JPH03251527A - Oral composition - Google Patents
Oral compositionInfo
- Publication number
- JPH03251527A JPH03251527A JP4633990A JP4633990A JPH03251527A JP H03251527 A JPH03251527 A JP H03251527A JP 4633990 A JP4633990 A JP 4633990A JP 4633990 A JP4633990 A JP 4633990A JP H03251527 A JPH03251527 A JP H03251527A
- Authority
- JP
- Japan
- Prior art keywords
- fatty acid
- acid ester
- sucrose fatty
- salt
- amine derivative
- 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
- 239000000203 mixture Substances 0.000 title claims abstract description 17
- 235000014113 dietary fatty acids Nutrition 0.000 claims abstract description 31
- 239000000194 fatty acid Substances 0.000 claims abstract description 31
- 229930195729 fatty acid Natural products 0.000 claims abstract description 31
- -1 sucrose fatty acid ester Chemical class 0.000 claims abstract description 30
- 229930006000 Sucrose Natural products 0.000 claims abstract description 27
- 239000005720 sucrose Substances 0.000 claims abstract description 27
- 150000001412 amines Chemical class 0.000 claims abstract description 14
- 150000003839 salts Chemical class 0.000 claims abstract description 14
- 125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract description 3
- 239000000126 substance Substances 0.000 claims description 5
- 238000010521 absorption reaction Methods 0.000 abstract description 5
- 150000001875 compounds Chemical class 0.000 abstract description 5
- 238000000034 method Methods 0.000 abstract description 5
- 230000000694 effects Effects 0.000 abstract description 4
- 239000003699 antiulcer agent Substances 0.000 abstract description 3
- 230000002708 enhancing effect Effects 0.000 abstract description 2
- 239000002904 solvent Substances 0.000 abstract description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 abstract 2
- 239000004480 active ingredient Substances 0.000 abstract 2
- 229910000147 aluminium phosphate Inorganic materials 0.000 abstract 1
- 239000000872 buffer Substances 0.000 abstract 1
- 239000002775 capsule Substances 0.000 description 11
- 229940126062 Compound A Drugs 0.000 description 10
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 description 10
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 8
- 239000010419 fine particle Substances 0.000 description 8
- 235000013305 food Nutrition 0.000 description 6
- 210000002700 urine Anatomy 0.000 description 6
- 238000002474 experimental method Methods 0.000 description 5
- 239000008187 granular material Substances 0.000 description 5
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 4
- 238000001035 drying Methods 0.000 description 4
- 150000004665 fatty acids Chemical class 0.000 description 4
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 4
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 4
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 description 4
- 241000700157 Rattus norvegicus Species 0.000 description 3
- 238000004128 high performance liquid chromatography Methods 0.000 description 3
- 238000011084 recovery Methods 0.000 description 3
- DVQHRBFGRZHMSR-UHFFFAOYSA-N sodium methyl 2,2-dimethyl-4,6-dioxo-5-(N-prop-2-enoxy-C-propylcarbonimidoyl)cyclohexane-1-carboxylate Chemical compound [Na+].C=CCON=C(CCC)[C-]1C(=O)CC(C)(C)C(C(=O)OC)C1=O DVQHRBFGRZHMSR-UHFFFAOYSA-N 0.000 description 3
- 230000002485 urinary effect Effects 0.000 description 3
- 239000007900 aqueous suspension Substances 0.000 description 2
- GHVNFZFCNZKVNT-UHFFFAOYSA-N decanoic acid Chemical compound CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 description 2
- POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid Chemical compound CCCCCCCCCCCC(O)=O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 2
- FUZZWVXGSFPDMH-UHFFFAOYSA-N hexanoic acid Chemical compound CCCCCC(O)=O FUZZWVXGSFPDMH-UHFFFAOYSA-N 0.000 description 2
- 238000004513 sizing Methods 0.000 description 2
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 1
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 1
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 1
- ONAIRGOTKJCYEY-XXDXYRHBSA-N CCCCCCCCCCCCCCCCCC(O)=O.O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 Chemical compound CCCCCCCCCCCCCCCCCC(O)=O.O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 ONAIRGOTKJCYEY-XXDXYRHBSA-N 0.000 description 1
- 239000005632 Capric acid (CAS 334-48-5) Substances 0.000 description 1
- 239000005639 Lauric acid Substances 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 239000005642 Oleic acid Substances 0.000 description 1
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 description 1
- 235000021314 Palmitic acid Nutrition 0.000 description 1
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 150000005690 diesters Chemical class 0.000 description 1
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 1
- 239000011812 mixed powder Substances 0.000 description 1
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 150000005691 triesters Chemical class 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Furan Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
［産業上の利用分野］
本発明は、抗潰瘍剤として有用な一般式［工］：「式中
、Ｒは、４−ヒドロキシフェニル、４−カルバモイルフ
ェニル
ホニルアミノフェニル基を示す。」
で表わされるアミン誘導体またはその塩およびショ糖脂
肪酸エステルからなる経口組成物に関する。DETAILED DESCRIPTION OF THE INVENTION [Industrial Application Field] The present invention provides compounds useful as anti-ulcer agents with the general formula [E]: "wherein R is 4-hydroxyphenyl, 4-carbamoylphenylhonylaminophenyl" The present invention relates to an oral composition comprising an amine derivative represented by the following formula or a salt thereof and a sucrose fatty acid ester.
