KR101200565B1 - Composition containing Codonopsis lanceolata extract for topical administration - Google Patents

Abstract

The present invention provides a topical formulation for applying dermat extract containing skin, which is secured in formulation stability and has an excellent release amount of a main drug.

Deodeok Extract, Topical Formulation, Release

Description

Composition containing Codonopsis lanceolata extract for topical administration

The present invention relates to a topical application formulation for skin application containing deodeok extract.

With increasing interest in skin and the development of technology, cosmetic research trends have shifted from simply focusing on moisturizing, protecting, and using the skin to emphasizing functional effects on the skin. It introduced the concept of functional cosmetics (cosmeceuticals) into the cosmetics industry, which is intended to be a medicinal product beyond the concept of cosmetics. In Korea, the market of functional cosmetics has been applied since 2000. Functional cosmetics are cosmetics that emphasize functional effects on the skin such as whitening, anti-aging, acne, and cosmetics that have been proven to be more effective than general cosmetics, and thus, researches on these functional cosmetics are being conducted in the field of medicine research.

In addition, there are many researches on topical application to the skin as a number of skin diseases have not been revealed in recent years, and in this case, as well as affinity with the skin, safety and stability of the product, Emissions should be secured.

Codonopsis lanceolata ) is a perennial herb belonging to the lantern family that grows or grows in the high mountains of Korea, China, and Japan, and is called by various names such as white ginseng, sasam ginseng, leaf, virtues, and jiji. Deodeok has been known for its excellent pharmacological effects such as tonic, fever, Jinhae, expectoration, detoxification and drainage. Deodeok root contains a lot of saponin, which has a unique scent, which helps to cough, cut phlegm, and is recognized as a good food for bronchitis, tonsillitis, and sore throat. In addition, the deodeok extract cleans the stratum corneum on the outermost surface of the skin, so it has good cosmetic properties for rough skin on the surface, and melanin production inhibitory effect is also being studied.

Homogeneous semi-solid external preparations, ointments, etc., which are easily applied to the skin, are composed of base and main medicine, and base is divided into hydrophobic base and hydrophilic base according to its physical properties. Hydrophobic bases are also referred to as oleaginous bases and are mineral and plant-like. Vaseline, paraffin, plastibase, and the like may be used for the mineral hydrophobic base, and vegetable and vegetable bases may include lead oils such as vegetable oil, wax, and beeswax, iron oil, and pork oil. Hydrophilic bases include emulsion bases and water soluble bases. There are two types of emulsion bases: oil-in-water, such as varnishing cream, and water-in-oil, such as cold cream.

In the development of topical application formulations containing deodeok extracts using these various types of formulations, the release of deodeok extracts from the preparation is the most important factor in determining the efficacy on the skin. The release of deodeok extract from topical skin application formulations, especially semi-solid formulations that are easy to apply to the skin, is thought to be influenced by many factors, including the composition of the semi-solid formulation, the solubility of the extract, the particle size of the emulsion, and the water content. . That is, in order to apply topically to the skin, the main drug should be released from the preparation for the efficacy and safety of the product, and the amount of the main drug released varies greatly depending on the physical properties of the drug, the type of external preparation, and the base component.

Therefore, the technical problem to be solved by the present invention is to provide a topical application formulation containing a deodeok extract with a stable formulation while having a good release, that is, excellent skin transfer efficiency.

In order to achieve the above technical problem, the present invention contains the deodeok extract as an active ingredient, the topical application containing the deodeok extract of oil-in-water emulsion type, characterized in that it comprises a deodeok extract in the water phase of the trauma Provide formulations.

The present invention also provides a Deodeok extract-containing topical application formulation containing Deodeok extract as an active ingredient and using polyethylene glycol as a main base.

The inventors of the present invention have attempted to prepare semi-solid preparations containing Deodeok extract, in particular, water-soluble extracts of Deodeok, and in particular, the formulation stability is secured, and as a result of the effort to produce a topical application formulation of the release of the Deodeok extract, the topical application formulation In particular, the invention was invented that the semi-solid formulation using polyethylene glycol as a main agent has an excellent effect on the release of the deodeok extract.

Formulations such as hydrophilic cream, O / W type emulsion cream, W / O type emulsion cream, lipophilic cream, etc. are prepared with various topical application formulations containing Deodeok extract. Evaluated. As a result of evaluating the amount of release, the release rate was higher in order of the hydrophilic cream-based polyethylene glycol base formulation, the O / W emulsion cream formulation consisting of specific ingredients, the W / O cream formulation, and the lipophilic cream formulation. The formulation was preferred as a topical application of the deodeok extract, and in particular, the topical formulation prepared using the polyethylene glycol base was the best in formulation stability during the manufacturing process, release of the deodeok extract, and the like.

