WO2022238969A1 - Distillate for the treatment of a skin condition or diseases - Google Patents
Distillate for the treatment of a skin condition or diseases Download PDFInfo
- Publication number
- WO2022238969A1 WO2022238969A1 PCT/IB2022/054470 IB2022054470W WO2022238969A1 WO 2022238969 A1 WO2022238969 A1 WO 2022238969A1 IB 2022054470 W IB2022054470 W IB 2022054470W WO 2022238969 A1 WO2022238969 A1 WO 2022238969A1
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- WO
- WIPO (PCT)
- Prior art keywords
- distillate
- wheat
- treatment
- spme
- range
- Prior art date
Links
- 238000011282 treatment Methods 0.000 title claims abstract description 50
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title description 15
- 201000010099 disease Diseases 0.000 title description 13
- 241000209140 Triticum Species 0.000 claims abstract description 67
- 235000021307 Triticum Nutrition 0.000 claims abstract description 67
- 238000000034 method Methods 0.000 claims abstract description 56
- 208000007514 Herpes zoster Diseases 0.000 claims abstract description 42
- 230000008569 process Effects 0.000 claims abstract description 24
- 208000017520 skin disease Diseases 0.000 claims abstract description 19
- 238000002360 preparation method Methods 0.000 claims abstract description 9
- 238000002290 gas chromatography-mass spectrometry Methods 0.000 claims description 46
- 238000002470 solid-phase micro-extraction Methods 0.000 claims description 33
- HYBBIBNJHNGZAN-UHFFFAOYSA-N furfural Chemical compound O=CC1=CC=CO1 HYBBIBNJHNGZAN-UHFFFAOYSA-N 0.000 claims description 29
- 235000013339 cereals Nutrition 0.000 claims description 21
- 238000010438 heat treatment Methods 0.000 claims description 17
- XPFVYQJUAUNWIW-UHFFFAOYSA-N furfuryl alcohol Chemical compound OCC1=CC=CO1 XPFVYQJUAUNWIW-UHFFFAOYSA-N 0.000 claims description 9
- 206010012438 Dermatitis atopic Diseases 0.000 claims description 8
- 201000008937 atopic dermatitis Diseases 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 8
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- SMNDYUVBFMFKNZ-UHFFFAOYSA-N 2-furoic acid Chemical compound OC(=O)C1=CC=CO1 SMNDYUVBFMFKNZ-UHFFFAOYSA-N 0.000 claims description 6
- 238000004821 distillation Methods 0.000 claims description 6
- ZWEHNKRNPOVVGH-UHFFFAOYSA-N Methyl ethyl ketone Natural products CCC(C)=O ZWEHNKRNPOVVGH-UHFFFAOYSA-N 0.000 claims description 5
- 239000003921 oil Substances 0.000 claims description 4
- 201000004624 Dermatitis Diseases 0.000 claims description 3
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- TZMFJUDUGYTVRY-UHFFFAOYSA-N pentane-2,3-dione Chemical compound CCC(=O)C(C)=O TZMFJUDUGYTVRY-UHFFFAOYSA-N 0.000 claims 2
- MZVBMFAXOBHFID-UHFFFAOYSA-N 1-(2-methylfuran-3-yl)ethanone Chemical compound CC(=O)C=1C=COC=1C MZVBMFAXOBHFID-UHFFFAOYSA-N 0.000 claims 1
- IEMMBWWQXVXBEU-UHFFFAOYSA-N 2-acetylfuran Chemical compound CC(=O)C1=CC=CO1 IEMMBWWQXVXBEU-UHFFFAOYSA-N 0.000 claims 1
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- MKUXAQIIEYXACX-UHFFFAOYSA-N aciclovir Chemical compound N1C(N)=NC(=O)C2=C1N(COCCO)C=N2 MKUXAQIIEYXACX-UHFFFAOYSA-N 0.000 description 3
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- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
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- XQFRJNBWHJMXHO-RRKCRQDMSA-N IDUR Chemical compound C1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C(I)=C1 XQFRJNBWHJMXHO-RRKCRQDMSA-N 0.000 description 2
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- GCQYYIHYQMVWLT-HQNLTJAPSA-N Sorivudine Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C(\C=C\Br)=C1 GCQYYIHYQMVWLT-HQNLTJAPSA-N 0.000 description 1
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- 201000005884 exanthem Diseases 0.000 description 1
- 229960004396 famciclovir Drugs 0.000 description 1
- GGXKWVWZWMLJEH-UHFFFAOYSA-N famcyclovir Chemical compound N1=C(N)N=C2N(CCC(COC(=O)C)COC(C)=O)C=NC2=C1 GGXKWVWZWMLJEH-UHFFFAOYSA-N 0.000 description 1
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- IRSCQMHQWWYFCW-UHFFFAOYSA-N ganciclovir Chemical compound O=C1NC(N)=NC2=C1N=CN2COC(CO)CO IRSCQMHQWWYFCW-UHFFFAOYSA-N 0.000 description 1
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- 229910052757 nitrogen Inorganic materials 0.000 description 1
- CXQXSVUQTKDNFP-UHFFFAOYSA-N octamethyltrisiloxane Chemical compound C[Si](C)(C)O[Si](C)(C)O[Si](C)(C)C CXQXSVUQTKDNFP-UHFFFAOYSA-N 0.000 description 1
- 210000004273 ophthalmic nerve Anatomy 0.000 description 1
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- 229960000329 ribavirin Drugs 0.000 description 1
- HZCAHMRRMINHDJ-DBRKOABJSA-N ribavirin Natural products O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1N=CN=C1 HZCAHMRRMINHDJ-DBRKOABJSA-N 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/88—Liliopsida (monocotyledons)
- A61K36/899—Poaceae or Gramineae (Grass family), e.g. bamboo, corn or sugar cane
-
- 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
- A61K9/10—Dispersions; Emulsions
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
- A61P31/22—Antivirals for DNA viruses for herpes viruses
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
- C07C49/385—Saturated compounds containing a keto group being part of a ring
- C07C49/395—Saturated compounds containing a keto group being part of a ring of a five-membered ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
- C07C49/587—Unsaturated compounds containing a keto groups being part of a ring
- C07C49/597—Unsaturated compounds containing a keto groups being part of a ring of a five-membered ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D307/40—Radicals substituted by oxygen atoms
- C07D307/42—Singly bound oxygen atoms
- C07D307/44—Furfuryl alcohol
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D307/40—Radicals substituted by oxygen atoms
- C07D307/46—Doubly bound oxygen atoms, or two oxygen atoms singly bound to the same carbon atom
- C07D307/48—Furfural
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D307/40—Radicals substituted by oxygen atoms
- C07D307/46—Doubly bound oxygen atoms, or two oxygen atoms singly bound to the same carbon atom
- C07D307/48—Furfural
- C07D307/50—Preparation from natural products
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
- C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
- C07C2601/10—Systems containing only non-condensed rings with a five-membered ring the ring being unsaturated
Definitions
- the invention concerns a process for the preparation of a wheat distillate, a wheat distillate obtainable from this process and uses thereof in the treatment of skin diseases and conditions.
- the invention concerns a wheat distillate for use in the treatment of Herpes Zoster.
- Herpes zoster is one of the skin diseases caused by the reactivation of the varicella- zoster virus (VZV). This reactivation occurs more frequently in the elderly or in immunosuppressed people. VZV is part of the Herpes virus family and is the etiological agent of childhood varicella, after which the virus remains in a latent state in the adjacent dorsal root ganglia. In conditions of immunosuppression, emotional stress, neoplasia, etc., as an elderly adult, the virus reactivates and causes vesicular lesions on the skin, preceded by itching, pain or a feeling of hyperesthesia, which form erythematous patches.
