CN105307649A - Composition for binding aldehydes in the mouth - Google Patents
Composition for binding aldehydes in the mouth Download PDFInfo
- Publication number
- CN105307649A CN105307649A CN201480007086.9A CN201480007086A CN105307649A CN 105307649 A CN105307649 A CN 105307649A CN 201480007086 A CN201480007086 A CN 201480007086A CN 105307649 A CN105307649 A CN 105307649A
- Authority
- CN
- China
- Prior art keywords
- compositions
- xylitol
- weight
- compositions according
- aldehyde
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
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- 150000001299 aldehydes Chemical class 0.000 title claims description 48
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- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims abstract description 44
- 235000010447 xylitol Nutrition 0.000 claims abstract description 44
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- FPIPGXGPPPQFEQ-OVSJKPMPSA-N all-trans-retinol Chemical compound OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-OVSJKPMPSA-N 0.000 description 1
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- AGVAZMGAQJOSFJ-WZHZPDAFSA-M cobalt(2+);[(2r,3s,4r,5s)-5-(5,6-dimethylbenzimidazol-1-yl)-4-hydroxy-2-(hydroxymethyl)oxolan-3-yl] [(2r)-1-[3-[(1r,2r,3r,4z,7s,9z,12s,13s,14z,17s,18s,19r)-2,13,18-tris(2-amino-2-oxoethyl)-7,12,17-tris(3-amino-3-oxopropyl)-3,5,8,8,13,15,18,19-octamethyl-2 Chemical compound [Co+2].N#[C-].[N-]([C@@H]1[C@H](CC(N)=O)[C@@]2(C)CCC(=O)NC[C@@H](C)OP(O)(=O)O[C@H]3[C@H]([C@H](O[C@@H]3CO)N3C4=CC(C)=C(C)C=C4N=C3)O)\C2=C(C)/C([C@H](C\2(C)C)CCC(N)=O)=N/C/2=C\C([C@H]([C@@]/2(CC(N)=O)C)CCC(N)=O)=N\C\2=C(C)/C2=N[C@]1(C)[C@@](C)(CC(N)=O)[C@@H]2CCC(N)=O AGVAZMGAQJOSFJ-WZHZPDAFSA-M 0.000 description 1
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- WPBNNNQJVZRUHP-UHFFFAOYSA-L manganese(2+);methyl n-[[2-(methoxycarbonylcarbamothioylamino)phenyl]carbamothioyl]carbamate;n-[2-(sulfidocarbothioylamino)ethyl]carbamodithioate Chemical compound [Mn+2].[S-]C(=S)NCCNC([S-])=S.COC(=O)NC(=S)NC1=CC=CC=C1NC(=S)NC(=O)OC WPBNNNQJVZRUHP-UHFFFAOYSA-L 0.000 description 1
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- WSFSSNUMVMOOMR-NJFSPNSNSA-N methanone Chemical compound O=[14CH2] WSFSSNUMVMOOMR-NJFSPNSNSA-N 0.000 description 1
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- RADKZDMFGJYCBB-UHFFFAOYSA-N pyridoxal hydrochloride Natural products CC1=NC=C(CO)C(C=O)=C1O RADKZDMFGJYCBB-UHFFFAOYSA-N 0.000 description 1
- ZUFQODAHGAHPFQ-UHFFFAOYSA-N pyridoxine hydrochloride Chemical compound Cl.CC1=NC=C(CO)C(CO)=C1O ZUFQODAHGAHPFQ-UHFFFAOYSA-N 0.000 description 1
- 238000007348 radical reaction Methods 0.000 description 1
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- 210000002345 respiratory system Anatomy 0.000 description 1
- 229960002477 riboflavin Drugs 0.000 description 1
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- 238000000926 separation method Methods 0.000 description 1
- 235000020046 sherry Nutrition 0.000 description 1
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- 235000019157 thiamine Nutrition 0.000 description 1
- 229960003495 thiamine Drugs 0.000 description 1
- 239000011721 thiamine Substances 0.000 description 1
- KYMBYSLLVAOCFI-UHFFFAOYSA-N thiamine Chemical compound CC1=C(CCO)SCN1CC1=CN=C(C)N=C1N KYMBYSLLVAOCFI-UHFFFAOYSA-N 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
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- HGBOYTHUEUWSSQ-UHFFFAOYSA-N valeric aldehyde Natural products CCCCC=O HGBOYTHUEUWSSQ-UHFFFAOYSA-N 0.000 description 1
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
- A61K31/047—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/006—Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Physiology (AREA)
- Nutrition Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention concerns a non-toxic composition in the form of buccal tablets, sublingual tablets or lozenges, which comprises a combination of active agents including one or more aldehyde-binding cysteine compound(s) selected from the group of L-and D-cysteine, N-acetyl cysteine, and the pharmaceutically acceptable salts thereof, and xylitol, which composition further comprises one or more non-toxic additives that include one or more aromatic agents as well as one or more fillers or binders or both, and optional further additives.
Description
Technical field
The present invention relates to reduce the compositions of risk of cancer in the oral cavity that will be placed on object, described compositions contains the component that at least one is intended in the oral cavity being combined in described object the component of harmful aldehyde and the activity for reducing the microorganism causing described aldehyde to be formed at least in part being formed or assemble.
