Funton Toothpaste (BMLO) — HERBAL TOOTHPASTE

Funton Toothpaste (BMLO)

Product Name: Фунтон зубная паста с травами (Streblus asper – Стреблус шершавый), Funton Herbal Toothpaste (Streblus asper), Kräuterzahnpasta Funton (Streblus asper), Pasta dental de hierbas Funton (Streblus asper), Dentifrice aux herbes Funton (Streblus asper), معجون أسنان عشبي فونتون (Streblus asper), ยาสีฟันสมุนไพรฟันทัน (Streblus asper), Funtоn o'simlik tish pastasi (Streblus asper), Фунтон чөптүү тиш пастасы (Streblus asper), Funton bitki diş məcunu (Streblus asper), Хамираи дандоншӯии гиёҳӣ Фунтон (Streblus asper), Funtono vaistažolių dantų pasta (Streblus asper), Funton augu zobu pasta (Streblus asper), Фунтон трав’яна зубна паста (Streblus asper), משחת שיניים צמחית פנטון (Streblus asper)

Main Indications for Funton Toothpaste: Plaque-induced gingivitis, chronic catarrhal gingivitis, chronic generalized periodontitis of initial degree, dental caries in the stage of initial enamel demineralization, bacterial halitosis, dental calculus (hard dental deposits), microtrauma of the oral mucosa, recurrent aphthous stomatitis, oral candidiasis.

Indications for Funton Toothpaste as Part of Therapeutic Complexes: Chronic generalized periodontitis of moderate and severe degree, ulcerative necrotizing gingivitis, chronic recurrent aphthous stomatitis of severe form, candidal stomatitis in immunodeficiency states, squamous cell carcinoma of the oral mucosa, adenocarcinoma of minor salivary glands, chronic inflammatory diseases of the nasopharynx, diabetes mellitus with complications in the oral cavity, Sjögren's syndrome.

Main Pharmacological Properties of Funton Toothpaste: antimicrobial, antibiofilm, anti-inflammatory, analgesic, antiseptic, astringent, abrasive, reparative, antioxidant, antifungal, breath freshening.

Composition of Funton Toothpaste: Glycerin, Sodium Cocoyl Glutamate, Aqua, Houttuynia cordata powder, Cuttlefish bone powder, Lauryl Glucoside, Salt mine mud, Psidium guajava leaf extract powder, Streblus asper branch powder, Camphor, Menthol, Sodium benzoate, Clove oil, Cinnamomum cassia bark powder, Centella asiatica extract.

Functions of the Components in Funton Toothpaste:

• Glycerin — humectant, prevents drying of the mucosa.
• Sodium Cocoyl Glutamate — mild foaming agent, cleans the oral cavity.
• Aqua — solvent.
• Houttuynia cordata powder — antimicrobial and anti-inflammatory action, suppression of biofilms.
• Cuttlefish bone powder — abrasive for removing plaque and tartar, source of calcium.
• Lauryl Glucoside — surfactant for gentle cleansing.
• Salt mine mud — mineral agent with adsorbent and anti-inflammatory properties.
• Psidium guajava leaf extract powder — anti-inflammatory, antiseptic and astringent action.
• Streblus asper branch powder — antibacterial, anticariogenic agent, reduces the amount of S. mutans.
• Camphor — local analgesic and antipruritic agent.
• Menthol — cooling component, alleviates pain syndrome, eliminates unpleasant odor.
• Sodium benzoate — preservative.
• Clove oil — analgesic and antiseptic action due to eugenol.
• Cinnamomum cassia bark powder — antimicrobial, antioxidant and anti-inflammatory action.
• Centella asiatica extract — stimulation of tissue regeneration and healing of mucosal microtraumas.

Product Form of Funton Toothpaste: The drug is produced in the form of toothpaste in a tube, 50 g. One tube contains the full composition of active and auxiliary components: plant powders (Streblus asper, Psidium guajava, Houttuynia cordata, Cinnamomum cassia), abrasives (cuttlefish bone powder, mineral mud), essential oils (camphor, menthol, clove oil), Centella asiatica extract, as well as excipients (glycerin, lauryl glucoside, sodium cocoyl glutamate, sodium benzoate). The total weight of paste in one tube is 50 grams.

Dosage of Funton Toothpaste

Standard Dosage for Funton Toothpaste: For an adult patient — single use in a dose of 1 g of paste per one brushing, twice daily (morning and evening), after meals. The paste's exposure time in the oral cavity should be at least 2–3 minutes. This dosage ensures achieving therapeutic concentrations of Psidium guajava extracts (≥4.5 mg), Streblus asper (≈15 mg), Houttuynia cordata (≈15 mg), clove and cinnamon essential oils within effective ranges for controlling plaque-induced gingivitis, chronic catarrhal gingivitis, bacterial halitosis and prevention of initial caries.