- VZV varicella- zoster virus
- viruses are not likely to be eliminated by treatment with antibiotics.
- chemicals are used that act on viral replication by inhibiting it.
- drugs both drugs for oral administration and drugs for topical application, which have shown excellent efficacy in the treatment of viral diseases caused by Herpes Zoster virus.
- aciclovir acycloguanosine
- famciclovir famciclovir
- ribavirin ribavirin
- ganciclovir sorivudine
- Treatments with steroids, interferons, etc. have also been developed.
- Aciclovir was the first antiviral drug for systemic application that needs to be triphosphorylated to exert its antiviral activity; its absorption is comprised between 10 and 20%. Treatment with said pharmaceutical product requires from 15 to 30 days of administration. However, it has been observed that the required dose of many of these mentioned products is such as to cause counterproductive and unsatisfactory effects: toxicity problems in vital organs, such as liver and kidneys (reversible nephropathies), gastrointestinal disorders and neuronal cell disorders. The aforementioned toxicity problems are a drawback to health and, therefore, alternative solutions are sought through the use of other antiviral pharmaceutical products that do not harm the human body and act with high efficacy against viruses. Another problem with such antiviral pharmaceuticals is the high price at which they are marketed due to the high costs for their research and large-scale production Therefore, it is necessary to provide an effective composition for the treatment of Herpes Zoster.
- the object of the present invention is therefore to provide a product not having the disadvantages noted above and which therefore allows the obtaining of a natural product with antiviral activity.
- the present invention originates from having identified a pharmacologically active wheat distillate that allows the successful treatment of certain skin diseases and conditions, by increasing the speed of the physiological processes/mechanisms of tissue repair.
- the invention therefore concerns a process for the preparation of a wheat distillate, comprising the steps of: a. heating a mass consisting of wheat grains until a vapor having a temperature in the range from 40°C to 95°C is formed in a closed environment; b. cooling said vapor of step a. in a closed environment, to obtain a wheat distillate; c. collecting said wheat distillate.
- the invention concerns a wheat distillate obtainable from the process comprising the above steps, wherein said distillate comprises furfural as determined by a chromatogram obtained by “Solid Phase Microextraction (SPME)” GC/MS technique performed using a TracelSQ QD Single Quadrupole GC-MS instrument (Thermo Fisher) and a Zebron-5MS plus column (60 m; 0.32 mm; 1 micron).
- SPME Solid Phase Microextraction
- said distillate comprises a percentage of furfural in the range from 3% to 15% determined as a percentage of area measured from a chromatogram obtained by “Solid Phase Microextraction (SPME)” GC/MS technique performed using a TracelSQ QD Single Quadrupole GC-MS instrument (Thermo Fisher) and a Zebron- 5MS plus column (60 m; 0.32 mm; 1 micron).
- SPME Solid Phase Microextraction
- the present invention relates to the medical use of the wheat distillate obtainable from the above described process and comprising furfural, preferably a percentage of furfural in the range from 3% to 15% determined as a percentage of area measured from a chromatogram obtained by Solid Phase Microextraction (SPME) GC/MS technique performed using a TracelSQ QD Single Quadrupole GC-MS instrument (Thermo Fisher) and a Zebron-5MS plus column (60 m; 0.32 mm; 1 micron).
- SPME Solid Phase Microextraction
- the invention concerns the use, in the treatment of a skin disease or condition, of the wheat distillate obtainable from the above described process and comprising furfural, preferably in a percentage in the range from 3% to 15% determined as percentage of area measured from a chromatogram obtained by Solid Phase Microextraction (SPME) GC/MS technique performed using a TracelSQ QD Single Quadrupole GC-MS instrument (Thermo Fisher) and a Zebron-5MS plus column (60 m; 0.32 mm; 1 micron).
- SPME Solid Phase Microextraction
- the wheat distillate is able to effectively treat Flerpes zoster, thus resulting to be an excellent antiviral agent, but without having the contraindications associated with known antivirals.
- the invention therefore concerns a distillation process to obtain a distillate that has demonstrated therapeutic activity against skin affections, in particular affections generated by viral agents.
- the step of heating a mass consisting only of wheat grains to form a vapor having a temperature in the range from 40°C to 95°C, preferably from 45°C to 60°C, in a closed environment is essential to obtain the therapeutic properties of the final distillate.
- the distillate in fact allows to have a characterization of compounds that enable it to treat skin diseases.
- the process provides the distillate with the ability to treat skin conditions, generated in particular by viruses, such as Herpes zoster.
- Figure 1 shows an example of an apparatus for carrying out the process of the invention
- Figure 2 shows a photograph of a container comprising the wheat distillate of the present invention
- Figure 4 (From top) SPME_GC/MS chromatogram of a blank, SPME_GC/MS chromatogram of the sample analyzed in duplicate, as explained in Example 2;
- Figure 5 shows photographs of a patient affected by Herpes Zoster in which the letters (A) and (B) identify, respectively, images of the patient before the treatment and before the blisters have burst, while the letters (C) and (D) identify, respectively, images of the patient after treatment when cicatrization (C) and healing (D) had occurred.
- Figure 6 shows images relating to a patient affected by Herpes Zoster in the leg, in which the letter (A) is the image of the affected part before the treatment and before the blisters have burst, the letter (B) corresponds to the image of the affected part during the treatment after the blisters have burst, while the letter (C) corresponds to the image of the treated part after the application of the distillate of the invention and when the cicatrization and healing had occurred.
- Figure 7 shows images of a patient affected by Herpes Zoster on the breast in which the letter (A) corresponds to the affected part before the treatment and before the blisters have burst, the letter (B) corresponds to the image of the part during the treatment after the blisters have burst, while the letter (C) is the image of the affected part after the treatment, when cicatrization and healing had occurred.
- Figure 8 shows images of a patient affected by Herpes Zoster on the breast in which the letter (A) corresponds to the image of the part before the treatment and before the blisters have burst and the letter (B) identifies the part after the treatment when cicatrization and healing had occurred.
- Figure 9 shows images of a patient affected by from atopic dermatitis on the hand in which the letter (A) corresponds to the image of the part before treatment and the letter (B) corresponds to the image of the part after the treatment when cicatrization and healing had occurred.
- the invention therefore concerns a process for the preparation of a wheat distillate, comprising the steps of: a. heating a mass consisting of wheat grains until a vapor having a temperature in the range from 40°C to 95°C is formed in a closed environment; b. cooling said vapor of step a. in a closed environment, to obtain a wheat distillate; c. collecting said wheat distillate.
- wax when used, it means the common name of the plant of the genus Triticum, also known as grain, and it is intended to include the fruit (grain or caryopsis) of the same plant.
- any wheat grain may be used, whether it comes from standard or organic agriculture.
- the process of the invention provides for a first step of heating a mass consisting only of wheat grains until a vapor having a temperature in the range from 40°C to 95°C is formed in a closed environment.
- the temperature of the vapor formed by heating the mass is in the range from 45°C to 60°C.
- a vapor having a temperature in the range from 40°C to 95°C when “heating until a vapor having a temperature in the range from 40°C to 95°C is formed” is used, it means the application of heat to the mass of wheat grains such as to determine an initial toasting and eventually burning the wheat grain.
- the wheat grain thus treated therefore generates a vapor which in a closed environment has a temperature from 40°C to 95°C, preferably from 45°C to 60°C, as measured by means of a thermometer placed in the closed environment in contact with the same vapors.
- said temperature of the vapor generated by heating the mass of wheat grains of step a. is in the range from 45°C to 60°C, more preferably from 45°C to 50°C, even more preferably said temperature of step a. is a temperature of about 48°C.