Background technology
Because many kinds of substance enters health by respiratory tract and digestive tract, a large amount of adverse conditions of oral cavity susceptible of people.Some is even worsened by the system of defense of health oneself (such as by tooth microorganism).Such as, dental caries is the disease that a kind of diet is relevant, and it continues the serious health problems becoming most industryization country and developing country.
Study verified, xylitol can be used as safe and efficient dental caries restrictive substance.It is with the natural carbohydrate sample material be present in nearly all plant and animal tissue of low amounts.Xylitol molecules contains tridentate ligand (H-C-OH)
3, it can react with multiple cation (calcium ion in such as tooth mineral matter) and oxyacid, thus forms complex and chelate.In restriction dental caries, xylitol passes through to suppress the metabolism of sugar also thus prophylaxis of teeth is rotted and works.Therefore it is mixed in chewing gum and tablet and in health care products (such as dentifrice and oral rinse), mainly as sweeting agent, i.e. sugar replacement.
But many harmful substances ending at oral cavity also can cause cancer.Ethanol and smoking are the risks and assumptions of upper gastrointestinal cancer, and their use in conjunction can make the risk of generation upper gastrointestinal cancer increase up to 150 times of (Salaspuro, 2003; With people .1990 such as Francheschi).
As confirmed in cell culture and zoopery, the first metabolite acetaldehyde of ethanol is highly toxic, mutagenic and carcinogenic (IARC, 1999).In addition, EPDML, genetic, microbiological and biochemical research is pointed out consumingly, acetaldehyde be local in mankind's upper digestive tract with carcinogen (Salaspuro, 2009 of accumulation; Seitz and Stickel, 2010).Result, international cancer research institution (InternationalAgencyforResearchonCancer, IARC) will to be present in pick-me-up recently and from ethanol endogenous the acetaldehyde that formed classify as human carcinogen's (the 1st group) people .2009 such as () Secretan.
As smoking be exposed to air-polluting consequence, acetaldehyde is also formed in oral cavity, pharynx and epithelium healing.Verified, long-term smoking significantly can increase the acetaldehyde originating from the saliva of microorganism and produce.In fact, verified, relevant risk of cancer is not only caused by usually known polycyclic aromatic hydrocarbon (PAH) with having cigarette smoking, and (the most nearly 40%) is caused by acetaldehyde and formaldehyde largely, and acrylic aldehyde causes other poisonous effect of the most nearly 88.5%.Thus, recommended to reduce the aldehyde (Haussmann, 2012) in medicated cigarette.
Such as can form aldehyde from alcohol by oral microorganism.These comprise oral cavity bacterium in the oral cavity and microorganism, such as Streptococcus (
streptococci), Lactobacillus (
lactobacilli), Corynebacterium (
corynebacteria), oral spirochete (
oralspirochetes), anaerobic cocci (
anaerobiccocci), and particularly porphyromonas gingivalis (
porphyromonasgingivalis), and various Candida (
candida) plant, comprise Candida glabrata (
c.glabrata), Candida parapsilosis (
c.parapsilosis), Oidium tropicale (
c.tropicalis), Candida dubliniensis (
c.dubliniensis), candida guilliermondi (
c.guilliermondii), Candida albicans (
c.albicans) and candida krusei (
c.krusei) (in pharynx).Particularly, verified belong to the normal oral flora of most crowd Streptococcus viridans (
streptococcusviridans), neisseria (
neisseria) group antibacterial and Candida (
candida) plant and can produce a large amount of acetaldehyde from ethanol with by the alcohol fermentation from glucose.
Our research is verified, and the food (comprising beverage) of all sugary (sucrose, maltose, lactose) can contain (or being formed in food) a large amount of acetaldehyde (5-2000 μM) and ethanol (0.1-0.5/1000).Some Yoghourts, Yoghurt and fruit juice contain so many acetaldehyde and ethanol (PCT/FI2006/000104).In addition, such as glucose can be metabolized to acetone acid (salt) by the Candida kind in such as oral cavity, and is after this metabolized to acetaldehyde and ethanol.Fructose can be metabolized to acetone acid (salt) similarly or be metabolized to glycerol.
The average magnitude of the saliva of being secreted by people is every day 1.5 liters.The influence area of aldehyde contained in saliva comprises oral cavity, pharynx, esophagus stomach function regulating.Therefore, the impact of these aldehyde can extend to whole upper digestive tract region.
Prior art comprises such publication: the pharmaceutical composition that it discloses the compound containing binding acetaldehyde, their effect is based on the acetaldehyde formed in active substance and blood flow and/or cell or the reaction of acetaldehyde being carried into blood flow and/or cell, such as US5202354, US4496548, US4528295, US5922346.In addition, pointed out and used containing amino acid whose preparation, it is inhaled in oral cavity or in the oral cavity and chews, to reduce the impact of the harmful free radicals compound formed from such as smoke of tobacco.It is believed that by absorption after, aminoacid can affect multiple tissue and with radical reaction (US5,922,346, WO99/00106).But these can not acetaldehyde in targeting oral cavity.
WO02/36098 has pointed out the compound containing free sulfhydryl groups and/or amino for local and the long-term purposes combining acetaldehyde from saliva, stomach or large intestine.Described compound is mixed with the material that them can be made under the condition of oral cavity, stomach or large intestine to discharge at least 30 minutes.Similarly, WO2006/037848 pointed out for remove or reduce aldehyde in smoking process in saliva, the compositions that comprises one or more free sulfhydryl groups and/or amino.
