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    6 views12 pages

    Amla Extract For Transdermal Application

    Uploaded by

    mazahir raza
    amla

    Copyright:

    © All Rights Reserved
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    "US 200902: us United States c2) Patent Application Publica oy 06) an @ @ Antony AMLA EXTRACT FOR TRANS APPLICATION Inventor: Benny Antony. Ankamaly (IN) 11TH Roberts Glen Court Potomac, MD 20854 (US) Appl.No: 12/382,602 Bile: Mar. 19, 2009 Continuation of application No. PCT/IN2006/000380, filed on Sep. 20, 2006. OAL ae iON (10) Pub. No.: US 2009/0238780 Al (43) Pub, Date Sep. 24, 2009 ication Classification Gl) Incl. ABIK 3/60 200501) AGIK 31/70 (200501) AGIK 31/7034 (2006.01) AGIK 36886 (2006.01), (2) US.CL 424/59, 514/23; 514/25; 424744 on ABSTRACT An extract of Embllew ofeinalis (Amis), Transdermal form Jation having an extact of Fnblicofficinals having exh iting greater migration of Viamin C across askin suriace as ‘compared to a transdermal formation having, Vitamin C ‘without the extract, Extract of EmBlica officinalis exhibiting {greater migration of Hons aeross a skin surface as com pared toa transdeemal formulation having Vitamin C alone. A {ransdermal formulation having an extract of Fimbli ofc nals, Method of preparing an extract of Emblic officials US 2009/0238780 Al AMLA EXTRACT FOR TRANSDERMAL APPLICATION RELATED APPLICATIONS, [0001] This Application is @ Continuation of co-pending PCT. Application Ser. No, PCT/IN2006°000380, filed Sep 20, 2006, which is incorporated in its entirety by reference BACKGROUND [0002] ‘The protein collagen in the dermis or the second layer ofthe skin provides a strong and healthy skin. Vitamin ‘Chas a crucial role to play in collagen synthesis. Collagen sytthesis is induced and supported by Vitamin ©. Vitamin C being highly water soluble, ace its availability atthesite oF ‘colligen synthesis is restricted since the parts ofthe skin ure Tipophilie and therefore Vitamin Cis easly eliminated from the body, During ageing collagen synthesis is retarded resul- ng inthe falling ofthe strength and support to the ska. This results in wrinkling and sogging of the skin. Hence it is rocestary to devise methods for inducing collagen synthesis vigorously by providing adequate concentrations of Vitamin ‘Cat the dermis. Any amount of Vitamin C ingested through ‘oral or other conventional routes cannot provide adquate ‘concentrations of Vitamin C a the site af collagen synthesis ‘andi isnaw wel recognized tht providing Vitamin C across the skin stractare throwgh topical application i the best way to achieve this, However due to the high water solubility of Vitamin C, its ransportation across lipophilic skin mem- branes is also slow. 10003] |The presence of radical oxygen converts dibydrox- ‘yphenylalanine (DOPA) to DOPA-quinone, which is further ‘Converted to melanin, Melanin is dark brown and it further polymerizes to black melanin pigment and these are respon- Sible forthe color of brown and black skins. it has been recognized tat the best way to prevent formation of these ‘melanin pigments is to inhibit the oxidation of DOPA to DOPA-Quinone and the conversion further Of the latte 10 rmelanin'pigments. Two agents that inhibit melanin pigment ormation are Vitamin C and hydrogen ions. Hydrogen ionsin the presence ofxocing agents ike Vitamin ean inhibit this ‘melanin synthesis and also reverse it, resting inthe whiten- ing of skin. 10004] _ One ofthe major causes of melanin pigmentation of the skin exposure to UV light present i the sun's radiation and various artificial lighting methods, There are ways 10 protect the skin from UV of actinic radiation by providing ‘pplications containing molecules that absorb UV light 10005) Vitamin C like activity is not confined to ascorbic fd, The Vitamin C bioactivity including ant seorbuticactiv- ity, promotion of collagen synthesis and various anti oxidant and fre radical seavenging properties, arise from the specific ‘chemical structural feature 1-ox0-2:ene-2, 