A traditional Chinese medicine external composition for treating hemorrhoids and a preparation method thereof

Abstract

The application discloses a traditional Chinese medicine external composition for treating hemorrhoids and a preparation method thereof, which is prepared from the following raw materials in parts by weight: 10-25 parts of carbonized white mulberry root, 8-20 parts of gallnut, 3-10 parts of dragon's blood, 1-5 parts of safflower, 5-15 parts of giant knotweed extract, 10-20 parts of pagoda tree fruit, 8-18 parts of Chinese cork tree, 5-15 parts of fried licorice, 5-12 parts of pearl powder, 6-16 parts of Chinese tallow, 20-50 parts of egg yolk oil, 15-40 parts of Chinese columbine oil and 2-8 parts of borneol. The traditional Chinese medicine external composition for treating hemorrhoids and the preparation method thereof have the advantages that hemostasis and blood circulation are combined, blood stasis is not caused by hemostasis, blood circulation is not caused by blood circulation, bleeding and pain can be rapidly relieved, heat clearing and toxin resolving (Chinese cork tree and giant knotweed) are combined with tissue repairing and sore closing, the penetration rate and bioavailability of fat-soluble and water-soluble effective components are greatly improved by using borneol as a penetration enhancer and using egg yolk oil- Chinese columbine oil compound oil as a base, the drug power can rapidly penetrate into deep hemorrhoid nuclei, and the target treatment is achieved.

Description

Technical Field

[0001] This invention relates to the field of traditional Chinese medicine technology, and in particular to a topical Chinese medicine composition for treating hemorrhoids and its preparation method. Background Technology

[0002] Currently, Western medicine external treatments for hemorrhoids often use ointments containing anesthetics such as lidocaine, hormones such as hydrocortisone, or astringents such as calamine. While these can temporarily relieve symptoms, they suffer from problems such as treating the symptoms but not the root cause, long-term use leading to side effects, and a high recurrence rate. Existing traditional Chinese medicine external formulas mainly focus on clearing heat and dampness, reducing swelling and relieving pain, but their comprehensive efficacy in rapidly stopping bleeding, promoting wound healing, and relieving acute pain is often insufficient. Furthermore, their formulations are often limited, and their permeability and user experience need improvement.

[0003] Therefore, it is necessary to provide a new topical Chinese medicine composition for treating hemorrhoids and its preparation method to solve the above-mentioned technical problems. Summary of the Invention

[0004] To address the aforementioned technical problems, this invention provides a compound topical preparation that integrates cooling the blood and stopping bleeding, promoting blood circulation and relieving pain, clearing heat and detoxifying, and astringing and promoting tissue regeneration. This composition places particular emphasis on the transdermal absorption and targeted action of the active ingredients, aiming to provide a topical treatment option that is fast-acting, long-lasting, comfortable to use, and easy to carry.

[0005] This invention provides a traditional Chinese medicine external application composition for treating hemorrhoids, made from the following raw materials in the indicated weight ratios: 10-25 parts of charred Sanguisorba officinalis, 8-20 parts of Gallnut, 3-10 parts of Dragon's Blood, 1-5 parts of Saffron, 5-15 parts of Polygonum cuspidatum extract, 10-20 parts of Sophora japonica fruit, 8-18 parts of Phellodendron chinense, 5-15 parts of prepared Glycyrrhiza uralensis, 5-12 parts of pearl powder, 6-16 parts of Orostachys chinensis, 20-50 parts of egg yolk oil, 15-40 parts of Lithospermum erythrorhizon oil, and 2-8 parts of borneol.

[0006] Preferably, it is made from the following raw materials in the indicated weight ratios: 12-20 parts of charred Sanguisorba officinalis, 10-15 parts of Gallnut, 4-8 parts of Dragon's Blood, 2-4 parts of Saffron, 8-12 parts of Polygonum cuspidatum extract, 12-18 parts of Sophora japonica fruit, 10-15 parts of Phellodendron chinense bark, 8-12 parts of prepared licorice root, 6-10 parts of pearl powder, 8-12 parts of Orostachys chinensis, 25-40 parts of egg yolk oil, 20-35 parts of Lithospermum erythrorhizon oil, and 3-6 parts of borneol.

