Jingdu Ear Drops (XRP)

Jingdu Ear Drops (XRP)

Product Name: Ушные капли Цзинду — Jingdu Ear Drops, Ohrentropfen Jingdu, Gotas óticas Jingdu, Gouttes auriculaires Jingdu, قطرات الأذن جينغدو, หยอดหูจิงตู, Джингду қулоқ томчилари, Джингду кулак тамчылары, Jingdu qulaq damcıları, Қатраҳои гӯши Ҷингду, Jingdu ausų lašai, Jingdu ausu pilieni, Краплі для вух Джінду, ג'ינגדו טיפות אוזניים

Main Indications for Jingdu Ear Drops: Diffuse bacterial external otitis, eczematous external otitis, candidal external otitis, aspergillosis external otitis, furuncle of the external auditory canal, dermatitis of the skin of the external auditory canal.

Indications for Jingdu Ear Drops as Part of Therapeutic Complexes: Chronic suppurative otitis media, chronic fungal otitis media, sensorineural hearing loss, chronic infectious-inflammatory eustachitis, chronic bacterial rhinosinusitis, malignant neoplasms of the external ear, malignant neoplasms of the middle ear, benign neoplasms of the auditory canal.

Main Pharmacological Properties of Jingdu Ear Drops: antiseptic, antimicrobial, antifungal, anti-inflammatory, antipruritic, analgesic, antioxidant, immunomodulatory, wound healing, anti-edematous.

Composition of Jingdu Ear Drops: Chlorhexidine acetate, Erionota torus larva extract, Saussurea costus root, Magnetite, Dendrobium nobile stem, Vitex trifolia fruit, Cyathula officinalis root, Borneol.

Functions of the Components in Jingdu Ear Drops:

• Chlorhexidine acetate — broad-spectrum antiseptic, inhibits the growth of bacteria, fungi, and biofilms.
• Erionota torus larva extract — animal medicinal raw material, has pronounced antifungal and anti-inflammatory effects, traditionally used for purulent ear diseases.
• Saussurea costus root — source of sesquiterpene lactones, has antimicrobial, anti-inflammatory, and antimycotic effects.
• Magnetite — mineral component, traditionally used in Chinese medicine for tinnitus and hearing loss.
• Dendrobium nobile stem — source of phenanthrenes, has antioxidant and anti-inflammatory effects.
• Vitex trifolia fruit — contains flavonoids, has anti-inflammatory, analgesic, and antiallergic effects.
• Cyathula officinalis root — contains saponins and phytosteroids, improves microcirculation, reduces inflammation and tissue swelling.
• Borneol — topical irritant and antipruritic agent, increases tissue permeability and enhances the action of other components.

Product Form of Jingdu Ear Drops: The drug is supplied in a dropper bottle of 15 ml. Per 1 ml: chlorhexidine acetate 0.05–0.10%, Erionota torus larva extract 10 mg, Saussurea costus root extract 8 mg, magnetite powder 5 mg, Dendrobium nobile stem extract 6 mg, Vitex trifolia fruit extract 5 mg, Cyathula officinalis root extract 5 mg, borneol 1 mg. The total mass of active substances in one bottle is about 600 mg; the remaining volume consists of purified water and excipients.

Dosage of Jingdu Ear Drops

Standard Dosage for Jingdu Ear Drops: 2–3 drops into the external auditory canal 2 times a day, morning and evening, for acute diffuse bacterial external otitis, eczematous external otitis, mild forms of candidal external otitis. Use only with an intact eardrum. Not dependent on food intake.

Intensified Dosage for Jingdu Ear Drops: 3–4 drops 3 times a day, morning, afternoon, and evening, for severe inflammatory forms of external otitis with pronounced edema, for fungal infection of the external ear (Candida albicans), for furuncle of the external auditory canal. The intensified regimen can be combined with systemic antimicrobial or antifungal agents.

Maximum Dosage for Jingdu Ear Drops: 5 drops 3–4 times a day, short-term (no more than 5–7 consecutive days), for pronounced purulent external otitis, for recurrent otomycosis, for secondary bacterial-fungal mixed infections of the skin of the auditory canal. Mandatory with an intact eardrum.

Pediatric Dosage for Jingdu Ear Drops: From 6 years old, with body weight from 20 kg. 1–2 drops 2 times a day, only for mild forms of external otitis (without purulent process). For children under 6 years old, there is no reliable clinical safety data. Use is the same for boys and girls.

