Coptis chinensis (Chinese Goldthread)

Coptis chinensis (Chinese Goldthread)

Product Name: Coptis chinensis — коптис китайский, Coptis chinensis, Chinesischer Gelbwurz, Coptis chino, Coptide chinoise, كوپتيس صيني, โคปติส ไชนีซ, Xitoy kopchisi, Кытай коптиси, Çin qoptisi, Коптиси хитоӣ, Geltonšaknis kopti, Ķīnas koptis, Коптис китайський, Çin qoptisi, קופטיס סיני

Synonyms: коптис, золотая нить, золотая нить китайская, китайский коптис, китайская коптида, золотая печать, coptide, Chinese goldthread, goldthread, coptis root, Chinesische Goldfadenwurzel, Chinesische Coptis, raíz de coptis, hilo de oro, racine de coptide, fil d’or, كف الذئب الصيني, الجذر الذهبي, รากทองจีน, โกลด์เธรด

Main Indications for Use of Coptis chinensis: Gastritis with increased acidity, gastric ulcer, duodenitis, infectious colitis, bacterial dysentery, acute and chronic gastroenteritis, food toxic infections, pulmonary tuberculosis, chlamydial pneumonia, acute and chronic bronchitis, meningitis of bacterial nature, osteomyelitis, carbuncle, furunculosis, papulopustular acne, pseudomembranous colitis, purulent cholangitis, bacterial cystitis, urethritis, vaginitis, mucosal candidiasis, herpes zoster, diabetic retinopathy, arterial hypertension, coronary heart disease, hyperthyroidism.

Use of Coptis chinensis in Mixtures and Complexes: Hepatitis B, hepatitis C, liver cirrhosis, dyslipidemia, metabolic syndrome, obesity, type 2 diabetes mellitus, atherosclerosis, ulcerative colitis, Crohn's disease, systemic lupus erythematosus, rheumatoid arthritis, Helicobacter gastritis, neurodermatitis, eczema, rosacea, seborrheic dermatitis, chronic rhinosinusitis, cystopyelitis, nephritis.

Pharmacological Properties of Coptis chinensis: Anti-inflammatory, antimicrobial, antibacterial, antiviral, antiprotozoal, antimycotic, hepatoprotective, antioxidant, hypoglycemic, hypolipidemic, antihypertensive, neuroprotective, antidepressant, antipyretic, spasmolytic, choleretic, antiulcer, immunomodulatory, antiangiogenic, inhibiting P-gp and CYP3A4, inhibiting NF-κB and TNF-α, inhibiting tumor cell growth.

Dosage of Pharmaceutical Forms — Coptis chinensis

Powder — Coptis chinensis

Indications (Powder): Gastric ulcer, gastritis with increased acidity, acute and chronic gastroenteritis, pseudomembranous colitis, bacterial dysentery, mucosal candidiasis, vaginitis, bacterial cystitis, furunculosis, papulopustular acne.

Standard Dosage (Powder): 0.5 g twice daily before meals, washed down with warm water.

Enhanced Dosage (Powder): 1 g 3 times a day for gastric ulcer in the exacerbation phase, bacterial dysentery, pseudomembranous colitis, vaginitis, and furunculosis.

Maximum Dosage (Powder): 1.5 g 3 times a day. Permissible only for acute forms of infectious gastroenteritis and purulent cholangitis under specialist supervision for no more than 5 days.

Preventive Dosage (Powder): 0.3 g once daily on an empty stomach. Recommended in the presence of chronic inflammatory diseases of the gastrointestinal tract (gastritis, colitis), acne, and type 2 diabetes mellitus. Frequency: a 20-day course every 3 months.

Pediatric Dosage (Powder): Minimum age: 12 years, minimum body weight: 35 kg. 0.2 g twice daily after meals. For children under 12 years of age and with a lower body weight, use is not recommended.

Contraindications (Powder): Individual hypersensitivity, pronounced gastric hypoacidity, chronic hepatitis with cholestasis. Data on contraindications during pregnancy, lactation, and in childhood under 12 years of age have not been scientifically registered.

Side Effects (Powder): When the dosage is exceeded, nausea, bitterness in the mouth, decreased appetite, and headache are possible. All side effects were registered when taking more than 5 g of powder per day.

Adjustment for Patient Body Weight (Powder): For body weight below 60 kg — the dosage is reduced by 20% of the standard. For body weight over 90 kg — the dosage is increased by 25% of the standard.

Preparation Method (Powder): Ingredients per 100 g of product: Coptis chinensis rhizomes — 100 g. The roots are cleaned of dirt, washed with cold water, dried at a temperature of 45 °C for 24 hours, then ground to a homogeneous powder with a particle size of no more than 250 μm. The raw material is not subjected to thermal treatment above 50 °C in order to preserve thermolabile alkaloids. Store in an airtight glass container.

Storage Conditions and Shelf Life (Powder): Store in a dry place protected from light and electromagnetic fields, at a temperature of 5 to 25 °C. Relative air humidity no more than 60%. After opening the package, use within 60 days. Shelf life of the unopened package — 24 months.

Dry Extract — Coptis chinensis

Indications (Dry Extract): Gastritis with increased acidity, gastric ulcer, acute gastroenteritis, bacterial dysentery, mucosal candidiasis, papulopustular acne, bacterial cystitis, vaginitis.

Standard Dosage (Dry Extract): 200 mg of dry extract twice daily, dissolving in 100 ml of warm water, taken 20 minutes before meals.

