DK201400720A1 - Anti-Snoring Composition - Google Patents
Anti-Snoring Composition Download PDFInfo
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- DK201400720A1 DK201400720A1 DK201400720A DKPA201400720A DK201400720A1 DK 201400720 A1 DK201400720 A1 DK 201400720A1 DK 201400720 A DK201400720 A DK 201400720A DK PA201400720 A DKPA201400720 A DK PA201400720A DK 201400720 A1 DK201400720 A1 DK 201400720A1
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- Prior art keywords
- snoring
- solution
- subject
- nose
- present
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- 206010041235 Snoring Diseases 0.000 title claims abstract description 110
- 239000000203 mixture Substances 0.000 title description 30
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 38
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 31
- 235000011187 glycerol Nutrition 0.000 claims abstract description 21
- 239000000126 substance Substances 0.000 claims abstract description 20
- 208000008784 apnea Diseases 0.000 claims abstract description 19
- 210000001331 nose Anatomy 0.000 claims abstract description 19
- 239000002738 chelating agent Substances 0.000 claims abstract description 17
- 150000003839 salts Chemical class 0.000 claims abstract description 17
- 230000003196 chaotropic effect Effects 0.000 claims abstract description 16
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims abstract description 15
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims abstract description 15
- 229940068968 polysorbate 80 Drugs 0.000 claims abstract description 15
- 229920000053 polysorbate 80 Polymers 0.000 claims abstract description 15
- 239000003755 preservative agent Substances 0.000 claims abstract description 13
- 239000007922 nasal spray Substances 0.000 claims abstract description 8
- 229940097496 nasal spray Drugs 0.000 claims abstract description 8
- 238000000151 deposition Methods 0.000 claims abstract description 7
- 210000003928 nasal cavity Anatomy 0.000 claims abstract description 7
- 230000002335 preservative effect Effects 0.000 claims abstract description 7
- 210000003128 head Anatomy 0.000 claims abstract description 6
- 210000003800 pharynx Anatomy 0.000 claims abstract 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical group [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 32
- 239000011780 sodium chloride Substances 0.000 claims description 18
- 239000004302 potassium sorbate Substances 0.000 claims description 16
- 229940069338 potassium sorbate Drugs 0.000 claims description 16
- 235000010241 potassium sorbate Nutrition 0.000 claims description 16
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims description 13
- 229940037001 sodium edetate Drugs 0.000 claims description 13
- CHHHXKFHOYLYRE-UHFFFAOYSA-M 2,4-Hexadienoic acid, potassium salt (1:1), (2E,4E)- Chemical compound [K+].CC=CC=CC([O-])=O CHHHXKFHOYLYRE-UHFFFAOYSA-M 0.000 claims description 12
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims description 9
- 229920000805 Polyaspartic acid Polymers 0.000 claims description 6
- 108010064470 polyaspartate Proteins 0.000 claims description 6
- PQHYOGIRXOKOEJ-UHFFFAOYSA-N 2-(1,2-dicarboxyethylamino)butanedioic acid Chemical compound OC(=O)CC(C(O)=O)NC(C(O)=O)CC(O)=O PQHYOGIRXOKOEJ-UHFFFAOYSA-N 0.000 claims description 5
- VKZRWSNIWNFCIQ-UHFFFAOYSA-N 2-[2-(1,2-dicarboxyethylamino)ethylamino]butanedioic acid Chemical compound OC(=O)CC(C(O)=O)NCCNC(C(O)=O)CC(O)=O VKZRWSNIWNFCIQ-UHFFFAOYSA-N 0.000 claims description 3
- VCVKIIDXVWEWSZ-YFKPBYRVSA-N (2s)-2-[bis(carboxymethyl)amino]pentanedioic acid Chemical compound OC(=O)CC[C@@H](C(O)=O)N(CC(O)=O)CC(O)=O VCVKIIDXVWEWSZ-YFKPBYRVSA-N 0.000 claims description 2
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical group [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract description 34
- 235000002639 sodium chloride Nutrition 0.000 abstract 1
- 239000000243 solution Substances 0.000 description 48
- 238000000034 method Methods 0.000 description 12
- 238000011282 treatment Methods 0.000 description 11
- UEUXEKPTXMALOB-UHFFFAOYSA-J tetrasodium;2-[2-[bis(carboxylatomethyl)amino]ethyl-(carboxylatomethyl)amino]acetate Chemical compound [Na+].[Na+].[Na+].[Na+].[O-]C(=O)CN(CC([O-])=O)CCN(CC([O-])=O)CC([O-])=O UEUXEKPTXMALOB-UHFFFAOYSA-J 0.000 description 9
