WO2007078117A1 - Extract of gentianae macrophyllae radix for the treatment of dermatological diseases - Google Patents

Extract of gentianae macrophyllae radix for the treatment of dermatological diseases Download PDF

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Publication number
WO2007078117A1
WO2007078117A1 PCT/KR2006/005868 KR2006005868W WO2007078117A1 WO 2007078117 A1 WO2007078117 A1 WO 2007078117A1 KR 2006005868 W KR2006005868 W KR 2006005868W WO 2007078117 A1 WO2007078117 A1 WO 2007078117A1
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Prior art keywords
extract
gentianae macrophyllae
macrophyllae radix
treatment
radix
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PCT/KR2006/005868
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French (fr)
Inventor
Wie-Jong Kwak
Yong-Baik Cho
Chang-Kyun Han
Eun Ju Lee
Joo Hyon Kim
Se Jun Yun
Soon Keun Lee
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Sk Chemicals Co., Ltd.
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Publication of WO2007078117A1 publication Critical patent/WO2007078117A1/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/51Gentianaceae (Gentian family)
    • A61K36/515Gentiana
    • 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
    • A61P17/06Antipsoriatics

Definitions

  • the present invention relates to an extract of Gentianae macrophyllae radix useful for the treatment of dermatological diseases, in particular, an extract of Gentianae macrophyllae radix which has an excellent inhibitory effect on epidermal hyperplasia thus being useful for the prevention and treatment of dermatological diseases such as psoriasis.
  • Psoriasis is a dermatological disease which is characterized in that a patient's epidermal surface is covered with whitish scaly skin cells thus clearly marking its boundary with the neighboring skin, and also producing scabs with various sizes in red spots which grow bigger as time passes. This disease often develops on the skins of elbows, knees, buttocks, head and also on hands and soles. The above skin areas appear to be more frequently affected than other parts of a body. Psoriasis develops regardless of a sex and occurs most highly in people in their early 20s.
  • Psoriasis is a progressive and chronic disease, which often recurs and is hardly cured completely once it is developed. Although many people have been suffering from chronic dermatological diseases such as psoriasis, there has not been developed any good cure for the treatment of the above diseases and only deterioration of the seriousness of the above diseases has been merely wished. Therefore, it is essential to develop a good therapeutic pharmaceutical drug with an excellent mechanism of action for the treatment of the above diseases. However, neither the main cause nor the substance, which may trigger the development of cures for the diseases, has been clearly identified and thus the developmental procedure of the therapeutic pharmaceutical agent has been long deterred.
  • the Gentianae macrophyllae radix used in the present invention is a perennial plant having a height of 40 - 60 cm and a strong but unelastic root. It is widely distributed in China such as Heilongjiang, Liaoning, Hebei, Heinan, Sichuan provinces. They are collected in Spring and Autumn.
  • the plants may be dried in the sunlight after removing stovers, fibrous roots and soils, or dried after piling them together. In general, when they become reddish yellow or yellowish gray they are scattered and dried in the sunlight.
  • the present invention relates to a therapeutic pharmaceutical agent comprising an extract of Gentianae macrophyllae radix as an active ingredient for the treatment of epidermal hyperplasia.
  • the present invention relates to an extract of crude Gentianae macrophyllae radix having an excellent inhibitory effect on epidermal proliferation of skin thus being useful for the prevention and treatment of dermatological diseases such as psoriasis.
  • the present invention relates to a method of preparing an extract of crude Gentianae macrophyllae radix comprising:
  • Gentianae macrophyllae radix is added with water or an aqueous alcohol solution and extracted under reflux for 2-5 hours.
  • the amount of water used is preferably in the range of 10-15 times of the weight of the Gentianae macrophyllae radix.
  • the mixture undergoes filtration and the resulting filtrate is collected.
  • water or an aqueous alcohol solution in the amount of 7-12 times of the weight of the Gentianae macrophyllae radix is added to the resulting residue, and the mixture is heated.
  • the mixture is reextracted for 2-5 hours, filtered and the resulting filtrate is combined with the filtrate obtained previously thereby increasing the extraction efficiency.
