CA2369697C - Process and composition for enhancing the action of vitamin a on the cellular activity of an individual, and use of vitamin c - Google Patents

Process and composition for enhancing the action of vitamin a on the cellular activity of an individual, and use of vitamin c Download PDF

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Publication number
CA2369697C
CA2369697C CA002369697A CA2369697A CA2369697C CA 2369697 C CA2369697 C CA 2369697C CA 002369697 A CA002369697 A CA 002369697A CA 2369697 A CA2369697 A CA 2369697A CA 2369697 C CA2369697 C CA 2369697C
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Prior art keywords
vitamin
composition according
group
microspheres
composition
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Expired - Fee Related
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CA002369697A
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French (fr)
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CA2369697A1 (en
Inventor
Roberto Alcantara Martins Zucchetti
Simoni Chitarra Souza
Luciana Villa Nova Silva
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Natura Cosmeticos SA
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Industria e Comercio de Cosmeticos Natura Ltda
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Publication of CA2369697A1 publication Critical patent/CA2369697A1/en
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Publication of CA2369697C publication Critical patent/CA2369697C/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/0241Containing particulates characterized by their shape and/or structure
    • A61K8/025Explicitly spheroidal or spherical shape
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67Vitamins
    • A61K8/671Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67Vitamins
    • A61K8/676Ascorbic acid, i.e. vitamin C
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/16Emollients or protectives, e.g. against radiation
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/56Compounds, absorbed onto or entrapped into a solid carrier, e.g. encapsulated perfumes, inclusion compounds, sustained release forms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/59Mixtures

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Birds (AREA)
  • Dermatology (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Toxicology (AREA)
  • Cosmetics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)

Abstract

The present invention refers to a process, a composition and the use of Vitamin C for enhancing the action of Vitamin A on the cellular activity of an individual. According to the invention, the association of Vitamin C to Vitamin A will be applied to said individual at a weight ratio ranging from 1:1 to about 10:1.

Description

Title: "PROCESS AND COMPOSITION FOR ENHANCING THE ACTION OF VITAMIN A
ON THE CELLULAR ACTIVITY OF AN INDIVIDUAL, AND USE OF VITAMIN C"

Field of the Invention The present invention refers to a process for improving the effects of Vitamin A
used in cosmetic compositions in order to enhance the cellular activity of an individual.
Background of the Invention The compound generically known as Vitamin A comprises retinol and its deriva-tives, also known as retinoids, in addition to its acidic or aldehyde form, respectively retinoic acid and retinal. Retinoic acid has application in the pharmaceutical and cosmetic industries being, however, prohibited in several countries for cosmetic use due to the adverse effects of irritability which it may cause. Examples of pharmaceutical applications of retinoic acid can be found in the article "Relationships between structure and activity of retinoids", published by Nature, Volume 236, pages 110-113, of September 9, 1996.

In the cosmetic area Vitamin A is usually employed in the form of retinol or some of its retinoids such as retinyl palmitate, and the use of retinol causes various biologic activities, many of which are highly desirable in cosmetic compositions, particularly in those intended to improve the general conditions of the skin of the individual subjected to the topic use thereof. Results achieved by the topic use of Vitamin A are described in passages con-tained in pages 82 - 119 of the article entitled "Vitamin A Complex", written by Wade Cheng, PhD and Shirley DePetris and published by Skin Inc., March/April 1998.

Moreover, regulation and balance of the epidermal cellular growth through the total synthesis of collagen, among others, such as retention of water in the skin, are also known as effects resulting from the use of Vitamin A in its pure form, called Retinol.
One problem resulting from the use of Vitamin A, either in its pure form or as a derivative, is that, on the one side it promotes the effects of increasing the cellular activity at the level of the dermis and epidermis, accelerating the process of proliferation and differ-entiation of the keratinocytes and reorganization of the fibers of the dermis (collagen and elastin). But on the other side it must be administered at low doses due to its toxicity. This fact limits the use of Vitamin A and its derivatives to iower contents or requires the utilization of other means that are able to minimize the discomfort of irritation in the skin.

