WO2001080945A1

WO2001080945A1 - Method for transdermal administration of ascorbic acid

Info

Publication number: WO2001080945A1
Application number: PCT/KR2001/000648
Authority: WO
Inventors: Won-Seok Kim; Jong-Wook Park; Hee-Yoon Cho
Original assignee: Doctors Tech Co., Ltd.
Priority date: 2000-04-21
Filing date: 2001-04-18
Publication date: 2001-11-01
Also published as: AU2001252733A1

Abstract

The present invention relates to a method for transdermal administration of ascorbic acid and to a skin-care apparatus. The present invention provides a method for transdermal administration of ascorbic acid, characterized in that a metal phosphate salt of ascorbic acid is penetrated into skin by iontophoresis, which comprises periodically applying a positive voltage of 3 to 20v, a negative voltage of 3 to 20v and current of 0.01 to 1.0 mA to transdermally administrate an aqueous solution composition comprising a metal phosphate salt of ascorbic acid, and a skin-care apparatus using the iontophoresis and ultrasonic waves. The method of the present invention exhibits the effects of freckle removal, melasma remove, acne removal, sebaceous matter removal, wrinkle removal, skin-aging prevention and whitening.

Description

Method for transdermal administration of ascorbic acid

BACKGROUND OF THE INVENTION

(a) Field of the Invention

The present invention relates to a method for transdermal

administration of ascorbic acid and to a skin care apparatus using ultrasonic

waves. More particularly, the present invention relates to a method for

transdermal administration of ascorbic acid that effectively penetrates

ascorbic acid that is unstable in an aqueous solution and has low

transdermal administration efficiency into skin, and to a skin-care apparatus

that enables the transdermal administration of vitamins by ultrasonic

cleansing and iontophoresis using one apparatus.

(b) Description of the Related Art

In general, ascorbic acid, also known as Vitamin C, has an efficacy

of maintaining healthy and attractive skin. In addition, medically, it

promotes the formation of collagen in human skin to slow down or prevent

skin-aging and the formation of wrinkles, and it is also known to have an

effect of preventing skin damage due to ultraviolet rays.

In addition, ascorbic acid is known to have an effect of inhibiting the

formation of histamine, which is believed to be a cause of the formation of melanin, which induces pigmentations, and various allergies, particularly skin

allergies appearing in persons having sensitive skin.

Accordingly, there has been an attempt to use ascorbic acid in

cosmetics or medicines having whitening effects for freckles as well as for

wrinkle-removing effects.

As methods for administrating ascorbic acid in human bodies, oral

administration and transdermal administration methods have been proposed.

According to the oral administration method, ascorbic acid can be stored and

used in a comparatively stable form, because the method employs powdered

ascorbic acid. However, since a transfer process to relevant skin is

inefficient, the actual efficiency, which is a ratio of active ingredients

penetrated into skin to total dose, is very low.

A transdermal administration method where ascorbic acid is directly

administrated into skin is preferable in order to increase the actual efficiency.

However, the efficiency for transdermal administration of ascorbic acid is low,

ascorbic acid has very low solubility in a non-aqueous medium, and if

dissolved in an aqueous medium it is easily oxidized and therefore loses its

unique function, and thus this method is not practical.

In order to improve such instability of ascorbic acid, U.S. Patent No.

4,983,382 has suggested a method of using water and organic solvents such

as ethanol together as a medium, and U.S. Patent No. 5,981 ,578 has

suggested a method of simultaneously applying a non-aqueous solution

comprising ascorbic acid and other products such as a wash and lotion containing water to skin.

As another method for improving instability of ascorbic acid, a

method for stabilizing it by combining it with other compounds to form a

derivative is known.

As examples, Korean Patent Application No. 97-23005 discloses

synthesizing ascorbic acid having excellent stability by reacting L-ascorbic

acid with 3-aminopropyl phosphate, and cosmetic formulations including a

lotion, a nutrition cream, a massage cream, an essence, etc. containing the

ascorbic acid derivatives as active ingredients. However, when ascorbic

acid is mixed with cosmetics and transdermally administrated, a transfer

process to skin is inefficient and thus the actual efficiency is low.

