A kind of gallwood extract gel and its preparation process

Abstract

The invention provides a gallwood extract gel and a preparation process thereof. The gallwood extract gel comprises the following raw materials in parts by weight: 1.8-5.8 parts of gallwood extract, 12.9-39.8 parts of aqueous gel matrix, 1.6-5.9 parts of penetration enhancer, 2.1-3.9 parts of nanocarriers and 1.2-1.9 parts of oligopeptides. The gallwood extract drug, the aqueous gel matrix, the penetration enhancer and the carrier nanomaterials are scientifically proportioned to synergistically exert the drug properties, and under the interaction between the stratum corneum and lipids of the skin, the diffusion resistance of the drug in the stratum corneum is reduced, the fluidity is enhanced, the onset time of the drug is shortened, the active ingredients of the drug in the gel are sustained-released within a certain period of time, and a higher permeability is achieved, so as to play a quick-acting role, and the highest permeability reaches 96.2% at 36 hours.

Description

Technical Field

[0001] The invention relates to the field of pharmaceutical preparations, and in particular to a gallwood extract gel and a preparation process thereof. Background Art

[0002] Nauclea officinalis, also known as ebony, bear gall tree, yellow sheep wood, etc., is included in the "Chinese Pharmacopoeia" (1977 edition, Part I), "Hainan Province Chinese Medicinal Materials Standard" (First Edition) and "Chinese Materia Medica". It is mainly distributed in Guangdong, Guangxi, Hainan (Li areas such as Wuzhishan) and other places in my country. It is the dried stem (with skin) and root of the Rubiaceae plant Nauclea officinalis Pierre ex Pitard. Its functions and indications are clearing away heat and detoxification. It is used for colds and fevers, sore throats, furuncles in the external auditory canal, furuncles on the skin, acute conjunctivitis, acute jaundice, stomachache and other diseases. At the same time, Nauclea officinalis is a characteristic Li medicine in Hainan Province, and it is also one of the key medicines for Hainan Province to deeply study the origin of traditional Li medicine and the material basis of its efficacy. As one of the important medicines in my country's tropical regions, Nauclea officinalis is also known as "Chinese medicine antibiotics" because of its antibacterial, antiviral and anti-inflammatory effects. Because of its low toxicity and high safety, it is a very promising Li medicine for clinical application. However, according to the planting and harvesting standards of the gallwood, the stems of the gallwood often need to be planted for 4-5 years to mature before they can be used as raw materials for medicine. The active ingredients of the drugs are combined with gels to make drug gels that can act directly on the skin surface. However, due to the natural characteristics of Chinese medicinal materials and differences in the growth environment, the ingredients and effects of Chinese medicine gels may have certain fluctuations. When Chinese medicine gels are applied topically, due to their high viscosity, there may be problems with poor permeability, or the active ingredients in the gel may be released too quickly, and some of the active ingredients will remain on the skin surface. The active ingredients are released too slowly and cannot play a good role, so that the efficacy cannot be fully exerted. Summary of the invention

[0003] In view of this, the present invention proposes a gallwood extract gel and a preparation process thereof to solve the above problems.

[0004] The technical solution of the present invention is achieved as follows: a gallwood extract gel comprises the following raw materials in parts by weight: 1.8-5.8 parts of gallwood extract, 12.9-39.8 parts of aqueous gel matrix, 1.6-5.9 parts of penetration enhancer, 2.1-3.9 parts of nanocarrier, and 1.2-1.9 parts of oligopeptide:

[0005] Furthermore, the gallwood extract gel comprises the following raw materials in parts by weight: 3.8 parts of gallwood extract, 28.4 parts of aqueous gel matrix, 3.5 parts of penetration enhancer, 3.7 parts of nanocarrier, and 1.5 parts of oligopeptide.

[0006] Furthermore, the aqueous gel matrix is ​​poloxamer, polyvinyl pyrrolidone, and cellulose derivatives in a mass ratio of (3.3-5.9):(1.2-3.9):(5.2-10.9).