In fact, the use of retinol at low contents is quite common, as shown by sev-eral studies, such as the one conducted by the Hamburg Clinic of Experimental Dermatol-ogy, in Germany, which doscioses tests with low contents of Retinol (0.034%) for men and women with age between 22 and 34 years and which show that such a concentration of retinol could reduce the amount and the deepness of wrinkles. Therefore, this study generi-cally shows the effect of reducing wrinkles by the use of low contents of retinol.

On the other hand, what has been observed is that, even though low concen-trations of retinol effectively cause little or no irritation, the results on the skin can remain below the desired levels for the present standards of demand of the consumers in view of the small amount of retinol incorporated in the cosmetic composition and available for its biological action.

In this respect, there have been attempts to obtain compositions of Vitamin A that present effective action and do not cause adverse effects, for instance, the irritation of the skin; examples as shown in United States Patent No. 5,516,793 and United States Patent No. 5,703,122 in the name of Avon Products, Inc. These documents describe a generic association of amounts ranging from 0.5 to 25% by weight of Vitamin C
with several irritating active principles, among which Vitamin A is included. This association, however, has the exclusive purpose of reducing irritation of the skin caused by Vitamin A.

It is therefore an objective of the present invention to provide an alternative for the use of Vitamin A at such concentrations that enable an increase in its properties which are beneficial to the skin, without presenting the problems cited above.

Summary of the Invention The present invention refers to a process for enhancing the action of Vitamin A on the cellular activity of an individual comprising the association of Vitamin C with Vitamin A, which will be applied to the referred-to individual at a weight ratio ranging from about 1:1 to about 10:1.

In another aspect, the invention refers to a composition for enhancing the ac-tion of Vitamin A on the cellular activity of an individual comprising Vitamin C in association with Vitamin A at a weight ratio in the range from about 1:1 to 10:1.

The invention further refers to the use of Vitamin C for enhancing the action of Vitamin A on the cellular activity of an individual.

According to one aspect of the present invention, there is provided a composition for enhancing the action of Vitamin A on the cellular activity of an individual, comprising a plurality of dispersed microspheres, said plurality of microspheres comprising Vitamin A and an antioxidant, inserted into a first group of microspheres, and Vitamin C inserted into a second group of microspheres.

Brief Description of the Drawings - Figure 1 shows a graph representing the increase obtained In the cellular activ-ity of a reconstituted skin by the synergistic effect of an association of Vitamin C with Vitamin A according to the invention as compared to the cellular activity of a reconstituted skin treated only with pure Vitamin A.

- Figure 2 shows the synergistic effect on the recuperation and the increase in the cellular activity in reconstituted skin treated with Vitamin A associated with Vitamin C
when subjected to ultraviolet irradiation.

Detaiied Description of the Invention After detailed studies the Inventors have found that the association of Vitamin C
added to compositions containing Vitamin A at a weight ratio ranging from about 1:1 to about 10:1, preferably from about 1:1 to about 5:1, and more preferably from about 1:1 to about 2:1, provides a surprising increase in the cellular activity effects of Vitamin A on an individual.

3a "Vitamin C" useful for the present invention comprises Vitamin C in its pure form or its derivatives, namely L-ascorbic acid in its molecular form as well as its salts and esters such as ascorbyl phosphate.

As used herein, the expression `an increase in the cellular activity" means the occurrence of a benefit brought about by the increase or improvement at least in one of the situations selected from the maintenance of the cellular condition, the cellular proliferation and the metabolic activity especially in cutaneous cells.
Tests carried out on reconstituted skin show that a treatment of the skin in vi-tro with the association of Vitamin C with Vitamin A according to the present invention pro-motes an unexpected synergistic increase in the cellular activity of 100% as compared to the cellular activity observed in the same skin treated exclusively with pure Vitamin A or retinol (figure 1).

In the same surprising way, it has been noted that the association of Vitamin C with Vitamin A promotes reconstitution, recuperation and increase in the cellular activity of the skin, even when the individual is subjected to ultraviolet irradiation, which is recognized to cause deleterious effects on the skin and its cells. Tests carried out to this respect show a synergistic effect of reconstitution and increase in the cellular activity of 5% on reconstituted skin treated with Vitamin A associated with Vitamin C when subjected to ultraviolet irradiation (figure 2).