SUMMARY OF THE INVENTION

It is an object of the present invention to provide an ascorbic acid

composition that can be transdermally administrated by iontophoresis.

It is another object of the present invention to provide an effective

method for transdermal administration of ascorbic acid.

It is another object of the present invention to provide a method for

transdermal administration, which can penetrate ascorbic acid into skin in a

stable form.

It is still another object of the present invention to provide a skin-

care apparatus enabling smooth transdermal administration of ascorbic acid.

In order to achieve these objects, the present invention provides an

ascorbic acid composition for iontophoresis comprising: (a) 1 to 10wt% of a mixture comprising:

(i) 1 to 80wt% of additives comprising α -G-rutin, trehalose,

aloe vera gel and alantoin in a weight ratio of 1 -25 : 1 -50 :

1 -50 : 1 -50; and

(ii) 20 to 99wt% of metal phosphate salt of ascorbic acid; and

(b) 90 to 99wt% of water.

In addition, the present invention provides a method for transdermal

administration of ascorbic acid, which penetrates metal phosphate salts of

ascorbic acid into skin by ionotophoresis. The iontophoresis is preferably

conducted by placing one electrode on the skin coated with an aqueous

solution containing metal phosphate salts of ascorbic acid and constituting a

circuit with the skin, thereby penetrating metal phosphate salts of ascorbic

acid into skin, and more preferably, it is conducted by periodically generating

a positive voltage of 3 to 20v at a pulse of 10-100Hz and a negative voltage

of 3 to 20v at a pulse of 60-1 OOOHz and applying them to the skin at current

of 0.01 to 1 .0mA.

In addition, the present invention provides a skin-care apparatus

compπsing:

an electric source part to which an alternating current (AC) is input;

a processor part that is operated by direct current (DC) supplied from

the electric source part, and that controls the amplitude of vibration,

operation time, and iontophoresis current amount;

a resonance part that is connected to the electric source part by AC and causes pulses to resonate to ultrasonic waves;

an amplification part that amplifies the resonated pulses; and

an iontophoresis-vibration part that is connected to the amplification

part, and which enables iontophoresis and ultrasonic massage to be

conducted by way of a contact plate that is in contact with skin, whereby

vibrations are generated by surface-attached piezoelectric elements.

BRIEF DESCRIPTION OF THE DRAWINGS

Fig. 1 is a block diagram showing the skin-care apparatus of the

present invention.

Fig. 2 is a planar view of a vibration part of the skin-care apparatus

of the present invention.

Fig. 3 is a side view of a vibration part of the skin-care apparatus of

the present invention.

Fig. 4 shows the iontophoresis apparatus used in the present

invention.

Fig. 5 is a photo of a patient having melasma before medical

treatment according to the present invention.

Fig. 6 is a photo of the same person of Fig. 5 after administrating an

ascorbic acid composition of the present invention.

Fig. 7 is a photo of a patient having melasma before medical

treatment according to the present invention.

Fig. 8 is a photo of the same person of Fig. 7 after ultrasonic

cleansing and administration of an ascorbic acid composition according to the present invention.

Fig. 9 is a photo of a patient having acne before medical treatment

according to the present invention.

Fig. 10 is a photo of the same person of Fig. 9 after administrating

an ascorbic acid composition of the present invention.

Fig. 1 1 is a photo of a patient having acne before medical treatment

according to the present invention.

Fig. 12 is a photo of the same person after ultrasonic cleansing and

administration of an ascorbic acid composition.

Fig. 13 is a photo showing the appearance around wrinkles before

medical treatment according to the present invention.

Fig. 14 is a photo showing the same part of Fig. 13 after ultrasonic

cleansing and administration of an ascorbic acid composition.