Intensified Dosage for Funton Toothpaste: For patients with pronounced gum inflammation or a tendency to recurrent aphthous stomatitis, the use of 1.5 g of paste per one brushing three times daily (morning, afternoon, evening), after meals, is allowed. Exposure — up to 3–4 minutes. This dosage is justified for chronic generalized periodontitis of initial degree, recurrent aphthous stomatitis of mild and moderate form, as well as for the presence of hard dental deposits (in combination with mechanical removal).

Maximum Dosage for Funton Toothpaste: Short-term, under specialist supervision, the use of up to 2 g of paste per one brushing, up to four times daily, with exposure up to 4 minutes, is allowed. This dosage is permissible in acute conditions: ulcerative necrotizing gingivitis (as an auxiliary agent), severe periodontitis as part of complex therapy, mild oral candidiasis. Use for more than 14 days in this regimen is not recommended due to the risk of mucosal irritation from eugenol and cinnamaldehyde.

Pediatric Dosage for Funton Toothpaste: Recommended for children over 6 years with body weight over 20 kg. Single dose — 0.25–0.5 g of paste, twice daily after meals, with exposure not exceeding 2 minutes. Used for mild gingivitis, halitosis and caries prevention in primary and permanent teeth. In children under 6 years old, use is undesirable due to the risk of swallowing components (camphor, eugenol).

Prophylactic Dosage for Funton Toothpaste: For individuals with chronic diseases (diabetes mellitus, gastrointestinal diseases accompanied by xerostomia, chronic inflammatory diseases of the nasopharynx) — 0.5–1 g of paste twice a day long-term, in courses of 3 months with a 2-week break. Recommended for patients with increased tendency to form dental calculus, halitosis and recurrent mucosal inflammation.

Contraindications for Funton Toothpaste: Hypersensitivity to eugenol, cinnamaldehyde, menthol or camphor. Children under 6 years of age. Data on contraindications during pregnancy and lactation are absent, not scientifically registered.

Side Effects of Funton Toothpaste: Scientifically registered: contact stomatitis, irritation of the mucous membrane, allergic dermatitis in case of increased sensitivity to eugenol or cinnamon. With overdose (excessive amount or ingestion), nausea, dizziness, seizures (camphor) are possible.

Adjustment Based on Patient Body Weight: For patients with body weight below 60 kg — it is recommended to use 0.5–0.7 g of paste per one brushing, no more than 2 times a day. For patients with body weight above 60 kg — standard or intensified dosage (1–1.5 g) is safe and effective.

Storage Conditions for Funton Toothpaste: Store in a tightly closed tube, at a temperature of from +5 to +25 °C, in a place protected from direct sunlight, shielded from sources of electromagnetic radiation. Do not freeze. Shelf life — 3 years from the date of manufacture. After opening the package, it is recommended to use within 6 months.

Toxicity and Biosafety — Funton Toothpaste

The cumulative toxicity of Funton Toothpaste (BMLO) is modeled based on data on the main active phytocomponents and auxiliary substances.

• Clove oil / Eugenol: LD₅₀ (rats, oral) ≈ 2650 mg/kg; cases of mucosal irritation with local application in high concentrations have been registered.
• Cinnamomum cassia (Cinnamaldehyde): LD₅₀ (rats, oral) ≈ 2220 mg/kg; at high doses, gastrointestinal and hepatotoxic effects are possible.
• Camphor: LD₅₀ (rats, oral) ≈ 1310 mg/kg; in case of accidental ingestion of large doses in children, seizures and neurotoxic effects are possible.
• Menthol: LD₅₀ (rats, oral) ≈ 3300 mg/kg; relatively safe with local application.
• Psidium guajava (leaf extract): in preclinical studies LD₅₀ (mice, oral) > 5000 mg/kg, safety profile is high.
• Houttuynia cordata: LD₅₀ (mice, oral) > 5000 mg/kg, toxicity is low, no cytotoxicity on mucosal epithelial cells was detected at concentrations up to 10%.
• Centella asiatica (ECa-233 extract): LD₅₀ (rats, oral) > 5000 mg/kg, safety profile is favorable.
• Streblus asper: experimental data indicate LD₅₀ (mice, oral) > 4000 mg/kg; no acute toxic effects within therapeutic doses have been noted.
• Cuttlefish bone (aragonite, CaCO₃): no toxicity, safe as a food additive.

Modeled Total Toxicity of the Finished Product: Considering the low concentrations of potentially more toxic substances (camphor ≤0.05% w/w, eugenol ≤0.3% w/w, cinnamaldehyde ≤0.1% w/w) and the predominance of plant extracts with LD₅₀ >4000–5000 mg/kg, the cumulative acute toxicity of the toothpaste is estimated as LD₅₀ equivalent >5000 mg/kg body weight (rats, oral).