[0007] Preferably, the cellulose derivative is any one of methyl cellulose, sodium carboxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxymethyl cellulose phthalate, polyvinyl pyrrolidone, cellulose acetate phthalate, sodium hyaluronate, or a combination of two or more thereof.

[0008] Furthermore, the penetration enhancer is α-tocopherol polyethylene glycol succinate, ergosterol, and cocamidopropyl betaine in a mass ratio of (1.3-5.2):(4.9-9.7):(2.5-5.9).

[0009] Furthermore, the nanocarrier is a magnetic nanoparticle.

[0010] Furthermore, the magnetic nanoparticles are one or a combination of carboxylated ferrosoferric oxide nanoparticles, citric acid-modified Prussian blue nanoparticles, carboxylated urea-formaldehyde resin magnetic beads or aminourea-formaldehyde resin magnetic beads.

[0011] Furthermore, the oligopeptide is one or a combination of two of marine osteopeptide, oyster oligopeptide, soybean oligopeptide or corn polypeptide.

[0012] Furthermore, the preparation method of the Gallwood extract gel comprises the following steps:

[0013] (2) Preparation of gallwood extract: Take the woody part of gallwood, dry it, and grind it into 80-120 mesh sieve, use 70-95% volume fraction of n-butanol to extract 2-4 times, the extraction temperature is 75-85°C, the extraction time is 30-60 min each time, the mass volume ratio of gallwood and n-butanol is 1:5-8 g / mL, the extracts are combined, the residue is reserved, and the extract is concentrated to a relative density of 1.1-1.2 at 50°C to obtain n-butanol extract;

[0014] Take the above-mentioned medicinal residue and add water, the mass volume ratio of the medicinal residue to water is 10-25:50 g / mL, decoct for 1-3 hours, filter, take the filtrate, concentrate, and obtain a water extract with a relative density of 1.1-1.2 at 50° C.;

[0015] The n-butanol extract and the water extract are heated to 50-80° C., mixed and stirred evenly to obtain a gallwood extract;

[0016] (2) Preparation of Gallwood Extract Gel:

[0017] S1. Mix the above aqueous gel matrix with water at a mass volume ratio of 10-30 g / mL according to the ratio, heat to 65-80° C., and stir homogenously for 15-30 min to obtain a gel mixed solvent;

[0018] S2, adding the gallwood extract to the gel mixed solvent, mixing, stirring evenly at 20-40° C., stirring at a rate of 200-300 rpm, stirring for 10-20 min to obtain the extract gel mixed solvent;

[0019] S3. Add the penetration enhancer, nanocarrier and oligopeptide into the extract gel mixed solvent, and then stir and mix them evenly under γ-rays at a stirring rate of 200-300 rpm to obtain the Gallwood extract gel.

[0020] Furthermore, the homogenization stirring rate is 400-800 rpm, and the homogenization pressure is 400-600 MPa.

[0021] Furthermore, the gamma ray radiation dose is 0.5-5 kGy, and the irradiation time is 20-40 min.

[0022] Compared with the prior art, the present invention has the following beneficial effects:

[0023] The present invention is scientifically proportioned by each raw material such as gallwood extract medicine, aqueous gel matrix, penetration enhancer and carrier nanometer, and its drug performance is synergistically exerted, so that the active pharmaceutical ingredient in the gel is sustained-released within a certain period of time, and a higher permeability is achieved; wherein, the penetration enhancer is combined according to a specific ratio by alpha-tocopherol polyethylene glycol succinate, ergosterol, and cocamidopropyl betaine, and the addition of a penetration enhancer can obviously improve the permeability of the drug gel; interact with the biological interface (such as skin, mucous membrane, etc.), improve the affinity of the drug and the biological interface, and promote the penetration and absorption of the drug; adding nanocarriers can effectively wrap and protect drug molecules, prevent them from being affected by environmental factors, extend the storage life of the drug, and can also accurately control the drug release rate by regulating the interaction between the drug and the gel. This helps to optimize the drug treatment scheme, achieve continuous, sustained release or targeted release, improve the efficacy and reduce side effects. In addition, the ionization chemical effect of gamma-ray radiation causes the drug and the gel to undergo a cross-linking reaction, regulates the interaction between the drug and the gel, improves its drug release characteristics, and achieves precise control of the drug release rate. The drug is released in a slow and continuous manner, thereby providing better drug concentration and efficacy. DETAILED DESCRIPTION

[0024] In order to better understand the technical content of the present invention, specific embodiments are provided below to further illustrate the present invention.

