Lincomycin-based compound external lotion

Abstract

The invention relates to a compound external lotion based on lincomycin, which is characterized in that every two or three of lincomycin, lidocaine and vitamin B6 are compounded to form a multi-effect synergistic local treatment composition. The lotion takes an antibacterial effect as a core, integrates the functions of easing pain, relieving itching, resisting inflammation and repairing, and can synchronously solve the problems of skin infection, pain and barrier injury. Lincomycin efficiently inhibits pathogenic microorganisms, lidocaine quickly relieves pain and itching symptoms, vitamin B6 promotes epidermis repair and metabolic regulation, the lincomycin, lidocaine and vitamin B6 are scientifically matched to achieve complementary synergism, and every two of the lincomycin, lidocaine and vitamin B6 are simplified and combined to meet different clinical requirements. The dosage form design covers solution, gel and suspension dosage forms, has permeability, adhesiveness and stability, and is suitable for various skin lesions such as acute exudation and chronic wound surfaces. According to the scheme, the systemic side effects are reduced through local administration, and the treatment safety and the patient compliance are remarkably improved through optimization of low-irritation auxiliary materials.

Description

Technical Field

[0001] The present invention relates to the technical field, and specifically to a compound topical lotion based on lincomycin. Background Art

[0002] In the clinical treatment of skin infectious diseases, topical antibiotics are the core means to control the proliferation of pathogenic microorganisms and reduce the inflammatory response. As a broad-spectrum bacteriostatic agent, lincomycin has a significant inhibitory effect on Gram-positive bacteria and has been widely used in the topical treatment of skin infections. However, single antibiotic preparations have obvious limitations: firstly, their mechanism of action focuses on antibacterial, lacking targeted relief of discomfort symptoms such as pain and itching caused by infection, resulting in reduced patient compliance; secondly, long-term use of single antibiotics is prone to induce the generation of drug-resistant strains, forcing clinicians to increase the drug concentration, thereby increasing the risk of skin irritation; thirdly, infectious skin lesions are often accompanied by epidermal barrier damage, and traditional antibacterial preparations lack functional components to promote repair, which may prolong the healing period.

[0003] Currently, some compound preparations attempt to combine antibiotics with local anesthetics to achieve antibacterial and analgesic effects simultaneously. However, such compounds mostly adopt fixed ratios, unable to adapt to the needs of different disease courses, and do not introduce skin metabolism regulating components, making it difficult to balance barrier repair and anti-inflammatory synergy. In addition, the existing topical dosage forms are single. Solution dosage forms have poor adsorption to exudative wounds, gel dosage forms have insufficient penetration into deep tissues, and suspension dosage forms have poor stability, resulting in limited efficacy. Some products are prone to cause contact dermatitis due to strong irritation of excipients, further exacerbating skin damage.

[0004] Therefore, there is an urgent need to develop a topical compound lotion with multi-effect synergy, flexible dosage form and low irritation. Through scientific compatibility of active ingredients and dosage form optimization, on the basis of efficient antibacterial, integrate symptom relief and tissue repair functions, and at the same time adapt to the personalized treatment needs of different clinical scenarios. Summary of the Invention

[0005] The present invention aims to solve the problems of the prior art and provides a compound topical lotion based on lincomycin.

[0006] To solve the above technical problems, the present invention is realized through the following technical solutions:

[0007] A compound topical lotion based on lincomycin, which is composed of the following active ingredients: lincomycin, lidocaine and vitamin B6, and pharmaceutically acceptable excipients, and the lotion is a topical local dosage form.

[0008] This application innovatively combines lincomycin, lidocaine, and vitamin B6 to develop a multi - effect topical lotion with antibacterial, analgesic, anti - inflammatory, and skin - repair functions. As a broad - spectrum antibiotic, lincomycin can effectively inhibit Gram - positive bacterial infections and reduce skin inflammatory reactions; lidocaine quickly relieves discomfort symptoms such as itching and pain through local anesthetic effects, improving patient compliance; vitamin B6 plays a role in regulating sebum metabolism, promoting epidermal repair, enhancing local microcirculation, and accelerating the healing of lesions. The synergy of the three not only achieves multi - target treatment of infection control, symptom relief, and tissue repair, but also reduces the risks of drug resistance or irritation caused by the use of a single component at a high concentration. In addition, by streamlining to two - component combinations (lincomycin + lidocaine or lincomycin + vitamin B6), precise treatment plans can be provided for different indications (such as infections mainly with pain or accompanied by severe skin lesions), combining flexibility and economy. This lotion uses a topical dosage form to avoid the side effects of systemic drug use, and ensures the stability of ingredients and the transdermal absorption efficiency by optimizing the ratio of excipients, and is applicable to skin diseases such as acne, folliculitis, and postoperative wounds that require antibacterial and anti - inflammatory treatment, with significant clinical application value

[0009] In a specific embodiment, the first active ingredient consists of lincomycin and lidocaine and does not contain vitamin B6.

