CN115969777A - Tetrahydropalmatine-rhizoma bletillae polysaccharide gel emulsion and preparation method thereof - Google Patents

Tetrahydropalmatine-rhizoma bletillae polysaccharide gel emulsion and preparation method thereof Download PDF

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CN115969777A
CN115969777A CN202310067982.5A CN202310067982A CN115969777A CN 115969777 A CN115969777 A CN 115969777A CN 202310067982 A CN202310067982 A CN 202310067982A CN 115969777 A CN115969777 A CN 115969777A
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tetrahydropalmatine
bletilla striata
gel emulsion
striata polysaccharide
polysaccharide gel
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赵鹏
张婷婷
刘思美
郭可
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Shaanxi University of Chinese Medicine
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Shaanxi University of Chinese Medicine
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Abstract

The invention belongs to the technical field of traditional Chinese medicine compounds, and discloses tetrahydropalmatine-bletilla striata polysaccharide gel emulsion and a preparation method thereof, wherein the preparation method comprises the following steps: grinding and mixing bletilla striata polysaccharide and konjac glucomannan together, and dissolving in a solvent to obtain a first mixed solution; centrifuging the first mixed solution to obtain a supernatant; uniformly mixing glycerol, triethanolamine and the supernatant, and preserving heat in a water bath to obtain a water phase; uniformly mixing tetrahydropalmatine, lavender essential oil and molten stearic acid to obtain an oil phase; and uniformly mixing the oil phase into the water phase, and homogenizing and emulsifying to obtain the O/W-type tetrahydropalmatine-bletilla striata polysaccharide gel emulsion. In conclusion, the tetrahydropalmatine-bletilla striata polysaccharide gel emulsion prepared by the invention has good physical properties and good transdermal absorption rate, and has analgesic effect and good wound repair effect compared with other similar products. In addition, the preparation method has simple steps and low cost.

Description

Tetrahydropalmatine-rhizoma bletillae polysaccharide gel emulsion and preparation method thereof
Technical Field
The invention belongs to the technical field of traditional Chinese medicine compounds, and particularly relates to tetrahydropalmatine-bletilla striata polysaccharide gel emulsion and a preparation method thereof.
Background
Corydalis yanhusuo, also known as corydalis yanhusuo and corydalis yanhusuo, is one of dried tubers of corydalis yanhusuo of papaveraceae, belongs to Zhe eight flavors, has the effects of promoting blood circulation, promoting qi circulation, relieving pain and the like, and can be used for various pains caused by blood stasis and qi stagnation. Modern pharmacological research shows that the corydalis tuber mainly contains alkaloids, steroids, organic acids and other chemical components, and relates to pharmacological effects of analgesia, myocardial ischemia resistance, cerebral ischemia resistance, tumor resistance, diabetes resistance and the like. And proved that the corydalis tuber has remarkable clinical analgesic effect, wherein the tetrahydropalmatine which is one of the effective components of the corydalis tuber has the strongest analgesic effect. At present, tetrahydropalmatine administration modes mainly comprise oral administration and intramuscular injection, wherein the oral administration has certain stimulation effect on gastrointestinal tracts and has liver first-pass effect, and the intramuscular injection administration also has allergy, so that the clinical application of the tetrahydropalmatine is severely limited.
Transdermal drug delivery is a mode that drug components reach tissues in a body through a skin barrier, and compared with traditional oral drug delivery and subcutaneous injection, the transdermal drug delivery can maintain constant drug concentration in the body to the maximum extent, is safe and simple to use, and can avoid pain, adverse reaction and the like caused by intramuscular injection.
The bletilla polysaccharide is also called as bletilla gum, and the bletilla mannan is a water-soluble high-molecular viscous polysaccharide extracted from traditional Chinese medicine bletilla, can form a viscous gel after being dissolved in water, has good biological adhesiveness, and is safe and nontoxic. In addition, the compound has pharmacological activities of ulcer resistance, inflammation resistance, procoagulant blood coagulation, oxidation resistance and the like, can be used as carrier materials of various external preparations, has higher commercial utilization value and research value, is widely applied to the fields of medicine raw materials, pharmaceutic adjuvants, biomedical materials and the like, and has good application prospect.