[0007] Preferably, the egg yolk oil and comfrey oil together serve as the active ingredient and oil phase matrix.

[0008] Preferably, the composition is a topical preparation, and the dosage form of the topical preparation is selected from ointments, suppositories, creams, or sprays.

[0009] A method for preparing a traditional Chinese medicine external application composition includes the following steps: S1: Raw material pretreatment: S11: Prepare the charred Sanguisorba officinalis, Gallnut, Dragon's Blood and Pearl Powder into fine powders respectively; S12: Process saffron into a fine powder; S13: Mix Phellodendron bark, prepared licorice root, Sophora japonica fruit and Oryza sativa, extract with ethanol, and concentrate to obtain the first extract; S14: Extract the Polygonum cuspidatum to obtain a Polygonum cuspidatum extract; S2. Oil phase preparation: Mix egg yolk oil and comfrey oil, add borneol, and stir to dissolve the borneol to form an oil phase mixture; S3. Mixing: Add the fine powder obtained in steps S11 and S12 to the oil phase mixture in step S2 and perform homogenization to obtain a suspension base material; S4. Forming the paste: Add the first extract obtained in step S13 and the Polygonum cuspidatum extract obtained in step S14 to the suspension base material in step S3, grind and mix evenly, and then age to obtain the paste.

[0010] Preferably, in steps S11 and S12, the particle size of the fine powder passes through a 200-mesh sieve; in step S13, the concentration of the ethanol is 60%-80%, and the reflux extraction method is used; in step S14, the preparation method of the Polygonum cuspidatum extract includes: boiling Polygonum cuspidatum in water, concentrating the decoction, adding ethanol to precipitate, and taking the supernatant to recover the ethanol.

[0011] Preferably, in step S2, the mixing is carried out at 60-70°C; in step S4, the aging is carried out by standing for 24-48 hours under sealed and light-proof conditions.

[0012] Preferably, the formulation also includes a formulation forming step S5: mixing the original ointment obtained after aging in step S4 with topical formulation excipients to form topical formulations of different dosage forms.

[0013] Preferably, the dosage form is an ointment, suppository, cream, or spray; when preparing a suppository, the excipients include semi-synthetic fatty acid glycerides.

[0014] The application of a traditional Chinese medicine external application composition in the preparation of a drug for treating hemorrhoids, wherein the drug is an external preparation for treating bleeding, pain, swelling, prolapse or itching caused by hemorrhoids.

[0015] Compared with related technologies, the traditional Chinese medicine external application composition for treating hemorrhoids and its preparation method provided by the present invention have the following beneficial effects: 1. Multi-target synergistic treatment, addressing both symptoms and root cause: This formula combines hemostasis (Sanguisorba officinalis charcoal, Gallnut) with blood-activating properties (Saffron, Dragon's Blood), stopping bleeding without causing blood stasis and activating blood without causing excessive bleeding, thus quickly relieving bleeding and pain. The combination of heat-clearing and detoxifying properties (Phellodendron chinense, Polygonum cuspidatum) with tissue-regenerating and wound-healing properties (Pearl powder, Egg yolk oil) promotes tissue repair.

[0016] 2. Enhanced efficacy and rapid onset of action: With borneol as a penetration enhancer and egg yolk oil-complex oil as a base, the transdermal rate and bioavailability of fat-soluble and water-soluble active ingredients are greatly improved, enabling the medicine to quickly penetrate deep into the hemorrhoids and achieve "targeted treatment".

[0017] 3. Strong dosage form adaptability and excellent user experience: The provided preparation method can be flexibly converted into various external dosage forms such as ointment, suppository, and spray, adapting to different usage scenarios (such as home and travel) and disease stages (acute phase and remission phase). The preparation is mild and has little irritation to the perianal mucosa.

