JP2001048809A - ポリグリセリンベヘニン酸エステル含有徐放性坐剤 - Google Patents
ポリグリセリンベヘニン酸エステル含有徐放性坐剤Info
- Publication number
- JP2001048809A JP2001048809A JP11226158A JP22615899A JP2001048809A JP 2001048809 A JP2001048809 A JP 2001048809A JP 11226158 A JP11226158 A JP 11226158A JP 22615899 A JP22615899 A JP 22615899A JP 2001048809 A JP2001048809 A JP 2001048809A
- Authority
- JP
- Japan
- Prior art keywords
- sustained
- suppository
- release
- behenate
- oily base
- 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
- 239000000829 suppository Substances 0.000 title claims abstract description 57
- 238000013268 sustained release Methods 0.000 title claims abstract description 40
- 239000012730 sustained-release form Substances 0.000 title claims abstract description 40
- 229940116224 behenate Drugs 0.000 title claims abstract description 24
- UKMSUNONTOPOIO-UHFFFAOYSA-M behenate Chemical compound CCCCCCCCCCCCCCCCCCCCCC([O-])=O UKMSUNONTOPOIO-UHFFFAOYSA-M 0.000 title claims abstract description 23
- 239000003814 drug Substances 0.000 claims abstract description 26
- 239000000203 mixture Substances 0.000 claims abstract description 23
- 229960005195 morphine hydrochloride Drugs 0.000 claims abstract description 22
- XELXKCKNPPSFNN-BJWPBXOKSA-N morphine hydrochloride trihydrate Chemical compound O.O.O.Cl.O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O XELXKCKNPPSFNN-BJWPBXOKSA-N 0.000 claims abstract description 22
- 239000004359 castor oil Substances 0.000 claims abstract description 17
- 235000019438 castor oil Nutrition 0.000 claims abstract description 17
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims abstract description 17
- 229960004715 morphine sulfate Drugs 0.000 claims abstract description 5
- GRVOTVYEFDAHCL-RTSZDRIGSA-N morphine sulfate pentahydrate Chemical compound O.O.O.O.O.OS(O)(=O)=O.O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O.O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O GRVOTVYEFDAHCL-RTSZDRIGSA-N 0.000 claims abstract description 5
- 238000010438 heat treatment Methods 0.000 claims abstract description 4
- 238000001816 cooling Methods 0.000 claims abstract description 3
- 229940079593 drug Drugs 0.000 claims description 21
- 238000000034 method Methods 0.000 claims description 2
- 235000014113 dietary fatty acids Nutrition 0.000 abstract description 17
- 239000000194 fatty acid Substances 0.000 abstract description 17
- 229930195729 fatty acid Natural products 0.000 abstract description 17
- -1 fatty acid ester Chemical class 0.000 abstract description 16
- 239000003795 chemical substances by application Substances 0.000 abstract 3
- 239000006185 dispersion Substances 0.000 abstract 2
- 238000013329 compounding Methods 0.000 abstract 1
- 239000000758 substrate Substances 0.000 abstract 1
- 238000009472 formulation Methods 0.000 description 15
- 238000004519 manufacturing process Methods 0.000 description 12
- 239000004615 ingredient Substances 0.000 description 11
- 239000003921 oil Substances 0.000 description 10
- 235000019198 oils Nutrition 0.000 description 10
- 230000000052 comparative effect Effects 0.000 description 9
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 6
- 150000004665 fatty acids Chemical class 0.000 description 5
- UKMSUNONTOPOIO-UHFFFAOYSA-N Behenic acid Natural products CCCCCCCCCCCCCCCCCCCCCC(O)=O UKMSUNONTOPOIO-UHFFFAOYSA-N 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 238000002360 preparation method Methods 0.000 description 4
- 239000003925 fat Substances 0.000 description 3
- 235000019197 fats Nutrition 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N glycerol group Chemical group OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- 238000002844 melting Methods 0.000 description 3
- 230000008018 melting Effects 0.000 description 3
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 3
- 229960005489 paracetamol Drugs 0.000 description 3
- 229920000223 polyglycerol Polymers 0.000 description 3
- 239000004094 surface-active agent Substances 0.000 description 3
- 235000021357 Behenic acid Nutrition 0.000 description 2