10 electric source part 20 processor part

22 LED lamp 24 switch

30 resonance part 40 amplification part

50 iontophoresis part 60 vibration part

70 case 72 contact plate

74 piezoelectric elements 76 aluminum plate

78 ground part 80 sponge cover

DETAILED DESCRIPTION AND THE PREFERRED EMBODIMENTS

The present invention will now be explained in more detail.

The present inventors have discovered that if ascorbic acid is converted to its metal phosphate salt form and transdermally administrated

by iontophoresis, the metal phosphate salts of ascorbic acid can be rapidly

and effectively penetrated into the skin. Once there, the metal phosphate

salts are decomposed by enzymes and changed to ascorbic acid, which

exhibits unique functions such as melanin-formation inhibiting effects, etc.,

and the oxidation of the ascorbic acids can be prevented or inhibited even in

aqueous forms.

A metal phosphate salt of ascorbic acid can be prepared by reacting

ascorbic acid, phosphorous oxychloride and a metal chloride salt, or it is

available from Sigma Company in the US, and Wako Company or Niko

Company in Japan.

The metal phosphate salts of ascorbic acid is preferably selected

from a group consisting of sodium phosphate salt, magnesium phosphate

salt, calcium phosphate salt and potassium phosphate salt of ascorbic acid,

and magnesium phosphate salt is most preferable.

The metal phosphate salt of ascorbic acid used in the present

invention can be prepared by the following method.

An L-ascorbic acid is mixed with acetone and strength oleum at 0^°C ,

the mixture is stirred for 6 hours, its temperature is lowered to -15^°C , and the

obtained crystallized solids are vacuum-dried. The vacuum-dried mixture is

mixed with water and pyridine, POCI₃ is slowly added thereto at 0^°C , and the

mixture is stirred for 30 minutes while maintaining a pH at 13. Hydrated

magnesium chloride (MgCI₂- 6H₂0) is added to the mixture, and the mixture is stirred for 1 to 2 hours and the produced crystals are removed. Methanol

is added to the mixture, the resultant mixture is stirred for 1 hour and the

produced crystals are removed. The solution is then evaporated from the

mixture and MgO and water are added thereto and stirred while maintaining

the pH at 8.5 to 9. The mixture is added to methanol, and the produced

crystals are filtered and washed with methanol to obtain a magnesium

phosphate salt of ascorbic acid.

When the obtained metal phosphate salt of ascorbic acid, preferably

magnesium-L-ascorbyl-2-phosphate, is penetrated into bodies, phosphate

and magnesium leave the salt during passage through cell membranes, and

the salt changes into ascorbic acid (Vitamin C), thereby making its effects

available for skin.

The ascorbic acid composition for transdermal administration of the

present invention is prepared by mixing α -G-rutin, alantoin, aloe vera gel,

and trehalose with the metal phosphate salt of ascorbic acid prepared by the

above-explained method. The composition of the present invention

preferably comprises 1 to 10wt% of a mixture comprising 20 to 99wt% of

metal phosphate salt of ascorbic acid and 1 to 80wt% of additives, and 90 to

99wt% of water.

The additives preferably comprise α -G-rutin, alantoin, aloe vera gel,

and trehalose in a weight ratio of 1 -25 : 1 -50 : 1 -50 : 1 -50. The metal

phosphate salt of ascorbic acid is stable even in an aqueous solution and

thus it is not decomposed, and it forms a very stable composition that does not show discoloration or precipitation with surfactants.

The ascorbic acid composition for transdermal administration is

administrated into skin by iontophoresis. The present invention includes

iontophoresis, which passes currents through electrolyte comprising ionic

materials, thereby penetrating the ionic materials into body tissues, and an

electrophoresis, which applies a voltage to skin to transfer uncharged

materials into bodies.

One example of iontophoresis is a method for transdermal

administration of active ingredients by constituting a circuit by contacting one

electrode each of an anode and a cathode with skin coated with an aqueous

solution composition containing a metal phosphate salt of ascorbic acid, and

thereby administrating the metal phosphate salt of ascorbic acid by voltage

differences. Apparatus for conducting such iontophoresis are commonly

known in the art, and the structure and direction for use thereof are disclosed

in, as examples, U.S. Patent No. 5,314,502, and Korean Patent Nos. 1541 12,

192161 and 203225.

