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Method and composition for treating rhinitis

a technology for rhinitis and composition, applied in the field of rhinitis treatment, can solve the problems of local irritation, adverse effect of local irritation on treatment efficacy, and side effects of sedation and dry mouth

Inactive Publication Date: 2007-02-01
BIOLIPOX AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The patent is about a method for treating rhinitis using a pharmaceutical composition containing liposomes. The method involves administering the composition nasally or through the eyes to provide quick relief from symptoms. The composition is made by combining a drug called cetirizine with liposomes, which are small particles made of fat. The liposomes help to reduce the irritation caused by the drug and improve its effectiveness. The method is effective in treating both allergic and non-allergic rhinitis. The patent also describes the use of liposomes to encapsulate other drugs for delivery through the nasal route."

Problems solved by technology

Sedation and dry mouth do however occur as side effects in orally treated patients.
At present, however, cetirizine dihydrochloride is not an approved medicine for local administration, although it has been administered in that manner in clinical trials.
However, the authors of this article speculated therein that local irritation had an adverse effect on treatment efficacy.
Indeed, due to the irritation of the nasal mucosa by cetirizine, it has been found to be necessary to decrease its immediate exposure in nasal administration.

Method used

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  • Method and composition for treating rhinitis
  • Method and composition for treating rhinitis
  • Method and composition for treating rhinitis

Examples

Experimental program
Comparison scheme
Effect test

example 2

[0086]

TABLE 3CompositionCetirizine dinitrate2.22 gPhospholipid (soybean; Lipoid S75; Lipoid GmbH, Germany)7.00 gCitric acid, anhydrous3.84 gSodium hydroxide, solid1.67 gAscorbic acid0.20 gEDTA sodium0.20 gHCl, 1 M and / or NaOH, 1 Mto pH 5.0Water for injectionto 200 mL

[0087] General procedure. For weights and volumes reference is made to Table 3. A buffer solution was prepared by dissolving anhydrous citric acid and solid sodium hydroxide in 160 mL water (80% of the total batch volume) in a 200 mL volumetric flask. The weighed amount of active agent was added and dissolved by stirring with a magnetic stirrer. The phospholipid was separately weighed and added to the cetirizine solution. Stirring was continued until a well dispersed suspension had been formed, the pH of which was adjusted to pH 5.0±0.1 with 1.0 M NaOH and / or 1.0 M HCl. The volume of the preparation was then brought to the final batch volume of 200 mL. The preparation was transferred to a high pressure homogeniser (Ranni...

example 3

[0088] In Table 4, a high pressure homogenation particle size reduction method, as described in Example 2, is compared with high speed homogenisation (Ultra Turrax® T25 homogeniser; Jankel & Kühnke, Germany), as described in Example

[0089] 1. The composition employed was that of Example 1. Particle size distribution was determined by dynamic light scattering (Zetasizer 4, Malvern Instruments, UK) at an angle of 90° and at room temperature, using a ZET5104 sizing cell and auto:CONTIN analysis mode.

TABLE 4Particle size reductionCetirizineZ averageTreatment(mg / mL)mean (nm)High speed homogenisation11.1282High pressure homogenisation at 500 bar11.177High pressure homogenisation at 800 bar11.150High pressure homogenisation at 500 bar0130High pressure homogenisation at 800 bar0121

[0090] The methods used for preparing these exemplary batch compositions were adapted for preparing the following additional examples.

example 4

[0091]

Cetirizine dinitrate 5.6 mgPhospholipid (soybean; Lipoid S75; Lipoid GmbH, Germany).35.0 mgDisodium phosphate dihydrate; Na2HPO4H2O10.7 mgPotassium dihydrogen phosphate; KH2PO4 5.5 mg1 M HCl and / or 1 M NaOHto pH 7.0Water for injectionto 1 mL

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Abstract

There is provided pharmaceutical compositions for the treatment of rhinitis by, for example, nasal or ocular administration comprising zwitterionic cetirizine, a polar lipid liposome and a pharmaceutical-acceptable aqueous carrier. The compositions are preferably homogeneous in their nature.

Description

FIELD OF THE INVENTION [0001] This invention relates to a method for treating rhinitis, and to a corresponding pharmaceutical composition. BACKGROUND AND PRIOR ART [0002] Allergic and non-allergic rhinitis are common disorders affecting about 30% of the population. Rhinitis has a considerable impact on quality of life. In fact, rhinitis is regarded to affect the quality of life more so than, e.g., asthma. [0003] Hay fever and perennial allergic rhinitis are characterised by sneezing, rhinorrhea, nasal congestion, pruritus, conjunctivitis and pharyngitis. In perennial rhinitis, chronic nasal obstruction is often prominent and may extend to eustachian tube obstruction. [0004] Oral or local antihistamines are first line treatments, and nasal steroids second line treatments for rhinitis. For most patients, topical corticosteroids and long acting antihistamine agents provide significant relief of symptoms. Antihistamines may also affect non-immunologically (non-IgE) mediated hypersensiti...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/495A61K9/127A61K9/00
CPCA61K9/0043A61K31/495A61K9/127A61K9/0048Y10S977/906Y10S977/907A61P11/02A61P37/00A61P37/08A61P43/00
Inventor PERESWETOFF-MORATH, LENACARLSSON, ANDERS
Owner BIOLIPOX AB
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