CN114712376A - Application of pulsatilla chinensis saponin B4 in preparation of external-use medicine for treating psoriasis - Google Patents
Application of pulsatilla chinensis saponin B4 in preparation of external-use medicine for treating psoriasis Download PDFInfo
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Abstract
The invention belongs to the medicine technology, and particularly relates to an application of pulsatilla chinensis saponin B4 in preparation of a medicine for treating psoriasis. In recent years, researches on some traditional Chinese medicines and active ingredients separated from the traditional Chinese medicines show that the traditional Chinese medicines have the effects of clearing heat and cooling blood, promoting blood circulation to remove blood stasis, nourishing blood and moistening dryness as main materials, and have the anti-psoriasis effects of different degrees on both a traditional Chinese medicine formula for tonifying spleen and promoting diuresis, and detoxifying and resolving masses and a single traditional Chinese medicine, but the effect of the traditional Chinese medicines needs to be improved. The invention prepares the pulsatilla chinensis saponin B4 as an active ingredient into an externally applied medicament for the first time, is convenient to use, and avoids side effects while exerting better treatment effect than the existing western medicines.
Description
Technical Field
The invention belongs to the medicine technology, and particularly relates to application of pulsatilla saponin B4 in preparation of an external medicine for treating psoriasis.
Background
Psoriasis is also called as psoriasis, is an inflammatory persistent dermatosis, is a common intractable chronic inflammatory dermatosis in dermatology, is characterized by difficult cure, long-lasting course of disease, easy recurrence of disease, frequently causes complications such as psoriatic arthritis, psoriatic cardiovascular and cerebrovascular complications, metabolic syndrome and the like, and often brings physical pain and large economic burden to patients. The pathogenesis of the disease is believed to be caused by the interaction of the immune system, self-antigens and various environmental factors, and is related to the induction factors of infection, trauma, environment, drugs and the like. Psoriasis is characterized pathologically by epidermal hyperplasia caused by hyperproliferation of keratinocytes and is manifested by a variety of phenotypes including psoriasis vulgaris, pustular psoriasis, erythrodermic psoriasis, and arthropathic forms. Psoriasis may develop multiple phenotypes in the same person. Symptoms common to all phenotypes may include itching, burning and soreness. The severity of psoriasis can be assessed using the area and severity of the psoriatic lesion (PASI). The PASI comprises four parts of area, erythema, scale and infiltration degree.
For a long time, the research on the pathogenesis of psoriasis mainly focuses on T cells, and at present, the clinical treatment medicines for psoriasis are mainly summarized into 5 major groups: oral medicine, topical medicine, physiotherapy, natural plant medicine and biological preparation. The side effects of the medicines are different, and the oral administration and the external application are often accompanied with skin atrophy, red swelling, stabbing pain, pruritus and burning sensation; physical therapy greatly increases the prevalence of skin cancer in patients; emerging biologics are mainly targeted to moderate to severe patients, often with severe infections and high prices, and clinical applications are limited. Therefore, the search for economic medicaments with less side effects has important significance for clinically treating psoriasis. In recent years, traditional Chinese medicines have become hot spots for research on psoriasis treatment medicines.
In recent years, researches on some traditional Chinese medicines and active ingredients separated from the traditional Chinese medicines show that the traditional Chinese medicines have the effects of clearing heat and cooling blood, promoting blood circulation to remove blood stasis, nourishing blood and moistening dryness as main materials, and have the anti-psoriasis effects of different degrees on both a traditional Chinese medicine formula for tonifying spleen and promoting diuresis, and detoxifying and resolving masses and a single traditional Chinese medicine. For example, one of the effective components of cortex Magnolia officinalis is magnolol, which can inhibit the expression of VEGFR-2 in skin tissue and treat psoriasis. Ginsenoside which is active in intestinal tract hydrolysis metabolizes compound K, inhibits activation of T cells, reduces differentiation of Th17 cells, inhibits expression of REG3A/Reg III g, and slows excessive proliferation of keratinocytes to relieve psoriasis skin damage. Artesunate of artemisinin derivative which is a traditional heat-clearing and detoxifying drug in China has pharmacological action of antimalarial effect, and recently, artesunate is found to be capable of reducing the thickening degree of the epidermis of a psoriasis mouse model. In addition, active ingredients extracted from many traditional Chinese medicines, such as polysaccharide, polyphenol, saponin and the like also have the effect of resisting the psoriasis skin damage. However, the effect of the existing traditional Chinese medicine needs to be improved, and compared with the conventional western medicine, the traditional Chinese medicine is poor in effect.
