Composite bath product containing lincomycin and vitamin B6 and preparation method thereof

Abstract

The invention relates to a compound bath product containing lincomycin and vitamin B6 and a preparation method of the compound bath product, and relates to the technical field of daily chemical products. Aiming at the problems of single effect, low component residence rate, poor medical component adaptability and the like of a traditional bath product in acne care, a triple synergistic formula of lincomycin (antibacterial), vitamin B6 (oil control) and glycyrrhizic acid / glycosylglycerol (anti-inflammatory) is innovatively constructed, and the adjuvant therapy effect on mild acne is effectively improved through clinical verification; a pH / temperature dual-response microcapsule wrapping technology is developed, so that the transdermal absorption rate of active ingredients is effectively improved, and the washing loss rate is less than or equal to 15%; the traditional Chinese medicine composition breaks through the limitation of medical cream types, is matched with bath carriers such as facial cleanser, shampoo, soap, shower gel and the like, and realizes daily application of acne care components. The product disclosed by the invention has the advantages of controlling oil within 6 hours and reducing the skin irritation by 42%, and fills up the technical blank of washing and caring products in medicine-grade efficacy and use convenience.

Description

Technical Field

[0001] The present invention relates to the technical field of bath products, and specifically to a composite bath product containing lincomycin and vitamin B6 and a preparation method thereof. Background Art

[0002] The following technical bottlenecks exist in the current bath products for acne care and oil control functions:

[0003] Single efficacy: Commercially available products mostly rely on a single active ingredient. For example, salicylic acid only controls oil, and tea tree essential oil only has antibacterial properties, lacking a composite system for inhibiting Propionibacterium acnes, controlling oil (regulating sebaceous glands), and reducing inflammation (alleviating swelling and redness);

[0004] Defect in ingredient retention: The loss rate of active ingredients during the rinsing process is >60%. For example, the retention rate of free lincomycin in traditional facial cleansers is only 53%, resulting in low transdermal absorption efficiency;

[0005] Lack of synergistic effect: In the prior art, antibacterial ingredients and oil control ingredients, such as benzoyl peroxide and zinc salts, mostly act independently, lacking a compatibility scheme for regulating the skin microecology, and not solving the coexistence problem of ingredient rinsing loss and irritation.

[0006] Therefore, a composite bath product containing lincomycin and vitamin B6 and a preparation method thereof are needed to solve the above problems. Summary of the Invention

[0007] In order to solve the problems of the prior art, the present invention provides a composite bath product containing lincomycin and vitamin B6 and a preparation method thereof.

[0008] In order to solve the above technical problems, the present invention is achieved through the following technical solutions: In the first aspect, a composite bath product containing lincomycin and vitamin B6, comprising active ingredients in the following weight percentages:

[0009] 0.1 - 1.5% of lincomycin or a pharmaceutically acceptable salt thereof;

[0010] 0.5 - 2% of vitamin B6;

[0011] 1 - 3% of a plant anti-inflammatory complex, and the plant anti-inflammatory complex comprises glycyrrhizic acid and glucosylglycerol;

[0012] Wherein the composition loads the active ingredients through microcapsule encapsulation technology, and is applicable to facial cleansers, facial wash products, soaps, toilet soaps, hair care products or bath products.

[0013] In this application, by compounding and matching lincomycin (antibacterial), vitamin B6 (oil control) and anti-inflammatory ingredients such as glycyrrhizic acid, and combining with the innovation of microcapsule encapsulation technology, three core functions are achieved:

[0014] Functional synergy: Break through the limitation of the single efficacy of traditional bathing products, simultaneously inhibit Propionibacterium acnes, regulate sebum secretion and relieve inflammatory reactions, especially suitable for skin problems such as facial acne and scalp seborrheic dermatitis;

[0015] Enhanced efficacy: Through the pH / temperature dual-responsive microcapsule carrier, the transdermal absorption rate of active ingredients is increased to 81% (53% higher than the traditional process), the ingredient loss rate during rinsing is reduced to less than 15%, and the residence time is extended;

[0016] Scene expansion: After the dosage form transformation of medical-grade acne treatment ingredients, they are extended to the fields of skin care products such as facial cleansers and shampoos, filling the technical gap between daily chemical products in the auxiliary treatment of mild acne and the demand for long-term oil control, and are suitable for multiple bathing carriers such as soaps and body washes.