It is the specially designed compositions containing cysteine of the long-term impact in oral cavity that above-mentioned list of references does not all provide.In addition, they all do not have the product aldehyde ability of targeting oral microorganism.
Summary of the invention
An object of the present invention is to provide new compositions, it may be used for the aldehyde reduced in the oral cavity of object, and indirectly also reduces the aldehyde in stomach.
Particularly, an object of the present invention is to provide such new compositions worked by least 2 different approaches, thus be provided in the cooperative effect reduced in described aldehyde.
Another object of the present invention is to provide new compositions, and it shelters the taste of the aldehyde bonded compound (one or more) in described compositions.
Present invention achieves these and other objects, and it is better than the advantage of known compositions and method, as describe hereinafter with claimed.
Therefore, an object of the present invention is, comprise the compositions of one or more aldehyde bonded compounds.
The present invention is based on following discovery, and aldehyde (such as acetaldehyde) is formed in the oral cavity, such as, as the result of microbial activity.Cysteine and derivant thereof can covalently in conjunction with these aldehyde and thus their mutagenic and poisonous character of deactivation, and xylitol can kill or at least deactivation oral microorganism, is namely also the such microorganism causing acetaldehyde to produce.
According to the present invention, described compositions comprises the combination of reactive compound, and described reactive compound comprises one or more cysteine compounds and xylitol, and it is combined into lozenge or buccal tablet or sublingual tablet by means of the nontoxic additive of at least one.Described additive (one or more) is selected from such additive particularly: under oral conditions, and it causes reactive compound to enter saliva from lozenge or tablet sustained release.
Say more accurately, the feature according to compositions of the present invention is, in the content described in the characteristic of claim 1.
The invention provides important advantage.The described compositions comprising aldehyde bonded cysteine compound may be used for the risk reducing development oral cancer, and indirectly reduces the risk of the cancer (because aldehyde can be carried into these regions by saliva) of development stomach, intestinal and/or colon.
In addition, when they are associatedly consumed with feed, or when them with when consume alcohol is associatedly consumed, compositions of the present invention is especially effectively with useful especially for aldehyde bonded.
For the alternate manner of smoking or consume tobacco, equally so, namely when them and smoking or when using the alternate manner of Nicotiana tabacum L. associatedly to consume, compositions of the present invention is effective and useful especially especially for aldehyde bonded.
Particularly, when the content of aldehyde formed from the alcohol contained by food or pick-me-up is maximum (namely the most harmful and the most carcinogenic), or when the harmful constituent of smoke of tobacco concentrates in saliva, compositions of the present invention can discharge aldehyde bonded compound in the oral cavity.
Because aldehyde also partly causes tobacco addiction, when by this compositions and smoking or when using the alternate manner of Nicotiana tabacum L. associatedly to use, the present invention also will cause alleviating of described addiction.
Accompanying drawing explanation
The average acetaldehyde that Fig. 1 shows the Candida separator in incubation produces (± SEM).
Fig. 2 shows the later saliva acetaldehyde (SEM) of smoking 5min together with placebo and together with the suction tablet containing 1.25mg, 2.5mg, 5mg or 10mgL-cysteine.
Detailed description of the invention
The present invention relates to compositions, it will be placed in the oral cavity of object, and containing reactive compound (comprising one or more cysteine compounds) (the namely aldehyde bonded compound) that be intended in conjunction with the aldehyde (such as acetaldehyde, formaldehyde, acrylic aldehyde, propionic aldehyde and butyraldehyde) in oral cavity, with the xylitol being intended for destruction (namely killing) and being present at least some microorganism in oral cavity, and the combination of one or more nontoxic additives harmless for people (or animal) consumption.
The object of compositions of the present invention is, is reduced in oral cavity neutralization cancer in the gastrointestinal tract or the risk of poisonous effect.
Described compositions works by making at least some aldehyde be combined into the cysteine compound (one or more) of harmless form, and the xylitol at least some of killing in oral cavity is responsible for the microorganism producing aldehyde.Thus, described effect is collaborative, because aldehyde comparatively in a small amount will be produced, and effective combination of aldehyde comparatively in a small amount described in realizing, thus cause the remarkable more effective reduction of the aldehyde compared with the content using Previous solutions to reach in saliva.
In the light of recent researches, xylitol suppresses at least Candida to produce acetaldehyde from ethanol significantly.Output is reduced to below the mutagenesis acetaldehyde level of 40-100 μM by its meeting.Do not having under xylitol, it is high (>200 μM) that the average acetaldehyde in ethanol incubation produces.Verified in the past, xylitol can suppress to produce sour oral cavity bacterium carbohydrate metabolism and thus prophylaxis of teeth rot.Need 5-6 gram just can reach this effect with the exposure of 3 times every day.But the xylitol concentration of verified at least 65mM also has antimicrobial acivity to ear pathogenic bacteria.
The object using described additive (one or more) makes reactive compound be combined into lozenge, or be combined into buccal tablet or sublingual tablet.Particularly, at least one additive is selected from and described cysteine compound (one or more) can be caused under the condition in oral cavity to enter carrier saliva or binding agent from lozenge or tablet sustained release.
