CN105560331A - Eczematous dermatitis prevention medicine, and preparation method and application thereof - Google Patents

Abstract

The invention discloses an eczematous dermatitis prevention medicine, and a preparation method and an application thereof. The medicine mainly comprises, by mass, 16-24% of purslane, 16-24% of honeysuckle flower, 0.5-1.2% of carbomer 940, 0.8-2.5% of azone, 0.8-4% of propylene glycol, 2-16% of glycerol, and the balance of water, and the sum of mass percentages of above components is 100%. The czematous dermatitis prevention medicine is uniform and fine; the medicine has good biocompatibility, so a transparent film can be formed after the medicine is coated on skins, and can be closely adhered to an action position for a long time; and the medicine has the advantages of good bio-adherence, fast medicine release, long detention time, easy absorption and no tight coverage after local administration, oily feeling, easy washing removal, no pollution to clothes, good stability, generation of sustained release, controlled release and pulsed release of medicine effects, no irritation to skins or mucous membranes, comfortable use, and suitableness for local external use on skins.

Description

A kind of medicine for anti-dermatitis and eczema and its preparation method and application

Technical field

The invention belongs to medicine and preparing technical field, be specifically related to a kind of medicine for anti-dermatitis and eczema, the invention still further relates to the preparation method and application of this medicine.

Background technology

Dermatitis and eczema is clinical common a kind of repeated relapsing chronic dermatosis, and be a kind of hypersensitivity inflammatory dermatoses, sickness rate is high, and global child morbidity rate is 10% ~ 20%; Eczema is suffered to the surveyee that the investigation of population shows 10.7% by U.S. 2007; The investigation eczema prevalence of China in the same year community's population is 7.5%; China's prevalence is relatively low but also have the trend increased gradually.The course of disease is longer.Primary disease poor prognosis, 85% recurrence, is difficult to radical cure, and the cause of disease is complicated, treats thorny, and patient's pruritus is obvious, has a strong impact on patients ' life quality.

The current Drug therapy for dermatitis and eczema mainly concentrates on the symptomatic treatment of hormone and Loratadine, effect is undesirable, easily cause the side effect such as atrophoderma, telangiectasis, pigmentation more obvious, simultaneously, glucocorticoid can suppress epidermis lipid synthesis, destroy horny layer integrity, thus destruction skin barrier function, cause the generation of subsequent inflammation.Separately, treatments period medicine repeatedly, life-time service, be very easy to make disease progression or heavy de novo common factors, especially infant because of skin delicate, horny layer space is large, and Transdermal absorption is higher, and prolonged application impact is grown, and produces hormone and rely on.Therefore research and develop curative effect certainly and the less anti-dermatitis and eczema medicine of side effect become clinical urgent needs.

Summary of the invention

The object of this invention is to provide a kind of medicine for anti-dermatitis and eczema, solve the undesirable and obvious problem of side effect of existing medication effect.

Another object of the present invention is to provide a kind of preparation method of the medicine for anti-dermatitis and eczema.

3rd object of the present invention is to provide a kind of application of said medicine.

The technical solution adopted in the present invention is, a kind of medicine for anti-dermatitis and eczema, key component comprises by mass percentage: Herba Portulacae 16% ~ 24%, Flos Lonicerae 16% ~ 24%, Acritamer 940 0.5% ~ 1.2%, permeation enhancers azone 0.8% ~ 2.5%, propylene glycol 0.8% ~ 4%, glycerol 2% ~ 16%, surplus is water, and said components mass percent sum is 100%.

Second technical scheme of the present invention is, a kind of preparation method of the medicine for anti-dermatitis and eczema is specifically implemented according to following steps:

Step 1, take Herba Portulacae 16% ~ 24% respectively by mass percentage, Flos Lonicerae 16% ~ 24%, Acritamer 940 0.5% ~ 1.2%, permeation enhancers azone 0.8% ~ 2.5%, propylene glycol 0.8% ~ 4%, glycerol 2% ~ 16%, surplus is water, and above constituent mass percentage ratio sum is 100%;

Step 2, Herba Portulacae, Flos Lonicerae powder are broken into coarse powder, and Herba Portulacae is colourless to siphon with the ethanol continuous circumfluence extraction of 8 times amount 80%, and Flos Lonicerae is colourless to siphon with 6 times amount 60% ethanol continuous circumfluence extractions, then merge mixing by adding water after extracting solution solvent recovery and form mixed solution, Acritamer 940 is evenly spread on mixed solution surface, and placing spends the night makes it fully swelling, then adds glycerol, propylene glycol, permeation enhancers azone, is finally adjusted to 6.8 ~ 7.0 with triethanolamine by pH, obtains final product.

