Medicinal solvent capable of inhibiting irritation of external medicament

Abstract

The invention discloses a medicinal solvent capable of inhibiting irritation of an external medicament, which is an external medicament solvent, and adopts an alcohol solvent which is easy to dissolve in water, not easy to volatilize and non-toxic to inhibit the irritation of the external medicament to the skin and inhibit the volatilization of volatile effective components in the external medicament, so that the irritation of the external medicament to the skin is inhibited. Therefore, absorption of skin to the medicament is promoted, no irritation is caused, and administration time is prolonged; the alcohol solvent can be ethylene triol, glycerol, ethylene glycol, propylene glycol, butanediol or diethylene glycol; different effective component extraction modes are implemented according to different temperature resistance of the effective components of the external medicament, including soaking extraction at the temperature of 0-70 DEG C, high-temperature extraction at the temperature of 100-170 DEG C and extraction of the external medicament insoluble in an alcohol solvent by means of a third solvent, so that the external medicament can carry sufficient effective components.

Description

Technical Field

[0001] This invention relates to pharmaceutical solvents, and more specifically to a pharmaceutical solvent that can inhibit the irritation of topical medications. Background Technology

[0002] Traditional Chinese medicines with the effects of promoting blood circulation, removing blood stasis, reducing swelling and relieving pain often have a certain degree of skin irritation. For example, menthol, camphor, safflower, chuanxiong, and peach kernel can stimulate the nerve endings of the skin, producing a warm or stinging sensation. Other drugs containing chemically synthesized ingredients, such as methyl salicylate (wintergreen oil), methyl nicotinic acid, and ethyl nicotinic acid, also have a strong irritant effect on the skin.

[0003] In existing technologies, volatile solvents are often used when extracting the active ingredients from traditional Chinese medicine. These solvents evaporate quickly, which shortens the time the drug remains on the skin surface and leaves residues that are difficult to penetrate effectively, thus affecting skin absorption and failing to achieve the required dosage. Furthermore, aqueous formulations typically contain low levels of active ingredients, making it difficult to meet the required dosage. Summary of the Invention

[0004] To overcome the shortcomings of the prior art, this invention proposes a pharmaceutical solvent that can suppress the irritation of topical medications. The solvent is a water-soluble, non-toxic alcohol containing hydroxyl groups, thereby eliminating the irritation of topical medications, enabling long-term drug delivery, solving the problem of insufficient drug delivery in topical medications, and improving the efficacy of topical medications.

[0005] The present invention adopts the following technical solution to solve the technical problem: The pharmaceutical solvent of this invention, which can suppress the irritation of topical medications, is characterized by the following: the pharmaceutical solvent refers to a topical medication solvent, which is a water-soluble, non-volatile, and non-toxic alcohol solvent, in order to suppress the irritation of the topical medication to the skin and inhibit the volatilization of volatile active ingredients in the topical medication, thereby promoting the absorption of the medication by the skin; the alcohol solvent is glycerol, glycerol, ethylene glycol, propylene glycol, butylene glycol, or diethylene glycol.

[0006] The pharmaceutical solvent of the present invention, which can suppress the irritation of topical medications, is also characterized in that: the alcohol solvent contains not less than 30% by weight in the topical medication.

[0007] The pharmaceutical solvent of this invention, which can suppress the irritation of topical medications, is also characterized by: selecting one or more different methods to extract the active ingredients of the topical medication to achieve the dosage required for skin absorption: Method 1: For the heat-sensitive active ingredients in the topical medicine, perform low-temperature soaking extraction using the alcohol solvent, setting the low-temperature soaking extraction temperature to 0℃~70℃; Method 2: For the heat-resistant active ingredients in the topical medicine, high-temperature soaking extraction is performed using the alcohol solvent, with the high-temperature soaking extraction temperature set at 100℃~170℃; Method 3: For the active ingredient in the topical medicine that is insoluble in alcohol solvents, firstly, solvent A is used to extract the active ingredient in the topical medicine to obtain a solution B containing the active ingredient in the topical medicine. Then, solution B is used to mix with the alcohol solvent. Solvent A refers to a solvent that can dissolve the active ingredient in the topical medicine.

[0008] The pharmaceutical solvent of the present invention, which can inhibit the irritation of topical medications, is also characterized in that: the topical medication does not contain preservatives, and the alcohol solvent inhibits bacteria.