Disclosure of Invention
Pulsatillae radix (Pulsatilla chinensis (Bunge) Regel) is a root of a plant of Pulsatilla of Ranunculaceae. It is originally recorded in Shen nong Ben Cao Jing (Shen nong's herbal Jing), enters stomach and large intestine meridians, has the effects of cooling blood, stopping dysentery, clearing heat and removing toxicity, etc., is the essential drug for treating bloody dysentery, and is widely used for treating bacillary dysentery, amoebic dysentery and malignant tumors. According to the chemical components of pulsatilla chinensis, which contains triterpenic acid, triterpenoid saponin, lignan, daucosterol and the like, comprehensive researches show that pulsatilla chinensis has toxicity to digestive systems, such as burning, pain, red swelling, nausea, vomiting, abdominal pain, diarrhea, serious patients or even hematochezia, so that the pulsatilla chinensis needs to be taken as internal medicine with caution and the harm of toxicity needs to be considered. Unlike other extracts, the molecular weight of the pulsatilla saponin B4 is 1220, the structure contains 5-molecule sugar, the prior art considers that the pulsatilla saponin B4 is difficult to permeate a skin barrier, and the pulsatilla saponin B4 has good water solubility and is not suitable for transdermal administration, so any prior art report of transdermal administration is not found; the invention overcomes the prejudice of the prior art, creatively designs various external administration forms for skin, is used for local administration of psoriasis, and has the advantages of obvious drug effect and small toxic and side effect. Particularly, the invention avoids the problems of obvious side effect and large dosage of oral administration, and the external administration treatment effect is obviously superior to the existing clinical administration, thereby obtaining unexpected technical effect.
The invention discloses application of pulsatilla chinensis saponin B4 (Anemoside B4) in preparation of a medicament for treating psoriasis.
The invention discloses an application of pulsatilla saponin B4 in preparing a medicine for treating skin erythema; the skin erythema is caused by psoriasis.
The invention discloses an application of pulsatilla saponin B4 in preparing a medicament for treating scales; the scales are caused by psoriasis.
The invention discloses an application of pulsatilla saponin B4 in preparing a medicament for treating skin damage and hypertrophy; the skin lesions are hypertrophic due to psoriasis.
The invention discloses application of pulsatilla saponin B4 in preparing a medicine for improving weight loss caused by psoriasis.
The invention discloses a medicine for treating psoriasis, the active component of which is pulsatilla saponin B4; and the composition also can comprise conventional pharmaceutical auxiliary materials, including one or more of diluent, dispersant, adhesive, lubricant and penetration enhancer.
The medicament for treating psoriasis is an external medicament, and the dosage form of the medicament comprises one or more of solution, gel, patch, paste, emulsion and film agent. Compared with other administration modes such as oral administration, the pulsatilla saponin B4 disclosed for the first time has the advantages of convenience and safety in administration as an external medicament for treating psoriasis, particularly, the problems of obvious side effect and large dosage of oral administration are solved, the external administration treatment effect is obviously superior to that of the existing clinical administration, and an unexpected technical effect is achieved. For example, the medicine for treating psoriasis takes the pulsatilla saponin B4 as an active ingredient, does not contain other pulsatilla extracts, and can obtain better technical effect than the halometasone cream which is considered to have good effect at present by small-dose administration. Preferably, in the psoriasis treatment drug of the present invention, the anemonin B4 is administered in an amount of less than 5mg/kg d, for example, 1 to 4.5mg/kg d, preferably 1 to 4mg/kg d, and more preferably 3 to 3.5mg/kg d. Animal experiment results show that the anemonin B4 has a protective effect on psoriasis skin lesion change, and the effect is better than that of glucocorticoid medicaments.