- Said heating step takes place in a closed environment.
- the heating step can take place for different lengths of time, depending on the amount of mass to be heated, and it is essential that the vapors generated by heating the wheat grains are at a temperature between 40°C and 95°C. For example, for 100 g of wheat grains, heating took place for a period of time from 10 minutes to 1 hour.
- the inventors believe that the step of heating a mass consisting only of wheat grains until a vapor having a temperature in the range from 40°C to 95°C, preferably from 45°C to 60°C, is formed in a closed environment is essential in order to obtain the therapeutic properties of the final distillate.
- the step b. of the process of the invention consists in cooling the vapors generated by the heating step, still in a closed environment. Preferably the vapors generated by heating are conveyed to a cooling area, where they are cooled and then conveyed to the part of recovering the final distillate obtained.
- steps a. and b. of the process of the invention are carried out with a distillation apparatus, such as for example the apparatus shown in Figure 1.
- step c. of the process of the invention consists in collecting the distillate obtained after cooling the vapor of step b.
- the invention concerns a wheat distillate obtainable from the process comprising the steps of: a. heating a mass consisting of wheat grains until a vapor having a temperature in the range from 40°C to 95°C is formed in a closed environment; b. cooling said vapor of step a. in a closed environment, to obtain a wheat distillate; c. collecting said wheat distillate.
- said distillate comprises furfural as determined by Solid Phase Microextraction (SPME) GC/MS technique performed using a TracelSQ QD Single Quadrupole GC-MS (Thermo Fisher) instrument and a Zebron-5MS plus column (60 m; 0.32 mm; 1 micron).
- the distillate of the invention has an appearance of an oily-looking liquid. It preferably has a very dense consistency, a black-yellow color, and is characterized, more preferably, by a strong smell of burnt bread.
- the distillate of the invention comprises a percentage of furfural in the range from 3% to 15% determined as a percentage of area measured from a chromatogram obtained by Solid Phase Microextraction (SPME) GC/MS technique performed using a TracelSQ QD Single Quadrupole GC-MS instrument (Thermo Fisher) and a Zebron-5MS plus column (60 m; 0.32 mm; 1 micron).
- SPME Solid Phase Microextraction
- the wheat distillate was further characterized and it was found that, in addition to comprising a percentage of furfural in the range from 3% to 15% (determined as a percentage of area measured from a chromatogram obtained by Solid Phase Microextraction (SPME) GC/MS technique performed using a TracelSQ QD Single Quadrupole GC-MS instrument (Thermo Fisher) and a Zebron-5MS plus column (60 m; 0.32 mm; 1 micron) , it preferably comprises further analytes selected from a group comprising: volatile organic compounds deriving from dehydrated natural products, and most of these are furfural derivatives.
- SPME Solid Phase Microextraction
- furfural derivatives are present in the following percentages (determined as a percentage of area measured from a chromatogram obtained by “Solid Phase Microextraction (SPME)” GC/MS technique performed using the instrument):
- volatile organic compounds the following compounds are present, more preferably in the following percentages (determined as a percentage of area measured from a chromatogram obtained by means of the “Solid Phase Microextraction (SPME)” GC/MS technique performed using the instrument):
- the distillate of the present invention may be added with one or more preservatives and/or one or more pharmacologically acceptable excipients, in the form of a composition.
- the present invention relates to the wheat distillate obtainable from the process described above for use as a medicament.
- the distillate for use as a medicament according to the invention is administered topically.
- the wheat distillate or the composition comprising the wheat distillate according to the present invention is then formulated in the form of an oil, ointment, paste, cream, or gel.
- the invention concerns the distillate of the invention for use in the treatment of a skin disease or condition.
- Said skin disease or condition according to the invention is advantageously Herpes Zoster.
- the distillate of the invention also has a marked efficacy in the treatment of other skin diseases.
- said skin disease or condition is preferably selected from the group consisting of Herpes simplex, Herpes zoster, burn, atopic dermatitis, simple dermatitis and sore. More preferably said skin disease or condition is selected from the group consisting of Herpes zoster or atopic dermatitis.
- the wheat distillate is able to effectively treat Herpes zoster, thus making it an excellent antiviral agent, but without having the contraindications associated with known antivirals.
- Herpes Zoster is caused by the Varicella-Zoster virus which causes a painful rash also known as shingles. It is the same virus that causes chickenpox which has the particularity of remaining inactive in the nervous tissue, reactivating years later with the very painful manifestations of Herpes Zoster.
- Symptoms of Herpes Zoster (HZ) infection include: an elongated, erythematous, area of skin covered by vesicles such as those chickenpox, burning or stabbing pain, fever, itching, headache, chills, stomach pain, and fatigue.
- Herpes zoster varies from 1 .2 to 3.4 cases per 1000 healthy individuals, increasing to 3.9-11 .8 per year per 1000 people among individuals over the age of 65. The peak occurs in subjects aged 75-79. As the elderly and frail population increases, an increase in HZ cases is expected in the near future. On average, about one in four people develop HZ over the course of their life and the disease affects about half of those living up to 85 years.
- the objectives of treating Herpes zoster with the wheat distillate of the present invention are focused on limiting the intensity of pain, reducing the duration of the episode, and avoiding complications with analgesic, antiviral products. Therefore, the distillate of the invention behaves like a real antiviral without having the side effects generally associated with said therapeutic category.
- the area affected by the disease can advantageously be pre-treated by bursting the vesicles typical of the disease itself. Subsequently, the pre-treated area can be cleaned and then treated with the distillate of the invention.
- the pre-treated and cleaned area therefore generally looks like an open sore that allows the distillate of the invention to convey through the blood.
- the distillate of the invention may be applied several times until complete healing.
- the inventors found that a scab was already forming, which advantageously was not to be removed until it fell naturally following cicatrization. Before subsequent applications, according to the invention, it was advantageous to control the onset of further new vesicles and evaluate the possible formation of pus on the area already treated with the previous application. The number of applications varies from case to case. In mild cases, the inventors found that even just two applications were enough. Generally, in the most severe cases of Herpes Zoster, the application of the distillate of the invention did not exceed a week. Advantageously, during the treatment with the distillate of the invention, the treated part was not cleaned.
- the distillate may also be applied without removing the vesicles, but this involved slower absorption through the skin.
- the distillate of the present invention ensured healing of Herpes Zoster According to the invention, the distillate is also suitable for use in the advantageously resolving treatment of all types of Herpes, pressure sores, burns and atopic dermatitis.
- the inventors in fact, realized that no traces of the disease were left following the treatment with the wheat distillate as described above, and the skin regenerated without any marks.
- the wheat distillate was obtained by extracting the substances (essential oils) by dry distilling the wheat as detailed below.
- a distillation apparatus was employed. Wheat grains were loaded into the tailed flask (specifically 50 grams of organic wheat), and the flask was heated for about 15 minutes, generating vapors from the wheat grains which had a temperature of about 48°C. In fact, due to the heat developed in the flask, a vapor having a temperature of about 48°C, which contained volatile substances, was generated. Said vapor was then conveyed to a refrigerant tube, where it was cooled and condensed inside. The volatile substances were then liquefied in the form of an oily distillate.
- This oily distillate is the wheat distillate of the present invention. It had a very dense consistency, was black-yellow in color and characterized by the strong smell of burnt bread (Figure2).
- Example 2 The wheat distillate obtained in Example 1 (sample) was analyzed and then characterized by GC/MS, GC/MS with headspace technique, with solid phase microextraction (SPME) and LC/MS.
- SPME solid phase microextraction
- the aqueous fractions were combined and analyzed by LC/MS technique.
- Sample preparation for SPME_GC/MS analysis 1.5 mL of sample and 4.5 mL of a NaCI saturated aqueous solution were loaded into a 20 mL headspace vial.