3rd technical scheme of the present invention is, said medicine is used for the application of anti-dermatitis and eczema.

The invention has the beneficial effects as follows,

1. the present invention is used for the medicine of anti-dermatitis and eczema, for transparent semisolid, homogeneous exquisiteness, as novel external preparation, owing to having good biocompatibility, be coated on skin and can form transparent thin film, can for a long time with site of action close adhesion, there is good bioadhesive, release is fast, holdup time is long, be easy to after topical absorb, without unhappy, greasy feeling, easy eccysis, not pollution clothes, good stability, especially slow release can be produced, controlled release and pulsed release effect, to skin and mucosa nonirritant, use comfortable, be applicable to local skin external.

2. the present invention is used for the preparation method of the medicine of anti-dermatitis and eczema, Herba Portulacae of the present invention is extracted with penetration power strong, extracts scope wide, high safety, the weak ethanol of toxic and side effects is extractant, technique is simple, gel prescription agents useful for same and adjuvant safety, stable preparation process, be easy to industrialization, prepare gained finished product and be easy to coating, homogeneous exquisiteness, and have no adverse reaction.

Detailed description of the invention

Below in conjunction with detailed description of the invention, the present invention is described in detail.

A kind of medicine for anti-dermatitis and eczema of the present invention, key component comprises by mass percentage: Herba Portulacae 16% ~ 24%, Flos Lonicerae 16% ~ 24%, Acritamer 940 0.5% ~ 1.2%, permeation enhancers azone 0.8% ~ 2.5%, propylene glycol 0.8% ~ 4%, glycerol 2% ~ 16%, surplus is water, and said components mass percent sum is 100%.

External treatment side's medicine has long history and origin in China, famous with features such as its good effect, few side effects, convenience are suitable for.

External treatment with Chinese medicine side's medicine is the important component part of TCM Recipe medicine, it is instruct with Basic Theories of Chinese Medicine, by medicament administration in positions such as skin, hole key, Yu caves, to play its dredging the meridian, regulate QI and blood, eliminating toxic substances to remove stasis, the effects such as strengthening vital QI to eliminate pathogenic factors, make unbalanced negative and positive of qi and blood be readjusted or improve, thus promote the recovery of body function, reach object of curing the disease.

Theory of Chinese medical science thinks that dermatitis and eczema is that damp and hot heresy is heavily steamed, and visitor in skin, and produces the symptoms such as decortication, ulcer.In treatment, the medicine of heat-clearing and toxic substances removing, expelling wind and removing dampness should be selected.Chinese medicine is thought, Herba Portulacae is a kind of natural Chinese medicine of curing food homology, and it is cold in nature, and sweet in the mouth acid, has heat-clearing and toxic substances removing, cooling blood for hemostasis, effect that dehumidifying is treating stranguria; Flos Lonicerae property sweet cold, gas is fragrant, has effect of dispelling wind-heat, heat-clearing and toxic substances removing.Two taste medicine synergism and reach the merit of heat-clearing and toxic substances removing, expelling wind and removing dampness.In two medicines, Herba Portulacae is monarch drug, and Flos Lonicerae is ministerial drug.

Modern pharmacological research shows, Herba Portulacae is containing abundant vitamin, protein, flavone, polysaccharide various active composition, be used for multicomponent in external jointly to play a role, Herba Portulacae is because containing abundant vitamin A, can promote that epithelial physiological function is tending towards normal, promote the healing of skin lesion, and have significant contraction to blood vessel; Polysaccharide from Portulaca oleracea, protein can play the effects such as nutrition, antioxidation, moisturizing to the pachylosis caused by dermatitis and eczema, drying, promote that caused by dermatitis and eczema, skin damage heals rapidly, plays the natural cover for defense effect of skin; Herba Portulacae can also improve cellular immune function.Effective ingredient in Flos Lonicerae has antibacterial, antivirus action, and Flos Lonicerae can promote lymphocyte transformation, strengthens leukocytic phagocytic function, improves body immunity.Papillary, can work in coordination with many-side and improve disease, promotes skin healing.

Usage and dosage:

External, 1 time on the one, spreads upon affected part and the surrounding skin thereof of clean dried.