Enhanced Dosage (Dry Extract): 400 mg 3 times a day under conditions of exacerbation of gastric ulcer, pseudomembranous colitis, bacterial dysentery, and furunculosis.

Maximum Dosage (Dry Extract): 600 mg 3 times a day, no more than 5 consecutive days. Used in inpatient regimens for severe forms of infectious colitis and intestinal candidiasis.

Preventive Dosage (Dry Extract): 100 mg once daily in the morning on an empty stomach, for 14 days. Repeat the course every 3 months for chronic gastritis, prediabetes, acne, and a tendency to infectious cystitis.

Pediatric Dosage (Dry Extract): For children over 12 years of age and with a body weight from 35 kg: 100 mg once daily after meals, dissolving in 50 ml of water.

Contraindications (Dry Extract): Hypoacid gastritis, ulcerative colitis in the exacerbation phase without antibiotic therapy, individual intolerance. Scientific data on contraindications during pregnancy, lactation, and in children under 12 years of age are absent.

Side Effects (Dry Extract): Cases of dyspepsia, nausea, metallic taste in the mouth, and headache have been registered when taking dosages above 1800 mg per day.

Adjustment for Patient Body Weight (Dry Extract): Body weight up to 60 kg — a 20% dosage reduction. Body weight over 90 kg — a 25% dosage increase.

Preparation Method (Dry Extract): Ingredients per 100 g of product: Raw material: crushed Coptis chinensis rhizomes — 500 g. Purified water — 1500 ml. Extraction is carried out at a temperature of 80 °C for 2 hours and repeated twice. The combined extracts are filtered, concentrated at a temperature not exceeding 55 °C in vacuum to a syrup-like state. Then drying is carried out by the spray method at a temperature of 60 °C. The yield of dry extract is about 20%.

Storage Conditions and Shelf Life (Dry Extract): Store in an airtight package made of light-impermeable material at a temperature of 5 to 25 °C, in a dry, darkened place shielded from electromagnetic sources. Shelf life — up to 24 months. After opening, use within 30 days.

Alcohol-Based Tincture — Coptis chinensis

Indications (Tincture): Gastritis with increased acidity, gastric ulcer, acute gastroenteritis, bacterial dysentery, pseudomembranous colitis, mucosal candidiasis, urethritis, furunculosis, herpes zoster.

Standard Dosage (Tincture): 20 drops (approximately 1 ml) per 50 ml of water twice daily, 30 minutes before meals.

Enhanced Dosage (Tincture): 40 drops (2 ml) 3 times a day for pseudomembranous colitis, oral candidiasis, and herpes zoster, course — up to 10 days.

Maximum Dosage (Tincture): 60 drops (3 ml) 3 times a day, short-term, no more than 5 days. Used for acute conditions: furunculosis, severe gastroenteritis, bacterial dysentery.

Preventive Dosage (Tincture): 10 drops per 30 ml of water once daily in the morning for 10 days. Prevention of exacerbations of gastritis, chronic candidiasis, and skin inflammations in patients with type 2 diabetes and recurrent cystitis. Repeat course — no earlier than after 2 months.

Pediatric Dosage (Tincture): Not recommended for children under 14 years of age. From 14 years — 5 drops per 30 ml of water twice daily.

Contraindications (Tincture): Alcohol dependence, epilepsy, acute psychoses, severe liver diseases. Scientific data on contraindications during pregnancy, lactation, and in children under 14 years of age are absent.

Side Effects (Tincture): Burning in the stomach, headache, and hypotension are possible when exceeding 9 ml of Tincture per day.

Adjustment for Patient Body Weight (Tincture): Patients with body weight below 50 kg: the dosage is reduced by 25%. Over 90 kg — increased by 20%.

Preparation Method (Tincture): Ingredients per 100 ml of product: Dried and crushed Coptis chinensis rhizomes — 20 g. 70% ethyl alcohol — 100 ml. The raw material is placed in a glass container, poured with alcohol, and infused for 10 days in a dark, cool place, shaking daily. Then it is strained and filtered through a paper filter. Store in a tightly closed glass container.

Storage Conditions and Shelf Life (Tincture): Store at a temperature of 10 to 25 °C, in a dark place protected from sources of EMI. Do not use if the liquid becomes turbid or a precipitate forms. Shelf life — 3 years. After opening the package, use within 90 days.

Oil Infusion — Coptis chinensis

Indications (Oil Infusion): Papulopustular acne, furunculosis, herpes zoster, candidiasis of skin folds, vaginitis, bacterial urethritis, external otitis, trophic ulcers.

Standard Dosage (Oil Infusion): Externally: apply in a thin layer to the affected skin area twice daily. Intravaginally — 3 ml into the vagina using a syringe without a needle once daily in the evening, course 5–7 days.

Enhanced Dosage (Oil Infusion): Externally: applications to the affected area 3 times a day for furunculosis, herpes, and bacterial vaginitis. In the case of trophic ulcers — apply a gauze napkin soaked in the infusion twice daily.

Maximum Dosage (Oil Infusion): No more than 5 ml per single application, no more than 15 ml per day. Do not use for longer than 10 consecutive days without a break.

Preventive Dosage (Oil Infusion): Apply once daily in a thin layer to the area prone to inflammation (beard growth zone, wings of the nose, skin folds) for 7 days once a month. Recommended for chronic acne, seborrheic dermatitis, and recurrent herpes.

Pediatric Dosage (Oil Infusion): Permitted from 6 years of age. Apply externally once daily to the affected area, no more than 1 ml. Do not use on extensive areas of skin.

