CA1250526A - Hot melt antihistamine formulations - Google Patents
Hot melt antihistamine formulationsInfo
- Publication number
- CA1250526A CA1250526A CA000489380A CA489380A CA1250526A CA 1250526 A CA1250526 A CA 1250526A CA 000489380 A CA000489380 A CA 000489380A CA 489380 A CA489380 A CA 489380A CA 1250526 A CA1250526 A CA 1250526A
- Authority
- CA
- Canada
- Prior art keywords
- terfenadine
- hot melt
- weight
- polyethylene glycol
- paraffin wax
- 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.)
- Expired
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 51
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 title claims abstract description 43
- 239000012943 hotmelt Substances 0.000 title claims abstract description 23
- 230000001387 anti-histamine Effects 0.000 title abstract description 4
- 239000000739 antihistaminic agent Substances 0.000 title abstract description 4
- 238000009472 formulation Methods 0.000 title description 15
- 238000011049 filling Methods 0.000 claims abstract description 12
- 229960000351 terfenadine Drugs 0.000 claims description 38
- 239000002775 capsule Substances 0.000 claims description 32
- 229920001223 polyethylene glycol Polymers 0.000 claims description 16
- 239000012188 paraffin wax Substances 0.000 claims description 14
- 239000002202 Polyethylene glycol Substances 0.000 claims description 13
- 150000003839 salts Chemical class 0.000 claims description 12
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000007788 liquid Substances 0.000 abstract description 13
- 239000007887 hard shell capsule Substances 0.000 abstract description 4
- 239000007886 soft shell capsule Substances 0.000 abstract description 4
- 238000013268 sustained release Methods 0.000 abstract description 3
- 239000012730 sustained-release form Substances 0.000 abstract description 3
- 239000000126 substance Substances 0.000 description 11
- 239000007787 solid Substances 0.000 description 8
- 239000007903 gelatin capsule Substances 0.000 description 7
- 230000002209 hydrophobic effect Effects 0.000 description 6
- 230000009974 thixotropic effect Effects 0.000 description 5
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 3
- 238000001816 cooling Methods 0.000 description 3
- 230000003247 decreasing effect Effects 0.000 description 3
- 239000012530 fluid Substances 0.000 description 3
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 description 2
- -1 ac2tic Chemical class 0.000 description 2
- 239000011230 binding agent Substances 0.000 description 2
- 230000015556 catabolic process Effects 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 238000000354 decomposition reaction Methods 0.000 description 2
- 238000006731 degradation reaction Methods 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 239000000314 lubricant Substances 0.000 description 2
- 238000010907 mechanical stirring Methods 0.000 description 2
- 238000002844 melting Methods 0.000 description 2
- 230000008018 melting Effects 0.000 description 2
- 150000007522 mineralic acids Chemical class 0.000 description 2
- 150000007524 organic acids Chemical class 0.000 description 2
- 239000006072 paste Substances 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 229920001187 thermosetting polymer Polymers 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- 125000005273 2-acetoxybenzoic acid group Chemical group 0.000 description 1
- 229910002012 Aerosil® Inorganic materials 0.000 description 1
- COVZYZSDYWQREU-UHFFFAOYSA-N Busulfan Chemical compound CS(=O)(=O)OCCCCOS(C)(=O)=O COVZYZSDYWQREU-UHFFFAOYSA-N 0.000 description 1
- 239000004705 High-molecular-weight polyethylene Substances 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000002009 allergenic effect Effects 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- 239000000043 antiallergic agent Substances 0.000 description 1
- 159000000032 aromatic acids Chemical class 0.000 description 1
- 235000013871 bee wax Nutrition 0.000 description 1
- 239000012166 beeswax Substances 0.000 description 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid group Chemical group C(C1=CC=CC=C1)(=O)O WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000007963 capsule composition Substances 0.000 description 1