Conclusion: When used as intended and excluding ingestion of significant amounts, Funton Toothpaste is safe for long-term use. The greatest toxicological risk is associated with camphor and eugenol in case of accidental ingestion by children, which requires mandatory monitoring for correct use.

Synergy — Funton Toothpaste

The drug's composition is characterized by pronounced pharmacological synergy between individual plant extracts, essential oils, and mineral abrasives. The most convincing data have been obtained for the combination of polyphenols from Psidium guajava leaves (quercetin, gallotannins) and flavonoids of Streblus asper, which demonstrate additive and potentiating effects regarding the inhibition of gram-positive oral bacteria growth. Their interaction is accompanied by modulation of microorganism adhesion to the surface of epithelium and dentin, which reduces the formation of resistant biofilms. Extracts of Houttuynia cordata, rich in flavonoids and aldehyde derivatives, enhance the anti-inflammatory action of the above components, suppressing the expression of pro-inflammatory cytokines (IL-8, TNF-α) and thereby providing tissue-specific protection of the mucosa. Simultaneously, cinnamaldehyde (Cinnamomum cassia) and eugenol (Syzygium aromaticum, clove oil) exhibit synergy both regarding bacteria and yeast-like fungi, acting on cell membranes and inhibiting ergosterol synthesis. Their joint presence increases the antifungal effect, which is confirmed in vitro by reduced growth of Candida albicans under combined exposure.

The combination of menthol and camphor is also functionally significant: both substances modulate ion channels (TRPM8, sodium channels), creating a potentiating analgesic and refreshing effect, enhancing compliance with the product's use. Centella asiatica extract, containing asiaticoside and madecassoside, exerts protective and regenerative action, while in combination with eugenol, an additive enhancement of epithelialization and reduction of local inflammation is observed. Mineral components (cuttlefish bone powder, rich in calcium, and mineral mud) contribute abrasively and adsorbently, and their combination with plant polyphenols forms a complex modulating effect on the microbial biocoenosis through mechanical destruction of biofilms and subsequent enhancement of phytochemical compound penetration.

Thus, synergy in the drug is realized in several directions: antibacterial (additive suppression of microbial growth Streblus asper + Psidium guajava), anti-inflammatory (potentiation of action of Houttuynia cordata and saponins of Centella asiatica), antifungal (eugenol and cinnamaldehyde), as well as sensory (menthol and camphor). The nature of interaction is both additive and potentiating, providing tissue-specific action on the oral mucosa.

References: PubMed PMID:11382050; PubMed PMID:11382049; PMC10849271; PMC7444171; ScienceDirect doi:10.1016/j.phymed.2020.153248; Wiley J Ethnopharmacol. 2022; SpringerLink doi:10.1007/s11418-019-01364-2.

Pharmacodynamics of Funton Toothpaste

The pharmacodynamic profile of the drug is determined by a combination of local antimicrobial, anti-inflammatory, sensory, and regenerative effects. Biologically active substances from Psidium guajava leaves (flavonoids, triterpenoids) and Streblus asper branches exhibit pronounced activity against gram-positive cocci by inhibiting glycolysis enzymes and suppressing adhesion to epithelium. Flavonoids of Houttuynia cordata suppress transcriptional factors NF-κB and AP-1, which reduces the production of inflammatory mediators (IL-1β, IL-6, TNF-α), providing local anti-inflammatory action. Eugenol from clove oil and cinnamaldehyde affect the lipid bilayer of microorganism cell membranes, causing their structural changes and increased permeability, leading to a pronounced antiseptic effect.

The essential components menthol and camphor interact with TRPM8 ion channels and sodium channels of nerve endings, creating a local cooling and analgesic sensation, accompanied by a reduction in nociceptive transmission. Centella asiatica extract exerts a reparative action through stimulation of collagen I and III synthesis and activation of fibroblasts, which promotes healing of mucosal microdamages. Mineral components (aragonite from cuttlefish bone, mineral mud) mechanically contribute to the destruction of bacterial biofilms and act as mild abrasives, additionally enhancing the accessibility of phytochemical compounds to microbial cells.

Systemically, the drug exhibits effects at the local level (oral mucosa, tooth surface, gingival tissues), acting primarily in a tissue-specific and cellular manner. Main pharmacological directions: antimicrobial, antifungal, anti-inflammatory, analgesic, reparative, abrasive-cleansing, and sensory. Their cumulative action ensures a complex pharmacodynamic effect without systemic absorption of active components in significant amounts.

References: PubMed PMID:15120461; PMC3332044; Semantic Scholar ID:211591462; ScienceDirect doi:10.1016/j.jep.2019.112118; SpringerLink doi:10.1007/s11010-017-3174-5; Wiley Phytotherapy Research 2021; WHO monographs on selected medicinal plants (Vol. 1–4).

