CN111150738A - External medicine for treating skin diseases - Google Patents

External medicine for treating skin diseases Download PDF

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Publication number
CN111150738A
CN111150738A CN202010081965.3A CN202010081965A CN111150738A CN 111150738 A CN111150738 A CN 111150738A CN 202010081965 A CN202010081965 A CN 202010081965A CN 111150738 A CN111150738 A CN 111150738A
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CN
China
Prior art keywords
rivanol
gentamicin
skin diseases
medicine
lidocaine
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Pending
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CN202010081965.3A
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Chinese (zh)
Inventor
郭坤
程传涛
耿松梅
曾维惠
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Second Affiliated Hospital School of Medicine of Xian Jiaotong University
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Second Affiliated Hospital School of Medicine of Xian Jiaotong University
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Priority to CN202010081965.3A priority Critical patent/CN111150738A/en
Publication of CN111150738A publication Critical patent/CN111150738A/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/7036Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/473Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention discloses an external medicine for treating skin diseases, belonging to the field of skin disease medicines. An external medicine for treating skin diseases comprises lidocaine, rivanol and gentamicin, wherein the mass ratio of the lidocaine, the rivanol and the gentamicin is (20-80): (125-500): (60-240). The gentamicin and the rivanol have the effects of mainly acting on gram-negative bacteria, the rivanol mainly acts on gram-positive bacteria, and the gentamicin and the rivanol can play a complementary and synergistic effect when being used in a combined manner, so that the gentamicin and the rivanol have an effective inhibition effect on most bacteria. The medicine has the advantages of strong anti-inflammatory, bactericidal and analgesic effects, quick response, wide dispersion, direct and small side effect and wide safety range of local external application, has no obvious side effect of the local external application, and has no irritation to skin injury parts.