  • extraction is performed twice, i.e., first extraction and re- extraction. This is because a single extraction in the case of a large scale production of extract may not guarantee relatively high extraction efficiency due to a great loss in water content contained in the crude drug itself during the extraction process, and by conducting a reextraction the resulting extract efficiency can be greatly increased.
  • the extract obtained by the double extraction using water or an aqueous alcohol solution is filtered and concentrated. Then impurities such as unnecessary proteins, polysaccharides, and fatty acids contained in the resulting concentrated filtrate are purified.
  • the filtrate is purified by fractionation of the filtrate 2-4 times and obtaining a solvent fraction using a low grade alcohol or a nonpolar solvent which is equal in amount to that of the filtrate.
  • a low grade alcohol is preferably a C1-C6 alcohol, more preferably butyl alcohol, propyl alcohol and isopropyl alcohol.
  • a nonpolar solvent may be selected from the group consisting of ethyl acetate, dichloro methane, chloroform, carbon tetrachloride, and methylethylketone.
  • the amount of the low grade alcohol or the nonpolar solvent is less than that of the filtrate, it forms granules from unnecessary components such as fatty acid thereby preventing a smooth separation of layers and also decreasing the content of active ingredients contained in the extract.
  • the purpose of using water in performing azeotropic concentration in this process is to effectively control the amount of the residual low grade alcohol for use of a crude drug extract as a source for a pharmaceutical agent.
  • the above extract then undergoes lyophilization and the final extract in the form of powder is obtained.
  • the extract has an excellent inhibitory effect on epidermal proliferation and is thus expected to be useful as a therapeutic pharmaceutical agent for the prevention and treatment of dermatological diseases such as psoriasis.
  • the extract of Gentianae macrophyllae radix prepared according to the present invention is formulated in the form of tablets, capsules, injections and the like.
  • the ratio between the combined amount of excipients, such as lactose, microcrystalline cellulose, magnesium stearate, and the amount of the above extract is preferred to be 2: 1 to attain a desired pharmaceutical activity for the prevention and treatment of dermatological diseases.
  • Crude drugs themselves may be directly used as pharmaceutical agents. However, they may be combined with pharmaceutically acceptable additives such as a carrier, a forming agent, or a diluent to be prepared in the form of powder, granules, capsules, injections and the like.
  • pharmaceutically acceptable additives such as a carrier, a forming agent, or a diluent to be prepared in the form of powder, granules, capsules, injections and the like.
  • the extract of Gentianae macrophyllae radix has been long used as a food or an oriental medicine. There has been no particular limitation on its dosage but its dosage may vary depending on the rate of body absorption, body weight, age, sex, health conditions, dosage time, type of administration, excretion rate, seriousness of diseases of a subject.
  • the extract of Gentianae macrophyllae radix is preferably administered about 0.1 - 10 mg/kg. Therefore, the extract comprising the active ingredient of the present invention may be manufactured in consideration of the effective dosage.
  • the formulated unit dosage prepared thereof can be administered once or a few times at regular intervals daily by means of specialized administration, upon necessity, according to the advice and/or the request of a specialist or a supervisor who monitors and supervises drug administration.
  • Each group consisted of 2 rats. They were orally respectively administered with the extract of Gentianae macrophyllae radix prepared in Preparation Examples 1 and 2 with a dosage of 1 g/kg/mL once. After the administration, the rats were observed of their deaths, clinical symptoms, and weight changes. Further, hematological test and hematobiochemical test were conducted and abnormalities on abdominal and pectoral organs were observed by naked eyes via autopsies. As a result, no significant clinical symptoms or dead rats were found, and also no toxicity was observed from the weight changes, blood test, hematobiochemical test and autopsies.
  • Gentianae macrophyllae radix of the present invention via wet granulation and dry granulation according to the following formulation.
  • Epidermal formulation was prepared by using the extract of crude Gentianae macrophyllae radix prepared according to the present invention.
  • the extract of Gentianae macrophyllae radix prepared according to the present invention has an excellent inhibitory effect on epidermal hyperplasia and is thus speculated to be very useful for the prevention and treatment of dermatological diseases such as psoriasis.