In conclusion, the invention provides the externally applied gel emulsion taking the bletilla polysaccharide and the tetrahydropalmatine as raw materials.
Disclosure of Invention
In view of the above, in order to solve the problems in the background art, the present invention aims to provide tetrahydropalmatine-bletilla striata polysaccharide gelata and a preparation method thereof.
In order to achieve the purpose, the invention provides the following technical scheme:
a method for preparing tetrahydropalmatine-bletilla striata polysaccharide gelata comprises the following steps:
grinding and mixing bletilla striata polysaccharide and konjac glucomannan together, and dissolving in a solvent to obtain a first mixed solution;
centrifuging the first mixed solution to obtain a supernatant;
uniformly mixing glycerol, triethanolamine and the supernatant, and preserving heat in a water bath to obtain a water phase;
uniformly mixing tetrahydropalmatine, lavender essential oil and molten stearic acid to obtain an oil phase;
and uniformly mixing the oil phase into the water phase, and homogenizing and emulsifying to obtain the O/W-type tetrahydropalmatine-bletilla striata polysaccharide gel emulsion.
Preferably, the following components:
the mixing mass ratio of the bletilla polysaccharide to the konjac glucomannan is 40-60: 1.
the triethanolamine accounts for 0.4-1.2% of the total mass of the tetrahydropalmatine-bletilla striata polysaccharide gel milk.
The stearic acid accounts for 1-3% of the total mass of the tetrahydropalmatine-rhizoma bletillae polysaccharide gel emulsion.
The solvent is hot purified water.
The centrifugal speed of the centrifugal treatment is 3000r/min, and the centrifugal time is 5min.
The temperature of the water bath heat preservation is 70 ℃.
The homogenizing and emulsifying comprises high-speed homogenizing and high-pressure homogenizing. Specifically, the high-speed homogenizing cycle is executed for 3 times, the homogenizing time is 1min each time, and the rotating speed of the high-speed homogenizing is 9000r/min; the high-pressure homogenization cycle is performed 15 times, and the pressure of the high-pressure homogenization is 1000bar.
The invention also provides tetrahydropalmatine-bletilla striata polysaccharide gel emulsion prepared by the preparation method.
Compared with the prior art, the invention has the following beneficial effects:
the tetrahydropalmatine-bletilla striata polysaccharide gel emulsion prepared by the invention has good physical properties and good transdermal absorption rate, has analgesic effect and good wound repair effect compared with other similar products, and can provide new technical means and application reference for further developing and utilizing tetrahydropalmatine. In addition, the preparation method has the advantages of simple steps, low cost and wide application prospect, and can be effectively suitable for industrial mass production.
Drawings
FIG. 1 is a liquid chromatogram of tetrahydropalmatine; ( a reference solution of tetrahydropalmatine standard; b sample solution of tetrahydropalmatine-bletilla striata polysaccharide gelata prepared by the invention )
FIG. 2-FIG. 3 are graphs showing particle size and PDI values of tetrahydropalmatine-bletilla striata polysaccharide gel emulsion prepared by the present invention;
FIG. 4 is a transmission electron microscope image of tetrahydropalmatine-bletilla striata polysaccharide gel emulsion prepared by the present invention;
FIG. 5 is a comparison of water loss test results;
FIG. 6 is a graph comparing the results of in vitro transdermal absorption experiments.
Detailed Description
The technical solutions in the embodiments of the present invention will be clearly and completely described below with reference to the drawings in the embodiments of the present invention, and it is obvious that the described embodiments are only a part of the embodiments of the present invention, and not all of the embodiments. All other embodiments, which can be obtained by a person skilled in the art without making any creative effort based on the embodiments in the present invention, belong to the protection scope of the present invention.
The invention provides a preparation method of tetrahydropalmatine-bletilla striata polysaccharide gel emulsion, which comprises the following steps:
preparing an aqueous phase: grinding and mixing bletilla striata polysaccharide and konjac glucomannan together, and dissolving in hot purified water to obtain a first mixed solution; centrifuging the first mixed solution at a rotating speed of 3000r/min for 5min, and taking supernatant; mixing glycerol, triethanolamine and the supernatant, and keeping temperature in 70 deg.C water bath to obtain water phase.
