WO2017170509A1 - Amorphizing agent, amorphous composition comprising amorphizing agent and utilization thereof - Google Patents
Amorphizing agent, amorphous composition comprising amorphizing agent and utilization thereof Download PDFInfo
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- 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
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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- 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
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
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- A—HUMAN NECESSITIES
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- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
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- 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
- A61K47/46—Ingredients of undetermined constitution or reaction products thereof, e.g. skin, bone, milk, cotton fibre, eggshell, oxgall or plant extracts
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- 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
- A61K9/08—Solutions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
Definitions
- water-soluble polymer and acid Only one kind of water-soluble polymer and acid can be used, or two or more kinds can be used in combination.
- a preferred embodiment is an embodiment in which a water-soluble polymer and an acid are used in combination.
- Example 2 About pharmaceutical composition 1 of the prescription shown below, the film formulation was manufactured in the procedure shown next.
Abstract
Description
[3] 前記ビニル系水溶性高分子は、ポリビニルピロリドン又はカルボキシビニルポリマーである、[2]に記載の非晶質化剤。
[4] 前記セルロース系水溶性高分子は、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロース、ヒドロキシエチルメチルセルロース、メチルセルロース又はエチルセルロースである、[2]に記載の非晶質化剤。
[5] 前記酸は、有機酸である、[1]~[4]の何れかに記載の非晶質化剤。
[6] 水溶性高分子及び酸からなる、[1]~[5]の何れかに記載の非晶質化剤。
[7] 前記一般式(1)で表される化合物は、ルリコナゾール又はラノコナゾールである、[1]~[6]の何れかに記載の非晶質化剤。 [2] The amorphizing agent according to [1], wherein the water-soluble polymer is a vinyl-based water-soluble polymer or a cellulose-based water-soluble polymer.
[3] The amorphizing agent according to [2], wherein the vinyl-based water-soluble polymer is polyvinylpyrrolidone or carboxyvinyl polymer.
[4] The amorphizing agent according to [2], wherein the cellulose-based water-soluble polymer is hydroxypropylcellulose, hydroxypropylmethylcellulose, hydroxyethylmethylcellulose, methylcellulose, or ethylcellulose.
[5] The amorphizing agent according to any one of [1] to [4], wherein the acid is an organic acid.
[6] The amorphizing agent according to any one of [1] to [5], comprising a water-soluble polymer and an acid.
[7] The amorphizing agent according to any one of [1] to [6], wherein the compound represented by the general formula (1) is luliconazole or lanoconazole.
[9] 一般式(1)で表される化合物及び/又はその塩と、該化合物及び/又はその塩の質量の0.05~10倍の質量の[1]~[7]の何れかに記載の非晶質化剤とを含んでなる非晶質の組成物。
[10] [9]に記載の非晶質の組成物を中間仕掛品として、該中間仕掛品を溶解する工程を含む、一般式(1)で表される化合物及び/又はその塩を含有する医薬組成物の製造方法。
[11] 一般式(1)で表される化合物及び/又はその塩と、該化合物及び/又はその塩の質量の0.05~10倍の質量の[1]~[7]の何れかに記載の非晶質化剤を含んでなる、組成物。
[12] 更に、揮散すべき溶媒を含む、[11]に記載の組成物。
[13] 医薬である、[11]又は[12]に記載の組成物。 [8] The compound represented by the general formula (1) and / or a salt thereof and any one of [1] to [7] having a mass of 0.05 to 10 times the mass of the compound and / or the salt thereof A method for amorphizing a compound represented by the general formula (1) and / or a salt thereof, comprising a step of uniformly mixing and solidifying the described amorphizing agent.
[9] The compound represented by the general formula (1) and / or a salt thereof and any one of [1] to [7] having a mass 0.05 to 10 times the mass of the compound and / or the salt thereof An amorphous composition comprising the described amorphizing agent.
[10] A compound represented by the general formula (1) and / or a salt thereof, comprising the step of dissolving the intermediate work-in-process using the amorphous composition described in [9] as an intermediate work-in-process. A method for producing a pharmaceutical composition.
[11] The compound represented by the general formula (1) and / or a salt thereof and any one of [1] to [7] having a mass of 0.05 to 10 times the mass of the compound and / or the salt thereof A composition comprising the described amorphizing agent.
[12] The composition according to [11], further comprising a solvent to be stripped.
[13] The composition according to [11] or [12], which is a medicine.
