US4801460A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Preparation of solid pharmaceutical forms
Assignee: BASF SE
•
Filing: 1987-04-06
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Granted: 1989-01-31
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Expires: 2007-04-06
Abstract
Abstract Process for the preparation of solid pharmaceutical forms by mixing one or more pharmaceutical active compounds with one or more fusible, pharmacologically tolerated binders and, if required, other conventional pharmaceutical auxiliaries, at from 50 DEG to 180 DEG C., and subjecting the mixture to injection molding or extrusion and shaping, wherein the fusible binder used is a NVP polymer which contains not less than 20% by weight of NVP as copolymerized units, and, where they are present, all of whose comonomers contain nitrogen and/or oxygen.
Inventors
- 👤 Hans-Helmut Goertz
- 👤 Roger G. Klimesch
- 👤 Klaus Laemmerhirt
- 👤 Siegfried Lang
- 👤 Axel Sanner
- 👤 Reinhard Spengler
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 18:10
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/2095; A61K9/2004; A61K9/2022; A61K9/2027; B; B29; B29K; B29K2105/00; B29K2105/0005; B29K2105/0035
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
138 words
A process for the preparation of a solid pharmaceutical form by mixing one or more pharmaceutical active compounds with one or more fusible pharmacologically tolerated binders and subjecting the mixture to injection molding or extrusion and shaping at from 50°to 180° C., wherein the fusible binder used is a solvent-free N-vinylpyrrolidone polymer which has a water content of not more than 3.5% by weight and contains not less than 20% by weight of N-vinylpyrrolid-2-one (as copolymerized units, all copolymerized comonomers contain) nitrogen and/or oxygen and, at least when the glass transition temperature of the mixture is above 120° C., N-vinylpyrrolidone polymer is used which is obtained by polymerization in an organic solvent or using an organic peroxide as an initiator in aqueous solution, and the mixture does not contain any thermoplastics which are sparingly soluble in gastric juice.
Claim 2
Dependent Claim
138 words
A process for the preparation of a solid pharmaceutical form by mixing one or more pharmaceutical active compounds with one or more fusible pharmacologically tolerated binders and subjecting the mixture to injection molding or extrusion and shaping at from 50°to 180° C., wherein the fusible binder used is a solvent-free N-vinylpyrrolidone polymer which has a water content of not more than 3.5% by weight and contains not less than 20% by weight of N-vinylpyrrolid-2-one (as copolymerized units, all copolymerized comonomers contain) nitrogen and/or oxygen and, at least when the glass transition temperature of the mixture is above 120° C., N-vinylpyrrolidone polymer is used which is obtained by polymerization in an organic solvent or using an organic peroxide as an initiator in aqueous solution, and the mixture does not contain any thermoplastics which are sparingly soluble in gastric juice.
Claim 3
Dependent Claim
24 words
A process as defined in claim 1, wherein the polymeric binder used contains not less than 60% by weight of N-vinylpyrrolidone as copolymerized units.
Claim 4
Dependent Claim
26 words
A process as defined in claim 1, wherein plasticizers are used in an amount of not more than 20% by weight, based on the N-vinylpyrrolidone polymer.
Claim 5
Dependent Claim
27 words
A process as defined in claim 1, wherein a polymeric binder used consists of N-vinylpyrrolidone or contains, in addition to N-vinyl-pyrrolidone, only vinyl acetate as copolymerized units.
Claim 6
Dependent Claim
70 words
A process as defined in claim 1, wherein a polymeric binder is used whose comonomers are selected from the following group: acrylic acid, meth-acrylic acid, crotonic acid, maleic acid, maleic anhydride, itaconic acid, itaconic anhydride and esters of the stated acids or half esters of the stated dicarboxylic acids with alcohols of 1 to 12 carbon atoms, and hydroxyethyl and hydroxypropyl acrylate and methacrylate, acrylamide, methacrylamide, N-vinylcaprolactam and vinyl propionate.
Claim 7
Dependent Claim
45 words
A process as defined in claim 1, wherein the active compound used is sparingly soluble in water, dissolves in the polymer melt without the addition of a solvent or water to give a molecular disperse solution, and forms a solid solution after the melt solidifies.
Claim 8
Dependent Claim
91 words
A process as defined in claim 1, wherein one or more active compounds from the following group are used: acetaminophen (paracetamol), acetohexamide, acetyldigoxin, acetylsalicylic acid, acromycin, anipamil, benzocaine, β-carotene, chloramphenicol, chlordiazepoxide, chlormadinone acetate, chlorothiazide, cinnarizine, clonazepam, codeine, dexamethasone, diazepam, dicoumarol, digitoxin, digoxin, dihydroergotamine, drotaverine, flunitrazepam, furosemide, gramicidin, griseofulvin, hexobarbital, hydrochlorothiazide, hydrocortisone, hydrofluormethiazide, indomethacin, ketoprofen, lonetil, medazepam, mefruside, methandrostenolone, methylprednisolone, methylsulfadiazine (sulfaperin), nalidixic acid, nifedipine, nitrazepam, nitrofurantoin, nystatin, estradiol, papaverine, phenacetin, phenobarbital, phenylbutazone phenytoin, prednisone, reserpine, spironolactone, streptomycin, sulfadimidine (sulfamethazine), sulfamethizole, sulfamethoxazole, sulfamethoxydiazine (sulfameter), sulfaperin, sulfathiazole, sulfisoxazole, testosterone, tolazamide, tolbutamide, trimethoprim, tyrothricin.
Claim 9
Dependent Claim
23 words
A process as defined in claim 1, wherein a N-vinylpyrrolidone polymer having a Fikentscher K value of from 10 to 50 is used.
Claim 10
Dependent Claim
23 words
A process as defined in claim 1, wherein a N-vinylpyrrolidone polymer having a Fikentscher K value of from 12 to 35 is used.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-01-31 | 1992-08-01 | 1993-01-31 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-01-31 | 1996-08-01 | 1997-01-31 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-01-31 | 2000-08-01 | 2001-01-31 | $7700.00 | Window Closed / Lapsed |