The association of Vitamin C with Vitamin A according to the present invention may be carried out at the moment of the application of these compounds to the individual, but it can also be advantageously formulated as a cosmetic composition containing the two vitamins at a weight ratio ranging from about 1:1 to about 10:1, preferably from about 1:1 to about 5:1, and more preferably from about 1:1 to about 2:1 of Vitamin C to Vitamin A.
According to a preferred embodiment of the invention, said cosmetic compo-sition comprises, by weight, about 0.01 to about 0.9% of Vitamin C and from about 0.008 to about 0.20% of Vitamin A, based on the total weight of the composition. Even more prefera-bly, the composition contains from about 0.02 to about 0.8% by weight of Vitamin C and from about 0.009 to about 0.16% by weight, of Vitamin A and even more preferably the composi-tion contains 0.02 wt.% of Vitamin C and from about 0.009 to about 0.02 wt%
Vitamin A, all the percentages based on the total weight of the composition.

It is noted that, even at very low concentrations, Vitamin A associated with Vitamin C as defined in the present invention achieves the desired effects of increase in the cellular activity.

The cosmetic compositions containing Vitamin A and Vitamin C at the propor-tions cited above can also contain other appropriate additives and formulation aids, such as antioxidants for combating free radicals. Among the useful antioxidants, Vitamin E stands out, both in its pure form presented by di-a-tocopherol, and as its derivatives such as dil-a-tocopherol, or 2,6-di-terc-buthyl-p-cresol (BHT).

The introduction of Vitamins C, A and E in mircospheres increases their action and makes it possible for them to reach the deeper layers of the skin with greater, or even total, integrity, without degeneration of the product in the path between the application area end the place of action.
In a particularly preferred way, the cosmetic compositions according to the present invention are formulated in such a manner, that their components are contained in organic vectors such as microspheres and, more particularly, in microspheres or microcapsules containing biologically active material ("Talasferas") such as those defined in US Patent 5,395,620, or in Brazilian patent application PI 9706994-7, filed in the name of this same applicant.

The composition as described above may contain a plurality of said microspheres, in a dispersed form, comprising Vitamin A and, for example, an antioxidant such as Vitamin E, inserted into a first group of microspheres, and Vitamin C inserted into a second group of microspheres. A particularly preferred composition comprises a first group of microspheres containing Vitamin A at an average concentration of 0.014% and Vitamin E at an average concentration of 0.0005% by weight, and a second group of microspheres containing 0.02%
by weight of Vitamin C.
Advantageously, in association to the groups of microspheres previously mentioned, such a composition may further contain, in addition to Vitamin A and Vitamin E, cosmetic compounds selected from the group comprising skin structures, preferably squalan and sphingolipide complexes, skin micronutrients, preferably seaweed extract, sensory agents, for example, moisteners such as glycerin and hydroxy prolisilan C, emollients such as butylene glycol and cetyl lactate and silicones such as cyclomethicone, solar protection factors such as ParsolTM 1789 and EusolexT"' 6300, emulsifiers, preferably CarbopolTM 1342 associated to trietanolamin and soybean lecithin, thickeners, preferably xanthan gum;
sequestrants, preferably EDTA, antioxidants such as BHT and dl-a-tocopherol, fragrances, conservants, water and mixtures thereof.

In one particular embodiment of the present invention, the composition containing Vitamin A and Vitamin C may be in the form of an emulsion and, in this case, the Vitamin C
preferably used is L-ascorbic acid stabilized by hydrogen bridge forming compounds. Such processes of stabilizing L-ascorbic acid are described in applications PI
9704418-0 and PI
9704728-7, also filed by this applicant.

v. = c. : u=... ... .~ _ . ~ . _ . _ _ _ _ .. _ - _ n: U_ n !G:4C D(:VANNE6'1ANn :!nMSEh` j:~!!b4.Z3UU _. f-iUB P.Q: :-~- -_.c As an Iliustratlve example of another possible embodiment or Itics Fmaadiil in-vention, the composition is formulated as a gel in which the weight ratio of Vrtamin C to Vita-min A is advantageously about 5:1, Vitamin C being present preferably in amounts of about ().756A and V"rtamin C being present In amounts of about 0.16 wt.%, based on the total weight of the composition. This gel composibon may further contain thickeners such ascar-bopol, fragrances, consenrants and water.

