JPS6115829A - 口腔粘膜適用徐放性ニフエジピン製剤 - Google Patents
口腔粘膜適用徐放性ニフエジピン製剤Info
- Publication number
- JPS6115829A JPS6115829A JP13623284A JP13623284A JPS6115829A JP S6115829 A JPS6115829 A JP S6115829A JP 13623284 A JP13623284 A JP 13623284A JP 13623284 A JP13623284 A JP 13623284A JP S6115829 A JPS6115829 A JP S6115829A
- Authority
- JP
- Japan
- Prior art keywords
- nifedipine
- polyvinylpyrrolidone
- layer
- solid solution
- pvp
- 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.)
- Granted
Links
- 229960001597 nifedipine Drugs 0.000 title claims abstract description 94
- HYIMSNHJOBLJNT-UHFFFAOYSA-N nifedipine Chemical compound COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1C1=CC=CC=C1[N+]([O-])=O HYIMSNHJOBLJNT-UHFFFAOYSA-N 0.000 title claims abstract description 93
- 238000013268 sustained release Methods 0.000 title claims abstract description 13
- 239000012730 sustained-release form Substances 0.000 title claims abstract description 13
- 210000002200 mouth mucosa Anatomy 0.000 title description 16
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims abstract description 69
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims abstract description 69
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims abstract description 69
- 239000006104 solid solution Substances 0.000 claims abstract description 42
- 239000000203 mixture Substances 0.000 claims abstract description 30
- 229920002125 Sokalan® Polymers 0.000 claims abstract description 17
- 239000004584 polyacrylic acid Substances 0.000 claims abstract description 17
- 150000003839 salts Chemical class 0.000 claims abstract description 14
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 8
- 238000002360 preparation method Methods 0.000 claims description 26
- 238000010828 elution Methods 0.000 claims description 9
- 239000008280 blood Substances 0.000 abstract description 17
- 210000004369 blood Anatomy 0.000 abstract description 17
- 238000004090 dissolution Methods 0.000 abstract description 8
- 238000010521 absorption reaction Methods 0.000 abstract description 6
- 230000003111 delayed effect Effects 0.000 abstract description 5
- 210000003296 saliva Anatomy 0.000 abstract description 4
- 239000003795 chemical substances by application Substances 0.000 abstract description 3
- 230000009471 action Effects 0.000 abstract description 2
- 230000001070 adhesive effect Effects 0.000 abstract description 2
- 239000007787 solid Substances 0.000 abstract description 2
- 230000002035 prolonged effect Effects 0.000 abstract 1
- 239000010410 layer Substances 0.000 description 62
- 239000003826 tablet Substances 0.000 description 35
- 230000000052 comparative effect Effects 0.000 description 28
- 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 15
- 239000000843 powder Substances 0.000 description 14
- 238000009472 formulation Methods 0.000 description 13
- 241000282472 Canis lupus familiaris Species 0.000 description 8
- 238000000034 method Methods 0.000 description 8
- 235000010355 mannitol Nutrition 0.000 description 7
- 230000035807 sensation Effects 0.000 description 7
- 235000019615 sensations Nutrition 0.000 description 7
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 6
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 6
- 206010002383 Angina Pectoris Diseases 0.000 description 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 5
- -1 alkali metal salts Chemical class 0.000 description 5
- 238000010998 test method Methods 0.000 description 5
- 229940079593 drug Drugs 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 description 3
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 3
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 239000011230 binding agent Substances 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 238000010586 diagram Methods 0.000 description 3
- 239000002552 dosage form Substances 0.000 description 3
- 230000035622 drinking Effects 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 239000000796 flavoring agent Substances 0.000 description 3
- 239000000314 lubricant Substances 0.000 description 3
