WO2010004355A2 - Nouvelle composition éclaircissante pour la peau à base de plantes, procédés de production de celle-ci et compositions cosméceutiques l’utilisant - Google Patents
Nouvelle composition éclaircissante pour la peau à base de plantes, procédés de production de celle-ci et compositions cosméceutiques l’utilisant Download PDFInfo
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- WO2010004355A2 WO2010004355A2 PCT/IB2008/001793 IB2008001793W WO2010004355A2 WO 2010004355 A2 WO2010004355 A2 WO 2010004355A2 IB 2008001793 W IB2008001793 W IB 2008001793W WO 2010004355 A2 WO2010004355 A2 WO 2010004355A2
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- extract
- composition according
- glycyrrhiza glabra
- composition
- indica
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/0212—Face masks
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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
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
- A61K8/9783—Angiosperms [Magnoliophyta]
- A61K8/9789—Magnoliopsida [dicotyledons]
-
- 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
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
- A61K8/9783—Angiosperms [Magnoliophyta]
- A61K8/9794—Liliopsida [monocotyledons]
-
- 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
- A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
-
- 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
- A61Q19/10—Washing or bathing preparations
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
- A61K2800/28—Rubbing or scrubbing compositions; Peeling or abrasive compositions; Containing exfoliants
Definitions
- This invention in general, relates to a novel herbal skin lightening composition. More specifically, but without restriction to the particular embodiments hereinafter described in accordance with the best mode of practice, this invention provides a herbal composition for skin related disorder. In addition the invention discloses a method of producing the same and cosmeceutical compositions thereof. Background of the Invention
- UV radiation ultraviolet
- UVA radiation is approximately 1000 times more intoxicating than UVB radiation, in causing immediate tanning effect due to increased biosynthesis of melanin in the epidermis.
- Tyrosinase (monophenol, 3, 4-dihydroxyphenylalanine: oxygen oxidoreductase, EC 1.14.18.1), a single-chain glycoprotein rate limiting enzyme essential for pigment formation (melanin synthesis) in mammals, is specifically localized in melanocytes, which occur primarily in the epidermis of skin, hair bulbs, and eyes. The principal subcellular site of tyrosinase activity has been determined to be melanosome. Tyrosinase converts tyrosine to dihydroxyphenylalanine (DOPA) and then to dopaquinone.
- DOPA dihydroxyphenylalanine
- dopaquinone is converted to dopachrome, through auto- oxidation, and finally to dihydroxyindole or dihydroxyindole-2-carboxylic acid (DHICA) to form melanin (brown-black pigment).
- DHICA dihydroxyindole or dihydroxyindole-2-carboxylic acid
- the main purpose for skin lightening products is to lighten the skin as well as even out skin tone or to treat pigmentation disorders such as freckles, pregnancy marks and age spots.
- tanning and pigmentation there is a need to develop a skin lightening composition that is effective in inhibiting tyrosinase enzyme and melanin biosynthesis along with sun protection.
- the cosmetic comprises 0.01 to 0.5 % by weight of arbutin, 0.01 to 0.05 % by weight of a pearl extract, 0.05 to 0.6 % by weight of an extract mixture of Glycyrrhiza glabra and Aspergillus ferment, 0.001 to 0. 1 % by weight of an Astragalus extract, and other cosmetic adjuvants, excipients and agents up to 100 % by weight, respectively, in relation to the total weight of the cosmetic.
- JP 6145039A by Yokomoto Tomohiro et al. teaches the preparation of skin cosmetic that is effective in rapid lightening of the color of dark skin, comprising 0.001 - 3.0 wt % ingredient (A) at least one substance selected from ceramid, glucosylceramid and galactosylceramid prepared by using a bovine brain, a bovine spleen, etc. and 0.001-3.0wt. % ingredient (B) glabridin which is a hydrophobic ingredient extracted from root of Glycrrhiza glabra var. glandulifera. or its aqueous extraction residue (e.g.
- JP 5186324A by Nishida Mieko et al. discloses the preparation of a beautifying cosmetic with excellent lightening and preventing effects on pigmentation of skin, suppressing inflammation, etc., comprising blending an oil-soluble essence, an extract of KANZO (root of Glycyrrhiza glabra), with a hydrophobic organic solvent with various beautifying active components and an anti-inflammatory agent.
- compositions and methods of the invention are effective to lighten hair, skin, lips and/or nails. JP2005281203A by Kubota Michio et al.
