JP2014062064A - バルサルタン含有錠剤の製造方法 - Google Patents
バルサルタン含有錠剤の製造方法 Download PDFInfo
- Publication number
- JP2014062064A JP2014062064A JP2012207754A JP2012207754A JP2014062064A JP 2014062064 A JP2014062064 A JP 2014062064A JP 2012207754 A JP2012207754 A JP 2012207754A JP 2012207754 A JP2012207754 A JP 2012207754A JP 2014062064 A JP2014062064 A JP 2014062064A
- Authority
- JP
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- Prior art keywords
- granules
- valsartan
- tableting
- mixture
- tablets
- 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
- 239000004072 C09CA03 - Valsartan Substances 0.000 title claims abstract description 37
- SJSNUMAYCRRIOM-QFIPXVFZSA-N valsartan Chemical compound C1=CC(CN(C(=O)CCCC)[C@@H](C(C)C)C(O)=O)=CC=C1C1=CC=CC=C1C1=NN=N[N]1 SJSNUMAYCRRIOM-QFIPXVFZSA-N 0.000 title claims abstract description 37
- 229960004699 valsartan Drugs 0.000 title claims abstract description 37
- 238000000034 method Methods 0.000 title abstract description 15
- 239000008187 granular material Substances 0.000 claims abstract description 80
- 239000000203 mixture Substances 0.000 claims abstract description 29
- 239000000654 additive Substances 0.000 claims abstract description 22
- 238000007908 dry granulation Methods 0.000 claims abstract description 15
- 238000004519 manufacturing process Methods 0.000 claims abstract description 13
- 238000007906 compression Methods 0.000 claims description 20
- 230000006835 compression Effects 0.000 claims description 20
- 238000004513 sizing Methods 0.000 claims description 17
- 230000000996 additive effect Effects 0.000 claims description 15
- 239000000314 lubricant Substances 0.000 claims description 6
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 6
- 239000011230 binding agent Substances 0.000 claims description 4
- 239000003381 stabilizer Substances 0.000 claims description 4
- 239000007884 disintegrant Substances 0.000 claims description 3
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 abstract description 56
- 235000012239 silicon dioxide Nutrition 0.000 abstract description 32
- RMAQACBXLXPBSY-UHFFFAOYSA-N silicic acid Chemical compound O[Si](O)(O)O RMAQACBXLXPBSY-UHFFFAOYSA-N 0.000 abstract description 31
- 235000019359 magnesium stearate Nutrition 0.000 abstract description 28
- 229920002678 cellulose Polymers 0.000 abstract description 21
- 239000001913 cellulose Substances 0.000 abstract description 21
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 abstract description 12
- 238000009776 industrial production Methods 0.000 abstract description 2
- 238000003825 pressing Methods 0.000 abstract 1
- 238000007873 sieving Methods 0.000 abstract 1
- 239000000843 powder Substances 0.000 description 18
- 239000000454 talc Substances 0.000 description 14
- 229910052623 talc Inorganic materials 0.000 description 14
- 235000012222 talc Nutrition 0.000 description 14
- 238000002156 mixing Methods 0.000 description 9
- 238000010298 pulverizing process Methods 0.000 description 9
- 230000000052 comparative effect Effects 0.000 description 5
- 238000005469 granulation Methods 0.000 description 5
- 230000003179 granulation Effects 0.000 description 5
- 238000009490 roller compaction Methods 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 3
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 2
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 2
- 229930006000 Sucrose Natural products 0.000 description 2
- 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 2
- 238000007796 conventional method Methods 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 238000001035 drying Methods 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 238000004128 high performance liquid chromatography Methods 0.000 description 2
- 239000002245 particle Substances 0.000 description 2
- 239000005720 sucrose Substances 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- 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
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- YASYEJJMZJALEJ-UHFFFAOYSA-N Citric acid monohydrate Chemical compound O.OC(=O)CC(O)(C(O)=O)CC(O)=O YASYEJJMZJALEJ-UHFFFAOYSA-N 0.000 description 1
- 229920002261 Corn starch Polymers 0.000 description 1
- 229920002785 Croscarmellose sodium Polymers 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 229920000881 Modified starch Polymers 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 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 description 1
- 239000000400 angiotensin II type 1 receptor blocker Substances 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 1
- 235000013539 calcium stearate Nutrition 0.000 description 1
- 239000008116 calcium stearate Substances 0.000 description 1