- 241001669679 Eleotris Species 0.000 description 6
- 150000001768 cations Chemical class 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 239000007923 nasal drop Substances 0.000 description 4
- 229940100662 nasal drops Drugs 0.000 description 4
- SNPLKNRPJHDVJA-ZETCQYMHSA-N D-panthenol Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCCO SNPLKNRPJHDVJA-ZETCQYMHSA-N 0.000 description 3
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 3
- 230000008901 benefit Effects 0.000 description 3
- 229910052739 hydrogen Inorganic materials 0.000 description 3
- 239000001257 hydrogen Substances 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- 229940101267 panthenol Drugs 0.000 description 3
- 235000020957 pantothenol Nutrition 0.000 description 3
- 239000011619 pantothenol Substances 0.000 description 3
- 229920000136 polysorbate Polymers 0.000 description 3
- 229950008882 polysorbate Drugs 0.000 description 3
- 230000001603 reducing effect Effects 0.000 description 3
- 230000029058 respiratory gaseous exchange Effects 0.000 description 3
- 239000011734 sodium Substances 0.000 description 3
- 229910052708 sodium Inorganic materials 0.000 description 3
- 238000001356 surgical procedure Methods 0.000 description 3
- BHPQYMZQTOCNFJ-UHFFFAOYSA-N Calcium cation Chemical compound [Ca+2] BHPQYMZQTOCNFJ-UHFFFAOYSA-N 0.000 description 2
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 2
- 206010044003 Tonsillar hypertrophy Diseases 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 239000000443 aerosol Substances 0.000 description 2
- 229910001424 calcium ion Inorganic materials 0.000 description 2
- 230000000052 comparative effect Effects 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 238000009499 grossing Methods 0.000 description 2
- 230000006872 improvement Effects 0.000 description 2
- 150000002500 ions Chemical class 0.000 description 2
- 239000007921 spray Substances 0.000 description 2
- 239000004094 surface-active agent Substances 0.000 description 2
- 241000282412 Homo Species 0.000 description 1
- WDJHALXBUFZDSR-UHFFFAOYSA-N acetoacetic acid Chemical compound CC(=O)CC(O)=O WDJHALXBUFZDSR-UHFFFAOYSA-N 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 238000000889 atomisation Methods 0.000 description 1
- 238000009835 boiling Methods 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000006196 drop Substances 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 229960002989 glutamic acid Drugs 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 238000011369 optimal treatment Methods 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 230000007363 regulatory process Effects 0.000 description 1
- -1 sodium chloride Chemical class 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
- 239000008174 sterile solution Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000011800 void material Substances 0.000 description 1
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- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
An anti-snoring solution comprising a physiological salt, polysorbate 80, glycerin 85% v/v, a chaotropic chelating agent, a preservative and demineralized water but not comprising ethanol; for use in treating or alleviating snoring or apnea by administering said anti-snoring substance to a human subject in need thereof; wherein when administering said anti-snoring substance, the subject´s head is generally tilted in a backwards or rearwards direction from a substantially upright position, so that the nose of the subject is in a substantially horizontal or slightly backwards tilted position relative to the ground; delivering said anti snoring solution to the throat of said subject using a nasal spray comprising a jet-stream style outlet nozzle, by inserting said nasal spray comprising said jet-stream style outlet nozzle into the subject´s nose and depositing said anti-snoring solution in said subject´s nose, nasal cavity and throat without depositing significant amounts of said anti-snoring substance in the nose or nasal cavity of said subject.