3-dil, which is referred to as aci-teictones or simply redictones, Tere are many such reductones in nature especialy in fruits and one ‘ch fui containing reductones isthe Indian pooseberry also Known as Amla in India whose sciatic nomenclatare is Emblica oficinalis Gaet 10006] The constiuents of the Indian goosehery dry ‘extract described by Ghosal in his patent U.S, Pat, No. 6,235, TAL as “CAPROS' is said © contin the Following compo: nents and the proportion indieated: An antioxidant blend con- sisting of, by weight: [0007] | Emblicanins and B, that is, [0008] the gallic acc-ellagic acid esters of 2-keto-ghicon- ‘delta Iactone: 35.58%, Sep. 24, 2009 [0009] 2.3-di-ogalloy!_4,6-S-herahylroxydipheaoylgln- ‘nie acid (Punigaconin) 415% 0010} 2.3,4.6,-bishexahydroxydiphenoyl glucose (Pedun- eulaginy: 10 0 20%, and [O11] about Sto 15% of 3.4.5,7-tetrabydrony avon O-rhamnoglucoside (Rutin), 0012} “Tannoids of gallie‘llagic acids 10-30%; [0013] Gallic acid 0-5% and [014] Elagic acid 0-5% [01S] Chaudhari eal in their U.S. Pat. No. 6,649,150 on skin lightening or whitening compositions have described the ‘eed to rstriet the presence of Ravonoids like rutin which are yellow colored and not desirable ina skin whitening compo- ition hased on the same Indian gooscheny exinict. (Chaudhuri etal deseribes method to sclet gengraphicelly oF naturity levels ofthe fruit or by removing by ehromatogra- phy the undesimblefavonoid pigment o the minimum that is, below 1% or better, 0.1% or more preferably 0.01% They have also described the Navonoid to have strong UV absorp- ‘ion in the wavelength region of 350 nanometers [0016] The composition Chaudhuri etal is reported to have the following content [0017] Emblicanin A: 20-35%: [018] Embicanin B 10-20%; [019] Pedunculogin 15-30% [0020] Punigluconin 3-12%; and, [021] Flavonoids less than 1%, ‘SUMMARY, [0022] The disclosed teachings provide a process for the isolation of an extract ofthe fits of Emblioaofeinalis by a specific sensitive process, whereby’ the extract has nearly no amc, such as, fee gallic and fee ellagic acid, which result from hydrolysis of galloellaitannins during processing of the fruits of Emblicaoftcinalis, of, oxidation and hydrolysis products ofthe antioxidants, An extactof Embliea officinalis Js provided which hae a superior transdermal rate of delivery ‘of Vitamin C and H* ions across the outer skin membrane (epidermis) into dhe dermis (inner skin) when ow concentr- tion of the extract is applied to the skin as compared 10 application of Vitamin C alone to the skin. A transdermal preparation including the extract of the fits of Emblica offeinalis highly suitable for the skin's sensitive layers is provided, [0023] Inoaeembodiment,anextractof Fmblica ofcinalis Tiuits provided, which includes, by weight, [0024] about 35.25% of galloclagitannin; [0025] about 1-9%% of Vitamin C: and, [0026] about $-60% of carbohydrate. Corilgin is about (0.5-S% ofthe palloellagitannin. Soluble fiber is about 2-25% of the carbohydrate 0027] Inoneembodiment,anextractof Publica ofcinalis ITuit is provided, which includes, by weight, about 35-50% polyphenol. Congin is about 0.5-3% of the polyphenol [0028] Inne embodiment, transdermal formulation haw ing an extract of Emblica ofcinalis trait is provided. The {ransdermal formulation having the extract exhibits about 2 {old greater migration of Vitamin C across askin surface as ‘compared oatransdermal formulation comprising Vitamin ‘without the extract. [0029] Inone embodiment, a transdermal formulation hav ing an extrct of Emblica ofcinalis trait is provided. The ‘eansdermal formulation having the extract exhibits about a2 US 2009/0238780 Al {old greater migration of H ions aeross a skin surface as ‘comparedtoa transdermal Jonmulation comprising Vitamin © ‘without the extroet. [0030] Inone embodiment a transdermal formulation hav- ing an extract of Emblicaofieinalis is provided. [0031] -Inoneembodiment, a dosage form ofa transdermal ormulation having an extract of Fmbliea officinalis i pro- vided. The dosage form can bea lotion, cream, ointment oF zl for application to skin [0032] "Inoneembodiment,anextract of Emblica officinalis Js provided, where the extract is prepared by: 10033] pulping o fruit of Emblica oficinalis in water at room temperature of about 27degree* C. to obtain pulps 10034) drying the pulp a a temperature of about 95 -100° Cand, under vaca of about 300-600 mm of Hg to obtain the extrot of Emblica ofcinalis. 