- 150000001735 carboxylic acids Chemical class 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- WZHCOOQXZCIUNC-UHFFFAOYSA-N cyclandelate Chemical class C1C(C)(C)CC(C)CC1OC(=O)C(O)C1=CC=CC=C1 WZHCOOQXZCIUNC-UHFFFAOYSA-N 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 239000002270 dispersing agent Substances 0.000 description 1
- 239000000428 dust Substances 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 239000007902 hard capsule Substances 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 229960001340 histamine Drugs 0.000 description 1
- UWYVPFMHMJIBHE-OWOJBTEDSA-N hydroxymaleic acid group Chemical group O/C(/C(=O)O)=C/C(=O)O UWYVPFMHMJIBHE-OWOJBTEDSA-N 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 239000012669 liquid formulation Substances 0.000 description 1
- 230000005923 long-lasting effect Effects 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 239000000155 melt Substances 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- 230000003287 optical effect Effects 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- WLJVXDMOQOGPHL-UHFFFAOYSA-N phenylacetic acid Chemical compound OC(=O)CC1=CC=CC=C1 WLJVXDMOQOGPHL-UHFFFAOYSA-N 0.000 description 1
- 235000011007 phosphoric acid Nutrition 0.000 description 1
- 150000003016 phosphoric acids Chemical class 0.000 description 1
- 229940050929 polyethylene glycol 3350 Drugs 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 238000005086 pumping Methods 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 150000003460 sulfonic acids Chemical class 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 239000007916 tablet composition Substances 0.000 description 1
- 230000009967 tasteless effect Effects 0.000 description 1
- 238000009736 wetting 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
- A—HUMAN NECESSITIES
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
Landscapes
- Health & Medical Sciences (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)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US64617984A | 1984-08-30 | 1984-08-30 | |
| US646,179 | 1984-08-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA1250526A true CA1250526A (en) | 1989-02-28 |
Family
ID=24592083
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA000489380A Expired CA1250526A (en) | 1984-08-30 | 1985-08-26 | Hot melt antihistamine formulations |
Country Status (19)
| Country | Link |
|---|---|
| EP (1) | EP0173293B1 (en, 2012) |
| JP (1) | JPH0621068B2 (en, 2012) |
| KR (1) | KR920007832B1 (en, 2012) |
| AR (1) | AR242341A1 (en, 2012) |
| AT (1) | ATE68972T1 (en, 2012) |
| AU (1) | AU579177B2 (en, 2012) |
| CA (1) | CA1250526A (en, 2012) |
| DE (1) | DE3584557D1 (en, 2012) |
| DK (1) | DK164642C (en, 2012) |
| ES (1) | ES8608866A1 (en, 2012) |
| FI (1) | FI87992C (en, 2012) |
| GR (1) | GR852078B (en, 2012) |
| HU (1) | HU195421B (en, 2012) |
| IE (1) | IE58080B1 (en, 2012) |
| IL (1) | IL76237A (en, 2012) |
| NZ (1) | NZ213248A (en, 2012) |
| PH (1) | PH21083A (en, 2012) |
| PT (1) | PT81028B (en, 2012) |
| ZA (1) | ZA856482B (en, 2012) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8507779D0 (en) * | 1985-03-26 | 1985-05-01 | Fujisawa Pharmaceutical Co | Drug carrier |
| AR240018A1 (es) * | 1987-10-07 | 1990-01-31 | Merrell Pharma Inc | Procedimiento para preparar una composicion que comprende derivados de piperidinoalcanol. |
| ZA90341B (en) * | 1989-01-23 | 1990-10-31 | Merrell Dow Pharma | Liquid pharmaceutical composition for piperidinoalkanol derivatives |
| EP0416585B1 (en) * | 1989-09-07 | 1996-06-05 | Fuji Photo Film Co., Ltd. | Method for processing a silver halide color photographic material |
| US5270064A (en) * | 1991-04-12 | 1993-12-14 | Avian Allure | Encapsulated food product with readily removable capsule |
| US5455045A (en) * | 1993-05-13 | 1995-10-03 | Syntex (U.S.A.) Inc. | High dose formulations |
| GB2281697A (en) * | 1993-09-14 | 1995-03-15 | Euro Celtique Sa | Laxative compositions in capsules |
| NZ302926A (en) * | 1995-02-28 | 1998-10-28 | Hoechst Marion Roussel Inc | Composition for use as antihistamines comprising piperidinoalkanol derivatives and inert ingredients |
| US5574045A (en) * | 1995-06-06 | 1996-11-12 | Hoechst Marion Roussel, Inc. | Oral pharmaceutical composition of piperidinoalkanol compounds in solution form |