- 210000000692 cap cell Anatomy 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 229940105329 carboxymethylcellulose Drugs 0.000 description 1
- 229940084030 carboxymethylcellulose calcium Drugs 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 239000008120 corn starch Substances 0.000 description 1
- 229960001681 croscarmellose sodium Drugs 0.000 description 1
- 229960000913 crospovidone Drugs 0.000 description 1
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 description 1
- 238000011049 filling Methods 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 239000011361 granulated particle Substances 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000010813 internal standard method Methods 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 238000004811 liquid chromatography Methods 0.000 description 1
- 230000014759 maintenance of location Effects 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 238000007909 melt granulation Methods 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- TZBAVQKIEKDGFH-UHFFFAOYSA-N n-[2-(diethylamino)ethyl]-1-benzothiophene-2-carboxamide;hydrochloride Chemical compound [Cl-].C1=CC=C2SC(C(=O)NCC[NH+](CC)CC)=CC2=C1 TZBAVQKIEKDGFH-UHFFFAOYSA-N 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 235000019198 oils Nutrition 0.000 description 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 229920001592 potato starch Polymers 0.000 description 1
- 229940069328 povidone Drugs 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 238000003908 quality control method Methods 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 229960004029 silicic acid Drugs 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 229940083542 sodium Drugs 0.000 description 1
- 229940045902 sodium stearyl fumarate Drugs 0.000 description 1
- 229910001220 stainless steel Inorganic materials 0.000 description 1
- 239000010935 stainless steel Substances 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 229940032147 starch Drugs 0.000 description 1
- 239000006068 taste-masking agent Substances 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2012207754A JP2014062064A (ja) | 2012-09-21 | 2012-09-21 | バルサルタン含有錠剤の製造方法 |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2012207754A JP2014062064A (ja) | 2012-09-21 | 2012-09-21 | バルサルタン含有錠剤の製造方法 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016039779A Division JP6141472B2 (ja) | 2016-03-02 | 2016-03-02 | バルサルタン含有錠剤の製造方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014062064A true JP2014062064A (ja) | 2014-04-10 |
| JP2014062064A5 JP2014062064A5 (enExample) | 2015-09-03 |
Family
ID=50617660
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012207754A Pending JP2014062064A (ja) | 2012-09-21 | 2012-09-21 | バルサルタン含有錠剤の製造方法 |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP2014062064A (enExample) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2014214125A (ja) * | 2013-04-25 | 2014-11-17 | 小林製薬株式会社 | 錠剤の製造方法 |
| JP2015209386A (ja) * | 2014-04-25 | 2015-11-24 | 沢井製薬株式会社 | バルサルタン含有錠剤及びその製造方法 |
| WO2020032159A1 (ja) * | 2018-08-10 | 2020-02-13 | 日本臓器製薬株式会社 | 粒状組成物及びその製造方法 |
| CN111343974A (zh) * | 2017-11-09 | 2020-06-26 | 日本脏器制药株式会社 | 对乙酰氨基酚制剂及其制造方法 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2000506540A (ja) * | 1996-06-27 | 2000-05-30 | ノバルティス アクチエンゲゼルシャフト | バルサルタンの固体経口剤形 |
| JP2001516365A (ja) * | 1997-11-17 | 2001-09-25 | ギスト ブロカデス ベスローテン フェンノートシャップ | クラブラネート及び１種以上の賦形剤を含む顆粒 |
-
2012
- 2012-09-21 JP JP2012207754A patent/JP2014062064A/ja active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2000506540A (ja) * | 1996-06-27 | 2000-05-30 | ノバルティス アクチエンゲゼルシャフト | バルサルタンの固体経口剤形 |
| JP2007238637A (ja) * | 1996-06-27 | 2007-09-20 | Novartis Ag | バルサルタンの固体経口剤形 |
| JP2001516365A (ja) * | 1997-11-17 | 2001-09-25 | ギスト ブロカデス ベスローテン フェンノートシャップ | クラブラネート及び１種以上の賦形剤を含む顆粒 |
Non-Patent Citations (3)
| Title |
|---|
| JPN6015032974; '乾式製粒法' 造粒便覧 , 1975, ｐ．４３６-４３９ * |
| JPN6015032976; '（ａ）重量偏差試験法' 薬剤製造法（上） ｐ．１５４-１５９, 1971 * |
| JPN6015049188; '２．７ 製錠' 製剤工学 , 1971, ｐ．２３０-２３２ * |
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2014214125A (ja) * | 2013-04-25 | 2014-11-17 | 小林製薬株式会社 | 錠剤の製造方法 |
| JP2015209386A (ja) * | 2014-04-25 | 2015-11-24 | 沢井製薬株式会社 | バルサルタン含有錠剤及びその製造方法 |
| CN111343974A (zh) * | 2017-11-09 | 2020-06-26 | 日本脏器制药株式会社 | 对乙酰氨基酚制剂及其制造方法 |
| CN111343974B (zh) * | 2017-11-09 | 2023-06-13 | 日本脏器制药株式会社 | 对乙酰氨基酚制剂及其制造方法 |
| WO2020032159A1 (ja) * | 2018-08-10 | 2020-02-13 | 日本臓器製薬株式会社 | 粒状組成物及びその製造方法 |
| JPWO2020032159A1 (ja) * | 2018-08-10 | 2021-08-10 | 日本臓器製薬株式会社 | 粒状組成物及びその製造方法 |
| JP7442193B2 (ja) | 2018-08-10 | 2024-03-04 | 日本臓器製薬株式会社 | 粒状組成物及びその製造方法 |
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