The preparation method of the above-mentioned medicine for anti-dermatitis and eczema, specifically implement according to following steps:

Step 1, take Herba Portulacae 16% ~ 24% respectively by mass percentage, Flos Lonicerae 16% ~ 24%, Acritamer 940 0.5% ~ 1.2%, permeation enhancers azone 0.8% ~ 2.5%, propylene glycol 0.8% ~ 4%, glycerol 2% ~ 16%, surplus is water, and above constituent mass percentage ratio sum is 100%;

Step 2, Herba Portulacae, Flos Lonicerae powder are broken into coarse powder, and Herba Portulacae is colourless to siphon with the ethanol continuous circumfluence extraction of 8 times amount 80%, and Flos Lonicerae is colourless to siphon with 6 times amount 60% ethanol continuous circumfluence extractions, then merge mixing by adding water after extracting solution solvent recovery and form mixed solution, Acritamer 940 is evenly spread on mixed solution surface, and placing spends the night makes it fully swelling, then adds glycerol, propylene glycol, permeation enhancers azone, is finally adjusted to 6.8 ~ 7.0 with triethanolamine by pH, obtains final product.

(1) Transdermal absorption experiment

(1) laboratory animal

SPF level ICR mice, 6-8 week age, body weight at 18-22g (purchased from The Fourth Military Medical University's Experimental Animal Center, SCXK (Shan) 2014-002), fasting 24h before experiment, but freely intake, test in Xi'an Medical University's pharmacological evaluation room (SYXK (Shan) 2010-002), and empirically animal uses 3R principle to give human care.

(2) preparation of rat skin in vitro

The neck that broken by mice is put to death, the clip back of the body, skin of abdomen immediately, the skin taken off is laid on clean glass plate, skin surface hair razor is shaved totally, and horny layer, carefully peels off subcutaneous layer of fat and connective tissue down, repeatedly rinse well with normal saline, be soaked in normal saline, and save backup in cryogenic refrigerator, tested in 1 week.The integrity of visual examination Corium Mus before each experiment, can not have any breakage.

(3) for the configuration of feeding

Containing the normal saline of 20% ethanol, get 4.5gNaCl, be mixed with the normal saline of 500ml0.9%NaCl; The normal saline prepared and dehydrated alcohol are mixed in proportion, obtain the normal saline containing 20% ethanol.

(4) penetrating absorption

Diffusion device is rectilinear Franz diffusion cell.From refrigerator, take out skin for subsequent use, blot the moisture on surface with filter paper, skin is fixed on Franz diffusion cell that (diffuser casing area is 2.27cm ²volume is 6.5mL), make stratum corneum side upwards, fix with alligator clamp, normal saline (about 6.5mL) containing 20% ethanol is filled it up with as receiving liquid in reception tank, in diffuser casing, add each gel prescription 0.5ml, with 37 DEG C of water bath heat preservations, magnetic stir bar stirs with the speed of 200r/min.One group in 1,2,4,6,8,12h takes out 2mL receiving liquid in receiving chamber, exist together mutually and add the fresh receiving liquid of isothermal equivalent all immediately, detect for ultraviolet spectrophotometry.

(5) content detection of flavone in receiving liquid

2ml receiving liquid is placed in 5ml volumetric flask, adds 5% sodium nitrite 0.2ml and shake up, leave standstill 6min; Add 10% aluminum nitrate 0.2ml again, shake up, leave standstill 6min; Add 4.3%NaOH solution 2.0ml again, be settled to 5ml with 75% ethanol, shake up, place 15min, survey absorbance at λ=506nm place.Experimental result shows, the cumulant of prescription III is maximum, and transdermal effect is best, is optimum prescription.The results are shown in Table 1.

Table 1 drug transdermal experiment 1-12h cumulant result (n=4) of the present invention

(2) anti-dermatitis and eczema experiments in vivo

(1) preparation of experiment reagent

7% dinitrochlorobenzene (DNCB): get dinitrochlorobenzene 70mg, is placed in clean dry 10ml volumetric flask, is settled to scale with acetone;

0.1% dinitrochlorobenzene (DNCB): get dinitrochlorobenzene 25mg, is placed in clean dry 25ml volumetric flask, is settled to scale with acetone; Therefrom pipette 1ml solution in 10ml volumetric flask, be settled to scale with acetone;

(2) laboratory animal

Select the SPF level mice 20 of male and female half and half, body weight 18g-22g, purchased from Xi'an Jiaotong University Medical College's Experimental Animal Center.Raise in Xi'an Medical University basis and translational medicine institute animal experimental center, room temperature controls at 20 DEG C-25 DEG C, and humidity is at 30%-60%, constant ventilation, sub-cage rearing, controls illumination round the clock, avoid too much noise and other interference, give mouse feed and raise, drinking-water adopts tap water not limit.