The psoriasis treating medicine may be solution of pulsatilla saponin B4, transdermal gelata of pulsatilla saponin B4, transdermal ointment of pulsatilla saponin B4, transdermal patch of pulsatilla saponin B4, transdermal microemulsion of pulsatilla saponin B4 and transdermal film spraying agent of pulsatilla saponin B4. The solution of the pulsatilla saponin B4 can be a pulsatilla saponin B4 aqueous solution (only pulsatilla saponin B4 is added into water), or a pulsatilla saponin B4 aqueous solution added with auxiliary materials, wherein the auxiliary materials are conventional substances such as glycerol, sodium benzoate, essence and the like; the anemonin B4 skin gel comprises conventional adjuvants such as carbomer, glycerol, propylene glycol, water, etc. in addition to anemonin B4; pulsatillae saponin B4 the skin ointment contains conventional adjuvants such as stearic acid, glyceryl monostearate, liquid paraffin, white vaseline, water, etc. in addition to Pulsatillae saponin B4; pulsatillae saponin B4 skin patch contains conventional adjuvants such as sodium polyacrylate, tranexamic acid, aluminum glycollate, EDTA (ethylene diamine tetraacetic acid), water, etc. besides Pulsatillae saponin B4; pulsatillae saponin B4 the microemulsion for skin comprises conventional adjuvants such as oleic acid, tween, auxiliary emulsifier, water, etc. in addition to Pulsatillae saponin B4; pulsatillae saponin B4 the skin spray film agent comprises conventional adjuvants such as polyvinylpyrrolidone, hydroxypropyl methylcellulose, water, etc. in addition to Pulsatillae saponin B4. In each dosage form, the dosage of the auxiliary materials is conventional technology, and the requirement of common external medicines is met.
The pulsatilla chinensis saponin B4 is used as the only active ingredient and is externally smeared on the psoriasis part to realize the effective treatment of the psoriasis, and furthermore, the medicine does not contain other pulsatilla chinensis extracts. The Chinese pulsatilla saponin B4 is firstly used as an active ingredient to prepare an externally applied medicament, so that the Chinese pulsatilla saponin B4 is convenient to use, and the side effect is avoided while the better treatment effect is exerted compared with the existing western medicine.
Drawings
FIG. 1 is a photograph of the skin on the back of a mouse within 7 days of administration.
Figure 2 is the PASI score of mice given 7 days of administration.
Figure 3 is the mouse erythema score for 7 days of dosing.
Figure 4 is the mouse scale score for 7 days of dosing.
Figure 5 is a mouse thickening score for 7 days of dosing.
FIG. 6 shows the body weight change of mice after 7 days of administration.
FIG. 7 is a graph of HE staining of skin in mice dosed for 7 days.
FIG. 8 is the mouse erythema score for 7 days following dosing (B5).
Detailed Description
The medicine for treating psoriasis can be a solution of pulsatilla saponin B4, a gel of pulsatilla saponin B4 for skin, an ointment of pulsatilla saponin B4 for skin, a skin patch of pulsatilla saponin B4, a microemulsion of pulsatilla saponin B4 for skin and a film spraying agent of pulsatilla saponin B4 for skin. The solution of the pulsatilla saponin B4 can be a pulsatilla saponin B4 aqueous solution (only pulsatilla saponin B4 is added into water), or a pulsatilla saponin B4 aqueous solution added with auxiliary materials, wherein the auxiliary materials are conventional substances such as glycerol, sodium benzoate, essence and the like; the anemonin B4 skin gel comprises conventional adjuvants such as carbomer, glycerol, propylene glycol, water, etc. in addition to anemonin B4; pulsatillae saponin B4 the skin ointment contains conventional adjuvants such as stearic acid, glyceryl monostearate, liquid paraffin, white vaseline, water, etc. in addition to Pulsatillae saponin B4; pulsatillae saponin B4 skin patch contains conventional adjuvants such as sodium polyacrylate, tranexamic acid, aluminum glycollate, EDTA (ethylene diamine tetraacetic acid), water, etc. besides Pulsatillae saponin B4; pulsatillae saponin B4 the microemulsion for skin comprises conventional adjuvants such as oleic acid, tween, auxiliary emulsifier, water, etc. in addition to Pulsatillae saponin B4; pulsatillae saponin B4 the skin spray film agent comprises conventional adjuvants such as polyvinylpyrrolidone, hydroxypropyl methylcellulose, water, etc. in addition to Pulsatillae saponin B4. In each dosage form, the dosage of the auxiliary materials is conventional technology, and the auxiliary materials meet the requirements of common external medicines, and are taken as examples:
pulsatillae saponin B4 gel for skin application. Carbomer 940 was weighed, sprinkled into distilled water, allowed to stand overnight, and allowed to swell sufficiently. Dissolving glycerol and propylene glycol in distilled water, pouring into the fully swelled carbomer 940, adding the pulsatilla chinensis saponin B4 aqueous solution, fully stirring, adding 10% sodium hydroxide solution, adjusting the pH value to 6.1-6.5, and adding distilled water to a fixed amount of 100 g to obtain the pulsatilla chinensis saponin B4 gel. The final concentration of each component is 40.1-2% of pulsatilla saponin B, 9400.2-2% of carbomer, 0.5-2% of glycerol and 0.5-2% of propylene glycol.