本発明の非晶質化剤は、一般式(1)で表される化合物及び/またはその塩の非晶質化剤であって、水溶性高分子及び酸から選ばれる1種又は2種以上からなることを特徴とする。
前記水溶性高分子としては、例えば、ポリビニルアルコール、ポリビニルピロリドン、カルボキシビニルポリマーなどのビニル系水溶性高分子、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロース、ヒドロキシプロピルメチルセルローステレフタレート、ヒドロキシエチルメチルセルロース、エチルセルロースなどのセルロース系水溶性高分子、アラビアゴム、トラガカントゴム、キサンタンゴムなどの多糖類水溶性高分子などが好適に例示できる。これらのうちビニル系水溶性高分子又はセルロース系水溶性高分子が好ましく例示できる。ビニル系高分子としては、ポリビニルピロリドン又はカルボキシビニルポリマーが好ましく例示でき、セルロース系水溶性高分子としては、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロース、ヒドロキシエチルメチルセルロース、メチルセルロース又はエチルセルロースが好ましく例示できる。水溶性高分子として、1種又は2種以上を用いることができる。 (1) Amorphizing agent of the present invention The amorphizing agent of the present invention is an amorphizing agent of a compound represented by the general formula (1) and / or a salt thereof, and is a water-soluble polymer. And one or more selected from acids.
Examples of the water-soluble polymer include vinyl-based water-soluble polymers such as polyvinyl alcohol, polyvinyl pyrrolidone, and carboxyvinyl polymer, and cellulose-based polymers such as hydroxypropylcellulose, hydroxypropylmethylcellulose, hydroxypropylmethylcellulose terephthalate, hydroxyethylmethylcellulose, and ethylcellulose. Preferable examples include water-soluble polymers, polysaccharide water-soluble polymers such as gum arabic, tragacanth gum, and xanthan gum. Of these, vinyl water-soluble polymers and cellulose water-soluble polymers are preferred. Preferred examples of the vinyl polymer include polyvinyl pyrrolidone and carboxyvinyl polymer, and preferred examples of the cellulose water-soluble polymer include hydroxypropyl cellulose, hydroxypropyl methyl cellulose, hydroxyethyl methyl cellulose, methyl cellulose, and ethyl cellulose. 1 type (s) or 2 or more types can be used as a water-soluble polymer.
本発明の非晶質化剤が対象とする化合物は、一般式(1)で表されることを特徴とする。
一般式(1)において、R1、R2で表される基は、水素原子又はハロゲン原子であり、当該ハロゲン原子としては、塩素原子、臭素原子、フッ素原子、ヨウ素原子などが好適に例示でき、水素原子又は塩素原子が特に好ましい。 (2) Compound represented by general formula (1) and / or salt thereof The compound targeted by the amorphizing agent of the present invention is represented by general formula (1).
In general formula (1), the groups represented by R 1 and R 2 are hydrogen atoms or halogen atoms, and preferred examples of the halogen atoms include chlorine atoms, bromine atoms, fluorine atoms, and iodine atoms. A hydrogen atom or a chlorine atom is particularly preferred.
かかる化合物は、例えば、特開昭60-218387号に記載されている方法に従って合成することができる。具体的には、下記式に記載の方法により合成することができる。即ち、以下のように、1-シアノメチルイミダゾールと二硫化炭素とを反応させ、(III)の化合物を得、これと脱離基を有する一般式(II)の化合物と反応させることにより、一般式(I)で表される化合物を得ることができる。脱離基としては、例えば、メタンスルホニルオキシ基、ベンゼンスルホニルオキシ基、p-トルエンスルホニルオキシ基又はハロゲン原子等が好適に例示できる。下記式中、R及びXは、水素原子又はハロゲン原子を表す。 Among the compounds represented by the general formula (1) and / or salts thereof, particularly preferred are luliconazole (R 1 = R 2 = Cl; (R)-(−)-(E)-[4- (2 , 4-dichlorophenyl) -1,3-dithiolane-2-ylidene] -1-imidazolylacetonitrile) and ranoconazole (R 1 = Cl, R 2 = H; 4- (2-chlorophenyl) -1,3-dithiolane-2 -Iridene-1-imidazolylacetonitrile), and luliconazole is particularly preferred.
Such a compound can be synthesized, for example, according to the method described in JP-A-60-218387. Specifically, it can be synthesized by the method described in the following formula. That is, as shown below, 1-cyanomethylimidazole and carbon disulfide are reacted to obtain a compound of (III), which is reacted with a compound of the general formula (II) having a leaving group. A compound represented by the formula (I) can be obtained. Preferable examples of the leaving group include a methanesulfonyloxy group, a benzenesulfonyloxy group, a p-toluenesulfonyloxy group, and a halogen atom. In the following formulae, R and X represent a hydrogen atom or a halogen atom.
