WO2019030772A1 - Formulation à base d'huile pour la prise en charge d'une guérison/douleur - Google Patents
Formulation à base d'huile pour la prise en charge d'une guérison/douleur Download PDFInfo
- Publication number
- WO2019030772A1 WO2019030772A1 PCT/IN2018/050515 IN2018050515W WO2019030772A1 WO 2019030772 A1 WO2019030772 A1 WO 2019030772A1 IN 2018050515 W IN2018050515 W IN 2018050515W WO 2019030772 A1 WO2019030772 A1 WO 2019030772A1
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- WIPO (PCT)
- Prior art keywords
- vitamin
- oil
- pain
- injuries
- formulation
- Prior art date
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/08—Anti-ageing preparations
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/67—Vitamins
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/67—Vitamins
- A61K8/671—Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/67—Vitamins
- A61K8/678—Tocopherol, i.e. vitamin E
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
- A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
- A61K8/925—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of animal origin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/007—Preparations for dry skin
Definitions
- the present invention relates to an oil based formulation for rapid tissue healing progressing to cure and resulting in rapid and lasting pain relief in musculoskeletal injuries and disease, cough and sore throat. More particularly, this invention relates to a composition/formulation comprising of vitamin D derivatives/analogues, vitamin E, vitamin A and vitamin K dissolved in a mixture of suitable oils, ethanol/propanol and pharmaceutically acceptable excipients and carriers. The invention also provides various formulations and methods of preparing the same.
- Pain results from age, nutritional deficiencies, wear & tear and injury. Pain is generally classified by multiple types and includes, but is not limited to: acute pain and chronic pain caused by damage to tissue such as bone, muscle, or organs. The onset of pain is often accompanied by anxiety or emotional distress and follows damaged tissue/nerve damage.
- Nociceptive pain is caused by noxious stimulation of nociceptors (e.g., a needle stick or skin pinch), which then transmit impulses over intact neural pathways to the spinal neurons and then to the brain.
- Neuropathic pain is caused by damage to neural structures, such as damage to peripheral nerve endings or nociceptors, which become extremely sensitive to stimulation and can generate impulses in the absence of stimulation.
- Oral/subcutaneous ways for pain relievers are typically prescribed for treatment of acute and chronic pain, including arthritic pain, musculoskeletal pain and neuropathic pain.
- Oral medicines presently in use may have various side effects including suitability, compatibility to patients, allergies, liver damage and also the amount of drug to be reached at the affected area through systemic circulation for efficacy of the drug and acts for few hours and require frequent repeat doses.
- compositions such as creams, gels, liniments, ointments, balm, lotion, emulsion, suspension, transdermal patch, dermal patch, liquid solution, powder and the like are useful in topical application for pain management.
- Compositions that readily coat the skin and at the same time provide effective adhesion to the skin surface are preferred.
- Oral or subcutaneous vitamin D is quite effective in disease and resultant pain associated with vitamin D deficiencies, but it takes longer to heal and provide relief or remove pain and may take months. This route does not provide immediate relief especially in joint disease, spinal disease, skin conditions related to vitamin D deficiencies and wounds. Surprisingly the topical/local vitamin D application provides immediate and lasting relief in all indicated conditions.
- Vitamin D is a steroid hormone that plays a vital role in calcium and phosphate absorption and tissue healing. It participates in and influences many biological reactions in body directly or indirectly. In recent studies, several associations between low levels of vitamin D and neuropsychiatric disorders have begun to surface. These disorders include, but are not limited to: Alzheimer's disease, Parkinson's disease, multiple sclerosis, epilepsy, schizophrenia, and autism and many more.
- Vitamin D includes Vitamin D-2 (ergocalciferol) and Vitamin D-3 (cholecalciferol). Vitamin D-3 is produced in human skin when it is exposed to ultraviolet B radiation present in sunlight. Vitamin D is known to regulate calcium and phosphorus levels in the blood. Vitamin D contributes to bone growth by helping bones with calcium supplies from food. Lack of adequate Vitamin D can result in bone softening diseases, including rickets and osteomalacia. Even in the absence of osteomalacia, persons with inadequate vitamin D intake may experience osteoporosis, also associated with joint pain, loss of bone density, increased bone fragility and muscular weakness. Vitamin D, in adequate quantities, is also believed to exhibit anti-tumor activity and prevents diabetes. As D-3 is produced in the skin, it can regulate skin cell proliferation and nourishes organs through which it passes on its journey to blood stream.