- This sample was analyzed using the SPME_GC/MS technique.
- GC/MS analyzes were performed using a TracelSQ QD Single Quadrupole GC-MS instrument (Thermo Fisher) and a Zebron-5MS plus column (60 m; 0.32 mm; 1 micron).
- LC/MS analyzes were carried out using a Thermo Fisher LCQ Fleet ion trap mass spectrometer interfaced with an UltiMateTM 3000 UPLC system containing a UV-vis detector.
- Results Figure 3 shows the GC/MS chromatograms obtained for the 2 extracts in ethyl acetate and that of a blank (ethyl acetate)
- Table 1 To verify also the analytes present in the volatile organic compounds (VOCs), the sample was also analyzed using the SPME_GC/MS technique.
- Figure 4 shows the chromatogram of the sample analyzed in duplicate (sample and second sample) and a blank reference (4.5 ml_ of NaCI saturated aqueous solution).
- the SPME_GC/MS chromatograms of the two sample aliquots were practically identical, ensuring the reproducibility of the analysis method.
- Table 2 shows the retention times of the peaks of the analytes contained and their recognition by matching with NIST2014 library.
- Table 2 retention times of the chromatogram related to the sample analyzed by SPME_GC/MS technique ( Figure 4) and identification of the peaks by matching with NIST2014 library.
- the analyses performed on the sample showed the presence of different types of analytes ranging from VOCs (volatile organic compounds) to products deriving from dehydrated natural products, most of these were furfural derivatives.
- VOCs volatile organic compounds
- the identification of the analytes determined by GC/MS technique was obtained by matching with NIST2014 library, reporting the first match (the most likely). Most of these were furfural derivatives.
- the wheat distillate comprised the furfural compound, preferably in a range from 3% to 15% determined as a percentage of area measured from a chromatogram obtained using Solid Phase Microextraction (SPME) “GC/MS technique performed using a TracelSQ QD Single Quadrupole GC-MS instrument (Thermo Fisher) and a Zebron-5MS plus column (60 m; 0.32 mm; 1 micron).
- SPME Solid Phase Microextraction
- Furfural derivatives were present in the following percentages (determined as a percentage of area measured from a chromatogram obtained using “Solid Phase Microextraction (SPME)” GC/MS technique performed using the instrument):
- Example 3 Evaluation of the therapeutic activity of the distillate of the invention: treatment of Flerpes Zoster
- the area affected by the disease was preventively treated by bursting the vesicles and, once cleaned, it appeared as an open sore.
- This pre treatment allowed the distillate to be conveyed through the blood.
- a scab was already formed which was not removed until its natural fall following cicatrization.
- a check was carried out in relation to formation of new vesicles and possible formation of pus.
- the distillate was then applied to the patients and the number of applications varied according to the disease severity. In this specific case, the patients were treated for 4-5 days with only one application per day.
- Figure 5 shows the images of the first patient affected by Herpes Zoster in the chest area, in which two photographs before the treatment (A and B) and two after the treatment (C and D) can be seen.
- Figure 6 shows three images of the second patient with Herpes Zoster in the leg. It is apparent that the treatment with the distillate of the invention has led to an improvement since in Figure A the vesicles are reddish and swollen, while after the topical application of the distillate (Figure 6B) the vesicles have become scabs in the healing phase ( Figure 6C).
- Figures 7 and 8 show the last two patients with Herpes Zoster in the breast and chest areas, in which the effect of the treatment with the distillate can be seen.
- Figure 7B a certain extension of reddish and swollen vesicles can be seen;
- Figure 7B the distillate of the invention has been topically applied to the vesicles covering them completely.
- Figure 7C the vesicles have all become scabs which have subsequently fallen off following complete healing.
- Example 4 Evaluation of the therapeutic activity of the distillate of the invention: treatment of cold sores
- the distillate of the invention obtained with the procedure described in Example 1 was used to treat the part affected by cold sores.
- Example 5 Evaluation of the therapeutic activity of the distillate of the invention: treatment of atopic dermatitis
- the distillate of the invention, obtained with the procedure described in Example 1 was used to treat the affected part of a patient suffering from atopic hand dermatitis.
- the area affected by atopic dermatitis was treated for a period of 7 days with one application per day.
- Figure 9 shows photographs of the patient's hand before and after treatment.
- Example 6 Evaluation of the therapeutic activity of the distillate of the invention: treatment of pressure sores
- the distillate of the invention obtained with the procedure described in Example 1 was used to treat a patient suffering from pressure sores on the buttocks. Specifically, the patient had large sores on the buttocks that healed after 5 days of daily treatment with the product of the invention.
- the distillate of the invention obtained with the procedure described in Example 1 was used to treat a patient with a burned wrist and hand.
- the patient showed a clear improvement even after the first applications of the distillate of the invention with a reduction in the affected area and a clear decrease in pain associated with the burn.
- this procedure has shown to be surprisingly and advantageously suitable for the preparation of a wheat distillate with surprising pharmacological activity for the treatment of skin diseases, such as Herpes zoster, atopic dermatitis, pressure sores, cold sores and burns.
- skin diseases such as Herpes zoster, atopic dermatitis, pressure sores, cold sores and burns.
- this method being fast and extremely easy to perform, can be conveniently carried out in any type of laboratory at low costs.
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Abstract
The invention concerns a process for the preparation of a wheat distillate, the wheat distillate obtainable from this process, and uses thereof in the treatment of skin diseases and conditions, preferably Herpes zoster.
Description
DISTILLATE FOR THE TREATMENT OF A SKIN CONDITION OR DISEASES
DESCRIPTION
FIELD OF THE INVENTION The invention concerns a process for the preparation of a wheat distillate, a wheat distillate obtainable from this process and uses thereof in the treatment of skin diseases and conditions. In a preferred and advantageous aspect, the invention concerns a wheat distillate for use in the treatment of Herpes Zoster.
STATE OF THE ART Herpes zoster is one of the skin diseases caused by the reactivation of the varicella- zoster virus (VZV). This reactivation occurs more frequently in the elderly or in immunosuppressed people. VZV is part of the Herpes virus family and is the etiological agent of childhood varicella, after which the virus remains in a latent state in the adjacent dorsal root ganglia. In conditions of immunosuppression, emotional stress, neoplasia, etc., as an elderly adult, the virus reactivates and causes vesicular lesions on the skin, preceded by itching, pain or a feeling of hyperesthesia, which form erythematous patches. These lesions are found mainly in the cephalic, cervical and trunk regions. Among the most frequent complications, post-herpetic neuralgia, ocular bacterial overinfection, which can be chronic and cause ophthalmic nerve disorders, and visceral disseminations in immunosuppressed patients, stand out.
A feature of viruses is that they are not likely to be eliminated by treatment with antibiotics. As a result, chemicals are used that act on viral replication by inhibiting it. However, there is still no 100% effective composition as an antiviral treatment. At the state of the art there are drugs, both drugs for oral administration and drugs for topical application, which have shown excellent efficacy in the treatment of viral diseases caused by Herpes Zoster virus. Among these drugs are aciclovir (acycloguanosine), famciclovir, ribavirin, ganciclovir, sorivudine, etc. Treatments with steroids, interferons, etc., have also been developed. Aciclovir was the first antiviral drug for systemic application that needs to be triphosphorylated to exert its antiviral activity; its absorption is comprised between 10 and 20%. Treatment with said pharmaceutical product requires from 15 to 30
days of administration. However, it has been observed that the required dose of many of these mentioned products is such as to cause counterproductive and unsatisfactory effects: toxicity problems in vital organs, such as liver and kidneys (reversible nephropathies), gastrointestinal disorders and neuronal cell disorders. The aforementioned toxicity problems are a drawback to health and, therefore, alternative solutions are sought through the use of other antiviral pharmaceutical products that do not harm the human body and act with high efficacy against viruses. Another problem with such antiviral pharmaceuticals is the high price at which they are marketed due to the high costs for their research and large-scale production Therefore, it is necessary to provide an effective composition for the treatment of Herpes Zoster.
