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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 side effects of sedation and dry mouth, adverse effects on treatment efficacy, etc., and achieve the effect of protecting the nasal mucosa

Inactive Publication Date: 2005-11-17
BIOLIPOX AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0009] It is an object of the present invention to provide a pharmaceutical composition for nasal administration of cetirizine that protects the nasal mucosa from irritation by the active agent.
[0014] The present invention is based on the finding that the presence of liposomes in an aqueous cetirizine solution of a pH at which its zwitterionic form predominates, such as a pH from about pH 4 or pH 5 to about pH 7 and even pH 8, reduces or even eliminates irritation of the nasal mucosa or the ocular mucosa caused by the drug.
[0049] Surprisingly it was found that the presence of cetirizine in a liposome vehicle resulted in a reduction of liposome size. Smaller liposomes are generally more stable physically and, due to their higher surface / volume ratio, easier resorbed by the mucosa.

Problems solved by technology

Sedation and dry mouth do however occur as side effects in orally treated patients.
However, the authors speculate that local irritation had an adverse effect on treatment efficacy.

Method used

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

Examples

Experimental program
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Effect test

example 1

[0054]

TABLE 1Batch formula of the composition of the inventionCetirizine dinitrate*22.2gPhospholipid (from soybean**)70.0gDisodium phosphate dihydrate; Na2HPO4.2H2O21.3gPotassium dihydrogenphosphate; KH2PO411.0g1 M Hydrochloric acid and / or 1 M sodium hydroxideto pH 7.0Water for injectionto 2.0L

*White solid, crystallized from THF / acetonitrile / water 2:1:0.28. Obtained from commercially available cetirizine dihydrochloride via neutralisation of the free base with nitric acid.

**Lipoid S75, Lipoid GmbH, Germany

[0055] General procedure. For weights and volumes reference is made to Table 1. A buffer solution is prepared by dissolving the buffering agents disodium phosphate dihydrate (Na2HPO4.2H2O) and potassium dihydrogen phosphate (KH2PO4) in 1600 ml water (80% of the total batch volume) in a 2000 mL volumetric flask. The weighed amount of active agent is added to the buffer solution and dissolved by stirring with a magnetic stirrer, followed by addition of 100 ml aqueous 1 M sodium hyd...

example 2

[0058]

TABLE 3Batch formula of the composition of the inventionCetirizine dinitrate2.22mgPhospholipid (soybean; Lipoid S75;7.00mgLipoid GmbH, Germany)Citric acid, anhydrous3.84mgSodium hydroxide, solid1.67mgAscorbic acid0.20mgEDTA sodium0.20mgHCl, 1 M and / or NaOH, 1 MTo pH 5.0Water for injectionTo 200mL

[0059] General procedure. For weights and volumes reference is made to Table 3. A buffer solution is 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 is added and dissolved by stirring with a magnetic stirrer. The phospholipid is separately weighed and added to the cetirizine solution. Stirring is continued until a well dispersed suspension has been formed, the pH of which is adjusted to pH 5.0±0.1 with 1.0 M NaOH and / or 1.0 M HCl. The volume of the preparation is then brought to the final batch volume of 200 mL. The preparation is transferred to a hig...

example 3

[0062]

TABLE 5Composition of the inventionCetirizine dinitrate5.6mgPhospholipid (soybean; Lipoid S75; Lipoid GmbH,35.0mgGermany)Disodium phosphate dihydrate; Na2HPO4.2H2O10.7mgPotassium dihydrogen phosphate; KH2PO45.5mg1 M HCl and / or 1 M NaOHTo pH 7.0Water for injectionTo 1mL

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Abstract

A pharmaceutical composition for the treatment of rhinitis by nasal or ocular administration comprises zwitterionic cetirizine, polar lipid liposome, a pharmaceutical acceptable aqueous carrier and, optionally, a pharmaceutically acceptable buffer capable of providing a pH of from pH 4.0 to pH 8.0, with the proviso that, if the polar lipid comprises phospholipid, the amount of phospholipid in the composition from is from 10 mg per mL to 120 mg per mL. Also disclosed are methods for its preparation and methods for treating rhinitis by its nasal or ocular administration.

Description

FIELD OF THE INVENTION [0001] The present invention relates to a method for treating rhinitis, and to a corresponding pharmaceutical composition. BACKGROUND OF THE INVENTION [0002] Allergic and non-allergic rhinitis are common disorders affecting about 30% of the population. Rhinitis does have considerable impact on quality of life. In fact, rhinitis is regarded to affect the quality of life, even 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. Oral or local antihistamines are first line treatment, and nasal steroids second line treatment 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 h...

Claims

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Application Information

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