CN105534881B - A kind of load roxithromycin nano structured lipid carrier gelling agent and preparation method thereof - Google Patents
A kind of load roxithromycin nano structured lipid carrier gelling agent and preparation method thereof Download PDFInfo
- Publication number
- CN105534881B CN105534881B CN201511013223.2A CN201511013223A CN105534881B CN 105534881 B CN105534881 B CN 105534881B CN 201511013223 A CN201511013223 A CN 201511013223A CN 105534881 B CN105534881 B CN 105534881B
- Authority
- CN
- China
- Prior art keywords
- roxithromycin
- lipid carrier
- structured lipid
- nano structured
- water
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/127—Liposomes
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Molecular Biology (AREA)
- Dermatology (AREA)
- Biophysics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses a kind of load roxithromycin nano structured lipid carrier gelling agents and preparation method thereof, belong to novel technique field, be divided into two and be partially fabricated: one, carrying roxithromycin nano structured lipid carrier: being grouped as by following material weight group: roxithromycin 1-7mg, solid lipid material 45-75mg, liquid fatty substance material 30-60mg, emulsifier 45-300mg, water 5-25mL；Two, it carries roxithromycin nano structured lipid carrier gelling agent: carrying roxithromycin nano structured lipid carrier freeze-dried powder 4-7g, gel-type vehicle 0.01-0.01g, moisturizer 1.0-3.0g, preservative 0.001-0.003g, pH adjusting agent 0.004-0.02g, water 5-15g；By roxithromycin, solid lipid material, liquid fatty substance material ethyl alcohol, emulsifier 45-300mg, water 10-20mL, it is heated to 50-80 DEG C, it is made and carries in roxithromycin content nano structured lipid carrier freeze-dried powder addition gel-type vehicle, it is sufficiently stirred to get roxithromycin nano structured lipid carrier gelling agent is carried.
Description
Technical field
The present invention relates to a kind of load roxithromycin nano structured lipid carrier gelling agents and preparation method thereof, belong to new drug skill
Art field.
Background technique
Roxithromycin (ROXYTHROMYCIN, abbreviation ROX) also known as Luo Xi erythromycin are macrolides antibiosis of new generation
Element, antibacterial action mechanism are to inhibit bacterio protein synthesis, are respiratory tract infection, pharyngitis, laryngitis, skin soft-tissue infection
Choice drug, external application can be used for treating the infection of the suppurative dermatosis such as impetigo and small-area burn, ulcer surface, common Cuo
Sore, epifolliculitis etc..
The study found that roxithromycin belongs to Time dependence antibiotic, the time that antibacterial efficacy is contacted with drug and bacterium
Directly proportional, since roxithromycin has suitable Determination of oil-water partition coefficient, percutaneous permeability is good, easily enters blood circulation, draws
Play the gastrointestinal side effects such as nausea,vomiting,diarrhea.Stop since drug easily penetrates skin, into blood circulation, in part
Time is short, for the roxithromycin with time dependence, and is unfavorable for the performance of drug effect.
Summary of the invention
In order to overcome above-mentioned deficiency, the object of the present invention is to provide a kind of load roxithromycin nano structured lipid carrier gels
Agent and preparation method thereof, a kind of load roxithromycin nano structured lipid carrier gelling agent and preparation method thereof can slowly continue
Drug release increases its hold-up in skin, extends drug treating time, improves bioavilability, is time dependence drug
Skin treating effect is improved, new dosage form selection is provided.
The technical scheme is that a kind of load roxithromycin nano structured lipid carrier gelling agent and preparation method thereof,
It is divided into two to be partially fabricated:
One, roxithromycin nano structured lipid carrier is carried:
It is grouped as by following material weight group:
Roxithromycin 1-7mg, solid lipid material 45-75mg, liquid fatty substance material 30-60mg,
Emulsifier 45-300mg, water 5-25mL；
The solid lipid material is single stearic acid glycerine lipoprotein, bi-tristearin, lecithin, stearic one kind
Or combination；
The liquid fatty substance material is MIGLYOL, isopropyl myristate, soybean oil, castor oil, the acid of medium chain triglyceride three
Ester, pungent/capric acid LABRAFIL M 1944CS is a kind of or combines；
The emulsifier is Gelucire 44/14, Emulsifier EL-60, the poly- hydrocarbon oxygen ester of castor oil, tween
80, F68(Poloxamer188), HS15(Solutol Hs15), polyoxyethylene ether (40) rilanit special,
One kind or combination of Tween 80；
Two, roxithromycin nano structured lipid carrier gelling agent is carried:
It is grouped as by following material weight group:
Carry roxithromycin nano structured lipid carrier freeze-dried powder 4-7g, gel-type vehicle 0.01-0.01g, moisturizer 1.0-
3.0g, preservative 0.001-0.003g, pH adjusting agent 0.004-0.02g, water 5-15g；
The gel-type vehicle is Carbopol or 940.