[0025] Unless otherwise specified, the experimental methods used in the embodiments of the present invention are all conventional methods.

[0026] Unless otherwise specified, the materials, reagents, etc. used in the embodiments of the present invention can be obtained from commercial sources.

[0027] Example 1

[0028] A gallwood extract gel, comprising the following raw materials in parts by weight: 1.8 parts of gallwood extract, 12.9 parts of aqueous gel matrix, 1.6 parts of penetration enhancer, 2.1 parts of nanocarrier, and 1.2 parts of oligopeptide; the aqueous gel matrix is ​​poloxamer, polyvinyl pyrrolidone, and cellulose derivatives in a mass ratio of 3.3:1.2:5.2; the cellulose derivative is methylcellulose; the penetration enhancer is α-tocopherol polyethylene glycol succinate, ergosterol, and cocamidopropyl betaine in a mass ratio of 1.3:4.9:2.5; the nanocarrier is magnetic nanoparticles, and the magnetic nanoparticles are carboxylated ferroferric oxide nanomagnetic particles; the oligopeptide is marine osteogenic peptide;

[0029] Example 2

[0030] A gallwood extract gel, comprising the following raw materials in parts by weight: 5.8 parts of gallwood extract, 39.8 parts of aqueous gel matrix, 5.9 parts of penetration enhancer, 3.9 parts of nanocarrier, and 1.9 parts of oligopeptide; the aqueous gel matrix is ​​poloxamer, polyvinyl pyrrolidone, and cellulose derivatives in a mass ratio of 5.9:3.9:10.9; the cellulose derivative is methylcellulose; the penetration enhancer is α-tocopherol polyethylene glycol succinate, ergosterol, and cocamidopropyl betaine in a mass ratio of 5.29.7:5.9; the nanocarrier is magnetic nanoparticles, and the magnetic nanoparticles are citric acid-modified Prussian blue nanoparticles; the oligopeptide is soybean oligopeptide;

[0031] Example 3

[0032] A gallwood extract gel, comprising the following raw materials in parts by weight: 3.8 parts of gallwood extract, 28.4 parts of aqueous gel matrix, 3.5 parts of penetration enhancer, 3.7 parts of nanocarrier, and 1.5 parts of oligopeptide; the aqueous gel matrix is ​​poloxamer, polyvinyl pyrrolidone, and cellulose derivatives in a mass ratio of 4.2:2.5:7.1; the cellulose derivative is methylcellulose; the penetration enhancer is α-tocopheryl polyethylene glycol succinate, ergosterol, and cocamidopropyl betaine in a mass ratio of 3.2:6.2:4.8; the nanocarrier is magnetic nanoparticles, and the magnetic nanoparticles are citric acid-modified Prussian blue nanoparticles; the oligopeptide is oyster oligopeptide;

[0033] The above examples 1-3 adopt the following preparation method:

[0034] (1) Preparation of Gallwood Extract: The woody part of Gallwood was taken, dried, crushed with a 100-mesh sieve, extracted three times with 85% by volume n-butanol, the extraction temperature was 80°C, the extraction time was 40 min each time, the mass volume ratio of Gallwood to n-butanol was 1:7 g / mL, the extracts were combined, the residue was set aside, and the extract was concentrated to a relative density of 1.2 at 50°C to obtain n-butanol extract;

[0035] Take the above-mentioned medicinal residue and add water, the mass volume ratio of the medicinal residue to water is 18:50 g / mL, decoct for 2 hours, filter, take the filtrate, concentrate, and obtain a water extract with a relative density of 1.1 at 50°C;

