JP2017002022A - Voriconazole-containing preparation - Google Patents
Voriconazole-containing preparation Download PDFInfo
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- JP2017002022A JP2017002022A JP2015130385A JP2015130385A JP2017002022A JP 2017002022 A JP2017002022 A JP 2017002022A JP 2015130385 A JP2015130385 A JP 2015130385A JP 2015130385 A JP2015130385 A JP 2015130385A JP 2017002022 A JP2017002022 A JP 2017002022A
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- 229960004740 voriconazole Drugs 0.000 title claims abstract description 39
- BCEHBSKCWLPMDN-MGPLVRAMSA-N voriconazole Chemical compound C1([C@H](C)[C@](O)(CN2N=CN=C2)C=2C(=CC(F)=CC=2)F)=NC=NC=C1F BCEHBSKCWLPMDN-MGPLVRAMSA-N 0.000 title claims abstract description 38
- 238000002360 preparation method Methods 0.000 title claims abstract description 18
- 229920002678 cellulose Polymers 0.000 claims abstract description 16
- 239000001913 cellulose Substances 0.000 claims abstract description 16
- 239000000825 pharmaceutical preparation Substances 0.000 claims abstract description 10
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- 239000000203 mixture Substances 0.000 abstract description 9
- 239000008187 granular material Substances 0.000 abstract description 5
- 238000002156 mixing Methods 0.000 abstract description 5
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 abstract description 4
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 abstract description 4
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 abstract description 4
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- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
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- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 description 2
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- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 description 1
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
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- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- 239000001856 Ethyl cellulose Substances 0.000 description 1
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 1
- 229930091371 Fructose Natural products 0.000 description 1
- 239000005715 Fructose Substances 0.000 description 1
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 description 1
- 206010017533 Fungal infection Diseases 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 229920002907 Guar gum Polymers 0.000 description 1
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 1
- 229920001244 Poly(D,L-lactide) Polymers 0.000 description 1
- 229920002125 Sokalan® Polymers 0.000 description 1
- 229930006000 Sucrose Natural products 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
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 235000012211 aluminium silicate Nutrition 0.000 description 1
- 229960004977 anhydrous lactose Drugs 0.000 description 1
- 229920001400 block copolymer Polymers 0.000 description 1
- 229910000019 calcium carbonate Inorganic materials 0.000 description 1
- 239000001506 calcium phosphate Substances 0.000 description 1
- 229910000389 calcium phosphate Inorganic materials 0.000 description 1
- 235000011010 calcium phosphates Nutrition 0.000 description 1
- 229960001631 carbomer Drugs 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 229960000913 crospovidone Drugs 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
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- 235000019325 ethyl cellulose Nutrition 0.000 description 1
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- 239000012467 final product Substances 0.000 description 1
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- 235000011852 gelatine desserts Nutrition 0.000 description 1
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- 239000000665 guar gum Substances 0.000 description 1
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- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- 229960003943 hypromellose Drugs 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 description 1
- 229960000829 kaolin Drugs 0.000 description 1
- 229960000448 lactic acid Drugs 0.000 description 1
- 239000000832 lactitol Substances 0.000 description 1
- VQHSOMBJVWLPSR-JVCRWLNRSA-N lactitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-JVCRWLNRSA-N 0.000 description 1
- 235000010448 lactitol Nutrition 0.000 description 1
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- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 1
- WVWZXTJUCNEUAE-UHFFFAOYSA-M potassium;1,2-bis(ethenyl)benzene;2-methylprop-2-enoate Chemical compound [K+].CC(=C)C([O-])=O.C=CC1=CC=CC=C1C=C WVWZXTJUCNEUAE-UHFFFAOYSA-M 0.000 description 1
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- OGIDPMRJRNCKJF-UHFFFAOYSA-N titanium oxide Inorganic materials [Ti]=O OGIDPMRJRNCKJF-UHFFFAOYSA-N 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- -1 voriconazole compound Chemical class 0.000 description 1
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- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
本発明は、安定性の向上したボリコナゾールの製剤に関する、具体的には、結晶セルロースを含有することを特徴とするボリコナゾール製剤に関する。さらに、錠剤が小型化されたことを特徴とするボリコナゾールの錠剤に関する。 The present invention relates to a formulation of voriconazole with improved stability, specifically to a voriconazole formulation characterized by containing crystalline cellulose. Further, the present invention relates to a voriconazole tablet characterized in that the tablet is miniaturized.