10035] One embodiment provides a method of increasing Transfer of Vitamin C across a skin surface by administering anexteactof Emblica oficial as comparedto administering ‘Vitamin C alone o the skin surface, [0036] | One embodiment provides a method of inereasing transfer of H* ios aoross askin surface by administering a cextrict of Emblica oficinalis as compared to administering Vitamin C alone othe skin surface, 10037] One embodiment provides a method of inhibiting melanin symthesis by administering an exact of Emblica officinalis 10038] One embodiment provides a method of protecting skin from aging by administering an extract of Fmblica off- inal 0039] One embodiment provides a method of protecting skin ftom aetinie radiation by administering an extract of Enblica oftcinals: [0040] One embodiment provides a method of protecting Skin from free radical damage by administering an extract of Emblica oficinalis, [0041] "One embodiment provides a method of protecting skin from ozone by administering an extract of Embliew off inal. 10042] | One embodiment provides a method of preparing an cextrct of Emblia ofcinalis by pulping the frit of EmMlica “officinalis in water at oom temperature of about 10° C. 10 ‘obtain a pulp. The pulp is dried at a temperature of about 60-70" Cand, under a vacuum of ess than about 10 torr © ‘obtain the extract of Emblica officinalis. DETAILED DESCRIPTION [0043] _ We discovered that one othe ative factions ofthe mature fruits of Emblica officinalis (Ue Indian gooseberry) ‘contains galloclagitannins, coilagin, Vitamin C, carbohy ‘date and soluble fibre in a proportion that provides ito be ‘eminently suitable fr the preparation of suitable cosmetic! pharmaceutical compositions. The extract of Emblica ofe- halis provides for a very rapid transport of the Vitamin C ‘active reduetones released from the polyphenol bonding fom the epidermis to the dermis. Therefor, the extract is usefl Jor various knov skin applications for augmenting or forthe regeneration and synthesis of collagen in the dermis, for Inhibiting melanin synthesis, for fee radical scavenging. and, ora healthy and fairer skin {0044} The process adopted by us for preparation of the Indian gooseberry extract includes specially mild and effe- tive techniques ike chilling the heny and the extracting with water alone or incon sth pharmaceutically aecept- Sep. 24, 2009 able polar solvents like ethanol, isopropanol ete. In one embodiment the extraction is performed with purified water nly to avoid introduction of solvent residues in the food ‘upplemeat/phannaceutical product. The extraction method jsbased on acold extraction procedure and by uses a techno- logically superior method of concentration, suchas, Agitated thin film evaporator (AFTE) and Agitated thin film drier (ATED) at low temperature under a vacuum of about 500- £00 mm of mereury (ig), to preserve the identity ofthe constituents naturally presen in the plant [0045] The composition of the product (extract of Bmhtia oficinals) so obtained contains ative hydrolysable tannins asshown bythe presence of allie acid in the dilute sulpsie acid hydrolyzed portion of the product hy its HPLC chro- ‘Some embodiments of the extract of Bmblica corilagin. Estimation of corikagin was by a HPLC based method. Carbohydrate was detected by & spectrophotometrie method, Soluble fibre was analyzed {through gravimetric method. Viamin Cand redvtones hav {ng Vitamin like moiety were detected bya tiation method sing dichlorindophensl Vitamin Cin the extact-of Fnblica oftcinalis was also qualitatively detected by HPTLC method. (0046) ‘Thus the undesirable rutin and any other flavonoid