Preparing an oil phase: heating stearic acid in 70 deg.C water bath until completely melted, and mixing tetrahydropalmatine, lavender essential oil and melted stearic acid to obtain oil phase.
Slowly adding the oil phase into the water phase, stirring and mixing while adding, uniformly mixing, and sequentially homogenizing and circulating for 3 times by a high-speed emulsification homogenizer at 9000r/min, wherein the homogenizing time is 1min each time, and homogenizing and circulating for 15 times by a high-pressure homogenizer at 1000bar to finally obtain the O/W type tetrahydropalmatine-bletilla striata polysaccharide gel emulsion.
Based on the above preparation method, the following specific examples are provided
Preparing materials:
tetrahydropalmatine (Shanghai Ji to Biochemical technology, inc., purity 98%); bletilla striata polysaccharide (purity 98.22%); konjac gum (shanghai source leaf biotechnology limited); triethanolamine (Shijiazhuanhaisen chemical Co., ltd.); glycerol (Zhejiang tunnel Changhukang pharmaceutical Co., ltd.); stearic acid (chemic chemical reagent ltd, camou, department, of tianjin); and (5) purifying the water.
High performance liquid chromatography (Waters-2695, waters corporation, USA); an evaporative light detector (Waters-2996, waters corporation, USA) was configured; a Malvern laser particle sizer (ZEN-3600 Malvern Zeta-master, malvern, UK); low speed desk centrifuge (TDZ 5-WS, hunan instruments laboratory Instrument development Co., ltd.); DF-101S heat collection type constant temperature heating magnetic stirrer (Henan Zhihua instrument Co., ltd.); high speed emulsification homogenizer (T18 DS25, IKA, germany); high pressure homogenizers (ATS, nanotechnology of antopis (suzhou)); transmission electron microscope (H-7650, hitachi, japan); electronic precision balances (FA 2004, shanghai national bridge balance factory); an intelligent transdermal tester (TP-6, technology of Sedrin Ind instruments Co., ltd.).
Example 1
The tetrahydropalmatine-bletilla striata polysaccharide gel emulsion is prepared according to the preparation method. In this embodiment, the triethanolamine accounts for 0.8% of the total mass of the tetrahydropalmatine-rhizoma bletillae polysaccharide gel emulsion, and the stearic acid accounts for 2% of the total mass of the tetrahydropalmatine-rhizoma bletillae polysaccharide gel emulsion.
In addition, the embodiment also provides the following embodiments of the ratio of the bletilla striata polysaccharide to the konjac glucomannan:
in embodiment 1-1, the ratio of the bletilla polysaccharide to the konjac glucomannan is 40:1;
in embodiment 1-2, the mixing mass ratio of the bletilla polysaccharide to the konjac glucomannan is 45:1;
in embodiments 1 to 3, the ratio of the bletilla polysaccharide to the konjac glucomannan is 50:1;
in embodiments 1 to 4, the mixing mass ratio of the bletilla polysaccharide to the konjac glucomannan is 55:1;
in embodiments 1 to 5, the mixing mass ratio of the bletilla polysaccharide to the konjac glucomannan is 60:1.
example 2
The tetrahydropalmatine-bletilla striata polysaccharide gel emulsion is prepared according to the preparation method. In this embodiment, the mixing mass ratio of the bletilla striata polysaccharide to the konjac glucomannan is 50:1, the stearic acid accounts for 2 percent of the total mass of the tetrahydropalmatine-bletilla striata polysaccharide gel emulsion.
In addition, the present embodiment also provides the following embodiments of the amount of triethanolamine:
in the embodiment 2-1, the triethanolamine accounts for 0.4 percent of the total mass of the tetrahydropalmatine-rhizoma bletillae polysaccharide gel emulsion;
in the embodiment 2-2, the triethanolamine accounts for 0.6% of the total weight of the tetrahydropalmatine-rhizoma bletillae polysaccharide gel emulsion;
in the embodiment 2-3, the triethanolamine accounts for 0.8% of the total weight of the tetrahydropalmatine-rhizoma bletillae polysaccharide gel emulsion;
in the embodiment 2-4, the triethanolamine accounts for 1.0% of the total weight of the tetrahydropalmatine-bletilla striata polysaccharide gel emulsion;
in embodiments 2-5, triethanolamine comprises 1.2% of the total weight of tetrahydropalmatine-bletilla striata polysaccharide gelata emulsion.
