Traditional Chinese medicine composition for promoting transdermal absorption and preparation method thereof

Abstract

The invention belongs to the technical field of medicines, and particularly provides a traditional Chinese medicine composition for promoting transdermal absorption and a preparation method thereof. According to the invention, fructus evodiae, szechwan chinaberry fruit, rhizoma anemarrhenae, cinnamon, golden cypress and honey-fried licorice root are adopted as raw materials and are proportioned by weight properly; under the combined action of all the medicine components, the effect of promoting transdermal absorption can be achieved. The pharmaceutical composition disclosed by the invention is good in transdermal absorption effect and non-irritant to skin; the medicine composition is used for assisting medicine transdermal absorption, especially aiming at acupuncture points such as navel and the like, the medicine composition is supplemented with a traditional oral administration prescription for a certain adaptation disease to be prepared into a patch, and the patch is matched with the corresponding acupuncture points for external application treatment. Finally, the same treatment effect can be achieved while the side effect of the oral medicine is effectively avoided.

Description

Technical Field

[0001] The present invention belongs to the technical field of traditional Chinese medicine, and particularly relates to a traditional Chinese medicine composition for promoting transdermal absorption and a preparation method thereof. Background Art

[0002] The navel is an important part of the human body, which is called Shenque acupoint in traditional Chinese medicine. Before a person is born, the fetus exchanges substances with the mother through the umbilical cord. After a person is born, the navel part after the umbilical cord falls off is still an important part of the body. The internal organs of a person can obtain partial oxygen through the navel. The navel is the weakest place in the human body's resistance to the outside world, and the navel circumference is the location of the stomach and intestines. If a person's resistance weakens, it is easy to cause disorders of gastrointestinal function and allow germs to invade the body.

[0003] Transdermal drug delivery preparations refer to new dosage forms in which drugs are applied on the skin surface and the drugs enter the systemic circulation at a constant rate through the skin to produce systemic or local therapeutic effects. Its advantages are as follows: drug absorption is not affected by factors such as pH, food, and transit time in the digestive tract; the first-pass effect of the liver is avoided; and adverse reactions caused by too high a blood drug concentration due to too fast absorption are overcome. However, transdermal absorption needs to overcome the barrier of the human skin to drug penetration and improve the bioavailability of drug transdermal absorption, which is also the key technical part of transdermal drug delivery preparations. Summary of the Invention

[0004] In order to solve the above problems existing in the prior art, the present invention provides a traditional Chinese medicine composition for promoting transdermal absorption with good transdermal absorption effect and no irritation to the skin and a preparation method thereof.

[0005] The technical solution adopted by the present invention is as follows: In a first aspect of the present invention, there is provided a traditional Chinese medicine composition for promoting transdermal absorption, and the raw material components include: 5-15 parts by weight of Evodia rutaecarpa, 5-15 parts by weight of Toosendan fruit, 5-15 parts by weight of Anemarrhena asphodeloides, 2-8 parts by weight of Cinnamon, 2-8 parts by weight of Phellodendron amurense, and 2-8 parts by weight of roasted licorice root.

[0006] Further preferably, the raw material components of the traditional Chinese medicine composition for promoting transdermal absorption include: 8-12 parts by weight of Evodia rutaecarpa, 8-12 parts by weight of Toosendan fruit, 8-12 parts by weight of Anemarrhena asphodeloides, 4-6 parts by weight of Cinnamon, 4-6 parts by weight of Phellodendron amurense, and 4-6 parts by weight of roasted licorice root.

[0007] Further preferably, the raw material components of the traditional Chinese medicine composition for promoting transdermal absorption include: 10 parts by weight of Evodia rutaecarpa, 10 parts by weight of Toosendan fruit, 10 parts by weight of Anemarrhena asphodeloides, 5 parts by weight of Cinnamon, 5 parts by weight of Phellodendron amurense, and 5 parts by weight of roasted licorice root.