[0036] The n-butanol extract and the water extract are heated to 70° C., mixed and stirred evenly to obtain a gallwood extract;

[0037] (2) Preparation of Gallwood Extract Gel:

[0038] S1. Mix the above aqueous gel matrix with water at a mass volume ratio of 20:1 (g / mL), heat to 70°C, and homogenize and stir for 22 minutes at a stirring rate of 600 rpm and a homogenization pressure of 500 MPa to obtain a gel mixed solvent;

[0039] S2, adding the extract of Gallwood to the gel mixed solvent, mixing, stirring evenly at 30° C., stirring at a rate of 250 rpm, stirring for 15 min, to obtain an extract gel mixed solvent;

[0040] S3. Add the penetration enhancer, nanocarrier and oligopeptide into the extract gel mixed solvent, and then stir and mix evenly under γ-rays, with a radiation dose of 3.2 kGy, irradiation for 30 min, and a stirring rate of 250 rpm to obtain the gallwood extract gel.

[0041] Example 4

[0042] A gallwood extract gel, comprising the following raw materials in parts by weight: 3.8 parts of gallwood extract, 28.4 parts of aqueous gel matrix, 3.5 parts of penetration enhancer, 3.7 parts of nanocarrier, and 1.5 parts of oligopeptide; the aqueous gel matrix is ​​poloxamer, polyvinyl pyrrolidone, and cellulose derivatives in a mass ratio of 4.2:2.5:7.1; the cellulose derivative is methylcellulose; the penetration enhancer is α-tocopheryl polyethylene glycol succinate, ergosterol, and cocamidopropyl betaine in a mass ratio of 3.2:6.2:4.8; the nanocarrier is magnetic nanoparticles, and the magnetic nanoparticles are citric acid-modified Prussian blue nanoparticles; the oligopeptide is oyster oligopeptide;

[0043] The gallwood extract gel is prepared by the following method:

[0044] (1) Preparation of Gallwood Extract: Take the wood part of Gallwood, dry it, grind it into 80 mesh sieve, extract it twice with 70% n-butanol by volume, the extraction temperature is 75°C, the extraction time is 30 min each time, the mass volume ratio of Gallwood and n-butanol is 1:5 g / mL, combine the extracts, and reserve the residues for later use. Then concentrate the extracts to obtain n-butanol extract with a relative density of 1.1 at 50°C;

[0045] Take the above-mentioned medicinal residue and add water, the mass volume ratio of the medicinal residue to water is 10:50 g / mL, decoct for 1 hour, filter, take the filtrate, concentrate, and obtain a water extract with a relative density of 1.1 at 50°C;

[0046] The n-butanol extract and the water extract are heated to 50° C., mixed and stirred evenly to obtain a gallwood extract;

[0047] (2) Preparation of Gallwood Extract Gel:

[0048] S1. Mix the above aqueous gel matrix with water at a mass volume ratio of 10:1 (g / mL), heat to 65°C, and homogenize and stir for 15 minutes at a stirring rate of 400 rpm and a homogenization pressure of 400 MPa to obtain a gel mixed solvent;

[0049] S2, adding the gallwood extract to the gel mixed solvent, mixing, stirring evenly at 20° C., stirring at a rate of 200 rpm, stirring for 10 min, to obtain an extract gel mixed solvent;

[0050] S3. Add the penetration enhancer, nanocarrier and oligopeptide into the extract gel mixed solvent, and then stir and mix them evenly under γ-rays. The radiation dose is 0.5 kGy, the irradiation time is 20 min, and the stirring rate is 200 rpm to obtain the gallwood extract gel.