本発明の非晶質の組成物は、前記本発明の非晶質化剤と、前記一般式(1)で表される化合物及び/又はその塩とを必須の構成とする。本発明の非晶質の組成物は、一般式(1)で表される化合物及び/又は塩と、該化合物/又はその塩の質量の0.05~10倍の質量の非晶質化剤を均一に混合し、溶媒揮散させ固化させて得ることができる。また、一般式(1)で表される化合物及び/又は塩と、該化合物及び/又はその塩の質量の0.05~10倍の質量の非晶質化剤を均一に混合させて得られる組成物は、本発明の組成物である。本発明の組成物は、一般式(1)で表される化合物及び/又は塩と、非晶質化剤に加え、さらに、溶媒を含んでもよい。本発明の組成物は、一般式(1)で表される化合物及び/又はその塩が、抗真菌効果を有することから、医薬組成物であってよく、好ましくは抗真菌医薬組成物、より好ましくは爪用の抗真菌医薬組成物である。また、本発明の組成物は、医薬品調製用の組成物、即ち、医薬品製造のための中間仕掛品であってよい。
本発明の非晶質の組成物もまた、一般式(1)で表される化合物及び/又はその塩が、抗真菌効果を有することから、医薬組成物であってよく、好ましくは抗真菌医薬組成物、より好ましくは爪用の抗真菌医薬組成物である。
該医薬組成物の剤形としては、被膜剤形が好ましい。その使用態様は、患者の体重、年令、性別、症状等を考慮して適宜選択できるが、通常成人の場合、一般式(1)で表される化合物及び/又はその塩を1日当たり0.01~1g投与するのが好ましい。また、真菌による疾病に通常使用されている一般式(1)で表される化合物及び/又はその塩の使用量を参考にすることができる。
例えば、一日に一回又は数回、疾病の箇所に適量を塗布することが例示でき、かかる処置は連日行われることが好ましい。 (3) Amorphous composition of the present invention The amorphous composition of the present invention comprises an amorphizing agent of the present invention, a compound represented by the general formula (1) and / or a salt thereof. Is an essential configuration. The amorphous composition of the present invention comprises a compound and / or salt represented by the general formula (1) and an amorphizing agent having a mass 0.05 to 10 times the mass of the compound / or salt thereof. Can be obtained by uniformly mixing, evaporating the solvent and solidifying. Further, it is obtained by uniformly mixing the compound and / or salt represented by the general formula (1) and the amorphizing agent having a mass of 0.05 to 10 times the mass of the compound and / or salt thereof. The composition is a composition of the present invention. The composition of the present invention may further contain a solvent in addition to the compound and / or salt represented by the general formula (1) and the amorphizing agent. The composition of the present invention may be a pharmaceutical composition, preferably an antifungal pharmaceutical composition, more preferably, since the compound represented by the general formula (1) and / or a salt thereof has an antifungal effect. Is an antifungal pharmaceutical composition for nails. The composition of the present invention may be a composition for preparing a pharmaceutical product, that is, an intermediate work-in-process for manufacturing a pharmaceutical product.
The amorphous composition of the present invention may also be a pharmaceutical composition since the compound represented by the general formula (1) and / or a salt thereof has an antifungal effect, and preferably an antifungal medicament. A composition, more preferably an antifungal pharmaceutical composition for nails.
The dosage form of the pharmaceutical composition is preferably a film dosage form. The mode of use can be appropriately selected in consideration of the patient's weight, age, sex, symptoms, etc. In general, in the case of an adult, the compound represented by the general formula (1) and / or a salt thereof is reduced to 0. It is preferable to administer 01 to 1 g. Moreover, the usage-amount of the compound represented by General formula (1) normally used for the disease by fungi and / or its salt can be referred.
For example, an appropriate amount can be applied to the site of the disease once or several times a day, and such treatment is preferably performed every day.
中間仕掛品としての本発明の非晶質の組成物は、溶解しやすい安定な中間仕掛品を提供する。この様な中間仕掛品を用いることにより、類縁体生成の少ない一般式(1)で表される化合物及び/又は塩を含有する医薬組成物の製造方法が提供できる。 Moreover, this invention uses the amorphous composition of this invention as an intermediate work-in-process, The pharmaceutical containing the compound and / or salt represented by General formula (1) including the process of melt | dissolving this intermediate work-in-process. The present invention relates to a method for producing a composition.