[0017] In a specific embodiment of the first aspect, the microcapsule encapsulation technology includes:

[0018] Using a pH-sensitive carrier to perform primary microencapsulation on lincomycin to form nano-microcapsules with a particle size ≤ 200 nm;

[0019] Using a temperature-responsive hydrogel to perform secondary encapsulation on vitamin B6, and the hydrogel contains a composite of sodium alginate and chitosan.

[0020] In a specific embodiment of the first aspect, the release rate of the pH-sensitive carrier is ≥ 80% in an environment with a pH of 5.0 - 6.5, and the swelling degree of the temperature-responsive hydrogel increases by 150 - 200% at 35 - 40 °C.

[0021] Second aspect, the uses of a composite bathing product containing lincomycin and vitamin B6 include at least one of the following application scenarios:

[0022] Cleaning and care of the seborrheic area of facial skin;

[0023] Adjuvant treatment of scalp seborrheic dermatitis;

[0024] Preventive care of acne on the trunk.

[0025] Third aspect, a preparation method of a composite bathing product containing lincomycin and vitamin B6 includes the following steps:

[0026] S1: Perform microencapsulation pretreatment on lincomycin and vitamin B6 respectively;

[0027] S2: Mix the microencapsulated products obtained in step S1 with a plant anti-inflammatory complex at 40 - 45 °C;

[0028] S3: homogenizing the mixture with the surfactant base at a shear rate of 800-1200 rpm;

[0029] S4: Adjust the pH value of the final product to the range of 5.5-6.2.

[0030] The beneficial effects of the present invention are:

[0031] 1. Triple effect collaborative innovation

[0032] Composite formula design: Breaking through the single function limitation of traditional bath products, through the synergistic compatibility of lincomycin (antibacterial), vitamin B6 (oil control), and glycyrrhizic acid (anti-inflammatory) (synergistic index FIC = 0.52), the inhibition rate of Propionibacterium acnes is increased by 21.2% (compared with a single ingredient), while reducing sebum secretion by 34.7% (6 hours of continuous oil control). Breakthrough process improvement, doubled transdermal efficiency: Using pH-sensitive (sodium alginate) and temperature-responsive (chitosan-glycerol glucoside) dual-carrier microencapsulation technology, the transdermal absorption rate of active ingredients is increased from 53% of the traditional process to 81.3% (Franz diffusion cell test), and the ingredient loss rate during rinsing is ≤15% (traditional products>60%). Adaptable to multiple dosage forms: The medical-grade ingredients (original cream dosage form) are successfully transformed into bath products, covering carriers such as facial cleansers, shampoos, and soaps (such as Examples 1-3), filling the technical gap between the pharmaceutical-grade efficacy of bath products and the convenience of daily use.

[0033] 2. Application scenario expansion, new use patent support: Based on the original indications of lincomycin vitamin B6 cream (acne, seborrheic dermatitis), it is expanded to the auxiliary treatment scenarios of bath products (such as scalp seborrheic dermatitis care, back acne prevention), and the scope of patent protection is expanded. Safety improvement: Patch test verification shows that the compound formula reduces irritation by 42% (compared with traditional antibacterial facial cleansers), meeting the long-term use needs of people with sensitive skin.

[0034] 3. Industrialization advantages: Controllable process parameters: Clarify core parameters such as microcapsule particle size (≤200nm), mixing temperature (40±2℃), shear rate (800-1200rpm), etc. to ensure production stability (accelerated test 3-month active ingredient retention rate>95%). Ingredient naming standards: Correct "lincomycin" to the standardized term "lincomycin" (as shown in the second picture) to avoid patent text description risks. DETAILED DESCRIPTION

[0035] Next, in combination with the embodiments of the present invention, the technical solutions in the embodiments of the present invention will be clearly and completely described. Obviously, the described embodiments are only a part of the embodiments of the present invention, rather than all 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.

[0036] A compound bathing product containing lincomycin and vitamin B6 and a preparation method thereof.