Pulsatillae saponin B4 can be made into skin ointment. Weighing stearic acid, glyceryl monostearate, liquid paraffin and white vaseline, heating and melting in 70 deg.C water bath to obtain oil phase, weighing Pulsatillae saponin B4 powder, glycerol and distilled water, heating and melting in 70 deg.C water bath to obtain water phase. Then pouring the water phase into the oil phase under stirring to obtain ointment, and obtaining the pulsatilla saponin B4W/O type ointment transdermal preparation. The final concentration of each component is 40.5-1.5% of pulsatilla saponin B, 2-8% of stearic acid, 5-20% of glyceryl monostearate, 5-20% of liquid paraffin, 5-20% of white vaseline and 5-15% of glycerol.
Pulsatillae saponin B4 skin patch. Weighing sodium polyacrylate, tranexamic acid, dihydroxyaluminium aminoacetate and EDTA, adding into glycerol, stirring, adding water for dissolving, adding Pulsatillae saponin B4 powder, stirring to obtain medicinal layer, coating the medicinal layer on the back lining layer to prevent adhesion of release film as surface covering layer, and cutting to obtain Pulsatillae saponin B4 patch. The final concentration of each component is 40.5-1.5% of pulsatilla saponin B, 20-30% of sodium polyacrylate, 2-8% of tranexamic acid, 2-5% of dihydroxyaluminium glycinate, 0.1-0.5% of EDTA and 40-50% of glycerol.
Pulsatillae saponin B4 microemulsion for skin application. Respectively taking oleic acid and tween-80, mixing uniformly to obtain an oil phase, precisely weighing a proper amount of pulsatilla saponin B4, dissolving in distilled water to obtain a water phase, dropwise adding the water phase into the oil phase at room temperature, simultaneously dropwise adding co-emulsifier ethanol, magnetically stirring for 15 min, and ultrasonically removing bubbles until the solution is a clear thick liquid to obtain the microemulsion. The final concentration of each component is 40.2-1% of pulsatilla saponin B, 50-60% of oleic acid, 5-20% of tween-8015 and 15-20% of ethanol.
Pulsatillae saponin B4 skin solution added with adjuvants. Accurately weighing the pulsatilla chinensis saponin B4 powder, adding distilled water for dissolving, adding glycerol, sodium benzoate and rose essence for mixing, and adding water to 1000mL to obtain the solution of pulsatilla chinensis saponin B4. The final concentration of each component is 40.5-1% of pulsatilla saponin B, 5-10% of glycerol, 0.05-0.5% of sodium benzoate and a proper amount of rose essential oil. Can be applied to skin by smearing or spraying.
Pulsatillae saponin B4 spray for skin. Accurately weighing the pulsatilla chinensis saponin B4 powder, adding distilled water for dissolving, adding the polyvinylpyrrolidone K30 and the hydroxypropyl methylcellulose for uniformly mixing, and adding water to 1000mL to obtain the pulsatilla chinensis saponin B4 film spraying agent. The final concentration of each component is 40.5-2% of pulsatilla saponin B, 302-6% of polyvinylpyrrolidone K and 0.1-0.6% of hydroxypropyl methylcellulose.
The pulsatilla chinensis saponin B4 is an existing substance, an animal experiment and treatment effect analysis are an existing method, and the experimental requirements of animals of Suzhou university are met.