- 235000021355 Stearic acid Nutrition 0.000 description 2
- 229940116226 behenic acid Drugs 0.000 description 2
- 230000036760 body temperature Effects 0.000 description 2
- 238000010828 elution Methods 0.000 description 2
- 235000011187 glycerol Nutrition 0.000 description 2
- BQJCRHHNABKAKU-KBQPJGBKSA-N morphine Chemical compound O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O BQJCRHHNABKAKU-KBQPJGBKSA-N 0.000 description 2
- 239000004084 narcotic analgesic agent Substances 0.000 description 2
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 2
- 239000008117 stearic acid Substances 0.000 description 2
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 2
- DKSZLDSPXIWGFO-BLOJGBSASA-N (4r,4ar,7s,7ar,12bs)-9-methoxy-3-methyl-2,4,4a,7,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-7-ol;phosphoric acid;hydrate Chemical compound O.OP(O)(O)=O.OP(O)(O)=O.C([C@H]1[C@H](N(CC[C@@]112)C)C3)=C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC.C([C@H]1[C@H](N(CC[C@@]112)C)C3)=C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC DKSZLDSPXIWGFO-BLOJGBSASA-N 0.000 description 1
- LDVVTQMJQSCDMK-UHFFFAOYSA-N 1,3-dihydroxypropan-2-yl formate Chemical compound OCC(CO)OC=O LDVVTQMJQSCDMK-UHFFFAOYSA-N 0.000 description 1
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 description 1
- XADCESSVHJOZHK-UHFFFAOYSA-N Meperidine Chemical compound C=1C=CC=CC=1C1(C(=O)OCC)CCN(C)CC1 XADCESSVHJOZHK-UHFFFAOYSA-N 0.000 description 1
- 229940124532 absorption promoter Drugs 0.000 description 1
- 229940036429 acetaminophen 60 mg Drugs 0.000 description 1
- 230000000954 anitussive effect Effects 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 239000000730 antalgic agent Substances 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 239000003434 antitussive agent Substances 0.000 description 1
- 229940124584 antitussives Drugs 0.000 description 1
- 235000013871 bee wax Nutrition 0.000 description 1
- 239000012166 beeswax Substances 0.000 description 1
- 229960001889 buprenorphine hydrochloride Drugs 0.000 description 1
- UAIXRPCCYXNJMQ-RZIPZOSSSA-N buprenorphine hydrochlorie Chemical compound [Cl-].C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]11CC[C@]3([C@H](C1)[C@](C)(O)C(C)(C)C)OC)C[NH+]2CC1CC1 UAIXRPCCYXNJMQ-RZIPZOSSSA-N 0.000 description 1
- 239000004203 carnauba wax Substances 0.000 description 1
- 235000013869 carnauba wax Nutrition 0.000 description 1
- 229940110456 cocoa butter Drugs 0.000 description 1
- 235000019868 cocoa butter Nutrition 0.000 description 1
- 239000003240 coconut oil Substances 0.000 description 1
- 235000019864 coconut oil Nutrition 0.000 description 1
- 229960004415 codeine phosphate Drugs 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 238000013270 controlled release Methods 0.000 description 1
- 239000002285 corn oil Substances 0.000 description 1
- 235000005687 corn oil Nutrition 0.000 description 1
- 235000012343 cottonseed oil Nutrition 0.000 description 1
- 239000002385 cottonseed oil Substances 0.000 description 1
- 238000000354 decomposition reaction Methods 0.000 description 1
- 229960001193 diclofenac sodium Drugs 0.000 description 1
- 230000037213 diet Effects 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 229960000920 dihydrocodeine Drugs 0.000 description 1
- RBOXVHNMENFORY-DNJOTXNNSA-N dihydrocodeine Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC RBOXVHNMENFORY-DNJOTXNNSA-N 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 229940057995 liquid paraffin Drugs 0.000 description 1
- 230000004807 localization Effects 0.000 description 1
- 239000002075 main ingredient Substances 0.000 description 1
- 150000002711 medium chain fatty acid esters Chemical class 0.000 description 1
- FBBDOOHMGLLEGJ-UHFFFAOYSA-N methane;hydrochloride Chemical compound C.Cl FBBDOOHMGLLEGJ-UHFFFAOYSA-N 0.000 description 1
- 239000004200 microcrystalline wax Substances 0.000 description 1
- 235000019808 microcrystalline wax Nutrition 0.000 description 1
- 229960005181 morphine Drugs 0.000 description 1
- 229960005250 naloxone hydrochloride Drugs 0.000 description 1
