CN104208042B - A kind of transdermal absorption formulation - Google Patents
A kind of transdermal absorption formulation Download PDFInfo
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- CN104208042B CN104208042B CN201410484374.5A CN201410484374A CN104208042B CN 104208042 B CN104208042 B CN 104208042B CN 201410484374 A CN201410484374 A CN 201410484374A CN 104208042 B CN104208042 B CN 104208042B
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- 239000000203 mixture Substances 0.000 title claims abstract description 25
- 238000010521 absorption reaction Methods 0.000 title claims description 13
- 238000009472 formulation Methods 0.000 title claims description 13
- 150000002576 ketones Chemical class 0.000 claims abstract description 12
- 239000003961 penetration enhancing agent Substances 0.000 claims abstract description 12
- MOTZDAYCYVMXPC-UHFFFAOYSA-N dodecyl hydrogen sulfate Chemical compound CCCCCCCCCCCCOS(O)(=O)=O MOTZDAYCYVMXPC-UHFFFAOYSA-N 0.000 claims abstract description 8
- 229940043264 dodecyl sulfate Drugs 0.000 claims abstract description 8
- 239000010410 layer Substances 0.000 claims description 46
- 239000012790 adhesive layer Substances 0.000 claims description 23
- 239000004820 Pressure-sensitive adhesive Substances 0.000 claims description 19
- 239000011241 protective layer Substances 0.000 claims description 11
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- 229920000915 polyvinyl chloride Polymers 0.000 claims description 8
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- DWNBOPVKNPVNQG-LURJTMIESA-N (2s)-4-hydroxy-2-(propylamino)butanoic acid Chemical compound CCCN[C@H](C(O)=O)CCO DWNBOPVKNPVNQG-LURJTMIESA-N 0.000 claims 1
- 238000002360 preparation method Methods 0.000 abstract description 15
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 abstract description 8
- VPUAYOJTHRDUTK-UHFFFAOYSA-N 1-ethylpyrrole Chemical compound CCN1C=CC=C1 VPUAYOJTHRDUTK-UHFFFAOYSA-N 0.000 abstract 1
- 125000003607 serino group Chemical group [H]N([H])[C@]([H])(C(=O)[*])C(O[H])([H])[H] 0.000 abstract 1
- 239000003814 drug Substances 0.000 description 19
- 230000000052 comparative effect Effects 0.000 description 15
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- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 description 2
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- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical group C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 2
- 229920002367 Polyisobutene Polymers 0.000 description 2
- 239000004372 Polyvinyl alcohol Substances 0.000 description 2
- 241000589517 Pseudomonas aeruginosa Species 0.000 description 2
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- 229910052708 sodium Inorganic materials 0.000 description 2
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- 238000003786 synthesis reaction Methods 0.000 description 2
- DTGKSKDOIYIVQL-WEDXCCLWSA-N (+)-borneol Chemical compound C1C[C@@]2(C)[C@@H](O)C[C@@H]1C2(C)C DTGKSKDOIYIVQL-WEDXCCLWSA-N 0.000 description 1
- REPVLJRCJUVQFA-UHFFFAOYSA-N (-)-isopinocampheol Natural products C1C(O)C(C)C2C(C)(C)C1C2 REPVLJRCJUVQFA-UHFFFAOYSA-N 0.000 description 1
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 1
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 1
- -1 70S compound Chemical class 0.000 description 1
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- 241000588914 Enterobacter Species 0.000 description 1
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- 239000005642 Oleic acid Substances 0.000 description 1
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- 206010035664 Pneumonia Diseases 0.000 description 1
- 241000588769 Proteus <enterobacteria> Species 0.000 description 1
- PYMYPHUHKUWMLA-LMVFSUKVSA-N Ribose Natural products OC[C@@H](O)[C@@H](O)[C@@H](O)C=O PYMYPHUHKUWMLA-LMVFSUKVSA-N 0.000 description 1
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- 241000607764 Shigella dysenteriae Species 0.000 description 1
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- 229920002125 Sokalan® Polymers 0.000 description 1
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- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 1