[0051] Example 5

[0052] A gallwood extract gel, comprising the following raw materials in parts by weight: 3.8 parts of gallwood extract, 28.4 parts of aqueous gel matrix, 3.5 parts of penetration enhancer, 3.7 parts of nanocarrier, and 1.5 parts of oligopeptide; the aqueous gel matrix is ​​poloxamer, polyvinyl pyrrolidone, and cellulose derivatives in a mass ratio of 4.2:2.5:7.1; the cellulose derivative is methylcellulose; the penetration enhancer is α-tocopheryl polyethylene glycol succinate, ergosterol, and cocamidopropyl betaine in a mass ratio of 3.2:6.2:4.8; the nanocarrier is magnetic nanoparticles, and the magnetic nanoparticles are citric acid-modified Prussian blue nanoparticles; the oligopeptide is oyster oligopeptide;

[0053] The gallwood extract gel is prepared by the following method:

[0054] (1) Preparation of Gallwood Extract: The woody part of Gallwood was taken, dried, and crushed to a 120-mesh sieve, and extracted four times with 95% by volume n-butanol at an extraction temperature of 85°C, each extraction time of 60 min, and the mass volume ratio of Gallwood to n-butanol was 1:8 g / mL. The extracts were combined and the residues were reserved. The extracts were then concentrated to a relative density of 1.2 at 50°C to obtain n-butanol extract;

[0055] Take the above-mentioned medicinal residue and add water, the mass volume ratio of the medicinal residue to water is 25:50 g / mL, decoct for 3 hours, filter, take the filtrate, concentrate, and obtain a water extract with a relative density of 1.2 at 50°C;

[0056] The n-butanol extract and the water extract are heated to 80° C., mixed and stirred evenly to obtain a gallwood extract;

[0057] (2) Preparation of Gallwood Extract Gel:

[0058] S1. Mix the above aqueous gel matrix with water at a mass volume ratio of 30:1 (g / mL), heat to 80°C, and homogenize and stir for 30 minutes at a stirring rate of 800 rpm and a homogenization pressure of 600 MPa to obtain a gel mixed solvent;

[0059] S2, adding the gallwood extract to the gel mixed solvent, stirring evenly at 40° C., at a stirring rate of 300 rpm, and stirring for 20 min to obtain an extract gel mixed solvent;

[0060] S3. Add the penetration enhancer, nanocarrier and oligopeptide into the mixed solvent of extract gel, and then stir and mix them evenly under γ-rays. The radiation dose is 5 kGy, the irradiation time is 40 min, and the stirring rate is 300 rpm to obtain the gallwood extract gel.

[0061] The permeability of the gallwood extract gel prepared in Examples 1-5 was measured, and the specific test method was as follows:

[0062] In vitro skin permeation experiment:

[0063] 1. Preparation of ex vivo mouse skin: Select several male mice weighing 25g, remove the hair, kill the mice, peel off the abdominal skin, remove the stratum corneum, subcutaneous tissue and fat, wash with saline, dry with filter paper, cut into uniform-sized skin membranes, place in sterile saline to ensure the integrity of the skin membranes, divide the skin pieces into 5 groups, and test three groups in each group. There is no interaction between the skin membranes and the drugs.

[0064] 2. Test methods:

[0065] The mouse skin membrane was fixed between the drug administration pool and the receiving pool using a Franz diffusion apparatus. The effective permeability area of ​​the diffusion pool was 2.80 cm 2 , the stratum corneum faces the supply chamber, the dermis faces the receiving chamber, 1 g of the gallwood extract gel sample of Examples 1-5 of the present invention is weighed, placed in the dosing pool, and evenly applied on the ex vivo mouse skin of the same size, kept at a constant temperature of (37±0.5)°C, and stirred continuously at 300rpm by electromagnetic constant speed, and 2.0 mL of receiving solution is taken after 2, 4, 8, 12, 24, and 36 hours, respectively, and the same temperature and equal volume of receiving solution are supplemented at the same time, the receiving solution is centrifuged, the supernatant is filtered through a microporous filter membrane, the absorbance of the filtrate is determined according to the given chromatographic conditions, and the cumulative permeation per unit area Q is calculated according to the following formula;

[0066]

[0067] Among them, C n is the drug concentration measured at the nth sampling point; V is the volume of the receiving pool; S is the effective diffusion area.

