BG104939A - Treatment of generalized anxiety disorder with paroxetine - Google Patents

Abstract

A method of treatment of generalized anxiety disorder, which method comprises administering an effective, non-toxic amount of paroxetine or a pharmaceutically acceptable salt or solvate thereof. 4 claims

Description

TREATMENT OF COMMON FEELING OF PAROXETINE WELCOME

TECHNICAL FIELD

The present invention relates to a method of treating general anxiety and specifically the use of paroxetine for such treatment.

BACKGROUND OF THE INVENTION

Pharmaceuticals with antidepressant and anti-Parkinson properties are described in US-A-3912743 and US-A-4007196. A particularly important compound is paroxetine, the (-) trans isomer of 4- (4 '' fluorophenyl) -3- (3 ', 4'-methylenedioxyphenoxymethyl) -piperidine (see Example 2 of US-A-4007196). The hydrochloride salt of paroxetine has been approved for use in humans for the treatment of inter-aiia depression, obsessive manic disorder and panic testing.

For commercial use, paroxetine hydrochloride is supplied as crystalline hemihydrate (see EP-A-0223403 from Beecham Group). Various crystalline anhydrous forms are also known (see WO 96/24595 on SmithKline Beecham pic.).

DESCRIPTION OF THE TECHNIQUE

Surprisingly, it has now been discovered that paroxetine has a potential therapeutic benefit as a remedy for the general feeling of anxiety.

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Accordingly, the present invention provides a method of treating a general feeling of anxiety, which method involves administering an effective, non-toxic amount of paroxetine or a pharmaceutically acceptable salt or solvate thereof, to a human or animal, as appropriate.

The present invention also provides for the use of paroxetine or a pharmaceutically acceptable salt or solvate thereof in the manufacture of medicaments for use in the treatment of general anxiety.

u A preferred pharmaceutically acceptable salt of paroxetine is

And crystalline hydrochloride. Convenient methods for the preparation of paroxetine hydrochloride include those mentioned in US patents 4009196, 4721723, 4902801, 4861893 and 5039803 and PCT / GB93 / 00721. Particularly preferred is the hemihydrate prepared as in EP-A-0223403.

DETAILED DESCRIPTION OF THE INVENTION

A medicament for use in the treatment of general anxiety can be prepared by mixing paroxetine or a pharmaceutically acceptable salt or solvate thereof with a suitable carrier, ©

which may contain a diluent, binder, filler, sprayer, flavoring agent, colorant, lubricant or preservative in a conventional manner.

Preferably, the drug is in unit dosage form and in a form adapted for use in medicine or veterinary medicine. For example, such compositions may be in packaged form, accompanied by written or printed instructions for use, such as the treatment of a common sense of anxiety.

The appropriate dosage range for paroxetine or a pharmaceutically acceptable salt or solvate thereof depends on how severe the form of

Ϊ j the widespread sense of anxiety and the patient's condition.

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It will also depend, inter alia, on the relationship between absorption capacity and the frequency and route of administration.

Paroxetine or a pharmaceutically acceptable salt or solvate thereof may be prepared for administration in any known manner and examples are orally, under the tongue, rectal, superficial, parenteral, intravenous or intramuscular administration. The compositions may, if desired, be prepared to provide a slow release of paroxetine a pharmaceutically acceptable salt or solvate thereof.

The drugs may be, for example, in the form of tablets, capsules, powders, vials, powders, granules, candies, substituted powders or liquid compositions, for example, solutions or suspensions or suppositories.

Drugs, such as those suitable for oral administration, may contain conventional additives such as binders, for example syrup, acacia, gelatin, sorbitol, tragacanth or polyvinylpyrrolidone; fillers, for example lactose, sugar, corn starch, calcium phosphate, sorbitol or glycerin; tabletting lubricants, for example magnesium stearate; dispersing agents, for example starch, polyvinylpyrrolidone, sodium starch glycolate or microcrystalline cellulose; or pharmaceutically acceptable stabilizing agents, such as sodium lauryl sulfate.

Solid drugs can be obtained by conventional methods of mixing, filling, tabletting and the like. Repeated mixing operations can be used to distribute paroxetine or its salt or solvate into those drugs that include large amounts of fillers. When the medicine is in the form of a tablet, powder or powder

I candy can be used in any carrier suitable for the preparation of a solid pharmaceutical composition, for example it can be magnesium stearate, starch, glucose, lactose, sugar, rice flour and chalk.