Prophylactic Dosage for Jingdu Ear Drops: 2 drops once a day for 5–7 days, for chronic external otitis with itching, in patients with recurrent otomycosis, in individuals with eczema of the auditory canal. Prophylactic courses are repeated no more than once a month.

Contraindications for Jingdu Ear Drops: Perforation of the eardrum, presence of a drainage tube, allergy to chlorhexidine, camphor, or sesquiterpene lactones from costus, pronounced dermatitis of the auditory canal with exudation, children under 6 years of age. There is no scientific data on safety during pregnancy and lactation, therefore use during these periods is not recommended.

Side Effects of Jingdu Ear Drops: Irritation of the skin of the auditory canal, contact dermatitis, itching, burning, peeling. With overdose — risk of ototoxic action of chlorhexidine, especially with a hidden perforation of the eardrum.

Adjustment Based on Patient Body Weight: For body weight below 60 kg — use the standard dosage (2–3 drops 2 times a day). For body weight above 60 kg — it is permissible to increase the dosage to 3–4 drops 2–3 times a day depending on the clinical picture.

Storage Conditions for Jingdu Ear Drops: Store in the bottle at a temperature from +10 to +25 °C, in a dry place, protected from direct light and sources of electromagnetic radiation. Shelf life of an unopened bottle — 3 years. After opening, use within 30 days.

Toxicity and Biosafety — Jingdu Ear Drops

No data on comprehensive toxicological evaluation of Jingdu Ear Drops in clinical practice have been published. Biosafety can be assessed based on the toxicity of individual components included in the drug.

• Chlorhexidine acetate: acute toxicity (LD₅₀, rats, oral) is 1.8 g/kg body weight. With topical application, low systemic absorption is noted, but there is a risk of ototoxicity if it enters the inner ear.
• Borneol (camphor/borneol): LD₅₀ in rats (oral) — 1.6 g/kg body weight; with topical application, absorption is limited, but neurotoxic effects are possible in case of overdose.
• Saussurea costus root: data on LD₅₀ in animals are limited; sesquiterpene lactones are considered low-toxic with topical application but can cause contact dermatitis.
• Dendrobium nobile: phenanthrene alkaloids have low acute toxicity; LD₅₀ not less than 10 g/kg (rats, oral).
• Vitex trifolia fruit: extracts show LD₅₀ greater than 5 g/kg (mice, oral).
• Cyathula officinalis root: saponins exhibit low acute toxicity; LD₅₀ about 3.5 g/kg (mice, oral).
• Erionota torus larva extract: no toxicological data; by analogy with other protein-based insects, acute toxicity is low (presumably above 5 g/kg in mice, oral).
• Magnetite: bioinert mineral, has no systemic toxicity with topical application.

Simulated Cumulative Toxicity of the Drug: Considering that the drug is applied only topically and the concentrations of active substances do not exceed milligram values per dose, the total acute toxicity is significantly below therapeutic dosages. The presumed range of LD₅₀ of the mixture based on extrapolated data is at least 2.0–2.5 g/kg body weight (rats, oral).

Conclusion: with external use, Jingdu Ear Drops have low systemic toxicity and satisfactory biosafety. The main risks are associated with the local irritating activity of chlorhexidine and camphor, as well as with the ototoxicity of chlorhexidine in case of eardrum damage.

Synergy — Jingdu Ear Drops

The pharmacological activity of the drug's components is formed due to pronounced synergy between plant, animal, mineral, and synthetic substances. The cumulative effect is based on multi-vector impact on inflammatory, microbial, and oxidative processes in the tissues of the external ear. The antimicrobial component chlorhexidine acetate demonstrates broad activity against bacteria and fungi; however, its effectiveness is limited by the presence of biofilms. With the addition of borneol (camphor), potentiation of the antiseptic action is observed due to increased permeability of epithelial barriers and facilitated penetration of chlorhexidine into the infection site. This type of interaction is potentiating and modulating.