- Vitamin D-3 is produced in the skin, it can regulate skin cell proliferation and nourishes organs through which it passes on its journey to blood stream.
- Vitamin D-3 synthesis is of high importance for the prevention of a broad variety of diseases, including various deficiencies and malignancies.
- Vitamin D-3 is produced in the epidermal skin layer during sun exposure by conversion of 7 -dch yd roch o lc sterol .
- 7- Dehydrocholesterol a cholesterol-like molecule present in the skin, is the precursor of Vitamin D-3 and forms cholecalciferol after being exposed to sunlight. Cholecalciferol is the inactive, unhydroxylated form of Vitamin D-3.
- Calcidiol Cholecalciferol is thereafter hydro xylated in the liver to become calcidiol (25- hydroxyvitamin D-3). Calcidiol is further hydro xylated in the kidney to become calcitriol (1, 25- dihydroxy vitamin D-3). Calcitriol is the active hormone form of Vitamin D-3. Furthermore, some vitamin D-3 metabolites have themselves been used as chemotherapeutic agents with anti-proliferative effects against several types of cancer including breast, colon, and prostate tumors, leukemia and lymphomas.
- Vitamin D is crucial for musculoskeletal health, maintenance, and function.
- D insufficiency is common among patients undergoing spine surgery. There is a high prevalence of hypo-vitaminosis D in patients with musculoskeletal pain regardless of surgical intervention.
- the components of the present invention act synergistically with acceptable pharmaceutically excipients and such composition/formulations have never been reported for topical applications with greatly enhanced efficacy.
- vitamin D can be applied topically in certain formulations that make the vitamin D bioavailable.
- this formulation is topically applied for spinal disorders, spinal disc compressions, sciatica, cervical spondylitis, damaged tissues due to injuries/ageing/nutritional deficiencies, cartilage damages, degraded/painful joints, injuries, wounds, sprains, penile fracture, thrombophlebitis, cough, sore throat, cracks and skin dryness etc. it provides immediate relief from pain and burning. It immediately results in tissue healing and pain & distress relief in around 15-20 minutes (the time taken for penetration of oil to reach affected area) along with removal of associated weakness.
- This topical application improves skin quality, skin tone, removes cracks, removes skin dryness, improves hair health, hair quality, hair tone and greatly reduces hair loss. It alleviates the need for pain killers, antibiotics and microbicidal. It delivers Vitamin D through topical route and removes vitamin D deficiency.
- an object of the present invention is to provide new synergistic composition(s) comprising a composition or formulation comprising of a vitamin D derivative or analogues, vitamin E. vitamin A and vitamin K dissolved in a mixture of suitable oil, ethanol/propanol and pharmaceutically acceptable excipients and carriers wherein the pharmaceutical composition is useful in the treatment of spinal disorders, spinal disc compressions, damaged tissues due to injuries/ageing/nutritional deficiencies, cartilage damages, degraded/painful joints, injuries, wounds, sprains, penile fracture, thrombophlebitis, boils, acne or abscess, cough, sore throat, cracks and skin dryness etc. and provides immediate relief from pain and burning.
- This topical application improves skin quality, skin tone, removes cracks, removes skin dryness, improves hair health, hair quality, hair tone and greatly reduces hair loss. It alleviates the need for pain killers and/or antibiotics and/or microbicidals. It delivers vitamin D through topical route and removes vitamin D deficiency.
- the present invention is thus based upon the discovery that vitamin D can effectively treat and heal spinal disorders, disc compressions, sciatica, cervical spondylitis, resultant numbness and/or weakness in legs or feet or shoulders or arms or hands, damaged tissues, multiple injuries, wounds, sprains, cartilage damage, damaged or degraded or painful joints, penile fracture, boils, acne, abscess, thrombophlebitis, cough and sore throat, dry skin, cracked skin, hair loss in a short duration by healing damaged tissues due to ageing, deficiencies or injuries when administered topically in a therapeutically effective formulation.