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  • Health & Medical Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
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  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Microbiology (AREA)
  • Medical Informatics (AREA)
  • Botany (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Mycology (AREA)
  • Dermatology (AREA)
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Abstract

Disclosed is an extract of Gentianae macrophyllae radix useful for the treatment of dermatological diseases, in particular, an extract of Gentianae macrophyllae radix which has an excellent inhibitory effect on epidermal proliferation of skin thus being useful for the prevention and treatment of dermatological diseases.

Description

Description EXTRACT OF GENTIANAE MACROPHYLLAE RADIX FOR
THE TREATMENT OF DERMATOLOGICAL DISEASES
Technical Field
[1]
[2] The present invention relates to an extract of Gentianae macrophyllae radix useful for the treatment of dermatological diseases, in particular, an extract of Gentianae macrophyllae radix which has an excellent inhibitory effect on epidermal hyperplasia thus being useful for the prevention and treatment of dermatological diseases such as psoriasis.
[3]
Background Art
[4]
[5] Psoriasis is a dermatological disease which is characterized in that a patient's epidermal surface is covered with whitish scaly skin cells thus clearly marking its boundary with the neighboring skin, and also producing scabs with various sizes in red spots which grow bigger as time passes. This disease often develops on the skins of elbows, knees, buttocks, head and also on hands and soles. The above skin areas appear to be more frequently affected than other parts of a body. Psoriasis develops regardless of a sex and occurs most highly in people in their early 20s.
[6] Although the direct cause of psoriasis has not been identified, it appears that the disease may be developed by combinatory reasons of genetic factors as well as environmental conditions such as hormonal change, stress, trauma, infectious disease such as tonsillitis, weather, dryness skin, drugs, genetic history and the like. Psoriasis, although being developed by various reasons as mentioned above, is specifically caused by the extremely fast growth of skin cells, which is about 6-7 times faster than those of normal cells, thereby inducing the peeling-off of the excessive and incompletely grown whitish scaly skin of a plurality of piled-up layers of keratinized cells.
[7] Psoriasis is a progressive and chronic disease, which often recurs and is hardly cured completely once it is developed. Although many people have been suffering from chronic dermatological diseases such as psoriasis, there has not been developed any good cure for the treatment of the above diseases and only deterioration of the seriousness of the above diseases has been merely wished. Therefore, it is essential to develop a good therapeutic pharmaceutical drug with an excellent mechanism of action for the treatment of the above diseases. However, neither the main cause nor the substance, which may trigger the development of cures for the diseases, has been clearly identified and thus the developmental procedure of the therapeutic pharmaceutical agent has been long deterred.
[8] Recent clinical studies on tissues of dermatological lesions in patients with the above-mentioned dermatological diseases disclosed infiltration of eosinophils, mast cells and neutrophils, and abnormal growth of skin epidermis (epidermal hyperplasia, epidermal hyperproliferation). The main reasons of the above symptoms were reported to be closely associated with epidermal differentiation as in keratin 6 and abnormal expression of genes which are involved in epidermal hyperplasia (Sugimura et al., Br. J. Dermatol. 152, 146-149, 2005). Since the epidermal proliferation is one of the major factors causing the dermatological diseases, any substance that can inhibit epidermal proliferation may be used as a therapeutic agent to treat dermatological diseases such as psoriasis.
[9] Nonetheless, not many chemical drugs have been known to inhibit epidermal proliferation, and they are not free from side effects when used for a long period of time. Therefore, it has been long wished to discover an extract isolated from herbal medicines which may prevent side effects even with a long term use.
[10] The Gentianae macrophyllae radix used in the present invention is a perennial plant having a height of 40 - 60 cm and a strong but unelastic root. It is widely distributed in China such as Heilongjiang, Liaoning, Hebei, Heinan, Sichuan provinces. They are collected in Spring and Autumn. The plants may be dried in the sunlight after removing stovers, fibrous roots and soils, or dried after piling them together. In general, when they become reddish yellow or yellowish gray they are scattered and dried in the sunlight.