In order to explore the effect of pulsatilla chinensis saponin on the improvement of mouse skin lesions, experiments are designed by taking an aqueous solution of pulsatilla chinensis saponin B4 as an example, and pulsatilla chinensis saponin B4 is added into water to prepare aqueous solutions of pulsatilla chinensis saponin B4 of 0.1 mg/ml and 0.33mg/ml respectively. Dividing 25 Balb/c mice into a normal control group, a model group, a halometasone positive drug group (5 mg/kg), a pulsatilla saponin low dose group (1 mg/kg) and a pulsatilla saponin high dose group (3.3 mg/kg) according to the weight at random, wherein each group comprises 5 mice. 3 days before modeling, depilatory cream and a shaver are used for depilating on the back of the mouse within the range of 2cm multiplied by 3cm, and on the day of modeling, the depilatory condition on the back of the mouse is observed for secondary depilating. About 62.5mg of imq cream (5%, imiquimod) was applied to the skin on the back of the mice except the normal control group, and an equal amount of petrolatum was applied to the back of the normal control group mice. Halometasone (0.1 g/mouse) is smeared with halomethasone cream 4 hours after the imiquimod of the group. After the administration group had been molded with imiquimod, 0.1ml of an aqueous solution of B4 (0.1 mg/ml and 0.33mg/ml, respectively) was applied 4 hours later. 0.1ml of pure water was applied 4 hours after the mold was assembled. And 7 d of continuous treatment. Skin lesion changes were recorded by digital photography at the same time period daily, and the mice were observed for the presence of characteristic changes in psoriasis, such as erythema, hypertrophy of skin lesions, and scaling, on the back, and a PASI score was recorded.
The method for scoring the severity degree of psoriasis-like dermatitis (PASI) of the mice comprises the steps of evaluating the severity degree of skin damage of a back unhairing region of the mice by adopting a visual observation method and evaluating according to a psoriasis skin damage area and severity degree evaluation method (PASI) which is commonly used in the prior art. According to the characteristics of erythema, scaling and pachynsis of the skin, the evaluation of each characteristic is 0-4 points according to the severity, wherein the evaluation is 0= none, 1= mild, 2= moderate, 3= severe and 4= extremely severe, and the evaluation standard is shown in a table 1.
Example effect of Pulsatillae saponin B4 on PASI score in psoriasis mice
The experimental results show that after imiquimod is applied, compared with the blank group, the skin of the model group has erythema, scale and infiltration, and generates psoriasis-like skin lesions. With the continuous action of the medicine, the skin damage of the model group becomes serious from the 2 nd day, scales are increased and thickened, the skin infiltration is obvious, and the PASI comprehensive scoring results of the control group and the model group have statistical significance in 3-7 days (P < 0.01), which indicates that the psoriasis mouse model is successfully established. Compared with a model group, the skin of the pulsatilla saponin high-dose group has the advantages that the skin damage symptom is obviously relieved, the skin is smooth, almost no erythema or scale is generated, and the infiltration thickening is light; the group of halomethasone positive drugs has slightly reddened skin, less scales and less infiltration thickening (see fig. 1). Wherein the difference result of the PASI comprehensive scores of the high dose group and the model group has statistical significance in 3-7 days (P < 0.01); the PASI comprehensive score difference between the positive medicine group and the model group has statistical significance in 4-7 days (P < 0.01), and the PASI comprehensive score difference between the low-dose group and the model group has statistical significance only in 5 days (P < 0.05); the high-dose group and the Halometasone positive medicine group PASI comprehensive score have statistical significance in 5 (P < 0.05) and 6-7 days (P < 0.01) (see figure 2). The experimental result indicates that the pulsatilla saponin has a protective effect on psoriasis skin lesion change caused by imiquimod and has a better effect than glucocorticoid effect.
Example Effect of Pulsatillae radix saponin B4 on erythema score in psoriatic mice
The erythema on the back of the mice in the model group and the low dose group appears from the 3 rd day after the administration, the erythema score is increased day by day until the curative effect observation period of the 7 th day, the back of the mice in the halomethasone administration group slightly becomes reddish from the 2 nd day after the administration until the erythema begins to subside in the curative effect observation period of the 7 th day, and the skin of the mice in the high dose group hardly has erythema. Wherein, the difference of erythema scores of the model group and the control group in 3 to 7 days (P < 0.01) has statistical significance, the difference result of erythema scores of the high-dose group and the model group in 3 to 7 days (P < 0.01) has statistical significance, the erythema scores of the positive medicine group and the model group in 2 days (P < 0.05) and 5 to 7 days (P < 0.01) have statistical significance, and the erythema scores of the low-dose group and the model group in only 5 days have statistical significance (P < 0.05); the erythema scores of the high-dose group and the halometasone positive medicine group have statistical significance in 2 (P < 0.05) and 6-7 days (P < 0.01) (see figure 3). The experimental result indicates that the anemoside can obviously reduce the erythema degree of psoriasis mice and has better effect than glucocorticoid effect.