AMENDED SHEET

Claims (17)

THE EMBODIMENTS OF THE INVENTION IN WHICH AN EXCLUSIVE
PROPERTY OR PRIVILEGE IS CLAIMED ARE DEFINED AS FOLLOWS:
1. A composition for enhancing the action of Vitamin A on the cellular activity of an individual, comprising a plurality of dispersed microspheres, said plurality of microspheres comprising Vitamin A and an antioxidant, inserted into a first group of microspheres, and Vitamin C inserted into a second group of microspheres.
2. The composition according to claim 1, wherein said Vitamin C is contained in the second group of microspheres at a concentration of 0.02%.
3. The composition according to claim 2, wherein Vitamin A is present at a concentration of between 0.009% and 0.02% by weight, based on the total weight composition.
4. The composition according to claim 3, wherein said first group of microspheres contains Vitamin A at an average concentration of 0.014% by weight, based on the total weight of the composition.
5. The composition according to claim 4, wherein said first group of microspheres contains Vitamin A at an average concentration of 0.014% and Vitamin E at an average concentration of 0.0005% by weight, and cosmetic compounds selected from the group consisting of skin structures, micronutrients of the skin, sensory agents, emollients, silicone, solar protection factors, emulsifiers, thickeners, sequestrants, antioxidants, fragrances, conservants, water and mixtures thereof.
6. The composition according to claim 1, comprising Vitamin C in association with Vitamin A at a weight ratio ranging from 1:1 to 10:1 of Vitamin C to Vitamin A.
7. The composition according to claim 5, wherein said skin structures are squalan and sphingolipide complexes.
8. The composition according to claim 5, wherein said micronutrients of the skin is seaweed extract.
9. The composition according to claim 5, wherein said sensory agents are selected from the group consisting of moisteners, and silicones.
10. The composition according to claim 1, wherein said antioxidant is Vitamin E.
11. The composition according to claim 9, wherein said moisteners are selected from the group consisting of glycerin, hydroxy prolisilane C, and combinations thereof.
12. The composition according to claim 5, wherein said silicone is cyclomethicone.
13. The composition according to claim 5, wherein said solar protection factors are selected from the group consisting of butyl methoxydibenzoyl methane, 3-(4-methylbenzylidene) camphor, and combinations thereof.
14. The composition according to claim 5, wherein said emulsifiers are selected from the group consisting of acrylates/C10-30 alkyl acrylate crosspolymer associated with trietanolamin, soybean lecithin, and combinations thereof.
15. The composition according to claim 5, wherein said thickener is xanthan gum.
16. The composition according to claim 5, wherein the sequestrant is ethylene diamine tetraacetate (EDTA).
17. The composition according to claim 5, wherein the antioxidants are selected from the group consisting of butyl hydroxytoluene (BHT), dl-.alpha.-tocopherol, and combinations thereof.
CA002369697A 1998-09-08 1999-09-03 Process and composition for enhancing the action of vitamin a on the cellular activity of an individual, and use of vitamin c Expired - Fee Related CA2369697C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
BRPI9803936-9 1998-09-08
BR9803936-9A BR9803936A (en) 1998-09-08 1998-09-08 Process and composition to increase the action of vitamin A on an individual's cellular activity and use of vitamin C.
PCT/BR1999/000072 WO2000013659A2 (en) 1998-09-08 1999-09-03 Process and composition for enhancing the action of vitamin a on the cellular activity of an individual, and use of vitamin c

Publications (2)

Publication Number Publication Date
CA2369697A1 CA2369697A1 (en) 2000-03-16
CA2369697C true CA2369697C (en) 2009-12-15

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CA002369697A Expired - Fee Related CA2369697C (en) 1998-09-08 1999-09-03 Process and composition for enhancing the action of vitamin a on the cellular activity of an individual, and use of vitamin c

Country Status (9)