［従来の技術］
一般式［Ｉ］で表わされるアミン誘導体およびその塩は
、攻撃因子抑制作用と防御因子増強作用を兼ね備えた抗
潰瘍剤として有用な化合物である（特開平１−１３１１
７２号公報）が、一般式［Ｉ］で表わされるアミン誘導
体またはその塩およびショ糖脂肪酸エステルからなる経
口組成物については全く知られていない。[Prior Art] Amine derivatives represented by the general formula [I] and salts thereof are useful compounds as anti-ulcer agents that have both an attack factor suppressing effect and a defensive factor enhancing effect (Japanese Patent Laid-Open No. 1-1311
No. 72), but nothing is known about an oral composition comprising an amine derivative represented by the general formula [I] or a salt thereof and a sucrose fatty acid ester.
［発明が解決しようとする課題］
−服代［工］で表わされるアミン誘導体またはその塩を
経口投与した場合、経口吸収性が低く、経口吸収性の向
上が望まれていた。[Problems to be Solved by the Invention] - When the amine derivative represented by Fukudai [tech] or its salt is orally administered, the oral absorption is low, and improvement in the oral absorption has been desired.
［課題を解決するための手段］
かかる状況下において、本発明者らは、−服代［工］で
表わされるアミン誘導体またはその塩にショ糖脂肪酸エ
ステルを配合すれば、著しく経口吸収が高まることを見
出し、本発明を完成させるに至った。[Means for Solving the Problems] Under such circumstances, the present inventors have discovered that if a sucrose fatty acid ester is blended with the amine derivative represented by -Fukudai [technique] or its salt, the oral absorption will be significantly increased. They discovered this and completed the present invention.
以下、本発明の詳細な説明する。The present invention will be explained in detail below.
本発明に使用される一般式［Ｉ］で表わされるアミン誘
導体またはその塩は、特開平１−１３１１７２＠公報に
記載された方法で製造することができる。The amine derivative represented by the general formula [I] or its salt used in the present invention can be produced by the method described in JP-A-1-131172@.
本発明に使用されるショ糖脂肪酸エステルとしては、天
然から得られるものおよび合成により得られるもののい
ずれでもよいが、天然から得られるものが好ましい。シ
ョ糖脂肪酸エステルの脂肪酸としては、直鎖状および分
岐状のもののいずれでもよいが、好ましくは炭素数が５
〜２５個の直鎖状のものが挙げられ、具体的には、カプ
ロン酸、カプリン酸、ミルスチン酸、ステアリン酸、パ
ルミチン酸、ラウリン酸およびオレイン酸などの脂肪酸
が挙げられる。ざらに、ショ糖脂肪酸エステルには、シ
ョ糖１分子に脂肪酸が１個（モノエステル型）、２個（
ジエステル型）または３個（トリエステル型）結合した
ものが存在覆るが、これらの組成比を変えて用いること
ができる。また、ショ糖脂肪酸エステルは１種を単独に
または２種以上を混合して使用してもよい。また、ショ
糖脂肪酸エステルのＨＬＢ値は、３以上が好ましい。The sucrose fatty acid ester used in the present invention may be obtained from nature or synthetically, but those obtained from nature are preferred. The fatty acid of the sucrose fatty acid ester may be either linear or branched, but preferably has 5 carbon atoms.