Example Effect of Tripulsatillae radix Saponin B4 on Scale score in psoriasis mice
The back scales of the model group and the low-dose group of mice appear from the day 4 after the administration, the scores of the back scales are increased day by day until the curative effect observation period of the day 7, while the back scales of the high-dose group of mice only appear fine scales after the day 7 after the administration, and no scales appear in the day 7 after the administration of the positive drug. Wherein, the difference of the scale scores of the model group and the control group in 4 th to 5 th (P < 0.05) days (P < 0.01) has statistical significance, and the difference result of the scale scores of the high dose group and the model group in 6 th to 7 th days (P < 0.01) has statistical significance; the positive medicine group and the model group have statistical significance in 4-5 days (P < 0.05) and 6-7 days (P < 0.01), and the scale score of the low-dose group and the model group has no statistical significance; the scale scores of the high dose group and halometasone positive group were not statistically significant (see fig. 4). The experimental result indicates that the pulsatilla chinensis saponin can obviously reduce the scale degree of psoriasis mice, and the effect is equivalent to that of glucocorticoid.
Example Effect of Pulsatillae saponin B4 on the thickening score in psoriatic mice
The thickening of the skin damage on the back of the mice in the model group and the low-dose group starts to appear from the 3 rd day after the administration, the thickening score is increased day by day until the curative effect observation period of the 7 th day, and the thickening of the skin on the back of the mice in the positive medicine group is lighter than that of the model group; while the dorsal skin lesions of the high dose group mice only appeared slightly thickened from day 6 after the administration. Wherein, the thickening score difference of the model group and the control group on 3 days (P < 0.05) and 4-7 days (P < 0.01) has statistical significance, and the thickening score difference of the high-dose group and the model group on 3 days (P < 0.05) and 4-7 days (P < 0.01) has statistical significance; the positive medicine group and the model group have statistical significance on 4 days (P < 0.05) and 5-7 days (P < 0.01), and the thickening score of the low-dose group and the model group has statistical significance on 5 days (P < 0.01) and 7 days (P < 0.05); the erythema scores of the high-dose group and the halometasone positive medicine group have statistical significance on 5 th to 6 th (P < 0.05) and 7 th (P < 0.01) (see figure 5). The experimental result indicates that the pulsatilla saponin B4 can obviously reduce the thickening degree of psoriasis mice, and the effect is better than that of glucocorticoid.
Example Effect of Pulsatillae radix saponin B4 on body weight in psoriasis mice
The weight average of the control group, the model group and each administration group was decreased within 5 days of administration, and thereafter the body weight was increased day by day until the observation period of the therapeutic effect on day 7. Compared with a control group, the weight of the model group and the weight of the positive medicine group are reduced obviously, wherein the weight difference between the model group and the control group has statistical significance in 2-8 days; the weight difference between the high-dose group and the model group has statistical significance in 2-8 days (P < 0.01); the weight difference between the positive medicine group and the model group has statistical significance on 5 days (P < 0.05) and 6-8 days (P < 0.01), and the weight difference between the low-dose group and the model group has no statistical significance; the weight difference between the high-dose group and the halometasone positive medicine group has statistical significance in 2-8 days (P < 0.01) (see figure 6). The experimental result shows that the pulsatilla saponin can obviously improve the psoriasis mouse weight loss induced by imiquimod, the glucocorticoid has obvious side effect, and the body weight reduction is especially obvious in seven days after the drug is taken, even exceeds that of a model group.
Example Effect of Pulsatillae radix saponin B4 on changes in skin pathology in psoriasis mice
And (4) observing and comparing the lesion degree of the skin tissue on the back of the mouse under a microscope after HE staining. Compared with the normal group, the skin damage epidermis of the mouse in the model group is obviously thickened and the characteristic pathological changes of psoriasis such as obvious hyperkeratosis, parakeratosis, spongiform edema, vasodilation, obvious hyperemia and the like are observed under an optical microscope. The high dose group of pasqueflower saponin B4 reduced epidermal thickening, and reduced hyperkeratosis, parakeratosis and acanthosis hypertrophy (fig. 7). The pulsatilla chinensis saponin B4 is proved to have good treatment effect on psoriasis.