本発明における有効成分であるボリコナゾールは、真菌感染症の治療に有用である医薬品であり、静脈内投与用溶液、経口懸濁液用の粉末（ひいては経口懸濁液）、および経口投与用のフィルムコート錠として入手可能である。ボリコナゾールは、欧州特許第０４４０３７２Ｂ１号明細書に開示されている。正確には、欧州特許第０４４０３７２Ｂ１号明細書の実施例７において、最終生成物であるボリコナゾールは、１２７℃の融点を示す結晶性固体として得られる。 Voriconazole, which is an active ingredient in the present invention, is a pharmaceutical useful for the treatment of fungal infection, and is a solution for intravenous administration, a powder for oral suspension (and thus an oral suspension), and a film for oral administration. Available as coated tablets. Voriconazole is disclosed in EP 0440372B1. Precisely, in Example 7 of EP 0440372B1, the final product voriconazole is obtained as a crystalline solid with a melting point of 127 ° C.
ボリコナゾールを含有する医療用製剤が既に知られている。特許５３８０５４９号（文献２）は、ボリコナゾールと「モノメトキシポリエチエングリコール−ポリ−ＤＬ−乳酸ブロック共重合体ｍＰＥＧ−ＰＤＬＬＡ」を含有する薬物製剤とすることで安定化を図った発明である。 Medical preparations containing voriconazole are already known. Japanese Patent No. 5380549 (Document 2) is an invention which is stabilized by preparing a drug preparation containing voriconazole and “monomethoxypolyethylene glycol-poly-DL-lactic acid block copolymer mPEG-PDLLA”.
しかしながら、文献２に記載されたボリコナゾール製剤、具体的には錠剤の崩壊性は十分なものとは言えない。また、ボリコナゾール製剤の崩壊性を向上させるような技術で、本発明に先行するものはない。すなわち、本出願の構成要件である、ボリコナゾール、結晶セルロースを含有する製剤、特に錠剤は従来まったく知られてはいない。 However, it cannot be said that the disintegration property of the voriconazole preparation described in Document 2, specifically, the tablet, is sufficient. In addition, there is no technology preceding the present invention that improves the disintegration property of voriconazole preparations. That is, a preparation containing voriconazole and crystalline cellulose, particularly a tablet, which is a constituent element of the present application, has not been known at all.
また、現在市販されているボリコナゾールを２００ｍｇ含有する錠剤は、長径は１５．５ｍｍ、短径は７．７ｍｍを有する大型の錠剤になっている。このような大型の錠剤は、小児や老人等にとっては嚥下が困難となる。したがって、２００ｍｇ錠剤については、より服用が容易な小型錠の開発が要望されていた。 Moreover, the tablet containing 200 mg of voriconazole currently marketed is a large tablet having a major axis of 15.5 mm and a minor axis of 7.7 mm. Such large tablets are difficult to swallow for children and the elderly. Therefore, for 200 mg tablets, there has been a demand for the development of small tablets that are easier to take.
本発明は、崩壊性が改善され、服用性が向上したボリコナゾール製剤を提供することにある。また、小型化されたボリコナゾール錠剤を提供することにある。 An object of the present invention is to provide a voriconazole preparation with improved disintegration and improved ingestion. Another object is to provide a miniaturized voriconazole tablet.
上記課題を解決するために種々検討を加えた結果、ボリコナゾール錠製剤に、結晶セルロースを含有させた錠剤が上記の課題を解決した良好な製剤を提供することを見出した。すなわち、ボリコナゾール、結晶セルロースを含有することを特徴とする製剤とすることにより、崩壊性が改善され、服用性が向上した製剤が得られること、さらに、より小型化されたボリコナゾールの錠剤が得られることを確認した。本発明はかかる知見に基づいて開発されたものである。すなわち、本発明は下記に掲げる錠剤である。
（１）結晶セルロースを含有することを特徴とするボリコナゾール含有医薬品製剤
（２）医薬品製剤が、錠剤であることを特徴とする（１）記載のボリコナゾール含有錠剤
（３）錠剤が、小型化されたことを特徴とする（２）に記載のボリコナゾール含有錠剤
（４）ボリコナゾール含有医薬品製剤が、部分α化デンプンを含有しないことを特徴とする（１）乃至（３）に記載のボリコナゾール含有製剤As a result of various studies to solve the above problems, it has been found that tablets containing crystalline cellulose in a voriconazole tablet preparation provide a good preparation in which the above problems are solved. That is, by preparing a preparation characterized by containing voriconazole and crystalline cellulose, a preparation with improved disintegration and improved ingestibility can be obtained, and a more compact voriconazole tablet can be obtained. It was confirmed. The present invention has been developed based on such knowledge. That is, this invention is the tablet hung up below.