[0018] 4. Combining Inheritance and Innovation: Based on the hemostatic and tissue-regenerating medicine (Sanguisorba officinalis charcoal with Gallnut, egg yolk oil with pearl powder), modern extraction technology (refining Polygonum cuspidatum extract) and formulation technology are introduced to ensure the stability and improvement of efficacy.

[0019] 5. Natural ingredients and high safety: The main ingredients are natural animal and plant medicinal materials, which are properly processed and formulated. They are highly safe for topical application, avoiding the gastrointestinal reactions that may be caused by oral medications and the potential risks of topical hormone medications. Detailed Implementation

[0020] To make the objectives, technical solutions, and advantages of this invention clearer, the technical solutions of this invention will be clearly and completely described below in conjunction with embodiments. Obviously, the described embodiments are only some, not all, of the embodiments of this invention. All other embodiments obtained by those skilled in the art based on the embodiments of this invention without creative effort are within the scope of protection of this invention.

[0021] Unless otherwise specified, the raw materials used in the following examples are all Chinese medicinal materials or processed slices that conform to the standards of the Chinese Pharmacopoeia, and the equipment used are all conventional equipment in the field.

[0022] Example 1 Preparation of ointment for treating hemorrhoids: Raw material ratio (by weight): 15 parts of charred Sanguisorba officinalis, 12 parts of Gallnut, 6 parts of Dragon's Blood, 2 parts of Saffron, 10 parts of Polygonum cuspidatum extract, 15 parts of Sophora japonica fruit, 12 parts of Phellodendron chinense, 10 parts of roasted licorice root, 8 parts of pearl powder, 10 parts of Orostachys chinensis, 35 parts of egg yolk oil, 30 parts of Lithospermum erythrorhizon oil, and 5 parts of borneol.

[0023] Preparation process: Raw material pretreatment: Take the prescribed amounts of charred Sanguisorba officinalis, Gallnut, Dragon's Blood, and Pearl Powder, and pulverize them separately using an ultra-fine pulverizer. Pass them through a 200-mesh sieve to obtain extremely fine powder for later use.

[0024] Take the prescribed amount of saffron, dry it at a low temperature of 40℃, grind it into powder, and pass it through a 200-mesh sieve for later use.

[0025] Take the prescribed amounts of Phellodendron bark, prepared licorice root, Sophora japonica fruit, and Oryza sativa, mix them thoroughly, add 8 times the total weight of the mixture in 70% ethanol, heat under reflux for 2 hours, filter, and collect the filtrate; add 6 times the amount of 70% ethanol to the residue, reflux for 1.5 hours, and filter. Combine the two filtrates, recover the ethanol under reduced pressure at 60℃, and concentrate to a thick extract with a relative density of 1.28 (measured at 60℃), which is designated as extract A, for later use.

[0026] Take the prescribed amount of Polygonum cuspidatum, add 10 times its weight of water, decoct for 1.5 hours, and filter. Add 8 times its weight of water to the dregs, decoct for 1 hour, and filter. Combine the two decoctions and concentrate to 1 / 4 of the original volume. Add 3 times the volume of 95% ethanol to the concentrate, stir, and let stand for 24 hours. Take the supernatant. Recover the ethanol from the supernatant under reduced pressure at 60°C, and concentrate until there is no alcohol odor to obtain the Polygonum cuspidatum extract, designated as extract B, for later use.

[0027] Synthesis and Aging: Take the prescribed amount of egg yolk oil and comfrey oil, place them in a homogenizing container, and mix them in a 65°C constant temperature water bath until well combined.

[0028] While continuously stirring at a slow speed, add the prescribed amount of borneol powder to the above oil phase, maintain the temperature, and stir until the borneol is completely dissolved.

[0029] Maintain the system temperature at 60-65℃, and sequentially add the pretreated Sanguisorba officinalis charcoal powder, Gallnut powder, Dragon's Blood powder, Pearl powder, and Saffron powder to the oil phase. Turn on the high-speed homogenizer and homogenize and disperse at 8000 rpm for 5-8 minutes to form a uniform and fine suspension paste base.