Description
TI TLE
Anti-Snoring Composition FIELD
The present invention relates to compositions which are useful as anti-snoring compositions in the treatment of s n o r i n g a n d ap n e a .
BACKGROUND
Snoring physiologically is a phenomenon that is ubiquitously observed in humans and can be characterized in a rattling noise during breathing while sleeping. In many cases, snoring is accompanied with apnea which is a potentially life threatening condition during sleep wherein the airways constrict and breathing is hindered or completely cut off. But apart from snoring being a significant impeder to healthy sleep in the affected person, it also affects the sleeping quality of partners sharing room or bed with the sleeper.
Amongst the causes of snoring obstructions of the airways plays the most significant role. When inhaling and exhaling the air is guided through complex flow paths. Unevenness in the same necessarily lead to turbulence in the airflows, creating breathing disabilities which are just slightly below the threshold of consciousness of the sleeper (but not necessarily of the bed partner) with the obstructions to the flow path and the resultant air turmoil resulting in localized negative pressures (involuntary suction) and the loud sounds known ubiquitously as snoring.
Apnea which often accompanies snoring is an aggravated condition of airflow restriction, most often caused by constricting airflow paths often due to loose or floppy skin or dry airways; or collapsing airflow paths usually from overweight portions of the sleeper's body relocating themselves during sleep to exert an upwards pressure towards the head region of the sleeper rather than downwards towards the feet as is usual during an upright waken position. Another common cause of apnea (and snoring) is enlarged tonsils, especially common to small children .
While apnea and snoring due to overweight can be cured or alleviated by reducing weight, and enlarged tonsils can be removed surgically, snoring and apnea caused by looser floppy skin or dry airways in the nasal and throat regions of a sleeper are more difficult to treat or alleviate. In special cases surgery can be applied but mostly, this option is not ubiquitously available and generally not desirable due to the inherent dangers of surgery and of surgery induced infections.
In the art, however, it is well known that some of the causes of snoring and apnea associated with e.g. loose or floppy skin or dry airways in the nasal and throat regions of a sleeper can be treated or alleviated by application of liquid compositions aimed at either tightening the skin up or aiding the body in keeping the airways moist during sleep.
Such compositions for treating or alleviating snoring or apnea e.g. by tightening up the skin or keeping the airways moist during sleep are well known in the art, and numerous methods of administration are known, encompassing e.g. nasal drops or aerosols, or orally administered liquids, sprays, or aerosols.
Some very successful compositions for treating or alleviating· snoring or apnea have been the compositions originally described in e.g. EP 0053754 A1. These compositions, which were administered to a human subject as drops of between 1 mg to 2 mg each to the subject's nostril prior to sleep, have been proven to be successful in treating or alleviating snoring or apnea in treatment ready subjects.
Recently, see e.g. WO 2012010358 and US 20110066136, improvements in the treatment efficacy of snoring or apnea have been achieved by the present inventor using an improved method of administering the compositions of EP 0053754 Ά1 to subjects in need thereof by. Using the improved method of administration, wherein a subject is treated to a composition of EP 0053754 A1 as a liquid jet administered through the nose of the subject but to the subject's throat, treatment efficacy rates as high as 75% of all subjects treated have been achieved (Post market consumer studies, two studies --- Konsumgottinnen (2012), Buzzador (2012), each comprising 1000 reporters). In a further comparative study (Sund Nu, 2012) seven dosage methods were compared, including direct spraying of the throat through the mouth, with the method of WO 2012/010358 found to be the most efficient, even (and surprisingly) although the throat of the snoring subjects were treated via the nose and into the throat.
The compositions of EP 0053754 Al, WO 2012010358 and US 20110066136 have been marketed and are sold, or have been sold, as over the counter (OTC) products without prescription under the brand name of Asonor.