The particular complication that characterizes these viruses, together with the difficulties in reaching an effective cure not having unwanted side effects, are at the basis of the need to provide new effective treatments that prevent the toxicity problems shown by the known compositions and at the same time can be prepared in a convenient way.
Products obtained by solvent extraction of plant parts are known, which are complicated and affected by the use of organic solvents or other liquids, which can be toxic, completely denaturing the initial plant part. The object of the present invention is therefore to provide a product not having the disadvantages noted above and which therefore allows the obtaining of a natural product with antiviral activity.
SUMMARY OF THE INVENTION
The present invention originates from having identified a pharmacologically active wheat distillate that allows the successful treatment of certain skin diseases and conditions, by increasing the speed of the physiological processes/mechanisms of tissue repair.
Surprisingly, the inventors have in fact discovered that starting from a mass consisting only of wheat grains, a distillate could be obtained by means of an appropriate distillation process and that said distillate had curative properties against some skin diseases.
In a first aspect, the invention therefore concerns a process for the preparation of a
wheat distillate, comprising the steps of: a. heating a mass consisting of wheat grains until a vapor having a temperature in the range from 40°C to 95°C is formed in a closed environment; b. cooling said vapor of step a. in a closed environment, to obtain a wheat distillate; c. collecting said wheat distillate.
In a second aspect, the invention concerns a wheat distillate obtainable from the process comprising the above steps, wherein said distillate comprises furfural as determined by a chromatogram obtained by “Solid Phase Microextraction (SPME)” GC/MS technique performed using a TracelSQ QD Single Quadrupole GC-MS instrument (Thermo Fisher) and a Zebron-5MS plus column (60 m; 0.32 mm; 1 micron).
Preferably, said distillate comprises a percentage of furfural in the range from 3% to 15% determined as a percentage of area measured from a chromatogram obtained by “Solid Phase Microextraction (SPME)” GC/MS technique performed using a TracelSQ QD Single Quadrupole GC-MS instrument (Thermo Fisher) and a Zebron- 5MS plus column (60 m; 0.32 mm; 1 micron).
In a third aspect, the present invention relates to the medical use of the wheat distillate obtainable from the above described process and comprising furfural, preferably a percentage of furfural in the range from 3% to 15% determined as a percentage of area measured from a chromatogram obtained by Solid Phase Microextraction (SPME) GC/MS technique performed using a TracelSQ QD Single Quadrupole GC-MS instrument (Thermo Fisher) and a Zebron-5MS plus column (60 m; 0.32 mm; 1 micron).
In a fourth aspect, the invention concerns the use, in the treatment of a skin disease or condition, of the wheat distillate obtainable from the above described process and comprising furfural, preferably in a percentage in the range from 3% to 15% determined as percentage of area measured from a chromatogram obtained by Solid Phase Microextraction (SPME) GC/MS technique performed using a TracelSQ QD Single Quadrupole GC-MS instrument (Thermo Fisher) and a Zebron-5MS plus column (60 m; 0.32 mm; 1 micron).
In a particular and advantageous embodiment of the invention, the wheat distillate is able to effectively treat Flerpes zoster, thus resulting to be an excellent antiviral
agent, but without having the contraindications associated with known antivirals. The invention therefore concerns a distillation process to obtain a distillate that has demonstrated therapeutic activity against skin affections, in particular affections generated by viral agents. Without being bound to any theory, the inventors believe that the step of heating a mass consisting only of wheat grains to form a vapor having a temperature in the range from 40°C to 95°C, preferably from 45°C to 60°C, in a closed environment, is essential to obtain the therapeutic properties of the final distillate. The distillate in fact allows to have a characterization of compounds that enable it to treat skin diseases.
Such distillation takes place directly on the solid, that is the wheat grain in the complete absence of any solvent. This characteristic allows to obtain a distillate which is active against skin diseases.
It has in fact been proven that the cold extraction of oils from the same wheat does not provide the product with the same healing properties. In fact, having tried the application of cold pressed wheat germ oil found on the market, it did not show any efficacy.
As will be apparent from the detailed description, the process provides the distillate with the ability to treat skin conditions, generated in particular by viruses, such as Herpes zoster.
DESCRIPTION OF THE FIGURES
The invention will now be described in detail and with reference to the attached Figures in which:
Figure 1 shows an example of an apparatus for carrying out the process of the invention;
Figure 2 shows a photograph of a container comprising the wheat distillate of the present invention;
Figure 3 (From top) GC/MS chromatogram of a blank (ethyl acetate), GC/MS chromatogram of Extract 1, GC/MS chromatogram of Extract 2, as explained in Example 2;
Figure 4 (From top) SPME_GC/MS chromatogram of a blank, SPME_GC/MS chromatogram of the sample analyzed in duplicate, as explained in Example 2;
Figure 5 shows photographs of a patient affected by Herpes Zoster in which the letters (A) and (B) identify, respectively, images of the patient before the treatment and before the blisters have burst, while the letters (C) and (D) identify, respectively, images of the patient after treatment when cicatrization (C) and healing (D) had occurred.
Figure 6 shows images relating to a patient affected by Herpes Zoster in the leg, in which the letter (A) is the image of the affected part before the treatment and before the blisters have burst, the letter (B) corresponds to the image of the affected part during the treatment after the blisters have burst, while the letter (C) corresponds to the image of the treated part after the application of the distillate of the invention and when the cicatrization and healing had occurred.
Figure 7 shows images of a patient affected by Herpes Zoster on the breast in which the letter (A) corresponds to the affected part before the treatment and before the blisters have burst, the letter (B) corresponds to the image of the part during the treatment after the blisters have burst, while the letter (C) is the image of the affected part after the treatment, when cicatrization and healing had occurred.
Figure 8 shows images of a patient affected by Herpes Zoster on the breast in which the letter (A) corresponds to the image of the part before the treatment and before the blisters have burst and the letter (B) identifies the part after the treatment when cicatrization and healing had occurred.
Figure 9 shows images of a patient affected by from atopic dermatitis on the hand in which the letter (A) corresponds to the image of the part before treatment and the letter (B) corresponds to the image of the part after the treatment when cicatrization and healing had occurred.
DETAILED DESCRIPTION OF THE INVENTION
The invention therefore concerns a process for the preparation of a wheat distillate, comprising the steps of: a. heating a mass consisting of wheat grains until a vapor having a temperature in the range from 40°C to 95°C is formed in a closed environment; b. cooling said vapor of step a. in a closed environment, to obtain a wheat distillate; c. collecting said wheat distillate.
In the present invention, when the term: “wheat” is used, it means the common name
of the plant of the genus Triticum, also known as grain, and it is intended to include the fruit (grain or caryopsis) of the same plant.
According to the invention, any wheat grain may be used, whether it comes from standard or organic agriculture.
The process of the invention provides for a first step of heating a mass consisting only of wheat grains until a vapor having a temperature in the range from 40°C to 95°C is formed in a closed environment. In a preferred embodiment, the temperature of the vapor formed by heating the mass is in the range from 45°C to 60°C.
In the present invention, when “heating until a vapor having a temperature in the range from 40°C to 95°C is formed” is used, it means the application of heat to the mass of wheat grains such as to determine an initial toasting and eventually burning the wheat grain. The wheat grain thus treated therefore generates a vapor which in a closed environment has a temperature from 40°C to 95°C, preferably from 45°C to 60°C, as measured by means of a thermometer placed in the closed environment in contact with the same vapors.