Description

External medicine for treating skin diseases
Technical Field
The invention belongs to the field of skin disease drugs, and particularly relates to an external drug for treating skin diseases.
Background
Currently, the most common types of topical drugs for the treatment of acute and chronic allergic, infectious and autoimmune skin diseases include: glucocorticoids, antibiotics, Chinese medicinal extract preparations, immunosuppressants, etc.
The typical drugs of the glucocorticoid external drugs include flumethasone ointment, fluticasone propionate cream, halcinonide cream, hydrocortisone butyrate cream and the like, and have the following advantages: the traditional Chinese medicine has the advantages of various types, easiness in purchase, wide application range and quick curative effect; also has the following disadvantages: the applied part is susceptible to secondary bacterial, viral and fungal infections, such as folliculitis, viral wart, herpes simplex, tinea corporis, etc.; the skin atrophy, thinning and expansion lines are easy to appear on the applied part; spreading the part for secondary telangiectasia; hirsutism and pigment loss or deposition appear at the coated part; the glucocorticoid can be absorbed by the skin to cause Cushing syndrome and the like after being externally applied to a large area and a large dose for a long time. Typical medicines of the antibiotic external medicine include fusidic acid cream, compound polymyxin B ointment and mupirocin ointment, and have good anti-inflammatory and bactericidal effects, but have the following defects: the composition is single, the medicine has weak osmosis effect on exudative diseases, and medicinal scabs are formed on the surface of skin lesions, so that the medicine is difficult to clean and aggravates infection; the effect is single, and the medicine is only effective on infectious diseases; ointment preparations have a slightly irritating response to the wound. The representative medicines of the traditional Chinese medicine extraction preparation comprise a rehabilitation new liquid, a compound yellow Po liquid, a ginseng-cypress lotion and the like, and as a non-hormone aqueous solution, the traditional Chinese medicine extraction preparation has good effects on exudation and erosion and does not cause the side effect of the hormone; but has the following disadvantages: the traditional Chinese medicine preparation has complex components and undefined pharmaceutical mechanism, only has the characteristic of convergence, is only effective on exudative diseases, does not have the functions of relieving pain and resisting bacteria, so the application range is narrow, and the effects on infectious, painful and autoimmune diseases are not good; some drugs are also prone to irritation. Typical immunoregulatory drugs include tacrolimus ointment and pimecrolimus cream, which are used as non-hormonal drugs and are used when the traditional therapy is poor or glucocorticoid drugs are not suitable; but has the following disadvantages: the skin has burning sensation, pruritus, erythema and other stimulation reactions; part of the medicine has photosensitivity, and part of the medicine is limited in use; the risk of local secondary infection, such as local folliculitis, herpes and the like can occur; has slow effect, long treatment course and easy rebound after stopping taking medicine.
As described above, many kinds of external drugs for treating skin diseases have a single action, and there is a lack of an external drug effective for acute and chronic allergic, infectious, painful, and autoimmune skin diseases characterized by exudation, erosion, ulcer, pain, and the like. At present, only a method for combining a plurality of medicines can be used for treating patients with acute and chronic allergic, infectious, painful and autoimmune skin diseases with the characteristics of exudation, erosion, ulcer, pain and the like, and the combined use of a plurality of medicines with different action mechanisms can play a certain role in treatment, but the following problems exist in the practical use: the medicines are various in types, and adverse reactions such as stimulation and pain are easy to occur after combined use; the general external medicine is applied for 2-3 times every day, at least half an hour is needed between every two medicines, 2-3 medicines are applied every day, so that the time cost is greatly increased, and the types or the use times of the medicines can be only reduced for patients in order not to influence normal life and work, so that the treatment effect is greatly reduced. Therefore, in clinical medicine use, an external medicine effective for acute and chronic allergic, infectious, painful and autoimmune skin diseases with characteristics of exudation, erosion, ulcer, pain and the like is urgently needed.
Disclosure of Invention
The invention aims to solve the problems that the existing dermatological drugs have single effect and cannot be used for treating the dermatosis with multiple symptoms, and provides an external medicine for treating the dermatosis.
In order to achieve the purpose, the invention adopts the following technical scheme to realize the purpose:
an external medicine for treating skin diseases comprises lidocaine, rivanol and gentamicin, wherein the mass ratio of the lidocaine, the rivanol and the gentamicin is (20-80): (125-500): (60-240).
Further, the external medicine for treating skin diseases is in the form of aqueous solution, cream, ointment or gel.
Further, for non-aqueous solution dosage forms, per 10 grams of gel, ointment or cream, lidocaine is 80mg, rivanol is 25mg, gentamicin is 12 mg.
Further, for the aqueous solution formulation, each 50mL of the aqueous solution contains 4mg of lidocaine, 25mg of rivanol, and 12mg of gentamicin.
Further, when used for treating exudative allergic dermatoses, the extract is administered at a dose of 50cm2Skin wound surface, corresponding amount is lidocaine 40mg, rivanol 250mg and gentamicin 120 mg.