(1) Voriconazole-containing pharmaceutical preparation characterized in that it contains crystalline cellulose (2) The pharmaceutical preparation is a tablet, and the voriconazole-containing tablet according to (1) (3) is reduced in size The voriconazole-containing tablet according to (1) to (3), wherein the voriconazole-containing tablet according to (2) is characterized in that the voriconazole-containing pharmaceutical preparation does not contain partially pregelatinized starch
本発明者らは、種々検討した結果、本発明の効果を十分に得るためには、結晶セルロースを用いた製剤、具体的には、錠剤の崩壊性が改善され、服用性が向上したとの結果が得られた。すなわち、本発明者らは、結晶セルロースを用いることにより崩壊性が改善されたことを見出した。中でも結晶セルロースを用いた錠剤が特に崩壊性に優れ、さらに、部分α化デンプンを含有しない錠剤は、特に顕著な崩壊性を示す錠剤であることを見出した。また、本発明者らは、本発明により得られるボリコナゾール錠剤が、従前のものより小型化できることを見出し、本発明を完成させた。 As a result of various studies, the present inventors have found that in order to sufficiently obtain the effects of the present invention, the preparation using crystalline cellulose, specifically, the disintegration property of the tablet has been improved and the ingestion has been improved. Results were obtained. That is, the present inventors found that disintegration was improved by using crystalline cellulose. Among these, it has been found that tablets using crystalline cellulose are particularly excellent in disintegration, and tablets that do not contain partially pregelatinized starch are tablets exhibiting particularly remarkable disintegration. In addition, the present inventors have found that voriconazole tablets obtained by the present invention can be made smaller than the conventional ones, and have completed the present invention.
ボリコナゾール化合物の配合量（ｗ／ｗ）は、特に限定されるものではないが、１〜８０％であり、好ましくは１０〜７０％、さらに好ましくは３０〜５０％の濃度である。 The blending amount (w / w) of the voriconazole compound is not particularly limited, but is 1 to 80%, preferably 10 to 70%, and more preferably 30 to 50%.
本発明に用いられる結晶セルロースは、医薬品用途に用いられるものであればいずれも用いることができる。結晶セルロースの添加量は、０．１％〜５０％、好ましくは１％〜１０％である。 Any crystalline cellulose can be used as long as it is used for pharmaceutical use. The amount of crystalline cellulose added is 0.1% to 50%, preferably 1% to 10%.
本発明の有効成分を含む錠剤の径は、５０ｍｇ錠の場合は、通常５〜９ｍｍ、好ましくは６〜７ｍｍである。２００ｍｇ錠の場合は、通常長径が１０〜１５ｍｍ、好ましくは１３．５ｍｍであり、短径は、５〜７ｍｍ、好ましくは６．５〜６．８ｍｍである。 In the case of a 50 mg tablet, the diameter of the tablet containing the active ingredient of the present invention is usually 5 to 9 mm, preferably 6 to 7 mm. In the case of a 200 mg tablet, the major axis is usually 10 to 15 mm, preferably 13.5 mm, and the minor axis is 5 to 7 mm, preferably 6.5 to 6.8 mm.
本発明の錠製剤には、上記添加剤以外に種々の崩壊剤、結合剤、希釈剤等を用いることができる。これらの崩壊剤等は、本発明の効果を損なうことの無い範囲で使用することができ、添加する量も適宜選択できる。 In the tablet preparation of the present invention, various disintegrants, binders, diluents and the like can be used in addition to the above additives. These disintegrants and the like can be used within a range that does not impair the effects of the present invention, and the amount to be added can be appropriately selected.