The compositions as disclosed in EP 0053754 A1 comprise a number of surface active components, including polysorbate 80, glycerin (85% w/w with water) and often also panthenol for enhanced effect. These surfactants aid in smoothing the skin of the airways and nave for polysorbate and. glycerol been found indispensable for the efficacy of these compositions. Further the compositions of WO 2012010358 and US 20110066136 comprise sodium edetate in an undisclosed amount,
Polysorbate and glycerol while water soluble in general will lead to increased viscosity of aqueous solutions comprising these compounds. This leads to difficulties in administering the compositions of EP 0053754 A1 since their flow properties are not adequate to reach and distribute over the entire target region of the throat and nasal regions where it is intended that the solution shall be brought to 'work. To counter this problem, the solutions contained in the examples of EP 0053754 A1 and used in the marketed compositions further comprise ethanol for reducing the viscosity of these compositions.
However, the presence of ethanol in over-the-counter (OTC) products is in general undesired. Some customers will be reluctant to the use products comprising ethanol for reasons of general health or for religious reasons, and this will narrow the market the compositions can target. It is therefore desirable to create compositions suitable for use in treatment or alleviation of snoring and/or apnea which are void of ethanol yet retaining the high efficacy rates generally known from. EP 0053754 A1, WO 2012010358 and US 20110066136,
It has now surprisingly been observed, that it is possible to dispense the anti-snoring solution of EP 0053754 without the presence of ethanol, when following the directions of the present invention and when the compositions of the present invention are administered to a person in need of treating and alleviating snoring or apnea following the method of admd.niste.ring an antisnoring composition according to WO 2012010358 and US 20110066136. Thereby improved and optimized anti-snoring formulations are prepared which overcome some of the limitations of the prior art.
SUMMARY OF THE INVENTION
According to the present invention there is disclosed in a first aspect and a first embodiment of the present invention an anti-snoring solution comprising on 1000 g of anti-snoring solution: -- a physiological salt : 8.5 to 9.5 g; - polysorbate 80 : 1.0 to 3,0 g; -- glycerin 8 5% (v/v) with water: 2.0 to 4.0 g; - a chaotropic chelating agent : 0.3 to 0.7 g; - a preservative : 1.0 to 2,0 g; - the balance demineralized water; - with the proviso that the anti-snoring solution shall not comprise ethanol; for use in treating or alleviating snoring or apnea by administering said anti-snoring substance to a human subject in need thereof; wherein when administering said anti-snoring substance, the subject's head is generally tilted in a backwards or rearwards direction from a substantially upright position, so that the nose of the subject is in a substantially horizontal or slightly backwards tilted position relative to the ground; delivering said anti-snoring solution to the throat of said subject using a nasal spray comprising a jet-stream, style outlet nozzle, by inserting said nasal spray comprising said jet-stream style outlet nozzle into the subjects nose and depositing said anti-snoring solution in s a id subj eet' s n o s e, na s a 1 c a vi t y a nd throat w i thout. depositing significant amounts of said anti-snoring substance in the nose or nasal cavity of said subject.
In a second embodiment of said anti-snoring solution of said first aspect; said chao tropic chelating agent, is selected from the list of EDTA, iminodisuccinic acid (IDS), polyaspartic acid (PAA), ethylenediamine-N,N'- disuccinic acid (EDDS), and L-glutamic acid N,N-diacetic acid (GLDA), and pharmaceutically acceptable salts thereof, such as e.g. sodium edetate.
In a third embodiment of said anti-snoring solution of said first and second embodiments of said first aspect; there is disclosed said anti-snoring solution wherein said chaotropic chelating agent is EDTA.
In a fourth embodiment of sard anti-snoring solution of said first to third embodiments of said first aspect; there is disclosed said anti-snoring solution wherein said chaotropic chelating agent is sodium edetate present in an amount of from 0.3 to 0.7 g, preferably present in an amount of 0.5 g.
In a fifth embodiment of said anti-snoring solution of said first to fourth embodiments of said first aspect; there is disclosed said anti-snoring solution wherein said physiological salt is sodium chloride, preferably sodium chloride present in an amount sufficient to create an isotonic anti-snoring solution, most preferably sodium chloride present in an amount of 9.0 g.
In a sixth embodiment of said anti-snoring solution of said first to fifth embodiments of said first aspect; there is disclosed said anti-snoring solution wherein said preservative is benzalchonium chloride or potassium sorbate, preferably potassium sorbate, present in an amount of 1.5 g.