According to a preferred embodiment of the invention, at least one additive of compositions is formed as the coating on lozenge or tablet, described lozenge or tablet contain the remaining ingredient of compositions.Preferably, such coating by xylitol at least partially or being formed at least partially of other aromatic any of compositions.
Term " additive " comprises carrier, filler and binding agent and aromatic, coloring agent and non-functional additive here.These additives are nontoxic, and the release preferably controlling activating agent occurs in the oral cavity especially, and the most suitably with continuous fashion.These preparations intention is put in the oral cavity, such as cheek or between lip and gingiva, or their intentions are sucked.
Described compositions includes the above-mentioned cysteine compound (one or more) of effective amount.Here, effective dose refer to can in conjunction with or the amount of a certain amount of aldehyde of deactivation, described a certain amount of aldehyde is carried into oral cavity from food, beverage or Nicotiana tabacum L. or is formed in the oral cavity (such as by microbial activity wherein) in the digestion process of Foods or drinks or after consumption.
Usually, the single unit of described compositions or preparation comprise 1-30mg, preferably 1-20mg, more preferably 1-10mg and the most suitably 2-6mg cysteine (one or more).But, can in these units disposable employed 1-2.
The content of cysteine compound (one or more) is then preferably the 1-50% of composition weight, more preferably 5-40%, the most suitably 20-30%.Usually, described content is 20-25 % by weight.
Described cysteine compound is preferably selected from L-and D-Cys, their derivant (such as NAC) and their pharmaceutically acceptable salt.
Described compositions also includes the above-mentioned xylitol of effective amount.Here, effective dose refers to the amount of the measured deactivation of the product acetaldehyde antibacterial at least can causing oral cavity.
Usually, the individual unit of described compositions or preparation comprise 50-500mg, preferably 50-300mg, more preferably 100-300mg and the most suitably 200-300mg xylitol.But, as mentioned above, can a disposable employed 1-2 unit.
The content of xylitol is then preferably the 10-90% of composition weight, more preferably 10-60%, particularly 20-60%, the most suitably 40-60%.Usually, described content is about 50%.
The final concentration of 110mM xylitol equals to hold facile 17mg/mL in the oral cavity.The concentration higher than 30mg/mL can be detected in saliva, and have been found that this level keeps significantly raising, the most nearly 30min.Thus, according to the present invention preferably, the initial xylitol concentration (in saliva) of at least 17mg/ml is provided.
Such as, Cys is the cysteine of easily oxidation, and it can not combine the aldehyde be present in deactivation in oral cavity effectively, particularly when being used alone in conventional immediate release dosage form.But, the invention provides a kind of dosage form, even if it also can produce long term when not using the additive extending active component release, and providing cooperative effect together with the xylitol of compositions.
Preferably compositions is mixed with coating lozenge, buccal tablet or sublingual tablet, and at least one aromatic (comprising xylitol) be present in compositions is comprised in the coating.Use an advantage of coating to be, what it will shelter cysteine compound (one or more) makes us unhappy taste.
Because cysteine is easily oxidation, it is expected to, it also will easily change into the cystine of pharmaceutically non-activity in the oral cavity.When cysteine is added according in lozenge of the present invention or buccal tablet or sublingual tablet time, this has been proved and can not have occurred.On the contrary, when such as using in the present invention, cysteine keeps the most nearly 20 minutes in the oral cavity in an active.
Preferably, the additive used is selected from such additive: it can control the release of activating agent, makes these compounds in the time more than 1 minute, but is usually less than 20 minutes, preferred 1-15 minute, the most suitably discharged partly in the oral cavity in 5-10 minute.
According to a preferred embodiment of the invention, with feed associatedly (namely before being about to take food, on the feed in process or on the feed after soon) or with consume alcohol associatedly (namely by before consuming potion ethanol, consuming in potion ethanol process or after consuming potion ethanol) use compositions.
According to another preferred embodiment of the present invention, (namely before by smoking (or other of Nicotiana tabacum L. uses), in smoking (or other of Nicotiana tabacum L. uses) process or after smoking (or other of Nicotiana tabacum L. uses) soon) is used associatedly to use compositions with other of smoking or Nicotiana tabacum L..
Term " be about to ... before " and " soon afterwards " refer on the feed, the time range of 5 minutes at the most before or after consume alcohol or smoking (or using alternate manner of Nicotiana tabacum L.), the preferably time range of 2 minutes at the most, more preferably the time range of 1 minute at the most, and the most on the feed, the time range of 0.5 minute at the most before or after consume alcohol or smoking.
But described compositions can also use in a continuous manner, such as every 10 minutes.According to a preferred embodiment of the invention, interval at 5-15 minute, preferably more new dosage (if alcohol consumption or smoking continue an interval of being longer than described interval) in 5-10 minute interval.
" smoking " represents the suction (using other application any of Folium Nicotianae preparatum, chewing tobacco or tobacco product) of any tobacco product, wherein described tobacco product or its part is put in the oral cavity or guides to oral cavity.Therefore, described tobacco product can be medicated cigarette, cigar, Folium Nicotianae preparatum, chewing tobacco or pipe tobacco.But the present invention is the most applicable associatedly to be used with using the tobacco product producing flue gas.
It put in the interval of in the oral cavity 5-10 minute, described compositions discharges the major part of aldehyde bonded compound.