[0008] The second aspect of the present invention provides a method for preparing the Chinese medicine composition for promoting transdermal absorption, comprising the following steps: (1) Taking Evodia rutaecarpa, Toosendan fruit and Rhizoma Anemarrhenae according to weight, and crushing them to obtain respective Chinese medicinal powders; (2) fully mixing the Chinese medicinal powders, then adding water for water extraction to obtain a water extract; (3) filtering and concentrating the aqueous extract of step (2) to obtain a concentrate; (4) drying and ultrafine grinding the concentrate in step (3) to obtain ultrafine powder; (5) Cinnamon bark, Phellodendron chinense and Radix Glycyrrhizae Radix are ultrafinely ground respectively, and then added to the ultrafine powder obtained in step (4) in sequence, and mixed thoroughly to obtain the Chinese medicine composition for promoting transdermal absorption.

[0009] In step (1), the particle size of each Chinese medicine powder is 80-100 mesh.

[0010] In step (2), the mass ratio of the Chinese medicine mixed powder to the added water is 1:4-1:8; and the water extraction treatment time is 1-2h.

[0011] In step (3), the concentration is concentrated under reduced pressure to a thick paste with a relative density of 1.30-1.35.

[0012] In step (4) and step (5), the particle size of the ultrafine powder obtained after ultrafine grinding is 800-1200 mesh.

[0013] In step (5), vaseline is added to the obtained traditional Chinese medicine composition, and the mixture is thoroughly mixed to obtain an ointment; The mass ratio of the traditional Chinese medicine mixed powder to vaseline is 1:1-1:2.

[0014] The application of the traditional Chinese medicine composition in preparing a medicine for promoting transdermal absorption.

[0015] Evodia rutaecarpa, pungent, bitter, hot in nature, used for headache due to Jueyin meridian, abdominal pain due to cold hernia, beriberi due to cold and dampness, abdominal pain during menstruation, abdominal distension and pain, vomiting and acid regurgitation, and diarrhea at dawn.

[0016] Toosendan fruit, bitter in taste, cold in nature, slightly toxic. It soothes the liver, promotes qi circulation, relieves pain, and drives away parasites. It is used for chest and flank pain, abdominal distension and pain, hernia pain, and abdominal pain caused by parasites.

[0017] Rhizoma Anemarrhenae, bitter and sweet in taste, cold in nature. It clears away heat and purges fire, promotes the production of body fluids and moistens dryness. It is used for exogenous febrile diseases, high fever and thirst, dry cough due to lung heat, hot flashes due to bone steaming, internal heat and thirst, and constipation due to dry intestines.

[0018] Cinnamon bark is spicy, sweet and hot in nature. It has the effects of replenishing fire and yang, guiding fire back to the origin, dispersing cold and relieving pain, warming the meridians, and warming and unblocking the meridians.

[0019] Phellodendron amurense Rupr., bitter in taste and cold in nature, clearing heat and drying dampness, purging fire and removing steaming, detoxifying and treating sores. It is used for damp-heat diarrhea, jaundice, leukorrhea, stranguria, beriberi, flaccidity, steaming bone fever, night sweats, spermatorrhea, sores and boils, eczema and pruritus. Phellodendron amurense Rupr. processed with salt nourishes yin and purges fire, and is used for yin deficiency and excessive fire, night sweats and steaming bone.

[0020] Prepared Licorice Root, sweet in taste and neutral in nature, invigorating the spleen and stomach, replenishing qi and restoring pulse. It is used for weakness of the spleen and stomach, lassitude and weakness, palpitation, and intermittent pulse.

[0021] The present invention has the following beneficial effects: The present invention provides a traditional Chinese medicine composition for promoting transdermal absorption, which uses Evodia rutaecarpa (Juss.) Benth., Melia toosendan Sieb. et Zucc., Anemarrhena asphodeloides Bunge, Cinnamomum cassia Presl, Phellodendron amurense Rupr., and Prepared Licorice Root as raw materials and performs appropriate weight ratios; under the combined action of the above drug components, it can achieve the effect of promoting transdermal absorption. The drug composition of the present invention has good transdermal absorption effect and no irritation to the skin; the drug composition of the present invention is used to assist drug transdermal absorption, especially for acupoints such as the navel, etc. The drug composition is supplemented with a traditional oral prescription for a certain indication to form a patch, and the patch is used for external application treatment in combination with the corresponding acupoints, and finally it can achieve the same therapeutic effect while effectively avoiding the side effects of oral medications. Detailed implementation manners

[0022] To make the objectives, technical solutions and advantages of the present invention clearer, the technical solutions of the present invention will be described in detail below. Obviously, the described embodiments are only a part of the embodiments of the present invention, rather than all of the embodiments. Based on the embodiments of the present invention, all other implementation manners obtained by those of ordinary skill in the art without creative efforts fall within the scope of protection of the present invention.