produto deseribed in patent U.S. Pat. No. 6,649,150 which Emphasizes the lower content of Bavonoids like rutin to be Jessthan0,1%asalvantageous ae excluded fom the extrac. ‘We have achieve this by the cold and mild extrction and concentration and drying procedure employing tate of heart technology, namely use of ATFE and ATED for processing. thereby extracting mostly the active tannins, namely the zallo-llagi tannins slong with one more hydrotysble tan- [0047] Studies showed that one embodiment ofthe extract of Emblica oftcinals had te following composition: {0048} -Gallolloge tannins: 35.5%: [0049] _ Vitamin (or redctone; or free Vitamin C andlor Vitamin € like molecules, of derivatives of Vitamin C): 8%: [0080] Contain: 0.759%; {0081} Carbohydrate: 29% [0082] Soluble fibre: 24.55%; [0088] FMagic acid: 196: and, (0054) Galle seid: 1.2% [0088] | One embodiment ofthe extract of Emblica of Tis has the following composition [0086], Gallocllagic tannins: 35=5%: {0087} _ Vitamin (which includes reduetones;or free Vita- ‘min C andor Vitamin C like molecules, or derivatives of Vitamin ©: 19%: [0088] Carbohydrate 5.85%: and, [0089] Soluble fiber 2-25%, and, [0060] wherein about 0.5-5% of the galloelagitannin is comprised of eorilagin, [0061] One embodiment of the Emblica officinalis exact has the composition as below {0062} Galfocagic tannins: 38.25% [0063] _ Vitamin C (which includes redustonesor free Vita- ‘min C and/or Vitamin C ike molecules) upto 1-5%; and (0064) Carbohydrate 5-60%%, [0065] wherein about 0.55% of the galloellagitannin is comprised of corlagin, and, wherein sbout 2-25% of the carbohydrate is comprised of soluble fiber. US 2009/0238780 Al [0066] Inoneembeal lis includes about 35% of galloelagic tannins; about 7% -9%6 of Vitamin C; about 2% free ella acid and, about 2% free gale acid [0067] Inoneembadimen, the extract of Emblioa ofcina- lis includes [0068] about35-50% of polyphenol Corilaginis about O.S- 5% of the polyphenol 10069] In some embodiments, it was found that the extract of Embliea oficinalis after dite sulphuric acid (10°%) hydrolysis gave gallc acid as the sole of most dominant produ is include ellagic acid in almost equal id, Some embodinents ofthe extract con ‘coming as a single peak along with substan Vitamin C and oiber gallo-tanins 10070] One embodiment provides an extract of mba “officinalis, prepared by pulping mature frits of Emblica oft- ‘inalisin water at room temperature of about 27°C. to obtai ‘pp then, drying the pulp atatemperatireof about 95-100 ‘Cy and, under a vacuun of about 500.600 mas of mercury to ‘obtain the extract of Emblica officinalis. [0071] In one embodiment, analysis of the extroct of Enmblica officinalis by titration with 2,6-dichloroindophenal ‘gave a vale of about 7 to about 9% of Vitamin C. HPTLC profile of the extract of Embica officinalis confirms! the presence of Vitamin C in the extract, Since, firstly, the qua Uitation of Vitamin C was performed using the dichloroin ‘dopheno! method, which detects the active moiety of Vitamin Cnamely the reductone; an, secondly, the reduetone moiety ‘ight be present in molecules other than in fre Vitamin C in the extract of Emblica officinalis, such as, in derivatives of Vitamin C, wherein the Vitamin C isnot fee but attached to eg, galloellagie tannins, therefore, the estimated Vitamin © ‘content in embodiments ofthe extract as provided incides reductones, or reductone equivalent which may’ include free Vitamin C and/or Vitamin C like molecules, [0072] In some embodiments of the extract of Fimblica ‘officinalis, the ellagie acid content is about the same percent fs gllic acid in the hydrolysate of the extract, {PTL analy- sis was used to detect gallc acid qualitatively and quantita- tively in the dy extract of Emblica ofcinalis. Ellagic acid was detected by HPLC. In some embodiments of the extract, {ie ellagic andor fre gallie acid are not found, The lack of Jee ellagie and fre gall acid, which are usually artisets of the extraction proces, showed tha the disclosed process ia mild process that