The amorphous composition of the present invention as an intermediate work-in-process provides a stable intermediate work-in-process that is easy to dissolve. By using such an intermediate work-in-process, it is possible to provide a method for producing a pharmaceutical composition containing a compound and / or a salt represented by the general formula (1) with little analog production.
ルリコナゾール1質量%含有エタノール溶液と、ルリコナゾール1質量%及びポリビニルピロリドン0.1質量%含有エタノール溶液を調製し、スライドグラス上に滴下し、その性状を、滴下直後、滴下後室温保存4時間、滴下後室温保存1日、滴下後室温保存4日に顕微鏡下観察した。顕微鏡観察は、通常の光学顕微鏡及び偏光顕微鏡で行った。結果を図1に示す。これより、本発明の非晶質化剤により、結晶化に差異が見られ、ポリビニルピロリドンが非晶質化剤として作用していることがわかる。このように、結晶と非晶質が混在する場合においても、本来結晶のみであるべき状態であるものが、本発明の非晶質化剤を含有することにより、非晶質が並存する(非晶質構造が現れる)場合には、本発明の非晶質化剤の効果と判断する。 <Example 1>
An ethanol solution containing 1% by mass of luliconazole and an ethanol solution containing 1% by mass of luliconazole and 0.1% by mass of polyvinylpyrrolidone were prepared and dropped on a slide glass. Thereafter, it was observed under a microscope for 1 day after storage at room temperature and 4 days after storage at room temperature. Microscopic observation was performed with a normal optical microscope and a polarizing microscope. The results are shown in FIG. From this, it can be seen that there is a difference in crystallization by the amorphizing agent of the present invention, and that polyvinylpyrrolidone acts as an amorphizing agent. Thus, even in the case where crystals and amorphous are mixed, what is originally in a state of being only crystals is amorphous by the inclusion of the amorphizing agent of the present invention (non-native). In the case where a crystalline structure appears), it is judged as an effect of the amorphizing agent of the present invention.
以下に示す処方の医薬組成物1について、次に示す手順で被膜製剤を製造した。 <Example 2>
About pharmaceutical composition 1 of the prescription shown below, the film formulation was manufactured in the procedure shown next.
医薬組成物1 1mLをチューブに取り、これに10mgのニュートラルレッドを200μLのメタノールで溶解させた液を100μL加え、良く攪拌した後、スライドグラスに滴下し、室温下、溶剤揮散、被膜形成過程を顕微鏡(400倍)で観察した。観察の経過を図2~4に示す。一様な相に、ミセル様の構造が現れはじめ(図2)、このミセル構造が増加し(図3)、連続相様の構造にミセル様の構造が一様に分散した非晶質の膜(図4)が観察された。これより、本発明の非晶質化剤である、ポリビニルピロリドンと乳酸の非晶質化効果が確かめられた。 <Film formation process of manufactured pharmaceutical composition 1>
Take 1 mL of pharmaceutical composition 1 in a tube, add 100 μL of 10 mg neutral red dissolved in 200 μL of methanol, stir well, drop it onto a slide glass, and evaporate the solvent at room temperature. It observed with the microscope (400 time). The course of observation is shown in FIGS. A micelle-like structure begins to appear in a uniform phase (FIG. 2), the micelle structure increases (FIG. 3), and an amorphous film in which the micelle-like structure is uniformly dispersed in a continuous phase-like structure (FIG. 4) was observed. This confirmed the amorphizing effect of polyvinylpyrrolidone and lactic acid, which are the amorphizing agents of the present invention.
実施例2に示す手順に従い、以下の表2に示す処方の医薬組成物2及び3(被膜製剤)を製造した。さらに、実施例2に記載する方法に従い被膜形成過程を顕微鏡(400倍)で観察した。医薬組成物1と同様に、医薬組成物2及び3には、連続相様の構造にミセル様の構造が一様に分散した非晶質の膜が観察され非晶質化効果が認められた。 <Example 3>
According to the procedure shown in Example 2,
Claims (13)
- 水溶性高分子及び酸から選ばれる1種又は2種以上からなる、以下の一般式(1)で表される化合物及び/又はその塩の非晶質化剤。
- 前記水溶性高分子は、ビニル系水溶性高分子又はセルロース系水溶性高分子である、請求項1に記載の非晶質化剤。 2. The amorphizing agent according to claim 1, wherein the water-soluble polymer is a vinyl-based water-soluble polymer or a cellulose-based water-soluble polymer.