Tablets can be coated according to well known methods in the

normal pharmaceutical practice, in particular with intestinal lining. The medicines may also be in the form of absorption capsules, for example, from gelatin containing paroxetine or a salt thereof, if desired with a carrier or other excipient.

Oral medicines, such as liquids, may be in the form of, for example, emulsions, syrups or elixirs or may be provided as dry products for mixing with water or other suitable solvent before use. Such liquid medicines may contain conventional additives such as suspending agents, for example sorbitol, glucose, methyl cellulose, gelatin, hydroxyethylcellulose, carboxymethylcellulose, aluminum stearate gel, hydrated edible fats; emulsifying agents, for example lecithin, sorbitan monooleate or acacia; aqueous and non-aqueous solvents, which include edible oils, for example almond oil, fractionated coconut oil, oily esters, such as esters of glycerol or propylene glycol, or ethyl alcohol, glycerin, water or plain saline; preservatives, for example methyl or propyl para-hydroxybenzoate or sorbitolic acid; and, if desired, conventional flavoring and coloring agents.

Paroxetine or a pharmaceutically acceptable salt or solvate thereof may also be administered by the non-oral route. In accordance with the conventional pharmaceutical method, drugs may be formulated, for example, for rectal administration, such as suppositories. They may also be formulated for injection, in aqueous or non-aqueous solution, suspension or emulsion in a pharmaceutically acceptable liquid, e.g. sterile pyrogen-free water or parenterally acceptable oil or mixture of liquids. The fluid may contain bacteriostatic agents, antioxidants or other preservatives, buffers or solutions that equate the isotonicity of the solution with blood, sealing agents, suspending agents or other pharmaceutically acceptable additives. Such forms will be presented in unit dosage form, such as ampoules or available injectable agents or in multidosage forms, as a bottle form in which a suitable dose can be withdrawn or a solid form or concentrate that can be used to prepare the composition for injection.

As noted previously, the effective dose of paroxetine or a pharmaceutically acceptable salt or solvate thereof depends on how severe the form of widespread anxiety to be treated, the patient's condition, frequency and route of administration. A single dose will typically contain from 2 to 1000 mg and preferably contain from 30 to 500 mg, especially 20, 50, 100, 150, 200, 250, 300, 350, 400, 450 or 500 mg. The composition may be administered one or more times daily, for example 2, 3 or 4 times daily and the total daily dose for an adult weighing 70 kg will normally be in the range of 100 to 3000 mg. Preferably, the unit dosage form will contain from 2 to 20 mg of paroxetine (calculated as free base) and repeatedly administered, if desired, the previous daily dose.

The present invention further provides a pharmaceutical composition for use in the treatment of a common sense of anxiety that includes an effective amount of paroxetine or a pharmaceutically acceptable salt or solvate thereof and a pharmaceutically acceptable carrier. Such compositions may be prepared in the manner described hereinbefore.

DESCRIPTION OF THE EXAMPLES

The following example shows a suitable pharmaceutical composition for use in the present invention.

An example

The following are mixed together in a conventional manner and compressed into tablets of are. 300 mg weight containing. 20 mg paroxetine (calculated as free base) ··

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Paroxetine hydrochloride hemihydrate 228.8 g Dual-base calcium phosphate dihydrate 2441.2 g Hydroxypropylmethyl cellulose 150.0 g Sodium starch glycolate 150.0 g Magnesium stearate 30.0 q Total weight of the tablet 3000.0 q

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Patent Claims

Claims (4)

Patent Claims A method of treating a general feeling of anxiety characterized by the administration of an effective, non-toxic amount of paroxetine or a pharmaceutically acceptable salt or solvate thereof to a human or animal, as appropriate. 2. Use of paroxetine or a pharmaceutically acceptable salt or solvate thereof in the manufacture of a medicament for use in the treatment of general anxiety. ί A pharmaceutical composition for use in treating a general feeling of anxiety, characterized in that it comprises an effective amount of paroxetine or a pharmaceutically acceptable salt or solvate thereof and a pharmaceutically acceptable carrier. The method according to claim 1, the use according to claim 2 or the pharmaceutical composition according to claim 3, characterized in that the pharmaceutically acceptable salt of paroxetine is hydrochloride.