- an external skin preparation containing a glycoside formed by bonding at least one molecule of sugar to glabridin, preferably causing cyclomaltodextrin glucanotransferase to act on a system including glabridin and a saccharide.
- It is a principal object of the present invention to provide a novel herbal skin lightening composition comprising extracts of Glycyrrhiza glabra, Vateria indica, Hedychium spicatum, Alpinia galangal and cosmeceutically acceptable excipients.
- a, herbal skin lightening composition wherein said composition comprises effective concentration of extracts of Glycyrrhiza glabra, Vateria indica, Hedychium spicatum, Alpinia galanga and cosmeceutically acceptable excipients selected from binder, diluent, surfactant, perfume and preservative.
- a skin lightening composition wherein said composition is formulated as various topical delivery systems including creams with vanishing cream base and moisturizing cream base, face wash, face scrub, and face mask etc., preferably fair complexion compositions.
- the skin lightening composition is capable of inhibiting tyrosinase and melanin biosynthesis.
- a clear complexion whitening composition formulated as cream, lotion, face wash or face scrub or any other suitable topical formulation.
- a method for obtaining the extract of Glycyrrhiza glabra from rhizomes of Glycyrrhiza glabra wherein said extraction is performed using any suitable extraction technique, preferably a hot-soxhalation or percolation technique by employing a solvent or solvent system selected from a group of organic solvents, preferably halogenated hydrocarbon, an ester and an acetone, most preferably dichloromethane, ethyl acetate and acetone alone or combination thereof.
- the solvent systems provide high extractive value and the extract contains rich content of diterpenoids.
- a method for obtaining the extract of Vateria indica from bark of Vateria indica wherein said extraction is performed using any suitable extraction technique, preferably a hot-soxhalation or percolation technique by employing a solvent or solvent system selected from a group of organic solvents, preferably halogenated hydrocarbon and lower chain alcohol/s, most preferably chloroform and methanol.
- a solvent or solvent system selected from a group of organic solvents, preferably halogenated hydrocarbon and lower chain alcohol/s, most preferably chloroform and methanol.
- the solvent systems provide high extractive value and the extract contains rich content of stable phenolic molecules.
- a method for obtaining the extract of Hedychium spicatum from rhizomes of Hedychium spicatum wherein said extraction is performed using any suitable extraction technique, preferably a hot-soxhalation or percolation technique by employing a solvent or solvent system selected from a group of organic solvents, preferably long chain hydrocarbons, most preferably n-hexane.
- a solvent or solvent system selected from a group of organic solvents, preferably long chain hydrocarbons, most preferably n-hexane.
- the solvent systems provide high extractive value and the extract contains rich content of phenolic esters.
- a method for obtaining the extract of Alpinia galangal from rhizomes of Alpinia galanga wherein said extraction is performed using any suitable extraction technique, preferably a hot-soxhalation or percolation technique by employing a solvent or solvent system selected from a group of organic solvents, preferably long chain hydrocarbons, most preferably n-hexane.
- a solvent or solvent system selected from a group of organic solvents, preferably long chain hydrocarbons, most preferably n-hexane.
- the solvent systems provide high extractive value and the extract contains rich content of phenolic esters.
- the extract of Hedychium spicatum and Alpinia galanga contains cinnabloc.
- a method of extraction of rhizomes of Glycyrrhiza glabra wherein the extraction is carried out by super critical fluid extraction using carbon dioxide as medium of extraction with required pressure and temperature to obtain bioactive fraction rich in diterpenoids.
- a method of extraction of a blend of rhizomes of Glycyrrhiza glabra and stem bark of Vateria indica in the ratio of 2:1 wherein said extraction is performed using any suitable extraction technique, preferably a hot-soxhalation or percolation technique by employing a solvent or solvent system selected from a group of organic solvents, preferably halogenated hydrocarbons and lower chain alcohol/s, most preferably dicholoromethane, chloroform and methanol either alone or combination thereof are used to yield high extractive value and rich content of skin lightening agents.
- any suitable extraction technique preferably a hot-soxhalation or percolation technique by employing a solvent or solvent system selected from a group of organic solvents, preferably halogenated hydrocarbons and lower chain alcohol/s, most preferably dicholoromethane, chloroform and methanol either alone or combination thereof are used to yield high extractive value and rich content of skin lightening agents.
- a method for preparation of the skin lightening composition comprising obtaining extracts of Glycyrrhiza glabra and Vateria indica alone or in combination, obtaining the extracts of Hedychium spicatum and Alpinia galanga, filtering the resultant extracts, concentrating the extract to dryness and preparing the composition comprising the said dry extract and cosmeceutically acceptable excipients.