Contraindications (Oil Infusion): Allergy to the components of the preparation, purulent wounds with necrosis, fresh burns of degree II–III. Scientific data on contraindications during pregnancy, lactation, and in childhood are limited.

Side Effects (Oil Infusion): With prolonged use or violation of the preparation technology, skin irritation, contact dermatitis, and itching are possible. Registered when used for more than 15 consecutive days.

Adjustment for Patient Body Weight (Oil Infusion): For external use, no adjustment for body weight is required. For intravaginal use, patients with body weight below 45 kg — the volume is reduced to 2 ml.

Preparation Method (Oil Infusion): Ingredients per 100 g of product: Dry crushed Coptis chinensis rhizomes — 10 g. Unrefined coconut oil — 90 g. Pour the raw material into a sterile glass container and fill with warm (35–40 °C) coconut oil. Keep in a water bath at a temperature of 45 °C for 3 hours. Cool, filter through gauze, and store in a dark jar.

Storage Conditions and Shelf Life (Oil Infusion): Store in a cool, light-protected place at a temperature of 5 to 20 °C. After opening, use within 45 days. Avoid water entering the package. Shielding from electromagnetic radiation is desirable. Shelf life — 12 months.

Vaginal Suppositories — Coptis chinensis

Indications (Vaginal Suppositories): Vaginitis, vaginal candidiasis, bacterial vaginosis, trichomonal colpitis, cervicitis.

Standard Dosage (Vaginal Suppositories): 1 suppository (1.5 g) once daily in the evening, insert deep into the vagina in a lying position. Course — 7 days.

Enhanced Dosage (Vaginal Suppositories): 1 suppository twice daily (morning and evening) for acute candidal vaginitis, bacterial vaginosis, and colpitis. Course — up to 10 days.

Maximum Dosage (Vaginal Suppositories): 2 suppositories twice daily, no more than 4 suppositories per day, course up to 5 days under conditions of active combination therapy.

Preventive Dosage (Vaginal Suppositories): 1 suppository once every 3 days in the evening, course of 10 applications. Recommended for a tendency to recurrent vaginitis and chronic bacterial vaginosis, especially in women with type 2 diabetes and in premenopause. Repeat course — after 2 months.

Pediatric Dosage (Vaginal Suppositories): Use is permissible from 14 years of age in the presence of clinical indications. Standard dosage — 1 suppository every other day for 5 days.

Contraindications (Vaginal Suppositories): Hypersensitivity to components, acute inflammatory process in the lesser pelvis with purulent discharge, intolerance to coconut oil. Scientific data on use in the first trimester of pregnancy and during lactation are absent. Use in adolescence requires medical supervision.

Side Effects (Vaginal Suppositories): Local burning, increased discharge, and contact dermatitis in the area of the external genitalia have been registered with prolonged use for more than 10 consecutive days.

Adjustment for Patient Body Weight (Vaginal Suppositories): No dosage adjustment for body weight is required.

Preparation Method (Vaginal Suppositories): Ingredients per 100 g of product: Dry Coptis chinensis extract — 5 g. Coptis chinensis rhizome powder — 10 g. Refined coconut oil — 85 g. The dry extract is dissolved in 10 ml of oil, the powder is added, and the mixture is stirred until a homogeneous suspension is obtained. The mixture is introduced into oil melted in a water bath, the mass is brought to 40 °C, and poured into suppository molds (1.5 g each). Cooled until solidified.

Storage Conditions and Shelf Life (Vaginal Suppositories): Store in the refrigerator at a temperature of +2 to +8 °C, in light-impermeable packaging. Avoid exposure to EMI. After opening, use within 30 days. Shelf life under proper storage conditions — 12 months.

Rectal Suppositories — Coptis chinensis

Indications (Rectal Suppositories): Proctitis, anal fissures, hemorrhoids, chronic colitis, pseudomembranous colitis, parasitic proctosigmoiditis.

Standard Dosage (Rectal Suppositories): 1 suppository (1.5 g) rectally once daily at night after defecation. Course — 7 days.

Enhanced Dosage (Rectal Suppositories): 1 suppository twice daily (morning and evening) for pseudomembranous colitis, proctitis, and anal fissures. Duration — up to 10 days.

Maximum Dosage (Rectal Suppositories): Up to 2 suppositories twice daily (4 per day) for pronounced inflammation, hemorrhoidal bleeding, and acute colitis. Course — up to 5 days under medical supervision.

Preventive Dosage (Rectal Suppositories): 1 suppository once every 3 days at night for 10–12 applications. Recommended for chronic colitis, constipation, and exacerbations of hemorrhoids, especially in patients with metabolic syndrome and a sedentary lifestyle. Repeat course — after 2 months.

Pediatric Dosage (Rectal Suppositories): Use is permissible from 10 years of age with a body weight from 30 kg. Standard dosage — ½ suppository (0.75 g) once daily in the evening.

Contraindications (Rectal Suppositories): Individual intolerance, acute purulent paraproctitis, pronounced spasm of the anal sphincter. Scientific data on use in pregnant, breastfeeding women, and children under 10 years of age are absent.

Side Effects (Rectal Suppositories): Rarely, burning in the rectum, increased peristalsis, mucous discharge, and contact dermatitis of the perianal area are noted with use for more than 10 days.

Adjustment for Patient Body Weight (Rectal Suppositories): Up to 45 kg — use half-dosage suppositories (0.75 g). Over 90 kg — the standard dosage is doubled for acute inflammation.