In a seventh embodiment of said anti-snoring solution of according to said first aspect and embodiment; there is disclosed said anti-snoring solution consisting of on 1000 g of anti-snoring solution: - Sodium chloride : 8.5 to 9.5 g -- Polysorbate 8 0 :1.0 to 3.0 g -- Glycerin 85% (v/v) with water : 2.0 to 4.0 g -- Sodium edetate : 0.3 to 0.7 g - Potassium sorbate : 1.0 to 2.0 g -- Balance demineralized water.
In an eighth embodiment of said anti-snoring solution of according to said first aspect and embodiment; there is disclosed said anti-snoring solution consisting of on 1000 g of anti-snoring solution: -- Sodium chloride : 9,0 g; - Polysorbate 80 :2.0 g; - Glycerin 85% (v/v) with water : 3,0 g; - Sodium edetate : 0.5 g; - Potassium sorbate : 1.5 g; - Demineralized water : 984.0 g.
DETAILED DESCRIPTION
According to the method of administering an anti-snoring substance to a subject in need thereof as disclosed in WO 2012/010358 the subject's head is generally tilted in a backwards or rearwards direction from a substantially upright position, so that the nose of the subject is in a substantially horizontal or slightly backwards tilted position relative to the ground. Once the head is in the tilted back position, a nasal spray comprising a jet-stream style outlet, nozzle, rather than a spray or atomization nozzle, is inserted into the subjects nose and the anti-snoring substance is delivered via the nose of the subject to the throat of the subject without depositing significantly in the nose or nasal cavity of said subject. Thereby a maximum amount of anti-snoring substance is delivered to the throat of the subject in need of treatment or alleviation from snoring or apnea, and the treatment efficacy of WO 2012010358 and US 20110066136 was found to be increased by about 50% over the treatment efficacy of EP 0053574 Al.
After delivery of an active amount of anti-snoring substance to the throat, the nasal spray is removed from the subject's nose and the subject can lie down to sleep.
When using the compositions disclosed in EP 0053754 Al, an active amount of anti-snoring composition is from about 0.5 ml to about 2 ml, with about 1 ml beinq considered optimal. Given the favorable improvement using the method of administering a substance as disclosed in WO 2012010358 and US 20110066136 over the nasal drops of EP 0053754 Al, it must be considered as reasonable that while nasal drops of about 1 ml where considered an optimal amount for nasal delivery, it cannot be considered an optimal treatment amount in general in relation to snoring and apnea. It is considered that this insufficiency of efficacy can be attributed to substantial amounts of anti-snoring substance remaining in the nose and nasal cavity of the subject treated with less than optimal amounts of anti-snoring substance reaching the throat of said subject, where the antisnoring substances of EP 0053754 Al are biologically active .
As detailed above EP 0053754 Al discloses the use of nasal drops, while WO 2012010358 and US 20110066136 discloses the use of a jet-stream type nozzle for improved administration. The advantage of using a jet-stream type nozzle has been found to lie in an increase delivery of anti-snoring substance to the throat of a patient, thereby increasing the amount of active substance available for treatment of the conditions 1 e a d i n g t o s η o r r n g ,
It has now surprisingly been discovered that, a further and unexpected benefit of administering the anti-snoring substances of EP 0053754 Al using! the method of administering an anti-snoring substance to a subject in need of treatment, or alleviation of snoring- or apnea known from WO 2012010358 and US 20110066136 is that the hitherto problematic high viscosities of the solutions of EP 0053754 Al, which without the presence of ethanol made these solutions unsuitable for use as anti-snoring solutions, do not present this problem when administering the anti-snoring solutions according the method known from WO 2012010358 and US 201100 66136 and hence it is possible to dispense with the presence of ethanol in anti-snoring solutions for use with the method of administering an anti-snoring solution according to WO 2012010358 and US 20110066136 if such anti-snoring solutions are modified according to the teaching's of the present invention.
