GB2392385A - Pharmaceutical preparations comprising a 5HT uptake inhibitor and a homopolymer or copolymer of N-vinyl pyrrolidone - Google Patents

Pharmaceutical preparations comprising a 5HT uptake inhibitor and a homopolymer or copolymer of N-vinyl pyrrolidone Download PDF

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Publication number
GB2392385A
GB2392385A GB0220334A GB0220334A GB2392385A GB 2392385 A GB2392385 A GB 2392385A GB 0220334 A GB0220334 A GB 0220334A GB 0220334 A GB0220334 A GB 0220334A GB 2392385 A GB2392385 A GB 2392385A
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pvp
uptake
homopolymer
uptake inhibitor
copolymer
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Rajendra Narayanrao Kankan
Dharmaraj Ramachandra Rao
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Cipla Ltd
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Cipla Ltd
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    • 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
    • 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
    • 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse

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  • Health & Medical Sciences (AREA)
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  • Veterinary Medicine (AREA)
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  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Neurosurgery (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Pharmaceutically acceptable preparations comprising one or more 5HT uptake inhibitors with an excipient matrix comprising a homopolymer or copolymer of N-vinyl pyrrolidone in which the 5HT uptake inhibitors are complexed with the homopolymer or copolymer. The 5HT uptake inhibitors are preferably in amorphous form and may be selected from citalopram, venlafaxine, desmethyl venlafaxine, sertraline, fluoxetine and their salts. The homopolymer or copolymer is preferably a polyvinylpyrrolidone or crospovidone. The preparations are suitable for the treatment of a range of diseases which are prevented, ameliorated or eliminated by the administration of a 5HT uptake inhibitor. Such diseases include depression, substance abuse and senile dementia. One or more 5HT uptake inhibitors together with a homopolymer or copolymer of N-vinyl pyrrolidone may be used in the treatment of such diseases.

Description

PHARMACEUTICAL PREPARATIONS AND COMPOSITIONS OF 5HT UPTAKE
INHIBITORS
The present invention relates to pharmaceutical preparations and compositions of SHT uptake inhibitors, especially pharmaceutical preparations and compositions containing 5HT uptake inhibitors such as sertraline, citalopram and venlafaxine.
Inhibitors of serotonin or 5-hydroxytryptamine (5HT) uptake are known to be useful in the treatment of depressive illnesses and related diseases. For example, a 5HT uptake inhibitor can be beneficial for use in the treatment of alcoholism, depression (for example adolescent depression), panic disorder, obesity, migraine, anorexia, substance abuse, anxiety, obsessive compulsive disorder, chronic pain, senile dementia, bulimia, social phobia, dysthymia and the like. Sertraline, citalopram and venlafaxine are examples of known 5HT uptake inhibitors. The preparation of sertraline is described in US4536518. The preparation of citalopram is described in US4136193. The preparation of venlafaxine is described in US4535186.
We have now developed pharmaceutical preparations containing 5HT uptake inhibitors, which are advantageous, for example in terms of providing the therapeutic agents in stable form, and exhibiting good solubility and formulation properties.
More particularly, the present invention provides pharmaceutically acceptable preparations for administering to an animal patient, including humans, suffering from, or susceptible to, a disease state prevented, ameliorated or eliminated by the administration of a 5HT uptake inhibitor, which preparation comprises an effective amount of one or more 5HT uptake inhibitors, preferably in amorphous form, together with an excipient matrix comprising at least a homopolymer or copolymer of N- vinyl pyrrolidone, wherein said homopolymer or copolymer of N-vinyl pyrrolidone is complexed with said one or more 5HT uptake inhibitors.