Further, when used for treating acute and chronic erosion, ulcer and infectious skin diseases, the dosage is 50cm2Skin wound, corresponding amounts are lidocaine 40mg, rivanol 500mg and gentamicin 240 mg.
Further, when used for treating autoimmune skin diseases of erosion, exudation, and pain, the composition is administered every 50cm2Skin wound, corresponding amounts of lidocaine 80mg, rivanol 500mg and gentamicin 240 mg.
Compared with the prior art, the invention has the following beneficial effects:
the external medicine for treating skin diseases comprises lidocaine, rivanol and gentamicin, wherein the mass ratio of the lidocaine, the rivanol and the gentamicin is (20-80): (125-500): (60-240); the invention changes the conventional using method of two medicaments, namely lidocaine and gentamicin, can reduce the side effect of the whole body, enables the medicaments to directly act on the focus part, and quickly plays the roles of relieving pain and sterilizing; the gentamicin and the rivanol have the effects of mainly acting on gram-negative bacteria, the rivanol mainly acts on gram-positive bacteria, and the gentamicin and the rivanol can play a complementary and synergistic effect when being used in a combined manner, so that the gentamicin and the rivanol have an effective inhibition effect on most bacteria. The medicine has the advantages of strong anti-inflammatory, bactericidal and analgesic effects, quick response, wide dispersion, direct and small side effect and wide safety range of local external application, has no obvious side effect of the local external application, and has no irritation to skin injury parts.
Detailed Description
Technical solutions in embodiments of the present invention are clearly and completely described in order to enable those skilled in the art to better understand the present invention, and it is obvious that the described embodiments are only a part of the embodiments of the present invention, and not all embodiments. All other embodiments, which can be derived by a person skilled in the art from the embodiments given herein without making any creative effort, shall fall within the protection scope of the present invention.
At present, a large number of patients with acute and chronic allergic, infectious, painful and autoimmune skin diseases are clinically suffered, skin rash of the patients has the characteristics of exudation, erosion, ulcer, pain and the like, a large number of antibiotics and hormones are usually required to be intravenously administered for treatment, although the treatment effect on the diseases can be achieved, a large number of side effects exist, and if the local skin rash is timely taken and nursed, the condition of the diseases can be relieved, and the side effect of systemic medication can be reduced. At present, an external medicine with the functions of resisting bacteria, relieving pain and astringing is lacking clinically, but the medicine has the characteristics, and in clinical practice, people use the medicine for acute and chronic allergic, infectious, painful and autoimmune skin diseases, and the medicine has the characteristics of quick response, good effect, low cost, no side effect of hormone medicines and the like.
1) Lidocaine is an amide local anesthetic, can interact with receptors on the inner side of the sodium channel axial pulp of a nerve cell membrane to block sodium ion inflow, reversibly blocks the impulse conduction of nerve fibers to generate a local anesthetic effect, has the characteristics of quick response, wide dispersion, strong penetrability and the like, and is mainly used for local or general anesthesia clinically. 2) Rivanol is a antiseptic disinfectant, can kill gram-positive cocci, and is commonly used for external application sterilization in dermatology. 3) Gentamicin is effective on gram-positive bacteria and gram-negative bacteria, and clinically, infections caused by escherichia coli, shigella dysenteriae, klebsiella pneumoniae and the like are mainly treated by intramuscular injection or intravenous administration, but the medicines are widely applied, and the number of drug-resistant strains is gradually increased. The drug resistance is caused by the fact that antibiotics repeatedly act on bacteria, so that the genetic materials of the bacteria are changed, the types of the bacteria are completely different from the types of pathogenic bacteria in a body, and the bacteria on the surface of the skin mainly comprise staphylococcus, streptococcus, pseudomonas aeruginosa, propionibacterium and the like. Therefore, the medicine of the invention is externally used, which not only can reuse antibiotics with systemic drug resistance, but also can kill skin epidermal bacteria.
The inventor, as a person skilled in the art, does not find incompatibility among the above three ingredients in the pharmacopoeia, and does not find the three ingredients in the combination in the prior art. After the maximum safe initial dose of the three drugs used in clinic is consulted and a plurality of cases are treated by combining repeated tracking in clinic, the domestic conventional using dose of the lidocaine is determined to be 20-80 mg, the conventional using dose of the rivanol is not more than 500mg, the using dose of the gentamicin is determined to be 60-240 mg, and the mass ratio of the three is (20-80): (125-500): (60-240). Determining specific medicine proportion according to skin lesion manifestations of different types of diseases, such as allergic skin diseases mainly based on exudation, and only increasing the proportion of rivanol plays a role in convergence; if the infectious skin diseases mainly including erosion and ulcer are caused, the proportion of rivanol and gentamicin is increased to play the roles of convergence and infection resistance; for autoimmune skin diseases such as erosion, exudation and pain, the three drugs are used to achieve the maximum safe dose and have the effects of astringing, relieving pain and resisting infection.