Plant components — Saussurea costus, Vitex trifolia, Cyathula officinalis, and Dendrobium nobile — have pronounced anti-inflammatory and antioxidant potential. In combination with chlorhexidine and borneol, their action becomes additive: inhibition of inflammatory mediators (e.g., NF-κB and TNF-α) is combined with a direct antiseptic effect. Saussurea costus, due to the presence of sesquiterpene lactones, enhances the antifungal action of chlorhexidine against yeast fungi of the Candida genus. Simultaneously, Vitex trifolia and Dendrobium nobile demonstrate antioxidant and antihistamine-like effects, which reduces tissue damage and itching, enhancing the protective action of the mineral component magnetite, traditionally used in medicine to stabilize auditory function.

A special place in the formula belongs to the animal raw material — Erionota torus larva. Literature shows that Lepidoptera larvae contain antimicrobial peptides with pronounced activity against fungi and bacteria. Their combination with chlorhexidine and phytosubstances creates an additive and partially potentiating antifungal effect. This type of interaction is tissue-specific synergy aimed at inhibiting the growth of pathogenic microorganisms in the external ear area. Additionally, Cyathula officinalis with its influence on microcirculation provides modulation of local blood flow, which may enhance the delivery of active substances to the tissues.

Overall, the drug implements a complex mechanism: synergy between the antiseptic and borneol ensures penetration and suppression of microbial factors; plant and animal components enhance anti-inflammatory and antifungal potential; the mineral component stabilizes tissue reactions. Thus, a modulating and potentiating nature of interactions is formed, ensuring multicomponent protection and regulation of local processes.

References: PubChem (chlorhexidine, borneol, sesquiterpene lactones), PubMed (AMPs in Lepidoptera larvae; Vitex flavonoids anti-inflammatory activity; Dendrobium phenanthrenes), SpringerLink (herbal synergism studies), ScienceDirect (Saussurea costus antimicrobial data).

Pharmacodynamics of Jingdu Ear Drops

The pharmacodynamic profile of the drug is characterized by a combination of local antimicrobial, anti-inflammatory, analgesic, and antioxidant action. The main point effect is the disruption of membrane structures of bacteria and fungi under the action of chlorhexidine acetate, accompanied by inhibition of biofilms and destruction of cell walls. This mechanism works at the cellular level and belongs to nonspecific antiseptic reactions.

Borneol modulates the pharmacodynamics of the entire complex by enhancing tissue permeability and facilitating transepithelial transport of other active substances. This increases local concentrations of phytochemical compounds, such as the sesquiterpene lactones of Saussurea costus, which have the ability to inhibit inflammatory mediators (IL-6, TNF-α). As a result, an additional anti-inflammatory and antimicrobial effect is realized at the cellular level.

Dendrobium nobile and Vitex trifolia provide antioxidant action due to phenanthrenes and flavonoids, which reduce the formation of reactive oxygen species and stabilize cell membranes. Cyathula officinalis has a local effect on microcirculation, leading to improved tissue nutrition and accelerated restoration of epithelial structures. The mineral component Magnetite, although not exhibiting direct pharmacological action on molecular cascades, is traditionally considered a stabilizer of tissue processes in the auditory apparatus area.

A special role belongs to the peptides of the Erionota torus larva, which have antimicrobial and antimycotic activity. At the cellular level, they can disrupt the integrity of fungal cell walls and suppress pathogen growth. Collectively, this enhances the action of chlorhexidine and plants, forming a synergistic antimicrobial effect.

Thus, the pharmacodynamics of Jingdu Ear Drops is characterized by multicomponent action: systemic suppression of inflammatory mediators, local inactivation of microorganisms, antioxidant protection, and modulation of tissue blood flow. These effects are realized at the cellular and tissue levels, with a predominantly local direction of action.

References: PubMed (chlorhexidine pharmacodynamics; borneol absorption enhancement; sesquiterpene lactones anti-inflammatory mechanisms; dendrobium phenanthrene activity; vitex flavonoids), PMC (insect antimicrobial peptides), Wiley (Cyathula officinalis pharmacology), WHO monographs on medicinal plants.

Pharmacokinetics of Jingdu Ear Drops

The pharmacokinetic profile of the drug is determined by the local route of administration — instillation into the external auditory canal. The main component, chlorhexidine, acts primarily locally: it is slowly and limitedly absorbed through intact epidermis and mucous membranes, practically does not enter the systemic circulation. In case of eardrum damage, penetration into the middle ear is possible, which is associated with the risk of ototoxic action. Camphor and borneol are characterized by lipophilicity and can quickly penetrate through epithelial barriers; they not only exhibit their own pharmacological activity but also enhance the transport of other substances, increasing their local concentration.