As used herein, the term "effective amount" means an amount of a 5HT uptake inhibitor which is capable of treating a disease state for which administration of a 5HT uptake inhibitor is indicated. The term "treatment" as used herein should be understood as encompassing preventing the onset of symptoms or complications of disease states for which administration of a 5HT uptake inhibitor is indicated, alleviating or ameliorating symptoms or complications of disease states for which administration of a 5HT uptake inhibitor is indicated or eliminating symptoms or complications of disease states for which administration of a 5HT uptake inhibitor is indicated. Disease states prevented, ameliorated or eliminated by the administration of a 5HT uptake inhibitor include, for example, alcoholism, depression (for example adolescent depression), panic disorder, obesity, migraine, anorexia, substance abuse, anxiety, obsessive compulsive disorder, chronic pain, senile dementia, bulimia, social phobia, dysthymia and the like. In particular, pharmaceutical preparations, compositions and medicaments according to the present invention are useful for treating depression.
By "pharmaceutically acceptable preparation" it is meant that the excipient matrix component or components must be compatible with a 5HT uptake inhibitor of the preparation, and not be deleterious to the recipient thereof.
The term "amorphous" as used herein denotes a physical state which is not crystalline and may be verified by x-ray diffraction and other means including but not limited to observation with a polarized light microscope and ditterential scanning calorimetry. Preferably, 5HT uptake inhibitors in amorphous form in accordance with the present invention are essentially *ee from the corresponding 5HT uptake inhibitors in crystalline form.
Among the 5HT uptake inhibitors and salts thereof, which may be used in the invention are citalopram, venlataxine, desmethyl venlafaxine, sertraline, fluoxetine and their salts.
Mixtures of one or more 5HT uptake inhibitors may be used if desired. In respect of those 5HT uptake inhibitors, which exist in various enantiomeric forms, the invention is applicable equally to racemates and to individual substantially pure enantiomers and mixtures of enantiomers. The invention is of particular interest in respect of substantially pure enantiomers. By substantially "pure enantiomers" we mean the Senantiomers and R-
enantiomers substantially *ee of the corresponding the R-enantiomers and S-enantiomers
respectively, preferably with an enantiomeric excess (e.e.) of least 90%, more preferably at least 95%.
A homopolymer of N-vinyl pyrrolidone suitable for use according to the present invention can comprise water soluble polyvinylpyrrolidones, such as PVP K-12, PVP K-15, PVP K-17, PVP K-25, PVP K-30, PVP K-60, PVP K-90 and PVP K-120. The higher the molecular weight the higher the viscosity of the solution obtained. We prefer to use any of PVP K-30, PVP K-60 or PVP K-90, which give solutions of intermediate viscosity and can be concentrated to free flowing powders on evaporation under vacuum at a temperature in the range of 40 to 50 C. Alternatively, a homopolymer of Nvinyl pyrrolidone suitable for use according to the present invention might comprise a water insoluble cross linked polyvinylpyrrolidone. A water insoluble cross linked polyvinylpyrrolidone that might be employed according to the present invention can include crospovidone.
The relative amounts of the one or more 5HT uptake inhibitors and the excipient matrix components in the preparations of the present invention can vary quite widely depending on the components of the preparations. Generally, however, the preparations will contain in the range of about 20% to 50% by weight of the one or more 5HT uptake inhibitors.
In addition to a homopolymer or copolymer of N-vinyl pyrrolidone substantially as hereinbefore described, preparations according to the present invention can include other excipient matrix components, such as hydroxypropyl-methylcellulose, polaxamer 407, polaxamer 188, copolyvidon, cyclodextrin, maize starch, lactose or the like.
The present invention enables 5HT uptake inhibitors to be prepared in a stable form, which typically exhibit greater solubility and stability than the 5HT uptake inhibitors per se. The complexes present in preparations according to the present invention are easily isolated in the form of stable white to off-white powders which exhibit excellent handling properties.
Pharmaceutical preparations according to the present invention can, for example, be easily and conveniently processed into final dosage forms (such as tablets, capsules and the like) without the need for stabilising precautions during processing.