Example 3
The tetrahydropalmatine-bletilla striata polysaccharide gel emulsion is prepared according to the preparation method. In this embodiment, the mixing mass ratio of the bletilla polysaccharide to the konjac glucomannan is 50:1, the triethanolamine accounts for 0.8 percent of the total mass of the tetrahydropalmatine-bletilla striata polysaccharide gel emulsion.
In addition, the present example also provides the following embodiments of the amount of stearic acid:
in the embodiment 3-1, stearic acid accounts for 1.0 percent of the total mass of the tetrahydropalmatine-bletilla striata polysaccharide gel emulsion;
in the embodiment 3-2, stearic acid accounts for 1.5 percent of the total mass of the tetrahydropalmatine-rhizoma bletillae polysaccharide gel emulsion;
in the embodiment 3-3, stearic acid accounts for 2.0 percent of the total mass of the tetrahydropalmatine-rhizoma bletillae polysaccharide gel emulsion;
in the embodiment 3-4, stearic acid accounts for 2.5 percent of the total mass of the tetrahydropalmatine-rhizoma bletillae polysaccharide gel emulsion;
in embodiments 3 to 5, stearic acid accounts for 3.0% of the total weight of tetrahydropalmatine-bletilla striata polysaccharide gel emulsion.
To sum up
One) the content of tetrahydropalmatine in the tetrahydropalmatine-bletilla striata polysaccharide gel emulsion (for convenience of description, the following is referred to as gel emulsion) prepared in the three examples is determined:
the measurement conditions were as follows: hypersilGOLDC 18 Chromatography columns (4.6 mm. Times.250mm, 5 μm); methanol-0.1% phosphoric acid solution (pH adjusted to 6.0 using triethylamine) (55; the flow rate is 1.0mL/min; the detection wavelength is 280nm; the column temperature was 25 ℃. The sample amount is 10 μ L, and the number of theoretical plates is not less than 3000 calculated according to tetrahydropalmatine peak.
Preparation of a control solution: precisely weighing 4mg of tetrahydropalmatine standard, placing in a 100mL volumetric flask, adding methanol to dissolve and dilute to scale, and shaking up to obtain a reference solution containing 0.04mg per 1 mL.
Sample solution preparation: precisely sucking 0.5mL of the gel emulsion, dissolving with water, diluting to a constant volume of 25mL, shaking, filtering with 0.45 μm microporous membrane, discarding the primary filtrate, and collecting the secondary filtrate as sample solution.
Preparation of a standard curve: precisely sucking 0.5mL, 1.0mL, 2.0 mL, 3.0 mL, 4.0 mL, 5.0 mL and 6.0mL of the reference substance solution, respectively placing in a 10mL measuring flask, diluting with methanol to scale to obtain a series of reference substance solutions, wherein the concentrations are as follows: 2. 4, 8, 12, 16, 20, 24, 40. Mu.g/mL. Each 10. Mu.L of the above control solutions was precisely aspirated, and the resulting solution was injected into a liquid chromatograph to measure the peak area. Specifically, referring to fig. 1a, a linear regression is performed with the chromatographic peak area a and the concentration of the reference substance, resulting in a standard linear equation Y =11994x +12404, the correlation coefficient r =0.9999, and tetrahydropalmatine is well linear in the concentration range of 2-100 μ g/mL.
And (3) measuring the content of the sample: precisely sucking 10 mu L of sample solution, injecting the sample solution into a liquid chromatograph, measuring the peak area, calculating the content of tetrahydropalmatine based on a standard linear equation, measuring 3 parts, and taking an average value.
Secondly), observing the appearance by adopting a visual observation method and a transmission electron microscope method. The particle size and PDI value of the particle are measured by a Malvern laser particle sizer. The physical stability of the product is examined by a high-speed centrifugation method and a storage method at different temperatures. And inspecting the moisture retention performance by adopting a water loss rate test. The skin spreadability was examined using the spreading test.