Comparative example pulsatilla saponin B5 scoring of psoriasis mouse erythema
The treatment effect of the pulsatilla chinensis saponin B4 is replaced by pulsatilla chinensis saponin B5, and the treatment effect is shown in figure 8, and more results are shown in the application previously filed by the applicant.
EXAMPLE seven
In the above embodiment, the aqueous solution of pulsatilla saponin B4 is used to fully illustrate the significant effect of the external drug of pulsatilla saponin B4 on psoriasis, and besides the solution dosage form, other dosage forms can also achieve the significant effect of the external drug of pulsatilla saponin B4 on psoriasis; unless otherwise specified, the concentrations referred to are mass concentrations.
Pulsatillae saponin B4 gel for skin application. Carbomer 940 was weighed, sprinkled into distilled water, allowed to stand overnight, and allowed to swell sufficiently. Dissolving glycerol and propylene glycol in distilled water, pouring into the fully swelled carbomer 940, adding the pulsatilla chinensis saponin B4 aqueous solution, fully stirring, adding 10% sodium hydroxide solution to adjust the pH value to 6.3, and adding distilled water to a fixed amount of 100 g to obtain the pulsatilla chinensis saponin B4 gel. The final concentration of each component is 41% of pulsatilla saponin B, 9401% of carbomer, 1% of glycerol and 1% of propylene glycol.
Pulsatillae saponin B4 can be made into skin ointment. Weighing stearic acid, glyceryl monostearate, liquid paraffin and white vaseline, heating and melting in 70 deg.C water bath to obtain oil phase, weighing Pulsatillae saponin B4 powder, glycerol and distilled water, heating and melting in 70 deg.C water bath to obtain water phase. Then pouring the water phase into the oil phase under stirring to obtain ointment, and obtaining the pulsatilla saponin B4W/O type ointment transdermal preparation. The final concentration of each component is 41% of pulsatilla saponin B, 5% of stearic acid, 10% of glyceryl monostearate, 10% of liquid paraffin, 10% of white vaseline and 10% of glycerol.
Pulsatillae saponin B4 skin patch. Weighing sodium polyacrylate, tranexamic acid, dihydroxyaluminium aminoacetate and EDTA, adding into glycerol, stirring, adding water for dissolving, adding Pulsatillae saponin B4 powder, stirring to obtain medicinal layer, coating the medicinal layer on the back lining layer to prevent adhesion of release film as surface covering layer, and cutting to obtain Pulsatillae saponin B4 patch. The final concentration of each component is anemonin B41%, sodium polyacrylate 25%, tranexamic acid 5%, aluminum glycollate 3%, EDTA 0.3%, and glycerin 45%.
Pulsatillae saponin B4 microemulsion for skin application. Respectively taking oleic acid and tween-80, mixing uniformly to obtain an oil phase, precisely weighing a proper amount of pulsatilla saponin B4, dissolving in distilled water to obtain a water phase, dropwise adding the water phase into the oil phase at room temperature, simultaneously dropwise adding co-emulsifier ethanol, magnetically stirring for 15 min, and ultrasonically removing bubbles until the solution is a clear thick liquid to obtain the microemulsion. The final concentration of each component is 40.5% of pulsatilla saponin B, 55% of oleic acid, 8020% of tween-and 15% of ethanol.
Pulsatillae saponin B4 skin solution added with adjuvants. Accurately weighing the pulsatilla chinensis saponin B4 powder, adding distilled water for dissolving, adding glycerol, sodium benzoate and rose essence for mixing, and adding water to 1000mL to obtain the solution of pulsatilla chinensis saponin B4. The final concentration of each component is 40.5% of pulsatilla saponin B, 5% of glycerol, 0.5% of sodium benzoate and 0.3% of rose essential oil.
Pulsatillae saponin B4 spray for skin. Accurately weighing the pulsatilla chinensis saponin B4 powder, adding distilled water for dissolving, adding the polyvinylpyrrolidone K30 and the hydroxypropyl methylcellulose for uniformly mixing, and adding water to 1000mL to obtain the pulsatilla chinensis saponin B4 film spraying agent. The final concentration of each component is pulsatilla saponin B41%, polyvinylpyrrolidone K305%, and hydroxypropyl methylcellulose 0.5%.