In a preferred embodiment, said temperature of the vapor generated by heating the mass of wheat grains of step a. is in the range from 45°C to 60°C, more preferably from 45°C to 50°C, even more preferably said temperature of step a. is a temperature of about 48°C.
Said heating step takes place in a closed environment.
The heating step can take place for different lengths of time, depending on the amount of mass to be heated, and it is essential that the vapors generated by heating the wheat grains are at a temperature between 40°C and 95°C. For example, for 100 g of wheat grains, heating took place for a period of time from 10 minutes to 1 hour.
Without being bound to any theory, the inventors believe that the step of heating a mass consisting only of wheat grains until a vapor having a temperature in the range from 40°C to 95°C, preferably from 45°C to 60°C, is formed in a closed environment is essential in order to obtain the therapeutic properties of the final distillate.
Heating takes place in a closed environment applied to the solid, that is the wheat grain in the complete absence of any solvent. This characteristic allows to obtain a distillate which is active against skin diseases.
It was in fact proved that the cold extraction of oils from the same wheat does not provide the product with the same healing properties. In fact, having tried the application of cold pressed wheat germ oil found on the market, it did not produce any efficacy. The step b. of the process of the invention consists in cooling the vapors generated by the heating step, still in a closed environment. Preferably the vapors generated by heating are conveyed to a cooling area, where they are cooled and then conveyed to the part of recovering the final distillate obtained.
Advantageously, steps a. and b. of the process of the invention, which take place in a closed environment, are carried out with a distillation apparatus, such as for example the apparatus shown in Figure 1.
The step c. of the process of the invention consists in collecting the distillate obtained after cooling the vapor of step b.
In a second aspect, the invention concerns a wheat distillate obtainable from the process comprising the steps of: a. heating a mass consisting of wheat grains until a vapor having a temperature in the range from 40°C to 95°C is formed in a closed environment; b. cooling said vapor of step a. in a closed environment, to obtain a wheat distillate; c. collecting said wheat distillate. wherein said distillate comprises furfural as determined by Solid Phase Microextraction (SPME) GC/MS technique performed using a TracelSQ QD Single Quadrupole GC-MS (Thermo Fisher) instrument and a Zebron-5MS plus column (60 m; 0.32 mm; 1 micron).
The distillate of the invention has an appearance of an oily-looking liquid. It preferably has a very dense consistency, a black-yellow color, and is characterized, more preferably, by a strong smell of burnt bread.
Preferably, the distillate of the invention comprises a percentage of furfural in the range from 3% to 15% determined as a percentage of area measured from a chromatogram obtained by Solid Phase Microextraction (SPME) GC/MS technique performed using a TracelSQ QD Single Quadrupole GC-MS instrument (Thermo Fisher) and a Zebron-5MS plus column (60 m; 0.32 mm; 1 micron).
As will be apparent from the experimental part that follows, the wheat distillate was
further characterized and it was found that, in addition to comprising a percentage of furfural in the range from 3% to 15% (determined as a percentage of area measured from a chromatogram obtained by Solid Phase Microextraction (SPME) GC/MS technique performed using a TracelSQ QD Single Quadrupole GC-MS instrument (Thermo Fisher) and a Zebron-5MS plus column (60 m; 0.32 mm; 1 micron) , it preferably comprises further analytes selected from a group comprising: volatile organic compounds deriving from dehydrated natural products, and most of these are furfural derivatives.
In particular, among furfural derivatives, the following can be mentioned:
- Furfuryl alcohol;
- 2-Acetylfuran;
- Acetyl methylfuran; and
- 2-Furoic acid.
Among volatile organic compounds, the following can be mentioned:
- 2,3-Pentandione;
- 2-Acetyl butanone; and
- Phenol.
In a preferred embodiment, furfural derivatives are present in the following percentages (determined as a percentage of area measured from a chromatogram obtained by “Solid Phase Microextraction (SPME)” GC/MS technique performed using the instrument):
- Furfuril alcohol in the range from 5 to 10%;
- 2-Acetylfuran in the range from 3 to 8%;
- Acetyl methylfuran in the range from 7 to 15%; and
- 2-Furoic acid in the range from 2 to 8%
In a preferred embodiment, among volatile organic compounds, the following compounds are present, more preferably in the following percentages (determined as a percentage of area measured from a chromatogram obtained by means of the “Solid Phase Microextraction (SPME)” GC/MS technique performed using the instrument):
- 2,3-Pentandione in the range from 5 to 12%;
- 2-Acetyl butanone in the range from 5 to 12%; and
- Phenol in the range from 2 to 10%.
In a preferred embodiment, the distillate of the present invention may be added with one or more preservatives and/or one or more pharmacologically acceptable excipients, in the form of a composition.
Therefore, in a third aspect, the present invention relates to the wheat distillate obtainable from the process described above for use as a medicament. Advantageously, the distillate for use as a medicament according to the invention is administered topically.
In a further embodiment, the wheat distillate or the composition comprising the wheat distillate according to the present invention is then formulated in the form of an oil, ointment, paste, cream, or gel.
In a fourth aspect, the invention concerns the distillate of the invention for use in the treatment of a skin disease or condition.
Said skin disease or condition according to the invention is advantageously Herpes Zoster.
It was surprisingly found that, in addition to being effective in the treatment of Herpes Zoster, the distillate of the invention also has a marked efficacy in the treatment of other skin diseases.
Therefore, said skin disease or condition is preferably selected from the group consisting of Herpes simplex, Herpes zoster, burn, atopic dermatitis, simple dermatitis and sore. More preferably said skin disease or condition is selected from the group consisting of Herpes zoster or atopic dermatitis.
In a particular and advantageous form of the invention, the wheat distillate is able to effectively treat Herpes zoster, thus making it an excellent antiviral agent, but without having the contraindications associated with known antivirals.
Herpes Zoster is caused by the Varicella-Zoster virus which causes a painful rash also known as shingles. It is the same virus that causes chickenpox which has the particularity of remaining inactive in the nervous tissue, reactivating years later with the very painful manifestations of Herpes Zoster.
Generally, the immune system produces enough antibodies to block the disease, but the virus can remain dormant in nerve tissue for years or even for a lifetime. The reactivation is thought to be linked to a sudden lowering of the immune defenses.
Symptoms of Herpes Zoster (HZ) infection include: an elongated, erythematous, area of skin covered by vesicles such as those chickenpox, burning or stabbing pain, fever, itching, headache, chills, stomach pain, and fatigue.
There are no preventive measures against HZ infection and shingles, which can reappear also several years later.
Worldwide, the annual incidence rate of Herpes zoster varies from 1 .2 to 3.4 cases per 1000 healthy individuals, increasing to 3.9-11 .8 per year per 1000 people among individuals over the age of 65. The peak occurs in subjects aged 75-79. As the elderly and frail population increases, an increase in HZ cases is expected in the near future. On average, about one in four people develop HZ over the course of their life and the disease affects about half of those living up to 85 years.
In Europe alone, around 2 million cases of Herpes Zoster occur each year.
The objectives of treating Herpes zoster with the wheat distillate of the present invention are focused on limiting the intensity of pain, reducing the duration of the episode, and avoiding complications with analgesic, antiviral products. Therefore, the distillate of the invention behaves like a real antiviral without having the side effects generally associated with said therapeutic category.
The area affected by the disease can advantageously be pre-treated by bursting the vesicles typical of the disease itself. Subsequently, the pre-treated area can be cleaned and then treated with the distillate of the invention. The pre-treated and cleaned area therefore generally looks like an open sore that allows the distillate of the invention to convey through the blood.