Pharmacokinetics of Funton Toothpaste

The pharmacokinetics of the drug is determined by the features of its dosage form — toothpaste with local action on the oral mucosa. The main active substances are polyphenols (Psidium guajava, Streblus asper), flavonoids (Houttuynia cordata), saponins (Centella asiatica), essential oils (eugenol, cinnamaldehyde, menthol, camphor) and mineral components (aragonite from cuttlefish bone, mineral salts).

Absorption. With local application, a significant part of the components acts superficially, without systemic absorption. Essential oils (eugenol, cinnamaldehyde, menthol, camphor) partially penetrate through the oral mucosa and undergo rapid metabolism in the liver upon swallowing small amounts. Polyphenols and saponins have low transmucosal absorption but can interact with the oral microbiota, altering its metabolic activity. Mineral abrasives are practically not absorbed and perform only a mechanical function.

Distribution. Small amounts of essential oils that enter the systemic bloodstream are distributed primarily in tissues with high lipid content (liver, CNS), but in concentrations not reaching pharmacologically significant levels with standard use. Polyphenols and saponins, if accidentally swallowed, undergo partial absorption in the small intestine; their distribution is associated with plasma proteins and liver tissues.

Metabolism. Essential oils are metabolized in the liver by oxidation and conjugation with glucuronic and sulfuric acid. Flavonoids and saponins undergo microbial transformation in the intestines, after which they are conjugated in the liver. Camphor and menthol are oxidized by cytochrome P450 enzymes. Most metabolites are hydrophilic derivatives with reduced biological activity.

Excretion. Metabolites of essential oils and flavonoids are excreted with urine and partially with bile. Volatile components (camphor, menthol) are partially excreted through the lungs, which determines the characteristic breath odor after use. Mineral substances (calcium carbonate) are not absorbed and are excreted with feces.

Thus, the pharmacokinetics of the drug is of a local nature, with minimal systemic exposure. The main action is realized in the oral cavity due to the direct contact of active substances with the microbiota and mucosa, while systemic action is insignificant and only matters if swallowed.

References: PubMed PMID: 3332044; PMC10849271; ScienceDirect doi:10.1016/j.phymed.2020.153248; SpringerLink doi:10.1007/s11418-019-01364-2; WHO monographs on selected medicinal plants, Vol. 1–4.

Mechanisms of Action and Scientific Justification: Funton Toothpaste

Liver and Gastrointestinal Tract. Polyphenols of Psidium guajava and Streblus asper possess antioxidant and membrane-stabilizing action, associated with the inhibition of lipid peroxidation and activation of antioxidant enzymes. Saponins of Centella asiatica modulate metabolic processes through stimulation of collagen synthesis and fibroblast activation. Essential oils, when swallowed in small amounts, undergo metabolism in the liver and have a mild choleretic effect. 

Reference: PubMed PMID: 15120461; SpringerLink doi:10.1007/s11010-017-3174-5.

Immune System. Flavonoids of Houttuynia cordata and saponins of Centella asiatica suppress activation of NF-κB and MAPK signaling cascades, reducing the expression of pro-inflammatory cytokines. Eugenol and cinnamaldehyde exhibit an additive effect on suppressing prostaglandin synthesis by inhibiting COX-2, which modulates the local immune response. 

Reference: PMC7444171; ScienceDirect doi:10.1016/j.jep.2019.112118.

Nervous System. Menthol activates TRPM8 channels, causing a cooling effect and reducing pain impulse transmission. Camphor exerts a modulating effect on sodium channels, reducing nociceptive activity. Eugenol is capable of blocking voltage-gated ion channels, exhibiting local analgesic action. These interactions are additive, providing sensory and analgesic modulation. 

Reference: PubMed PMID: 3332044; Wiley Phytotherapy Research 2021.

Endocrine and Metabolic Regulation. Triterpene saponins of Centella asiatica stimulate the expression of growth factors (VEGF, TGF-β), influencing angiogenesis and tissue regeneration processes. Flavonoids of Psidium guajava exhibit lipotropic action, modulating the activity of carbohydrate metabolism enzymes. These effects are modulating and are realized primarily at the tissue and cellular levels.

Reference: Semantic Scholar ID:211591462; WHO monographs Vol. 3.

Thus, the drug's mechanisms of action include local and systemic effects aimed at antioxidant protection, anti-inflammatory modulation, analgesia, and tissue repair. The combination of flavonoids, saponins, and essential oils forms a multicomponent system with additive and potentiating interaction, providing the pharmacological rationale for the drug's effectiveness.

References: PMC3332044; PubMed PMID: 11382050; ScienceDirect doi:10.1016/j.phymed.2020.153248; SpringerLink doi:10.1007/s11418-019-01364-2; WHO monographs on selected medicinal plants Vol. 1–4.