The method for transdermal administration of ascorbic acid of the

present invention is preferably conducted by periodically generating a

positive voltage of 3 to 20v at a pulse of 10-100Hz and a negative voltage of

3 to 20v at a pulse of 60-1 OOOHz, and applying them to skin at current of

0.01 to 1.0mA, while applying ultrasonic vibrations of 23-40kHz to skin at a

cycle of 1 -100Hz. If the voltage exceeds 20v, the epidermal layer of skin

may have hypersensitive responses due to chlorine or medicine, and if the voltage is less than 3v, the formed electric energy will be insufficient for the

metal phosphate salt of ascorbic acid to permeate the cell membrane of the

epidermal layer. Charged ascorbic acid salt penetrates into skin through

cell holes formed by electrical shock, and then phosphate salt is isolated by

phosphatase located on the intracellular membrane, which leaves only

ascorbic acid. The produced ascorbic acid reduces dopaquinone at a

melanocyte, which is an important intermediate of tyrosinase reaction, and

thus inhibits melanin formation thereby exhibiting pigment-removing effects.

In addition, it can prevent and remove wrinkles by accumulating collagen.

In addition, according to the iontophoresis of the present invention, a

transdermal administration rate of metal phosphate salt of ascorbic acid can

be increased, and additional effects of promoting dissolution and discharge

of waste products of skin are obtained by supplying currents to skin.

Accordingly, acne and melasma, which are continuously produced on the

surface of skin and cause skin troubles such as excretion difficulty in the

openings of sebaceous glands as well as skin-contaminations, can be

removed, and thus healthy skin can be maintained.

In addition, ultrasonic massage of skin preceding transdermal

administration of a metal phosphate salt of ascorbic acid by iontophoresis

may further improve transdermal administration effects of ascorbic acid. In

the present invention, ultrasonic vibrations are generated through 3 steps of

skin-cleansing in which ultrasonic vibrations of 20 to 40kHz with a weak

amplitude are generated, skin-scaling in which ultrasonic vibrations of 20 to 40kHz with a strong amplitude are generated, and lifting in which ultrasonic

waves of 20 to 40 kHz at a cycle of 1 -100Hz and a pulse current of 0.01 -

0.1 mA are generated. The lifting step can be conducted after iontophoresis.

The most preferable ultrasonic massage method comprises cleansing,

scaling, iontophoresis and lifting.

The ultrasonic massage according to the above method penetrates

ultrasonic energies into deep parts of bodies as well as skin tissues to

activate cells of skin, nerve, lymphatics, blood vessels and muscle layers,

and it promotes metabolism to elevate effects of ascorbic acid.

In addition, the present invention provides a skin-care apparatus for

transdermal administration of ascorbic acid. The skin-care apparatus of the

present invention comprises an electric source part to which an alternating

current (AC) electric source is input; a processor part that is operated by

direct current (DC) supplied from the electric source part, and that controls

the amplitude of vibrations, operation time and the amount of iontophoresis

current; a resonance part that is connected to the electric source part by AC

and causes pulses to resonate to ultrasonic waves; an amplification part that

amplifies the resonated pulses; and an iontophoresis-vibration part that is

connected to the amplification part, and which enables the iontophoresis and

ultrasonic massage to be conducted by way of a contact plate that is in

contact with skin, whereby surface-attached piezoelectric elements generate

vibrations.

The present invention will now be explained in more detail with reference to the desired embodiment.

Fig. 1 is a block diagram showing the skin-care apparatus of the

present invention.

An alternating current (AC) electric source is applied to an electric

source part (10), and the applied AC electric source is converted to DC or left

at AC and input in a processor part or a resonance part, as will be explained.