- a therapeutically effective formulation it is meant that the active substance is bioavailable, which is able to exert a biological activity when administered in that formulation. Such formulations effectively exhibit the biological activity of vitamin D in diminishing or completely alleviating the distress involved in such conditions.
- the formulation is also pharmaceutically acceptable for topical application.
- Vitamin D3 or D2 or their derivatives or analogues along with vitamins A, E and K dissolved in ethanol/propanol oils and pharmaceutically accepted excipients are effective in healing, providing cure and pain relief through topical application in injured or degraded tissues/body parts due to age, nutritional deficiencies or diseases, such as Thrombophlebitis, Cervical spondylitis, pain in neck, backache, spine, shoulders, arms, hands, associated numbness and removal of spinal disc compressions.
- Heals acne boils and provides immediate relief from pain, itching and burning. Heals and provides immediate pain relief in cracks. Removes skin dryness, improves skin tone, and heals cracked skin. It also alleviates need for pain killers and/or antibiotics and/or microbicidals.
- Vitamin D is essential in many biological processes and involved in biological reactions directly or indirectly. Vitamin D deficiency causes gap in these processes and healing does not take place effectively and immediately.
- Vitamin D is delivered locally by topical application body's natural healing and defense mechanism is activated locally which also results in immediate pain relief. Since the topical application follows natural route of vitamin D so it provides healing and relief naturally (vitamin D is synthesized in skin upon exposure to ultraviolet rays mainly from sun, gets dissolved in skin oil and is transported to bloodstream. Following this route it nourishes and heals organs through which it passes during its journey to blood stream).
- vitamin D is also included within the scope of this invention and within the meaning of the term vitamin D.
- analogs of vitamin D are well known in the ait and such compounds can have modifications in the side ch ain and/or changes in the nuclear part of the secosteroid molecule.
- Vitamin D analogs can contain side chain modify cations involving introduction of unsaturation; transposing, adding, removing or substituting hydroxyl groups; substituting hydrogens; forming carbocyclic structure; introducing a heteroatom link; inverting stereo chemically; removing or adding a Iky I groups and changing the number of links in the side chain.
- the present invention relates to novel synergistic composition); s ) comprising new synergistic composition); s ) comprising vitamin D, its derivative or analogue, vitamin E, vitamin K and vitamin A and Alcohols.
- topical administration or “topical delivery” means intradermal administration of a pharmaceutical by administration of the pharmaceutical or a composition comprising the pharmaceutical to intact/perforated skin. For instance, applying or rubbing a composition of the present invention onto an area of intact/perforated skin or by placing an intradermal patch comprising a composition of the invention onto an area of intact/perforated skin for desired effect .
- topical composition means a pharmaceutical composition designed for topical administration and containing a pharmaceutical.
- intradermal ly-acceptable means any pharmaceutical, excipient or other component of a topical formulation that is safe, non-irritating or approved for intradermal or topical administration in mammals.
- the present invention relates to novel synergistic composition(s) or formulations comprising a vitamin D derivatives or analogues, vitamin E, vitamin A and vitamin K dissolved in a mixture of suitable oil including medicinal oils, ethanol/propanol and pharmaceutically acceptable excipients and carriers.
- suitable oil including medicinal oils, ethanol/propanol and pharmaceutically acceptable excipients and carriers.
- surfactants include sodium lauryl sulfate, cetostearyl alcohol, ceteareth 12, cet caret h 20, cetearyl alcohol, Cetomacrogol 1000, stearic acid, and poloxamer.
- Suitable penetration enhancers include propylene glycol.
- Suitable preservatives include mcthylparaben. propylparaben, ethylhexylglycerin, phenoxyethanol/propanoL chlorocresol, potassium sorbate, sorbic acid, bronopol, methychloroisothiazolinone, and methylisothiazolinone.
- additives may be included to modify the colour or aroma of the topical compositions described herein.
- the application provides a process for preparing the formulation of the present invention.
- the process comprises weighing individual ingredients and mixing with suitable oil base to obtain a stable solution.
- the solution obtained was kept in closed container and advised to shake well before application.
- composition is prepared by dissolving vitamin D in oil base along with pharmaceutically acceptable excipients.