Example 1
The external medicine for treating skin diseases of example 1 is in the form of an aqueous solution containing 8mg of lidocaine, 50mg of rivanol and 24mg of gentamicin per 100mL of the aqueous solution.
Case 1 female, 20 years old, visit our hospital with the complaint of "erythema, blisters, exudation with pruritus for 6 days on both upper limbs". The admission diagnosis is: eczema (allergic dermatitis). Admission to the examinee: vital signs: the body temperature is 36.4 ℃, the pulse is 78 times/minute, the breath is 20 times/minute, the blood pressure is 110/92mmHg, and no obvious abnormality is seen in the heart, the lung and the abdomen. Dermatological conditions: diffuse erythema can be seen on both upper limbs, erythema boundary is unclear, the surface can be seen dispersed in the water blister with different distribution sizes, the blister liquid is clear, a large amount of yellow exudate is on the surface of the water blister, and part of the water blister forms yellow scab.
The medicine of example 1 is used for wet-compressing the skin wound of a patient, 3 times a day, 50mL of the medicine is used each time, 10min is used each time, and 3 times a day; after 3 days of treatment, the erythema on both upper limbs became obviously lighter, the surface exudation was obviously reduced, and most of the blisters were dry and crusted. The pruritus is obviously relieved in the using process of the medicine, no obvious discomfort exists, and the vital signs are stable; on day 7 of treatment, erythema on both upper extremities subsided substantially, superficial blisters subsided, and crusts fell off. The body temperature is 36.8 ℃, the pulse is 80 times/minute, the breath is 21 times/minute, the blood pressure is 120/95mmHg, and the physical examination is not abnormal.
Example 2
The external medicine for treating skin diseases of example 2 is in the form of an aqueous solution, and 8mg of lidocaine, 100mg of rivanol, and 48mg of gentamicin are contained in each 100mL of the aqueous solution.
Case 2 female, 65 years old, visit our hospital with a complaint of "red blotches, blisters, pustules with pain for 7 days on the left back and back". The admission diagnosis is: herpes zoster secondary infection (infectious skin disease). Admission to the examinee: vital signs: the body temperature is 38.4 ℃, the pulse is 89 times/minute, the respiration is 23 times/minute, the blood pressure is 140/90mmHg, and no obvious abnormality is seen in the heart, the lung and the abdomen. Dermatological conditions: diffuse erythema with zonal distribution can be seen on the left waist and back, the erythema boundary is clear, densely distributed blisters with different sizes, pustules and turbid bleb liquid can be seen on the surface, and partial small blebs are fused into large blebs. The medicine of example 2 is applied to the affected part in a wet manner, 50mL each time, 10 min/time, 3 times daily. After 5 days of treatment, the red spots on the left waist and the back obviously become light, the surface exudation is obviously reduced, part of small blisters are dried and scabbed, and the pain feeling is obviously relieved. The patient has no obvious discomfort and the vital signs are stable in the using process of the medicine. The erythema on the left waist and back basically subsides on the 7 th day of treatment, the blisters on the surfaces are mostly scabbed and shed, and brown pigmentation is remained on the parts; the body temperature is 36.8 ℃, the pulse is 80 times/minute, the breath is 21 times/minute, the blood pressure is 130/80mmHg, and the physical examination is not abnormal.
Example 3
The external medicine for treating skin diseases of example 3 was in the form of an aqueous solution (16 mg of lidocaine, 100mg of rivanol, and 48mg of gentamicin per 100 mL) and a cream (8 mg of lidocaine, 25mg of rivanol, and 12mg of gentamicin per 10g of cream).
Case 3 the male, 35 years old, came to the hospital with the complaint of "ulceration of the left lower limb, exudation with pain for 7 days". The admission diagnosis is: pyoderma gangrenosum (autoimmune disease). Admission to the examinee: vital signs: the body temperature is 36.4 ℃, the pulse is 76 times/minute, the respiration is 21 times/minute, the blood pressure is 120/80mmHg, and no obvious abnormality is seen in the heart, the lung and the abdomen. Dermatological conditions: the front of the shin of the left lower limb can be seen with 3cm multiplied by 4cm ulcer surface, the ulcer boundary is not clear, the edge is slightly raised, the ulcer surface has yellow exudate, the tenderness is positive, and the bacteria culture of local secretion shows staphylococcus aureus +; after the aqueous solution medicament of the example 3 is used, 50mL of the medicament is used each time, 10min is used each time, and 3 times of treatment are carried out each day for 5 days, the exudation on the surface of the ulcer of the left lower limb is obviously reduced, the pain sensation of the left lower limb is obviously relieved, the ulcer edge becomes shallow, the area becomes small, the bacterial culture of local secretion is negative, at the moment, the emulsifiable paste of the example 3 is added after the medicinal liquid is wet-coated, the patient has no obvious discomfort in the using process of the medicament, and the vital signs are stable; on the 7 th day of treatment, no secretion exists on the surface of the ulcer surface, the ulcer surface is further reduced and becomes shallow, and no pain exists; the body temperature is 36.6 ℃, the pulse is 76 times/minute, the breath is 21 times/minute, the blood pressure is 120/80mmHg, and the physical examination is not abnormal.
The above-mentioned contents are only for illustrating the technical idea of the present invention, and the protection scope of the present invention is not limited thereby, and any modification made on the basis of the technical idea of the present invention falls within the protection scope of the claims of the present invention.

