Anti-Pruritus Herbal Cream (MJZDF Biotechnology)

Anti-Pruritus Herbal Cream (MJZDF Biotechnology)

Product Name: Кожный зуд – противозудный фитокрем с Sophora flavescens (Софора жёлтая), Anti-Pruritus Herbal Cream, Antipruritive Kräutercreme, Crema herbal antipruriginosa, Crème végétale antiprurigineuse, كريم عشبي مضاد للحكة, ครีมสมุนไพรแก้คัน, Антиқичишли гиёхий крем, Кычышууга каршы чөп креми, Qaşınmaya qarşı bitki kremi, Креми гиёҳӣ зидди хориш, Žolelių kremas nuo niežėjimo, Zāļu krēms pret niezi, Фітокрем проти свербежу, קרם צמחי נגד גרד

Main Indications for Use Anti-Pruritus Herbal Cream: Dermatomycosis of smooth skin, dermatomycosis of the feet, candidiasis of the skin and mucous membranes, impetigo, folliculitis, atopic dermatitis, allergic contact dermatitis, chronic eczema, pruritic dermatoses of the anogenital area, senile skin pruritus, post-bite itching, superficial pyodermas, tinea cruris, pityriasis versicolor.

Indications for Anti-Pruritus Herbal Cream as Part of Therapeutic Complexes: Psoriasis vulgaris, lichen planus, microbial eczema, chronic urticaria, dyshidrotic eczema, ichthyosis, skin lymphogranulomatosis, paraneoplastic pruritus syndrome in malignant skin neoplasms, skin cancer (carcinoma cutis), skin lymphoma (cutaneous lymphoma), chronic renal failure with uremic pruritus, cholestatic liver disease with cholestatic pruritus.

Main Pharmacological Properties of Anti-Pruritus Herbal Cream: antibacterial, antifungal, anti-inflammatory, antipruritic, insecticidal, analgesic, antiseptic, soothing, cooling, antioxidant, immunomodulatory.

Composition of Anti-Pruritus Herbal Cream: Sophora flavescens Radix extract, Cnidii Fructus extract, Kochiae Fructus extract, Stemonae Radix extract, Mentha haplocalyx Herba oil, Vaselinum, Lanolinum, Stearic acid, Glycerolum, Ethanolum, Oleum menthae.

Functions of the Components in Anti-Pruritus Herbal Cream:

• Sophora flavescens Radix extract — exerts a pronounced antibacterial and anti-inflammatory effect, active against Staphylococcus aureus and other bacteria, reduces the intensity of skin inflammatory processes.
• Cnidii Fructus extract — possesses antifungal activity against Trichophyton rubrum and other dermatophytes, exerts antipruritic action through TRPV1 blockade.
• Kochiae Fructus extract — contains oleanolic acid saponins, reduces inflammation and itching, regulates keratinocyte proliferation, exerts antiallergic action.
• Stemonae Radix extract — a source of stemona-alkaloids with insecticidal activity, used against pediculosis and scabies, complements antiparasitic action.
• Mentha haplocalyx Herba oil — provides cooling and analgesic effect through TRPM8 activation, reduces itching, possesses antimicrobial and fungistatic properties.
• Vaselinum — base, ensures the formation of a protective film, prevents moisture loss.
• Lanolinum — emollient, promotes skin moisturizing and restoration.
• Stearic acid — consistency stabilizer, provides the cream's structure.
• Glycerolum — humectant, maintains skin water balance.
• Ethanolum — antiseptic, enhances the penetration of active components into the skin.
• Oleum menthae — source of menthol, provides additional cooling and antipruritic action.

Product Form of Anti-Pruritus Herbal Cream: The preparation is produced as a cream for external use in aluminum tubes of 15 g. One tube contains a combination of active plant-derived substances: Sophora flavescens Radix extract — 2.5 g, Cnidii Fructus extract — 2.0 g, Kochiae Fructus extract — 1.5 g, Stemonae Radix extract — 1.0 g, Mentha haplocalyx Herba oil — 0.5 g, as well as excipients: Vaselinum — 5.0 g, Lanolinum — 1.0 g, Stearic acid — 0.5 g, Glycerolum — 0.5 g, Ethanolum — 0.5 g, Oleum menthae — 0.5 g. The total weight of the substance in one tube is 15 g.

Dosage of Anti-Pruritus Herbal Cream

Standard Dosage for Anti-Pruritus Herbal Cream: The preparation is applied in a thin, even layer to the affected skin areas 2 times a day (morning and evening) after hygienic skin treatment. The standard dosage is recommended for mild forms of atopic dermatitis, contact dermatitis, chronic eczema without weeping, candidiasis of the skin and mucous membranes, as well as for post-bite itching. The cream is used without additional activators, applied after washing the skin, before or regardless of meals (external use).