- 229940041616 menthol Drugs 0.000 description 3
- 239000002356 single layer Substances 0.000 description 3
- 229940095064 tartrate Drugs 0.000 description 3
- 229920003169 water-soluble polymer Polymers 0.000 description 3
- 206010020772 Hypertension Diseases 0.000 description 2
- 229920002472 Starch Polymers 0.000 description 2
- 230000008859 change Effects 0.000 description 2
- 238000002788 crimping Methods 0.000 description 2
- 238000001035 drying Methods 0.000 description 2
- 235000019441 ethanol Nutrition 0.000 description 2
- 235000013355 food flavoring agent Nutrition 0.000 description 2
- 238000004817 gas chromatography Methods 0.000 description 2
- 239000007942 layered tablet Substances 0.000 description 2
- 230000005923 long-lasting effect Effects 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 239000000178 monomer Substances 0.000 description 2
- 238000000465 moulding Methods 0.000 description 2
- 239000000047 product Substances 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 239000008107 starch Substances 0.000 description 2
- 235000019698 starch Nutrition 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- 241000416162 Astragalus gummifer Species 0.000 description 1
- 241000207199 Citrus Species 0.000 description 1
- 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
- 239000004375 Dextrin Substances 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- HTTJABKRGRZYRN-UHFFFAOYSA-N Heparin Chemical compound OC1C(NC(=O)C)C(O)OC(COS(O)(=O)=O)C1OC1C(OS(O)(=O)=O)C(O)C(OC2C(C(OS(O)(=O)=O)C(OC3C(C(O)C(O)C(O3)C(O)=O)OS(O)(=O)=O)C(CO)O2)NS(O)(=O)=O)C(C(O)=O)O1 HTTJABKRGRZYRN-UHFFFAOYSA-N 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 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
- VCUFZILGIRCDQQ-KRWDZBQOSA-N N-[[(5S)-2-oxo-3-(2-oxo-3H-1,3-benzoxazol-6-yl)-1,3-oxazolidin-5-yl]methyl]-2-[[3-(trifluoromethoxy)phenyl]methylamino]pyrimidine-5-carboxamide Chemical group O=C1O[C@H](CN1C1=CC2=C(NC(O2)=O)C=C1)CNC(=O)C=1C=NC(=NC=1)NCC1=CC(=CC=C1)OC(F)(F)F VCUFZILGIRCDQQ-KRWDZBQOSA-N 0.000 description 1
- 229910000805 Pig iron Inorganic materials 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 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
- 229920001615 Tragacanth Polymers 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 239000000853 adhesive Substances 0.000 description 1
- 229910052783 alkali metal Inorganic materials 0.000 description 1
- 229910052784 alkaline earth metal Inorganic materials 0.000 description 1
- 229920005603 alternating copolymer Polymers 0.000 description 1
- 150000003863 ammonium salts Chemical class 0.000 description 1
- 230000003276 anti-hypertensive effect Effects 0.000 description 1
- 230000008901 benefit Effects 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
- 159000000007 calcium salts Chemical class 0.000 description 1
- 239000012159 carrier gas Substances 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 238000005119 centrifugation Methods 0.000 description 1
- 235000020971 citrus fruits Nutrition 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 229920001577 copolymer Polymers 0.000 description 1
- 238000007334 copolymerization reaction Methods 0.000 description 1
- 229920006037 cross link polymer Polymers 0.000 description 1
- 239000003431 cross linking reagent Substances 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 230000001934 delay Effects 0.000 description 1
- 239000003405 delayed action preparation Substances 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- DWNAQMUDCDVSLT-UHFFFAOYSA-N diphenyl phthalate Chemical compound C=1C=CC=C(C(=O)OC=2C=CC=CC=2)C=1C(=O)OC1=CC=CC=C1 DWNAQMUDCDVSLT-UHFFFAOYSA-N 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 238000013265 extended release Methods 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 239000013022 formulation composition Substances 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 239000007789 gas Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 238000005469 granulation Methods 0.000 description 1