[0037] Example 1: Preparation of oil-control facial cleanser containing microencapsulated active ingredients

[0038] Formulation composition (weight percentage):

[0039] Lincomycin 0.8% (encapsulated by pH-sensitive sodium alginate microcapsules, particle size 182 ± 15 nm)

[0040] Vitamin B6 1.2% (coated with temperature-responsive chitosan-glyceroglucoside hydrogel)

[0041] Plant anti-inflammatory complex 2.5% (glycyrrhizic acid extract: glyceroglucoside = 1:1.5)

[0042] Surfactant base 15% (sodium methyl cocoyl taurate)

[0043] The balance is deionized water, thickener (carbomer 940) and pH regulator (citric acid)

[0044] Preparation process:

[0045] Pretreatment of active ingredients:

[0046] Mix lincomycin with 1.5% sodium alginate solution at pH 4.0, and prepare nano-microcapsules by high-pressure microfluidization technology (pressure 120 MPa), and centrifuge to collect microcapsule particles with a particle size ≤ 200 nm.

[0047] Crosslink vitamin B6 with 3% chitosan solution and 2% glyceroglucoside at 50 °C for 30 minutes to form temperature-responsive hydrogel particles.

[0048] Mixing and homogenization:

[0049] Stir and mix the microencapsulated lincomycin, vitamin B6 hydrogel particles and plant anti-inflammatory complex in a 40 °C water bath (rotation speed 600 rpm, time 20 minutes).

[0050] Add the surfactant base and the pre-sol of carbomer 940, and homogenize at a rate of 1000 rpm in a shear homogenizer for 15 minutes.

[0051] Final product adjustment:

[0052] Adjust the pH to 5.8 ± 0.2 with citric acid, add 0.5% phenoxyethanol as a preservative, and fill to obtain.

[0053] Example 2: Preparation of a scalp seborrheic dermatitis care shampoo

[0054] Formulation composition (weight percentage):

[0055] Lincomycin 1.0% (pH-sensitive microcapsules, particle size 195 ± 20 nm)

[0056] Vitamin B6 1.5% (temperature-responsive hydrogel particles)

[0057] Synergistic enhancer 1.8% (tea tree essential oil nanoemulsion)

[0058] Surfactant base 20% (sodium lauryl polyether sulfate + cocamidopropyl betaine)

[0059] The balance is deionized water, sodium chloride and fragrance

[0060] Preparation process:

[0061] Active ingredient loading:

[0062] The preparation of lincomycin microcapsules is the same as in Example 1, and the concentration of the microcapsule solution is increased to 2.5%.

[0063] Add 0.5% polysorbate 80 to the vitamin B6 hydrogel particles to improve scalp permeability.

[0064] Compound and stabilization:

[0065] Premix the microencapsulated active ingredient and the tea tree essential oil nanoemulsion at 35°C, and add ultrasonic dispersion (frequency 40 kHz, time 10 minutes) after adding the surfactant base.

[0066] Adjust the system viscosity to 8000 - 10000 cP (25°C), and control the pH at 6.0 - 6.3.

[0067] Example 3: Preparation of an acne preventive care soap

[0068] Formulation composition:

[0069] Lincomycin 0.5% (premixed with soap base after microencapsulation)

[0070] Vitamin B6 0.8% (sustained-release particles with magnesium stearate as a stabilizer)

[0071] Plant anti-inflammatory complex 1.2% (dipotassium glycyrrhizinate)

[0072] Soap base matrix 82% (coconut oil / palm oil sodium soap)

[0073] Auxiliary components: glycerin 3%, titanium dioxide 0.5%

[0074] Preparation process:

[0075] Mix lincomycin microcapsules, vitamin B6 sustained-release granules and dipotassium glycyrrhizinate dry powder, and pass through a 100-mesh sieve to ensure uniform dispersion.

[0076] Add the active ingredient mixture during the soap base melting stage (75 - 80 °C), stir until completely fused, and then inject into a mold for molding.

[0077] Comparative experiment design

[0078] Experimental group setting

[0079]

[0080] Key experimental data

[0081] 1. Verification of the synergistic effect of the composite formula (in vitro experiment)

[0082] Antibacterial experiment: inhibition zone diameter against Propionibacterium acnes (24 h).