(3) experimental drug and grouping

Herba Portulacae gel (make by oneself, lot number: 20150315) by pharmaceutical analysis teaching and research room; By 42 SPF level mices by different prescription be divided at random 5 experimental grouies, positive controls, blank group.

(4) the copying of acute eczema animal model

Mice is fetched rear adaptability and feeds 1-2 days, temperature 20-24 DEG C.Test first 1 day, select 3cm × 3cm size area to shave hair in mouse back; Test the 1st day, draw 100 μ L7%DNCB and be coated with mice outward and shave a mao back sensitization; Test the 2nd day, same procedure coating sensitization again; Test beginning in the 6th day, excite with outer painting 5 μ L0.1%DNCB inside mouse right ear, interval repeats to excite once for three days, excites for totally four times; Excite rear 24h, 48h, 72h to observe mouse ear back dermatitis and eczema situation of change at every turn, then give relative medicine treatment respectively.

(5) administration

After modeling, start drug treatment, experimental group: smear Herba Portulacae gel 0.05mL inside auris dextra, continue to make it even in 1 minute; Herba Portulacae gel 0.4mL is smeared at back, continues to make it even in 3 minutes; Positive controls smears hydrocortisone butyrate ointment by with experimental group same procedure to mouse ear, back; Not administration after the modeling of blank group.

(6) measurement that the collection gill of otic tissues is thick

Within after last drug withdrawal 1 day, put to death mice with cervical dislocation; Fast along auricle baseline clip ear, vernier caliper measurement two auricle thickness, calculates the difference of two auricle thickness;

(7) result

A Mice Auricle left and right ear thickness difference

Table 2 is group experiment mice left and right ear thickness difference (n=3) respectively

As shown in Table 2, experimental group maximum left and right ear thickness difference is prescription 1, namely 0.174 ± 0.02 μm, minimum left and right ear thickness difference is prescription 2, namely 0.048 ± 0.057 μm, positive controls 0.146 ± 0.0408 μm falls between, blank group 0.262 ± 0.137 μm, obviously be greater than experimental group and positive controls, illustrative experiment group has ear's swelling and obviously alleviates effect.

B back skin lesion

A. symptom score standard, as shown in table 3

Table 3 skin of back Syndrome Scale table

Skin lesion recovery situation in back when b. having treated

Perusal mouse back excites area skin to occur acute eczema sample outward appearance, and show as erythema in various degree, edema, hair is lived again, incrustation.To exciting also drug treatment to complete period after successful from mouse skin modeling, the recovery situation of the symptom of the inflammation skin part of mice and recovery time aspect effect be better than blank group, close in symptom compared with positive controls, but be obviously better than positive controls falling on the crust time; Draw optimal treatment medicine at this point.Show Herba Portulacae gel, to dermatitis and eczema, there is obvious therapeutical effect.Can show that prescription 5 is excellent by table 4.

Back skin lesion recovery situation table when table 4 has been treated

As shown in Table 4, when terminating treatment, experimental group erythema, hair is lived again and more blank group of decrustation experimental group has obvious recovery, close with positive controls, and experimental group-prescription 5 on the time of decrustation comparatively positive controls obviously shift to an earlier date, experiment shows that Herba Portulacae gel recovers the skin symptom of dermatitis and eczema to have obvious therapeutical effect.

B. skin injury table recovery time, as shown in table 5

Table 5 skin injury table recovery time

C. back recovery scoring, as shown in table 6.

The recovery scoring of table 6 back

Herba Portulacae gel test group can alleviate the edema at model mice dermatitis and eczema position, alleviate the tissue inflammation pathological change at eczema position, in anti-inflammatory, effect is better than blank group, lower slightly in anti-inflammatory compared with matched group, but in the hair of recovered part is lived again, experimental group is better than matched group; Experiment shows that Herba Portulacae gel has obvious therapeutical effect to dermatitis and eczema.