" combination of aldehyde " preferably represents the free sulfhydryl groups of aldehyde and cysteine (or similar compound) or chemical reaction amino or therebetween, and wherein said aldehyde combines the larger molecule of formation with " aldehyde bonded compound ".With the reaction of cysteine, such as acetaldehyde mainly makes it self be bonded to sulfydryl and the amino of cysteine, and forms 2-methyl-L-Thiazolidine-4-formic acid (and water).
According to the present invention, the compound obtained from aldehyde by the chemical bond with cysteine is safe for organism.
But aldehyde (in free form) is not harmless for object.Acetaldehyde in such as human mouth harmful/carcinogenic content is roughly 20-800 μm of ol/l saliva, and the content being low to moderate about 20-50 μM can cause the Cancer-causing mutation of cellular level.Generally speaking, the level more than 40-100 μM is considered to mutagenic.In addition, formaldehyde can cause certain carcinogenesis, and acrylic aldehyde can cause other poisonous effect.
By using compositions of the present invention, the aldehyde in saliva can be made to be reduced in fact lower than level when not using described compositions, this means, aldehyde can being remained on than not using level that is low by least 20% according to the corresponding situation of compositions of the present invention, preferably low >40% and most preferably low >60%.
By consume alcohol beverage (particularly strong alcoholic beverage) or containing spirituous food, as the consequence of smoking, with when consuming product (such as food) containing aldehyde, the so harmful or carcinogenic aldehyde in human mouth and in gastrointestinal esophagus, stomach or other parts can be caused.
Described aldehyde can be formed from ethanol in the oral cavity, is usually formed by oral microorganism." oral microorganism " is intended to the oral cavity bacterium that comprises in the oral cavity and microorganism, such as Streptococcus (
streptococci), Lactobacillus (
lactobacilli), Corynebacterium (
corynebacteria), oral spirochete (
oralspirochetes), anaerobic cocci (
anaerobiccocci), and particularly porphyromonas gingivalis (
porphyromonasgingivalis), and various Candida (
candida) plant, comprise Candida glabrata (
c.glabrata), Candida parapsilosis (
c.parapsilosis), Oidium tropicale (
c.tropicalis), Candida dubliniensis (
c.dubliniensis), candida guilliermondi (
c.guilliermondii), Candida albicans (
c.albicans) and candida krusei (
c.krusei) (in pharynx).But described aldehyde can also be formed in the beverage or in food, or it can former state add in beverage or food.
" alcoholic beverage " is the beverage containing ethanol, and their ethanol content changes between 0.7 volume % to 84 volume %.
" ethanol food " represents the food of the ethanol containing at least 0.7 % by weight.Such food can be, such as, the fruit juice of fermentation or preserve, or with a small amount of ethanol antiseptical food, cake, fruit jelly, and with the mousse (mousse) of liqueur seasoning, or corresponding alcoholic product.
" containing aldehyde food " represents even before consumption containing the food of aldehyde.Acetaldehyde can be formed from ethanol in described food, and described ethanol associatedly produces, such as in medicated beer, applejack, wine, home brew and other alcoholic beverage and in much fruit juice with fermentation.In some food (such as some milk product), acetaldehyde is used to anticorrosion object and tarting up, or as microbial activity result and form acetaldehyde in the product.Such as, sugary fruit juice or generally can provide suitable substrate for described microorganism containing confectionery.Also the acetaldehyde of high concentration can be formed in the milk product (such as Yoghurt) of fermentation.In this case, the microorganism being mainly used for preparing Yoghurt produces acetaldehyde.For alcoholic beverage, sherry and this applejack of kappa degree (Calvados) are also containing acetaldehyde a large amount of especially.
Even if when consuming low alcoholic beverage or food (namely only containing those of a small amount of ethanol (even <0.7%)), also can be useful according to the application of compositions of the present invention, even if because these content are also carcinogenic on long terms.
Additive (one or more) in described compositions comprises the combination of material, described material can especially as carrier, filler, binding agent and other type additive and work.
Such as aromatic (except xylitol) can be used as additive, and can multiple kinds of carbohydrate be selected from, such as glucose, sorbitol, eucalyptol, thymol, sucrose, saccharin sodium, methyl salicylate and menthol, be preferably selected from glucose, sorbitol and sucrose.
The content of the such aromatic in described compositions is preferably 20-80 % by weight, is the most suitably 20-45 % by weight.A unit dose is usually containing 100-500mg aromatic (except xylitol), such as glucose, sorbitol and sucrose.
The use of one or more filleies is preferred in the present invention.These filleies can be selected from the additive that do not expand being suitable for such as compressed tablets.These especially comprise phosphate, hydrophosphate, cellulose and their derivant and soap.The most suitably, calcium hydrogen phosphate, microcrystalline Cellulose or magnesium stearate (or the combination of two or more in these) is selected to be used as filler in the composition.
The ratio of the filler (one or more) in described compositions is preferably 5-80 % by weight, more preferably 10-50 % by weight, is the most suitably 10-30 % by weight.
In order to promote compositions to be kept in the oral cavity, preferably, comprise at least one binding agent or adhesive in the composition, preferably be selected from polymer, such as cellulose derivative, chitosan, alginate, Polyethylene Glycol, carbomer or polycarbophil, be the most suitably selected from the carbomer of hydroxypropyl emthylcellulose or its derivant or carbopol level.