The processor part (20) is operated by DC that is input through the

electric source part (10), and it controls the vibration amplitude of pulses,

operation time and the amount of iontophoresis current.

In addition, an LED lamp (22) and a switch (24) are connected to the

processor part (20), and the degree of operation progress of ultrasonic

cleansing of skin or iontophoresis and the skin-care step in progress can be

identified.

The resonance part (30) comprises a coil and a condenser, and it

causes a resonance when the frequency of the electric source concurs with

a characteristic frequency.

At this time, the frequency that is resonated to its maximum by the

resonance part is amplified to a degree of 20 to 40kHz, and more preferably

to 25 kHz, at an amplification part (40).

An iontophoresis-vibration part is divided into an iontophoresis part

(50) and a vibration part (60), and they have a contact plate (72) in common,

where current is communicated with the amplification part (40) inside a case

(70), as shown in Figs. 2 and 3. The contact plate (72) is made of stainless steel that is harmless to

human bodies and has a good contact feel.

Specifically, on the front end of the contact plate (72), which directly

contacts human bodies, a coating film made of titanium nitride (TiN) or

zirconium nitride (ZrN) is formed so as to protect skin that is sensitive to

metals and that shows allergic responses.

The coating film can be deposited using a Chemical Vapor

Deposition method that is used in semiconductor processes, or a sputtering

method.

An aluminum plate (76) where piezoelectric elements (74) are fixed

is attached to the upper and lower sides of the contact plate (72), as shown

in Fig. 3, and the aluminum plate can be replaced by duralumin.

A circuit for iontophoresis is connected to the stainless steel contact

plate, and a circuit for ultrasonic cleansing is connected to the piezoelectric

elements (74).

Thus the ultrasonic cleansing can be individually conducted, or the

ultrasonic massage and the iontophoresis can be simultaneously conducted.

A ground part (78) can be connected to the contact plate (72). By

current communication with the ground part (78), the current of one electrode

from the electric source part (10) is transferred via a contact plate (72) to the

contacted skin and reaches to the other electrode in the ground part (78) that

is held by hand to form a circuit.

The electrodes of the electric source (10) and the ground part (78) can be positive voltage/negative voltage or negative voltage/positive voltage.

Meanwhile, a sponge cover (80) can be inserted into the front end of

the contact plate (72), which is used when transdermally administrated

agents such as medicines, cosmetics or an ascorbic acid composition, etc.

are penetrated into skin by iontophoresis.

Specifically, the sponge cover (80) is inserted into the front end of

the contact plate (72), and the front end is dampened with the ascorbic acid

composition of the present invention so that the aqueous solution can be

absorbed in the sponge cover (80), under which condition the iontophoresis

is conducted.

It is preferable to form inserting grooves on both sides of the front

end so that the sponge cover (80) can be securely inserted in the front end

of the contact plate (72).

With the skin-care apparatus of the present invention, skin-care can

be performed in 4 modes, as will be explained.

The 4 skin-care modes include a cleansing mode, a scaling mode, a

vitamin mode and a lifting mode, among which the cleansing and scaling

modes use ultrasonic waves, and the vitamin and lifting modes use both

ultrasonic waves and iontophoresis.

When a cleansing mode is selected after supplying an electric

source to the electric source part (10), the processor part (20) controls the

vibration amplitude of ultrasonic waves and operation time suitable for the

cleansing mode. Thus resonance is generated in the resonance part (30) to become

vibrations of 20 to 40kHz with a weak amplitude, and the contact plate (72)

begins to vibrate as the piezoelectric elements (74) vibrate.

Next, prepared clean water is applied to the skin in a suitable amount,

and the front end of the contact plate is adhered closely to the skin and

vibrations are applied for 5 minutes while maintaining the angle between the

front end of the contact plate and skin surface at 45° .

In the case of a scaling mode, vibrations of 20 to 40kHz with a strong

amplitude are applied to the skin for 5 minutes.