The present invention further provides, therefore, pharmaceutically acceptable compositions for administering to an animal patient, including humans, suffering from, or susceptible to, a disease state prevented, ameliorated or eliminated by the administration of a 5HT uptake inhibitor, which composition comprises a pharmaceutical preparation substantially as hereinbefore described, together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
By "pharmaceutically acceptable composition" it is meant that the carrier, diluent or excipient must be compatible with a 5HT uptake inhibitor of the composition, and not be deleterious to the recipient thereof. Pharmaceutical compositions can be prepared by procedures known in the art. For example, a 5HT uptake inhibitor of this invention can be formulated with common carriers, diluents or excipients, and formed into tablets, capsules, and the like.
Examples of carriers, diluents or excipients that are suitable for such compositions include the following: fillers and extenders; binding agents; moisturising agents; surface active agents; and lubricants. Final pharmaceutical forms may be: pills, tablets, powders, lozenges, sachets, cachets, or sterile packaged powders, and the like, depending on the type of excipient used. The particular dosage of a 5HT uptake inhibitor required to prevent, ameliorate or eliminate a disease state treated by the administration of a 5HT uptake inhibitor as described herein in an animal patient, including humans, will depend upon the particular disease state or condition, and the symptoms, and severity thereof. Dosage, routes of administration, and frequency of dosing is best decided by an attending physician.
The present invention further provides a preparation substantially as hereinbefore described (or an effective amount of one or more 5HT uptake inhibitors, and one or more excipient matrix components substantially as hereinbefore described) for use in the manufacture of a medicament for the treatment of a disease state prevented, ameliorated or eliminated by the administration of a 5HT uptake inhibitor as described herein.
Preferred preparations and / or compositions and / or / medicaments according to the present invention may comprise any of the following complexes:
an effective amount of citalopram in amorphous form, complexed with a polyvinylpyrrolidone; an effective amount of venlafaxine in amorphous form, complexed with a polyvinylpyrrolidone; an effective amount of desmethyl venlafaxine in amorphous form, complexed with a polyvinylpyrrolidone; an effective amount of sertraline in amorphous form, complexed with a polyvinylpyrrolidone; an effective amount of fluoxetine in amorphous form, complexed with a polyvinylpyrrolidone. Preferably a polyvinylpyrrolidone present in the above mentioned complexes can be any of PVP K-30, PVP K-60 or PVP K-90 substantially as hereinbefore described.
The present invention also provides a method of treating a disease state prevented, ameliorated or eliminated by the administration of a 5HT uptake inhibitor in an animal patient in need of such treatment, which method comprises administering to the animal patient an effective amount of a 5HT uptake inhibitor preferably in amorphous form, by way of a preparation, composition or medicament substantially as hereinbefore described.
Still further provided by way of the instant invention are processes of preparing a preparation, composition or medicament as herein described.
In another aspect, the present invention, therefore, provides a process of preparing a preparation substantially as hereinbefore described, which process comprises complexing an effective amount of one or more 5HT uptake inhibitors substantially as hereinbefore described, with at least a homopolymer or copolymer of N-vinyl pyrrolidone.
Suitably, either or both of the one or more 5HT uptake inhibitors and the homopolymer or copolymer of N-vinyl pyrrolidone is or are present in solution. Preferably, the 5HT uptake inhibitors are in solution, to which the homopolymer or copolymer of N-vinyl pyrrolidone is or are added. Alternatively, the homopolymer or copolymer of N-vinyl pyrrolidone may
initially be provided in solution and the one or more 5HT uptake inhibitors are present in solid form. Suspensions can also be employed.
When the one or more 5HT uptake inhibitors is or are present in solution, we prefer to use a suitable organic solvent such as methanol, ethanol, isopropanol, acetone, ethyl acetate or any suitable solvent. When the homopolymer or copolymer of N-vinyl pyrrolidone is in solution, suitable solvents include methanol, ethanol, isopropanol or any other suitable solvent.
When a complex present in a preparation according to the present invention is formed in solution, it is advantageously recovered from the solution for storage or use in solid form.