[0009] Topical medications for promoting blood circulation and removing blood stasis are most commonly found in plasters, sprays, and medicinal wines. While they have some effect on common injuries, rheumatic paralysis, and lower back and leg pain, the results are not ideal. Firstly, the spiciness and irritation to the skin cause discomfort, preventing prolonged application and resulting in insufficient dosage. Secondly, the use of volatile solvent-based topical medications leads to rapid solvent evaporation, preventing the medication from penetrating the skin after drying, significantly reducing its effectiveness. Thirdly, while aqueous medications can be administered for extended periods, they carry less of the active ingredients, still resulting in insufficient dosage and unsatisfactory effects. This invention utilizes a medicinal solvent to inhibit skin irritation from topical medications, promote skin absorption, prolong the administration time, and carry more of the active ingredients, achieving a dosage sufficient for skin absorption. Compared to existing technologies, the beneficial effects of this invention are as follows: 1. The pharmaceutical solvent of this invention can suppress the irritation of topical medications, thus eliminating the discomfort caused by the irritation of topical medications; 2. The pharmaceutical solvent of this invention can suppress the irritation of topical medications, eliminate the irritation of topical medications to the skin, inhibit the volatilization of volatile active ingredients in topical medications, and improve the efficacy of the medication by extending the administration time; 3. The pharmaceutical solvent of this invention can suppress the irritation of topical medications, dissolve more of the active ingredients in the topical medications, and can carry more medication. 4. This invention employs different extraction methods for the active ingredients of topical medications based on their varying temperature resistance, including soaking extraction at 0°C to 70°C, high-temperature extraction at 100°C to 170°C, and extraction of topical medications incompatible with alcohol solvents using a third solvent. This ensures that the topical medication carries sufficient active ingredients to achieve the dosage required for skin absorption. 5. This invention employs multiple extraction methods for medicinal agents, enriching the effective components of traditional Chinese medicine in external medicines and enhancing their efficacy. Attached Figure Description

[0010] Figure 1The image shows a skin irritation test of a 2% capsaicin solution prepared according to the present invention by mixing glycerol and capsaicin.

[0011] Figure 2 These are images from a skin irritation test of a commercially available 0.025% capsaicin cream. Detailed Implementation

[0012] Common topical medications for promoting blood circulation and removing blood stasis include safflower oil and topical washes made from herbs such as Panax notoginseng, peach kernel, safflower, and Salvia miltiorrhiza. These medications have the effects of warming the meridians and promoting blood circulation, dispelling cold and removing blood stasis, and clearing the meridians. In traditional Chinese medicine, they can be divided into categories such as blood-activating and wound-healing drugs, blood-activating and pain-relieving drugs, and blood-activating and menstrual-regulating drugs. Their common dosage forms include plasters, sprays, and medicinal wines.

[0013] These topical medications are effective for common injuries, rheumatic pain, and lower back and leg pain, with relatively few side effects overall. However, some medications may irritate the skin, causing temporary burning, stinging, or itching; some individuals with sensitive skin may experience more pronounced reactions. Furthermore, to enhance efficacy, it is sometimes recommended to wrap the medication with plastic wrap after application. This may further aggravate skin irritation and affect patient adherence.

[0014] Example 1: Water-soluble and non-toxic alcohol solvents are used as solvents for irritating topical medications to inhibit the skin irritation caused by the topical medications and to inhibit the volatilization of volatile active ingredients in the topical medications, thereby promoting the absorption of the medications by the skin.

[0015] Inhibiting skin irritation from topical medications and promoting skin absorption of the medication are specifically manifested in the following aspects: Firstly, the moisturizing properties of alcohol solvents eliminate the irritation of topical medications to the skin; alcohols, as solvents, have water-absorbing properties, absorbing moisture from the skin and promoting the penetration of the medication into the skin; the active ingredients of topical medications can move in the solution, replenishing the active ingredients of the topical medication on the skin surface at any time; in contrast, thick ointments, because the active ingredients cannot flow, the skin can only absorb the active ingredients that are close to the skin, and most of the active ingredients are wasted.

[0016] Secondly, on the one hand, alcohol solvents inhibit the volatilization of topical medications and irritate the skin; on the other hand, alcohol solvents themselves are almost non-volatile, enabling long-term skin administration, promoting skin absorption, and ensuring that the administration time meets the dosage required by the skin.