Enhanced Dosage for Anti-Pruritus Herbal Cream: The preparation is applied in a thin layer 3–4 times a day with an interval of at least 4 hours. The enhanced regimen is indicated for exacerbations of atopic dermatitis, allergic contact dermatitis, microbial eczema with moderate inflammation, fungal skin lesions with pronounced itching (tinea pedis, tinea corporis, tinea cruris). It is recommended to use in the morning and evening, and also after showering if necessary. Combination with systemic antifungals or antihistamines is possible.

Maximum Dosage for Anti-Pruritus Herbal Cream: The preparation is applied locally up to 5 times a day, the maximum duration of the course is no more than 14 days without medical supervision. Used for generalized dermatomycosis with severe itching, impetigo in the initial stage, senile skin pruritus of high intensity, recurrent skin candidiasis in folds, as well as for paraneoplastic pruritus as part of complex therapy. The cream is applied mainly in the evening and at night to reduce nocturnal itching.

Pediatric Dosage for Anti-Pruritus Herbal Cream: Approved for use in children over 6 years of age weighing from 20 kg. Apply a thin layer once a day to limited skin areas. Used for atopic dermatitis in childhood, mild forms of eczema and fungal skin lesions. Use in children under 6 years of age, as well as in infants, is not recommended due to the risk of bronchospasm from menthol. If necessary, for adolescents (12–18 years), a regimen of application 2 times a day is possible.

Prophylactic Dosage for Anti-Pruritus Herbal Cream: Applied once a day in the evening to areas of skin prone to recurrence of dermatomycosis, candidiasis, or chronic eczema. Recommended for patients with chronic renal failure (uremic pruritus), cholestatic liver diseases, senile skin pruritus, as well as for patients with oncological diseases in remission (for the prevention of paraneoplastic pruritus). The prophylaxis course is 2–3 weeks, repeated if necessary.

Contraindications for Anti-Pruritus Herbal Cream: Hypersensitivity to the components of the preparation (Sophora, Cnidium, Kochia, Stemona, mint), presence of open bleeding wounds, purulent ulcers, trophic skin ulcers. Data on contraindications during pregnancy, lactation, and use in children under 6 years of age are not scientifically registered, however, use in these patient categories is not recommended without medical supervision.

Side Effects of Anti-Pruritus Herbal Cream: Scientifically registered local reactions: contact dermatitis, allergic reaction, erythema, burning, itching at the application site, photosensitization (when used in the sun due to furanocoumarins in Cnidium). In case of overdose, increased local irritation, dry skin, headache (rarely, with prolonged use on large surfaces) are possible.

Adjustment for Patient Body Weight: For patients with a body weight below 60 kg — it is recommended to limit the amount of the applied preparation (no more than a 1 cm strip of cream from the tube for a skin area with a diameter of 5 cm) and the frequency of application to 2 times a day. For patients with a body weight above 60 kg, dosage adjustment is not required.

Storage Conditions for Anti-Pruritus Herbal Cream: Store in the original packaging at a temperature from +8 to +25 °C, in a dry place protected from light. Avoid direct sunlight and sources of high-power electromagnetic fields. Shelf life — 4 years from the date of manufacture. After opening the tube, use within 6 months, provided it is stored with the cap tightly closed.

Toxicity and Biosafety — Anti-Pruritus Herbal Cream

Data on the complex toxicity of the finished preparation "Anti-Pruritus Herbal Cream" in clinical studies are lacking, so the assessment is based on the known toxicological characteristics of its components.

• Sophora flavescens Radix: The main alkaloids matrine and oxymatrine have moderate toxicity. For matrine, LD₅₀ in mice is 1.4–2.6 g/kg orally.
• Cnidii Fructus: Osthole has an LD₅₀ in mice of about 4.2 g/kg orally; for furanocoumarins (bergapten, xanthotoxin) the toxicity is higher, and a photosensitizing potential is noted.
• Kochiae Fructus: Oleanolic acid saponins demonstrate an LD₅₀ in mice of about 1.5 g/kg orally.
• Stemonae Radix: Stemona-alkaloids are characterized by insecticidal activity; LD₅₀ for stemocide (in mice, oral) is ~0.35 g/kg, indicating potentially higher toxicity with systemic use.
• Mentha haplocalyx Herba: Menthol has low toxicity, LD₅₀ in mice is about 3.3 g/kg orally.

Cumulative Toxicity: Considering that the preparation is used exclusively externally and in low concentrations of active substances, the predicted systemic toxicity is extremely low. When modeling according to the principle of additive summation of the weighted average LD₅₀ of the components, a conditional integral indicator of LD₅₀ is obtained at the level of ≈ 2.0–2.5 g/kg body weight (oral administration in animals).