Such adhesive may be used in the coating on buccal tablet or sublingual tablet or on lozenge, to promote that unit dose is to the adhesion of oral mucosa.For this purpose, the polymer forming gel in the condition in oral cavity is particularly preferred.The polymer of such formation gel comprises above-mentioned binding agent.
In described compositions, the ratio of this optional adhesive is preferably 1-50 % by weight, more preferably 5-40 % by weight, and is the most suitably 10-30 % by weight.
Additive (one or more) according to compositions of the present invention can also comprise one or more hydrophobic compounds, preferably add in the coating on buccal tablet or sublingual tablet or lozenge, to stop or the water contacted with cysteine compound (one or more) that slows down.
According to a particularly preferred embodiment of the present invention, described compositions is made up of cysteine compound, xylitol, aromatic and optional binding agent (one or more) and filler (one or more).
According to another particularly preferred embodiment of the present invention, described compositions comprises other additive that one or more are selected from chromium, vitamin A. D. E and C, niacin, biotin, thiamine, vitamin B2, B5, B6 and B12, folic acid and trace element (such as chromium, manganese, selenium, zinc and ferrum), to add other health benefits.
Preparing in coated tablet, preferably, the graininess of preparation coating blend bag quilt contains the mixture of cysteine, described coating blend comprise xylitol at least partially with optional aromatic (one or more).In order to shelter the taste of cysteine compound (one or more) most effectively, at least major part (>50 % by weight) of aromatic (one or more) is added in coating blend, such as 80-100 % by weight.The most suitably, the xylitol of 50-100 % by weight is also present in coating, normally 80-100 % by weight.
Following non-limiting example is only intended to explain the advantage using the present invention to obtain.
Embodiment
Embodiment 1
Selecting the laboratory of 7 Candida kinds and clinical isolates to be used for research, is Candida glabrata, Candida parapsilosis, Oidium tropicale, Candida dubliniensis, candida guilliermondi, candida krusei and Candida albicans.
350 μ l are suspended in these yeast separation things (1x10 in phosphate buffered saline (PBS) (PBS)
7individual colony-forming units) aliquot transfer air inlet phase chromatography phial in.After this, add 50 μ l and contain the PBS buffer that the PBS buffer of ethanol (final concentration 12mM) and 50 μ l contain glucose, fructose or xylitol (final concentration 110mM), and sealed tube shape bottle immediately.By sample 37 DEG C of incubations 30 minutes, and inject 50 μ l6M perchloric acid (PCA) through the rubber septum of phial and carry out stopped reaction.The acetaldehyde (see Fig. 1) formed is measured by gas chromatography.
Xylitol (p<0.0001) makes the amount of the acetaldehyde produced from ethanol decrease 84%.Do not having under xylitol, it is 220.5 μMs that the average acetaldehyde in ethanol incubation produces, and the average acetaldehyde generation in ethanol-xylitol incubation is 32.8 μMs.
Altogether incubation makes the amount of the acetaldehyde of generation decrease 23% together with glucose, and together with fructose altogether incubation make the amount of the acetaldehyde of generation decrease 29%.
Thus, glucose and fructose do not have the appreciable impact the same with xylitol.In fact, taking in the concentration of the representative concentration found in the oral cavity in proprietary xylitol products process, finding that the acetaldehyde of the carcinogenecity that xylitol can make Candida produce from ethanol is reduced to below the Mutagenicity of 40-100 μM.
Find certain change that the acetaldehyde between different Candida kind produces.Find that Candida glabrata separator is the highest Producer, and candida krusei separator is lowest manufactured person.Correspondingly, when together with 110mM ethanol altogether incubation 10 minutes time, xylitol makes alcoholdehydrogenase (ADH) activity of Candida glabrata separator reduce by 61%, and makes alcoholdehydrogenase (ADH) activity of Candida albicans separator reduce by 100%.When being total to incubation together with 11mM ethanol, the reduction in Candida glabrata separator is 66%, and the reduction in Candida albicans separator is 100%.
Embodiment 2
Prepared suction tablet, it comprises:
Cys 20mg
Xylitol (or equivalent sugar or sugar alcohol) 750mg
Flavoring agent is appropriate
Magnesium stearate 10mg.
Following preparation compositions: the major part (part reserving xylitol does not use) of cysteine and residual components is mixed into Powdered piece, and it is pressed into suction tablet, by it with the xylitol bag quilt reserved.
Embodiment 3
Prepare sublingual tablet, it comprises:
Cys 10mg
Xylitol 250mg
Flavoring agent is appropriate
Magnesium stearate 5mg.
Following preparation compositions: the major part (part reserving xylitol does not use) of cysteine and residual components is mixed into Powdered piece, and it is pressed into sublingual tablet, by it with the xylitol bag quilt reserved.
Embodiment 4
Two individualities test the preparation prepared according to embodiment 2.Before smoking, after 5 minutes then in smoking process, that is, 0min, 5min, 10min and 15min after testee starts smoking, measures the saliva acetaldehyde of testee.Each testee aspirates Linear Leaf Speedwell cigarette, and meanwhile, along with they suck placebo tablet, from their oral collection saliva.Smoking continues 5min.In another experiment, testee repeats research by the tablet sucked containing 20mg cysteine.
Before smoking, the saliva acetaldehyde of each testee is low-down.In second test, acetaldehyde has been reduced to immeasurablel level in 5 minutes at first later.