The oil-in-water emulsion formulation of the present invention is preferably composed of an oil phase including polyglyceryl-3-methylglucose distearate, stearic acid, cetyl alcohol and liquid paraffin and an aqueous phase containing glycerin, except for deodeok extract. 1-5% by weight of polyglyceryl-3-methylglucose distearate, 2-10% by weight stearic acid, 0.5-3.5% by weight cetyl alcohol, 3-10% by weight liquid paraffin, 6-14% by weight glycerin And a residual amount of water is more preferred.

In addition, in the topical application formulation using the polyethylene glycol of the present invention, the polyethylene glycol is preferably a mixture of polyethylene glycol 400 and polyethylene glycol 4000, and 50 to 70% by weight of polyethylene glycol 400, polyethylene glycol 4000 20 based on the total weight of the formulation except the deodeok extract. More preferably consisting of -40% by weight and residual water.

Topical application formulations of the present invention may include, but are not limited to, other ingredients such as flavoring agents, colorants, stabilizers, pH adjusting agents, etc. without departing from the object of the present invention.

The present invention provides a topical application formulation containing Deodeok extract, which is secured in formulation stability and has an excellent release amount of the main drug.

Hereinafter, embodiments of the present invention will be described in detail to facilitate understanding of the present invention. However, embodiments according to the present invention can be modified in many different forms, the scope of the invention should not be construed as limited to the following examples. Embodiments of the present invention are provided to more fully describe the present invention to those skilled in the art.

Example 1 Preparation of Deodeok Extract

Deodeok extract was prepared as follows. Codonopsis lanceolata ) was cut and extracted for 12 hours using hot water at 90 ° C. at a rate of 20 g / 500 ml. Filter filtration to remove insoluble matter, hexane was added and shaken at room temperature. Thereafter, the hexane layer was removed, chloroform was further added to the aqueous layer, shaken at room temperature, and the chloroform layer was removed. Thereafter, ethyl acetate was added to the aqueous layer, followed by shaking at room temperature, and the ethyl acetate layer was removed. After shaking with butanol in the same manner, the butanol layer was removed to obtain an aqueous layer. Thereafter, the aqueous layer was dried under reduced pressure to obtain a final deodeok extract, which was used in the following examples.

Example 2 Evaluation of Solubility of Deodeok Extract

To evaluate the solubility of the deodeok extract and to evaluate the comparison with the results of the release experiment obtained in the following examples to design an external agent having an optimum release efficiency. To select an appropriate test solution in the in vitro release test, the solvent was tested using purified water, ethanol, acetonitrile and methanol. An excess of Deodeok extract was added to the test solution, followed by shaking and agitation. After 12 hours, the test solution was filtered to evaluate the solubility of the Deodeok extract with an ultraviolet visible absorption spectrophotometer.

As a result, the deodeok extract was found to be most easily dissolved in purified water. Float was seen in the remaining solvent. With reference to these results and the extract manufacturing process, it was confirmed that the deodeok extract used in the present invention is water-soluble. More than about 0.5-1 g of Deodeok extract could be dissolved in 1 ml of purified water.

Example 3 Preparation of Deodeok Extract-Containing Semi-Solid Formulations

Four cream formulations were prepared, namely O / W creams, W / O creams, hydrophilic creams and lipophilic creams, in order to evaluate the release properties of the deodeok extracts from the various solubility preparations. In all cases, the content of deodeok extract was fixed at 3% by weight, and the preparation methods of O / W cream, W / O cream, hydrophilic cream and lipophilic cream were as follows.

O / W Cream

O / W cream was prepared according to the formulation of Table 1 below. Polyglyceryl-3-methylglucos distearate, stearic acid, cetyl alcohol and liquid paraffin were added as prescribed and warmed at 65 ° C. to prepare an oil phase. Glycerin, purified water and Deodeok extracts were added and warmed at 65 ° C to completely dissolve the aqueous phase. The oil phase was added to the water phase at the same temperature, emulsified for several minutes using a homogenizer, and cooled to prepare an O / W cream.

ingredient weight% Polyglyceryl-3-methylglucose distearate 3 Stearic acid 5 Cethyl alcohol 2 Mineral oil 7 Glycerin 10 Water 73

W / O Cream

W / O cream was prepared according to the prescription of Table 2 below. An aqueous phase in which the deodeok extract was dissolved at 65 ° C was prepared. Sesquioleic acid sorbitan, Tween 80, liquid paraffin, white petrolatum and cetyl alcohol are completely dissolved at 65 ° C. according to the prescription to prepare an oil phase, and the aqueous phase is put into an oil phase and emulsified for a few minutes using a homogenizer for W / O cream. Was prepared.

ingredient weight% Sorbitan sesquioleate 4 Tween 80 6 Paraffin liquid 8 Vaseline 12 Cethyl alcohol 20 Water 50

Hydrophilic cream

Hydrophilic creams were prepared according to the formulation of Table 3 below. After polyethylene glycol 400 and polyethylene glycol 4000 were completely dissolved by heating at 70 ° C., the aqueous phase in which the extracts were dissolved was added to the polyethylene glycol mixture at the same temperature, followed by sufficient stirring. Stirring was continued until solidification while cooling to 30 ° C. to prepare a hydrophilic cream.