The anti-snoring solutions disclosed in EP 0053754 A1 and hitherto used in the anti-snoring solutions for use with the method of administering such an anti-snoring solution of WO 2012010358 and US 20110066136 have the below composition according to either example 1 or example 2 of EP 0053754 A1:
Comparative :
Example 1 of EP 0053754 A1:
On 1000 ml of demineralized water:
Sodrum chloride : 8.5 to 9,5 g
Polysorbate 80 : 1.3 to 3.5 g
Glycerin : 2.0 to 4,0 g
Ethanol 90° (v/v) : 3.0 to 8.0 g
Panthenol : 1.5 to 4.0 g
Benzalchonium chloride : 0.01 to 0.15 g
Benzalchonium chloride is present in the solutions of EP 0053754 A1 as a preservative and is known to have some reducing effect on snoring and apnea due to this compound additionally being surface active. C o mp a rati ve:
Example 2 of EP 0053754 A1:
On 1000 ml of isotonic water (demineralized water and sodium chloride):
Polysorbate 80 : 2 g
Glycerin : 3 g
Ethanol 90° (v/v) : 6 g
Panthenol : 2 g
Benzalchonium chloride : 0.02g
It has now been observed, that ethanol can be substituted by a strong chelator which has the same hydrogen bond disrupting effect as ethanol. In general, the inventor considers (without being bound by this theory) that the presence of a strong chelator, such as e.g. EDTA, rather than ethanol the serves to create a chaotropic environment for glycerin and polysorbate 80, an environment which is considered necessary in order to compensate for the increased viscosity due to the strong hydrogen bonding between water and these two molecules. In this respect, the inventor considers that the mode of acting of ethanol was as a chaotropic agent (by breaking hydrogen bonds) in the anti-snoring formulations of the prior art.
It is therefore suggested that the compositions of EP 0053754 A1 can be improved by substituting ethanol by a chaotropic chelating agent selected from the list of e t hy1ene di ami ne-tetr a a ce t i c a c i d (EDTA), i mi no d i s u c c i ni c acid (IDS), polyaspartic acid (PAA), ethylenediamine-N,Ν'-disuccinic acid (EDDS), and L-glutamic acid N,N~ diacetic acid (GLDA), and pharmaceutically acceptable salts thereof. A pharmaceutically acceptable salt of EDTA could e.g. be sodium EDTA or sodium edetate.
It has therefore been observed that improved anti-snoring solutions not comprising ethanol can be formulated according- to the present invention as given below:
Example 1 of the Invention: 0 η 1 0 0 0 g of a n t i - s n o r i n g s o 1 u t i ο n : A physiological salt : 8.5 to 9.5 g
Polysorbate 80 : 1.0 to 3.0 g
Glycerin 85% (v/'v) with water : 2.0 to 4.0 g A chaotropic chelating agent : 0.3 to 0.7 g A preservative : 1.0 to 2.0 g
Balance demineralized water
It is important that the solutions of the present invention comprise physiological salt, such as sodium chloride, securing that the anti-snoring solution is isotonic. The skilled person will know how to measure salt and ionic strength and adjust an anti-snoring composition of the present invention to obtain an isotonic anti-snoring solution.
Glycerin preferably is added to the anti-snoring solution of the present invention in concentrated form (85% v/v with water) but the skilled person will know how to adjust the amount of glycerin when other concentrations of glycerin to water are used.
The chaotropic chelating agent is present in the antisnoring solutions of the present inventions in an amount based on chelator weight plus weight of dissolvable counter ions, i.e. if the chaotropic chelating agent is EDTA, then EDTA must be present as EDTA with appropriate counter ions, e.g. present as sodium edetate. The weight of the chaotropic chelating agent is then the weight of sodium edetate and not of EDTA alone.
Further, preservatives like benzalchonium chloride or potassium sorbate must be added to the composition in order to secure a sterile solution for treatment and storage. There is an advantage of using benzalchonium chloride or potassium sorbate due to their surface activity and hence these preservatives are preferred.
The anti- snoring solutions of the invention can be made in simple manner by mixing the ingredients and stirring until mixed, eventually under heating below boiling.