protects the aetive components of Embica officinalis, suchas galloeliogtannins, from hydrolysis during the extrotion 10073] Polyphenols include tannins, including galloeligi- tannin. Other components of polyphenols may inclide fs vonoids and anthocyanins. lI tannins including galloellagie tannins are polyphenols. However, not all polyphenols are 10074) | Galloetiagitannins ae glucose derivatives of palic and ellagic acid Corlagin ea galloellagitannin. Corin is ‘ao a hydrolysable galloellag tannin, Corilagin content of the exirict of Emblicaoficinals canbe determined by high performance liquid chromatography (HPLC) method, [0075] -Tannins include bydrolysablesnd non-hydrolysable tannins. Non-hydrolysabe tannins aealso relerredtoascon- ‘densed tains, Hydrolysable tannins include glucose deriva ul the extract of Embliceoffcina- Sep. 24, 2009 Lives of gallic and ella acid, which are water soluble Hiydrolysable tannin content ofthe extract of Emblicn ofc nals can be deerme by (1) Hydrlyzing the dey extact of Erblica finals with ucts such as hydrochloric eid, and estimating the released ellagic acid by methods such as HPLC, and estimating the released gale aid by methods such ay HPTLC. This step yields the ftal lage and allie eed coutent of the dry eetrct of Endlicaofcinals. (2) Estimating the amount of Silage aid and gor acid inthe unreted dry extract of Frnbleaofcinalls The content ofellage acid and galic acid obtained rm the untreated dy extract of Ebon finals isthe fee gllic and ellie ci eotent ofthe dey extract of Enbiicaoftinls. 3) The hydrolysable gallic and cllagic acid conteat of the dey extract of Emblem ofcinalis is bined by subuocting the valu of the fe alicandellagic aid oblanedin step) from te ttl pale and ella acid content obtained in stp (1, [0076] Carbohydrate ineldes soluble fiber and insoluble components. Insoluble components inelode insoluble fiber dun) starch. Carbohydrate content of the dry exact of Frnblca oficinalis can be determined by spectophotometic method using anthrone reagent. Soluble Uber centent of the tac of Emblioa ofcinalis can bedstermined by grevimet- Fe metho. (0077) Fibers largely carbohydrate The bung blocks ofall earbolyratesarediffren peso sugars and they ean be clastifed according to how many sugar molecules are combined inthe carbohydrate. Simple susars consist of 1-2 sugar molecules such as plucose tse, svrase, maltose, lactose, Oligosaccharides consist of 10 glucose molecules joined together. Starch polysaccharides have more than 10 cose molecules joined togetie. Non-strch poyssccha- rides have more than 10 sugar molecules such #8 xylose, Ambinose, and mannose. Dietary fibre inludes now-starch Polysaccharides, olgonaccaries, Tgiin (oot carbo Gate) ad associated pant substances {0078} Soluble fiberissoluble"in water: When mixed with water it forms #gelike substance and swells. Soluble ber Js many bene inling moderating blod gcose eels and lowering cholesterol. The seeatiie mes for soluble ers inciode pein, guns, milage and some hence Iuloses. Good sources of soluble fer inlude oats td rea, legumes (peas, beans, lentil), barley, fais and veR™ cables (especialy oranges, apples an aro). (0079) - Werhave during our investigation and eles to fne- tionally extract the most desirable constituents and leave ot tho less soluble and undesirable constituents by a very mild ‘traction, concentration and drying procedie 8 mentioned shove sneceedd in getting 8 superoeprodict having a come bination of ingredints described that have the unexpectedly superoe property of several fold apd intadmaal transport of (1) Vitamin C derived from gallo~llag tannins and 2) Iydeogen ions, especially on higher dluton ofthe exe, whichis pauper ideally stole forskinapplications sing Jow doses of exact. Compositions having the extract of bia ofcnais wll beuseful forall he skin applications of Vitamin € setive compositions as described in erste Jes. One cmbedient ofthe extract of Eble ofcnalis x refered to ay °C-COSI™" {0080) In onc.mbodiment, strana fomlation hav ing an extn of