In the case of a vitamin mode, it is preferable to periodically generate

a positive voltage of 3 to 20v at a pulse of 10-100Hz and a negative voltage

of 3 to 20v at a pulse of 60-100Hz, and to apply current of 0.01 to 1.0mA to

the skin, while applying ultrasonic vibrations of 23-40kHz with a cycle of 1 to

100Hz for 10 minutes.

If the voltage exceeds 20v, the epidermal layer of the skin may have

hypersensitive response due to chlorine or medicine, and if it is less than 3v,

the formed energies will be insufficient for the metal phosphate salt of

ascorbic acid to penetrate cell membranes of the epidermal layer.

When conducting the vitamin mode, the sponge cover (80) covers

the front end of the contact plate (72), and it is dampened with the ascorbic

acid composition.

At this time, iontophoresis and ultrasonic massage can be

simultaneously conducted since the iontophoresis and vibration are simultaneously employed.

Particularly, if the ground part (78) is held by hand, ascorbic acid will

be penetrated into the skin by the current.

Finally, in the case of the lifting mode, a moisturizing agent is

sufficiently and uniformly applied to the face, and vibrations of 23 to 40kHz

with a cycle of 1 to 100Hz and a pulse current of 0.01 to 1.0mA/cm², are

applied to the skin for 10 minutes. At this time, face muscles are tensed

and released at a most optimal frequency, which results in the highest

massaging effects.

The present invention will be explained in more detail with reference

to the following Example. However, the Example is to illustrate the present

invention and the present invention is not limited thereto.

[Example 1]

Preparation of Magnesium Ascorbyl Phosphate

480 in? of acetone and 43g of strength oleum were added to 120g of

L-ascorbic acid at 0^°C , and the mixture was stirred for 6 hours, cooled to -

15^°C and the formed crystals were vacuum-dried. 1.2 liters of water and

300 in-? of pyridine were mixed with the vacuum-dried mixture, 146g of POCI₃

were slowly added thereto at 0^°C , and the mixture was stirred for 30 minutes

at a pH of 13. 70g of hydrated magnesium chloride (MgCI₂ ^• 6H₂0) were

added thereto and the mixture was stirred for 2 hours and then filtered. 1

liter of methanol was added to the filtrate, the filtrate was stirred for 1 hour and filtered, and solutions were evaporated from the filtrate. 39g of MgO

were added thereto with water and stirred while maintaining pH at 8.5 to 9.

The mixed solution was slowly added to 1.2 liters of methanol, and the

obtained crystals were filtered and washed with 300 mi of methanol to obtain

magnesium ascorbyl phosphate.

Preparation of Composition for Transdermal Administration

0.2g of the prepared magnesium ascorbyl phosphate, 0.02g of α -G-

rutin, 0.1 g of alantoin, 0.1 g of aloe vera gel, 0.1 g of trehalose and 5g of

water were mixed to prepare an ascorbic acid composition for transdermal

administration.

Iontophoresis Treating Method

Fig. 4 shows the iontophoresis device used in the present invention,

which comprises an electric source part (1 ), 6 piezoelectric elements (2), a

stainless steel plate ((3):SUS), and a bar (4). One electrode current from

the electric source part is transferred via the stainless steel plate to the

contacted skin, and it reaches another electrode in a hand-held bar to form a

circuit. At this time, the electrodes of the electric source part and the bar

can be positive voltage/negative voltage or negative voltage/positive voltage.

In addition, the iontophoresis device of Fig. 4 can tansdermally

transfer ultrasonic vibrations using piezoelectric elements and thus it can be

used in ultrasonic massage.

A method for transdermal administration of the ascorbic acid

composition by iontophoresis was conducted as follows: 3 to 10 i of the ascorbic acid composition were coated on the face,

a positive voltage of 3 to 20v at a pulse of 60Hz and a negative voltage of 3

to 20v at a pulse of 500Hz were periodically generated and applied to skin at

a current of 0.01 to 1.0mA. These operations were conducted twice a week.