[0068] Cumulative permeability per unit area K = [Q / m] × 100%; m is the amount of active ingredients of Gallwood extract in 1g of gel;

[0069] 3. Results

[0070]

[0071]

[0072] It can be seen from the above results that the extract gel prepared by the present invention has a good permeability. The present invention adopts a combination of various raw materials to synergistically exert their characteristics. Under the interaction between the stratum corneum and lipids of the skin, the diffusion resistance of the drug in the stratum corneum can be reduced, the fluidity can be enhanced, the onset time of the drug can be shortened, and a rapid effect can be achieved. At 36 hours, the permeability of each embodiment is between 90.5% and 96.2%, among which Example 3 reaches the highest 96.2%.

[0073] For the permeability results of Example 3, the following comparative test was set up:

[0074] Comparative Example 1

[0075] The difference between this comparative example and Example 3 is that the gallwood extract gel comprises the following raw materials in parts by weight: 8.9 parts of gallwood extract, 10.3 parts of aqueous gel matrix, 1.0 part of penetration enhancer, 5.2 parts of nanocarrier, and 3.3 parts of oligopeptide.

[0076] Comparative Example 2

[0077] The difference between this comparative example and Example 3 is that the raw material of the gallwood extract gel does not contain a penetration enhancer, and the other ingredients are the same, specifically comprising the following raw materials in parts by weight: 3.8 parts of gallwood extract, 28.4 parts of aqueous gel matrix, 3.7 parts of nanocarriers, and 1.5 parts of oligopeptides; the aqueous gel matrix is ​​poloxamer, polyvinyl pyrrolidone, and cellulose derivatives in a mass ratio of 4.2:2.5:7.1; the cellulose derivative is methylcellulose; the nanocarrier is magnetic nanoparticles, and the magnetic nanoparticles are citric acid-modified Prussian blue nanoparticles; the oligopeptide is oyster oligopeptide;

[0078] The following preparation method was used:

[0079] (1) Preparation of Gallwood Extract: The woody part of Gallwood was taken, dried, crushed with a 100-mesh sieve, extracted three times with 85% by volume n-butanol, the extraction temperature was 80°C, the extraction time was 40 min each time, the mass volume ratio of Gallwood to n-butanol was 1:7 g / mL, the extracts were combined, the residue was set aside, and the extract was concentrated to a relative density of 1.2 at 50°C to obtain n-butanol extract;

[0080] Take the above-mentioned medicinal residue and add water, the mass volume ratio of the medicinal residue to water is 18:50 g / mL, decoct for 2 hours, filter, take the filtrate, concentrate, and obtain a water extract with a relative density of 1.1 at 50°C;

[0081] The n-butanol extract and the water extract are heated to 70° C., mixed and stirred evenly to obtain a gallwood extract;

[0082] (2) Preparation of Gallwood Extract Gel:

[0083] S1. Mix the above aqueous gel matrix with water at a mass volume ratio of 20:1 (g / mL), heat to 70°C, and homogenize and stir for 22 minutes at a stirring rate of 600 rpm and a homogenization pressure of 500 MPa to obtain a gel mixed solvent;

[0084] S2, adding the extract of Gallwood to the gel mixed solvent, mixing, stirring evenly at 30° C., stirring at a rate of 250 rpm, stirring for 15 min, to obtain an extract gel mixed solvent;

[0085] S3. Add the nanocarrier and oligopeptide into the mixed solvent of the extract gel, and then stir and mix them evenly under γ-rays. The radiation dose is 3.2 kGy, the irradiation time is 30 min, and the stirring rate is 250 rpm to obtain the gallwood extract gel.