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US (1) US6967217B1 (en)
EP (1) EP1112059A2 (en)
JP (1) JP2002524405A (en)
AR (1) AR023047A1 (en)
BR (1) BR9803936A (en)
CA (1) CA2369697C (en)
CO (1) CO5150198A1 (en)
PE (1) PE20000896A1 (en)
WO (1) WO2000013659A2 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040136938A1 (en) * 2000-09-11 2004-07-15 Robert Ladislas Composition of vitamin c and/or vitamin a
US20030232091A1 (en) * 2002-06-17 2003-12-18 Adi Shefer Stabilized retinol for cosmetic dermatological, and pharmaceutical compositions, and use thereof
AU2003250967B2 (en) * 2002-07-24 2009-05-28 Basf Aktiengesellschaft Ascorbic acid salt suspensions and use thereof as antioxidants
US11576850B1 (en) 2020-01-06 2023-02-14 Platinum Skin Care, Inc. Face peel formulation and method of application

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Publication number Priority date Publication date Assignee Title
JPH0717504B2 (en) * 1985-03-09 1995-03-01 美浜 久春 Composition for preventing and treating thrombosis
FR2591105B1 (en) * 1985-12-11 1989-03-24 Moet Hennessy Rech PHARMACEUTICAL COMPOSITION, IN PARTICULAR DERMATOLOGICAL, OR COSMETIC, BASED ON HYDRATED LIPID LAMELLAR PHASES OR LIPOSOMES CONTAINING A RETINOIDE OR A STRUCTURAL ANALOG OF SUCH A RETINOID AS A CAROTENOID.
US4704280A (en) 1986-12-19 1987-11-03 Bates Harry L Cosmetic lotion
FR2612775B1 (en) * 1987-03-25 1991-10-11 Thorel Jean COMPOSITIONS FOR THE PREVENTION AND TREATMENT OF SKIN DEGENERATION
DK0381543T3 (en) * 1989-01-31 1993-10-04 Coletica Use of solutions of atelocollagen and polyholosides, e.g. glucosaminoglycans, for the preparation of microcapsules, microcapsules prepared in this manner, processes for the preparation of such microcapsules and cosmetic or pharmaceutical compositions or food compositions in which they are present
US5395620A (en) * 1989-01-31 1995-03-07 Coletica Biodegradable microcapsules having walls composed of crosslinked atelocollagen and polyholoside
US5230836A (en) 1991-06-20 1993-07-27 Kalamazoo Holdings, Inc. Low micron-sized ascorbic acid particles, especially a suspension thereof in a medium in which they are insoluble, and the use thereof as an antioxidant for mediums in which the particles remain insoluble
GB9223235D0 (en) 1992-11-05 1992-12-16 Unilever Plc Cosmetic composition
US5720805A (en) * 1993-04-13 1998-02-24 Southwest Research Institute Titanium-tin-oxide nanoparticles, compositions utilizing the same, and the method of forming the same
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KR20000016721A (en) * 1997-05-02 2000-03-25 한스 발터 라벤 Stable vitamin c concentrates
US6194452B1 (en) 1997-11-07 2001-02-27 Howard Murad Stable pharmaceutical compositions including ascorbic acid and methods of using same
US6015548A (en) 1998-07-10 2000-01-18 Shaklee Corporation High efficiency skin protection formulation with sunscreen agents and antioxidants
JP4150501B2 (en) * 1997-12-24 2008-09-17 シャクリー コーポレイション Composition with high efficiency skin protection from the damaging effects of ultraviolet light
US6228894B1 (en) * 1998-04-17 2001-05-08 Enhanced Derm Technologies, Inc. Softgel-compatible composition containing retinol
US5891470A (en) 1998-04-17 1999-04-06 Advanced Polymer Systems, Inc. Softgel formulation containing retinol

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EP1112059A2 (en) 2001-07-04
US6967217B1 (en) 2005-11-22
AR023047A1 (en) 2002-09-04
CO5150198A1 (en) 2002-04-29
CA2369697A1 (en) 2000-03-16
BR9803936A (en) 2000-04-04
WO2000013659A3 (en) 2000-07-27
PE20000896A1 (en) 2000-11-08
JP2002524405A (en) 2002-08-06
WO2000013659A2 (en) 2000-03-16

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