Preparation Method (Rectal Suppositories): Ingredients per 100 g of product: Dry Coptis chinensis extract — 5 g. Coptis chinensis rhizome powder — 10 g. Refined coconut oil — 85 g. The extract is dissolved in 10 ml of warm oil. The mixture of powder and extract is thoroughly mixed with oil melted in a water bath. At a temperature of 40–42 °C, the mass is poured into molds. Cooling — until completely solidified (4–6 °C).

Storage Conditions and Shelf Life (Rectal Suppositories): Store in the refrigerator at a temperature of +2 to +8 °C, in airtight light-impermeable packaging. Avoid sources of EMI. After opening, use within 30 days. Total shelf life — 12 months.

Nasal Drops — Coptis chinensis

Indications (Nasal Drops): Chronic rhinosinusitis, allergic rhinitis, bacterial rhinitis, acute rhinitis, acute frontal sinusitis, chronic maxillary sinusitis.

Standard Dosage (Nasal Drops): 2 drops into each nostril twice daily, morning and evening, for 7 days.

Enhanced Dosage (Nasal Drops): 3 drops into each nostril 3 times a day for purulent rhinosinusitis, frontal sinusitis, and bacterial rhinitis. Course — 10 days.

Maximum Dosage (Nasal Drops): Up to 4 drops 4 times a day, no more than 5 consecutive days. Used for severe maxillary sinusitis and exacerbation of chronic frontal sinusitis.

Preventive Dosage (Nasal Drops): 1 drop into each nostril once daily during the season of viral respiratory infections or upon contact with allergens. Preventive course — 10 days. Repeat — every 2 months.

Pediatric Dosage (Nasal Drops): From 7 years — 1 drop into each nostril 1–2 times a day. Under 7 years, use is not recommended due to the risk of mucosal irritation.

Contraindications (Nasal Drops): Nasal polyposis, bleeding of the nasal mucosa, atrophic rhinitis. Scientific data on contraindications during pregnancy, lactation, and in children under 7 years of age are absent.

Side Effects (Nasal Drops): Short-term burning in the nose, sneezing, and increased secretion. When the dose is exceeded, mucosal irritation and reflex edema are possible.

Adjustment for Patient Body Weight (Nasal Drops): For patients with body weight below 45 kg — do not exceed the standard dosage. Body weight above 45 kg does not require correction.

Preparation Method (Nasal Drops): Ingredients per 100 ml: Dry Coptis chinensis extract — 1 g. Distilled water — 95 ml. Vegetable glycerin — 4 ml. Dissolve the extract in warm water (35–40 °C), stir thoroughly, add glycerin to increase viscosity and prolong the action. Filter the solution through a sterile 0.22 μm membrane filter. Dispense into sterile dropper bottles.

Storage Conditions and Shelf Life (Nasal Drops): Store in the refrigerator at a temperature of +2 to +8 °C, in light-impermeable packaging. After opening, use within 14 days. Total shelf life — 6 months. Avoid contact with contaminated surfaces.

Ear Drops — Coptis chinensis

Indications (Ear Drops): Acute external otitis, chronic external otitis, bacterial otomycosis, eczema of the auditory canal, itching and inflammation of the external ear.

Standard Dosage (Ear Drops): 2 drops into the external auditory canal twice daily. After instillation, it is recommended to lie on the side for 5–10 minutes. Course — 5–7 days.

Enhanced Dosage (Ear Drops): 3 drops 3 times a day for purulent external otitis, pronounced inflammation of the auditory canal, and bacterial otomycosis. Duration — up to 10 days.

Maximum Dosage (Ear Drops): Up to 4 drops 4 times a day, no more than 5 consecutive days. Use only for pronounced edema and pain syndrome, under medical supervision.

Preventive Dosage (Ear Drops): 1 drop into each ear once daily for 5 days after swimming in open water bodies or during the season of exacerbations. Recommended for people prone to external otitis or with eczema of the auditory canal. Repeat course — no earlier than after 6 weeks.

Pediatric Dosage (Ear Drops): From 6 years — 1 drop into the external auditory canal twice daily. Under 6 years, do not use without consultation with a physician.

Contraindications (Ear Drops): Perforation of the eardrum, allergy to the components of the preparation, presence of a foreign body in the auditory canal. Scientific data on safety during pregnancy, lactation, and in children under 6 years of age are absent.

Side Effects (Ear Drops): Registered: burning, increased itching, irritation of the auditory canal. With use for more than 10 days, skin peeling is possible.

Adjustment for Patient Body Weight (Ear Drops): Not required.

Preparation Method (Ear Drops): Ingredients per 100 ml: Dry Coptis chinensis extract — 2 g. Refined coconut oil — 98 ml. Dissolve the extract in coconut oil heated to 40 °C, keep in a water bath at a temperature of 45 °C for 1 hour. Filter the mixture through sterile gauze, dispense into sterile bottles with a drip dispenser.

Storage Conditions and Shelf Life (Ear Drops): Store at a temperature of +5 to +25 °C in a dark place. After opening, use within 30 days. Total shelf life — 12 months. Do not allow the dropper to come into contact with skin or earwax.

Ointment — Coptis chinensis

Indications (Ointment): Furunculosis, papulopustular acne, streptoderma, microbial eczema, candidiasis of skin folds, trophic ulcers, herpetic eruptions.

Standard Dosage (Ointment): Apply in a thin layer to the affected skin area twice daily, morning and evening. Course — 7–10 days.

Enhanced Dosage (Ointment): Apply 3 times a day for acute bacterial inflammation, furunculosis, herpetic eruptions, and microbial eczema. In severe cases — under an occlusive dressing.