[11] The plants have been used in oriental medicine for the purpose of eliminating
'wind'(a term in oriental medicine indicating a severe intermittent headache), 'damp'( a term in oriental medicine indicating a patient with damp syndrome), harmonize 'acupoint '( a term in oriental medicine indicating acupoint small pools of the circulating Gi and blood of channels and viscera where acupuncture or moxibustion is applied), releasing heat by releasing muscles and tendons and urinating. Therefore, the plants have been used for the treatment of paralytic pain, musculoskeletal cramps, jaundice, bloody stool (hematochezia), urination disorder. The major ingredients are known to contain ingredients such as gentianine, gentianidine, gentianol, gen- tiopicroside and the like. However, the role of the Gentianae macrophyllae radix regarding its therapeutic treatment of dermatological diseases has not been reported (Encyclopedia of Chinese Medicine, Jungdam Publishing Co., Ltd., pp. 5171-5177; 1998, Standards of Natural Drug Not Listed in Korea Pharmacopoeia, Korea Medical Index Co., Ltd., p. 352; 1988]. [12]
Disclosure
[13]
[14] The present invention relates to a therapeutic pharmaceutical agent comprising an extract of Gentianae macrophyllae radix as an active ingredient for the treatment of epidermal hyperplasia.
[15] The present invention is described in detail herein below.
[16] In one aspect, the present invention relates to an extract of crude Gentianae macrophyllae radix having an excellent inhibitory effect on epidermal proliferation of skin thus being useful for the prevention and treatment of dermatological diseases such as psoriasis.
[17] In another aspect, the present invention relates to a method of preparing an extract of crude Gentianae macrophyllae radix comprising:
[18] 1) a) extracting Gentianae macrophyllae radix under reflux using water or an aqueous alcohol solution in the amount of 10-15 times of the weight of the Gentianae macrophyllae radix, filtering the mixture;
[19] b) adding water or an aqueous alcohol solution to the resulting residue thereto in the amount of 7-12 times of the weight of the Gentianae macrophyllae radix, heating the mixture, reextracting the mixture, filtering the mixture;
[20] c) combining the resulting filtrate obtained in step b) with the filtrate obtained in step a), and filtering the mixed filtrate;
[21] 2) fractionating layers of the mixed filtrate obtained in the above step 1) using an equal amount of a low grade alcohol or a nonpolar solvent, and concentrating under reduced pressure at 60 - 70 ° C; and
[22] 3) performing azeotropic concentration of the above concentrate obtained in step 2) with water in the amount of 25-50 times of the weight of the above concentrate obtained in step 2), suspending the resulting concentrate homogeneously in an equal amount of water, and performing lyophilization.
[23] The above process is described in more detail herein below. In the above process,
Gentianae macrophyllae radix is added with water or an aqueous alcohol solution and extracted under reflux for 2-5 hours. The amount of water used is preferably in the range of 10-15 times of the weight of the Gentianae macrophyllae radix. The mixture undergoes filtration and the resulting filtrate is collected. Then, water or an aqueous alcohol solution in the amount of 7-12 times of the weight of the Gentianae macrophyllae radix is added to the resulting residue, and the mixture is heated. The mixture is reextracted for 2-5 hours, filtered and the resulting filtrate is combined with the filtrate obtained previously thereby increasing the extraction efficiency.
[24] Here, if the amount of water is not sufficient it will make stirring difficult and decrease the solubility of the extract thus decreasing the extraction efficiency. In contrast, if the amount of water is excessive it will increase the amount of the low grade alcohol and the nonpolar solvent to be used in the subsequent purification step thus increasing cost and may also raise problems in proceeding the process.
[25] In the present invention, extraction is performed twice, i.e., first extraction and re- extraction. This is because a single extraction in the case of a large scale production of extract may not guarantee relatively high extraction efficiency due to a great loss in water content contained in the crude drug itself during the extraction process, and by conducting a reextraction the resulting extract efficiency can be greatly increased.
[26] The double extraction, i.e., performing first extraction and reextraction, results in collection of about 80-90% of the total amount of extract, while an extraction of 3 times or more is found not economical.