Advantageously, the distillate of the invention may be applied several times until complete healing.
After the first application, the inventors found that a scab was already forming, which advantageously was not to be removed until it fell naturally following cicatrization. Before subsequent applications, according to the invention, it was advantageous to control the onset of further new vesicles and evaluate the possible formation of pus on the area already treated with the previous application. The number of applications varies from case to case. In mild cases, the inventors found that even just two applications were enough. Generally, in the most severe cases of Herpes Zoster, the application of the distillate of the invention did not exceed a week.
Advantageously, during the treatment with the distillate of the invention, the treated part was not cleaned.
Should the disease occur in the absence of vesicles filled with pus, and therefore through the formation of dry vesicles, a pre-treatment of said vesicles was advantageous in order to release some droplets of blood before treatment with the distillate of the invention. By doing so, healing times were shortened.
According to the invention, the distillate may also be applied without removing the vesicles, but this involved slower absorption through the skin.
Surprisingly, the distillate of the present invention ensured healing of Herpes Zoster According to the invention, the distillate is also suitable for use in the advantageously resolving treatment of all types of Herpes, pressure sores, burns and atopic dermatitis.
The inventors, in fact, realized that no traces of the disease were left following the treatment with the wheat distillate as described above, and the skin regenerated without any marks.
The distillate of the invention, even in the absence of preservatives, persisted over time and did not lose its effectiveness for up to 6 months of storage in jars. Examples of embodiments of the present invention, provided for illustrative and non limiting purposes of the invention, are given below. EXAMPLES
Example 1 : Preparation of the wheat distillate
The wheat distillate was obtained by extracting the substances (essential oils) by dry distilling the wheat as detailed below.
With reference to FIG. 1 , a distillation apparatus was employed. Wheat grains were loaded into the tailed flask (specifically 50 grams of organic wheat), and the flask was heated for about 15 minutes, generating vapors from the wheat grains which had a temperature of about 48°C. In fact, due to the heat developed in the flask, a vapor having a temperature of about 48°C, which contained volatile substances, was generated. Said vapor was then conveyed to a refrigerant tube, where it was cooled and condensed inside. The volatile substances were then liquefied in the form of an oily distillate.
This oily distillate is the wheat distillate of the present invention. It had a very dense
consistency, was black-yellow in color and characterized by the strong smell of burnt bread (Figure2).
Example 2: Distillate analysis
The wheat distillate obtained in Example 1 (sample) was analyzed and then characterized by GC/MS, GC/MS with headspace technique, with solid phase microextraction (SPME) and LC/MS.
Sample preparation for GC/MS and LC/MS analysis
An aliquot of the sample was extracted with three successive aliquots of ethyl acetate. The organic fractions, appropriately collected, were gently evaporated under a light flow of nitrogen until dryness. The extract was redissolved in 1 mL of ethyl acetate, diluted, and analyzed by GC/MS technique.
The aqueous fractions were combined and analyzed by LC/MS technique.
The procedure was repeated with a second aliquot of the sample.
Sample preparation for SPME_GC/MS analysis 1.5 mL of sample and 4.5 mL of a NaCI saturated aqueous solution were loaded into a 20 mL headspace vial.
This sample was analyzed using the SPME_GC/MS technique.
The procedure was repeated with a second aliquot of the sample.
Analysis technique GC/MS analyzes were performed using a TracelSQ QD Single Quadrupole GC-MS instrument (Thermo Fisher) and a Zebron-5MS plus column (60 m; 0.32 mm; 1 micron).
As regards the solid phase microextraction, a 50/30 mm divinylbenzene/Carboxen/polydimethylsiloxane (DVB/CAR/PDMS) (Supelco) fiber was used.
LC/MS analyzes were carried out using a Thermo Fisher LCQ Fleet ion trap mass spectrometer interfaced with an UltiMate™ 3000 UPLC system containing a UV-vis detector.
Results Figure 3 shows the GC/MS chromatograms obtained for the 2 extracts in ethyl acetate and that of a blank (ethyl acetate)
The GC/MS chromatograms of the two extracts were practically identical, ensuring
reproducibility of the extraction method and analysis.
The relevant peaks of the possible analytes present in the distillate sample were then identified, and the identity of the individual analytes was identified by matching with the retention values contained in the NIST2014 library. Table 1 therefore shows the retention times of the analyte peaks contained in the extract and their recognition by matching with NIST2014 library.
Table 1:
To verify also the analytes present in the volatile organic compounds (VOCs), the sample was also analyzed using the SPME_GC/MS technique. Figure 4 shows the chromatogram of the sample analyzed in duplicate (sample and second sample) and a blank reference (4.5 ml_ of NaCI saturated aqueous solution). The SPME_GC/MS chromatograms of the two sample aliquots were practically identical, ensuring the reproducibility of the analysis method.
Table 2 shows the retention times of the peaks of the analytes contained and their recognition by matching with NIST2014 library.
Table 2: retention times of the chromatogram related to the sample analyzed by SPME_GC/MS technique (Figure 4) and identification of the peaks by matching with NIST2014 library.
As can be seen from Table 2, although some of the analytes found using the SPME_GC/MS technique are the same as those reported in Table 1 , there are many others exclusively present in the volatile portion of the sample. Analytes with lower retention times were found to be very volatile compounds.
Conclusions
The analyses performed on the sample showed the presence of different types of analytes ranging from VOCs (volatile organic compounds) to products deriving from dehydrated natural products, most of these were furfural derivatives. The identification of the analytes determined by GC/MS technique was obtained by matching with NIST2014 library, reporting the first match (the most likely). Most of these were furfural derivatives.
In order to also quantitatively evaluate the presence of analytes in the distillate of the invention, the areas of the peaks in the respective chromatograms were determined. As can be seen, in all tables the values of the % areas are reported, but a total sum equal to 100% cannot be obtained as many low intensity signals are not reported as they are not very characteristic. These percentages correspond to the percentages of area determined with the instrument used in the analysis and therefore dependent on its analytical sensitivity. As can be seen from Tables 1 and 2, the wheat distillate comprised the furfural compound, preferably in a range from 3% to 15% determined as a percentage of area measured from a chromatogram obtained using Solid Phase Microextraction (SPME) “GC/MS technique performed using a TracelSQ QD Single Quadrupole GC-MS instrument (Thermo Fisher) and a Zebron-5MS plus column (60 m; 0.32 mm; 1 micron).
It preferably comprised further analytes selected from the group comprising: volatile organic compounds and dehydrated natural products, and most of these were furfural derivatives.
In particular, among furfural derivatives, the following were highlighted as characteristic peaks:
- Furfuryl alcohol;
- 2-Acetylfuran;
- Acetyl methylfuran; and
- 2-Furoic acid.
Among volatile organic compounds, the following were highlighted as characteristic peaks: - 2,3-Pentandione;
- 2-Acetyl butanone; and
- Phenol.
Furfural derivatives were present in the following percentages (determined as a percentage of area measured from a chromatogram obtained using “Solid Phase Microextraction (SPME)” GC/MS technique performed using the instrument):
- Furfuryl alcohol in the range from 5 to 10%;
- 2-Acetylfuran in the range from 3 to 8%;
- Acetyl methylfuran in the range from 7 to 15%; and
- 2-Furoic acid in the range from 2 to 8% Among volatile organic compounds, the following compounds were detected in the following percentages (determined as a percentage of area measured from a chromatogram obtained using “Solid Phase Microextraction (SPME)” GC/MS technique performed using the instrument):
- 2,3-Pentandione in the range from 5 to 12%; - 2-Acetyl butanone in the range from 5 to 12%; and
- Phenol in the range from 2 to 10%.