Thus, for example, solvent can be removed from the solution such as by evaporation, to cause the complex to precipitate. Other recovery methods can also be used such as, for example, spray drying. However, care needs to be taken not to expose the complex to temperatures at which 5HT uptake inhibitors might be degraded. For evaporative techniques, we prefer to use a vacuum and to keep the temperature below about 40 C. An amorphous solid is thus formed. The present invention will now be further illustrated by the following Examples, which do not limit the scope of the invention in any way.
Example I
To a solution of citalopram (25g) in ethanol (125ml) was added polyvinyl pyrrolidone K30 (75g) slowly with stirring at room temperature to obtain a clear solution. The solution was stirred for 30 minutes and then concentrated under vacuum at a temperature below 40 C to give an amorphous solid, which was filtered off.
The amorphous character of the solid was confirmed by X-ray crystallography.
The amount of citalopram in the complex was determined by HPLC analyses.
The complex contained from 22% to 28% by weight citalopram.
Example 2
To a solution of venlafaxine (25g) in ethanol (125ml) was added polyvinyl pyrrolidone K30 (75g) slowly with stirring at room temperature to obtain a clear solution. The solution was stirred for 30 minutes and then concentrated under vacuum to a temperature below 40 C to give an amorphous solid, which was filtered off. The amorphous character of the solid was confirmed by X-ray crystallography.
The amount of venlafaxine in the complex was determined by HPLC analyses. The complex contained from 22% to 28% by weight venlafaxine.
Example 3
To a solution of sertraline (25g) in ethanol (125ml) was added polyvinyl pyrrolidone K30 (25g) slowly with stirring at room temperature to obtain a clear solution. The solution was stirred for 30 minutes and then concentrated under vacuum at a temperature below 40 C to give an amorphous solid, which was filtered off. The amorphous character of the solid was confirmed by X-ray crystallography.
The amount of sertraline in the complex was determined by HPLC analyses. The complex contained from 45% to 50% by weight sertraline.
Example 4
The formulation of solid oral can be manufactured by any granulation process known in the art. Example given hereunder is only an illustration of one of the processes.
l Ingredient Quantity/tablet (mg) Venlafaxine PVP-K30 complex 100.00 Microcrystalline cellulose 43.21 Starch 17.50 Sodium starch glycollate 7. 50 Starch 2.50 Purified water q.s.
Sodium starch glycollate 7.50 Colloidal silicon oxide 1.50 Magnesium stearate 1.00 Talc 1.00 Venlafaxine PVP-K30 complex is dry mixed with other excipients. This dry mix is granulated with purified water. The granules are then dried, sized and milled. These granules are blended with excipients and then lubricated with magnesium stearate. Lubricated granules are then compressed.

Claims (18)

1. A pharmaceutically acceptable preparation for administering to an animal patient, suffering from, or susceptible to, a disease state prevented, ameliorated or eliminated by the administration of a SHT uptake inhibitor, which preparation comprises an effective amount of one or more 5HT uptake inhibitors, together with an excipient matrix comprising at least a homopolymer or copolymer of N-vinyl pyrrolidone, wherein said homopolymer or copolymer of N-vinyl pyrrolidone is complexed with said one or more 5HT uptake inhibitors.
2. A preparation according to claim 1, wherein said 5HT uptake inhibitor or inhibitors is or are in amorphous form essentially free from the corresponding 5HT uptake inhibitor or inhibitors in crystalline form.
3. A preparation according to claim I or 2, wherein the 5HT uptake inhibitor is selected from the group consisting of citalopram, venlaf'axine, desmethyl venlafaxine, sertraline, fluoxetine and their salts.
4. A preparation according to any of claims 1 to 3, wherein the homopolyrner of N-vinyl pyrrolidone is a water soluble polyvinylpyrrolidone.