[0086] Comparative Example 3

[0087] The difference between this comparative example and Example 3 is that the raw material of the gallwood extract gel does not contain nanocarriers, and specifically includes the following raw materials in parts by weight: 3.8 parts of gallwood extract, 28.4 parts of aqueous gel matrix, 3.5 parts of penetration enhancer, and 1.5 parts of oligopeptide; the aqueous gel matrix is ​​poloxamer, polyvinyl pyrrolidone, and cellulose derivatives in a mass ratio of 4.2:2.5:7.1; the cellulose derivative is methylcellulose; the penetration enhancer is α-tocopherol polyethylene glycol succinate, ergosterol, and cocamidopropyl betaine in a mass ratio of 3.2:6.2:4.8; the oligopeptide is oyster oligopeptide;

[0088] The following preparation method was used:

[0089] (1) Preparation of Gallwood Extract: The woody part of Gallwood was taken, dried, crushed with a 100-mesh sieve, extracted three times with 85% by volume n-butanol, the extraction temperature was 80°C, the extraction time was 40 min each time, the mass volume ratio of Gallwood to n-butanol was 1:7 g / mL, the extracts were combined, the residue was set aside, and the extract was concentrated to a relative density of 1.2 at 50°C to obtain n-butanol extract;

[0090] Take the above-mentioned medicinal residue and add water, the mass volume ratio of the medicinal residue to water is 18:50 g / mL, decoct for 2 hours, filter, take the filtrate, concentrate, and obtain a water extract with a relative density of 1.1 at 50°C;

[0091] The n-butanol extract and the water extract are heated to 70° C., mixed and stirred evenly to obtain a gallwood extract;

[0092] (2) Preparation of Gallwood Extract Gel:

[0093] S1. Mix the above aqueous gel matrix with water at a mass volume ratio of 20:1 (g / mL), heat to 70°C, and homogenize and stir for 22 minutes at a stirring rate of 600 rpm and a homogenization pressure of 500 MPa to obtain a gel mixed solvent;

[0094] S2, adding the extract of Gallwood to the gel mixed solvent, mixing, stirring evenly at 30° C., stirring at a rate of 250 rpm, stirring for 15 min, to obtain an extract gel mixed solvent;

[0095] S3. Add the penetration enhancer and oligopeptide into the mixed solvent of the extract gel, and then stir and mix evenly under γ-rays. The radiation dose is 3.2 kGy, the irradiation time is 30 min, and the stirring rate is 250 rpm to obtain the gallwood extract gel.

[0096] Comparative Example 4

[0097] The difference between this comparative example and Example 3 is that the preparation process of the gallwood extract gel is not irradiated with gamma rays. Specifically, the preparation of the gallwood extract gel comprises the following steps:

[0098] S1. Mix the above aqueous gel matrix with water at a mass volume ratio of 20:1 (g / mL), heat to 70°C, and homogenize and stir for 22 minutes at a stirring rate of 600 rpm and a homogenization pressure of 500 MPa to obtain a gel mixed solvent;

[0099] S2, adding the extract of Gallwood to the gel mixed solvent, mixing, stirring evenly at 30° C., stirring at a rate of 250 rpm, stirring for 15 min, to obtain an extract gel mixed solvent;

[0100] S3. Add the penetration enhancer, nanocarrier and oligopeptide into the extract gel mixed solvent and stir for 30 minutes at a stirring rate of 250 rpm to obtain the gallwood extract gel.

[0101] Each comparative example was tested according to the above test method, and the test results are as follows:

[0102]

[0103]

[0104] Result analysis:

[0105] Compared with Comparative Example 1, the raw materials of the gallwood extract gel of the present invention are scientifically proportioned, and their main properties are synergistically exerted, and have good permeability, so that the active pharmaceutical ingredients in the gel are slowly released within 36 hours, achieving higher permeability;

[0106] Compared with Comparative Example 2, the addition of a permeation enhancer interacts with the components in the gel, reduces the solubility of the gel, makes it more permeable, helps the drug molecules diffuse in the gel, and increases the drug release rate; destroys the network structure or gelation state of the gel, makes it looser and more permeable, and helps the drug molecules penetrate and diffuse in the gel. Interacts with drug molecules, increases the solubility of the drug, and helps increase the drug release rate and bioavailability. Changes the viscosity and fluidity of the gel, reduces the viscosity of the gel, and makes it easier to diffuse;

[0107] Compared with comparative example 3, the use of nanomaterials as carriers can improve the stability of drugs, reduce the degradation and inactivation of drugs, effectively encapsulate and protect drug molecules, prevent them from being affected by environmental factors, extend the storage life of drugs, and increase the dispersibility and permeability of drugs in gels, thereby improving the absorption effect of drugs; compared with comparative example 4, gamma-ray radiation ionization chemical effect drugs and penetration enhancers, nanocarriers, oligopeptides, etc. are cross-linked during the stirring process to change the pore structure and permeability of the gel, increase the stability and mechanical strength of the gel, and improve its drug release characteristics, thereby achieving precise control of the drug release rate.