[0030] Mix extract A and extract B evenly, and under grinding conditions (using a three-roll mill or grinding thoroughly by hand in the same direction), slowly add them to the above-mentioned suspension ointment base material, and continue grinding until the ointment has a uniform color (deep brownish-red), is fine and shiny, and has no visible particles or lumps.

[0031] The obtained ointment was transferred into a sealed, light-proof container and left to stand and age in a cool place (below 25°C) for 36 hours to obtain the original ointment of the traditional Chinese medicine external application composition.

[0032] Formulation: The aged ointment is directly dispensed into 10g pharmaceutical aluminum-plastic tubes and sealed to obtain the hemorrhoid treatment ointment of the present invention.

[0033] Example 2 Preparation of hemorrhoid suppositories raw material: The original ointment of the traditional Chinese medicine external application composition prepared in Example 1.

[0034] Preparation process: Weigh 50g of the original paste prepared in Example 1, place it in a water bath, and heat it at a low temperature below 40°C until it melts into a fluid state.

[0035] Alternatively, take 50g of semi-synthetic fatty acid glycerides (model: S-40) and melt them in a 40℃ water bath.

[0036] Quickly mix the molten paste with the molten suppository base and stir until homogeneous.

[0037] While still hot, pour the mixed medicine solution into the anal suppository mold pre-coated with release agent.

[0038] After cooling until completely solidified, demold.

[0039] The prepared suppositories are sealed in aluminum foil to obtain hemorrhoid suppositories, each weighing approximately 2.5g. This dosage form is suitable for internal hemorrhoids and the internal hemorrhoid portion of mixed hemorrhoids.

[0040] Example 3 Preparation of hemorrhoid cream Raw material ratio (by weight, the ratio of raw medicinal materials is the same as in Example 1): The traditional Chinese medicine external application composition (prepared according to the method of Example 1) consists of 40 parts of raw ointment, 10 parts of stearic acid, 4 parts of glyceryl monostearate, 10 parts of liquid paraffin, 10 parts of glycerin, 1 part of triethanolamine, 0.1 parts of ethylparaben, and purified water to 100 parts.

[0041] Preparation process: Oil phase preparation: Take stearic acid, glyceryl monostearate, liquid paraffin and the original ointment of traditional Chinese medicine external application composition, mix them, heat to 75-80℃ to melt, stir well, and keep warm.

[0042] Aqueous phase preparation: Add glycerol, triethanolamine, and ethylparaben to purified water, heat to 75-80℃, stir until dissolved, and keep warm.

[0043] Emulsification: Under high-speed stirring (approximately 2000 rpm), slowly add the aqueous phase to the oil phase and continue stirring until emulsification is complete.

[0044] Cooling and filling: Stop heating and continue stirring until the temperature drops to about 50°C. Add an appropriate amount of fragrance (optional) and continue stirring until it solidifies into a paste. Dispense into cream boxes to obtain the hemorrhoid cream.

[0045] Example 4 Preparation of Hemorrhoid Spray (Oil-based) Raw material ratio (by weight, the ratio of raw medicinal materials is the same as in Example 1): 20 parts of the original ointment of traditional Chinese medicine external application composition (prepared according to the method of Example 1), 30 parts of isopropyl myristate, and anhydrous ethanol to 100 parts.

[0046] Preparation process: The original ointment of the traditional Chinese medicine external application composition prepared in Example 1 was mixed with isopropyl myristate and stirred in a water bath at 50°C until completely dissolved and mixed.

[0047] Transfer the above mixture to a preparation tank, add the prescribed amount of anhydrous ethanol, and stir until homogeneous.

[0048] The solution was filtered through a microporous membrane (0.45 μm) to obtain a clear solution.

[0049] The medication is filled into a pressure-resistant bottle with a metered spray valve, sealed, and the hemorrhoid spray is obtained. It can be sprayed directly onto the affected area.

[0050] Example 5 Preparation of ointments with different ratios of compositions This embodiment aims to illustrate the feasibility within the range of raw material proportions.