- 230000003179 granulation Effects 0.000 description 1
- 229960002897 heparin Drugs 0.000 description 1
- 229920000669 heparin Polymers 0.000 description 1
- 239000008240 homogeneous mixture Substances 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- FPYJFEHAWHCUMM-UHFFFAOYSA-N maleic anhydride Chemical compound O=C1OC(=O)C=C1 FPYJFEHAWHCUMM-UHFFFAOYSA-N 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- XJRBAMWJDBPFIM-UHFFFAOYSA-N methyl vinyl ether Chemical compound COC=C XJRBAMWJDBPFIM-UHFFFAOYSA-N 0.000 description 1
- 235000013336 milk Nutrition 0.000 description 1
- 239000008267 milk Substances 0.000 description 1
- 210000004080 milk Anatomy 0.000 description 1
- 239000012046 mixed solvent Substances 0.000 description 1
- 229940079467 nifedipine 10 mg Drugs 0.000 description 1
- 235000016709 nutrition Nutrition 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
- 239000003960 organic solvent Substances 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 159000000001 potassium salts Chemical class 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 description 1
- 230000000979 retarding effect Effects 0.000 description 1
- 230000000391 smoking effect Effects 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000007901 soft capsule Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 239000010409 thin film Substances 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 229940116362 tragacanth Drugs 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
- 210000001364 upper extremity Anatomy 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
- 230000002747 voluntary effect Effects 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
Classifications
-
- 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
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/006—Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
Landscapes
- Health & Medical Sciences (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Preparation (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP13623284A JPS6115829A (ja) | 1984-06-29 | 1984-06-29 | 口腔粘膜適用徐放性ニフエジピン製剤 |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP13623284A JPS6115829A (ja) | 1984-06-29 | 1984-06-29 | 口腔粘膜適用徐放性ニフエジピン製剤 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS6115829A true JPS6115829A (ja) | 1986-01-23 |
| JPH0566366B2 JPH0566366B2 (enExample) | 1993-09-21 |
Family
ID=15170369
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP13623284A Granted JPS6115829A (ja) | 1984-06-29 | 1984-06-29 | 口腔粘膜適用徐放性ニフエジピン製剤 |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS6115829A (enExample) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS63174929A (ja) * | 1987-01-09 | 1988-07-19 | エラン コ−ポレ−シヨン ピ− エル シ− | 徐放性カプセルもしくは錠剤製剤及びその調製方法 |
| US5047244A (en) * | 1988-06-03 | 1991-09-10 | Watson Laboratories, Inc. | Mucoadhesive carrier for delivery of therapeutical agent |
| WO2004041239A1 (de) * | 2002-11-08 | 2004-05-21 | Lts Lohmann Therapie-Systeme Ag | Transmucosale pharmazeutische darreichungsform |
| US20180015643A1 (en) * | 2001-10-09 | 2018-01-18 | Arrow Greentech Limited | Method Of Manufacturing Embedded Water Soluble Film Carrier |
-
1984
- 1984-06-29 JP JP13623284A patent/JPS6115829A/ja active Granted
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS63174929A (ja) * | 1987-01-09 | 1988-07-19 | エラン コ−ポレ−シヨン ピ− エル シ− | 徐放性カプセルもしくは錠剤製剤及びその調製方法 |
| US5047244A (en) * | 1988-06-03 | 1991-09-10 | Watson Laboratories, Inc. | Mucoadhesive carrier for delivery of therapeutical agent |
| US20180015643A1 (en) * | 2001-10-09 | 2018-01-18 | Arrow Greentech Limited | Method Of Manufacturing Embedded Water Soluble Film Carrier |
| WO2004041239A1 (de) * | 2002-11-08 | 2004-05-21 | Lts Lohmann Therapie-Systeme Ag | Transmucosale pharmazeutische darreichungsform |
| AU2003274030B2 (en) * | 2002-11-08 | 2008-09-04 | Lts Lohmann Therapie-Systeme Ag | Transmucosal pharmaceutical administration form |
Also Published As
| Publication number | Publication date |
|---|---|
| JPH0566366B2 (enExample) | 1993-09-21 |
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