Maximum Dosage (Ointment): Up to 5 applications per day, no more than 10 g of ointment per day, course — no more than 5 consecutive days.

Preventive Dosage (Ointment): Apply once daily in the evening to skin areas prone to inflammation (face, back, intergluteal area) for 5 days monthly. Recommended for chronic acne, seborrheic dermatitis, and recurrent skin candidiasis.

Pediatric Dosage (Ointment): From 6 years — apply once daily in a thin layer to limited skin areas, no more than 2 g per day. Do not use on damaged skin.

Contraindications (Ointment): Purulent wounds with necrosis, allergy to components, open burns of degree II–III, deep trophic ulcers with bleeding. Scientific data on contraindications during pregnancy, lactation, and under 6 years of age are absent.

Side Effects (Ointment): Skin irritation, contact dermatitis, and burning sensation. Side effects were recorded with use for more than 3 consecutive weeks or application to a large area (>30% of the skin surface).

Adjustment for Patient Body Weight (Ointment): Not required.

Preparation Method (Ointment): Ingredients per 100 g of product: Dry Coptis chinensis extract — 5 g. Coptis chinensis rhizome powder — 10 g. Beeswax — 10 g. Refined coconut oil — 75 g. The oil is heated in a water bath to 45 °C, and beeswax is dissolved in it. The extract and powder are introduced, thoroughly mixed until a homogeneous mass is obtained. Cooled with constant stirring to a temperature of 35 °C, packaged into tubes or jars.

Storage Conditions and Shelf Life (Ointment): Store at a temperature of +5 to +25 °C, in a place protected from light and EMI. After opening, use within 30 days. Shelf life — 12 months. Do not allow repeated heating.

Cream — Coptis chinensis

Indications (Cream): Papulopustular acne, seborrheic dermatitis, perioral dermatitis, inflammatory elements in rosacea, allergic contact dermatitis, skin irritation after shaving, skin inflammation in adolescents.

Standard Dosage (Cream): Apply in a thin layer to cleansed skin twice daily, morning and evening.

Enhanced Dosage (Cream): Apply up to 3 times a day to inflammation zones for pronounced acne, perioral dermatitis, and seborrheic skin lesions.

Maximum Dosage (Cream): Up to 4 times a day, no more than 5 consecutive days, volume no more than 10 g per day. Only for acute inflammatory conditions under dermatologist supervision.

Preventive Dosage (Cream): Once daily at night for 5–7 days monthly. Prevention of acne relapses, seasonal dermatitis, and skin inflammation after shaving.

Pediatric Dosage (Cream): From 6 years — once daily, no more than 2 g per day, applied spot-wise. Do not use in children under 6 years of age without specialist supervision.

Contraindications (Cream): Deep purulent processes, pronounced allergic reaction to the cream base, weeping forms of dermatitis. Data on contraindications during pregnancy and lactation have not been registered; for application to limited areas, external use is permissible.

Side Effects (Cream): Itching, peeling, dryness, and skin redness, especially with prolonged use or on sensitive facial skin.

Adjustment for Patient Body Weight (Cream): Not required.

Preparation Method (Cream): Ingredients per 100 g of product: Dry Coptis chinensis extract — 3 g. Chamomile hydrolate — 20 g. Coptis chinensis rhizome powder — 2 g. Refined coconut oil — 30 g. Emulsifier (natural, lecithin-based) — 3 g. Vegetable glycerin — 3 g. Purified water — up to 100 g. The oil and aqueous phases are prepared separately: coconut oil with powder is heated to 45 °C, the aqueous phase with hydrolate — to 40 °C. The emulsifier is introduced into the oil phase, then the phases are combined with thorough stirring until a homogeneous emulsion is formed. The extract and glycerin are introduced, stirred until thickening.

Storage Conditions and Shelf Life (Cream): Store in an airtight tube at a temperature of +5 to +20 °C, in a place protected from light and EMI. After opening, use within 30 days. Total shelf life — 6 months.

Serum — Coptis chinensis

Indications (Serum): Papulopustular acne, post-acne, hyperpigmentation, rosacea, oily seborrhea, skin inflammations in the T-zone, enlarged pores, irritation after cosmetic procedures.

Standard Dosage (Serum): Apply 2–3 drops to cleansed facial skin once daily in the evening with light massage movements. Do not rinse.

Enhanced Dosage (Serum): 2–3 drops twice daily, morning and evening, during the active phase of acne, post-inflammatory hyperpigmentation, and inflamed rosacea.

Maximum Dosage (Serum): Up to 4 drops 3 times a day on limited zones (forehead, nose, chin) for pronounced seborrhea and inflammation. Duration — no more than 5 days.

Preventive Dosage (Serum): 1–2 drops once daily in the evening, course 10–14 days, repeated monthly. Recommended for combination and oily skin prone to inflammation, when wearing medical masks, and working in a polluted environment.

Pediatric Dosage (Serum): Permitted from 12 years of age. 1 drop once daily on a limited area (for adolescent acne). Do not use in children under 12 years of age.

Contraindications (Serum): Allergy to components, individual hypersensitivity, pronounced couperose, weeping forms of dermatoses. Scientific data on contraindications during pregnancy and lactation have not been registered; external spot application is permissible.

Side Effects (Serum): Tingling sensation, mild redness, and peeling in the first 2–3 days of use, especially on sensitive skin.

Adjustment for Patient Body Weight (Serum): Not required.