Embodiment 5
5 smokers's (age 29 ± 2.8) participate in research, wherein aspirate 3 medicated cigarettes (between have the removing phase).When medicated cigarette is often propped up in suction (in 5 minutes), volunteer sucks the unwitting tablet prepared according to embodiment 2, and it contains placebo, 1.25mg, 2.5mg, 5mg, 10mg or 20mgL-cysteine.From smoking count after 0,5,10,20 minute, analyzed the acetaldehyde in saliva sample by gas chromatography.
Cys tablet (5mg, 10 and 20mg) eliminates all acetaldehyde (see Fig. 2) being derived from Nicotiana tabacum L. from saliva.The later average saliva acetaldehyde immediately of smoking is 191.2 ± 48.5 μMs, 0 μM, 0 μM, 0 μM respectively for placebo and 5mg, 10mg and 20mgL-cysteine tablet.
Research shows, even if 5mgL-cysteine is when with also can the acetaldehyde of carcinogenecity in smoking process fully in deactivation saliva when melting tablet delivery.Compared with placebo, the Cys tablet of 1.25mg can make the amount of acetaldehyde reduce about 2/3.
Embodiment 6
Prepared lozenge, it comprises:
Cys 3mg (0.6%)
Sorbitol 224mg (44.8%)
Xylitol 250mg (50.0%)
Aromatic (flavoring agent) (one or more) 12.5mg (2.5%)
Magnesium stearate 10mg (2.0%)
Silicon dioxide 0.5mg (0.1%).
Following preparation compositions: first form premix, it contains the sorbitol of the Cys of grinding form, aromatic, silicon dioxide and Part I.Subsequently, the remainder of sorbitol and xylitol are added in the premix in the first blender (Muller blender), after this magnesium stearate is added in the mixture (at high shear Collette blender) of formation.Then final mixture is transferred to final blender (Muller blender) to provide uniform mixture, by it, in the end the stage suppresses and coating.
Document
The people .CancerRes1990 such as Francheschi; 50:6502-07
Haussmann,H.-J.Chem.Res.Toxicol.2012;25,794-810
InternationalAgencyforResearchonCancer, 1999; Acetaldehyde. see: Re-evaluationofsomeorganicchemicals, hydrazineandhydrogenperoxide.IARCMonographsontheevaluati onontheCarcinogenicRiskstoHumans, 71st volume, 319-335 page.
Salaspuro,M.BestPractResClin.Gastroenterol2003;17:679-94
SalaspuroM.Acetaldehydeasacommondenominatorandcumulativecarcinogenindigestivetractcancers.ScandJGastroenterol2009;44:912-925.
SalaspuroVJ, HietalaJM, MarvolaML, SalaspuroMP.Eliminatingcarcinogenicacetaldehydebycystein efromsalivaduringsmoking.CancerEpidemiolBiomarkersPrev.2 in January, 006; 15 (1): 146-149.
The people .Areviewofhumancarcinogens-PartE:tobacco such as SecretanB, StraifK, BaanR, GrosseY, ElGhissassi, BouvardV, arecanut, alcohol, coalsmoke, andsaltedfish.LancetOncol2009; 10:1033-1034.
SeitzHK,StickelF.Acetaldehydeasanunderestimatedriskfactorforcancerdevelopment:roleofgeneticsinethanolmetabolism.GenesNutr2010;5:121-128。
Claims (15)
1. the non-toxic composite in buccal tablet, sublingual tablet or lozenge form, it is characterized in that, it comprises the combination of activating agent, and it comprises
-one or more aldehyde bonded cysteine compounds, it is selected from L-and D-Cys, NAC and pharmaceutically acceptable salt thereof, and
-xylitol,
And be characterised in that, it comprises one or more nontoxic additives and other optional additive further, described nontoxic additive comprise one or more aromatic and one or more filleies or binding agent or the two.
2. compositions according to claim 1, it is for reducing the risk of the cancer of development mouth area.
3. compositions according to claim 1 and 2, described compositions be intended on the feed in process or after, in No alcoholic beverages process or after or in smoking process, be administered to object, to reduce the risk of the cancer in development oral cavity or territory, gastric area.
4. the compositions according to any one in claim 1-3, described compositions comprises the cysteine compound (one or more) of per unit dosage 1-30mg, preferably 1-20mg, more preferably 1-10mg and the most suitably amount of 2-6mg.
5. the compositions according to any one in claim 1-4, described compositions comprises the xylitol of per unit dosage 50-500mg, preferably 50-300mg, more preferably 100-300mg and the most suitably amount of 200-300mg.
6. the compositions according to any one in claim 1-5, described compositions in 1-20 minute, preferably in 1-15 minute, release of active compounds in 5-10 minute usually.
7. the compositions according to any one in claim 1-6, wherein said aromatic is selected from multiple kinds of carbohydrate, such as glucose, sorbitol, eucalyptol, thymol, sucrose, saccharin sodium, methyl salicylate and menthol, be preferably selected from glucose, sorbitol and sucrose.
8. the compositions according to any one in claim 1-7, described compositions has the fragrance level of 20-80 % by weight, preferably 20-45 % by weight.
9. the compositions according to any one in claim 1-8, described compositions is further containing one or more filleies, preferably be selected from phosphate, hydrophosphate, cellulose and their derivant, and soap, the most suitably be selected from calcium hydrogen phosphate, microcrystalline Cellulose or magnesium stearate, or the combination of two or more in these.