Moisturizer is propylene glycol.
Penetrating agent is azone.
Preservative is sorbic acid.
Firstly, load roxithromycin nano structured lipid carrier is made in roxithromycin, its step are as follows:
Step 1: solid lipid material 45-75mg, liquid fatty substance material 30-60mg are dissolved in 1- by roxithromycin 1-7mg
5mL ethyl alcohol, is heated to 50-80 DEG C, spare as oily phase；
Step 2: water 10-20mL is heated to 50-80 DEG C, spare as water phase by emulsifier 45-300mg；
Step 3: be mutually slowly added into oil in water phase under 10-800r/min temperature constant magnetic stirring, after being added dropwise to complete,
Continue to stir 10-40min, obtains suspension；Suspension is shifted while hot, and Probe Ultrasonic Searching 1-30min, ultrasonic power 20-
400w；
Step 4: suspension is shifted while hot, and Probe Ultrasonic Searching 1-30min, ultrasonic power 20-400w；
It is carried step 5: suspension to be solidified to 5-60min in ice-water bath to get roxithromycin content nanostructured lipid is carried
Body.
Secondly, making load roxithromycin nano structured lipid carrier gelling agent again, its step are as follows:
Step 1: carrying roxithromycin nano structured lipid carrier solution, in -80 DEG C or less freezing at least 12h, shift rapidly
It is lyophilized under to freeze drier for 24 hours, obtains and carry roxithromycin nano structured lipid carrier freeze-dried powder；
Roxithromycin nano structured lipid carrier freeze-dried powder 4-7g is carried step 2: weighing, is dissolved in 4-7g water to get Luo Hong is carried
Mycin nano structured lipid carrier suspension, it is spare；
Step 3: weighing carbomer powder 0.01-0.01g, 1-11g water is added to be swelled overnight, pH adjusting agent 0.004- is added dropwise
0.02g, adjusting pH value is the blank carbomer matrix that 6-8 is 0.1%-1% to get concentration；
Step 4: 0.001-0.003g sorbic acid and 1.0-3.0g moisturizing agent composition is added to blank carbomer matrix,
Penetrating agent 0-1g, is sufficiently stirred；Complete nanoparticle suspension will be dissolved to be added in above-mentioned gel-type vehicle, be sufficiently stirred, i.e.,
Roxithromycin nano structured lipid carrier gelling agent must be carried.
The beneficial effects of the present invention are: nano structured lipid carrier (NANOSTRUCTRUED lipid CARRIES, NLC)
The lipid materials for using good biocompatibility, toxicity low joined the very big fluid oil of chemical differences for carrier, make nanoparticle with
Crystal defect type or undefined structure exist, and the phenomenon that avoiding or reduce drug efflux in SLN placement process, improve the packet of drug
Envelope rate and stability.Carrier of the NLC as percutaneous drug delivery has following features: 1. slow-releasing and controlled-releasing action can be such that drug ties up for a long time
It holds in effective concentration；2. skin targeting, can promote that Active components enter epidermis through cuticula and to be stranded in epidermis deep layer thin
Born of the same parents and play effect；3. physiological compatibility, the NLC of preparation and skin has good compatibility, it can promote active constituent and exist
It is permeated in skin, useful effect is in the deep layer cells of skin, and lipid is biodegradable, safe and non-toxic；4. closed effect,
One layer of closure film can be formed in skin surface, the evaporation of delaying skin moisture can promote the absorption of active constituent；5. storage is steady
It is qualitative good, it is not susceptible to drug leakage；6. being suitable for industrial mass production.Gelling agent (gel) refer to drug be suitable for it is auxiliary
The transparent or semitransparent semisolid or glop preparation of uniform made of material, suspension or emulsion-type, wherein applying the most
It is widely hydrogel.It is not soluble in water under physiological condition, there is good physiological compatibility.Hydrogel is dimensional network structure,
Drug can be stored, adhesiveness is increased, improves drug local concentration, due to remaining portion of water in the skeleton of hydrogel,
So gel quality is fine and smooth, it is applied to after skin without greasy feeling and irritation, is suitble to local skin external application, is used widely.