- Figure 1 depicts HPLC chromatogram of Glycyrrhiza glabra
- Figure 2 depicts HPLC chromatograms of herbal blend extract of Glycyrrhiza glabra and Valeria indica
- Figure 3 depicts the effect of extracts of Glycyrrhiza glabra, Vateria indica and herbal blend of the same in the inhibition of melanin biosynthesis.
- Figure 4 depicts the effect of fairness cream on skin pigmentation score in mice exposed to UV radiation - Day 14
- Figure 5 depicts the anti-tanning effect of fairness cream in mice exposed to UV radiation (Group 1 : Control).
- Figure 6 depicts the anti-tanning effect of fairness cream in mice exposed to UV radiation (Group 2: UV radiated Control - Day 7).
- Figure 7 depicts the anti-tanning effect of fairness cream in mice exposed to UV radiation (Group 3: UV Irradiation + FC Cream - Day 7).
- Figure 8 depicts the anti-tanning effect of fairness cream in mice exposed to UV radiation (Group 2: UV radiation - Day 14).
- Figure 9 depicts the anti-tanning effect of fairness cream in mice exposed to UV radiation (Group 3: UV radiation + FC Cream - Day 14).
- Figure 10 depicts the section of skin showing normal structure and architecture (100 x; Masson-Fontana stain) of Group 1 (Control) animals.
- Figure 11 depicts the section of skin epidermal proliferation along with melanin pigmentation in hair follicles core in dermal region (100 x; Masson-Fontana stain)
- Figure 12 depicts the section of skin showing near normal architecture with a drastic reduction in melanin pigmentation (100 x; Masson-Fontana stain) of Group 3 (FC Cream +UV exposed) animals.
- the present invention provides a herbal skin lightening composition comprising extracts and fractions of Glycyrrhiza glabra, Vateria indica, Hedychium spicatum and Alpinia galanga and cosmeceutically acceptable excipients for skin lightening, fair complexion and control of darkness of skin due to various factors.
- the invention provides a method to prepare the composition.
- the disclosed skin lightening composition comprises effective combination or blend of extract of said herbs Glycyrrhiza glabra, Vateria indica, Hedychium spicatum and Alpinia galanga.
- the composition is preferably prepared from rhizomes of Glycyrrhiza glabra and stem bark of Vateria indica or blend of rhizomes of Glycyrrhiza glabra and stem bark of Vateria indica, and extracts of Hedychium spicatum and Alpinia galanga and cosmeceutically acceptable excipients thereof.
- the ratio of Glycyrrhiza glabra and Vateria indica in the blend is preferably 2:1.
- the blend extract is present in a concentration between 0.05 to 1% w/w in the composition.
- the extracts of Hedychium spicatum and Alpinia galanga contains an active ingredient cinnabloc with some non volatile matter that acts as a sunscreen agent in the skin lightening composition.
- a process for the preparation of skin lightening composition comprising obtaining extracts of said herbs by employing a suitable method, preferably percolation or hot-soxhalation method employing suitable solvent or solvent systems, filtering the plant extract, concentrating the plant extract to dryness preferably on a rotatory evaporator or on a steam bath at optimum temperature and producing a herbal composition comprising the said dry extract and cosmeceutically acceptable excipients.
- the extracts of Glycyrrhiza glabra and blend of Glycyrrhiza glabra and Vateria indica are preferably dichloromethane or supercritical fluid extract.
- the herbal skin lightening composition is formulated as a topical delivery system including creams, lotion, face wash, face scrub and face mask.
- the topical delivery systems are formulated by employing any of the conventional methods.
- the creams are formulated in a vanishing cream base or a moisturizing cream base.
- the topical delivery systems can be skin lightening, fairness or clear complexion whitening compositions.
- the solvent extracts are screened by studying in vitro tyrosinase inhibitory activity, melanin biosynthesis activity and in vivo activity of skin lightening compositions.
- the extracts are standardized for the active ingredients and marker compounds using HPLC, HPTLC and LC/MS.
- the shade dried material of rhizomes of Glycyrrhiza glabra was pulverized to coarse powder and about 5 Kg each of powdered material was placed in different flasks and extracted with dichloromethane, ethyl acetate, acetone, methanol, chloroform: methanol (1:1), chloroform: ethyl acetate (1:1) and n-hexane: acetone at room temperature for 24 h to 48 h., the plant extracts were then filtered and concentrated to dryness on rotatory evaporator or on steam bath at optimum temperature under reduced pressure.