(1) Particle diameter and PDI value
Particle size and polydispersity index (PDI) of the gel milk were measured using a Malvern particle size detector: a1 mL sample of the gelled milk was aspirated, placed in a beaker, and the sample diluted with 50mL of purified water and shaken well (to avoid multiple scattering effects). Adding a proper amount of diluted sample into a sample pool of a Malvern particle size detector, measuring the particle size and PDI value of the gel milk sample at 25 ℃, measuring in parallel for 3 times, and taking an average value.
Regarding example 1, the particle size and PDI detection results of the gel milk prepared in each embodiment thereof are shown in fig. 2A. It can be seen from the figure that under the condition of other fixed conditions, the particle size and the PDI value of the gel emulsion show the trend of decreasing first and then increasing along with the increase of the adding amount ratio of the bletilla polysaccharide to the konjac gum. The reasons are that: when the konjac gum content is increased, the viscosity of the solution is increased, the emulsification effect is influenced, and the particle size and PDI value of the gel emulsion are higher; when the amount of the bletilla polysaccharide is increased, the addition amount of the konjac glucomannan is correspondingly reduced, the oil-water interfacial tension is reduced, and the particle size and PDI value of the gel emulsion are reduced; the ratio of the two components is further increased, the viscosity is increased, the particle size is also increased, and the PDI value tends to be increased. In summary, m (bletilla striata polysaccharides): m (konjac glucomannan) =50:1.
regarding example 2, the particle size and PDI detection results of the gel milk prepared in each embodiment thereof are shown in fig. 2B. It can be seen from the figure that under other conditions, the particle size and PDI value of the gel emulsion both tend to decrease and then increase with the increase of the amount of triethanolamine used. The reason is that: when the dosage of the triethanolamine is 0.4%, the emulsification effect is poor, the stability of the gel emulsion is influenced, and the particle size and the PDI value of the gel emulsion are high; when the dosage is continuously increased to 1.2%, the viscosity of the solution is increased, and the particle size and the PDI value are influenced. In conclusion, the preferable content of triethanolamine is 0.8% of the total weight of tetrahydropalmatine-rhizoma bletillae polysaccharide gel emulsion.
Regarding example 3, the particle size and PDI detection results of the gel milk prepared in each embodiment thereof are shown in fig. 2C. As can be seen from the figure, under otherwise constant conditions, the particle size and PDI value of the gel emulsion both tend to decrease and then increase as the amount of stearic acid used increases. The reasons are that: when the consumption of stearic acid is small, the proportion of the water phase is large, the emulsification effect is poor, and the particle size and the PDI value of the gel emulsion are increased; and the excessive consumption reduces the uniformity of the gel emulsion, has the tendency of oil-water stratification and influences the particle size and PDI value of the gel emulsion. In conclusion, stearic acid is preferably 2.0% of the total mass of tetrahydropalmatine-bletilla striata polysaccharide gel milk.
To summarize, at m (bletilla striata polysaccharide): m (konjac glucomannan) =50:1. in the preferable mixture ratio of 0.8% triethanolamine and 2.0% stearic acid, as can be seen from FIG. 3, the average particle size of the gel emulsion is about 1.56 μm, the distribution is uniform, and the PDI value is 0.434. In addition, as can be seen from fig. 1b, the content of tetrahydropalmatine in the gel milk is preferably 0.079% at the preferred ratio.
The following detailed description will be made with reference to the above preferred mixture ratio
(2) Appearance form
Based on visual observation, the gel emulsion prepared according to the preferable proportion is milky white, has certain viscosity and fluidity, is fine and uniform, and has glittering and translucent luster.
Based on a transmission electron microscope: taking a proper amount of gel emulsion sample, dropwise adding the gel emulsion sample onto a copper net of a carbon film, standing for 5min, sucking away excessive samples, cleaning with purified water for 3 times, then dropwise adding 2.0% phosphotungstic acid solution for negative dyeing for 5min, sucking away excessive dye solution with filter paper, naturally airing, and then placing under a Transmission Electron Microscope (TEM) to observe the particle morphology and the particle size of the gel emulsion. As can be seen from FIG. 4, most of the tetrahydropalmatine particles were spherical and uniform in size, and were free from aggregation, and had a particle size of about 2 μm.
(3) Physical stability
Taking a proper amount of gel emulsion sample, centrifuging at 5000r/min for 15min, and no oil-water separation.