- 前記ビニル系水溶性高分子は、ポリビニルピロリドン又はカルボキシビニルポリマーである、請求項2に記載の非晶質化剤。 3. The amorphizing agent according to claim 2, wherein the vinyl-based water-soluble polymer is polyvinylpyrrolidone or carboxyvinyl polymer.
- 前記セルロース系水溶性高分子は、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロース、ヒドロキシエチルメチルセルロース、メチルセルロース又はエチルセルロースである、請求項2に記載の非晶質化剤。 3. The amorphizing agent according to claim 2, wherein the cellulose-based water-soluble polymer is hydroxypropylcellulose, hydroxypropylmethylcellulose, hydroxyethylmethylcellulose, methylcellulose or ethylcellulose.
- 前記酸は、有機酸である、請求項1~4の何れか1項に記載の非晶質化剤。 The amorphizing agent according to any one of claims 1 to 4, wherein the acid is an organic acid.
- 水溶性高分子及び酸からなる、請求項1~5の何れか1項に記載の非晶質化剤。 The amorphizing agent according to any one of claims 1 to 5, comprising a water-soluble polymer and an acid.
- 一般式(1)で表される化合物及び/又はその塩と、該化合物及び/又はその塩の質量の0.05~10倍の質量の請求項1~7の何れか1項に記載の非晶質化剤を均一に混合し、固化させる工程を含む、一般式(1)で表される化合物及び/又はその塩の非晶質化方法。 The compound represented by the general formula (1) and / or a salt thereof and the non-reactive substance according to any one of claims 1 to 7 having a mass of 0.05 to 10 times the mass of the compound and / or the salt thereof. A method for amorphizing a compound represented by the general formula (1) and / or a salt thereof, comprising a step of uniformly mixing and solidifying a crystallization agent.
- 一般式(1)で表される化合物及び/又はその塩と、該化合物及び/又はその塩の質量の0.05~10倍の質量の請求項1~7の何れか1項に記載の非晶質化剤とを含んでなる非晶質の組成物。 The compound represented by the general formula (1) and / or a salt thereof and the non-reactive substance according to any one of claims 1 to 7 having a mass of 0.05 to 10 times the mass of the compound and / or the salt thereof. An amorphous composition comprising a crystallizing agent.
- 請求項9に記載の非晶質の組成物を中間仕掛品として、該中間仕掛品を溶解する工程を含む、
一般式(1)で表される化合物及び/又はその塩を含有する医薬組成物の製造方法。 Including the step of dissolving the intermediate work-in-process as the intermediate work-in-process using the amorphous composition according to claim 9 as an intermediate work-in-process.
A method for producing a pharmaceutical composition comprising a compound represented by the general formula (1) and / or a salt thereof. - 一般式(1)で表される化合物及び/又はその塩と、該化合物及び/又はその塩の質量の0.05~10倍の質量の請求項1~7の何れか1項に記載の非晶質化剤を含んでなる、組成物。 The compound represented by the general formula (1) and / or a salt thereof and the non-reactive substance according to any one of claims 1 to 7 having a mass of 0.05 to 10 times the mass of the compound and / or the salt thereof. A composition comprising a crystallizing agent.
- 更に、揮散すべき溶媒を含む、請求項11に記載の組成物。 Furthermore, the composition of Claim 11 containing the solvent which should be volatilized.
- 医薬である、請求項11又は12に記載の組成物。 The composition according to claim 11 or 12, which is a medicine.
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SG11201808660UA SG11201808660UA (en) | 2016-03-31 | 2017-03-28 | Amorphizing agent, amorphous composition comprising amorphizing agent and utilization thereof |
KR1020187031311A KR102359641B1 (en) | 2016-03-31 | 2017-03-28 | An amorphous agent, an amorphous composition comprising an amorphous agent, and use thereof |
AU2017244688A AU2017244688B2 (en) | 2016-03-31 | 2017-03-28 | Amorphizing agent, Amorphous composition comprising Amorphizing agent and utilization thereof |
CN201780021615.4A CN108883190B (en) | 2016-03-31 | 2017-03-28 | Amorphizing agent, amorphous composition containing amorphizing agent, and use thereof |
MYPI2018703583A MY197992A (en) | 2016-03-31 | 2017-03-28 | Amorphizing agent, amorphous composition comprising amorphizing agent and utilization thereof |
PH12018502095A PH12018502095A1 (en) | 2016-03-31 | 2018-09-28 | Amorphizing agent, amorphous composition comprising amorphizing agent and utilization thereof |
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AU2017244688A1 (en) | 2018-11-22 |
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