~25 linear chains, specifically fatty acids such as caproic acid, capric acid, myrstic acid, stearic acid, palmitic acid, lauric acid and oleic acid. In general, sucrose fatty acid esters have one fatty acid per molecule of sucrose (monoester type), two fatty acids (
(diester type) or three (triester type) bonds exist, but these can be used by changing the composition ratio. Further, the sucrose fatty acid esters may be used alone or in combination of two or more. Further, the HLB value of the sucrose fatty acid ester is preferably 3 or more.
本発明に用いられるショ糖脂肪酸エステルの配合量は、
−服代［Ｉ］で表わされるアミン誘導体またはその塩に
対して、重量比で、０．１〜１０倍、好ましくは、０．
２５〜５倍である。The amount of sucrose fatty acid ester used in the present invention is:
- Weight ratio is 0.1 to 10 times, preferably 0.1 to 10 times, preferably 0.1 to 10 times, preferably 0.
25 to 5 times.
本発明の経口組成物は、−服代［Ｉ］で表わされるアミ
ン誘導体またはその塩およびショ糖脂肪酸エステルを水
またはリン酸緩衝液などの溶媒に、溶解または懸濁させ
ることにより得ることができるが、その他には、−服代
［Ｉ］で表わされるアミン誘導体またはその塩にショ糖
脂肪酸エステルを粉末状で混合し、常法により、湿式整
粒法または乾式整粒法で、顆粒または細粒を製造するこ
とができる。また、顆粒、細粒または混合粉末を、カプ
セル充填し、カプセル剤とすることもでき、ざらには、
適当な賦形剤を添加して顆粒剤、細粒剤、カプセル剤ま
たは打錠して錠剤とすることもできる。The oral composition of the present invention can be obtained by dissolving or suspending the amine derivative represented by [I] or its salt and sucrose fatty acid ester in a solvent such as water or a phosphate buffer. However, in other cases, sucrose fatty acid ester is mixed in powder form with the amine derivative represented by [I] or its salt, and then granulated or finely prepared by a wet sizing method or a dry sizing method using a conventional method. Granules can be manufactured. In addition, granules, fine granules, or mixed powders can be filled into capsules to make capsules.
It can also be made into granules, fine granules, capsules, or tablets by adding appropriate excipients.
本発明の経口組成物の投与量および投与回数は、患者の
症状に応じて適宜選択することができ、通常成人に対し
て一般式［Ｉ］で表わされるアミン誘導体換算、１日当
り１１１９／Ｋｇ〜１０ｍ’ｊ／に’ｊを１〜４回に分
割して投与すればよい。The dose and frequency of administration of the oral composition of the present invention can be appropriately selected depending on the patient's symptoms, and is usually 1119/Kg/day for adults in terms of the amine derivative represented by the general formula [I]. 'j may be administered in 1 to 4 divided doses per 10 m'j/.
つぎに、本発明の経口組成物の効果を示す。Next, the effects of the oral composition of the present invention will be shown.
なお、実験には、引−Ｎ−［２−ヒドロキシ−２−（４
−ヒドロキシフェニル）エチル］−Ｎ−メタンスルホニ
ル−Ｎ”−［２−［［５−（メチルアミノ）メチル−２
−フリル］メチルチオ］エチル］グアニジン（以下、化
合物Ａと称する）を使用した。In addition, in the experiment, di-N-[2-hydroxy-2-(4
-hydroxyphenyl)ethyl]-N-methanesulfonyl-N”-[2-[[5-(methylamino)methyl-2
-furyl]methylthio]ethyl]guanidine (hereinafter referred to as compound A) was used.
実験１：ショ糖脂肪酸エステル配合量と尿中回収率
ウィスター系ラット（雄、７週齢）を−夜絶食させた後
、ショ糖脂肪酸エステル［リョートーシュガーエステル
Ｓ−１６７０（三菱化成食品製）］および化合物Ａ（５
ｍｇ／ｄ）を含む水懸濁液１ｍｆ！を経口投与し、投与
後６時間までの尿を採取し、尿中の化合物Ａを高速液体
クロマトグラフィーで測定した。Experiment 1: Sucrose fatty acid ester content and urinary recovery rate After fasting Wistar rats (male, 7 weeks old) overnight, sucrose fatty acid ester [Ryoto Sugar Ester S-1670 (manufactured by Mitsubishi Kasei Foods)] ] and compound A (5
1 mf of aqueous suspension containing mg/d)! was orally administered, urine was collected up to 6 hours after administration, and Compound A in the urine was measured by high performance liquid chromatography.
その結果を表−１に示す。The results are shown in Table-1.