[27] The extract obtained by the double extraction using water or an aqueous alcohol solution is filtered and concentrated. Then impurities such as unnecessary proteins, polysaccharides, and fatty acids contained in the resulting concentrated filtrate are purified. In the present invention, the filtrate is purified by fractionation of the filtrate 2-4 times and obtaining a solvent fraction using a low grade alcohol or a nonpolar solvent which is equal in amount to that of the filtrate.
[28] A low grade alcohol is preferably a C1-C6 alcohol, more preferably butyl alcohol, propyl alcohol and isopropyl alcohol.
[29] A nonpolar solvent may be selected from the group consisting of ethyl acetate, dichloro methane, chloroform, carbon tetrachloride, and methylethylketone.
[30] In case the amount of the low grade alcohol or the nonpolar solvent is less than that of the filtrate, it forms granules from unnecessary components such as fatty acid thereby preventing a smooth separation of layers and also decreasing the content of active ingredients contained in the extract.
[31] The fractions of a low grade alcohol or a nonpolar solvent obtained as a result of fractionation are concentrated under reduced pressure at 60-70 ° C, and the residual solvent is eliminated. Thus obtained concentrate undergoes azeotropic concentration 2-3 times using water in the amount of 25-50 times of the total amount of the concentrate, and then suspended homogeneously in an equal volume of water.
[32] The purpose of using water in performing azeotropic concentration in this process is to effectively control the amount of the residual low grade alcohol for use of a crude drug extract as a source for a pharmaceutical agent.
[33] The above extract then undergoes lyophilization and the final extract in the form of powder is obtained. The extract has an excellent inhibitory effect on epidermal proliferation and is thus expected to be useful as a therapeutic pharmaceutical agent for the prevention and treatment of dermatological diseases such as psoriasis. [34] In an embodiment of the present invention, the extract of Gentianae macrophyllae radix prepared according to the present invention is formulated in the form of tablets, capsules, injections and the like.
[35] In preparing tablets, the ratio between the combined amount of excipients, such as lactose, microcrystalline cellulose, magnesium stearate, and the amount of the above extract is preferred to be 2: 1 to attain a desired pharmaceutical activity for the prevention and treatment of dermatological diseases.
[36] Crude drugs themselves may be directly used as pharmaceutical agents. However, they may be combined with pharmaceutically acceptable additives such as a carrier, a forming agent, or a diluent to be prepared in the form of powder, granules, capsules, injections and the like.
[37] The extract of Gentianae macrophyllae radix has been long used as a food or an oriental medicine. There has been no particular limitation on its dosage but its dosage may vary depending on the rate of body absorption, body weight, age, sex, health conditions, dosage time, type of administration, excretion rate, seriousness of diseases of a subject. In general, the extract of Gentianae macrophyllae radix is preferably administered about 0.1 - 10 mg/kg. Therefore, the extract comprising the active ingredient of the present invention may be manufactured in consideration of the effective dosage. Further, the formulated unit dosage prepared thereof can be administered once or a few times at regular intervals daily by means of specialized administration, upon necessity, according to the advice and/or the request of a specialist or a supervisor who monitors and supervises drug administration.
[38]
Best Mode
[39]
[40] The present invention is described in more details with reference to the following examples. However, they should not be construed as limiting the scope of the present invention.
[41]
[42] Preparation Example 1 : Preparation of an Extract of Gentianae macrophyllae radix
[43] Two hundred fifty grams of crude Gentianae macrophyllae radix, minced to a size of about 3.0 cm, was homogeneously mixed, added with 2 L of water, and heat extracted for 5 hours while stirring. The extract was filtered and the filtrate was collected. The resulting residue was added with 2 L of water and heat extracted for 3 hours and filtered to obtain a second filtrate. The two filtrates were combined and concentrated to 1 L, which then underwent separation of layers 3 times by adding an equal amount of water-saturated n-butyl alcohol. The n-butyl alcohol was recovered and con- centrated under reduced pressure at 65 ° C until all crude drugs were completely dried. After most of n-butyl alcohol and water were evaporated, the resultant was added with 0.1 L of water and underwent azeotropic concentration 2 times, resuspended in equal amount of distilled water, lyophilized and finally obtained the extract of Gentianae macrophyllae radix in the form of powder.
[44]
[45] Preparation Example 2 : Preparation of an Extract of Gentianae macrophyllae radix
[46] Two hundred fifty grams of crude Gentianae macrophyllae radix was washed with water to remove impurities, dried, added with 2L of 50%(v/v) ethanol solution and then extracted under reflux for 6 hours while stirring. The extract was filtered and then collected. The remaining residue was added with 1.5 L of 50%(v/v) ethanol solution, and then heat extracted for 3 hours. The two filtrates were combined and concentrated to 1 L, which then underwent separation of layers 3 times by adding an equal amount of water-saturated n-butyl alcohol. The n-butyl alcohol was recovered and concentrated under reduced pressure at 65 ° C until all crude drugs were completely dried. After most of n-butyl alcohol and water were evaporated, the resultant was added with 0.3 L of water and underwent azeotropic concentration 2 times, resuspended in equal amount of distilled water, lyophilized and finally obtained the extract of Gentianae macrophyllae radix in the form of powder.
[47]
[48] Example 1: Test of Acute Toxicity of Oral Administrative Formulation in Rats
[49] A test of acute toxicity was performed by using 6-week-old specific pathogen free
(SPF) SD rats as follows.
[50] Each group consisted of 2 rats. They were orally respectively administered with the extract of Gentianae macrophyllae radix prepared in Preparation Examples 1 and 2 with a dosage of 1 g/kg/mL once. After the administration, the rats were observed of their deaths, clinical symptoms, and weight changes. Further, hematological test and hematobiochemical test were conducted and abnormalities on abdominal and pectoral organs were observed by naked eyes via autopsies. As a result, no significant clinical symptoms or dead rats were found, and also no toxicity was observed from the weight changes, blood test, hematobiochemical test and autopsies. In summary, there was no toxicity observed in experimental rats by the administration of the extract of Gentianae macrophyllae radix when used up to dosage of 2,000 mg/kg. Its lethal dosage (LD ) for oral administration was shown to be greater than 2,000 mg/kg thus showing the safety of the above extract.
[51]
[52] Formulation Example 1: Preparation of Tablets [53] Tablets for oral administration were manufactured by using the extract of crude
Gentianae macrophyllae radix of the present invention via wet granulation and dry granulation according to the following formulation. [54]
[55] [Formulation]
[56] extract of Gentianae macrophyllae radix 200 mg
[57] Light Anhydrous Silicic Acid 10 mg
[58] magnesium stearate 2 mg
[59] microcrystalline cellulose 50 mg
[60] sodium starch glycolate 25 mg
[61] corn starch 113 mg
[62] anhydrous ethanol adequate [63]
[64] Formulation Example 2: Preparation of Ointments
[65] Ointments were manufactured by using the extract of crude Gentianae macrophyllae radix of the present invention according to the following formulation. [66]
[67] [Formulation]
[68] extract of Gentianae macrophyllae radix 5 g
[69] cetylpalmitate 20 g
[70] cetanol 40 g
[71] stearyl alcohol 40 g
[72] isopropyl myristate 80 g
[73] sorbitan monostearate 20 g
[74] polysolvate 60 g
[75] propyl parahydroxy benzoic acid 1 g
[76] methyl parahydroxy benzoic acid 1 g
[77] phosphate and distilled water adequate amount [78]
[79] Formulation Example 3: Preparation of Injections
[80] An injection was prepared by using the extract of crude Gentianae macrophyllae radix prepared according to the present invention using the following formulation. [81]
[82] [Formulation]
[83] extract of Gentianae macrophyllae radix 100 mg
[84] mannitol 180 mg
[85] Na 2HPO 4 - 12H2O 25 mg
[86] water for injection 2974 mg [88] Formulation Example 4: Preparation of Topical Formulation
[89] Epidermal formulation was prepared by using the extract of crude Gentianae macrophyllae radix prepared according to the present invention.
[90]
[91] [Formulation 1]
[92] extract of Gentianae macrophyllae radix 0.4 g
[93] sodium polyacrylate 1.3 g
[94] glycerine 3.6 g,
[95] aluminum hydroxide 0.04 g
[96] methyl paraben 0.2 g
[97] water 14.0 g
[98]
[99] [Formulation 2]
[100] extract of Gentianae macrophyllae radix 0.8 g
[101] propylene glycol 1.6 g
[102] liquid paraffin 0.8 g
[103] isopropyl myristate 0.4 g
[104] Gelba 1430 16.4 g
[105]
Industrial Applicability
[106]
[107] As stated above, the extract of Gentianae macrophyllae radix prepared according to the present invention has an excellent inhibitory effect on epidermal hyperplasia and is thus speculated to be very useful for the prevention and treatment of dermatological diseases such as psoriasis.
[108] The invention has been described in detail with reference to preferred embodiments thereof. However, it will be appreciated by those skilled in the art that changes may be made in these embodiments without departing from the principles and spirit of the invention, the scope of which is defined in the appended claims and their equivalents.

Claims

Claims
[1] A therapeutic pharmaceutical agent for the treatment of epidermal hyperplasia of skin comprising an extract of Gentianae macrophyllae radix as an active ingredient.
[2] The therapeutic pharmaceutical agent according to claim 1, wherein said derma- tological disease caused by epidermal hyperplasia of skin cells is psoriasis.
PCT/KR2006/005868 2005-12-30 2006-12-29 Extract of gentianae macrophyllae radix for the treatment of dermatological diseases WO2007078117A1 (en)

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Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20000043996A (en) * 1998-12-29 2000-07-15 조민호 Extraction and purification method of active substance from gentianae macrophyllae radix and crudedrug composition comprising the same
KR20060102620A (en) * 2005-03-24 2006-09-28 한국 한의학 연구원 Composition containing gentianae macrophyllae radix extract for treatment hypersensitive skin disease

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20000043996A (en) * 1998-12-29 2000-07-15 조민호 Extraction and purification method of active substance from gentianae macrophyllae radix and crudedrug composition comprising the same
KR20060102620A (en) * 2005-03-24 2006-09-28 한국 한의학 연구원 Composition containing gentianae macrophyllae radix extract for treatment hypersensitive skin disease

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
CHINESE JOURNAL OF MODERN DEVELOPMENTS IN TRADITIONAL MEDICINE, vol. 9, no. 3, March 1989 (1989-03-01), pages 156 - 157 *
DATABASE MEDLINE [online] YUAN Z.Z. ET AL.: "Observation on the treatment of systemic lupus erythematous with a Gentiana macrophylla complex tablet and a minimal dose of prednisone", XP003015388, Database accession no. (NLM2736700) *

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