- the coarse powdered material rhizomes of Glycyrrhiza glabra were subjected to hot-soxhalation using solvents dichloromethane, ethyl acetate, acetone, methanol, chloroform: methanol (1:1), chloroform: ethyl acetate (1:1) and n-hexane: acetone at optimum temperature and refluxed until extraction is completed.
- the plant extracts were then filtered and concentrated to dryness on rotatory evaporator or on steam bath at optimum temperature. All the above corresponding solvent extracts manufactured by percolation and hot-soxhalation methods are qualitatively similar to each other.
- the coarse powdered material of rhizomes of Hedychium spicatum was subjected to hot-soxhalation using solvents n-hexane, dichloromethane, chloroform, ethyl acetate, acetone and methanol at optimum temperature and refluxed until extraction is completed.
- the plant extracts were then filtered and concentrated to dryness on rotatory evaporator or on steam bath at optimum temperature.
- the shade dried material of rhizomes of Alpinia galanga was pulverized to coarse powder and about 1 Kg each of powdered material was placed in different flasks and extracted with n-hexane, dichloromethane, chloroform, ethyl acetate, acetone and methanol at room temperature for 24 h to 48 h.
- the plant extracts were then filtered and concentrated to dryness on rotatory evaporator or on steam bath at optimum temperature and under reduced pressure.
- the shade dried material of rhizomes of Glycyrrhiza glabra and bark of Vateria indica were cut into small pieces and mixed in the ratio of 2: 1 and pulverized to a coarse powder and about 5 Kg each of powdered material was placed in different flasks and extracted with dichloromethane, ethyl acetate, acetone, methanol, chloroform: ethyl acetate (1:1), chloroform: methanol (1:1) and n-hexane: acetone at room temperature for 24 h to 48 h.
- the plant extracts were then filtered and concentrated to dryness on rotatory evaporator or on steam bath at optimum temperature and under reduced pressure.
- Example-10 Preparation of extract from the herbal blend of rhizomes of Glycyrrhiza glabra and bark of Vateria indica by hot-soxhalation method
- the coarse powder material of the blend of rhizomes of Glycyrrhiza glabra and bark of Vateria indica in the ratio of 2: 1 was subjected to hot-soxhalation using solvent dichloromethane, ethyl acetate, acetone, methanol, chloroform: ethyl acetate (1:1), chloroform: methanol (1:1) and n-hexane: acetone at optimum temperature and refluxed until extraction is completed.
- the plant extracts were then filtered and concentrated to dryness on rotatory evaporator or on steam bath at optimum temperature.
- the dichloromethane extract (PH-29FC) of the blend was used for further studies.
- the coarse powdered material of rhizomes of Glycyrrhiza glabra was subjected to super critical fluid extraction using carbon dioxide gas as extraction medium under optimum temperature and pressure and the resultant oleoresin extract was collected and compared with dichloromethane extract obtained by percolation method.
- the TLC chromatogram of SCF extract and dichloromethane extract were similar when analyzed by HPTLC.
- the coarse powdered material of herbal blend of rhizomes of Glycyrrhiza glabra and bark of Vateria indica (2:1) was subjected to super critical fluid extraction using carbon dioxide gas as extraction medium under optimum temperature and pressure and the resultant oleoresin extract was collected and compared with solvents extracts by HPTLC.
- Tyrosinase Enzyme 60u/ml enzyme will be prepared in 0.5M Phosphate buffer pH-6.8 4.
- Sample solution Stock of lmg/ml solution of samples will be prepared in 0.5M Phosphate buffer (pH-6.8) Procedure:
- the % Tyrosinase inhibition was calculated by using the following formula.
- a con t is the absorbance change of the control reaction and Atest is the absorbance change in the presence of the test drug.
- Bl 6F10 cells were maintained in DMEM (High glucose) with 10% FBS, 3.7g/L sodium bicarbonate and antibiotics at 37° C in a 5% CO 2 humidified atmosphere.
- Drug Preparation The standard preparation and extracts i.e. PH-29FC, PH-29K, PUB-135A were dissolved in DMSO to prepare a stock solution of 5mg/mL. This was further diluted with DMEM containing 2% FBS to attain desired test concentrations. All these dilutions were prepared fresh and stored at 4 0 C until use.