[0017] Third, alcohol solvents, with their solvent properties, can carry the dosage required for skin absorption. As a solvent, alcohol solvents can dissolve more active ingredients in the drug than water, thus carrying more active ingredients. On the other hand, they can help other active ingredients (such as plant extracts such as enzymes and alkaloids) penetrate more evenly into the stratum corneum, improving the overall effectiveness.

[0018] Fourth, by utilizing the selective solubility of solvents in the active ingredients of traditional Chinese medicine, these ingredients are separated from the medicinal matrix, ensuring that easily volatile and easily decomposed active ingredients are preserved in alcohol solvents.

[0019] Fifth, volatile Chinese medicinal herbs such as peppermint, asarum, musk, borneol, and styrax are dissolved in alcohol solvents. Through a dual mechanism of thermodynamics (reducing vapor pressure) and kinetics (increasing diffusion resistance), alcohol solvents effectively "tame" their volatility, making them more durable and stable.

[0020] In this embodiment, the alcohol solvent is glycerol, glycerol, ethylene glycol, propylene glycol, butylene glycol, or diethylene glycol, and the alcohol solvent contains no less than 30% by weight in the topical medicine.

[0021] Capsaicin, methyl salicylate (wintergreen oil), and methyl nicotinic acid are highly irritating to the skin, and their effects on the skin are representative. Capsaicin relieves chronic pain caused by arthritis, neuralgia, and muscle aches. The irritant effects of capsaicin on the skin mainly manifest as a burning sensation, redness, and stinging, which can lead to skin redness, blisters, and even epidermal peeling if used improperly. Dissolving capsaicin in a solution such as glycerin satisfies the need to relieve arthritis, neuralgia, and muscle aches while avoiding skin irritation, redness, blisters, and epidermal peeling.

[0022] Comparative test: Skin irritation test of capsaicin Capsaicin is one of the most potent skin irritants.

[0023] Capsaicin dosage instructions: (1) Low concentration range (common in ordinary heat patches and muscle pain relief patches), the capsaicin content is usually between 0.025% and 0.1%, which is sufficient to produce a noticeable and continuous warming sensation and a slight "burning sensation". (2) Higher concentration range (used for stronger analgesia, should be used with caution), some products specifically for joint pain (such as arthritis) may have a concentration of 0.25% or even higher (such as 0.75%). These products usually produce a strong burning sensation in the early stages of use, and users need to build up tolerance. They must be used under the guidance of a doctor or pharmacist and should not be used on broken skin.

[0024] Experiment 1: Skin irritation test of a mixture of glycerol and capsaicin according to the present invention. (1) Experimental ratio: 49 grams of glycerol and 1 gram of capsaicin were mixed to obtain capsaicin with a concentration of 2%, which is far higher than the concentration of commercially available capsaicin products.

[0025] (2) Experimental method: Capsaicin, which was prepared by mixing with glycerol to a concentration of 2%, was applied to the back of the hands of four subjects. Photos were taken at 5 minutes, 10 minutes, 20 minutes, 40 minutes and 60 minutes. The capsaicin was wiped off at 60 minutes and the skin condition was observed.

[0026] Figure 1 The backs of the hands of four subjects are represented by a, b, c, and d. The experimental results are as follows: Take a photo 5 minutes after applying the medication: Figure 1 In Figures (a1), (b1), (c1), and (d1), none of the four individuals experienced any irritation or burning sensation. Take a photo 10 minutes after applying the medication: (e.g.) Figure 1 In Figures (a2), (b2), (c2), and (d2), none of the four individuals experienced any irritation or burning sensation. Take a photo 20 minutes after applying the medication: Figure 1 In the figures (a3), (b3), (c3), and (d3), one person experienced an ant-bite sensation, while the other three people did not experience any irritation or burning sensation. Take a photo 40 minutes after applying the medication: Figure 1 In Figures (a4), (b4), (c4), and (d4), two people experienced ant bite sensations, while the other two people did not experience any irritation or burning sensation. Take a photo 60 minutes after applying the medication: Figure 1 In Figures (a5), (b5), (c5), and (d5), two people experienced ant bite sensations, while the other two experienced no irritation or burning sensation. Wipe dry the area 60 minutes after applying the medication, and take a photo after drying. Figure 1 Figures (a6), (b6), (c6), and (d6) show the results at the end of the experiment: all four participants had no irritation marks or burning sensation on the backs of their hands.