本発明に使用される崩壊剤としては、固形医薬組成物に一般に使用される崩壊剤が挙げられる。崩壊剤の例としては、アルギン酸、クロスカルメロースナトリウム、クロスポビドン、ポラクリリンカリウム、澱粉グリコール酸ナトリウム、及び澱粉が挙げられる。崩壊剤としては、澱粉グリコール酸ナトリウム、又は澱粉のうちの少なくとも１種が好ましい。崩壊剤は通常、組成物の約５重量％〜約１５重量％の量で存在する。 Disintegrants used in the present invention include disintegrants commonly used in solid pharmaceutical compositions. Examples of disintegrants include alginic acid, croscarmellose sodium, crospovidone, polacrilin potassium, sodium starch glycolate, and starch. As the disintegrant, sodium starch glycolate or at least one of starch is preferable. The disintegrant is usually present in an amount of about 5% to about 15% by weight of the composition.
結合剤の例としては、アルギン酸、カルボマー、カルボキシメチルセルロースナトリウム、デキストリン、エチルセルロース、ゼラチン、グルコース、グアールガム、ヒドロキシプロピルセルロース、マルトース、メチルセルロース、ポビドン、澱粉、メチルセルロース、又はポリエチレンオキシドが挙げられる。結合剤としてはヒドロキシプロピルセルロースが好ましい。結合剤は通常、組成物の約１重量％〜約５重量％の量で存在する。 Examples of binders include alginic acid, carbomer, sodium carboxymethylcellulose, dextrin, ethylcellulose, gelatin, glucose, guar gum, hydroxypropylcellulose, maltose, methylcellulose, povidone, starch, methylcellulose, or polyethylene oxide. As the binder, hydroxypropylcellulose is preferred. The binder is typically present in an amount from about 1% to about 5% by weight of the composition.
本発明に使用される希釈剤としては、固形医薬組成物に一般に使用される希釈剤が挙げられる。希釈剤の例としては、炭酸カルシウム、リン酸カルシウム（二塩基性又は三塩基性）、硫酸カルシウム、デキストレート、デキストリン、デキストロース賦形剤、フルクトース、カオリン、ラクチトール、無水ラクトース、ラクトース一水和物、マルトース、マンニトール、ソルビトール、スクロース、澱粉、予めゼラチン化された澱粉、又はタルクが挙げられる。希釈剤としては、ラクトース一水和物、澱粉、又はマンニトールのうちの少なくとも１種が好ましい。希釈剤は通常、組成物の約６０重量％〜約９５重量％の量で存在する。 Diluents used in the present invention include diluents commonly used in solid pharmaceutical compositions. Examples of diluents include calcium carbonate, calcium phosphate (dibasic or tribasic), calcium sulfate, dextrate, dextrin, dextrose excipient, fructose, kaolin, lactitol, anhydrous lactose, lactose monohydrate, maltose Mannitol, sorbitol, sucrose, starch, pregelatinized starch, or talc. As the diluent, at least one of lactose monohydrate, starch, and mannitol is preferable. The diluent is typically present in an amount of about 60% to about 95% by weight of the composition.
本発明によって、具体的には、ボリコナゾール、結晶セルロースを含有することによって、崩壊性が改善され、服用性が向上したボリコナゾール製剤を得ること、また、小型化されたボリコナゾールの錠剤を得ることができる。 According to the present invention, specifically, by containing voriconazole and crystalline cellulose, it is possible to obtain a voriconazole preparation with improved disintegration and improved ingestibility, and to obtain a miniaturized voriconazole tablet. .
以下、実施例、比較例、および試験例を示し、本発明を更に具体的に説明するが、これらは本発明を限定するものではない。 EXAMPLES Hereinafter, although an Example, a comparative example, and a test example are shown and this invention is demonstrated further more concretely, these do not limit this invention.
実施例１
（１）素錠の製造
ボリコナゾール、乳糖水和物、ポビドンをバーチカルグラニュレータで混合した。粉末混合物に精製水を添加し、混合した。得られた湿潤顆粒を乾燥した。乾燥した顆粒を３０号ふるいで篩過した。顆粒に結晶セルロース及びクロスカルメロースナトリウムを添加した。これらの成分を混合した後、ステアリン酸マグネシウムを添加し、混合した。この混合末を圧縮成形して錠剤とした。
（２）フィルムコーティング錠の製造
（１）で得た素錠を用いたコーティング錠を用いて、以下の手順でフィルムコーティング錠を製造した。フィルムコーティング液：精製水、エタノールを混合した。この混合液にヒプロメロースを添加し撹拌溶解した。その後、酸化チタンを添加し撹拌分散させ懸濁液を調整した。この液を２８０号ふるいで篩過し、フィルムコーティング液を得た。フィルムコーティング錠：素錠をハイコーター（フロイント産業製）に投入し、フィルムコーティング液を噴霧することでフィルムコーティング錠を得た。Example 1
(1) Production of uncoated tablet Voriconazole, lactose hydrate, and povidone were mixed with a vertical granulator. Purified water was added to the powder mixture and mixed. The obtained wet granules were dried. The dried granules were sieved through a No. 30 sieve. Crystalline cellulose and croscarmellose sodium were added to the granules. After mixing these ingredients, magnesium stearate was added and mixed. This mixed powder was compression-molded into tablets.