Detailed description of the invention
The present invention is further described with reference to the accompanying drawings and detailed description.
Fig. 1 carries roxithromycin nano structured lipid carrier grain size distribution.
Fig. 2 carries roxithromycin nano structured lipid carrier electron microscope.
Fig. 3 carries roxithromycin nano structured lipid carrier DTA figure.
The skin hold-up comparison diagram of Fig. 4 load roxithromycin nano structured lipid carrier gelling agent.
Specific embodiment
A kind of load roxithromycin nano structured lipid carrier gelling agent and preparation method thereof, is divided into two and is partially fabricated:
One, roxithromycin nano structured lipid carrier is carried:
It is grouped as by following material weight group:
Roxithromycin 1-7mg, solid lipid material 45-75mg, liquid fatty substance material 30-60mg,
Emulsifier 45-300mg, water 5-25mL；
The solid lipid material is single stearic acid glycerine lipoprotein, bi-tristearin, lecithin, stearic one kind
Or combination；
The liquid fatty substance material is Miglyol, isopropyl myristate, soybean oil, castor oil, the acid of medium chain triglyceride three
Ester, pungent/capric acid LABRAFIL M 1944CS is a kind of or combines；
The emulsifier is Gelucire 44/14, Emulsifier EL-60, the poly- hydrocarbon oxygen ester of castor oil, tween
80, F68(Poloxamer188), HS15(Solutol Hs15), polyoxyethylene ether (40) rilanit special,
One kind or combination of Tween 80；
Two, roxithromycin nano structured lipid carrier gelling agent is carried:
It is grouped as by following material weight group:
Carry roxithromycin nano structured lipid carrier freeze-dried powder 4-7g, gel-type vehicle 0.01-0.01g, moisturizer 1.0-
3.0g, preservative 0.001-0.003g, pH adjusting agent 0.004-0.02g, water 5-15g；
The gel-type vehicle is Carbopol or 940.
Moisturizer is propylene glycol.
Penetrating agent is azone.
Preservative is sorbic acid.
Firstly, load roxithromycin nano structured lipid carrier is made in roxithromycin, its step are as follows:
Step 1: solid lipid material 45-75mg, liquid fatty substance material 30-60mg are dissolved in 1- by roxithromycin 1-7mg
5mL ethyl alcohol, is heated to 50-80 DEG C, spare as oily phase；
Step 2: water 10-20mL is heated to 50-80 DEG C, spare as water phase by emulsifier 45-300mg；
Step 3: be mutually slowly added into oil in water phase under 10-800r/min temperature constant magnetic stirring, after being added dropwise to complete,
Continue to stir 10-40min, obtains suspension；Suspension is shifted while hot, and Probe Ultrasonic Searching 1-30min, ultrasonic power 20-
400w；
Step 4: suspension is shifted while hot, and Probe Ultrasonic Searching 1-30min, ultrasonic power 20-400w；
It is carried step 5: suspension to be solidified to 5-60min in ice-water bath to get roxithromycin content nanostructured lipid is carried
Body.
Secondly, making load roxithromycin nano structured lipid carrier gelling agent again, its step are as follows:
Step 1: carrying roxithromycin nano structured lipid carrier solution, in -80 DEG C or less freezing at least 12h, shift rapidly
It is lyophilized under to freeze drier for 24 hours, obtains and carry roxithromycin nano structured lipid carrier freeze-dried powder；
Roxithromycin nano structured lipid carrier freeze-dried powder 4-7g is carried step 2: weighing, is dissolved in 4-7g water to get Luo Hong is carried
Mycin nano structured lipid carrier suspension, it is spare；
Step 3: weighing carbomer powder 0.01-0.01g, 1-11g water is added to be swelled overnight, pH adjusting agent 0.004- is added dropwise
0.02g, adjusting pH value is the blank carbomer matrix that 6-8 is 0.1%-1% to get concentration；
Step 4: 0.001-0.003g sorbic acid and 1.0-3.0g moisturizing agent composition is added to blank carbomer matrix,
Penetrating agent 0-1g, is sufficiently stirred；Complete nanoparticle suspension will be dissolved to be added in above-mentioned gel-type vehicle, be sufficiently stirred, i.e.,
Roxithromycin nano structured lipid carrier gelling agent must be carried.