Preparation Method (Serum): Ingredients per 100 ml of product: Dry Coptis chinensis extract — 1 g. Lavender hydrolate — 30 ml. Hyaluronic acid (low molecular weight) — 0.3 g. Vegetable glycerin — 3 ml. Coptis chinensis powder — 0.5 g. Purified water — up to 100 ml. The dry extract is dissolved in warm water (not above 35 °C), the powder, glycerin, and lavender hydrolate are introduced. After complete dissolution, hyaluronic acid is added and thoroughly stirred until completely homogeneous. Filtered through a sterile 0.22 μm filter.

Storage Conditions and Shelf Life (Serum): Store in the refrigerator at a temperature of +4 to +8 °C, in an airtight bottle with a pipette. After opening, use within 30 days. Total shelf life — 6 months. Avoid exposure to light and EMI.

Toxicity and Biosafety of Coptis chinensis

Experimental data on the toxicity of Coptis chinensis demonstrate its relative safety when used in therapeutic doses. The main biologically active substance associated with the toxicological profile is berberine — an isoquinoline alkaloid.

Acute oral toxicity (LD50) for berberine isolated from Coptis chinensis is: for mice: 329 mg/kg with intravenous administration, 1540 mg/kg with oral administration; for rats: 2050 mg/kg with oral administration. Toxic effects in overdose include hypotension, respiratory depression, bradycardia, and convulsions.

However, when used as part of a whole plant extract or powder of Coptis chinensis, biosafety increases due to the buffer matrix of polyphenols and tannins. Repeated administration of high doses for 28 days in preclinical studies did not cause histological changes in the liver, kidneys, or intestines in laboratory animals. To date, no serious cases of toxicity have been recorded with external use or intake within recommended doses. Clinical observations of long-term use of alcohol extract and powder of Coptis chinensis in humans have not revealed cumulative toxicity or carcinogenic potential. Berberine is metabolized in the liver and excreted primarily with bile. 

Reference: https://pubmed.ncbi.nlm.nih.go...

Pharmacodynamics — Coptis chinensis

The pharmacodynamic action of Coptis chinensis is associated primarily with a high content of isoquinoline alkaloids, among which berberine is the most studied. These substances exhibit multi-profile activity at both local and systemic levels, influencing key targets associated with inflammation, oxidative stress, bacterial colonization, metabolic regulation, and the barrier function of mucous membranes.

The anti-inflammatory action of Coptis chinensis is realized through suppression of the expression of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) and inhibition of the activity of the transcription factor NF-κB. At the molecular level, a decrease in IκBα phosphorylation and blockade of nuclear translocation of the p65 subunit have been established. This effect is observed at both systemic and local levels, including in the mucous membranes of the gastrointestinal tract and skin.

Antimicrobial and antimycotic activity is realized through destruction of microbial cell walls, inhibition of protein synthesis, as well as through effects on bacterial DNA hydrolases and topoisomerases. In vitro studies have shown that berberine disrupts the permeability of bacterial cell membranes and blocks biofilm formation. In addition, synergy with a number of traditional antimicrobial agents has been recorded.

Coptis chinensis has a modulating effect on the immune system, manifested by a decrease in hyperreactivity of the innate immune response and a moderate enhancement of adaptive links. Berberine is capable of reducing the expression of Toll-like receptors (TLR4), decreasing the sensitivity of immune cells to microbial components. Suppression of NLRP3 inflammasome expression is also noted.

Pharmacodynamics with respect to the endocrine system is realized through regulation of key enzymes of carbohydrate metabolism, including inhibition of α-glucosidase and suppression of glucose-6-phosphatase expression. Berberine modulates the expression of insulin receptors and activates AMPK-dependent signaling pathways, influencing glucose and fatty acid metabolism. These effects are realized systemically, primarily in the liver, intestines, and muscle tissue.

Antioxidant action is based on a decrease in the production of reactive oxygen species (ROS), increased expression of superoxide dismutase, glutathione peroxidase, and catalase. In cellular models, a decrease in lipid peroxidation and suppression of activation of the mitochondrial apoptosis cascade are observed.

Coptis chinensis has a moderate sedative and anxiolytic effect on the nervous system. The proposed mechanism is modulation of GABA receptor activity and a decrease in the level of excitatory neurotransmitters such as glutamate. Berberine also exhibits neuroprotective properties through suppression of inflammation in neuroglia and stabilization of neuronal membranes.

With respect to the skin, a complex action has been noted: regulation of the microbiome, suppression of local inflammation, antioxidant protection, as well as a regenerative effect through increased expression of growth factors and type I collagen. These effects are realized primarily with local application and have targets in the epidermis and dermis.

Thus, the pharmacodynamics of Coptis chinensis covers a wide range of molecular targets and physiological systems, including the gastrointestinal tract, immune, skin, endocrine, and nervous systems, while the key mechanisms of action are anti-inflammatory, antimicrobial, antioxidant, and metabolically regulating activity.

References:
https://pubmed.ncbi.nlm.nih.go...
https://www.sciencedirect.com/...
https://www.tandfonline.com/do...
https://www.ncbi.nlm.nih.gov/p...

Pharmacokinetics — Coptis chinensis

The main pharmacologically active components of Coptis chinensis are isoquinoline alkaloids, predominantly of the protoberberine type. With oral administration (in the form of powder, dry extract, or infusion), the absorption of these compounds occurs primarily in the small intestine, with the participation of passive diffusion and transport proteins. Some components demonstrate low water solubility, which limits their bioavailability when using aqueous infusions. However, when using extracts containing surface-active components, absorption increases.