Example 2 of the Invention:
In an anti-snoring solution comprising EDTA according to the present invention there is disclosed for 1000 g of anti-snoring so1utiοn:
Sodium chloride : 8.5 to 9.5 g Polysorbate 80 : 1.0 to 3.0 g Glycerin 85% (v/v) with water : 2.0 to 4.0 g Sodium edetate : 0.3 to 0.7 g Potassium sorbate : 1.0 to 2.0 g
Balance demineralized water
In general, EDTA will interact well with physiological salts and preservatives not comprising divalent cations such as e.g. calcium ions. Accordingly, sodium chloride and potassium sorbate can be exchanged for other physiological salts and preservatives not comprising divalent cations.
Example 3 of the Invention:
In particular the anti-snoring solutions of the present i n ve n t i ο n c ο n t a in i n g E D TA c ompris e: 0n 10 0 0 g o f a n t i-s no r i ng s o1u ti ο n:
Sodium chloride : 9.0 g
Polysorbate 80 :2.0 g
Glycerin 85% (v/v) with water : 3.0 g
Sodium edetate : 0.5 g
Potassium sorbate : 1.5 g
Demineralized water : 984.0 g
Example 4 of the Invention:
In an anti-snoring solution comprising EDDS according to the present invention there is disclosed for 1000 g of ant i - snor ing so 1 ut,i οn :
Sodium chloride : 8.5 to 9,5 g
Polysorbate 80 : 1.0 to 3.0 g
Glycerin 85% (v/v) with water : 2.0 to 4.0 g
Sodium EDDS : 0.3 to 0,7 g
Potassium sorbate : 1.0 to 2.0 g
Balance demineralized water
In general, EDDS will interact well with physiological salts and preservatives not comprising divalent cations such as e.g. calcium ions. Accordingly, sodium chloride and potassium sorbate can be exchanged for other physiological salts and preservatives not comprising divalent cations.
Example 4 of the Invention:
In particular the anti-snoring solutions of the present invention containing EDDS comprise: 0n 10 0 0 g o f a n t i-s no r i ng so1u ti ο n:
Sodium chloride : 9.0 g
Polysorbate 80 :2.0 g
Glycerin 85% (v/v) with water : 3.0 g
Sodium EDDS : 0.5 g
Potassium sorbate : 1.5 g
Demineralized water : 984.0 g
While all of the anti-snoring solutions of the invention may comprise additional surfactants with skin smoothing effect, it is generally preferred for regulatory reasons that the anti-snoring solutions of the present, invention as detailed in the embodiments 1, 2 and 3 contain only the components specified in these embodiments, with the exception of simple analogous substituents without influence on the regulatory process, such as e.g. exchanging sodium. chloride for another equivalent physiological salt.
CLOSING COMMENTS
The term "comprising" as used in the claims does not exclude other elements or steps. The term "a" or "an" as used in the claims does not exclude a plurality. A single processor or other unit may fulfill the functions of several means recited in the claims.
Although the present invention has been described in detail for purpose of illustration, it is understood that such detail is solely for that purpose, and variations can be made therein by those skilled in the art without departing from the scope of the invention.
Claims (8)
1. An anti-snoring solution comprising on 1000 g of anti-snoring solution: -- a physiological salt : 8.5 to 9,5 g; - polysorbate 80 : 1.0 to 3.0 g; - glycerin 85% (v/v) with water: 2.0 to 4.0 g; - a chaotropic chelating agent : 0.3 to 0.7 g; -- a preservative : 1.0 to 2.0 g; - the balance demineralized water; - with the proviso that the anti-snoring solution s hall n o t c omprise e thaη o1; for use in treating or alleviating snoring or apnea by administering said anti-snoring substance to a human subject in need thereof; wherein when administering said anti-snoring substance, the subject's head is generally tilted in a backwards or rearwards direction from a substantially upright position, so that the nose of the subject is in a substantially horizontal or slightly backwards tilted position relative to the ground; delivering said anti-snoring solution to the throat of said subject, using a nasal spray comprising a jet-stream, style outlet nozzle, by inserting said nasal spray comprising said jet-stream style outlet nozzle into the subject's nose and depositing said anti-snoring solution in said subject's nose, nasal cavity and throat without depositing significant amounts of said anti-snoring substance in the nose or nasal cavity of said subject.