[0027] The experimental results show that a 2% capsaicin glycerol solution has very little irritation to the skin and effectively inhibits the irritation of the skin by topical medications, achieving the goal of this invention to inhibit the irritation of the skin by topical medications, and can also inhibit the irritation of inorganic topical medications.

[0028] Experiment 2: Skin irritation test of capsaicin cream (1) Purchase a commercially available brand of capsaicin cream: 10 grams, containing 0.25 mg of capsaicin, which is equivalent to a content of 0.025%. Figure 2 As shown in Figure (e).

[0029] (2) Experimental method: Before application, take a photo. Apply capsaicin cream to the back of the hands of 4 people and take a photo. Wipe it off after 60 minutes and take a photo. The subjects describe their feelings at 5, 10, 20, 40 and 60 minutes after application.

[0030] like Figure 2 The four backs of the hands are represented by a, b, c, and d. The experimental results are as follows: Take a photo before application: such as Figure 2 Figures (1a), (1b), (1c) and (1d) are shown in the middle. Take a photo after applying capsaicin cream: (e.g.) Figure 2 Figures (3a), (3b), (3c) and (3d) are shown in the middle.

[0031] Take a photo after wiping off the capsaicin cream from the back of your hand 60 minutes after applying it: (See attached image) Figure 2 In Figures (2a), (2b), (2c), and (2d), the backs of the hands of the four people are red due to stimulation. Subjects' perceptions of the degree of stimulation during the experiment: 5 minutes after applying capsaicin cream, all 4 subjects described feeling irritation; 10 minutes later, all 4 subjects described feeling a burning sensation; 20 minutes later, all 4 subjects experienced a burning sensation; 40 minutes later, all 4 subjects experienced a strong burning sensation; 60 minutes later, all 4 subjects experienced a strong burning sensation; the irritation gradually weakened and subsided 10 minutes after the capsaicin cream was removed.

[0032] The comparison of the two experiments shows that alcohol solvents have a good effect in inhibiting the irritation of topical medications.

[0033] Example 2: For the active ingredients of topical medications, one or more different extraction methods are selected to achieve a dosage sufficient for skin absorption: Method 1: For topical medications containing heat-sensitive active ingredients, extract the medication by soaking it in a solvent between 0°C and 70°C. If the active ingredients of traditional Chinese medicine are bio-enzymes or low-temperature alkaloids, this extraction method can be used. When the temperature is too high, the three-dimensional spatial structure of the enzyme will be destroyed, leading to denaturation and inactivation, thus losing its activity. This inactivation temperature range is usually between 60℃ and 80℃. If the active ingredients are denatured at high temperatures, such as bromelain, which has anti-inflammatory and swelling-reducing properties, low-temperature extraction is only suitable.

[0034] Low-temperature alkaloids generally refer to alkaloid compounds extracted or processed under low-temperature conditions, such as heat-sensitive natural products like belladonna alkaloids.

[0035] Low-temperature extraction technology effectively reduces the risk of thermal decomposition and maintains the structure and bioactivity of compounds by controlling the temperature within the range of 0 to 70°C. The core principle of low-temperature extraction technology is to inhibit the degradation of heat-sensitive substances by lowering the temperature, while enhancing the selective solubility of the solvent for the target compound. Specific advantages include: (1) Maintaining bioactivity: The low-temperature environment can avoid the pyrolysis or hydrolysis of belladonna alkaloids (such as scopolamine and atropine), thereby enhancing the pharmacological activity of the extract. (2) Protecting the integrity of the raw materials: Reducing side reactions such as oxidation and pyrolysis caused by high temperature, and maintaining the structural stability of the raw materials.

[0036] Method 2: For the effective components of heat-resistant topical medications, the Chinese herbal medicines are soaked and extracted in a solvent between 100℃ and 170℃.

[0037] For example, glycerol, also known as glycerin, has a boiling point of 290℃. When glycerol is used as an alcohol solvent, it can be used to quickly extract the active ingredients at 170℃, and also to dissolve more of the active ingredients to enhance the therapeutic effect.

[0038] Some potent blood-activating herbs, such as raw aconite, raw aconitum carmichaelii, raw aconitum kusnezoffii, and raw arisaema, are processed to remove toxins and then heated with glycerol to 100–170°C to extract the active ingredients from the herbs. This process accelerates the extraction process and allows for the extraction of more active ingredients.