Embodiment 1:
1. carrying roxithromycin nano structured lipid carrier
Precision weighs roxithromycin 1mg, bi-tristearin 75mg, pungent/glycerol decanoate 45mg, soybean lecithin
67mg is dissolved in 1mL ethyl alcohol, and water-bath melts at 75 DEG C, as oily phase；Precision weighs each 80mg of Tween 80, F18, dissolution
In 20mL water, as water phase.Under water bath with thermostatic control magnetic agitation, oil is mutually slowly added into water phase, rate of addition
0.2mL/min after being all added dropwise to complete, continues to stir 30 min, shift while hot, 90 s of Probe Ultrasonic Searching under 20% ultrasonic power,
It is transferred quickly to solidify 20min under ice-water bath, through 0.22 μm of filtering with microporous membrane, obtains roxithromycin nanostructured lipid load
Body.
2. carrying roxithromycin nano structured lipid carrier gelling agent
Preparation, which weighs, carries roxithromycin nano structured lipid carrier freeze-dried powder 4g, is dissolved with 4mL water to get roxithromycin is carried
Nano structured lipid carrier suspension, it is spare；Carbomer powder 0.002g is weighed, 1mL water is added to be swelled overnight, triethylamine 4 is added dropwise
Drop, adjusting pH value is 6-8 to get bare substrate；To blank carbomer matrix, 0.001g sorbic acid, 1g propylene glycol, 0.5g is added
Azone is sufficiently stirred；The good load roxithromycin nano structured lipid carrier suspension of above-mentioned dissolution is added to above-mentioned gel base
In matter, it is sufficiently stirred to get roxithromycin nano structured lipid carrier gelling agent is carried.
Embodiment 2:
1. carrying roxithromycin nano structured lipid carrier
Precision weighs roxithromycin 4mg, bi-tristearin 45mg, pungent/capric acid LABRAFIL M 1944CS 30mg, soybean
Lecithin 67mg is dissolved in 3mL ethyl alcohol, and water-bath melts at 75 DEG C, forms oily phase；It is each that precision weighs Tween 80, F68
38mg is dissolved in 10mL water, forms water phase.Under water bath with thermostatic control magnetic agitation, oil is mutually slowly added into water phase, is added dropwise
Speed 0.2mL/min after being all added dropwise to complete, continues to stir 30 min, is transferred quickly to solidify 30min under ice-water bath, pass through
0.22 μm of filtering with microporous membrane, obtains roxithromycin nano structured lipid carrier.
2. carrying roxithromycin nano structured lipid carrier gelling agent
Preparation, which weighs, carries roxithromycin nano structured lipid carrier freeze-dried powder 5.5g, spare after the dissolution of 7mL water；It weighs
Carbomer powder 0.01g, adds 3mL water to be swelled overnight, and triethylamine 4 is added dropwise and drips, and adjusting pH value is 6-8 to get bare substrate；To sky
White carbomer matrix is added 0.003g sorbic acid, 0.5g propylene glycol, 2g azone, is sufficiently stirred；By the good load Luo Hong of above-mentioned dissolution
Mycin nano structured lipid carrier suspension is added in above-mentioned gel-type vehicle, is sufficiently stirred to get roxithromycin nano junction is carried
Structure lipid carrier gelling agent.