Experiments are carried out by referring to the high-dose group (3.3 mg/kg) of the water solution of the pulsatilla saponin B4, and the pulsatilla saponin B4 solution, the pulsatilla saponin B4 gel for skin, the pulsatilla saponin B4 ointment for skin, the pulsatilla saponin B4 skin patch, the pulsatilla saponin B4 microemulsion for skin and the pulsatilla saponin B4 spray film agent which are added with auxiliary materials can obtain better curative effects than the existing medicines.
Claims (10)
1. The application of the pulsatilla chinensis saponin B4 in preparing the medicine for treating psoriasis is characterized in that the medicine for treating psoriasis is an external medicine.
2. The application of the pulsatilla chinensis saponin B4 in preparing medicines for treating skin erythema, or the application of the pulsatilla chinensis saponin B4 in preparing medicines for treating scales, or the application of the pulsatilla chinensis saponin B4 in preparing medicines for treating skin hypertrophy, or the application of the pulsatilla chinensis saponin B4 in preparing medicines for improving weight loss.
3. Use according to claim 2, characterized in that said cutaneous erythema is caused by psoriasis; the scales are caused by psoriasis; the skin damage is hypertrophic due to psoriasis; the weight loss is caused by psoriasis.
4. The use of claim 2, wherein the medicament is a topical medicament.
5. The use according to claim 1 or 2, wherein the medicament comprises anemonin B4 and conventional pharmaceutical excipients.
6. The use according to claim 5, wherein the conventional pharmaceutical excipients comprise one or more of diluents, dispersants, binders, lubricants, penetration enhancers.
7. The use of claim 1 or 2, wherein the medicament is in a dosage form of one or more of solution, gel, patch, paste, emulsion and film.
8. A topical medicine for the treatment of psoriasis contains Pulsatillae saponin B4 as active ingredient.
9. The external medicine for treating psoriasis according to claim 8, wherein the external medicine for treating psoriasis takes pulsatilla saponin B4 as the only active ingredient.
10. The external medicine for treating psoriasis according to claim 8, wherein the dosage form of the medicine comprises one or more of solution, gel, patch, ointment, emulsion and film.
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| PCT/CN2022/126910 WO2023168948A1 (en) | 2022-03-09 | 2022-10-24 | Use of pulsatilla chinensis saponin b4 in preparation of topical drug for treating psoriasis |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2023168948A1 (en) * | 2022-03-09 | 2023-09-14 | 苏州大学 | Use of pulsatilla chinensis saponin b4 in preparation of topical drug for treating psoriasis |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20160019772A (en) * | 2014-08-12 | 2016-02-22 | 주식회사 엘지생활건강 | Cosmetic or pharmaceutical composition for skin whitening or anti-inflammation comprising pulchinenoside B4 |
| CN112370461A (en) * | 2020-12-04 | 2021-02-19 | 广西馨海药业科技有限公司 | Application of pulsatilla saponin B4 in preparation of medicine for treating hemorrhoids |
| CN114159453A (en) * | 2021-12-24 | 2022-03-11 | 广西馨海药业科技有限公司 | Application of pulsatilla chinensis saponin B4 in preparation of medicine for treating or preventing psoriasis |
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| CN114712376A (en) * | 2022-03-09 | 2022-07-08 | 苏州大学 | Application of pulsatilla chinensis saponin B4 in preparation of external-use medicine for treating psoriasis |
| CN114796248B (en) * | 2022-05-16 | 2024-04-12 | 广西馨海药业科技有限公司 | Pulsatilla saponin composition and application thereof in preparation of medicines for treating skin diseases |
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- 2022-04-22 CN CN202210430851.4A patent/CN114712376A/en active Pending
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20160019772A (en) * | 2014-08-12 | 2016-02-22 | 주식회사 엘지생활건강 | Cosmetic or pharmaceutical composition for skin whitening or anti-inflammation comprising pulchinenoside B4 |
| CN112370461A (en) * | 2020-12-04 | 2021-02-19 | 广西馨海药业科技有限公司 | Application of pulsatilla saponin B4 in preparation of medicine for treating hemorrhoids |
| CN114159453A (en) * | 2021-12-24 | 2022-03-11 | 广西馨海药业科技有限公司 | Application of pulsatilla chinensis saponin B4 in preparation of medicine for treating or preventing psoriasis |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2023168948A1 (en) * | 2022-03-09 | 2023-09-14 | 苏州大学 | Use of pulsatilla chinensis saponin b4 in preparation of topical drug for treating psoriasis |
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