- RGPDIGOSVORSAK-STHHAXOLSA-N naloxone hydrochloride Chemical compound Cl.O=C([C@@H]1O2)CC[C@@]3(O)[C@H]4CC5=CC=C(O)C2=C5[C@@]13CCN4CC=C RGPDIGOSVORSAK-STHHAXOLSA-N 0.000 description 1
- 239000004081 narcotic agent Substances 0.000 description 1
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 description 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 description 1
- VOKSWYLNZZRQPF-GDIGMMSISA-N pentazocine Chemical compound C1C2=CC=C(O)C=C2[C@@]2(C)[C@@H](C)[C@@H]1N(CC=C(C)C)CC2 VOKSWYLNZZRQPF-GDIGMMSISA-N 0.000 description 1
- 229960005301 pentazocine Drugs 0.000 description 1
- 229960000482 pethidine Drugs 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
- 239000003223 protective agent Substances 0.000 description 1
- JGMJQSFLQWGYMQ-UHFFFAOYSA-M sodium;2,6-dichloro-n-phenylaniline;acetate Chemical compound [Na+].CC([O-])=O.ClC1=CC=CC(Cl)=C1NC1=CC=CC=C1 JGMJQSFLQWGYMQ-UHFFFAOYSA-M 0.000 description 1
- 239000003549 soybean oil Substances 0.000 description 1
- 235000012424 soybean oil Nutrition 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 229940099259 vaseline Drugs 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP11226158A JP2001048809A (ja) | 1999-08-10 | 1999-08-10 | ポリグリセリンベヘニン酸エステル含有徐放性坐剤 |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP11226158A JP2001048809A (ja) | 1999-08-10 | 1999-08-10 | ポリグリセリンベヘニン酸エステル含有徐放性坐剤 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2001048809A true JP2001048809A (ja) | 2001-02-20 |
| JP2001048809A5 JP2001048809A5 (enExample) | 2006-08-24 |
Family
ID=16840781
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP11226158A Pending JP2001048809A (ja) | 1999-08-10 | 1999-08-10 | ポリグリセリンベヘニン酸エステル含有徐放性坐剤 |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP2001048809A (enExample) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005314241A (ja) * | 2004-04-27 | 2005-11-10 | Tendou Seiyaku Kk | ヒビ・ワレの発生が抑制された坐剤基剤及びその製造方法 |
| CN102670593A (zh) * | 2011-03-10 | 2012-09-19 | 丽珠集团丽珠制药厂 | 一种吲哚美辛沙丁胺醇栓剂、其制备方法、检测方法和应用 |
| JP2022500367A (ja) * | 2018-09-07 | 2022-01-04 | アール．ピー．シェーラー テクノロジーズ，エルエルシー | 硬化および低ｈｌｂ界面活性剤の添加による固体または半固体脂質ベースの剤形の安定化 |
| US12324857B2 (en) | 2018-11-29 | 2025-06-10 | R.P. Scherer Technologies, Llc | Apparatus and process for secondary encapsulation of solid inclusions using the rotary die process |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH05132416A (ja) * | 1991-04-19 | 1993-05-28 | Takeda Chem Ind Ltd | 消化管粘膜付着性マトリツクス、製剤およびコーテイング剤 |
| JPH06298667A (ja) * | 1993-04-13 | 1994-10-25 | Dainippon Pharmaceut Co Ltd | 徐放性坐剤 |
| JPH07126189A (ja) * | 1993-09-09 | 1995-05-16 | Takeda Chem Ind Ltd | 抗潰瘍併用療法用製剤 |
| JPH07316052A (ja) * | 1993-08-31 | 1995-12-05 | Takeda Chem Ind Ltd | 直腸内投与組成物 |
| JPH10324643A (ja) * | 1997-03-25 | 1998-12-08 | Takeda Chem Ind Ltd | 消化管粘膜付着性抗ヘリコバクター・ピロリ組成物 |
-
1999
- 1999-08-10 JP JP11226158A patent/JP2001048809A/ja active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH05132416A (ja) * | 1991-04-19 | 1993-05-28 | Takeda Chem Ind Ltd | 消化管粘膜付着性マトリツクス、製剤およびコーテイング剤 |
| JPH06298667A (ja) * | 1993-04-13 | 1994-10-25 | Dainippon Pharmaceut Co Ltd | 徐放性坐剤 |
| JPH07316052A (ja) * | 1993-08-31 | 1995-12-05 | Takeda Chem Ind Ltd | 直腸内投与組成物 |
| JPH07126189A (ja) * | 1993-09-09 | 1995-05-16 | Takeda Chem Ind Ltd | 抗潰瘍併用療法用製剤 |
| JPH10324643A (ja) * | 1997-03-25 | 1998-12-08 | Takeda Chem Ind Ltd | 消化管粘膜付着性抗ヘリコバクター・ピロリ組成物 |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005314241A (ja) * | 2004-04-27 | 2005-11-10 | Tendou Seiyaku Kk | ヒビ・ワレの発生が抑制された坐剤基剤及びその製造方法 |
| CN102670593A (zh) * | 2011-03-10 | 2012-09-19 | 丽珠集团丽珠制药厂 | 一种吲哚美辛沙丁胺醇栓剂、其制备方法、检测方法和应用 |
| JP2022500367A (ja) * | 2018-09-07 | 2022-01-04 | アール．ピー．シェーラー テクノロジーズ，エルエルシー | 硬化および低ｈｌｂ界面活性剤の添加による固体または半固体脂質ベースの剤形の安定化 |
| JP7556847B2 (ja) | 2018-09-07 | 2024-09-26 | アール．ピー．シェーラー テクノロジーズ，エルエルシー | 硬化および低ｈｌｂ界面活性剤の添加による固体または半固体脂質ベースの剤形の安定化 |
| US12324857B2 (en) | 2018-11-29 | 2025-06-10 | R.P. Scherer Technologies, Llc | Apparatus and process for secondary encapsulation of solid inclusions using the rotary die process |
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