2. The anti-snoring solution of claim 1 wherein said chaotropic chelating agent is selected from the list of EDTA, iminodisuccinic acid (IDS), polyaspartic acid (PAA), ethylenediamine-N,N'-disuccinic acid (EDDS), and L-glutamic acid N,N-diacetic acid (GLDA), and pharmaceutically acceptable salts thereof ,
3. The anti-snoring solution of claim 1 or 2 wherein said chaotropic chelating agent is EDTA.
4. The anti-snoring solution of any of the claims 1 to 3 wherein said chaotropic chelating agent is sodium edetate present in an amount of from 0,3 to 0,7 g, preferably present in an amount, of 0.5 g.
5. The anti-snoring solution of any of the claims 1 to 4 wherein said physiological salt is sodium chloride, preferably sodium chloride present in an amount sufficient to create an isotonic anti-snoring solution, most preferably sodium chloride present in an amount of 9.0 g.
6. The anti-snoring solution of any of the claims 1 to 5 wherein said preservative is benzalchonium chloride or potassium sorbate, preferably potassium sorbate, present in an amount of 1.5 g.
7. The anti-snoring· solution of claim 1 consisting of on 1000 g of anti-snoring solution: - sodium chloride : 8.5 to 9.5 g; - polysorbate 80 :1.0 to 3.0 g; - glycerin 85% (v/v) with water: 2.0 to 4.0 g; --- sodium edetate : 0.3 to 0,7 g; - potassium sorbate : 1.0 to 2.0 g; - balance demineralized water,
8. The anti-snoring solution of claim 1 consisting of on 1000 g of anti-snoring solution: -- sodium chloride : 9.0 g; - polysorbate 80 :2.0 g; - glycerin 85% (v/v) with water : 3.0 g; -- sodium edetate : 0.5 g; - potassium sorbate : 1.5 g; - demineralized water : 984.0 g.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DK201400720A DK201400720A1 (en) | 2014-12-11 | 2014-12-11 | Anti-Snoring Composition |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DK201400720 | 2014-12-11 | ||
| DK201400720A DK201400720A1 (en) | 2014-12-11 | 2014-12-11 | Anti-Snoring Composition |
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| Publication Number | Publication Date |
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| DK201400720A1 true DK201400720A1 (en) | 2015-08-24 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK201400720A DK201400720A1 (en) | 2014-12-11 | 2014-12-11 | Anti-Snoring Composition |
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| DK (1) | DK201400720A1 (en) |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0053754A1 (en) * | 1980-12-06 | 1982-06-16 | Reichert, Dietrich, Dr. med. | Drug for antagonizing snore, and method for its application |
| EP0137302A2 (en) * | 1983-09-12 | 1985-04-17 | Anasco GmbH | Means for preventing snoring |
| US20110066136A1 (en) * | 2009-09-11 | 2011-03-17 | Tanner Medico A/S | Use of pump to deliver a solution to reduce snoring |
| CN102166225A (en) * | 2010-11-29 | 2011-08-31 | 吴克 | Snore stopping liquid and preparation process thereof |
| WO2012010358A1 (en) * | 2010-07-23 | 2012-01-26 | Tannermedico A/S | Nasal spray apparatus |
-
2014
- 2014-12-11 DK DK201400720A patent/DK201400720A1/en not_active Application Discontinuation
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0053754A1 (en) * | 1980-12-06 | 1982-06-16 | Reichert, Dietrich, Dr. med. | Drug for antagonizing snore, and method for its application |
| EP0137302A2 (en) * | 1983-09-12 | 1985-04-17 | Anasco GmbH | Means for preventing snoring |
| US20110066136A1 (en) * | 2009-09-11 | 2011-03-17 | Tanner Medico A/S | Use of pump to deliver a solution to reduce snoring |
| WO2012010358A1 (en) * | 2010-07-23 | 2012-01-26 | Tannermedico A/S | Nasal spray apparatus |
| CN102166225A (en) * | 2010-11-29 | 2011-08-31 | 吴克 | Snore stopping liquid and preparation process thereof |
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