[0023] Unless otherwise specified, the reagents involved in the detailed implementation manners of the present invention are all commercially available products and can be obtained through commercial channels.

[0024] In the following examples, 1 part by weight represents 1 g.

[0025] Example 1 This example provides a traditional Chinese medicine composition for promoting transdermal absorption, and the raw material components include: 5 parts by weight of Evodia rutaecarpa (Juss.) Benth., 15 parts by weight of Melia toosendan Sieb. et Zucc., 5 parts by weight of Anemarrhena asphodeloides Bunge, 8 parts by weight of Cinnamomum cassia Presl, 2 parts by weight of Phellodendron amurense Rupr., and 8 parts by weight of Prepared Licorice Root.

[0026] The preparation method of the traditional Chinese medicine composition for promoting transdermal absorption includes the following steps: (1) Take Evodia rutaecarpa (Juss.) Benth., Melia toosendan Sieb. et Zucc., and Anemarrhena asphodeloides Bunge according to parts by weight, and after pulverization, obtain each traditional Chinese medicine powder with a particle size of 80 mesh; (2) Thoroughly mix all the traditional Chinese medicine powders evenly, and then add 4 times the mass of water for water extraction for 2 hours to obtain a water extract. (3) After filtering the water extract described in step (2), concentrate it to a thick paste with a relative density of 1.30 to obtain a concentrate. (4) After drying the concentrate described in step (3), perform ultrafine grinding to obtain an ultrafine powder with a particle size of 800 mesh. (5) Take cinnamon, phellodendron bark, and roasted licorice root. After separately ultrafinely grinding them to a particle size of 800 mesh, add them to the ultrafine powder obtained in step (4) and mix evenly to obtain the traditional Chinese medicine composition for promoting transdermal absorption.

[0027] Example 2 This example provides a traditional Chinese medicine composition for promoting transdermal absorption, and its raw material components include: Evodia rutaecarpa 15 parts by weight, Toosendan fruit 5 parts by weight, Anemarrhena asphodeloides 15 parts by weight, Cinnamon 2 parts by weight, Phellodendron bark 8 parts by weight, Roasted licorice root 2 parts by weight.

[0028] The preparation method of the traditional Chinese medicine composition for promoting transdermal absorption includes the following steps: (1) Take Evodia rutaecarpa, Toosendan fruit, and Anemarrhena asphodeloides according to parts by weight. After pulverization, obtain each traditional Chinese medicine powder with a particle size of 100 mesh. (2) Thoroughly mix all the traditional Chinese medicine powders evenly, and then add 8 times the mass of water for water extraction for 1 hour to obtain a water extract. (3) After filtering the water extract described in step (2), concentrate it to a thick paste with a relative density of 1.35 to obtain a concentrate. (4) After drying the concentrate described in step (3), perform ultrafine grinding to obtain an ultrafine powder with a particle size of 1200 mesh. (5) Take cinnamon, phellodendron bark, and roasted licorice root. After separately ultrafinely grinding them to a particle size of 1200 mesh, add them to the ultrafine powder obtained in step (4) and mix evenly to obtain the traditional Chinese medicine composition for promoting transdermal absorption.

[0029] Example 3 This example provides a traditional Chinese medicine composition for promoting transdermal absorption, and its raw material components include: Evodia rutaecarpa 8 parts by weight, Toosendan fruit 12 parts by weight, Anemarrhena asphodeloides 8 parts by weight, Cinnamon 6 parts by weight, Phellodendron bark 4 parts by weight, Roasted licorice root 6 parts by weight.