Flavonoids (luteolin, vitexin, casticin) and phenanthrenes of dendrobium exhibit limited absorption through the skin, but upon contact with mucous membranes and damaged tissues, their penetration increases. These compounds are metabolized primarily in the liver (glucuronidation, sulfation); if absorbed systemically, they are excreted with bile and urine. Saponins of Cyathula may enhance mucosal permeability and exert local membrane-stabilizing action; when absorbed, they are metabolized by intestinal microflora, but with external use, the systemic effect is minimal.

Protein and peptide substances of the Erionota torus larva, possessing antimicrobial activity, act mainly locally. They are able to bind to cell walls of microorganisms and do not penetrate deeply into tissues. Their metabolism is carried out by local proteases; no systemic accumulation has been identified. The mineral component magnetite is bioinert and does not undergo systemic metabolism; with topical application, it serves the role of a traditional tissue stabilizer.

Collectively, the pharmacokinetics of Jingdu Ear Drops is characterized by local direction, minimal systemic absorption, and predominant excretion of insignificant amounts of metabolites through the liver and kidneys. The main active compounds realize pharmacological action at the site of application, which reduces the risk of systemic toxicity and ensures tissue-specific action on the epithelium of the external auditory canal.

References: PubMed (chlorhexidine absorption and ototoxicity), PMC (borneol permeation enhancers), ScienceDirect (flavonoid metabolism and excretion), SpringerLink (Dendrobium phenanthrenes pharmacokinetics), Wiley (saponins and mucosal permeability).

Mechanisms of Action and Scientific Justification: Jingdu Ear Drops

Liver and Gastrointestinal Tract. Flavonoids of Vitex trifolia and phenanthrenes of Dendrobium nobile have antioxidant and membrane-stabilizing properties, reduce lipid peroxidation, and inhibit the activity of cytochrome P450 enzymes, which reduces the level of toxic metabolites. Saponins of Cyathula officinalis modulate bile secretion and participate in lipotropic regulation. The nature of interaction is additive, the level of action is systemic, pharmacological targets are antioxidant defense enzymes and membrane lipids.

Reference: https://pubmed.ncbi.nlm.nih.gov/28757555/

Immune System. Sesquiterpene lactones of Saussurea costus inhibit the NF-κB cascade and reduce the production of pro-inflammatory cytokines (TNF-α, IL-6), acting on macrophages and neutrophils. Peptides of the Erionota torus larva demonstrate direct interaction with cell membranes of microorganisms, causing their lysis, and simultaneously stimulate innate immunity by activating local immune cells. The combination of these components forms a potentiating nature of interaction with a cellular level of action.

Reference: https://pmc.ncbi.nlm.nih.gov/articles/PMC8788269/

Nervous System. Borneol and camphor exert a modulating influence on TRP channel receptors, reducing the severity of itching and pain sensations. The influence is realized at the level of peripheral nerve endings of the auditory canal, acting as local sensory modulators. The nature of action is additive, targets are sensory neurons of the skin and mucous membranes.

Reference: https://pubmed.ncbi.nlm.nih.gov/29925288/

Endocrine and Metabolic Regulation. Flavonoids of Vitex trifolia exert a modulating effect on prostaglandin levels through inhibition of COX and LOX enzymes, which influences the regulation of inflammatory processes and tissue metabolism. Dendrobium alkaloids additionally exhibit antiglycolytic activity, regulating energy metabolism in cells. The nature of interaction is modulating, the level of action is cellular and tissue, pharmacological targets are COX/LOX enzymes and metabolic cascades.

Reference: https://www.sciencedirect.com/science/article/pii/S0378874119302862

General Conclusion. The mechanisms of action of Jingdu Ear Drops are realized through synergistic interaction of the antiseptic component (chlorhexidine), phytochemical compounds (flavonoids, saponins, lactones), peptides of animal origin (Erionota torus), and auxiliary substances (borneol). As a result, multicomponent action is achieved: antioxidant, anti-inflammatory, modulating, membrane-stabilizing, antibacterial, and antimycotic.

References: PubMed (chlorhexidine, borneol, Saussurea lactones, Vitex flavonoids), PMC (insect antimicrobial peptides), ScienceDirect (Dendrobium phenanthrenes), SpringerLink (Cyathula saponins), Wiley (flavonoid COX/LOX modulation).