Embodiment 3:
1. carrying roxithromycin nano structured lipid carrier
Precision weighs roxithromycin 7mg, glycerin monostearate 60mg, median chain triglyceride oil 60mg, soybean lecithin
67mg is dissolved in 5mL ethyl alcohol, and water-bath melts at 75 DEG C, forms oily phase；Precision weighs each 150mg of Tween 80, HS15, molten
Solution forms water phase in recipe quantity water.Under water bath with thermostatic control magnetic agitation, oil is mutually slowly added into water phase, rate of addition
0.2mL/min after being all added dropwise to complete, continues to stir 30 min, is transferred quickly to solidify 10min under ice-water bath, through 0.22 μm
Filtering with microporous membrane obtains roxithromycin nano structured lipid carrier.
2. carrying roxithromycin nano structured lipid carrier gelling agent
Preparation, which weighs, carries roxithromycin nano structured lipid carrier freeze-dried powder 7g, is dissolved with 7mL water to get roxithromycin is carried
Nano structured lipid carrier suspension, it is spare；Carbomer powder 0.3g is weighed, 3mL water is added to be swelled overnight, triethylamine 3 is added dropwise and drips,
Adjusting pH value is 6-8 to get bare substrate；To blank carbomer matrix, 0.001g sorbic acid, 3g propylene glycol is added, sufficiently stirs
It mixes；The good load roxithromycin nano structured lipid carrier suspension of above-mentioned dissolution is added in above-mentioned gel-type vehicle, is sufficiently stirred
It mixes to get roxithromycin nano structured lipid carrier gelling agent is carried.
After the above-mentioned roxithromycin nano structured lipid carrier prepared is diluted with water, in Malvern ZETASIZER
Nanoparticle partial size, about 120nm or so are measured under Nano-ZS90.As shown in Figure 1, observing nanoparticle at Hitachi S-576
Fractions distribution, nanoparticle city ellipse, and fractions distribution is uniform；As shown in Fig. 2, in Malvern ZETASIZER Nano-
Nanoparticle partial size, about 45nm or so are measured under ZS90；As shown in figure 3, being physically present using permanent differential thermal analyzer measurement nanoparticle
The fusing point of state, roxithromycin changes, and exists with amorphous forms.
In vitro in transdermal experiment, in vitro mouse part skin is fixed on Franz diffusion cell, stratum corneum side is to confession
To pond, dissolution medium is 17mL20% ethyl alcohol-Tween 80 PBS solution, 32 DEG C of waters bath with thermostatic control, and 600rpm magnetic agitation takes respectively
1g small particle-load roxithromycin nano structured lipid carrier gelling agent (this patent), roxithromycin ordinary gel (control) and big
Partial size-load roxithromycin nano structured lipid carrier gelling agent (control) is uniformly coated on keratoderma.For 24 hours afterwards by skin
It removes, cleans, shred grinding with operating scissors, the roxithromycin being trapped in skin layer is extracted with ethyl alcohol.Simultaneously by small particle-load
Roxithromycin nano structured lipid carrier gelling agent (this patent), roxithromycin ordinary gel (control) and big partial size-load Luo Hong
Mycin nano structured lipid carrier gelling agent (control) is demulsified with ethyl alcohol to be dissolved, i.e., total dose in sample.Samples taken is carried out
Processing measures medicament contg into HPLC.
Conclusion: as shown in Figure 4.The transdermal release difference of three kinds of preparations is compared, the intradermal hold-up of nanoparticle gelling agent is bright
Aobvious to be higher than ordinary preparation, small particle-intradermal hold-up of nano structured lipid carrier carrier gel is apparently higher than big partial size-nano junction
Structure lipid carrier carrier gel.
Claims (6)
1. a kind of load roxithromycin nano structured lipid carrier gelling agent, it is characterised in that: be divided into two and be partially fabricated:
1. carrying roxithromycin nano structured lipid carrier: roxithromycin 1mg, bi-tristearin 75mg, pungent/glycerol decanoate
45mg, soybean lecithin 67mg, ethyl alcohol 1mL, each 80mg of Tween 80, F68, water 20mL；2. carrying roxithromycin nanostructured lipid
Carrier gel: carrying roxithromycin nano structured lipid carrier freeze-dried powder 4g, carbomer powder 0.002g, water 5mL, and triethylamine 4 drips,
Sorbic acid 0.001g, propylene glycol 1g, azone 0.5g.