[0051] The raw material ratios (by weight, ratio 1-3) are shown in Table 1:

[0052] Preparation process: Raw materials were weighed according to the three formulations described above, and the preparation process was carried out in accordance with the process described in Example 1. All three formulations successfully produced hemorrhoid treatment ointments with uniform and stable textures. Observation showed that the ointments prepared according to the three formulations met the requirements in terms of appearance, fineness, and spreadability.

[0053] Example 6 Substitution of parameters in the preparation method: This example illustrates the feasibility of the method within the range of weight parameters, based on the proportions in Example 1.

[0054] Changes in alcohol extraction process parameters: In Example 1, the extraction solvent for medicinal materials such as Phellodendron bark was replaced with 65% ethanol, and the extraction was carried out by reflux twice (10 times the amount for 1.5 hours the first time, and 8 times the amount for 1 hour the second time). The extract A could still be successfully concentrated.

[0055] Changes in aging conditions: Adjusting the aging time in Example 1 to 24 hours or 48 hours yields a stable paste. Aging helps the components to blend further, making the paste more delicate and uniform.

[0056] Changes in fine powder particle size: Even if medicinal materials such as Sanguisorba officinalis charcoal are pulverized to pass through a 180-mesh sieve, they can still be used in the preparation. The resulting paste is slightly less fine than the product sieved through a 200-mesh sieve, but it is still a qualified preparation.

[0057] Clinical effects of the topical Chinese medicine composition for treating hemorrhoids provided by this invention: Based on family history of use and feedback from observations of over a hundred patients in recent years, this product can significantly reduce or stop bleeding in grade I and II internal hemorrhoids within 24-48 hours after application; for acute swelling and pain caused by thrombosed external hemorrhoids, a cooling and soothing sensation can be felt within a few hours after external application, and the swelling and pain will subside significantly within 1-3 days; for postpartum hemorrhoids and prolapsed hemorrhoids in the elderly, it can help improve local circulation and enhance the resilience of supporting tissues while relieving symptoms.

[0058] The present invention provides a traditional Chinese medicine external application composition for treating hemorrhoids and its preparation method: Synergistic multi-target approach for both symptomatic and root-cause treatment: This formula combines hemostasis (Sanguisorba officinalis charcoal, Gallnut) with blood-activating properties (Saffron, Dragon's Blood), stopping bleeding without causing blood stasis and activating blood without causing excessive bleeding, thus quickly relieving bleeding and pain. The combination of heat-clearing and detoxifying properties (Phellodendron chinense, Polygonum cuspidatum) with tissue-regenerating and wound-healing properties (Pearl powder, Egg yolk oil) promotes tissue repair.

[0059] Enhanced efficacy and rapid onset of action: = Using borneol as a penetration enhancer and egg yolk oil-complex oil as a base, it greatly improves the transdermal rate and bioavailability of fat-soluble and water-soluble active ingredients, enabling the medicine to quickly penetrate deep into the hemorrhoids and achieve "targeted treatment".

[0060] Highly adaptable to different dosage forms and excellent user experience: The provided preparation methods can be flexibly converted into various external dosage forms such as ointments, suppositories, and sprays, adapting to different usage scenarios (such as home and travel) and disease stages (acute phase and remission phase). The formulation is mild and has low irritation to the perianal mucosa.

[0061] Combining tradition and innovation: Based on the hemostatic and tissue-regenerating medicine (Sanguisorba officinalis charcoal with Gallnut, egg yolk oil with pearl powder), modern extraction technology (refining Polygonum cuspidatum extract) and formulation technology are introduced to ensure the stability and improvement of efficacy.

[0062] Made with natural ingredients and with high safety: The main ingredients are natural animal and plant medicinal materials, which are properly processed and formulated. They are safe for topical application and avoid the gastrointestinal reactions that may be caused by oral medications and the potential risks of topical hormone medications.

[0063] The above description is merely an embodiment of the present invention and does not limit the patent scope of the present invention. Any equivalent structural or procedural transformations made based on the content of the present invention specification, or direct or indirect applications in other related technical fields, are similarly included within the patent protection scope of the present invention.