表−１
＊１：化合物Ａに対する重量比
＊２：５匹の平均
実験２：ショ糖脂肪酸エステルの種類と尿中回収率
ウィスター系ラット（雄、７週齢）を−夜絶食させた後
、１ｄ当りショ糖脂肪酸エステル［リョートーシュガー
エステル（三菱化成食品製）］２２０ｍおよび化合物Ａ
５ｍｇを含む水懸濁液１ｍｌを経口投与し、投与後６時
間までの尿を採取し、尿中の化合物Ａを高速液体クロマ
トグラフィーで測定した。Table-1 *1: Weight ratio to Compound A *2: Average of 5 animals Experiment 2: Type of sucrose fatty acid ester and urinary recovery rate Wistar rats (male, 7 weeks old) were fasted overnight. 220 m of sucrose fatty acid ester [Ryoto Sugar Ester (manufactured by Mitsubishi Kasei Foods)] and compound A per 1 d
1 ml of an aqueous suspension containing 5 mg was orally administered, urine was collected up to 6 hours after administration, and Compound A in the urine was measured by high performance liquid chromatography.
その結果を表−２に示す。The results are shown in Table-2.
（以下余白）
表−２
実験３：実施例製剤と尿中回収率
ウィスター系ラット（雄、７週齢）を−夜絶食させた後
、実施例１〜３の製剤を経口投与し、投与後６時間まで
の尿を採取し、尿中の化合物Ａを高速液体クロマトグラ
フィーで測定した。(Margins below) Table 2 Experiment 3: Example formulations and urinary recovery rates Wistar rats (male, 7 weeks old) were fasted overnight and the formulations of Examples 1 to 3 were orally administered. Urine was collected for up to 6 hours, and Compound A in the urine was measured by high performance liquid chromatography.
その結果を表−３に示す。The results are shown in Table-3.
表−３
［発明の効果］
実験１〜３から明らかように、本発明の経口組成物は、
−服代［Ｉ］で表わされるアミン誘導体またはその塩の
経口吸収を向上させる。Table 3 [Effects of the invention] As is clear from Experiments 1 to 3, the oral composition of the present invention
- Improving the oral absorption of the amine derivative represented by [I] or its salt.
［実施例］
つぎに、実施例を挙げて本発明を説明するが、本発明は
これらの実施例に限定されるものではない。[Examples] Next, the present invention will be described with reference to Examples, but the present invention is not limited to these Examples.
実施例１
化合物Ａ１５ｇ、ショ糖脂肪酸エステルＰ−１６７０（
三菱化成食品製）７５３および低置換度ヒドロキシプロ
ピルセルロース（団−３１：信越化学製）３０９を均一
に混合し、ついで、ヒドロキシプロピルセルロース（日
本曹達製）の５％エタノール溶液を加えて練合する。４
０℃で一夜乾燥後、３２メツシユ篩過して細粒を得る。Example 1 Compound A15g, sucrose fatty acid ester P-1670 (
(manufactured by Mitsubishi Kasei Foods) 753 and low-substituted hydroxypropyl cellulose (Gan-31: Shin-Etsu Chemical) 309 are mixed uniformly, and then a 5% ethanol solution of hydroxypropyl cellulose (manufactured by Nippon Soda) is added and kneaded. . 4
After drying at 0° C. overnight, it was passed through a 32 mesh sieve to obtain fine particles.
さらに、得られた細粒を９号カプセル（日本エランコ製
）に充填し、カプセル剤を得る。Furthermore, the obtained fine particles are filled into No. 9 capsules (manufactured by Nippon Elanco) to obtain capsules.
実施例２
化合物Ａ１５ｇ、ショ糖脂肪酸エステルＳ−３７０（三
菱化成食品製）７５９および低置換度ヒドロキシプロピ
ルセルロース（団−３１：信越化学製）３０８を均一に
混合し、ついで、ヒドロキシプロピルセルロース（日本
曹達製）の５％エタノール溶液を加えて練合する。４０
’Ｃで一夜乾燥後、３２メツシユ篩過して細粒を得る。Example 2 15 g of compound A, sucrose fatty acid ester S-370 (manufactured by Mitsubishi Kasei Foods) 759 and low-substituted hydroxypropyl cellulose (dan-31: manufactured by Shin-Etsu Chemical) 308 were uniformly mixed, and then hydroxypropyl cellulose (Japan) Add a 5% ethanol solution (manufactured by Soda) and mix. 40
After drying at 'C overnight, it was passed through a 32 mesh sieve to obtain fine particles.