2. a kind of load roxithromycin nano structured lipid carrier gelling agent, it is characterised in that: be divided into two and be partially fabricated:
1. carrying roxithromycin nano structured lipid carrier: the poly- second two of roxithromycin 4mg, bi-tristearin 45mg, pungent/capric acid
Alcohol glyceride 30mg, soybean lecithin 67mg, ethyl alcohol 3mL, Tween 80, F68 each 38mg, water 10mL；2. carrying roxithromycin nanometer
Structured lipid carrier gel: carrying roxithromycin nano structured lipid carrier freeze-dried powder 5.5g, carbomer powder 0.01g, water 10mL,
Triethylamine 4 drips, sorbic acid 0.003g, propylene glycol 0.5g, azone 2g.
3. a kind of load roxithromycin nano structured lipid carrier gelling agent, it is characterised in that: be divided into two and be partially fabricated:
1. carrying roxithromycin nano structured lipid carrier: roxithromycin 7mg, glycerin monostearate 60mg, three acid of medium chain triglyceride
Ester 60mg, soybean lecithin 67mg, ethyl alcohol 5mL, each 150mg of Tween 80, HS15 and water；2. carrying roxithromycin nanostructure rouge
Matter carrier gel: roxithromycin nano structured lipid carrier freeze-dried powder 7g, carbomer powder 0.3g, water 10mL, triethylamine 3 are carried
Drop, sorbic acid 0.001g, propylene glycol 3g.
4. a kind of preparation method for carrying roxithromycin nano structured lipid carrier gelling agent according to claim 1, special
Sign is:
Roxithromycin nano structured lipid carrier is carried firstly, roxithromycin is made, its step are as follows:
Step 1: by roxithromycin 1mg, bi-tristearin 75mg, pungent/glycerol decanoate 45mg, soybean lecithin 67mg,
It is dissolved in ethyl alcohol 1mL, is heated to 50-80 DEG C, it is spare as oily phase；
Step 2: Tween 80, each 80mg of F68 are added in 20mL water, it is heated to 50-80 DEG C, it is spare as water phase；
Step 3: being mutually slowly added into oil in water phase under 10-800r/min temperature constant magnetic stirring, after being added dropwise to complete, continue
10-40min is stirred, suspension is obtained；
Step 4: suspension is shifted while hot, and Probe Ultrasonic Searching 1-30min, ultrasonic power 20-400w；
Step 5: suspension to be solidified to 5-60min in ice-water bath to get roxithromycin nano structured lipid carrier is carried；
Secondly, making load roxithromycin nano structured lipid carrier gelling agent again, its step are as follows:
It is transferred quickly to cold step 1: carrying roxithromycin nano structured lipid carrier solution in -80 DEG C or less freezing at least 12h
It is lyophilized under lyophilizer for 24 hours, obtains and carry roxithromycin nano structured lipid carrier freeze-dried powder；
Roxithromycin nano structured lipid carrier freeze-dried powder 4g is carried step 2: weighing, is dissolved in 4mL water to get roxithromycin is carried
Nano structured lipid carrier suspension, it is spare；
Step 3: weighing carbomer powder 0.002g, water 1mL being added to be swelled overnight, triethylamine 4 is added dropwise and drips, adjusting pH value is 6-8,
Up to bare substrate；
Step 4: sorbic acid 0.001g and propylene glycol 1g mixture is added, and azone 0.5g is added to blank carbomer matrix,
It is sufficiently stirred；Roxithromycin nano structured lipid carrier suspension is added in above-mentioned gel-type vehicle, is sufficiently stirred to get load
Roxithromycin nano structured lipid carrier gelling agent.
