Dri-nasal sprays

a nasal spray and spray technology, applied in the field of dri, can solve the problems of difficult preservation of nasal sprays, easy contamination of products by bacteria, and uncomfortable us

Inactive Publication Date: 2004-03-25
MACKLES LEONARD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These aqueous sprays are wet, cold and drip from the nose.
They are very uncomfortable to use.
Since they are aqueous based and the nozzle is inserted in the nostril, bacterial contamination of the product easily occurs.
Nasal sprays are difficult to preserve.
The mucous layer lining the epithelium represents a barrier to drug absorption along with mucociliary clearance mechanisms of the nose leads to short residence time of aqueous systems at the site of absorption which limits the systemic availability of the drug.
Furthermore because the system is anhydrous, it will wet out and cling to the mucous membrane of the nasal passages.
In fact, the efficacy of squeeze bottle system is comparable to the more expensive pump spray delivery.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example # 1

Example #1 Nasal Decongestant 12 Hour Duration

[0024]

1 1. Oxymetazoline.HCl 0.05 2. Propylene Glycol 2.50 3. C.sub.12--C.sub.15 Alkyl Lactate 20.00 4. Dimethylcyclopentasiloxane 77.45 100.00

[0025] Components # 1 and #2 are heated to 50.degree. C. until clear and uniform then the batch is cooled the #3 is added with mixing and when clear, #4 is added and mixed. The batch may then be charged to a spray container in suitable quantities.

example # 2

Example #2 Nasal Decongestant 8 Hour Duration

[0026]

2 1. Xylometazoline.HCl 0.10 2. Propylene Glycol 2.50 3. C.sub.12--C.sub.15 Alkyl Lactate 20.00 4. Cyclopentasiloxane 77.40 100.00

[0027] This mixture is prepared in accordance with the procedures of Example #1

example # 3

Example #3 Nasal Decongestant 4 Hour Duration

[0028]

3 1. Phenylephrine.HCl 0.50 2. Propylene Glycol 5.00 3. C.sub.12--C.sub.15 Alkyl Lactate 30.00 4. Cyclopentasiloxane 64.50 100.00

[0029] This mixture is prepared in accordance with the procedures of Example #1

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Abstract

There is provided non-aqueous liquid spray compositions comprising a pharmacologically acceptable non aqueous liquid carrier in which said bioactive material is directly insoluble, a pharmacologically acceptable water insoluble ester of a water soluble acid soluble in said carrier, a pharmacologically acceptable water soluble glycol soluble in said ester and a pharmacologically acceptable water soluble bio-active material soluble in said glycol but not directly soluble in the carrier. There are also provided methods of producing and administering such compositions.

Description

[0001] This application is a continuation in part of applicants copending application Ser. No. 10 / 253,073, filed Sep. 23, 2002.[0002] Safe, non irritating, non aqueous spray compositions administrable via the nasal cavity.DISCUSSION OF THE PRIOR ART[0003] The use of nasal sprays to provide relief from the nasal stuffiness of colds and allergic rhinitis is widespread. Various sympathomimetic amines have been used to provide relief. Nasal decongestants stimulate the alpha-adrenergic receptors of the vascular smooth muscle. This constriction results in shrinkage of the engorged mucous membranes which promotes drainage; improves nasal ventilation and relieves the feeling of stuffiness.[0004] Many decongestants are commercially available and are used to give various lengths of relief from 4 hours up to 12 hours. All of these decongestants are water soluble and are delivered in aqueous spray Systems.[0005] The decongestant solutions are delivered by spray from either a flexible plastic co...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/00A61K47/10A61K47/14A61K47/24
CPCA61K9/0043A61K47/10Y10S514/958A61K47/24Y10S514/957A61K47/14
Inventor MACKLES, LEONARD
Owner MACKLES LEONARD
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