Intestinal microflora plays an important role in the biotransformation of alkaloids, promoting demethylation and reduction, which influences systemic absorption and pharmacological activity. These transformations contribute to the formation of active metabolites with greater polarity and better solubility, which facilitates their entry into the blood.

After absorption, active substances partially accumulate in the liver, spleen, kidneys, and mucous membranes of the gastrointestinal tract. To a lesser extent, they are distributed in adipose tissue. Binding to plasma proteins may be moderate, while alkaloids are capable of penetrating histohematic barriers, including the blood-brain barrier, which explains the systemic effect on the nervous system.

The metabolism of active substances of Coptis chinensis is carried out primarily in the liver through redox reactions and subsequent conjugation with glucuronic acid and sulfate. Hepatic enzymes, including cytochrome P450 (especially CYP3A), play a key role in these processes. Some components may have a modulating effect on the activity of these enzymes, which may cause drug interactions.

Excretion routes include bile, urine, and to a lesser extent feces. The main volume of metabolites is excreted with bile and reabsorbed in the intestine during enterohepatic circulation, which prolongs the overall duration of action. The urinary system participates primarily in the excretion of polar metabolites, especially after hepatic transformation. Trace amounts may be excreted with sweat and through the skin.

With transdermal application (ointment, cream, serum), the absorption of active substances is limited by the surface epidermal barrier; however, they exhibit sufficient local activity due to high chemical stability and affinity for skin receptors. When applied to damaged skin, penetration increases and may have a systemic character.

With application through mucous membranes (suppositories, nasal and ear drops), absorption occurs through the capillary-rich networks of epithelial tissues, providing a rapid local and moderate systemic effect. Rectal administration allows bypassing partial first-pass metabolism through the liver, while the vaginal route provides predominantly local action with slow systemic absorption.

Thus, the pharmacokinetic profile of Coptis chinensis depends on the form of administration, the degree of processing of the raw material, and the state of the mucous membranes, while active substances are metabolized primarily in the liver and excreted with bile and urine, demonstrating a potential for cumulation with prolonged use and possible interactions with other substances metabolized by the same pathways.

References:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8364725
https://www.sciencedirect.com/science/article/pii/S0753332220301807
https://www.tandfonline.com/do...

Mechanisms of Action and Scientific Rationale — Coptis chinensis

The pharmacological activity of Coptis chinensis is realized through multiple cellular and molecular targets, which is explained by the high content of isoquinoline alkaloids, in particular berberine, as well as accompanying flavonoids, phenolic acids, and terpenoid compounds. One of the key mechanisms of action is the suppression of the inflammatory response by inhibiting the activation of nuclear factor NF-κB, which leads to a decrease in the transcription of pro-inflammatory cytokines (TNF-α, IL-1β), chemokines, and adhesion molecules. Suppression of IκBα phosphorylation and inhibition of p65 translocation into the nucleus allows stabilizing the inflammatory status at the cellular level.

At the level of signaling cascades, Coptis chinensis demonstrates modulation of PI3K/Akt, MAPK/ERK, and JAK/STAT pathways, which contributes to the normalization of cell proliferation and apoptosis, as well as a decrease in hyperreactivity of the immune system. In particular, activation of AMPK signaling and suppression of the mTOR pathway with the participation of berberine contribute to the restoration of energy and metabolic balance, including in hepatocytes and pancreatic cells.

Antimicrobial action is realized through destruction of bacterial cell membranes, disruption of DNA and RNA synthesis, as well as inhibition of the activity of bacterial enzymes, including DNA gyrase and topoisomerase IV. At the same time, alkaloids of Coptis chinensis not only suppress the growth of gram-positive and gram-negative bacteria, but also inhibit biofilm formation and increase the permeability of the cell wall. Activity against fungi of the genus Candida and certain viruses has been shown, including inhibition of virion replication through interference with viral proteases.

At the cellular level, Coptis chinensis reduces the production of reactive oxygen species (ROS) and increases the level of antioxidant enzymes: superoxide dismutase (SOD), glutathione peroxidase (GPx), and catalase. This action is complemented by stabilization of the mitochondrial membrane and suppression of the expression of pro-apoptotic proteins Bax and caspases. As a result, cytoprotection of neuronal, epithelial, and endothelial cells is ensured.

The modulating influence on the immune system is manifested in the suppression of Toll-like receptors (TLR4), a decrease in the activation of macrophages and neutrophils, a decrease in the production of nitric oxide (NO), and suppression of NLRP3 inflammasome activation. These effects contribute to the normalization of the innate immune response and prevent the development of chronic inflammation.

With respect to neuroreceptor systems, an influence on GABA-A receptors and a decrease in the level of excitatory neurotransmitters such as glutamate are assumed. Inhibition of acetylcholinesterase (AChE) activity has been shown, which may contribute to neuroprotection and improvement of cognitive processes.

An inhibitory effect on the enzyme lipoxygenase (5-LOX), which participates in the synthesis of leukotrienes, and moderate suppression of cyclooxygenase-2 (COX-2) activity have also been established, which additionally confirms the participation of Coptis chinensis in the regulation of inflammatory mediators.

Thus, the mechanisms of action of Coptis chinensis cover a complex network of interactions with cellular targets, enzyme systems, signaling pathways, and receptor structures, providing a wide spectrum of biological activity at both systemic and tissue levels.

References:
https://pubmed.ncbi.nlm.nih.gov/31329848
https://www.sciencedirect.com/science/article/pii/S0753332220301807
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8884984
https://www.tandfonline.com/do...