5. a kind of preparation method for carrying roxithromycin nano structured lipid carrier gelling agent according to claim 2, special
Sign is:
Roxithromycin nano structured lipid carrier is carried firstly, roxithromycin is made, its step are as follows:
Step 1: by roxithromycin 4mg, bi-tristearin 45mg, pungent/glycerol decanoate 30mg, soybean lecithin 67mg,
It is dissolved in ethyl alcohol 3mL, is heated to 50-80 DEG C, it is spare as oily phase；
Step 2: Tween 80, each 38mg of F68 are added in 10mL water, it is heated to 50-80 DEG C, it is spare as water phase；
Step 3: being mutually slowly added into oil in water phase under 10-800r/min temperature constant magnetic stirring, after being added dropwise to complete, continue
10-40min is stirred, suspension is obtained；
Step 4: suspension is shifted while hot, and Probe Ultrasonic Searching 1-30min, ultrasonic power 20-400w；
Step 5: suspension to be solidified to 5-60min in ice-water bath to get roxithromycin nano structured lipid carrier is carried；
Secondly, making load roxithromycin nano structured lipid carrier gelling agent again, its step are as follows:
It is transferred quickly to cold step 1: carrying roxithromycin nano structured lipid carrier solution in -80 DEG C or less freezing at least 12h
It is lyophilized under lyophilizer for 24 hours, obtains and carry roxithromycin nano structured lipid carrier freeze-dried powder；
Roxithromycin nano structured lipid carrier freeze-dried powder 5.5g is carried step 2: weighing, is dissolved in 7mL water mould to get Luo Hong is carried
Plain nano structured lipid carrier suspension, it is spare；
Step 3: weighing carbomer powder 0.01g, water 3mL is added to be swelled overnight, triethylamine 4 is added dropwise and drips, adjusting pH value is 6-8, i.e.,
Obtain bare substrate；
Step 4: sorbic acid 0.003g and propylene glycol 0.5g mixture is added, and azone 2g is added to blank carbomer matrix,
It is sufficiently stirred；Roxithromycin nano structured lipid carrier suspension is added in above-mentioned gel-type vehicle, is sufficiently stirred to get load
Roxithromycin nano structured lipid carrier gelling agent.
6. a kind of preparation method for carrying roxithromycin nano structured lipid carrier gelling agent according to claim 3, special
Sign is:
Roxithromycin nano structured lipid carrier is carried firstly, roxithromycin is made, its step are as follows:
Step 1: by roxithromycin 7mg, bi-tristearin 60mg, pungent/glycerol decanoate 60mg, soybean lecithin 67mg,
It is dissolved in ethyl alcohol 5mL, is heated to 50-80 DEG C, it is spare as oily phase；
Step 2: Tween 80, each 150mg of F68 are added to the water, it is heated to 50-80 DEG C, it is spare as water phase；
Step 3: being mutually slowly added into oil in water phase under 10-800r/min temperature constant magnetic stirring, after being added dropwise to complete, continue
10-40min is stirred, suspension is obtained；
Step 4: suspension is shifted while hot, and Probe Ultrasonic Searching 1-30min, ultrasonic power 20-400w；
Step 5: suspension to be solidified to 5-60min in ice-water bath to get roxithromycin nano structured lipid carrier is carried；
Secondly, making load roxithromycin nano structured lipid carrier gelling agent again, its step are as follows:
It is transferred quickly to cold step 1: carrying roxithromycin nano structured lipid carrier solution in -80 DEG C or less freezing at least 12h
It is lyophilized under lyophilizer for 24 hours, obtains and carry roxithromycin nano structured lipid carrier freeze-dried powder；
Roxithromycin nano structured lipid carrier freeze-dried powder 7g is carried step 2: weighing, is dissolved in 7mL water to get roxithromycin is carried
Nano structured lipid carrier suspension, it is spare；
Step 3: weighing carbomer powder 0.3g, water 3mL is added to be swelled overnight, triethylamine 3 is added dropwise and drips, adjusting pH value is 6-8, i.e.,
Obtain bare substrate；
Step 4: sorbic acid 0.001g and propylene glycol 3g mixture is added, is sufficiently stirred to blank carbomer matrix；By Luo Hong
Mycin nano structured lipid carrier suspension is added in above-mentioned gel-type vehicle, is sufficiently stirred to get roxithromycin nano junction is carried
Structure lipid carrier gelling agent.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201511013223.2A CN105534881B (en) | 2015-12-31 | 2015-12-31 | A kind of load roxithromycin nano structured lipid carrier gelling agent and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201511013223.2A CN105534881B (en) | 2015-12-31 | 2015-12-31 | A kind of load roxithromycin nano structured lipid carrier gelling agent and preparation method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105534881A CN105534881A (en) | 2016-05-04 |