[Example 2]

Directions for Use of the Apparatus

Ultrasonic cleansing and iontophoresis were conducted using the

apparatus of Fig. 4 as follows:

(1 ) Cleansing : Water was applied to skin and vibrations of 25kHz

with a weak amplitude were applied to the skin for 5 minutes.

(2) Scaling : Vibrations of 25kHz with a strong amplitude were

applied to the skin for 5 minutes.

(3) Vitamin : Ultrasonic vibrations of 25kHz were applied to the skin

for 10 minutes at a cycle of 10Hz, while applying pulse current of

0.05 to 0.5mA/cm2 to skin and contacting sponge dampened with

vitamin C solution with skin.

(4) Lifting : Pulse AC current of 0.01 -0.1 mA and ultrasonic vibrations

of 25kHz with a cycle of 10Hz were applied to skin for 10 minutes.

[Experiment]

The ascorbic acid was transdermally administrated to persons

having serious melasma, acne or wrinkles twice a week, according to the

methods of Example 1 and 2. After 1 month and 2 months had elapsed, the

effects were observed. The results are presented in Table 1 . The degree of effects were measured by the naked-eye and gave 0 points for the poorest,

and 10 points for the best.

[Table 1]

Figs. 5 to 14 are photos showing the results of Table 1. Fig. 5

shows the appearance of a patient having melasma before treating with the

ascorbic acid composition, and Fig. 6 shows the same person after treating

with the ascorbic acid composition for 2 months. Fig. 7 shows the

appearance of a patient having melasma before treating with the ascorbic

acid composition, and Fig. 8 shows the same person after treating with the

ascorbic acid composition and ultrasonic cleansing for 2 months. Fig. 9

shows the appearance of a patient having acne before treating with the

ascorbic acid composition, and Fig. 10 shows the same person after treating

with the ascorbic acid composition for 2 months. Fig. 11 shows the

appearance of a patient having acne before treating with the ascorbic acid composition, and Fig. 12 shows the same person after treating with

ultrasonic cleansing and the ascorbic acid composition for 2 months. Fig.

13 shows the appearance around wrinkles before treating with the ascorbic

acid composition, and Fig. 14 shows the appearance of the same part after

treating with ultrasonic cleansing and the ascorbic acid composition for 2

months. It can be seen that the ascorbic acid composition of the present

invention showed excellent effects for removing melasma, acne and wrinkles,

and simultaneous ultrasonic cleaning improved the effects.

As stated above, according to the present invention, the ascorbic

acid composition is transdermally administrated by iontophoresis using a

skin-care apparatus, thereby exhibiting the effects of melasma removal, acne

removal, sebaceous matter removal, wrinkle removal, skin aging prevention

and whitening.

In addition, ultrasonic cleaning preceding the transdermal

administration of ascorbic acid by iontophoresis causes synergetic effects for

skin beauty.

Claims

WHAT IS CLAIMED IS:

1. An ascorbic acid composition for inotophoresis comprising:

(a) 1 to 10wt% of a mixture comprising:

(i) 1 to 80wt% of additives comprising α -G-rutin, trehalose, aloe

vera gel and alantoin in a weight ratio of 1 -25 : 1 -50 : 1 -50 : 1 -50; and

(ii) 20 to 99wt% of a metal phosphate salt of ascorbic acid; and

(b) 90 to 99wt% of water.

2. The ascorbic acid composition for inotophoresis according to claim 1 ,

wherein the metal phosphate salt of ascorbic acid is selected from a group

consisting of sodium ascorbyl phosphate, magnesium ascorbyl phosphate,

calcium ascorbyl phosphate and potassium ascorbyl phosphate.

3. The ascorbic acid composition for inotophoresis according to claim 1 ,

wherein the metal phosphate salt of ascorbic acid is magnesium ascorbyl

phosphate.

4. A method for transdermal administration of ascorbic acid, characterized

in that a metal phosphate salt of ascorbic acid is penetrated into skin by

inotophoresis.