Embicaafiinalis fat exhibits about a 2 {old grate migration of Vain C (hich includes ei= Pike US 2009/0238780 Al smolecules) aes askin surfaces compared to a tans mal formulation ving Vitamin (or ascorbic acid) without the extmet. In one embodiment, tansdermal foemulation having an extrt of Fmblicaofcinalisexbibitsabout 2 fold to bouta 7 fold arcater migration of Vitamin Cacros askin surface as compared to 2 transdemal formulation having Vitamin C without the exint a one embdioent trans ermal formulation having an of Embliea oficinalis exhibits shot a2 fold to about Sfoldarcatermiarationot Vitamin across skin surface a compared oa transdermal formu tion having Vitamin C without the extn. In one embod ment, tansdemal formulation having about 10 mg ofthe ‘extract exhibits about a 2-fld preter gration of Vitamin C eos guines pig abdominal skin a compared ta transder ‘hal formulation havingabout 10mg of Vitamin without the ‘extract. [none embodiment, ransdemal formulation ha= ingabout 1Omgor te extract exhibits abouta 2-oldto about 25 fold greater migration of Vitamin C across guinea pia sibdominal skin 48 compared to transdermal fonnulation having sot 10 mg of Vitamin C without the ext. Inone ‘embodiment, a transdermal formulation having sbout 10 a ‘ofthe extraet exhibits about a2-old to about aS Told greeter tnigraton of Vitam C across guinea pig abdominal skin as ‘compared toa transdermal fomltion having about 10mgo? Vitamin € without the extract. {0081} _Asorheeimportnt discovery that has of been made uring our investigation afte extract of Enblicaoficinalis isthat theresa sever fold fester ransfer oH ons om the application of the extract of EmBlica oficial othe ski surface int the skin layers. The presence of active oxy ‘converts DOPA lg DOPA-Quinone whichis further converted ‘omlanin which s dark brown andi futher polymeries to black melanin pigment which is responsible for black and bron skins. thas come o our abservation ding oe inves Satins that the extmt of Embl offcinlis toaster hydrogen ions across the membrane far aster thn Vitamin © preprations do, Surprisingly we sso discovered tht the rte ‘ftansfer a these hyeogen ions was exponentially propor tional to the dilation oftheextrat of Eni oficnals Tae resis showed that the extract of Bmblicaofcinai, which ‘vas prepared the disclosed mild process was sulablews a ‘agent for delivering greater amountsof Vitamin and greater ‘mount of hydrogen fons as compared to administration of Vitamin (escorbie aed) alone 10082} Inone embovtiment, a transdemal formation hav= ing an extoet of Fmbiceoficinls fut exhibits about a 2 fold greater migration of 1” ons across a skin surface as compared to a tramdermal formulation having Vitamin C without the extract. In one embodiment, a transdermal for ratio having an xtractot EmBli ofcinaisitexbibits thot a2 fold about #13 fold acatr migration of fons ‘cross askin surface as compare to transdermal formulae thon having Vitamin C without the exit In one embod ‘ment a ansral formation having an extract of Embica “oficinalseitexhibtsabout 2 fold to about 2 10 fold greeter ‘of H™ fons across shi srfae a compared io 4 teansdermal formulation having. Vitamin C without the ‘extract. none embodiment ausdeemal formulation ha= ingen extract of Zmblicsoficinai rit exibits sboot 2 old to about 8 fold greater migration of FP ons gros askin surface as compared to 8 transdemal formletion having Vitamin C without the eximet none embioent trans ermal formilation having an extmet of Emflioaoficinalis Fruitexhibits about 2 fold to about 25 fold prester arto Sep. 24, 2009 fH" ions across skin surice as compared to stander ‘ormulation having Vitamin C without the extrct, In one embodiment, a transdermal formulation having an extact of Enblica officinalis frit includes about 10 mg ofthe extract, and, the composition exhibitsabouta2-fold greater migration ‘of H fons across guinea pig abominal skin as compared t0 transdermal formulation having about 10 mg of Vitamin ‘without the extract. In one embodiment, a transdeemal fore ‘mulation