- Formula 1 An example of formulation comprises Cholecalciferol as 1 gm in 3300 gms (0.03%)
- Formula 2 An example of formulation comprises Cholecalciferol as 1 gm in
- Formula 3 An example of formulation comprises Cholecalciferol as 1 gm in 2500gms (0.04%)
- Formula 4 An example of formulation comprises Cholecalciferol as 1 gm in 330gms (0.3%)
- Formula 5 An example of formulation comprises Cholecalciferol as 1 gm in 100 gms (0.1%)
- Formula 6 An example of formulation comprises Cholecalciferol as 1 gm in 33000 gms (0.003%) Carrier medium / solvent base:
- Oil (Coconut, Sesame, Flax Seed, olive oil, peanut oil, almond oil, soya bean oil, mustard oil. sunflower oil. cod liver oil. medicinal oil or a mixture thereof.)
- Vitamin E 0.1 - 5%
- Vitamin A 0.1 - 5%
- Vitamin K 0.001 - 1 %
- the preferable ratio of vitamin D in oil base is 1: 3000 w/v.
- compositions of vitamin D in oil base are prepared with different ratios, wherein the ratio of vitamin D in oil is 1:2200 w/v, 1:3300 w/v and 1 :2500 w/v, 1:330 w/v, 1 : 100 w/v. 1:33000 w/v
- composition of vitamin D with different oil base are prepared.
- composition comprising :-
- Patient 1 History: N. K. Chaudhary, age-45, Male, Executive with 4 years history of Slip disc in L4. L5 causing back pain.
- Patient 2 History: Geeta, Age-35, female, Office Assistant, Foot sprain with swelling and pain.
- Patient 3 History: William, age-50, Male, Security Guard had sudden back ache followed by severe pain in thighs. Complaining of inability to walk or stand. After one month of his trouble the patient applied the test formulation with vitamin D3 by massaging the oil in spinal area twice a day. The patient got completely relieved in 20 days of his backache and pain in thighs. It is mentioned that patient did not apply test formulation on his thighs and the pain in thighs went away because of spinal disc corrections. And there was no use of any other medication or exercise during period of treatment.
- Patient 4 History: Abhay S harm a. age-50, Male, Govt. Executive with 8 years history of slip disc had various types of treatment except surgery. Used test formulation for one month applied once every third day got 95% improvement and relief. The patient had recently developed knee joint pain and was total relieved of his ailment in one month without use of any other medicine or therapy.
- Patient 5 History: Om Prakash, age-25, Male. Masson met with an accident on his motorcycle was severely injured having deep and long cut near his elbow and large bruised area over his shoulder with blue color and was unable to lift his arm. He was having severe pain. Applied test formulation on second day. In 20 minutes he experienced no pain and was able to lift his arm freely. Oil was applied for three days three times a day. His bruises dried in forty hours and his deep cut healed in three days. No other pain killer, antibiotic or microbicidal was used during period of treatment with test formulation and patient felt no pain during this period.
- Patient 6 History: Ramesh Kumar, age -46. Male, Gardner, got his tow crushed by- concrete stone had severe pain and bleeding. Applied test formulation after 15 minutes of injury the pain stopped in 15 minutes. Test formulation was applied for three days three times a day and the wound completely healed in 3 days. No other pain killer, antibiotic or microbicidal was used during period of treatment with test formulation and patient felt no pain during this period.
- Patient 7 History: Jameela, age-55, Female, Canteen employee, had severe knee pain for last one year, was not able to walk and the life was difficult for her. Her mobility was restricted. Started using test formulation in 1 t week of February 2018, applied it once a daily and she was completely relived of her pain in 15 days. No other medicine and pain killers were used during this period. She applies test formulation around seven times per month and is leading trouble free and pain free life since then.
- the oil used in preparing the formulation is selected from suitable and compatible oil selected from the organic oils, vegetable oils and medicinal oils.
- the specific oils are selected among the oils from but not limited to the Coconut. Sesame, Flax Seed, olive oil. peanut oil, almond oil, soya bean oil, mustard oil, sunflower oil, cod liver oil, medicinal oil or a mixture thereof.
- Vitamin D is synthesized in skin by action of UV (295-315) on 7-dehydrocholestrol and performs autocrine and paracrine functions in skin. Vitamin D in blood nourishes organs and heals the malfunctions/deficiencies in various organs including spine, muscles and other tissues.