[0039] Method 3: For topical medications whose active ingredients are insoluble in alcohol solvents, first use solvent A to extract the active ingredients of the topical medication to obtain solution B containing the active ingredients of the topical medication. Then, use solution B to mix with an alcohol solvent. Solvent A refers to a solvent that can dissolve the active ingredients of the topical medication.

[0040] Most solvents are miscible with alcohol solvents, so the active ingredients can be extracted first using solvent extraction and then dissolved in alcohol solvents, thus integrating the active ingredients of these traditional Chinese medicines into the alcohol solvent.

[0041] For Chinese herbal medicines containing volatile oils and aromatic properties that promote blood circulation, such as Chuanxiong, Danggui, Boswellia carterii, Commiphora myrrha, Curcuma longa, Cinnamomum cassia, Mentha haplocalyx, and Borneol, the main active ingredients are volatile oils (ligustilide, curcumin, eucalyptol, etc.) and terpenes. First, dissolve the volatile oils in ethanol, and then mix the ethanol solution containing the volatile oils with glycerol to inhibit volatilization and enhance the efficacy.

[0042] Example 3: Preparation of a topical medicine for promoting blood circulation, removing blood stasis, and clearing the meridians: 20g of myrrh, 0.5g of capsaicin, 0.5g of wintergreen oil, 30g of mulberry mistletoe, 30g of chicken blood vine, 20g of broad-leaved vine, 30g of epimedium root, 20g of turmeric, and 200g of glycerol were mixed and soaked at a low temperature of 30℃~40℃ for 24 hours to extract the effective components such as biological enzymes and low-temperature alkaloids from these Chinese herbal medicines, resulting in solution C1; 20g of myrrh, 30g of mulberry mistletoe, 30g of chicken blood vine, 20g of broad-leaved vine, 30g of epimedium root, 20g of turmeric, 10g of frankincense, and 200g of glycerol were mixed and heated to 150℃~170℃ for 24 hours to extract the effective components such as high-temperature alkaloids from these Chinese herbal medicines, resulting in solution C2; 5g of borneol and 5g of natural camphor were dissolved in 50g of ethanol to obtain solution C3. Solutions C1, C2, and C3 are mixed to prepare a topical medication for promoting blood circulation, removing blood stasis, and clearing the meridians. Utilizing the antibacterial properties of alcohol solvents, no preservatives are added to the topical medication, eliminating the potential impact of preservatives on the medication.

Claims

1. A pharmaceutical solvent that can inhibit the irritation of topical medications, characterized in that: The pharmaceutical solvent refers to the solvent for topical medications. The pharmaceutical solvent is an alcohol solvent that is easily soluble in water, does not easily evaporate, and is non-toxic, in order to inhibit the irritation of the topical medication to the skin and inhibit the volatilization of volatile active ingredients in the topical medication, thereby promoting the absorption of the medication by the skin. The alcohol solvent is glycerol, glycerol, ethylene glycol, propylene glycol, butylene glycol, or diethylene glycol.

2. The pharmaceutical solvent for inhibiting the irritation of topical medications according to claim 1, characterized in that: The alcohol solvent contains not less than 30% by weight in the topical medication.

3. The pharmaceutical solvent for inhibiting the irritation of topical medications according to claim 1, characterized in that: For the aforementioned topical medication, one or more different methods are selected for extracting the active ingredients to achieve the dosage required for skin absorption: Method 1: For the heat-sensitive active ingredients in the topical medicine, perform low-temperature soaking extraction using the alcohol solvent, setting the low-temperature soaking extraction temperature to 0℃~70℃; Method 2: For the heat-resistant active ingredients in the topical medicine, high-temperature soaking extraction is performed using the alcohol solvent, with the high-temperature soaking extraction temperature set at 100℃~170℃; Method 3: For the active ingredient in the topical medicine that is insoluble in alcohol solvents, firstly, solvent A is used to extract the active ingredient in the topical medicine to obtain a solution B containing the active ingredient in the topical medicine. Then, solution B is used to mix with the alcohol solvent. Solvent A refers to a solvent that can dissolve the active ingredient in the topical medicine.

4. The pharmaceutical solvent for inhibiting the irritation of topical medications according to claim 1, characterized in that: The topical medication does not contain preservatives and uses alcohol solvents for antibacterial activity.

Images