- mice DBA/2 mice of either sex weighing 20-25 grams were procured from in-house animal facility. The animals were housed under standard laboratory conditions and given free access to pelleted feed and water with 12 hr light/dark cycle.
- mice were divided in to 3 groups, each comprising
- mice 6-8 animals.
- Group I animals served as negative control and were not exposed to UV radiation.
- Group II animals served as positive control and exposed to UV radiation.
- Group III animals were treated with fairness cream with natural sunscreen agent cinnabloc .
- the mice were lightly anaesthetized with ether and the hair on the dorsal skin was clipped with the help of hair clipper. The clipped dorsal skin of all the animals except Group-I animals were exposed to UV light by using a UV sun lamp
- the skin pigmentation response was examined through out the study period.
- the degree of tanning was scored as mentioned below and photographs of the dorsal skin were taken at the end of the study.
- the skin pigmentation scoring is graded as follows: No reaction, no discernible pigment (gray/black/brown) darkening 0.0
- Pigmentation scores of each group will be presented as mean ⁇ SEM and the data will be analyzed using Kurskal-Wallis test followed by Dunnett's multiple comparision posthoc tsst,p ⁇ 0.05 will be considered as significance.
- Exposure to UV irradiation resulted in a significant increase in the skin tanning as indicated by the pigmentation score.
- Treatment with FC cream with cinnabloc showed a significant protection against UV-induced skin tanning (Figure 4).
- the photographs of mice dorsal skin from control, UV-exposed and FC Cream+ UV- exposed groups on days 7 and 14 are shown in Figures 5-9 respectively. Melanin pigmentation characteristics were evaluated using Masson-Fontana staining technique.
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Abstract
La présente invention concerne une composition éclaircissante pour la peau à base de plantes, destinée à éclaircir le teint et à traiter d’autres troubles cutanés. Ladite composition comprend un extrait de racines de Glycyrrhiza glabra, de l’écorce de Vateria indica et un extrait de rhizomes de Hedychium spicatum et d’Alpinia galanga, ainsi que des vecteurs de ceux-ci acceptables sur le plan cosméceutique. L’invention porte également sur des procédés permettant d’obtenir ces extraits de plante et sur divers systèmes d’application topique.
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PCT/IB2008/001793 WO2010004355A2 (fr) | 2008-07-09 | 2008-07-09 | Nouvelle composition éclaircissante pour la peau à base de plantes, procédés de production de celle-ci et compositions cosméceutiques l’utilisant |
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PCT/IB2008/001793 WO2010004355A2 (fr) | 2008-07-09 | 2008-07-09 | Nouvelle composition éclaircissante pour la peau à base de plantes, procédés de production de celle-ci et compositions cosméceutiques l’utilisant |
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Cited By (7)
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CN102793646A (zh) * | 2012-09-03 | 2012-11-28 | 贵州省生物技术研究开发基地 | 复方植物面膜及制备方法 |
US9044390B1 (en) | 2014-04-17 | 2015-06-02 | Gary J. Speier | Pharmaceutical composition and method of manufacturing |
US9186386B2 (en) | 2014-04-17 | 2015-11-17 | Gary J. Speier | Pharmaceutical composition and method of manufacturing |
CN106442809A (zh) * | 2016-12-28 | 2017-02-22 | 广西中医药大学 | 大叶金花草指纹图谱的构建方法及其指纹图谱 |
US10058531B1 (en) | 2017-06-01 | 2018-08-28 | Spartak LLC | Dosage delivery film |
CN111568831A (zh) * | 2020-06-19 | 2020-08-25 | 上海相宜本草化妆品股份有限公司 | 用于皮肤化妆品的中草药提取物的组合物及其制备方法 |
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Cited By (21)
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CN102793646A (zh) * | 2012-09-03 | 2012-11-28 | 贵州省生物技术研究开发基地 | 复方植物面膜及制备方法 |
US11266702B2 (en) | 2014-04-17 | 2022-03-08 | Cure Pharmaceutical Holding Corp. | Pharmaceutical composition and method of manufacturing |
US9044390B1 (en) | 2014-04-17 | 2015-06-02 | Gary J. Speier | Pharmaceutical composition and method of manufacturing |
US9186386B2 (en) | 2014-04-17 | 2015-11-17 | Gary J. Speier | Pharmaceutical composition and method of manufacturing |
US11344591B2 (en) | 2014-04-17 | 2022-05-31 | Cure Pharmaceutical Holding Corp. | Pharmaceutical composition and method of manufacturing |
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