[0083] Experimental group A: 18.3 ± 0.5 mm (synergy index FIC of lincomycin + VB6 = 0.52). Lincomycin alone: 15.1 ± 0.3 mm.

[0084] Vitamin B6 alone: no inhibition zone.

[0085] Anti-inflammatory experiment: inhibition rate of TNF-α in LPS-induced macrophages.

[0086] Experimental group A: 67.2% → glycyrrhizic acid and lincomycin produce a synergistic anti-inflammatory effect (p < 0.01).

[0087] 2. Verification of the microencapsulation process (ex vivo skin experiment)

[0088] Transdermal absorption rate (Franz diffusion cell, 6 h):

[0089] Experimental group A: 81.3% ± 3.2% (microencapsulated lincomycin).

[0090] Experimental group B: 52.7% ± 2.8% (free lincomycin).

[0091] Rinsing residue rate (simulated rinsing with artificial skin membrane):

[0092] Experimental group A: 14.6% active ingredient remaining → the anti-rinsing property of the microcapsule is increased by 3.2 times.

[0093] 3. Verification of the new use effect (human experiment)

[0094] Improvement rate of mild acne (12 weeks, n = 60):

[0095] Experimental group A: 78.3% (≥ 50% reduction in inflammatory papules).

[0096] Control group C: 65.6% (p = 0.032).

[0097] Oil control timeliness (measured by sebum meter):

[0098] Experimental group A: 34.7% reduction in sebum secretion in 6 hours.

[0099] Experimental group B: Only a 18.2% reduction (significant microcapsule sustained-release effect).

[0100] Experimental conclusion

[0101] Synergistic effect: The antibacterial effect of the composite formula is increased by 21.2% compared with the single ingredient (p < 0.05), and the anti-inflammatory activity exceeds the superposition effect of single ingredients.

[0102] Process advantage: The microcapsule technology increases the effective utilization rate of active ingredients from 53% of the traditional process to 81%.

[0103] Scene adaptation: In the field of adjuvant treatment of acne, the clinical effective rate of experimental group A is increased by 12.7 percentage points compared with commercially available salicylic acid products.

[0104] 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, and the scope of the present invention is defined by the appended claims and their equivalents.

Claims

1. A compound bath product containing lincomycin and vitamin B6, characterized in that, Contains active ingredients in the following weight percentages: 0.1 - 1.5% of lincomycin or its pharmaceutically acceptable salt; 0.5 - 2% of vitamin B6; 1 - 3% of a plant anti-inflammatory complex, said plant anti-inflammatory complex containing glycyrrhizic acid and glucosylglycerol; Wherein the composition loads active ingredients through microencapsulation technology and is applicable to facial cleansers, facial wash products, soaps, toilet soaps, hair care products or bath products.

2. The composite bath product containing lincomycin and vitamin B6 according to claim 1, wherein: The microencapsulation technology includes: Performing primary microencapsulation on lincomycin using a pH-sensitive carrier to form nano-microcapsules with a particle size ≤ 200 nm; Performing secondary encapsulation on vitamin B6 using a temperature-responsive hydrogel, said hydrogel containing a complex of sodium alginate and chitosan.

3. The composite bath product containing lincomycin and vitamin B6 according to claim 2 and its preparation method are characterized in that: The release rate of the pH-sensitive carrier is ≥ 80% in an environment with a pH of 5.0 - 6.5, and the swelling degree of the temperature-responsive hydrogel increases by 150 - 200% at 35 - 40 °C.

4. Use of a compound bath product containing lincomycin and vitamin B6, characterized in that: Includes at least one of the following application scenarios: Cleaning and caring for the seborrheic areas of facial skin; Adjuvant treatment of scalp seborrheic dermatitis; Preventive care for acne on the trunk.

5. A preparation method of a compound bath product containing lincomycin and vitamin B6, characterized in that: Includes the following steps: S1: Performing microencapsulation pretreatment on lincomycin and vitamin B6 separately; S2: Mixing the microencapsulation products obtained in step S1 with the plant anti-inflammatory complex at 40 - 45 °C; S3: Homogenizing the mixture with a surfactant base at a shear rate of 800 - 1200 rpm; S4: Adjusting the pH value of the final product to the range of 5.5 - 6.2.

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