[0030] The preparation method of the traditional Chinese medicine composition for promoting transdermal absorption includes the following steps: (1) Take Evodia rutaecarpa, Toosendan fruit, and Anemarrhena asphodeloides according to parts by weight. After pulverization, obtain each traditional Chinese medicine powder with a particle size of 90 mesh. (2) Mix all the traditional Chinese medicine powders thoroughly, and then add 6 times the mass of water for water extraction for 1.5 h to obtain a water extract. (3) After filtering the water extract described in step (2), concentrate it to a thick paste with a relative density of 1.33 to obtain a concentrate. (4) After drying the concentrate described in step (3), perform ultrafine grinding to obtain an ultrafine powder with a particle size of 1000 mesh. (5) Take cinnamon, phellodendron bark, and roasted licorice root. After separately ultrafinely grinding them to a particle size of 1000 mesh, add them to the ultrafine powder obtained in step (4) and mix thoroughly to obtain the traditional Chinese medicine composition for promoting transdermal absorption. Add vaseline to the obtained traditional Chinese medicine composition. The mass ratio of the traditional Chinese medicine mixed powder to vaseline is 1:1, and mix thoroughly to obtain a paste for promoting transdermal absorption.

[0031] Example 4 This example provides a traditional Chinese medicine composition for promoting transdermal absorption, and the raw material components include: Evodia rutaecarpa 12 parts by weight, Toosendan fruit 8 parts by weight, Anemarrhena asphodeloides 12 parts by weight, Cinnamon 4 parts by weight, Phellodendron bark 6 parts by weight, Roasted licorice root 4 parts by weight.

[0032] The preparation method of the traditional Chinese medicine composition for promoting transdermal absorption includes the following steps: (1) Take Evodia rutaecarpa, Toosendan fruit, and Anemarrhena asphodeloides according to parts by weight. After pulverization, obtain each traditional Chinese medicine powder with a particle size of 90 mesh. (2) Mix all the traditional Chinese medicine powders thoroughly, and then add 6 times the mass of water for water extraction for 2 h to obtain a water extract. (3) After filtering the water extract described in step (2), concentrate it to a thick paste with a relative density of 1.34 to obtain a concentrate. (4) After drying the concentrate described in step (3), perform ultrafine grinding to obtain an ultrafine powder with a particle size of 1100 mesh. (5) Take cinnamon, phellodendron bark, and roasted licorice root. After separately ultrafinely grinding them to a particle size of 1100 mesh, add them to the ultrafine powder obtained in step (4) and mix thoroughly to obtain the traditional Chinese medicine composition for promoting transdermal absorption. Add vaseline to the obtained traditional Chinese medicine composition. The mass ratio of the traditional Chinese medicine mixed powder to vaseline is 1:2, and mix thoroughly to obtain a paste for promoting transdermal absorption.

[0033] Example 5 This example provides a traditional Chinese medicine composition for promoting transdermal absorption, and the raw material components include: Evodia rutaecarpa 10 parts by weight, Toosendan fruit 10 parts by weight, Anemarrhena asphodeloides 10 parts by weight, Cinnamon 5 parts by weight, Phellodendron bark 5 parts by weight, Roasted licorice root 5 parts by weight.

[0034] The preparation method of the traditional Chinese medicine composition for promoting transdermal absorption comprises the following steps: (1) Take Evodia rutaecarpa, Toosendan fruit and Anemarrhena rhizome by weight, and after pulverization, obtain each traditional Chinese medicine powder with a particle size of 90 mesh; (2) Mix each traditional Chinese medicine powder evenly, and then add 6 times the mass of water for water extraction for 1.5 h to obtain a water extract; (3) After filtering the water extract obtained in step (2), concentrate it to a thick paste with a relative density of 1.33 to obtain a concentrate; (4) After drying the concentrate obtained in step (3), perform ultrafine pulverization to obtain an ultrafine powder with a particle size of 1000 mesh; (5) Take Cinnamon Bark, Phellodendron bark and Honey-fried Licorice Root, after separately performing ultrafine pulverization to a particle size of 1000 mesh, add them to the ultrafine powder obtained in step (4), and mix evenly to obtain the traditional Chinese medicine composition for promoting transdermal absorption.