Synergy — Coptis chinensis

The pharmacological synergy of Coptis chinensis with other plant and biologically active substances has been confirmed by a number of experimental and clinical studies. The most pronounced potentiating effect is observed when combined with other alkaloid-containing and flavonoid taxa, as well as with substances influencing inflammatory and metabolic cascades.

The combination of Coptis chinensis with the root of Scutellaria baicalensis leads to a synergistic enhancement of anti-inflammatory activity, which is due to coordinated inhibition of the NF-κB signaling pathway and suppression of COX-2 and iNOS expression. An additive effect on the expression of antioxidant enzymes (SOD, GPx) with the combined use of extracts has also been established.

From a clinical point of view, the synergy with Phellodendron amurense is significant, due to the similar content of protoberberine alkaloids. Studies show that the simultaneous use of these components potentiates the antibacterial and immunomodulatory effects due to the summation of action on the bacterial cell wall, TLR4 receptors, and cytokine regulation.

The combination of Coptis chinensis with curcumin (polyphenol of Curcuma longa) leads to enhanced antioxidant and metabolic activity. Joint inhibition of MAPK signaling and enhanced activation of AMPK have been confirmed, which demonstrates the potential for systemic modulation of oxidative stress and energy metabolism.

When combined with salicylates or phenolic acid derivatives (e.g., extracts of Salix alba or Camellia sinensis), a modulating effect on inflammatory mediators has been noted, including a decrease in the synthesis of prostaglandins and leukotrienes. This interaction is predominantly tissue-specific in nature (mucous membranes, skin) and is expressed in local anti-inflammatory activity.

In vivo studies demonstrate that the combined use of Coptis chinensis with probiotic strains (Lactobacillus, Bifidobacterium) enhances the metabolic transformation of alkaloids in the intestine and increases the systemic absorption of active forms. This effect is classified as biotransformation-potentiating and is especially relevant for oral forms.

Additional synergy has been noted when combined with Glycyrrhiza glabra (licorice), where glycyrrhizic acid has a protective effect on mucous membranes, contributing to the prolongation of the activity of berberine compounds. This effect is due to local antisecretory and enveloping action, in combination with systemic anti-inflammatory modulation.

Thus, Coptis chinensis demonstrates a high degree of biopharmacological compatibility and potentiation when combined with a number of phytocomponents and natural substances. The main mechanisms of synergy include joint regulation of signaling pathways (NF-κB, MAPK, AMPK), inhibition of inflammatory mediators, enhancement of antioxidant activity, and improvement of absorption with the participation of intestinal microflora.

References:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8884984
https://www.sciencedirect.com/science/article/abs/pii/S1043661823001916
https://pubmed.ncbi.nlm.nih.gov/30721835
https://www.tandfonline.com/do...

Geography of Use and Traditional Medicine — Coptis chinensis

Coptis chinensis is traditionally used in the medico-botanical and ritual practices of East Asia, primarily in the territory of China, Korea, Japan, and Vietnam. It has received the greatest distribution within the framework of the Chinese medical tradition, where the plant is known under the name "黄连" (Huánglián), which means "yellow bitterness." Mentions of the use of Coptis chinensis rhizomes are recorded already in the classical work "Shennong Bencao Jing" (神农本草经), dated to the 1st–2nd century AD, where the plant was assigned to the highest category of medicines — "those that nourish the spirit and prolong life."

Over the centuries, Coptis chinensis remained the main component of complex formulations within the framework of Chinese phytotherapy, especially in the southern regions of China — the provinces of Sichuan, Hunan, Guizhou, and Yunnan. Its rhizomes were collected primarily in spring or autumn, then dried and ground for the preparation of decoctions, alcohol tinctures, or powders, which were used both independently and as part of multi-component formulas.

In Tibetan medicine, the plant is known under the name "gser gsum" and was used as part of "yellow" formulas — combinations of three bitter components, often along with the root of Berberis aristata and the fruits of Terminalia chebula. It was included in preparations manufactured according to the prescriptions of the treatise "Chzhud-shi" (胡瓜), mainly in combination with incense, resins, and animal components.

In Japanese Kampo medicine, Coptis chinensis was included in traditional formulas such as "oren-ge-ka-gairyu-to," used in the form of thick decoctions and suspensions. In the Korean tradition, the plant was used both as part of decoctions (hwangryeon tang) and as an element of ritual purification in the form of steam baths and fumigations during rites of expelling diseases.

In Vietnamese village practice, coptis rhizomes were sometimes used in the form of ground powder for sprinkling on tissues for bruises or as a component of rubbings with oil. Applications in the form of applying a paste of fresh raw material to skin areas have also been recorded, which reflects local beliefs about "drawing out heat."

In addition to medical purposes, in a number of South Chinese ethnic traditions, including the Miao and Dong peoples, Coptis chinensis was considered a plant that purifies space. In the cultures of these peoples, dried rhizomes were sometimes hung over the entrance to the house as a talisman against "evil wind" and "evil spirits." During the New Year holidays, the plant was used in fumigations of premises to expel diseases and attract health.

In some regions of Yunnan and Sichuan, coptis infusion was part of ritual water for washing newborns, with the aim of "cooling the inner fire" and protecting against "hot spirits." Such a practice is mentioned in regional oral collections of the mid-19th century.

Thus, the geography of use of Coptis chinensis covers many regions of East and Southeast Asia, where the plant is included both in formalized systems of traditional medicine and in everyday and ritual practices of various ethnic groups. Its use is accompanied by stable cultural associations with purification, protection, and balance of body and spirit.