[0108] The above description is only a preferred embodiment of the present invention and is not intended to limit the present invention. Any modifications, equivalent substitutions, improvements, etc. made within the spirit and principle of the present invention should be included in the protection scope of the present invention.

Claims

1. A gelatinous extract of Gallwood, characterized in that: The gallwood extract gel is prepared from the following raw materials in parts by weight: 1.8-5.8 parts of gallwood extract, 12.9-39.8 parts of aqueous gel matrix, 1.6-5.9 parts of penetration enhancer, 2.1-3.9 parts of nanocarrier, and 1.2-1.9 parts of oligopeptide; the aqueous gel matrix is ​​poloxamer, polyvinyl pyrrolidone, and cellulose derivative in a mass ratio of (3.3-5.9):(1.2-3.9):(5.2-10.9); the cellulose The derivative is methylcellulose, the penetration enhancer is α-tocopherol polyethylene glycol succinate, ergosterol, and cocamidopropyl betaine in a mass ratio of (1.3-5.2):(4.9-9.7):(2.5-5.9); the nanocarrier is magnetic nanoparticles, and the magnetic nanoparticles are carboxylated ferroferric oxide nanoparticles or citric acid-modified Prussian blue nanoparticles; the oligopeptide is marine bone peptide, oyster oligopeptide or soybean oligopeptide; The preparation method of the gallwood extract gel comprises the following steps: (1) Preparation of Gallwood Extract: Take the woody part of Gallwood, dry it, grind it into 80-120 mesh, extract it 2-4 times with n-butanol with a volume fraction of 70-95%, the extraction temperature is 75-85°C, the extraction time is 30-60 min each time, the mass volume ratio of Gallwood and n-butanol is 1:5-8 g / mL, the extracts are combined, the residue is reserved, and the extract is concentrated to a relative density of 1.1-1.2 at 50°C to obtain n-butanol extract; Take the above-mentioned medicinal residue and add water, the mass volume ratio of the medicinal residue to water is 10-25:50 g / mL, decoct for 1-3 hours, filter, take the filtrate, concentrate, and obtain a water extract with a relative density of 1.1-1.2 at 50° C.; The n-butanol extract and the water extract are heated to 50-80° C., mixed and stirred evenly to obtain a gallwood extract; (2) Preparation of Gallwood Extract Gel: S1. Mix the above aqueous gel matrix with water at a mass volume ratio of 10-30:1 g / mL according to the ratio, heat to 65-80° C., homogenize and stir for 15-30 min, at a homogenization stirring rate of 400-800 rpm and a homogenization pressure of 400-600 MPa to obtain a gel mixed solvent; S2, add the gallwood extract to the gel mixed solvent, mix, stir evenly at 20-40° C., at a stirring rate of 200-300 rpm, and stir for 10-20 min to obtain the extract gel mixed solvent; S3. Add the penetration enhancer, nanocarrier and oligopeptide into the mixed solvent of extract gel, and then stir and mix them evenly under γ-ray, with a γ-ray radiation dose of 0.5-5 kGy, irradiation for 20-40 minutes, and a stirring rate of 200-300 rpm to obtain the gallwood extract gel.

2. A gallwood extract gel as claimed in claim 1, characterized in that: The gallwood extract gel is prepared from the following raw materials in parts by weight: 3.8 parts of gallwood extract, 28.4 parts of aqueous gel matrix, 3.5 parts of penetration enhancer, 3.7 parts of nanocarrier, and 1.5 parts of oligopeptide.

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