Claims

1. A traditional Chinese medicine external application composition for treating hemorrhoids, characterized in that, It is made from the following raw materials in the following weight proportions: 10-25 parts of charred Sanguisorba officinalis, 8-20 parts of Gallnut, 3-10 parts of Dragon's Blood, 1-5 parts of Saffron, 5-15 parts of Polygonum cuspidatum extract, 10-20 parts of Sophora japonica fruit, 8-18 parts of Phellodendron chinense, 5-15 parts of roasted licorice root, 5-12 parts of pearl powder, 6-16 parts of Orostachys chinensis, 20-50 parts of egg yolk oil, 15-40 parts of Lithospermum erythrorhizon oil, and 2-8 parts of borneol.

2. The traditional Chinese medicine external application composition according to claim 1, characterized in that, It is made from the following ingredients in the indicated weight proportions: 12-20 parts of charred Sanguisorba officinalis, 10-15 parts of Gallnut, 4-8 parts of Dragon's Blood, 2-4 parts of Saffron, 8-12 parts of Polygonum cuspidatum extract, 12-18 parts of Sophora japonica fruit, 10-15 parts of Phellodendron chinense, 8-12 parts of prepared licorice root, 6-10 parts of pearl powder, 8-12 parts of Orostachys chinensis, 25-40 parts of egg yolk oil, 20-35 parts of Lithospermum erythrorhizon oil, and 3-6 parts of borneol.

3. The traditional Chinese medicine external application composition according to claim 1, characterized in that, The egg yolk oil and comfrey oil together serve as the active ingredients and oil phase matrix.

4. The traditional Chinese medicine external application composition according to claim 1, characterized in that, The composition is a topical preparation, and the dosage form of the topical preparation is selected from ointments, suppositories, creams, or sprays.

5. A method for preparing the traditional Chinese medicine external application composition according to any one of claims 1-4, characterized in that, Includes the following steps: S1: Raw material pretreatment: S11: Prepare the charred Sanguisorba officinalis, Gallnut, Dragon's Blood and Pearl Powder into fine powders respectively; S12: Process saffron into a fine powder; S13: Mix Phellodendron bark, prepared licorice root, Sophora japonica fruit and Oryza sativa, extract with ethanol, and concentrate to obtain the first extract; S14: Extract the Polygonum cuspidatum to obtain a Polygonum cuspidatum extract; S2. Oil phase preparation: Mix egg yolk oil and comfrey oil, add borneol, and stir to dissolve the borneol to form an oil phase mixture; S3. Mixing: Add the fine powder obtained in steps S11 and S12 to the oil phase mixture in step S2 and perform homogenization to obtain a suspension base material; S4. Forming the paste: Add the first extract obtained in step S13 and the Polygonum cuspidatum extract obtained in step S14 to the suspension base material in step S3, grind and mix evenly, and then age to obtain the paste.

6. The method according to claim 5, characterized in that, In steps S11 and S12, the fine powder has a particle size that passes through a 200-mesh sieve; in step S13, the concentration of ethanol is 60%-80%, and reflux extraction is used; in step S14, the preparation method of the Polygonum cuspidatum extract includes: boiling Polygonum cuspidatum in water, concentrating the decoction, adding ethanol to precipitate, and taking the supernatant to recover the ethanol.

7. The method according to claim 5, characterized in that, In step S2, the mixing is carried out at 60-70°C; in step S4, the aging is carried out by standing for 24-48 hours under sealed and light-proof conditions.

8. The method according to claim 5, characterized in that, It also includes formulation forming step S5: mixing the original ointment obtained after aging in step S4 with topical formulation excipients to form topical formulations of different dosage forms.

9. The method according to claim 8, characterized in that, The dosage form is an ointment, suppository, cream, or spray; when preparing suppositories, the excipients include semi-synthetic fatty acid glycerides.

10. The use of the traditional Chinese medicine external application composition according to any one of claims 1-4 in the preparation of a medicament for treating hemorrhoids, characterized in that, The medication is a topical preparation used to treat bleeding, pain, swelling, prolapse, or itching caused by hemorrhoids.

Images