(2) Production of film-coated tablets Film-coated tablets were produced by the following procedure using the coated tablets using the uncoated tablets obtained in (1). Film coating solution: Purified water and ethanol were mixed. Hypromellose was added to this mixed solution and dissolved by stirring. Thereafter, titanium oxide was added and dispersed by stirring to prepare a suspension. This solution was passed through a No. 280 sieve to obtain a film coating solution. Film-coated tablet: An uncoated tablet was placed in a high coater (Freund Sangyo) and a film-coated tablet was obtained by spraying a film coating solution.
実施例２
実施例１同様に下記フィルムコーティング錠を得た。Example 2
The following film-coated tablets were obtained in the same manner as in Example 1.
比較例１
実施例１同様に下記処方の素錠を得た。Comparative Example 1
As in Example 1, an uncoated tablet having the following formulation was obtained.
比較例２
実施例１同様に下記処方の素錠を得た。Comparative Example 2
As in Example 1, an uncoated tablet having the following formulation was obtained.
試験例１
崩壊性試験
評価方法
上記実施例及び比較例で得られたそれぞれの素錠を、約５５℃の精製水２０ｍＬに錠剤を投入し、５分毎にスパーテルで３〜４回程度撹拌して、外観を観察した。Test example 1
Disintegration test evaluation method Each uncoated tablet obtained in the above Examples and Comparative Examples was put into 20 mL of purified water at about 55 ° C., and stirred for 3 to 4 times with a spatula every 5 minutes. Was observed.
崩壊性が改善され、服用しやすいといった特徴を有するボリコナゾール含有医薬品製剤を提供することができる。また、小型化されたボリコナゾール錠剤を提供することができる。 A voriconazole-containing pharmaceutical preparation having characteristics such as improved disintegration and easy administration can be provided. In addition, a miniaturized voriconazole tablet can be provided.
Claims (4)
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| Application Number | Priority Date | Filing Date | Title |
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| JP2015130385A JP2017002022A (en) | 2015-06-12 | 2015-06-12 | Voriconazole-containing preparation |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2015130385A JP2017002022A (en) | 2015-06-12 | 2015-06-12 | Voriconazole-containing preparation |
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| JP2017002022A true JP2017002022A (en) | 2017-01-05 |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108186581A (en) * | 2018-02-11 | 2018-06-22 | 海南锦瑞制药有限公司 | A kind of voriconazole preparation and preparation method thereof |
| CN115317460A (en) * | 2021-05-11 | 2022-11-11 | 长春海悦药业股份有限公司 | Voriconazole tablet and preparation method thereof |
| CN115518046A (en) * | 2021-06-26 | 2022-12-27 | 扬子江药业集团南京海陵药业有限公司 | Voriconazole dispersible tablet and preparation method thereof |
-
2015
- 2015-06-12 JP JP2015130385A patent/JP2017002022A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108186581A (en) * | 2018-02-11 | 2018-06-22 | 海南锦瑞制药有限公司 | A kind of voriconazole preparation and preparation method thereof |
| CN108186581B (en) * | 2018-02-11 | 2021-08-31 | 海南锦瑞制药有限公司 | Voriconazole preparation and preparation method thereof |
| CN115317460A (en) * | 2021-05-11 | 2022-11-11 | 长春海悦药业股份有限公司 | Voriconazole tablet and preparation method thereof |
| CN115317460B (en) * | 2021-05-11 | 2024-11-15 | 长春海悦药业股份有限公司 | A kind of voriconazole tablet and preparation method thereof |
| CN115518046A (en) * | 2021-06-26 | 2022-12-27 | 扬子江药业集团南京海陵药业有限公司 | Voriconazole dispersible tablet and preparation method thereof |
| CN115518046B (en) * | 2021-06-26 | 2024-02-06 | 扬子江药业集团南京海陵药业有限公司 | Voriconazole dispersible tablet and preparation method thereof |
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