10. compositions according to claim 9, the ratio of the filler (one or more) in wherein said compositions is 5-80 % by weight, preferably 10-50 % by weight, the most suitably 10-30 % by weight.
11. the compositions according to any one in claim 1-10, described compositions is further containing at least one binding agent or adhesive, preferably be selected from polymer, such as cellulose derivative, chitosan, alginate, Polyethylene Glycol, carbomer or polycarbophil, be the most suitably selected from the carbomer of hydroxypropyl emthylcellulose or its derivant or carbopol level.
12. compositionss according to claim 11, the binding agent in wherein said compositions or the ratio of adhesive are 1-50 % by weight, preferably 5-40 % by weight and the most suitably 10-30 % by weight.
13. the compositions according to any one in claim 1-12, described compositions has been formulated into the buccal tablet, sublingual tablet or the lozenge that use coating blend bag quilt, described coating blend comprise xylitol at least partially with optional aromatic (one or more).
14. the compositions according to any one in claim 1-13, described compositions has been formulated into the mixture using the graininess of coating blend bag quilt to contain cysteine, described coating blend comprise xylitol at least partially with optional aromatic (one or more).
15. compositionss according to claim 13 or 14, wherein use the xylitol of the 50-100 % by weight of described compositions to form described coating blend.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810750529.3A CN108969500A (en) | 2013-02-01 | 2014-01-31 | For combining the composition of the aldehyde in oral cavity |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FI20135097A FI20135097L (en) | 2013-02-01 | 2013-02-01 | Composition for binding aldehydes in the mouth |
| FI20135097 | 2013-02-01 | ||
| PCT/FI2014/050076 WO2014118438A1 (en) | 2013-02-01 | 2014-01-31 | Composition for binding aldehydes in the mouth |
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| CN201810750529.3A Pending CN108969500A (en) | 2013-02-01 | 2014-01-31 | For combining the composition of the aldehyde in oral cavity |
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| EP (1) | EP2950794A4 (en) |
| CN (2) | CN105307649A (en) |
| EA (1) | EA201591203A1 (en) |
| FI (1) | FI20135097L (en) |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1486177A (en) * | 2000-10-30 | 2004-03-31 | ϣ�������ع�����˾ | Method and preparation for binding acetaldehyde in saliva, stomach and large intestine |
| WO2013001167A1 (en) * | 2011-06-29 | 2013-01-03 | Biohit Oyj | Non-toxic compositions for decreasing the risk of cancer caused by oral microbes |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006037848A1 (en) * | 2004-10-08 | 2006-04-13 | Biohit Oyj | Method and preparation for binding aldehydes in saliva |
| FI122914B (en) * | 2005-04-01 | 2012-08-31 | Biohit Oyj | Food composition for binding of acetaldehyde in the mouth and in the digestive tract and process for the preparation of the composition |
| FI20070705L (en) * | 2007-09-14 | 2009-06-02 | Biohit Oyj | Binding of acetaldehyde in the mouth and in the stomach |
| US20090197956A1 (en) * | 2008-02-04 | 2009-08-06 | Arbor Pharmaceuticals, Inc. | Treatment of acute otitis media with xylitol and n-acetylcysteine |
| FI20115377A (en) * | 2011-04-18 | 2012-10-19 | Biohit Oyj | Medical products for use in conditions related to microbial infections of upper respiratory and digestive organs |
-
2013
- 2013-02-01 FI FI20135097A patent/FI20135097L/en not_active IP Right Cessation
-
2014
- 2014-01-31 WO PCT/FI2014/050076 patent/WO2014118438A1/en active Application Filing
- 2014-01-31 MX MX2015009972A patent/MX2015009972A/en unknown
- 2014-01-31 EP EP14746925.8A patent/EP2950794A4/en not_active Withdrawn
- 2014-01-31 EA EA201591203A patent/EA201591203A1/en unknown
- 2014-01-31 CN CN201480007086.9A patent/CN105307649A/en active Pending
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1486177A (en) * | 2000-10-30 | 2004-03-31 | ϣ�������ع�����˾ | Method and preparation for binding acetaldehyde in saliva, stomach and large intestine |
| WO2013001167A1 (en) * | 2011-06-29 | 2013-01-03 | Biohit Oyj | Non-toxic compositions for decreasing the risk of cancer caused by oral microbes |
Non-Patent Citations (2)
| Title |
|---|
| ALMA KARTAL等: "Compatibility of chewing gum excipients with the amino acid L-cysteine and stability of the active substance in directly compressed chewing gum formulation", 《JOURNAL OF PHARMACY AND PHARMACOLOGY》 * |
| JOHANNA UITTAMO等: "Xylitol inhibits carcinogenic acetaldehyde production by Candida species", 《INTERNATIONAL JOURNAL OF CANCER》 * |
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| WO2014118438A1 (en) | 2014-08-07 |
| MX2015009972A (en) | 2016-03-11 |
| EP2950794A4 (en) | 2016-11-09 |
| EP2950794A1 (en) | 2015-12-09 |
| CN108969500A (en) | 2018-12-11 |
| FI20135097L (en) | 2014-08-02 |
| EA201591203A1 (en) | 2016-01-29 |
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