Taking 4 equal gel milk samples, storing at 4 deg.C, 25 deg.C, 40 deg.C, 60 deg.C for 10 days, respectively, sampling at 3 days, 5 days, and 10 days for observation. The gel milk sample has no delamination during the storage at the temperature of 4 ℃,25 ℃ and 40 ℃, and the particle size distribution has no obvious change; oil-water separation tendency can be seen in 10 days at 40 ℃. Therefore, the gel milk sample has better physical stability at normal temperature.
(4) Moisture retention (Water loss rate experiment)
Two 0.22 μm microporous filter membranes were placed on a water-impermeable double-silicon paper and marked as No. 1 and No. 2 at a temperature of 25 ℃ and a humidity of 40%. Uniformly coating a proper amount of gel emulsion sample on the No. 2 filter membrane, then dripping 5 drops of purified water on the No. 1 filter membrane and the No. 2 filter membrane, weighing, and then respectively measuring the water loss rate of the two filter membranes at 5min, 15min, 30 min, 60 min and 120 min. As can be seen from FIG. 5, the water loss rate of the No. 2 filter membrane is obviously lower than that of the No. 1 filter membrane, so that the gel emulsion prepared by the invention has a good moisturizing effect, can improve the skin elasticity and promote the skin hydration, thereby increasing the transdermal permeability of active ingredients and enhancing the pharmacological action.
(5) Spreading property of skin
A proper amount of the gel emulsion sample is taken and coated on double-silicon paper (with hydrophobicity similar to that of skin) for observation, and the gel emulsion sample is uniformly coated without aggregation phenomenon. Based on the results, the gel emulsion prepared by the invention has good skin spreadability, and tetrahydropalmatine is dispersed in the water-soluble polymer material in the form of particles, is beneficial to full contact absorption with skin, and has the advantages of moistening, easy coating, fragrant smell, no greasy feeling and the like.
Third) transdermal absorption experiment of gel emulsion (taking gel emulsion in optimal proportion as an example)
Preparation of in vitro skin: cleaning SD rat (weight 190 + -20 g, male), removing neck, removing hair, removing sternum and abdomen hair, cutting off appropriate size of abdomen skin, removing subcutaneous tissue and fat (ensuring no damage to skin cuticle during removal), washing with normal saline, wrapping clean and intact skin with aluminum foil paper, and freezing at-20 deg.C for one week.
Preparing a transdermal receiving solution: 0.9% normal saline and ethanol were mixed according to 80:20 to obtain the receiving liquid for the in-vitro transdermal absorption experiment.
In vitro skin permeability study:
in vitro skin permeability of the gel milk was examined by Franz diffusion cell method (effective permeation area 0.785 cm) 2 The receiving chamber volume was 15 mL).
Thawing rat in vitro skin at room temperature, washing with normal saline, cutting to appropriate size, fixing between the supply chamber and the receiving chamber of the transdermal absorption device, keeping skin flat with stratum corneum facing the supply chamber, adding receiving liquid into the receiving chamber, and exhausting bubbles to make skin and receiving liquid in close contact.
The water bath temperature (37 +/-0.5) DEG C, the magnetic stirring speed of 350r/min and the balance of 20min.
Precisely measuring 0.5mL of gel emulsion, preparing tetrahydropalmatine solution with the same concentration as a blank control, loading under the same condition, sampling 0.5mL of receiving solution at 0.5, 1, 2, 4, 6, 8, 10, 12 and 24h, supplementing fresh receiving solution with the same volume, and removing bubbles. And filtering the receiving solution taken out at corresponding time through a 0.22 mu m microporous filter membrane to obtain an experimental sample solution.
Measuring the content of tetrahydropalmatine in the experimental sample solution (chromatographic method), calculating the mass concentration of the medicine at the corresponding time, and calculating the cumulative permeation amount of the tetrahydropalmatine at the corresponding time according to the following formula:
Figure BDA0004063430490000091
in the formula, Q n Cumulative penetration (. Mu.g/cm) per unit area at the nth time point 2 ) V is the volume of receiving fluid (mL), 0.5 is the sample volume (mL), and S is the effective skin penetration area (cm) 2 ),C n The mass concentration of the drug in the receiving cell (μ g/mL), C, for the nth time point i Is the drug mass concentration (. Mu.g/mL) at a time point prior to the nth time point.