| CN105534881B true CN105534881B (en) | 2019-04-05 |
Family
ID=55814815
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201511013223.2A Active CN105534881B (en) | 2015-12-31 | 2015-12-31 | A kind of load roxithromycin nano structured lipid carrier gelling agent and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105534881B (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107115218A (en) * | 2017-05-03 | 2017-09-01 | 中国人民解放军第四军医大学 | A kind of nano-lipid carrier sun protection gel and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102225205A (en) * | 2011-06-17 | 2011-10-26 | 江苏省中医药研究院 | Tripterine nano structure lipid carrier and preparation method and application thereof |
| CN103417481A (en) * | 2012-05-14 | 2013-12-04 | 中国中医科学院中药研究所 | Preparation methods for multiple breviscapinum lipid carriers and gels thereof |
-
2015
- 2015-12-31 CN CN201511013223.2A patent/CN105534881B/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102225205A (en) * | 2011-06-17 | 2011-10-26 | 江苏省中医药研究院 | Tripterine nano structure lipid carrier and preparation method and application thereof |
| CN103417481A (en) * | 2012-05-14 | 2013-12-04 | 中国中医科学院中药研究所 | Preparation methods for multiple breviscapinum lipid carriers and gels thereof |
Non-Patent Citations (1)
| Title |
|---|
| "Roxithromycin-loaded lipid nanoparticles for follicular targeting";Hanna Wosicka-Frackowiak et al.;《International Journal of Pharmaceutics》;20151130;第495卷(第2期);第807-815页 |
Also Published As
| Publication number | Publication date |
|---|---|
| CN105534881A (en) | 2016-05-04 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Chen et al. | Development and evaluation of resveratrol, Vitamin E, and epigallocatechin gallate loaded lipid nanoparticles for skin care applications | |
| Mali et al. | Niosomes as a vesicular carrier for topical administration of minoxidil: formulation and in vitro assessment | |
| Elnaggar et al. | Lecithin-based nanostructured gels for skin delivery: an update on state of art and recent applications | |
| Chen et al. | Evaluation of paeonol-loaded transethosomes as transdermal delivery carriers | |
| Yang et al. | Development of triptolide-nanoemulsion gels for percutaneous administration: physicochemical, transport, pharmacokinetic and pharmacodynamic characteristics | |
| KR101329907B1 (en) | Transdermal absorption accelerator | |
| ElMeshad et al. | Transdermal delivery of an anti-cancer drug via w/o emulsions based on alkyl polyglycosides and lecithin: design, characterization, and in vivo evaluation of the possible irritation potential in rats | |
| Nayak et al. | A comprehensive review on preparation, evaluation and applications of deformable liposomes | |
| Ortan et al. | Rheological study of a liposomal hydrogel based on carbopol | |
| KR101249716B1 (en) | Cosmetic composition comprising double-shell Nano-structure | |
| JPH06183949A (en) | Composition for treatment of acne containing salicylic acid dedivative | |
| CN102665766A (en) | Lipid layer forming composition for administration onto a surface of a living organism | |
| CN1114876A (en) | Use of a spin trap in a cosmetic or dermatological composition | |
| Boskabadi et al. | Topical gel of vitamin A solid lipid nanoparticles: a hopeful promise as a dermal delivery system | |
| KR100949848B1 (en) | Nanoemulsion composition comprising Vitamin-C derivative and method for preparing thereof | |
| CN103893122A (en) | Madecassoside lipidosome and preparation method and application thereof | |
| CN112336649A (en) | Preparation method and product of skin co-permeation carrier of ceramide and fat-soluble active substance | |
| EP2416759A2 (en) | Stable pharmaceutical compositions of diclofenac | |
| Kwon et al. | In vitro skin permeation of cubosomes containing water soluble extracts of Korean barberry | |
| Wu et al. | Cholesterol and phospholipid-free multilamellar niosomes regulate transdermal permeation of a hydrophobic agent potentially administrated for treating diseases in deep hair follicles | |
| CN105534881B (en) | A kind of load roxithromycin nano structured lipid carrier gelling agent and preparation method thereof | |
| WO2021192861A1 (en) | Ionic liquid, solvent, preparation, and transdermally absorbable agent | |
| JPH07108166A (en) | Liposome | |
| KR100757043B1 (en) | Cationic polymer nanocapsules for the enhancement of skin penetration, and the cosmetic composition containing the same | |
| Sangale et al. | Organogel: A novel approach for transdermal drug delivery system |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant |