JP7587929B2 - Cheilitis relief agent - Google Patents
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- JP7587929B2 JP7587929B2 JP2020096715A JP2020096715A JP7587929B2 JP 7587929 B2 JP7587929 B2 JP 7587929B2 JP 2020096715 A JP2020096715 A JP 2020096715A JP 2020096715 A JP2020096715 A JP 2020096715A JP 7587929 B2 JP7587929 B2 JP 7587929B2
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Description
本発明は、口唇炎改善剤に関する。 The present invention relates to an agent for improving cheilitis.
口唇は、解剖学的には粘膜の性格を有し、毛細血管が豊富で血流が多い、特殊な部位である。(非特許文献1)。口唇は粘膜上皮層を持つが、角層は持たないため、バリア機能を保つことが困難である(非特許文献2)。口唇は、そのような特殊な構造であるにも関わらず外界に接していることで常に物理的刺激や化学的刺激に晒されているため、トラブルを起こしやすい部位でもある。口唇はターンオーバーが平均3.5日と非常に短いが、修復段階でも刺激が繰り返し加わるため立て続けにトラブルが発生し、回復しない状態となる。 The lips are a special part of the body that, anatomically, has the characteristics of a mucous membrane, is rich in capillaries, and has a high blood flow (Non-Patent Document 1). The lips have a mucous epithelial layer, but do not have a stratum corneum, making it difficult to maintain their barrier function (Non-Patent Document 2). Despite this special structure, the lips are in contact with the outside world and are constantly exposed to physical and chemical stimuli, making them a part of the body that is prone to problems. The turnover rate of the lips is very short, averaging 3.5 days, but repeated stimuli are applied even during the repair stage, causing problems to occur one after another, leading to a state where recovery does not occur.
一方、当帰飲子は、10種の生薬からなる漢方であり、骨髄造血促進作用を有する「四物湯」(非特許文献3)をベースとしている。このため、当帰飲子は、「血」が不足した「血虚」の状態に対して「血」を補給するもの(特許文献4)として、「冷え症のものの次の諸症:慢性湿疹(分泌物の少ないもの)、かゆみ」(非特許文献5)に適用される。 On the other hand, Toki-inshi is a traditional Chinese medicine made up of 10 kinds of herbal medicines, and is based on "Shimotsuto" (Non-Patent Document 3), which has the effect of promoting hematopoiesis in the bone marrow. For this reason, Toki-inshi is used to replenish "blood" in the "blood deficiency" state (Patent Document 4), and is applied to "the following symptoms of people with poor circulation: chronic eczema (with little secretion), itching" (Non-Patent Document 5).
当帰飲子は「血虚」の状態にある慢性湿疹などに対して用いられているが、口唇炎に対して有効であることは知られていない。そもそも、口唇が粘膜の延長であり、皮膚とは構造が大きく異なること、及び口唇には毛細血管が豊富で血流が多いことから、当帰飲子に口唇炎を改善する作用は期待できなかった。 Angelica extract is used to treat conditions such as chronic eczema caused by "blood deficiency," but it is not known to be effective against cheilitis. First of all, the lips are an extension of the mucous membrane and have a structure very different from that of the skin, and the lips are rich in capillaries and have a high blood flow, so Angelica extract cannot be expected to have any effect on improving cheilitis.
本発明は、口唇炎を改善できる薬剤を提供することを目的とする。 The present invention aims to provide a drug that can improve cheilitis.
本発明者は、鋭意検討を行ったところ、当帰飲子に、口唇炎を改善する作用があることを新たに見出した。本発明は、かかる知見に基づいて、更に検討を重ねることにより完成したものである。 After extensive research, the inventors discovered that Angelica sinensis has the effect of improving cheilitis. Based on this knowledge, the present invention was completed through further research.
即ち、本発明は、下記に掲げる態様の発明を提供する。
項1. 当帰飲子エキスを含有する、口唇炎改善剤。
項2. 内服薬である、項1に記載の口唇炎改善剤。
項3. 剥脱性口唇炎に用いられる、項1又は2に記載の口唇炎改善剤。
That is, the present invention provides the following aspects.
Item 1. A cheilitis improving agent containing Angelica sinensis extract.
Item 2. The cheilitis improving agent according to Item 1, which is an oral medication.
Item 3. The agent for improving cheilitis according to Item 1 or 2, which is used for exfoliative cheilitis.
本発明によれば、口唇炎を改善できる薬剤が提供される。 The present invention provides a drug that can improve cheilitis.
本発明の口唇炎改善剤は、当帰飲子エキスを含有し、口唇炎の改善に用いられることを特徴とする。以下、本発明の口唇炎改善剤について詳述する。 The cheilitis improving agent of the present invention is characterized by containing Angelica sinensis extract and being used to improve cheilitis. The cheilitis improving agent of the present invention is described in detail below.
当帰飲子エキス
当帰飲子の漢方処方としては、「新 一般用漢方処方の手引き」(合田 幸広・袴塚 高志監修、日本漢方生薬製剤協会編集、株式会社じほう発行)に記載されている漢方処方が好ましく、具体的には、トウキ、シャクヤク、センキュウ、シツリシ、ボウフウ、ジオウ、ケイガイ、オウギ、カシュウ、及びカンゾウからなる混合生薬が挙げられる。また、当帰飲子には、漢方生薬調査会により定められた「漢方製剤の基本的取扱い方針」に規定されるように、現在繁用されている漢方関係の書簡に記載されている混合生薬(漢方処方)が包含される。
As the herbal prescription for Angelica sinensis extract , the herbal prescription described in "New Guide to General Herbal Prescriptions" (supervised by Yukihiro Goda and Takashi Hakamzuka, edited by the Japanese Association of Herbal Medicine Preparations, published by Jiho Co., Ltd.) is preferred, specifically including mixed herbal medicines consisting of Angelica sinensis, Peony root, Cnidium officinale, Scutellaria baicalensis, Bougainvillea Root, Rehmannia Root, Astragalus Root, Polygala Root, and Licorice Root. In addition, Angelica sinensis includes mixed herbal medicines (herbal prescriptions) described in currently widely used letters related to herbal medicine, as stipulated in the "Basic Handling Policy for Herbal Medicine Preparations" established by the Kampo Herbal Medicine Research Committee.
また、当帰飲子を構成する各生薬の分量としては、トウキが2.5~10重量部、好ましくは3~7重量部;シャクヤクが1.5~6重量部、好ましくは2~4重量部;センキュウが1.5~6重量部、好ましくは2~4重量部;シツリシが1.5~6重量部、好ましくは2~4重量部;ボウフウが1.5~6重量部、好ましくは2~4重量部;ジオウが2~8重量部、好ましくは3~6重量部;ケイガイが0.75~3重量部、好ましくは1~2重量部;オウギが0.75~3重量部、好ましくは1~2重量部;カシュウが1~4重量部、好ましくは1.5~3重量部;及びカンゾウが0.5~2重量部、好ましくは0.75~1.5重量部が挙げられる。 The amounts of each herb that makes up Angelica Root in Angelica Root are 2.5 to 10 parts by weight, preferably 3 to 7 parts by weight; Peony Root ...
本発明で使用される当帰飲子エキスの製造に供される生薬調合物の好適な例としては、トウキ5重量部、シャクヤク3重量部、センキュウ3重量部、シツリシ3重量部、ボウフウ3重量部、ジオウ4重量部、ケイガイ1.5重量部、オウギ1.5重量部、カシュウ2重量部、及びカンゾウ1重量部が挙げられる。 Suitable examples of herbal medicine preparations used in the manufacture of the Angelica Root extract used in the present invention include 5 parts by weight of Angelica Root, 3 parts by weight of Peony Root, 3 parts by weight of Cnidium Root, 3 parts by weight of Citrus Fruit, 3 parts by weight of Bougainvillea Root, 4 parts by weight of Rehmannia Root, 1.5 parts by weight of Astragalus Root, 1.5 parts by weight of Polygala Root, 2 parts by weight of Polygala Root, and 1 part by weight of Licorice Root.
当帰飲子のエキスの形態としては、流エキス、軟エキス等の液状のエキス、又は固形状の乾燥エキス末のいずれであってもよい。 The form of the extract of Angelica sinensis may be either a liquid extract such as a liquid extract or a soft extract, or a solid dried extract powder.
当帰飲子の液状のエキスは、当帰飲子処方に従った混合生薬を抽出処理し、得られた抽出液を必要に応じて濃縮することにより得ることができる。また、当帰飲子の乾燥エキス末は、液状のエキスを乾燥処理することにより得ることができる。 A liquid extract of Angelica sinensis can be obtained by extracting the mixed herbs according to the Angelica sinensis prescription and concentrating the resulting extract as necessary. A dried Angelica sinensis extract powder can be obtained by drying the liquid extract.
当帰飲子のエキスの製造において、抽出処理に使用される抽出溶媒としては、特に限定されず、水又は含水エタノールが挙げられる。当帰飲子の抽出処理としては、特に限定されないが、例えば、当帰飲子に含まれる生薬の総重量(乾燥重量換算)に対して、5~10倍量程度の抽出溶媒で抽出した後、1/2容量になるまで濃縮し、固形分を除いたものを、当帰飲子の液状エキスとして得る方法が挙げられる。また、この液状エキスを乾燥処理に供することにより、当帰飲子の乾燥エキス末が得られる。乾燥処理としては、特に限定されず、公知の方法を用いればよく、例えば、スプレードライ法や、エキスの濃度を高めた軟エキスに適当な吸着剤(例えば無水ケイ酸、デンプン等)を加えて吸着末とする方法等が挙げられる。 In the production of the extract of Angelica sinensis, the extraction solvent used in the extraction process is not particularly limited, and may be water or aqueous ethanol. The extraction process of Angelica sinensis is not particularly limited, and may be, for example, a method in which the total weight (converted to dry weight) of the herbal medicine contained in Angelica sinensis is extracted with an extraction solvent in an amount of about 5 to 10 times, and then the mixture is concentrated to 1/2 the volume, and the solids are removed to obtain a liquid extract of Angelica sinensis. This liquid extract can be dried to obtain a dried extract powder of Angelica sinensis. The drying process is not particularly limited, and may be any known method, such as a spray drying method or a method in which a suitable adsorbent (e.g., silicic anhydride, starch, etc.) is added to a soft extract with a high extract concentration to obtain an adsorbed powder.
本発明において当帰飲子としてエキスを使用する場合、前述の方法で調製したエキスを使用してもよいし、市販されるものを使用してもよい。 When using an extract as a toki-in-shi in the present invention, the extract prepared by the method described above may be used, or a commercially available extract may be used.
本発明の口唇炎改善剤において、当帰飲子エキスの含有量としては、本発明の効果を奏する限り、特に限定されないが、当帰飲子エキスの乾燥エキス末量換算で、通常5~100重量%、好ましくは10~90重量%、より好ましくは20~80重量%、更に好ましくは30~60重量%が挙げられる。なお、本発明において、当帰飲子の乾燥エキス末量換算とは、当帰飲子の乾燥エキス末を使用する場合にはそれ自体の量であり当帰飲子の液状のエキスを使用する場合には、溶媒を除去した残量に換算した量である。また、当帰飲子の乾燥エキス末が、製造時に添加される吸着剤等の添加剤を含む場合は、当該添加剤を除いた量である。 In the cheilitis improving agent of the present invention, the content of Angelica sinensis extract is not particularly limited as long as the effect of the present invention is achieved, but is usually 5 to 100% by weight, preferably 10 to 90% by weight, more preferably 20 to 80% by weight, and even more preferably 30 to 60% by weight, calculated as the amount of dried extract powder of Angelica sinensis extract. In the present invention, the amount of dried extract powder of Angelica sinensis refers to the amount of the dried extract powder itself when a dried extract powder of Angelica sinensis is used, and refers to the amount converted to the amount remaining after removing the solvent when a liquid extract of Angelica sinensis is used. In addition, when the dried extract powder of Angelica sinensis contains additives such as adsorbents added during production, the amount refers to the amount excluding the additives.
その他の成分
本発明の口唇炎改善剤は、当帰飲子エキス単独からなるものであってもよく、製剤形態に応じた添加剤や基剤を含んでいてもよい。このような添加剤及び基剤としては、薬学的に許容されることを限度として特に制限されないが、例えば、賦形剤、結合剤、崩壊剤、滑沢剤、等張化剤、可塑剤、分散剤、乳化剤、溶解補助剤、湿潤化剤、安定化剤、懸濁化剤、粘着剤、コーティング剤、光沢化剤、水、油脂類、ロウ類、炭化水素類、脂肪酸類、高級アルコール類、エステル類、水溶性高分子、界面活性剤、金属石鹸、低級アルコール類、多価アルコール、pH調整剤、緩衝剤、酸化防止剤、紫外線防止剤、防腐剤、矯味剤、香料、粉体、増粘剤、色素、キレート剤等が挙げられる。これらの添加剤は、1種単独で使用してもよく、また2種以上を組み合わせて使用してもよい。また、これらの添加剤及び基剤の含有量については、使用する添加剤及び基剤の種類、口唇炎改善剤の製剤形態等に応じて適宜設定される。
Other components The cheilitis improving agent of the present invention may be composed of Angelica sinensis extract alone, or may contain additives and bases according to the formulation. Such additives and bases are not particularly limited as long as they are pharmacologic acceptable, and examples thereof include excipients, binders, disintegrants, lubricants, isotonicity agents, plasticizers, dispersants, emulsifiers, solubilizers, wetting agents, stabilizers, suspending agents, adhesives, coating agents, glossing agents, water, oils and fats, waxes, hydrocarbons, fatty acids, higher alcohols, esters, water-soluble polymers, surfactants, metal soaps, lower alcohols, polyhydric alcohols, pH adjusters, buffers, antioxidants, UV inhibitors, preservatives, flavorings, fragrances, powders, thickeners, dyes, and chelating agents. These additives may be used alone or in combination of two or more. The content of these additives and bases is appropriately set according to the types of additives and bases used, the formulation form of the cheilitis improving agent, and the like.
また、本発明の口唇炎改善剤は、当帰飲子エキスの他に、必要に応じて、他の栄養成分や薬理成分を含有していてもよい。このような栄養成分や薬理成分としては、薬学的に許容されることを限度として特に制限されないが、例えば、制酸剤、健胃剤、消化剤、整腸剤、鎮痙剤、粘膜修復剤、抗炎症剤、収れん剤、鎮吐剤、鎮咳剤、去痰剤、消炎酵素剤、鎮静催眠剤、抗ヒスタミン剤、カフェイン類、強心利尿剤、抗菌剤、血管収縮剤、血管拡張剤、局所麻酔剤、生薬エキス、ビタミン類、メントール類等が挙げられる。これらの栄養成分や薬理成分は、1種単独で使用してもよく、また2種以上を組み合わせて使用してもよい。また、これらの成分の含有量については、使用する成分の種類、口唇炎改善剤の製剤形態等に応じて適宜設定される。 In addition, the cheilitis improving agent of the present invention may contain other nutritional components and pharmacological components as necessary in addition to the Angelica sinensis extract. Such nutritional components and pharmacological components are not particularly limited as long as they are pharmacologic acceptable, but examples thereof include antacids, stomachic agents, digestive agents, intestinal regulators, antispasmodics, mucosal repair agents, anti-inflammatory agents, astringents, antiemetics, antitussives, expectorants, anti-inflammatory enzymes, sedatives, hypnotics, antihistamines, caffeine, cardiac diuretics, antibacterial agents, vasoconstrictors, vasodilators, local anesthetics, herbal extracts, vitamins, and menthols. These nutritional components and pharmacological components may be used alone or in combination of two or more. The content of these components is appropriately set depending on the type of components used and the formulation form of the cheilitis improving agent.
製剤形態
本発明の口唇炎改善剤の製剤形態については特に限定されないが、好ましくは経口投与が可能である製剤形態が挙げられ、例えば、散剤、細粒剤、顆粒剤(ドライシロップを含む)、錠剤、丸剤、カプセル剤(軟カプセル剤、硬カプセル剤)等の固形状製剤;ゼリー剤等の半固形状製剤;液剤、懸濁剤、シロップ剤等の液状製剤が挙げられる。これらの製剤形態の中でも、含有成分の安定性や携帯性等の観点から、好ましくは固形状製剤が挙げられる。
The formulation form of the cheilitis improving agent of the present invention is not particularly limited, but preferably includes formulation forms that can be orally administered, such as solid formulations such as powders, fine granules, granules (including dry syrup), tablets, pills, capsules (soft capsules, hard capsules), etc.; semi-solid formulations such as jellies; and liquid formulations such as liquids, suspensions, syrups, etc. Among these formulation forms, solid formulations are preferred from the viewpoints of the stability and portability of the contained ingredients.
本発明の口唇炎改善剤を前記製剤形態に調製するには、当帰飲子エキス、並びに必要に応じて添加される添加剤、基剤、及び/又は薬理成分を用いて、医薬分野で採用されている通常の製剤化手法に従って製剤化すればよい。 To prepare the cheilitis improving agent of the present invention in the above-mentioned formulation form, the agent may be formulated according to the usual formulation method used in the pharmaceutical field using Angelica sinensis extract, and additives, bases, and/or pharmacological ingredients that are added as necessary.
用途
本発明の口唇炎改善剤は、口唇炎を改善することを目的として用いられる。口唇炎としては特に限定されず、剥脱性口唇炎、接触性口唇炎、光線性口唇炎等が挙げられ、これらの中でも、好ましくは剥脱性口唇炎が挙げられる。
The cheilitis improving agent of the present invention is used for the purpose of improving cheilitis. Cheilitis is not particularly limited, and examples thereof include exfoliative cheilitis, contact cheilitis, and actinic cheilitis, and among these, exfoliative cheilitis is preferred.
また、本発明の口唇炎改善剤は、毛細血管が豊富で血流が多い口唇に生じる口唇炎を改善できるため、適用対象としては、口唇炎を有する人であれば、「血虚」に該当しない人、例えば、貧血でない人、冷え性でない人も挙げられる。 In addition, since the cheilitis improving agent of the present invention can improve cheilitis that occurs on the lips, which have a rich number of capillaries and a high blood flow, its application can also include people who have cheilitis but do not fall under the category of "blood deficiency," such as those who are not anemic or prone to cold.
用量・用法
本発明の口唇炎改善剤の投与形態としては特に限定されないが、好ましくは経口投与によって使用される。本発明の口唇炎改善剤の用量については、投与対象者の年齢、性別、体質、症状の程度等に応じて適宜設定されるが、例えば、ヒト1人に対して1日当たり、当帰飲子エキスの乾燥エキス末量換算で0.5~20g程度、好ましくは1~10g程度、より好ましくは2~6g程度、さらに好ましくは2~4g程度となる量で、1日1~3回、好ましくは2又は3回の頻度で服用すればよい。服用タイミングについては、特に制限されず、食前、食後、又は食間のいずれであってもよいが、食前(食事の30分前)又は食間(食後2時間後)が好ましい。
Dosage and Usage: The dosage form of the cheilitis improving agent of the present invention is not particularly limited, but is preferably administered orally. The dosage of the cheilitis improving agent of the present invention is appropriately set according to the age, sex, constitution, and severity of symptoms of the person to be administered, but for example, the amount of about 0.5 to 20 g, preferably about 1 to 10 g, more preferably about 2 to 6 g, and even more preferably about 2 to 4 g of the dried extract powder of Angelica sinensis extract per person per day may be taken 1 to 3 times a day, preferably 2 or 3 times a day. The timing of taking the agent is not particularly limited, and may be before, after, or between meals, but it is preferable to take the agent before (30 minutes before a meal) or between meals (2 hours after a meal).
以下、本発明を実施例により具体的に説明するが、本発明はこれらの実施例に限定されるものではない。 The present invention will be described in detail below with reference to examples, but the present invention is not limited to these examples.
当帰飲子エキス末の製造
原料生薬を、トウキ5重量部、シャクヤク3重量部、センキュウ3重量部、シツリシ3重量部、ボウフウ3重量部、ジオウ4重量部、ケイガイ1.5重量部、オウギ1.5重量部、カシュウ2重量部、及びカンゾウ1重量部の割合で用い、これらを刻んだ後、水20倍重量(540重量部)を用いて約100℃で1時間抽出し、遠心分離して抽出液を得、減圧下で濃縮してスプレードライヤーを用いて乾燥し、当帰飲子エキス末を得た。得られた当帰飲子エキス末は、原料生薬混合物100g当たり10.8gであった。なお、スプレードライヤーによる乾燥は、抽出液を回転数10000rpmのアトマイザーに落下させ、150℃の空気の熱風を供給して行った。
The raw herbs used for the production of Angelica sinensis extract powder were 5 parts by weight of Angelica sinensis , 3 parts by weight of Peony root, 3 parts by weight of Cnidium officinale, 3 parts by weight of Scutellaria baicalensis, 3 parts by weight of Bougainvillea Root, 4 parts by weight of Rehmannia Root, 1.5 parts by weight of Astragalus Root, 1.5 parts by weight of Astragalus Root, 2 parts by weight of Polygala Root, and 1 part by weight of Licorice Root, which were then chopped and extracted with 20 times the weight of water (540 parts by weight) at about 100°C for 1 hour, centrifuged to obtain an extract, which was concentrated under reduced pressure and dried using a spray dryer to obtain Angelica sinensis extract powder. The obtained Angelica sinensis extract powder was 10.8g per 100g of raw herbal mixture. The drying using a spray dryer was performed by dropping the extract into an atomizer rotating at 10,000 rpm and supplying hot air at 150°C.
試験例
剥脱性口唇炎が認められる被験者10名(いずれも冷え性及び貧血の症状を有していなかった。)に、当帰飲子エキス末を、1日当たり2.85g(乾燥エキス量換算、3回/日に分けて食後に服用)を1週間服用させた。
Test Example: Ten subjects with exfoliative cheilitis (none of whom had symptoms of poor circulation or anemia) were given 2.85 g of Angelica sinensis extract powder per day (equivalent to the amount of dried extract, taken three times a day after meals) for one week.
服用前及び服用後において、顔画像解析装置VISIA(ニュースキンジャパン株式会社)を用いて、口唇の荒れが生じている面積(pixel2)を算出した。その結果、服用前の口唇における荒れ面積は平均6,773pixel2に対し、服用後の口唇における荒れ面積は僅か平均639pixel2であった。つまり、当帰飲子エキス末の服用によって、剥脱性口唇炎が大幅に改善した。 The area of chapped lips (pixels 2 ) was calculated using a face image analyzer VISIA (Nuskin Japan Co., Ltd.) before and after taking the drug. The results showed that the area of chapped lips before taking the drug was an average of 6,773 pixels 2 , while the area of chapped lips after taking the drug was only an average of 639 pixels 2. In other words, taking Angelica sinensis extract powder significantly improved exfoliative cheilitis.
さらに、被験者の1人について、服用前後の口唇の写真を、図1(服用前;荒れ面積8,258pixel2)及び図2(服用後;荒れ面積399pixel2)に示す。図示されるとおり、この被験者の剥脱性口唇炎は、僅か1週間の当帰飲子の服用でほぼ完治していた。 Furthermore, for one of the subjects, photographs of the lips before and after administration are shown in Figure 1 (before administration; rough area 8,258 pixels 2 ) and Figure 2 (after administration; rough area 399 pixels 2 ). As shown in the figure, the exfoliative cheilitis of this subject was almost completely cured after only one week of administration of Angelica sinensis.
さらに、被験者に口唇炎の改善の実感についてアンケート評価したところ、満足又はどちらかといえば満足と回答した被験者は90%にも達した。 Furthermore, when subjects were asked to complete a questionnaire to assess their experience of improvement in their cheilitis, 90% of them answered that they were satisfied or somewhat satisfied.
Claims (1)
An oral medication containing Angelica sinensis extract that is used to treat exfoliative cheilitis.
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| CN103877200A (en) | 2014-03-13 | 2014-06-25 | 王斌 | Traditional Chinese medicine for treating exfoliative cheilitis |
| CN107753837A (en) | 2017-10-26 | 2018-03-06 | 四川聚豪生物科技有限公司 | A kind of new medicine composition for treating chronic cheilitis and preparation method |
| CN109865103A (en) | 2017-12-05 | 2019-06-11 | 李澎 | A kind of Chinese traditional medicine composition for treating the exfoliative inflammation of lips |
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| CN103877200A (en) | 2014-03-13 | 2014-06-25 | 王斌 | Traditional Chinese medicine for treating exfoliative cheilitis |
| CN107753837A (en) | 2017-10-26 | 2018-03-06 | 四川聚豪生物科技有限公司 | A kind of new medicine composition for treating chronic cheilitis and preparation method |
| CN109865103A (en) | 2017-12-05 | 2019-06-11 | 李澎 | A kind of Chinese traditional medicine composition for treating the exfoliative inflammation of lips |
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