ingredient weight% Polyethylene glycol 400 60 Polyethylene glycol 4000 30 Water 10

Lipophilic  cream

A lipophilic cream was prepared according to the formulation of Table 4 below. The white petrolatum was warmed at 70 ° C. to completely dissolve it, and the liquid paraffin containing Deodeok extract was dissolved at 70 ° C., and then added to the white petrolatum and stirred sufficiently. Stirring was continued until it solidified cooling to 30 degreeC, and the lipophilic cream was manufactured.

ingredient weight% Vaseline 90 Paraffin liquid 10

Example 4 Evaluation of Release of Deodeok Extract from Semi-Solid Formulations

When evaluating drug release and / or transdermal absorption of external preparations, appropriate animal skin such as mice or various synthetic polymer membranes having properties similar to those of actual skin are used as diffusion membranes. Especially, in vitro diffusion using semipermeable membranes as synthetic polymer membranes is used. Experiments were often used in drug release experiments. Therefore, in this embodiment, the release aspect of the prepared cream formulation (O / W cream, W / O cream, hydrophilic cream and lipophilic cream) containing the deodeok extract was evaluated by the Immersion method using a cellulose membrane. In order to evaluate whether the extract is continuously released, the sampling time of the sample was up to 4 hours.

The used cellulose membrane was previously activated in phosphate buffer. A cylindrical polypropylene tube (3.2 cm in diameter, 11.5 cm in length) was used to measure the release of Deodeok extract in a shake incubator. Put the cream of each prescription into the dialysis membrane and seal it at both ends into a cylindrical polypropylene tube filled with 50 ml of pH 7.4 isotonic phosphate buffer, stirring the shake incubator at 50 rpm to evaluate the continuous release. After holding, 1 ml of release medium was taken at 0.5, 1, 2, 3 and 4 hours. The same amount of medium was replenished at each collection. The collected sample was filtered with a 0.45 um syringe filter, which was analyzed at 240 nm using an ultraviolet-visible spectrophotometer. The same experiment was repeated three times and the average value was shown in FIG. 2, and the experimental apparatus used for the release experiment is shown in FIG. 1.

As shown in Figure 2, the release amount of each of the four cream formulations containing the deodeok extract was measured, about 4 hours after the start of the release experiment in the order of hydrophilic cream, O / W cream, W / O cream and lipophilic cream Emissions of 74%, 44%, 24% and 18% are shown. As a result of evaluating the release pattern of the O / W cream, the release rate was 15% at 30 minutes, 26% at 60 minutes, 41% at 120 minutes, and 45% at 180 minutes. The emission amount was%. The release of W / O cream was 6% at 30 minutes, 11% at 60 minutes, 18% at 120 minutes, 22% at 180 minutes, and 24% at 240 minutes. Finally, about 20% of the emission amount was about half that of the O / W cream. The release pattern of the hydrophilic cream was 7% at 30 minutes, 18% at 60 minutes, 30% at 120 minutes, 41% at 180 minutes, and 74% at 240 minutes. After 1 hour, the release rate increased rapidly and after 3 hours, the emission rate increased rapidly. . The release of lipophilic cream was 1% at 30 minutes, 9% at 60 minutes, 11% at 120 minutes, 14% at 180 minutes and 18% at 240 minutes.

As shown in the above results, as a topical application of the deodeok extract, O / W cream and hydrophilic cream were preferred. In addition, comparing the release pattern of the deodorant extract of O / W cream and hydrophilic cream, hydrophilic cream showed a continuous increase, while O / W cream increased up to about 2 hours, but the release after 2 hours It did not increase much and was less desirable than hydrophilic creams.

For the W / O cream formulation and the lipophilic cream formulation, only about one half of the O / W cream formulation and about one quarter of the hydrophilic cream formulation were based on 4 hours. In the case of the W / O cream formulation and the lipophilic cream formulation, it is assumed that the oily ingredient surrounding the deodeok extract acted as a diffusion barrier of the deodeok extract.

1 is a device for evaluating the release of a deodeok extract containing topical formulation according to the invention. In Figure 1, A is a deodorant extract-containing cream formulation, B is a dialysis membrane, C is a sieve, D is a shaking incubator, E is a phosphate buffer, and F is a weighted closure. , G denotes a cylindrical polypropylene tube.

Figure 2 is a graph showing the results of the release experiment of the deodeok extract containing topical application formulations. In Figure 2 ◆ indicates an O / W cream formulation, ▲ indicates a W / O cream formulation, □ indicates a hydrophilic cream formulation, and × indicates a lipophilic cream formulation.

Claims (4)

delete delete Comprising the deodeok extract as an active ingredient and formulating it based on polyethylene glycol, Polyethylene glycol is a mixture of polyethylene glycol 400 and polyethylene glycol 4000, A method for preparing a topical formulation containing deodeok extract, characterized in that sustained release of the deodeok extract in a topical formulation. delete

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