[0035] Comparative Example 1 The difference between this comparative example and Example 5 is only the different raw material components. In the raw material components of this comparative example, the mass ratio of Evodia rutaecarpa, Toosendan fruit and Anemarrhena rhizome is 4:1:4, that is, 48 parts by weight of Evodia rutaecarpa, 12 parts by weight of Toosendan fruit, 48 parts by weight of Anemarrhena rhizome, and the dosages of other raw materials and the preparation method are the same as those in Example 1.

[0036] Comparative Example 2 The difference between this comparative example and Example 5 is only the different raw material components. In the raw material components of this comparative example, the mass ratio of Cinnamon Bark, Phellodendron bark and Honey-fried Licorice Root is 1:3:1, that is, 6 parts by weight of Cinnamon Bark, 18 parts by weight of Phellodendron bark, 6 parts by weight of Honey-fried Licorice Root, and the dosages of other raw materials and the preparation method are the same as those in Example 1.

[0037] Comparative Example 3 The difference between this comparative example and Example 5 is only the different preparation method. The preparation method of this comparative example is as follows: (1) Take each raw material component by weight, and after pulverization, obtain each traditional Chinese medicine powder with a particle size of 120 mesh; (2) Mix the traditional Chinese medicine powders obtained in step (1) evenly to obtain a traditional Chinese medicine mixed powder; (3) Add 6 times the mass of water to the traditional Chinese medicine mixed powder obtained in step (2) for reflux extraction for 2 h, and repeat the reflux extraction 2 times, and combine the extraction liquids to obtain a water extract; (4) After filtering the water extract obtained in step (3), concentrate it under reduced pressure to a thick paste with a relative density of 1.32 to obtain a concentrate; (5) First dry the concentrate obtained in step (4) at 100 °C, and then perform pulverization to obtain a traditional Chinese medicine composition.

[0038] Experimental Example The drug compositions obtained in Examples 1-5 of the present invention and Comparative Examples 1-3 were mixed with montmorillonite powder, and vaseline was added to form a paste, which was further applied to the leak-proof ring of the umbilical patch. After cooling, an anti-adhesive layer was covered to obtain the umbilical patch. The effect of the above umbilical patch on diarrhea induced by senna in mice was detected.

[0039] Fifty male Kunming mice, 3 months old, were randomly divided into 5 groups, namely the test drug group, the control group and the blank model group, with 10 mice in each group. Before administration, the abdomen of the mice was depilated, and the area was about 3 cm 2 or so, fasting but not water deprivation. After 3 h, the umbilical patches prepared based on the drugs of Examples 1-5 and Comparative Examples 1-3 were respectively applied to the abdomen of the mice in the test drug group, and the application area was 3 cm 2 . The control group was fed with montmorillonite powder, and the blank group was applied with a blank matrix. Each group was fixed with adhesive tape to prevent falling off. After 6 h, each group of mice was intragastrically administered with senna extract (senna was boiled with water for 10 min, filtered and concentrated to 0.3 g of medicinal materials / ml) at 25 mL / kg. The mice were observed individually in a single cage, and filter paper was laid underneath for weighing the loose stools. The degree of diarrhea was expressed by the weight of the loose stools, and the weight was measured once per hour. The total number of loose stools at each time point was calculated cumulatively. During this period, the filter paper was replaced in time and the loose stools were cleaned up. The results are shown in Table 1.

[0040] Table 1 - Comparison of the therapeutic effects of various drugs on diarrhea induced by senna extract in mice As can be seen from Table 1, the umbilical patches prepared based on the drugs of Examples 1-5 and traditional oral drugs have good therapeutic effects on diarrhea, which are equivalent to the efficacy of taking the drugs orally. Especially for Example 5, by reasonably controlling the dosage of each traditional Chinese medicine component, the synergistic effect of each traditional Chinese medicine component is exerted, and the obtained drug composition has the optimal transdermal absorption effect and therapeutic effect; in Comparative Examples 1-3, the content of some traditional Chinese medicine components is not within the scope defined in the present invention or different preparation methods are adopted, which will to a certain extent affect the transdermal absorption effect of the drug, and the effect is lower than that of the examples. It shows that the traditional Chinese medicine composition prepared by the present invention by adopting a specific combination of raw materials, dosage and appropriate preparation method can achieve the same therapeutic effect while effectively avoiding the side effects of oral drugs.