The cumulative penetration Q of tetrahydropalmatine in the gel at different time points n Plotted as the ordinate and the sample time t as the abscissa, is the cumulative permeation-time curve shown in fig. 6. As can be seen from FIG. 6, the cumulative permeation rate increased with time, and the 24h cumulative permeation rate of tetrahydropalmatine in the blank control group was 198.79. Mu.g/cm 2 While the 24h cumulative penetration of tetrahydropalmatine in the gel milk reaches 910.22 mu g/cm 2 Therefore, the tetrahydropalmatine-bletilla striata polysaccharide gel emulsion prepared by the invention can be used for improving the in-vitro transdermal absorption effect of the tetrahydropalmatine to a great extent.
In summary, the tetrahydropalmatine-rhizoma bletillae polysaccharide gel emulsion is prepared by combining a new soap method and a high-pressure homogeneous emulsification method, and m (rhizoma bletillae polysaccharide) in all raw materials is preferably selected: m (konjac gum) =50:1. 0.8% of triethanolamine and 2.0% of stearic acid. Based on the optimal proportion, the obtained tetrahydropalmatine-bletilla striata polysaccharide gel emulsion has the average particle size of about 1.56 mu m, the PDI of 0.434, uniform, fine and smooth appearance, glittering and translucent luster, better viscosity and fluidity, easy coating, good moisture retention, good physical stability and good in-vitro transdermal absorption effect, thereby providing a new technical means for the application of tetrahydropalmatine and having wide application prospect.
Although embodiments of the present invention have been shown and described, it will be appreciated by those skilled in the art that changes, modifications, substitutions and alterations can be made in these embodiments without departing from the principles and spirit of the invention, the scope of which is defined in the appended claims and their equivalents.

Claims (10)

1. A preparation method of tetrahydropalmatine-bletilla striata polysaccharide gel emulsion is characterized by comprising the following steps:
grinding and mixing bletilla striata polysaccharide and konjac glucomannan together, and dissolving in a solvent to obtain a first mixed solution;
centrifuging the first mixed solution to obtain a supernatant;
uniformly mixing glycerol, triethanolamine and the supernatant, and preserving heat in a water bath to obtain a water phase;
uniformly mixing tetrahydropalmatine, lavender essential oil and molten stearic acid to obtain an oil phase;
and uniformly mixing the oil phase into the water phase, and homogenizing and emulsifying to obtain the O/W-type tetrahydropalmatine-bletilla striata polysaccharide gel emulsion.
2. The method of claim 1, wherein: the mixing mass ratio of the bletilla striata polysaccharide to the konjac glucomannan is 40-60: 1.
3. the method of claim 1, wherein: the triethanolamine accounts for 0.4 to 1.2 percent of the total mass of the tetrahydropalmatine-bletilla striata polysaccharide gel milk.
4. The method of claim 1, wherein: the stearic acid accounts for 1-3% of the total mass of the tetrahydropalmatine-rhizoma bletillae polysaccharide gel emulsion.
5. The production method according to claim 1, characterized in that: the solvent is hot purified water.
6. The production method according to claim 1, characterized in that: the centrifugal speed of the centrifugal treatment is 3000r/min, and the centrifugal time is 5min.
7. The method of claim 1, wherein: the temperature of the water bath was maintained at 70 ℃.
8. The method of claim 1, wherein: the homogenizing and emulsifying comprises high-speed homogenizing and high-pressure homogenizing.
9. The method for producing according to claim 8, characterized in that: the high-speed homogenizing cycle is executed for 3 times, the homogenizing time is 1min each time, and the rotating speed of the high-speed homogenizing is 9000r/min; the high-pressure homogenization cycle is performed 15 times, and the pressure of the high-pressure homogenization is 1000bar.
10. Tetrahydropalmatine-bletilla striata polysaccharide gel emulsion, which is characterized by being prepared by the preparation method of any one of claims 1 to 9.
CN202310067982.5A 2023-01-30 2023-01-30 Tetrahydropalmatine-rhizoma bletillae polysaccharide gel emulsion and preparation method thereof Pending CN115969777A (en)

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