Embodiment 1

Step 1, takes Herba Portulacae 16% by mass percentage respectively, Flos Lonicerae 20%, Acritamer 940 0.8%, permeation enhancers azone 2.5%, propylene glycol 0.8%, glycerol 2%, and surplus is water, and above constituent mass percentage ratio sum is 100%;

Step 2, Herba Portulacae, Flos Lonicerae powder are broken into coarse powder, and Herba Portulacae is colourless to siphon with the ethanol continuous circumfluence extraction of 8 times amount 80%, and Flos Lonicerae is colourless to siphon with 6 times amount 60% ethanol continuous circumfluence extractions, then merge mixing by adding water after extracting solution solvent recovery and form mixed solution, Acritamer 940 is evenly spread on mixed solution surface, and placing spends the night makes it fully swelling, then adds glycerol, propylene glycol, permeation enhancers azone, is finally adjusted to 6.8 ~ 7.0 with triethanolamine by pH, obtains final product.

Embodiment 2

Step 1, takes Herba Portulacae 20% by mass percentage respectively, Flos Lonicerae 24%, Acritamer 940 1.2%, permeation enhancers azone 0.8%, propylene glycol 2.5%, glycerol 16%, and surplus is water, and above constituent mass percentage ratio sum is 100%;

Step 2, Herba Portulacae, Flos Lonicerae powder are broken into coarse powder, and Herba Portulacae is colourless to siphon with the ethanol continuous circumfluence extraction of 8 times amount 80%, and Flos Lonicerae is colourless to siphon with 6 times amount 60% ethanol continuous circumfluence extractions, then merge mixing by adding water after extracting solution solvent recovery and form mixed solution, Acritamer 940 is evenly spread on mixed solution surface, and placing spends the night makes it fully swelling, then adds glycerol, propylene glycol, permeation enhancers azone, is finally adjusted to 6.8 ~ 7.0 with triethanolamine by pH, obtains final product.

Embodiment 3

Step 1, takes Herba Portulacae 24% by mass percentage respectively, Flos Lonicerae 16%, Acritamer 940 0.5%, permeation enhancers azone 1.6%, propylene glycol 4%, glycerol 10%, and surplus is water, and above constituent mass percentage ratio sum is 100%;

Step 2, Herba Portulacae, Flos Lonicerae powder are broken into coarse powder, and Herba Portulacae is colourless to siphon with the ethanol continuous circumfluence extraction of 8 times amount 80%, and Flos Lonicerae is colourless to siphon with 6 times amount 60% ethanol continuous circumfluence extractions, then merge mixing by adding water after extracting solution solvent recovery and form mixed solution, Acritamer 940 is evenly spread on mixed solution surface, and placing spends the night makes it fully swelling, then adds glycerol, propylene glycol, permeation enhancers azone, is finally adjusted to 6.8 ~ 7.0 with triethanolamine by pH, obtains final product.

Claims (3)

1. the medicine for anti-dermatitis and eczema, it is characterized in that, key component comprises by mass percentage: Herba Portulacae 16% ~ 24%, Flos Lonicerae 16% ~ 24%, Acritamer 940 0.5% ~ 1.2%, permeation enhancers azone 0.8% ~ 2.5%, propylene glycol 0.8% ~ 4%, glycerol 2% ~ 16%, surplus is water, and said components mass percent sum is 100%.

2. for a preparation method for the medicine of anti-dermatitis and eczema, it is characterized in that, specifically implement according to following steps:

Step 1, take Herba Portulacae 16% ~ 24% respectively by mass percentage, Flos Lonicerae 16% ~ 24%, Acritamer 940 0.5% ~ 1.2%, permeation enhancers azone 0.8% ~ 2.5%, propylene glycol 0.8% ~ 4%, glycerol 2% ~ 16%, surplus is water, and above constituent mass percentage ratio sum is 100%;

Step 2, Herba Portulacae, Flos Lonicerae powder are broken into coarse powder, and Herba Portulacae is colourless to siphon with the ethanol continuous circumfluence extraction of 8 times amount 80%, and Flos Lonicerae is colourless to siphon with 6 times amount 60% ethanol continuous circumfluence extractions, then merge mixing by adding water after extracting solution solvent recovery and form mixed solution, Acritamer 940 is evenly spread on mixed solution surface, and placing spends the night makes it fully swelling, then adds glycerol, propylene glycol, permeation enhancers azone, is finally adjusted to 6.8 ~ 7.0 with triethanolamine by pH, obtains final product.

3. a medicine as claimed in claim 1 is used for the application of anti-dermatitis and eczema.