- the same natural path is utilized in this innovation of vitamin D oil application to provide similar benefits. Based on the application following the natural path, the formulation is applied topically and it is found to affect cure in the organs beneath area of application and relieves pain as immediately when it reaches the affected tissue normally in 15 to 20 minutes of application.
- the topical pharmaceutical composition may be used in the treatment of backache, spinal disorders, disc compressions and damaged tissue due to ageing, deficiencies or injuries. It corrects spinal disorders, removes pain and heals tissues, and is able to cure sciatica and associated pain & numbness in lower limbs, cervical spondylitis and associated pain and numbness in shoulders, arms or hands, when applied over spine only.
- the topical pharmaceutical composition may be used in the treatment of spinal disorders, disc compressions, sciatica, cervical spondylitis, resultant numbness of associated limbs, boils, acne, dry or cracked skin, wounds, sprains, injuries and joint disease etc.
- the topical formulation is also useful for the conditions wherein cutaneous nerves may be involved.
- the present invention also relates to process of preparation of the compositions or formulations of the present invention.
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- Oil, Petroleum & Natural Gas (AREA)
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Abstract
La présente invention concerne une formulation à base d'huile pour la prise en charge d'une guérison et d'une douleur. Plus particulièrement, la présente invention concerne une composition ou une formulation comprenant un dérivé ou analogue de vitamine D, de la vitamine E, de la vitamine A et de la vitamine K dissous dans un mélange d'huiles appropriées, d'éthanol/propanol et d'excipients et véhicules pharmaceutiquement acceptables. La composition pharmaceutique topique peut être utilisée dans le traitement et la guérison de : troubles rachidiens, compressions de disque vertébral, sciatique et douleur et engourdissement associés, spondylarthrite cervicale et douleur et engourdissement associés, entorse, blessures sportives, lésions multiples, cartilage endommagé entraînant des articulations douloureuses/enflammées, tissus endommagés en raison du vieillissement/de déficiences ou de lésions, douleurs articulaires, faiblesse articulaire, inflammation articulaire, plaies, furoncles, acné, sècheresse cutanée, fissures. La formulation topique est également utile pour les affections dans lesquelles des nerfs cutanés peuvent être atteints. Elle élimine/corrige en outre les déficits en vitamine D.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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IN201711028017 | 2017-08-07 | ||
IN201711028017 | 2017-08-07 |
Publications (1)
Publication Number | Publication Date |
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WO2019030772A1 true WO2019030772A1 (fr) | 2019-02-14 |
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PCT/IN2018/050515 WO2019030772A1 (fr) | 2017-08-07 | 2018-08-07 | Formulation à base d'huile pour la prise en charge d'une guérison/douleur |
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US11497714B2 (en) | 2020-10-06 | 2022-11-15 | Sadat A. Al Ali | Nano-carrier topical composition with vitamin D3 |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4743442A (en) * | 1983-08-02 | 1988-05-10 | Blendax-Werke R. Schneider Gmbh & Co. | Skin care composition |
US20060292080A1 (en) * | 1998-09-11 | 2006-12-28 | Connetics Australia Pty Ltd | Vitamin formulation |
US8821921B2 (en) * | 2009-01-16 | 2014-09-02 | Anzamed International Limited | Vitamin D3 for the transdermal treatment of pain and inflammation |
US8895034B2 (en) * | 2011-11-02 | 2014-11-25 | Mark K Bennett | Collagen production compound |
-
2018
- 2018-08-07 WO PCT/IN2018/050515 patent/WO2019030772A1/fr active Application Filing
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4743442A (en) * | 1983-08-02 | 1988-05-10 | Blendax-Werke R. Schneider Gmbh & Co. | Skin care composition |
US20060292080A1 (en) * | 1998-09-11 | 2006-12-28 | Connetics Australia Pty Ltd | Vitamin formulation |
US8821921B2 (en) * | 2009-01-16 | 2014-09-02 | Anzamed International Limited | Vitamin D3 for the transdermal treatment of pain and inflammation |
US8895034B2 (en) * | 2011-11-02 | 2014-11-25 | Mark K Bennett | Collagen production compound |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US11497714B2 (en) | 2020-10-06 | 2022-11-15 | Sadat A. Al Ali | Nano-carrier topical composition with vitamin D3 |
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