5. A preparation according to claim 4, wherein the water soluble polyvinylpyrrolidone is selected from the group consisting of PVP K-12, PVP K-15, PVP K-17, PVP K-25, PVP K-3O, PVP K-6O, PVP K-90 and PVP K-120.
6. A preparation according to claim 5, wherein the water soluble polyvinylpyrrolidone comprises any of PVP K-3O, PVP K-60 or PVP K-90.
7. A preparation according to any of claims I to 6, which comprises 20% to 50% by weight of said one or more 5HT uptake inhibitors.
8. A preparation according to any of claims 1 to 7, wherein the disease state prevented, ameliorated or eliminated by the administration of a SHT uptake inhibitor includes any of alcoholism, depression, panic disorder, obesity, migraine, anorexia, substance abuse, anxiety, obsessive compulsive disorder, chronic pain, senile dementia, bulimia, social phobia and dysthymia.
9. A pharmaceutically acceptable composition for administering to an animal patient suffering from, or susceptible to, a disease state prevented, ameliorated or eliminated by the administration of a 5HT uptake inhibitor, which composition comprises a pharmaceutical preparation according to any of claims 1 to 8, together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
10. A preparation as defined in any of claims 1 to 8, or a composition as defined in claim 9, comprising any of the following complexes: an effective amount of citalopram in amorphous form, complexed with a polyvinylpyrrolidone; an effective amount of venlafaxine in amorphous form, complexed with a polyvinylpyrrolidone; an effective amount of desmethyl venlafaxine in amorphous form, complexed with a polyvinylpyrrol id one; an effective amount of sertraline in amorphous form, complexed with a polyvinylpyrrolidone; an effective amount of fluoxetine in amorphous form, complexed with a polyvinylpyrrolidone.
11. A preparation according to any of claims 1 to 8, for use in the manufacture of a medicament for the treatment of a disease state prevented, ameliorated or eliminated by the administration of a 5HT uptake inhibitor.
12. An effective amount of one or mom 5HT uptake inhibitors, preferably in amorphous form, together with a homopolymer or copolymer of N-vinyl pyrrolidone, for use in the manufacture of a medicament for the treatment of a disease state prevented, ameliorated or eliminated by the administration of a 5HT uptake inhibitor.
13. Use according to claim 11 or 12, wherein disease states prevented, ameliorated or eliminated by the administration of a 5HT uptake inhibitor include alcoholism, depression, panic disorder, obesity, migraine, anorexia, substance abuse, anxiety, obsessive compulsive disorder, chronic pain, senile dementia, bulimia, social phobia, and dysthymia.
14. A method of treating a disease state prevented, ameliorated or eliminated by the administration of a 5HT uptake inhibitor in an animal patient in need of such treatment, which method comprises administering to the animal patient an effective amount of a 5HT uptake inhibitor preferably in amorphous form, by way of a preparation as defined in any of claims 1 to 8, or a composition as defined in claim 9.
15. A process of preparing a preparation according to any of claims 1 to 8, which process comprises complexing an effective amount of one or more 5HT uptake inhibitors, with a homopolymer or copolymer of N-vinyl pyrrolidone.
16. A process according to claim 15, where either or both of the one or more 5HT uptake inhibitors, and a homopolymer or copolymer of N-vinyl pyrrolidone, is or are present in solution
17. A process according to claim 16, wherein the 5HT uptake inhibitor or inhibitors is or are present in solution, to which a homopolymer or copolymer of N-vinyl pyrrolidone in solid form is added.
18. A preparation substantially as described in any of the Examples.
GB0220334A 2002-09-02 2002-09-02 Pharmaceutical preparations comprising a 5HT uptake inhibitor and a homopolymer or copolymer of N-vinyl pyrrolidone Withdrawn GB2392385A (en)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005079787A1 (en) * 2004-02-17 2005-09-01 Sepracor Inc. Treatment or prophylaxis of migraine or headache disorders using citalopram, escitalopram or citalopram metabolites

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