The following Examples 3-7 will describe the results obtained using the distillate of the invention on patients with different skin diseases and conditions. All patients gave their consent to the use of information and photographic images. Example 3: Evaluation of the therapeutic activity of the distillate of the invention: treatment of Flerpes Zoster
Four patients affected by Flerpes Zoster were treated with the distillate of the invention.
Four patients, two men (aged 70 and 65 years) affected by Flerpes Zoster in the chest area and leg, respectively, and two women (aged 55 and 45 years), affected by Flerpes Zoster on the breast and in the chest area, respectively, were treated. Specifically, the distillate obtained as described in Example 1, did not undergo any
filtration, purification, or dilution treatments.
Advantageously, the area affected by the disease was preventively treated by bursting the vesicles and, once cleaned, it appeared as an open sore. This pre treatment allowed the distillate to be conveyed through the blood. After the first application, a scab was already formed which was not removed until its natural fall following cicatrization. In the following sessions, a check was carried out in relation to formation of new vesicles and possible formation of pus.
The distillate was then applied to the patients and the number of applications varied according to the disease severity. In this specific case, the patients were treated for 4-5 days with only one application per day.
Upon application, the patient immediately felt a strong burning sensation (shingles) which lasted for a few seconds and was followed by a feeling of well-being. In fact, since the first treatment, the patient already reported a significant benefit.
Following treatment with the distillate according to the present invention, all patients suffering from Herpes Zoster were healed and the onset of the disease never occurred.
Figure 5 shows the images of the first patient affected by Herpes Zoster in the chest area, in which two photographs before the treatment (A and B) and two after the treatment (C and D) can be seen.
As can be seen, the large and reddish vesicles became scabs thus indicating the beginning of the healing process.
Figure 6 shows three images of the second patient with Herpes Zoster in the leg. It is apparent that the treatment with the distillate of the invention has led to an improvement since in Figure A the vesicles are reddish and swollen, while after the topical application of the distillate (Figure 6B) the vesicles have become scabs in the healing phase (Figure 6C).
Figures 7 and 8 show the last two patients with Herpes Zoster in the breast and chest areas, in which the effect of the treatment with the distillate can be seen. Referring to Figure 7, in part A a certain extension of reddish and swollen vesicles can be seen; in Figure 7B the distillate of the invention has been topically applied to the vesicles covering them completely. In Figure 7C the vesicles have all become scabs which have subsequently fallen off following complete healing.
In Figure 8 the healing process is even more apparent since the reddish and swollen vesicles of Figure 8A become scabs in some parts of the breast or thorax and only a few reddish spots in other parts, resulting in a decrease in the extension of the disease thus confirming the healing in place.
Example 4: Evaluation of the therapeutic activity of the distillate of the invention: treatment of cold sores
The distillate of the invention, obtained with the procedure described in Example 1 was used to treat the part affected by cold sores.
The area where herpes had occurred was treated by directly applying the distillate, as obtained from Example 1 once a day for 3-4 days, without any special pre treatments. The cold sores disappeared quickly without subsequent treatments. Example 5: Evaluation of the therapeutic activity of the distillate of the invention: treatment of atopic dermatitis The distillate of the invention, obtained with the procedure described in Example 1 was used to treat the affected part of a patient suffering from atopic hand dermatitis. The area affected by atopic dermatitis was treated for a period of 7 days with one application per day.
Figure 9 shows photographs of the patient's hand before and after treatment.
As can be seen from Figure 9A, the dermatitis appeared as a large, open and painful vesicle on the hand. In Figure 9B, obtained after treatment with the distillate, the vesicle was already transformed into a scab in the healing phase that no longer produced any pain to the patient.
Example 6: Evaluation of the therapeutic activity of the distillate of the invention: treatment of pressure sores The distillate of the invention, obtained with the procedure described in Example 1 was used to treat a patient suffering from pressure sores on the buttocks. Specifically, the patient had large sores on the buttocks that healed after 5 days of daily treatment with the product of the invention.
Example 7: Treatment of burns
The distillate of the invention, obtained with the procedure described in Example 1 was used to treat a patient with a burned wrist and hand.
Specifically, the patient showed a clear improvement even after the first applications
of the distillate of the invention with a reduction in the affected area and a clear decrease in pain associated with the burn.
From the detailed description and the Examples reported above, the advantages achieved by the process of the present invention are apparent. In particular, this procedure has shown to be surprisingly and advantageously suitable for the preparation of a wheat distillate with surprising pharmacological activity for the treatment of skin diseases, such as Herpes zoster, atopic dermatitis, pressure sores, cold sores and burns. At the same time, this method, being fast and extremely easy to perform, can be conveniently carried out in any type of laboratory at low costs.
Claims
1. A process for the preparation of a wheat distillate, comprising the steps of: a. heating a mass consisting of wheat grains until a vapor having a temperature in the range from 40°C to 95°C is formed in a closed environment; b. cooling said vapor of step a. in a closed environment, to obtain a wheat distillate; c. collecting said wheat distillate.
2. The process according to claim 1, wherein said process takes place in the complete absence of solvents.
3. The process according to claim 1 or 2, wherein said mass is heated to form a vapor having a temperature in the range from 45°C to 60°C, preferably from 45°C to 50°C, more preferably of about 48°C.
4. The process according to any one of claims 1 to 3, wherein the steps a. and b. in a closed environment take place in a distillation apparatus.
5. A wheat distillate obtainable by the process according to any one of claims 1 to 4, wherein said distillate comprises furfural as determined by “Solid Phase
Microextraction (SPME)” GC/MS technique, performed using a TracelSQ QD Single Quadrupole GC-MS (Thermo Fisher) instrument and a Zebron-5MS plus column (60 m; 0.32 mm; 1 micron).
6. The wheat distillate according to claim 5, wherein said distillate comprises a percentage of furfural in the range from 3% to 15%, determined as a percentage of area measured from a chromatogram obtained by “Solid Phase Microextraction (SPME)” GC/MS technique, performed using a TracelSQ QD Single Quadrupole GC-MS (Thermo Fisher) instrument and a Zebron-5MS plus column (60 m; 0.32 mm; 1 micron).
7. The distillate according to claim 5 or claim 6, wherein said distillate comprises analytes selected from a group consisting of furfuryl alcohol; 2-acetylfuran; acetyl methylfuran; 2-furoic acid, 2,3-pentanedione; 2-acetyl butanone; and phenol, as determined by “Solid Phase Microextraction (SPME)” GC/MS technique performed using a TracelSQ QD Single Quadrupole GC-MS (Thermo Fisher) instrument and a Zebron-5MS plus column (60 m; 0.32 mm; 1 micron).
8. The wheat distillate according to any one of claims 5 to 7, for use as a medicament.
9. The wheat distillate for use according to claim 8, in the form of oil, ointment, paste, cream or gel.
10. The wheat distillate for use according to claim 8 or 9, wherein said distillate is administered topically.
11. A wheat distillate according to any one of claims 5 to 8, for use in the treatment of a skin disease or condition.
12. The distillate for use according to claim 11, wherein said skin disease or condition is selected from the group consisting of Herpes simplex, Herpes zoster, burn, atopic dermatitis, simple dermatitis, and sore 13. The distillate for use according to claim 12, wherein said skin disease or condition is Herpes zoster.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT102021000012332A IT202100012332A1 (en) | 2021-05-13 | 2021-05-13 | DISTILLATE FOR THE TREATMENT OF A SKIN CONDITION OR DISEASE |
| IT102021000012332 | 2021-05-13 |
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| WO2022238969A1 true WO2022238969A1 (en) | 2022-11-17 |
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| WO (1) | WO2022238969A1 (en) |
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