[0010] In a specific embodiment, the active ingredient consists of lincomycin and vitamin B6 and does not contain lidocaine.

[0011] In a specific embodiment, the dosage form is a solution - type, suspension - type, or gel - type lotion.

[0012] In a specific embodiment, the concentration of lincomycin is 0.1 - 5% w / w, the concentration of lidocaine is 0.5 - 3% w / w, and the concentration of vitamin B6 is 0.1 - 2% w / w (when included).

[0013] In a specific embodiment, pharmaceutically acceptable excipients include at least one of a solvent, a thickening agent, a preservative, or a pH regulator.

[0014] The beneficial effects of the present invention are as follows:

[0015] 1. By innovatively compounding lincomycin, lidocaine, and vitamin B6, the limitations of single components are overcome, achieving synergistic effects with multiple treatment mechanisms. Lincomycin provides broad-spectrum antibacterial action, inhibiting the proliferation of pathogenic microorganisms at the source; lidocaine rapidly relieves pain and itching through local anesthesia, significantly enhancing the treatment comfort of patients; vitamin B6 targets skin barrier repair and metabolic regulation, accelerating the recovery of damaged tissues. The complementary effects of the three not only cover the full-course requirements of infection control, symptom relief, and tissue repair, but also reduce the risk of drug resistance and skin irritation by synergistically decreasing the usage concentration of single components. In addition, two simplified compound formulations (lincomycin + lidocaine or lincomycin + vitamin B6) can be flexibly adapted to different clinical scenarios, such as acute infections mainly characterized by pain or chronic inflammation accompanied by skin lesions, providing diverse options for precise treatment;

[0016] 2. By optimizing the design of the lotion dosage form, the advantages of topical application are fully exploited, avoiding the metabolic burden and systemic side effects that may be caused by systemic drug administration. The solution-type lotion can rapidly penetrate deep into the lesion, being suitable for acute exudative skin lesions; the gel dosage form has strong adhesiveness, prolonging the residence time of the drug, and is suitable for easily friction-prone parts such as joints and folds; the suspension dosage form can stably carry poorly soluble active ingredients, expanding the scope of application. All dosage forms pay attention to skin affinity, reducing irritation by scientifically formulating excipients and enhancing patient compliance. At the same time, the modular design of the compound ratio facilitates the adjustment of the formula according to individual differences or disease stages, taking into account treatment efficiency and economy, and providing a safe, convenient, and customizable skin external treatment solution for clinical practice. Brief Description of the Drawings

[0017] Figure 1 It is a schematic diagram of the formula ratio of the present invention. Detailed Embodiments

[0018] Next, the technical solutions in the embodiments of the present invention will be clearly and completely described in conjunction with the embodiments of the present invention. Obviously, the described embodiments are only a part of the embodiments of the present invention, rather than all of the embodiments. All other embodiments obtained by those of ordinary skill in the art based on the embodiments of the present invention without creative efforts shall fall within the protection scope of the present invention.

[0019] As Figure 1 shown: A compound topical lotion based on lincomycin.

[0020] Example 1: Lincomycin + Lidocaine + Vitamin B6 Compound Solution-Type Lotion

[0021] Formulation (by weight percentage):

[0022] Lincomycin: 1.2%

[0023] Lidocaine: 2.0%

[0024] Vitamin B6 (Pyridoxine Hydrochloride): 0.5%

[0025] Ethanol (solvent): 20%

[0026] Glycerol (humectant): 5%

[0027] Phenoxyethanol (preservative): 0.5%

[0028] Purified water: the balance

[0029] Preparation steps:

[0030] Dissolve the active ingredients: Dissolve lincomycin in ethanol and stir until completely dissolved; add lidocaine and vitamin B6, and continue to stir for 10 minutes to form a homogeneous solution.

[0031] Mix the excipients: Mix glycerol, phenoxyethanol and purified water, heat to 40 °C and stir until transparent.

[0032] Compound: Slowly add the active ingredient solution to the excipient solution while stirring (rotation speed 300 rpm), and adjust the pH to 5.5 - 6.0 after mixing (using citric acid or sodium hydroxide for adjustment).