5. The method for transdermal administration of ascorbic acid according to

claim 4, wherein the inotophoresis is conducted by placing one electrode on

skin that is coated with an aqueous solution composition comprising a metal

phosphate salt of ascorbic acid and constituting a circuit with the skin,

thereby penetrating a metal phosphate salt of ascorbic acid into the skin.

6. The method for transdermal administration of ascorbic acid according to

claim 4, wherein the inotophoresis is conducted by periodically generating a

positive voltage of 3 to 20v at a pulse of 10-100Hz and a negative voltage of

3 to 20v at a pulse of 60-1 OOOHz, and applying them to skin at current of

0.01 to 1.0 mA, while applying ultrasonic vibrations of 23-40kHz to skin at a

cycle of 1 -100Hz.

7. The method for transdermal administration of ascorbic acid according to

claim 5, wherein the aqueous solution composition comprises:

(a) 1 to 10wt% of a mixture of

(i) 20 to 99wt% of a metal phosphate salt of ascorbic acid; and

(ii) 1 to 80wt% of additives; and

(b) 90 to 99wt% of water.

8. The method for transdermal administration of ascorbic acid according to

claim 7, wherein the additives comprise α -G-rutin, trehalose, aloe vera gel

and alantoin in a weight ratio of 1 -25 : 1 -50 : 1 -50 : 1 -50.

9. The method for transdermal administration of ascorbic acid according to

claim 4, wherein the metal phosphate salt of ascorbic acid is selected from a

group consisting of sodium ascorbyl phosphate, magnesium ascorbyl

phosphate, calcium ascorbyl phosphate, and potassium ascorbyl phosphate.

10. The method for transdermal administration of ascorbic acid according

to claim 4, further comprising the step of ultrasonic cleansing of the skin

before conducting the iontophoresis.

1 1. The method for transdermal administration of ascorbic acid according to claim 10, wherein ultrasonic vibrations are generated through the following

steps:

a skin-cleansing step in which ultrasonic vibrations of 20 to 40 kHz

with a weak amplitude are generated;

a skin-scaling step in which ultrasonic vibrations of 20 to 40 kHz with

a strong amplitude are generated; and

a lifting step in which ultrasonic vibrations of 20 to 40 kHz with a

cycle of 1 -100Hz and a pulse current of 0.01 -0.1 mA are generated.

12. The method for transdermal administration of ascorbic acid according

to claim 4, further comprising a ultrasonic cleansing step before conducting

the iontophoresis and a lifting step after the iontophoresis.

13. The method for transdermal administration of ascorbic acid according to

claim 12, wherein the ultrasonic vibrations are generated through the

following steps:

a skin-cleansing step in which ultrasonic vibrations of 20 to 40 kHz

with a weak amplitude are generated; and

a skin-scaling step in which ultrasonic vibrations of 20 to 40 kHz with

a strong amplitude are generated.

14. A skin-care apparatus comprising:

an electric source part to which an alternating current (AC) electric

source is input;

a processor part that is operated by direct current (DC) supplied from

the electric source part, and that controls the amplitude of vibrations, operation time and an amount of iontophoresis current;

a resonance part that is connected to the electric source part by

alternating current (AC) and causes pulses to resonate to ultrasonic waves;

an amplification part where the resonated pulses are amplified; and

an iontophoresis-vibration part that is connected to the amplification

part, and that enables the iontophoresis and ultrasonic cleansing to be

conducted by way of a contact plate that is in contact with skin, whereby

vibrations are generated by piezoelectric elements attached to its surface.

15. The skin-care apparatus according to claim 14, further comprising a

ground part that is connected to the contact plate.

16. The skin-care apparatus according to claim 14, further comprising a

sponge cover that is inserted into an end of the contact plate, when

transdermally administrated agents are penetrated into skin by iontophoresis.

17. The skin-care apparatus according to claim 16, wherein an insert

groove is formed on both sides of the contact plate.

18. The skin-care apparatus according to claim 14, wherein a coating film

made of titanium nitride or zirconium nitride is formed on a front end of the

contact plate that is in contact with skin.