2002532535A (ja) * 1998-12-22 2002-10-02 アメリカ合衆国 水不溶性薬剤送達システム

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS63264467A (ja) * 1986-04-30 1988-11-01 Dainippon Pharmaceut Co Ltd ベンズアミド誘導体
JP2002532535A (ja) * 1998-12-22 2002-10-02 アメリカ合衆国 水不溶性薬剤送達システム

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
"6306.Mosapride", THE MERCK INDEX (13TH EDITION), 2001, pages 1122 - 1123, XP008041234 *
IYAKUHIN TENKABUTSU KENKYUKAI: "Jitsuyo iyakuhin tenkabutsu", KAGAKU KOGOYOSHA, 5 March 1974 (1974-03-05), pages 126 - 134, XP002984603 *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007083679A1 (fr) * 2006-01-20 2007-07-26 Dainippon Sumitomo Pharma Co., Ltd. Nouveau comprimé pelliculé
JP4972563B2 (ja) * 2006-01-20 2012-07-11 大日本住友製薬株式会社 新規なフィルムコーティング錠
JP2010515740A (ja) * 2007-01-10 2010-05-13 ノバルティス アーゲー デアセチラーゼインヒビター製剤
JP2013522320A (ja) * 2010-03-18 2013-06-13 イノファーマ，インコーポレイテッド 安定なボルテゾミブ製剤

Also Published As

Publication number Publication date
JPWO2004096229A1 (ja) 2006-07-13
KR101169478B1 (ko) 2012-07-27
CN1812794B (zh) 2011-06-29
HK1095737A1 (en) 2007-05-18
TW200509941A (en) 2005-03-16
KR20060004964A (ko) 2006-01-16
JP4607761B2 (ja) 2011-01-05
CN1812794A (zh) 2006-08-02

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