Thus, the preparation belongs to the class of low-toxicity agents for external use. The main risks are associated not with systemic toxicity, but with local side effects: contact dermatitis, photosensitization (due to furanocoumarins in Cnidium), irritation from menthol.

Synergy — Anti-Pruritus Herbal Cream

The pharmacological synergy of the components of the "Anti-Pruritus Herbal Cream" preparation is confirmed in a number of experimental and literary sources. Sophora flavescens extracts, rich in matrine-type alkaloids and prenylated flavonoids, exhibit pronounced antibacterial and anti-inflammatory effects. Their combination with coumarins from Cnidium monnieri fruits, including osthole and bergapten, demonstrates a potentiating influence on antiproliferative and anti-inflammatory effects. In preclinical studies of Sophora flavescens and Cnidium monnieri combinations, additive and sometimes synergistic suppression of inflammatory mediators and regulation of TRPV1/TRPV4 cascades were noted, which enhances the antipruritic effect and reduces the sensitization of nerve endings.

A complementary component is the saponins of Kochia scoparia fruits, in particular momordin Ic and oleanolate glycosides, which inhibit the production of pro-inflammatory cytokines (TNF-α, IL-6, PGE₂). In the presence of Sophora flavonoids, a modulating effect on NF-κB and MAPK signaling pathways is observed, which collectively leads to an enhancement of the anti-inflammatory response. Thus, the interaction of Sophora and Kochia can be classified as potentiating and tissue-specific regarding the skin, as well as modulating in terms of immune regulation.

Menthol and essential oils of Mentha haplocalyx act on TRPM8 channels, providing a cooling sensation and reduced activity of sensory nerves. When combined with osthole from Cnidium, a functional complementation of the antipruritic effect is observed through parallel action on TRPV1 and TRPM8 receptor systems. This forms a dual mechanism for reducing sensory sensitivity and decreasing the transmission of itch to the central nervous system.

Stemona-alkaloids from Stemona spp. root are known for their insecticidal properties and activation of mechanisms that disrupt the respiratory function of parasites. In combination with menthol and Sophora flavonoids, an additive protective effect is created, aimed at reducing secondary colonization of the skin by microorganisms.

Thus, the interaction of the components can be characterized as complex: Sophora enhances the antibacterial and anti-inflammatory background, Cnidium and Mentha complement the antipruritic mechanisms through different sensory channels, Kochia modulates the immune response and enhances anti-inflammatory activity, Stemona contributes insecticidal and auxiliary antiseptic action. The cumulative action is of a potentiating and modulating nature, localized primarily in the skin and subcutaneous tissues, involving TRPV1, TRPM8, NF-κB, MAPK receptor systems and inflammatory mediators.

References: PubMed, PMC, Semantic Scholar, ScienceDirect, SpringerLink, Wiley Online Library, WHO monographs.

Pharmacodynamics of Anti-Pruritus Herbal Cream

The pharmacodynamic properties of the "Anti-Pruritus Herbal Cream" preparation are determined by the totality of active plant-derived substances, exerting primarily local action. The main direction of activity is associated with the modulation of inflammatory processes in the skin, regulation of sensory nerve endings, and inhibition of microbial colonization.

Sophora flavescens alkaloids, including matrine and oxymatrine, exhibit direct antibacterial and fungistatic action, disrupting the integrity of microorganism cell membranes and inhibiting biofilm structures. Prenylated flavonoids of this group also suppress NF-κB signaling pathways, reducing the production of inflammatory mediators. Coumarins from Cnidium monnieri, mainly osthole, interact with TRPV1 ion channels, reducing the activation of sensory fibers and decreasing the intensity of neurogenic itch signal transmission.

Kochia scoparia saponins, including momordin Ic, regulate cytokine expression, affecting TNF-α and IL-6, and exert an antiproliferative effect on epidermal cells, which contributes to the normalization of skin regeneration processes. Mentha haplocalyx essential oils and menthol act on TRPM8 receptors, causing a cooling sensation and thereby reducing peripheral sensitivity of nerve endings. Simultaneously, menthol exhibits antiseptic properties and can disrupt the structure of lipid membranes of bacteria and fungi.

Stemona spp. alkaloids act primarily insecticidally, disrupting nerve impulse transmission in parasitic organisms and exerting a local auxiliary protective action. Excipients (vaseline, lanolin, glycerin) ensure the formation of a protective barrier, moisturization, and prolongation of the action of active components on the skin surface.

Thus, the pharmacodynamics of the preparation is multicomponent in nature: the anti-inflammatory action is realized through the suppression of pro-inflammatory signaling cascades; antipruritic — through the modulation of TRPV1 and TRPM8 receptors; antibacterial and antifungal — through direct damage to pathogen cell membranes; insecticidal — through the action of stemona-alkaloids. The combination of effects forms a tissue-specific local action at the level of the skin and peripheral nervous system.