| IL133420A (en) * | 1997-08-26 | 2004-07-25 | Aventis Pharma Inc | Tablet-shaped pharmaceutical preparation containing a combination of piperidinoalkanol and antihistamines and reduces symptomatic congestion |
| AUPP279698A0 (en) * | 1998-04-03 | 1998-04-30 | Sunscape Developments Limited | Sustained release formulation |
| FR2838349B1 (fr) * | 2002-04-15 | 2004-06-25 | Laurence Paris | Compositions liquides pour capsules molle a liberation prolongee et leur procede de fabrication |
| EP1829541A1 (en) * | 2002-12-17 | 2007-09-05 | Abbott GmbH & Co. KG | Formulation comprising fenofibric acid or a physiologically acceptable salt thereof |
| JP2006511541A (ja) * | 2002-12-17 | 2006-04-06 | アボット ゲーエムベーハー ウント カンパニー カーゲー | フェノフィブル酸、その生理学的に許容し得る塩または誘導体を含有してなる製剤 |
| EP2042165A1 (de) * | 2007-09-28 | 2009-04-01 | Swiss Caps Rechte und Lizenzen AG | Hot-Melt-Befüllte Weichkapseln |
| FR2999937B1 (fr) * | 2012-12-21 | 2015-01-09 | Sanofi Sa | Unite solide a haute teneur en fexofenadine et son procede de preparation |
| US20170119680A1 (en) | 2015-10-30 | 2017-05-04 | R.P. Scherer Technologies, Llc | Extended release film-coated capsules |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3139383A (en) * | 1961-06-26 | 1964-06-30 | Norton Co | Encapsulated time release pellets and method for encapsulating the same |
| US3878217A (en) * | 1972-01-28 | 1975-04-15 | Richardson Merrell Inc | Alpha-aryl-4-substituted piperidinoalkanol derivatives |
| GB2118040A (en) * | 1982-02-15 | 1983-10-26 | Hoechst Uk Ltd | Oral anti-diabetic preparation |
| DE3237814A1 (de) * | 1982-10-12 | 1984-04-12 | Warner-Lambert Co., 07950 Morris Plains, N.J. | Wasserfreie emulsionen und verwendung derselben |
-
1985
- 1985-08-23 DK DK384985A patent/DK164642C/da not_active IP Right Cessation
- 1985-08-26 PT PT81028A patent/PT81028B/pt unknown
- 1985-08-26 ZA ZA856482A patent/ZA856482B/xx unknown
- 1985-08-26 CA CA000489380A patent/CA1250526A/en not_active Expired
- 1985-08-27 EP EP85110726A patent/EP0173293B1/en not_active Expired - Lifetime
- 1985-08-27 AT AT85110726T patent/ATE68972T1/de active
- 1985-08-27 DE DE8585110726T patent/DE3584557D1/de not_active Expired - Lifetime
- 1985-08-27 NZ NZ213248A patent/NZ213248A/xx unknown
- 1985-08-27 PH PH32706A patent/PH21083A/en unknown
- 1985-08-27 AU AU46692/85A patent/AU579177B2/en not_active Expired
- 1985-08-27 FI FI853275A patent/FI87992C/fi not_active IP Right Cessation
- 1985-08-28 IL IL76237A patent/IL76237A/xx not_active IP Right Cessation
- 1985-08-28 GR GR852078A patent/GR852078B/el unknown
- 1985-08-28 AR AR85301438A patent/AR242341A1/es active
- 1985-08-29 ES ES546545A patent/ES8608866A1/es not_active Expired
- 1985-08-29 JP JP60188736A patent/JPH0621068B2/ja not_active Expired - Lifetime
- 1985-08-29 HU HU853290A patent/HU195421B/hu unknown
- 1985-08-29 IE IE213485A patent/IE58080B1/en not_active IP Right Cessation
- 1985-08-30 KR KR1019850006317A patent/KR920007832B1/ko not_active Expired
Also Published As
| Publication number | Publication date |
|---|---|
| PT81028A (en) | 1985-09-01 |
| IL76237A (en) | 1989-01-31 |
| HUT38248A (en) | 1986-05-28 |
| JPH0621068B2 (ja) | 1994-03-23 |
| DE3584557D1 (de) | 1991-12-05 |
| PT81028B (pt) | 1987-09-18 |
| EP0173293B1 (en) | 1991-10-30 |
| DK384985D0 (da) | 1985-08-23 |
| GR852078B (en, 2012) | 1985-12-30 |
| NZ213248A (en) | 1988-07-28 |
| FI853275L (fi) | 1986-03-01 |
| IE58080B1 (en) | 1993-06-30 |
| IL76237A0 (en) | 1986-01-31 |
| FI853275A0 (fi) | 1985-08-27 |
| HU195421B (en) | 1988-05-30 |
| FI87992C (fi) | 1993-03-25 |
| EP0173293A3 (en) | 1987-07-01 |
| FI87992B (fi) | 1992-12-15 |
| KR870001830A (ko) | 1987-03-28 |
| EP0173293A2 (en) | 1986-03-05 |
| ZA856482B (en) | 1986-05-28 |
| AU579177B2 (en) | 1988-11-17 |
| ES546545A0 (es) | 1986-07-16 |
| IE852134L (en) | 1986-02-28 |
| KR920007832B1 (ko) | 1992-09-18 |
| AR242341A1 (es) | 1993-03-31 |
| ATE68972T1 (de) | 1991-11-15 |
| ES8608866A1 (es) | 1986-07-16 |
| AU4669285A (en) | 1986-03-06 |
| DK164642B (da) | 1992-07-27 |
| JPS6160613A (ja) | 1986-03-28 |
| DK384985A (da) | 1986-03-01 |
| DK164642C (da) | 1992-12-14 |
| PH21083A (en) | 1987-07-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MKEX | Expiry | ||
| MKEX | Expiry |
Effective date: 20060228 |