Claims (7)

1. An external medicine for treating skin diseases is characterized by comprising lidocaine, rivanol and gentamicin, wherein the mass ratio of the lidocaine, the rivanol and the gentamicin is (20-80): (125-500): (60-240).
2. The external medicine for treating skin diseases according to claim 1, wherein the external medicine for treating skin diseases is in the form of an aqueous solution, cream, ointment or gel.
3. The external medicine for treating skin diseases according to claim 2, wherein the lidocaine is 80mg, the rivanol is 25mg and the gentamicin is 12mg per 10g of the gel, ointment or cream for the non-aqueous solution dosage form.
4. The external medicine for treating skin diseases according to claim 2, wherein the amount of lidocaine is 4mg, rivanol is 25mg, and gentamicin is 12mg per 50mL of aqueous solution for the aqueous solution dosage form.
5. The external preparation for skin diseases according to claim 1, wherein the external preparation is used for the treatment of exudative allergic skin diseases at a rate of 50cm per day2The corresponding amount of the skin wound surface of (1) is 40mg of lidocaine, 250mg of rivanol and 120mg of gentamicin.
6. The external medicine for treating skin diseases according to claim 1, wherein the medicine is used for treating acute and chronic erosion, ulcer and infectious skin diseases, and the dosage of the medicine is 50cm per time2The corresponding amount of the skin wound surface of (1) is 40mg of lidocaine, 500mg of rivanol and 240mg of gentamicin.
7. The external medicine for treating skin diseases according to claim 1, wherein the medicine is used for treating erosive, exudative, painful autoimmune skin diseases at a dose of 50cm per dose2The corresponding amount of lidocaine 80mg, rivanol 500mg and gentamicin 240 mg.
CN202010081965.3A 2020-02-06 2020-02-06 External medicine for treating skin diseases Pending CN111150738A (en)

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CN202010081965.3A CN111150738A (en) 2020-02-06 2020-02-06 External medicine for treating skin diseases

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022254363A1 (en) * 2021-06-03 2022-12-08 Stichting Medische Kliniek Velsen Lidocaine or articaine for treating covid-19, autoimmune disease or cytokine storm response

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CN101703775A (en) * 2009-08-05 2010-05-12 厦门金日制药有限公司 Medicinal composition for treating canker sore and local infection of body surface and reducing inflammation, product and application thereof

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Publication number Priority date Publication date Assignee Title
CN1151286A (en) * 1995-11-28 1997-06-11 高凤岐 Rivanol and lignocaine mixture
KR20010007724A (en) * 2000-07-04 2001-02-05 임준기 The band with an anesthesia effect and sterilization
JP2004210668A (en) * 2002-12-27 2004-07-29 Lion Corp Medicine composition for external use
CN101703775A (en) * 2009-08-05 2010-05-12 厦门金日制药有限公司 Medicinal composition for treating canker sore and local infection of body surface and reducing inflammation, product and application thereof

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刘丽影等: "25 例恶性肿瘤患者放疗并发带状疱疹的护理", 《中国城乡企业卫生》 *
刘玲等: "中西医综合治疗带状疱疹的临床观察", 《医药论坛杂志》 *
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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022254363A1 (en) * 2021-06-03 2022-12-08 Stichting Medische Kliniek Velsen Lidocaine or articaine for treating covid-19, autoimmune disease or cytokine storm response
GB2607584A (en) * 2021-06-03 2022-12-14 Stichting Medische Kliniek Velsen Composition and method of treatment
GB2607584B (en) * 2021-06-03 2024-07-17 Stichting Medische Kliniek Velsen Composition and method of treatment

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Application publication date: 20200515

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