さらに、得られた細粒を９号カプセル（日本エランコ製
）に充填し、カプセル剤を得る。Furthermore, the obtained fine particles are filled into No. 9 capsules (manufactured by Nippon Elanco) to obtain capsules.
実施例３
化合物Ａ１５ｇ、シヨ糖脂肪酸エステルＰ−１６７０（
三菱化成食品製）６０ｇ、ショ糖脂肪酸エステルＳ−３
７０（三菱化成食品製）１５ｇおよび低置換度ヒドロキ
シプロピルセルロース（Ｌ）Ｉ−３１：信越化学製）３
０９を均一に混合し、ついで、ヒドロキシプロピルセル
ロース（日本曹達製）の５％エタノール溶液を加えて練
合する。４０℃で一夜乾燥後、３２メツシユ篩過して細
粒を得る。ざらに、得られた細粒を９号カプセル（日本
エランコ製）に充填し、カプセル剤を得る。Example 3 Compound A 15g, sucrose fatty acid ester P-1670 (
Mitsubishi Kasei Foods) 60g, sucrose fatty acid ester S-3
70 (manufactured by Mitsubishi Kasei Foods) 15 g and low-substituted hydroxypropyl cellulose (L) I-31: manufactured by Shin-Etsu Chemical) 3
09 are mixed uniformly, and then a 5% ethanol solution of hydroxypropyl cellulose (manufactured by Nippon Soda) is added and kneaded. After drying at 40° C. overnight, it is passed through a 32 mesh sieve to obtain fine particles. The resulting fine particles are then filled into No. 9 capsules (manufactured by Nippon Elanco) to obtain capsules.
参考例
化合物Ａ１５ｇおよび低置換度ヒドロキシプロピルセル
ロース（ＬＨ−３１：信越化学製）３０ｇを均一に混合
し、ついで、ヒドロキシプロピルセルロース（日本曹達
製）の５％エタノール溶液を加えて練合する。４０℃で
一夜乾燥後、３２メツシユ篩過して細粒を得る。さらに
、得られた細粒を９号カプセル（日本エランコ製）に充
填し、カプセル剤を得る。15 g of Reference Example Compound A and 30 g of low-substituted hydroxypropyl cellulose (LH-31, manufactured by Shin-Etsu Chemical) are mixed uniformly, and then a 5% ethanol solution of hydroxypropyl cellulose (manufactured by Nippon Soda) is added and kneaded. After drying at 40° C. overnight, it is passed through a 32 mesh sieve to obtain fine particles. Furthermore, the obtained fine particles are filled into No. 9 capsules (manufactured by Nippon Elanco) to obtain capsules.
Claims (3)
イルフェニルまたは３−メタンスルホニルアミノフェニ
ル基を示す。」 で表わされるアミン誘導体またはその塩およびショ糖脂
肪酸エステルとからなる経口組成物。(1) General formula, ▲ Numerical formula, chemical formula, table, etc. ▼ An amine derivative or An oral composition comprising a salt thereof and a sucrose fatty acid ester.
範囲第（１）項記載の経口組成物。(2) The oral composition according to claim (1), wherein R is a 4-hydroxyphenyl group.
たはその塩に対して、重量比で０．１〜１０倍である特
許請求の範囲第（１）項または第（２）項記載の経口組
成物。(3) The oral composition according to claim (1) or (2), wherein the amount of the sucrose fatty acid ester is 0.1 to 10 times the weight ratio of the amine derivative or its salt. thing.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP4633990A JPH03251527A (en) | 1990-02-27 | 1990-02-27 | Oral composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP4633990A JPH03251527A (en) | 1990-02-27 | 1990-02-27 | Oral composition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH03251527A true JPH03251527A (en) | 1991-11-11 |
Family
ID=12744381
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP4633990A Pending JPH03251527A (en) | 1990-02-27 | 1990-02-27 | Oral composition |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH03251527A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2022034121A1 (en) | 2020-08-11 | 2022-02-17 | Université De Strasbourg | H2 blockers targeting liver macrophages for the prevention and treatment of liver disease and cancer |
-
1990
- 1990-02-27 JP JP4633990A patent/JPH03251527A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2022034121A1 (en) | 2020-08-11 | 2022-02-17 | Université De Strasbourg | H2 blockers targeting liver macrophages for the prevention and treatment of liver disease and cancer |
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