[0033] Homogenize: Process twice through a homogenizer (pressure 20 MPa) to ensure the stability of the system without stratification.

[0034] Fill: Filter and then dispense into light - resistant bottles, and store sealed.

[0035] Effect verification:

[0036] Stability test (40 °C / 75% RH, 3 months) shows that the component content decreases by < 5% and no crystallization occurs.

[0037] In vitro transdermal experiment shows that the transdermal rate of lidocaine reaches 12 μg / cm 2 / h, and it can take effect quickly.

[0038] Example 2: Lincomycin + Lidocaine Gel - type Lotion (without vitamin B6)

[0039] Formulation (w / w):

[0040] Lincomycin: 0.8%

[0041] Lidocaine: 1.5%

[0042] Carbomer 940 (gel matrix): 1.0%

[0043] Propylene glycol (penetration enhancer): 4%

[0044] Triethanolamine (pH regulator): 0.3%

[0045] Methylparaben (preservative): 0.1%

[0046] Purified water: the balance

[0047] Preparation steps:

[0048] Swelling the matrix: Disperse Carbomer 940 in purified water and let it stand for swelling for 12 hours.

[0049] Dissolving the drug: Dissolve lincomycin and lidocaine in propylene glycol and sonicate for 10 minutes.

[0050] Mixing: Slowly add the drug solution to the Carbomer matrix and dropwise add triethanolamine with stirring until a gel is formed (pH 6.2 - 6.5).

[0051] Homogenization and sterilization: Homogenize and then autoclave at 121 °C for 15 minutes. After cooling, add the methylparaben solution and stir well.

[0052] Sub-packaging: Fill into aluminum tubes and store in the dark.

[0053] Features:

[0054] The gel dosage form has a moderate viscosity (measured by Brookfield viscometer: 4500 cP), is easy to apply and does not drip.

[0055] Example 3: Lincomycin + Vitamin B6 Suspension Lotion (without lidocaine)

[0056] Formula (w / w):

[0057] Lincomycin: 1.0%

[0058] Vitamin B6 (micronized): 0.8%

[0059] Xanthan gum (thickener): 0.2%

[0060] Polysorbate 80 (dispersant): 0.5%

[0061] Potassium sorbate (preservative): 0.2%

[0062] Purified water: the balance

[0063] Preparation steps:

[0064] Dispersing the drug: Mix micronized vitamin B6 with polysorbate 80 and ball mill for 2 hours until the particle size ≤ 50 μm.

[0065] Preparing the suspension: Dissolve lincomycin in purified water, add xanthan gum and stir until swollen; slowly add the vitamin B6 dispersion and homogenize (15,000 rpm) for 5 minutes.

[0066] Adjustment and filling: Add potassium sorbate, adjust the pH to 4.8 - 5.2 (to suit the stability of lincomycin), dispense into brown bottles, and shake well before use.

[0067] Application scenarios:

[0068] Suitable for patients with acne combined with seborrheic dermatitis. Vitamin B6 can regulate sebum secretion, and lincomycin inhibits Propionibacterium acnes.

[0069] Although the embodiments of the present invention have been shown and described, it will be understood by those of ordinary skill in the art that various changes, modifications, substitutions, and variations can be made to these embodiments without departing from the principles and spirit of the present invention. The scope of the present invention is defined by the appended claims and their equivalents.

Claims

1. A compound external lotion based on lincomycin, characterized in that, It consists of the following active ingredients: lincomycin, lidocaine and vitamin B6, as well as pharmaceutically acceptable excipients, and the lotion is a topical dosage form for external use.

2. The compound external lotion based on lincomycin according to claim 1, characterized in that, The active ingredients consist of lincomycin and lidocaine, and do not contain vitamin B6.

3. The compound external lotion based on lincomycin according to claim 1, wherein The active ingredients consist of lincomycin and vitamin B6, and do not contain lidocaine.

4. A compound topical lotion based on lincomycin according to any one of claims 1 to 3, characterized in that, The dosage form is a solution, suspension or gel lotion.

5. A compound topical lotion based on lincomycin according to any one of claims 1 to 3, characterized in that, The concentration of lincomycin is 0.1 - 5% w / w, the concentration of lidocaine is 0.5 - 3% w / w, and the concentration of vitamin B6 is 0.1 - 2% w / w (when included).

6. A compound topical lotion based on lincomycin according to any one of claims 1 to 3, characterized in that, Pharmaceutically acceptable excipients include at least one of a solvent, a thickening agent, a preservative or a pH regulator.

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