Warming, dredging and pain relieving gel health-care patch and preparation method thereof

Abstract

The invention relates to a warming and pain-relieving gel health-care patch and a preparation method thereof, and belongs to the field of external traditional Chinese medicine preparations. The gel patch is prepared from traditional Chinese medicine extracts such as liquidambar formosana hance, caulis spatholobi and radix clematidis and auxiliary materials such as turpentine and carbomer copolymer according to a scientific ratio and a special process. The product has the effects of promoting blood circulation to remove blood stasis and activating meridians to stop pain, and is suitable for relieving sub-health symptoms such as limb swelling and pain and limited joint movement. The traditional Chinese medicine is creatively combined with a modern transdermal drug delivery technology, the drug transdermal absorption rate is remarkably improved through a specific matrix formula, and the patch has the advantages of being comfortable to apply, free of residues, lasting in effect and the like. Clinical verifications show that the analgesic effective rate for the initial stage of soft tissue injury reaches 92%, and the improvement rate of the joint activity reaches 85%.

Description

Technical Background

[0001] Most existing pain-relieving patches use a rubber paste matrix, which has problems such as poor air permeability, easy allergy, and unstable drug release. The transdermal absorption rate of the active ingredients in traditional Chinese medicine patches is generally lower than 15%, and there are also defects such as slow onset and short action time. Through screening specific Chinese medicine combinations and optimizing the extraction process, and combining with carbomer thermosensitive gel matrix, the present invention increases the transdermal absorption rate of drugs to more than 28%, and can continuously release for 6-8 hours. Animal experiments show that the inhibition rate of this preparation on acetic acid-induced writhing reaction is 40% higher than that of ordinary patches, and the skin irritation test meets the medical material standards.

[0002] Examples of Specific Embodiments

[0003] Example 1:

[0004] Prepared according to the following ratio:

[0005] 15 parts of Liquidambar formosana Hance, 20 parts of Spatholobus suberectus Dunn, 12 parts of Clematis chinensis Osbeck, 8 parts of Dry Ginger, 8 parts of Acorus tatarinowii Schott, 12 parts of Ligusticum wallichii Franch., 8 parts of Olibanum, 8 parts of Myrrha, 15 parts of Epimedium brevicornu Maxim., 18 parts of Tinospora sinensis (Lour.) Merr. Preparation process:

[0006] 1. Chinese medicine extraction: The crude powder of the medicinal materials is first refluxed and extracted twice with 65% ethanol (8 times the amount, 6 times the amount), and the filtrate is collected and concentrated to an extract of 1.20 g / ml;

[0007] 2. Matrix preparation: Slowly add 1.2% carbomer 940 to purified water, and add 0.2% potassium sorbate after stirring and swelling;

[0008] 3. Add the Chinese medicine extract (12%) and turpentine (5%) to the matrix, process with a homogenizer at 3000 rpm for 10 minutes, degas under vacuum and then coat on a non-woven fabric substrate, controlling the thickness of the gel layer to 2 mm. Specific Embodiments

[0009] 1. Optimization of the preparation parameters of the Chinese medicine extract adopts a hierarchical alcohol extraction process, and the specific parameters are as follows: The first extraction: 65% ethanol, solid-liquid ratio 1:8, reflux extraction at 85°C for 2 hours, collect volatile components and fat-soluble active substances

[0010] The second extraction: 45% ethanol, solid-liquid ratio 1:10, warm soaking extraction at 75°C for 3 hours, extract water-soluble active ingredients Verification of extraction times: Detect the extraction rate of ferulic acid by HPLC, and the dissolution rate of components reaches 98.2% after three extractions, so it is determined that two extractions are the best process Concentration parameters: The vacuum degree of the double-effect concentrator is -0.08 MPa, the temperature is 60°C, and it is concentrated to a relative density of 1.20 ± 0.05 (measured at 25°C)

[0011] 2. Quality detection method

[0012] Adopt a dual-index control system:

[0013] Qualitative detection: Identify Ligusticum chuanxiong by TLC method (the Rf value of the ligustilide spot is 0.32), and identify Olibanum by color reaction of acetyl-11-keto-β-boswellic acid

[0014] Quantitative detection:

[0015] Content of ferulic acid: HPLC method (chromatographic column: C18, mobile phase: acetonitrile - 0.1% phosphoric acid, detection wavelength: 316 nm), and it is required that each gram of extract contains ≥1.2 mg of ferulic acid

[0016] Content of total flavonoids: Ultraviolet spectrophotometry (calculated as rutin), and it is required that each patch contains ≥8 mg of total flavonoids

[0017] pH value control: The pH value of the gel patch is 5.5 - 6.5 (measured by PHB-4 type pH meter)

[0018] 3. Stability test data

[0019] Pass the national drug packaging material standard YBB00142002 test:

[0020] 4. Transdermal absorption comparison test

[0021] Adopt the Franz diffusion cell method (isolated mouse skin): 5. Clinical efficacy verification Select 60 patients with limb swelling and pain (the diagnosis conforms to the Diagnostic and Therapeutic Criteria for Traditional Chinese Medical Diseases and Syndromes): Grouping: 30 cases in the experimental group (this product), 30 cases in the control group (a certain Huoxue Zhitong Plaster)

[0022] Efficacy criteria:

[0023] Marked effect: The VAS score of pain decreases by ≥70%, and the joint range of motion improves by ≥50%

[0024] Effective: The VAS decreases by 30 - 69%, and the joint range of motion improves by 20 - 49%

[0025] Ineffective: Not meeting the above criteria

[0026] Typical cases:

[0027] Case 1: Li Mou, female, 52 years old, right wrist tendovaginitis. After applying the patch for 24 hours, the VAS score decreased from 7 points to 3 points, and after 7 days, the joint range of motion recovered to 85% of the normal level

[0028] Case 2: Wang Mou, male, 65 years old, knee osteoarthritis. After continuous use for 14 days, the Lysholm score increased from 48 points to 72 points

[0029] Innovation description

[0030] 1. Process innovation: The extraction rate of ferulic acid is increased by 42% through graded alcohol extraction, while retaining heat-sensitive components such as icariin (HPLC detection retention rate > 95%)

[0031] 2. Dosage form innovation: Carbomer 940 and turpentine form a thermosensitive gel system (phase transition temperature 32°C), and the adhesion after application reaches 0.8N / cm 2 , significantly higher than traditional plasters (0.3-0.5N / cm 2 )

[0032] 3. Innovation in quality control: Establish a fingerprint spectrum (similarity > 0.95) and specify 9 characteristic peaks as quality control indicators. BRIEF DESCRIPTION OF THE DRAWINGS

[0033] Figure 1 The present invention is a process flow chart of a warming and analgesic gel health care patch.

Claims

1. A warming and dredging pain-relieving gel health patch, characterized in that It is made from the following raw materials by weight percentage: 8 - 15% of traditional Chinese medicine extract composition, 3 - 8% of turpentine, 0.8 - 1.5% of carbomer copolymer, 0.1 - 0.3% of potassium sorbate, and the balance is purified water; The traditional Chinese medicine extract composition is prepared from the following raw materials by weight: 10 - 20 parts of fructus liquidambaris, 15 - 25 parts of caulis spatholobi, 8 - 15 parts of clematis chinensis, 5 - 12 parts of dried ginger, 6 - 10 parts of acorus tatarinowii, 8 - 15 parts of ligusticum wallichii, 5 - 10 parts of frankincense, 5 - 10 parts of myrrh, 10 - 18 parts of epimedium, 12 - 20 parts of peristrophe roxburghiana.

2. The gel health patch according to claim 1, wherein The traditional Chinese medicine extract composition is prepared by a step - by - step alcohol extraction process: first, volatile components are extracted with 60 - 70% ethanol, and then water - soluble components are extracted with 40 - 50% ethanol.

3. The preparation method according to claim 1, characterized in that It includes the following steps: (1) Preparation of traditional Chinese medicine extract: The Chinese medicinal materials are crushed and extracted with ethanol in two times, and the extraction solutions are combined and concentrated to an extract with a relative density of 1.15 - 1.25; (2) Preparation of matrix: The carbomer copolymer is dispersed in purified water and swollen, and then potassium sorbate is added; (3) The traditional Chinese medicine extract, turpentine and matrix are mixed and homogenized, and after vacuum degassing, they are coated and formed.

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