[0041] In summary, the drug composition of the present invention has good transdermal absorption effect and no irritation to the skin; the drug composition of the present invention is used to assist the transdermal absorption of drugs, especially for acupoints such as the navel. The drug composition is supplemented with a traditional oral prescription for a certain indication to form a patch, and the patch is used for external application treatment in combination with the corresponding acupoints, and finally the same therapeutic effect can be achieved while effectively avoiding the side effects of oral drugs.

Claims

1. A Chinese medicine composition for promoting transdermal absorption, characterized in that: The raw material components include: 5-15 parts by weight of Evodia rutaecarpa, 5-15 parts by weight of Toosendan fruit, 5-15 parts by weight of Rhizoma Anemarrhenae, 2-8 parts by weight of Cinnamomum cassia bark, 2-8 parts by weight of Phellodendron amurense, and 2-8 parts by weight of Radix Glycyrrhizae Preparata.

2. The Chinese medicine composition for promoting transdermal absorption according to claim 1, characterized in that: The raw material components include: 8-12 parts by weight of Evodia rutaecarpa, 8-12 parts by weight of Toosendan fruit, 8-12 parts by weight of Rhizoma Anemarrhenae, 4-6 parts by weight of Cinnamomum cassia bark, 4-6 parts by weight of Phellodendron amurense, and 4-6 parts by weight of Radix Glycyrrhizae Preparata.

3. The Chinese medicine composition for promoting transdermal absorption according to claim 1, characterized in that: The raw material components include: 10 parts by weight of Evodia rutaecarpa, 10 parts by weight of Toosendan fruit, 10 parts by weight of Rhizoma Anemarrhenae, 5 parts by weight of Cinnamomum cassia bark, 5 parts by weight of Phellodendron amurense and 5 parts by weight of Radix Glycyrrhizae Preparata.

4. The method for preparing the Chinese medicine composition for promoting transdermal absorption according to any one of claims 1 to 3, characterized in that: The steps include: (1) Taking Evodia rutaecarpa, Toosendan fruit and Rhizoma Anemarrhenae according to weight, and crushing them to obtain respective Chinese medicinal powders; (2) fully mixing the Chinese medicinal powders, then adding water for water extraction to obtain a water extract; (3) filtering and concentrating the aqueous extract of step (2) to obtain a concentrate; (4) drying and ultrafine grinding the concentrate in step (3) to obtain ultrafine powder; (5) Cinnamon bark, Phellodendron chinense and Radix Glycyrrhizae Radix are ultrafinely ground respectively, and then added to the ultrafine powder obtained in step (4) in sequence, and mixed thoroughly to obtain the Chinese medicine composition for promoting transdermal absorption.

5. The method for preparing the Chinese medicine composition for promoting transdermal absorption according to claim 4, characterized in that: In step (1), the particle size of each Chinese medicine powder is 80-100 mesh.

6. The method for preparing the Chinese medicine composition for promoting transdermal absorption according to claim 4, characterized in that: In step (2), the mass ratio of the Chinese medicine mixed powder to the added water is 1:4-1:8; and the water extraction treatment time is 1-2h.

7. The method for preparing the Chinese medicine composition for promoting transdermal absorption according to claim 4, characterized in that: In step (3), the concentration is concentrated under reduced pressure to a thick paste with a relative density of 1.30-1.

35.

8. The method for preparing the Chinese medicine composition for promoting transdermal absorption according to claim 4, characterized in that: In step (4) and step (5), the particle size of the ultrafine powder obtained after ultrafine grinding is 800-1200 mesh.

9. The method for preparing the Chinese medicine composition for promoting transdermal absorption according to claim 4, characterized in that: In step (5), vaseline is added to the obtained traditional Chinese medicine composition, and the mixture is thoroughly mixed to obtain an ointment; The mass ratio of the traditional Chinese medicine mixed powder to vaseline is 1:1-1:

2.

10. Use of the Chinese medicine composition according to any one of claims 1 to 3 or the Chinese medicine composition prepared by the method according to any one of claims 3 to 9 in the preparation of a drug for promoting transdermal absorption.

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