having an extract of Einhicaofeimalis eit, which includes about 10 mg of the extract. The a transdermal fore ‘mulation having the extract exhibits about a 2-fold greater rigration of H* ons across guinea pig abdominal skin as ‘compared to a transdenmal formulation having an about 10 mg of Vitamin C without the extract. In one embodiment, a transdermal formation having an extract of Emi ofc nls fest inckades shout 10mg ofthe extract, and, the com- position exhibits about a 2-fold to about 13 fold greater migration of H* ions aeross guinea pig abominal skin as ‘compared oa transdermal formulation having about LOmgot Vitamin C without the extract, la one embodiment, tans- dermal formulation having an extract of Emblica officinalis fruit includes about 10 mg of the extract and, the tnsdermal ormolation exhibits about a 2-fold to about a 10 fold greater ‘migration of [1° ions across guinea pig abominal skin as compared oa transdermal formulation having about LOmgor Vitamin C without the extract. In one embodiment, a trans- dermal formulation having an extract of Emblica officinalis fruit includes about 10 mg ofthe extract, nd the tarsdermal ormulation exhibits about a 2-fold to abouts 8 fold greater migration of f° ions across gvinea pig abdominal skin as ‘compared oa transderma formulation having about LOmgor Vitamin C without the extract la one embodiment, a trans- {dermal formulation having an extract of Emblica officinalis {iit includes about LOmgo the extract, aad, thecomposition exhibits about a 2-fld t about a 5 fold greater migration of TH ions across guinea pig abdominal skin as compared to @ ‘transdermal formulation having about 10 mg of Vitamin C without the extrt. [0083] still more interesting phenomenon we observed is tat the polyphenols become attached tothe outer skin and behave as a protectiveagent against UV light. UV radiation is responsible for initiating the formation of melanin pigments fad also fice radicals. The formation of the UV protecting Jayer by the polyphenols protets the skin against UV light and its deleteriows effects and discoloration of the skin and should cumulatively prevent melanoma, which is @ form of ‘cancer of the skin, We furher discovered that not even a trace ‘ofthe polyphenols crossed the skin in the in vitro study sing auinea-pigskin [0084] 1s Tikely thatthe migration of the Vitamin C or ‘molecules having Vitamin C Tike activity, or the reductone ‘oely of Vitamin C aeross the skin surface is closely asso- iatec withthe binding of the polyphenol to the skin surface. PPlyphenol might bind with the skin proteins providing pro- ‘ection against che passing of sete (UV) light ino the kin 0085} Sot bocomes evident that theres some relationship ‘ofthe combining ofthe polypienols with the outer sue the skin and the faster release of the Vitamin C present it less stable furanose (G-memberod ring) structure, possibly ‘changing over tothe linear structure and crossing the epider ris ofthe skin and assuming is naturally stable pyranose (G-membered ring) stricture and contising withthe normal ‘antioxidant and induetive fonction Tor collagen synthesis, US 2009/0238780 Al 10086] With these results we have discovered an improved product, namely, anextractof Emblica ofcinals, amethod to prepare the same and properties of the extract of Embica ‘ffcinals tat are immensely superior to any existing skin ‘application, in that the extract of Emblica oficial provides ‘superior rate of tunsfer of Vitamin C and hydrogen ions ‘across the skin, and thereby, provides protection against aging. acts as a free radical scavenger, as an inhibitor of mieanin synthesis and asa protector against UV and possibly clher forms of actinic radiation, and, from polluting agents like ozone, 10087] -Trunsdermal Transport Ses. [0088] The difsion studies were caried out across the tunes pig abdominal skin, The difusion cell had aa upper ‘chamber anda lowerchamber. The guinea pigalsdominal skin was placed between the upper and lower chambers of the

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