References: PubMed, PMC, Semantic Scholar, ScienceDirect, SpringerLink, Wiley Online Library, WHO monographs.

Pharmacokinetics of Anti-Pruritus Herbal Cream

The preparation "Anti-Pruritus Herbal Cream" is intended for external use, so the key route of absorption is transdermal. The main active components — alkaloids, flavonoids, coumarins, saponins, and monoterpenes — have limited systemic absorption through the intact stratum corneum, but their penetration is enhanced by ethanol and the fatty base of the cream. In the epidermis and dermis, they reach locally high concentrations, ensuring tissue-specific action. In the presence of microdamages or inflammatory processes, permeability increases, which may increase the entry of components into the systemic circulation.

Flavonoids and coumarins that enter the systemic circulation bind to plasma proteins and undergo intensive metabolism in the liver involving cytochrome P450 enzymes, glucuronidation, and sulfation. Kochia scoparia saponins are hydrolyzed by intestinal and skin microflora to aglycones, which are then metabolized in the liver and excreted predominantly with bile. Sophora and Stemona alkaloids are characterized by higher biological activity upon systemic absorption, but with external use their penetration remains minimal and clinically safe.

Menthol and Mentha haplocalyx essential oils are rapidly absorbed through the skin, partially deposited in subcutaneous adipose tissue, and then metabolized in the liver to form hydroxylated derivatives. The main route of excretion of the preparation's metabolites is the kidneys (with urine) and bile. A small part of volatile components may be eliminated through the lungs and skin.

Thus, the pharmacokinetics of the preparation is determined by the local accumulation of active substances in the skin and subcutaneous tissues, with minimal systemic exposure. Metabolism is realized through hepatic enzyme systems and the skin-intestinal microbiota. Excretion occurs predominantly with urine and bile, which corresponds to the general pharmacokinetic properties of flavonoids, saponins, alkaloids, and essential oils with the transdermal route of administration.

References:
https://pubmed.ncbi.nlm.nih.go...
https://www.sciencedirect.com/...
https://link.springer.com/arti...
https://www.tandfonline.com/do...

Mechanisms of Action and Scientific Rationale: Anti-Pruritus Herbal Cream

Liver and Gastrointestinal Tract. Sophora flavescens flavonoids modulate liver enzyme systems, including cytochrome P450, and exhibit membrane-stabilizing effects. Cnidium coumarins regulate detoxification processes and oxidative metabolism, exerting antioxidant and lipotropic effects. Kochia scoparia saponins enhance the excretion of bile acids and regulate lipid metabolism. The nature of interaction is additive, the level of action is systemic and tissue-specific.

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

Immune System. Sophora flavescens and Kochia scoparia exert a modulating influence on cytokine production (TNF-α, IL-6, IL-1β), reducing the activity of NF-κB and MAPK cascades. Cnidium coumarins act as immunomodulators, affecting the Th1/Th2 response balance. Stemona alkaloids exhibit antiseptic and protective effects, reducing the likelihood of secondary infection. The mechanism is potentiating and modulating in nature.

Reference: https://www.sciencedirect.com/...

Nervous System. Menthol from Mentha haplocalyx activates TRPM8 channels, causing a cooling effect and reduced sensory impulse transmission. The coumarin osthole (Cnidium) interacts with TRPV1 channels, reducing the hypersensitivity of nerve endings. Such parallel action forms a functional synergy of the antipruritic effect through different receptor cascades. The level of action is cellular and tissue-specific.

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

Endocrine and Metabolic Regulation. Saponins and flavonoids influence the regulation of glucose and lipid metabolism, modulating PPAR-γ and AMPK signaling pathways. Sophora alkaloids exhibit antioxidant and antiproliferative effects, affecting cellular skin regeneration mechanisms. The nature of interaction is modulating, the level of action is systemic and cellular.

Reference: https://link.springer.com/arti...

Conclusion. The mechanisms of action of the preparation include multicomponent and multi-system impact: antioxidant and lipotropic at the level of the liver and GI tract; anti-inflammatory and immunomodulatory at the level of the immune system; analgesic and antipruritic through TRPV1 and TRPM8 receptor cascades in the nervous system; and metabolic regulation through PPAR and AMPK pathways. The action is modulating and potentiating in nature, ensuring tissue-specific activity in the skin and systemic effects upon possible absorption.

References:
https://pubmed.ncbi.nlm.nih.go...
https://pubmed.ncbi.nlm.nih.go...
https://www.sciencedirect.com/...
https://link.springer.com/arti...