- 239000005864 Sulphur Substances 0.000 description 1
- 210000001015 abdomen Anatomy 0.000 description 1
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- HMFHBZSHGGEWLO-UHFFFAOYSA-N alpha-D-Furanose-Ribose Natural products OCC1OC(O)C(O)C1O HMFHBZSHGGEWLO-UHFFFAOYSA-N 0.000 description 1
- 229940126575 aminoglycoside Drugs 0.000 description 1
- 239000002647 aminoglycoside antibiotic agent Substances 0.000 description 1
- 229910021529 ammonia Inorganic materials 0.000 description 1
- 230000000845 anti-microbial effect Effects 0.000 description 1
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- 210000003445 biliary tract Anatomy 0.000 description 1
- 210000000988 bone and bone Anatomy 0.000 description 1
- 229940116229 borneol Drugs 0.000 description 1
- CKDOCTFBFTVPSN-UHFFFAOYSA-N borneol Natural products C1CC2(C)C(C)CC1C2(C)C CKDOCTFBFTVPSN-UHFFFAOYSA-N 0.000 description 1
- 229960001631 carbomer Drugs 0.000 description 1
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- 238000009792 diffusion process Methods 0.000 description 1
- DTGKSKDOIYIVQL-UHFFFAOYSA-N dl-isoborneol Natural products C1CC2(C)C(O)CC1C2(C)C DTGKSKDOIYIVQL-UHFFFAOYSA-N 0.000 description 1
- 239000003889 eye drop Substances 0.000 description 1
- 229940012356 eye drops Drugs 0.000 description 1
- 239000004744 fabric Substances 0.000 description 1
- 210000003746 feather Anatomy 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 239000012467 final product Substances 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 1
- 210000005229 liver cell Anatomy 0.000 description 1
- 108020004999 messenger RNA Proteins 0.000 description 1
- 239000012982 microporous membrane Substances 0.000 description 1
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 1
- 230000000149 penetrating effect Effects 0.000 description 1
- 239000008021 pharmaceutical thickening agent Substances 0.000 description 1
- 239000011505 plaster Substances 0.000 description 1
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- 208000013223 septicemia Diseases 0.000 description 1
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Abstract
The application relates to a kind of external application TDS preparation, specifically, being the matrix-type transdermal absorbable preparation with TOB as active component and preparation technology thereof, wherein use the composition of serine, N N-ethyl pyrrole N ketone and sldium lauryl sulfate as penetration enhancer, the part by weight of three is 1:4:6.
Description
Technical field
The application relates to a kind of external application TDS preparation, specifically, is the skeleton with TOB as active component
Type transdermal absorption formulation and preparation technology thereof.
Background technology
TOB is a kind of aminoglycoside medicine, through active transport by bacterial cell membrane, with bacterium ribose
The specific receptor protein combination of body 30S subunit, initial multiple between interference messenger ribonucleic acid and 30S subunit
The formation of compound, suppression albumen synthesis；Make DNA mispronounce, cause the synthesis of non-functioning protein；Make
Polysome divides and loses the function of synthetic proteins.It is clinically used for external eyes caused by sensitive bacterial and attached
The local infection of device.It is compared with other aminoglycoside antibiotics, and antimicrobial spectrum is wider, and curative effect is higher, poison
Property reaction little.Some in staphylococcus aureus in gram positive bacteria, streptococcus etc. and gram-negative bacteria
Serratia marcecens and shigella dysenteriae etc. are all sensitive to TOB.
TOB can be bound up on the coupled position of 30S and 50S, hinders the formation of 70S compound, makes
MRNA can not translate into protein, causes cell death.Mainly to gram-negative bacteria, such as Pseudomonas aeruginosa, big
Enterobacteria, klebsiella bacillus, Enterobacter, proteus, citrobacter are effective.Clinic is mainly used in
The severe infections that sensitive bacterial causes, such as gram-negative bacteria particularly Pseudomonas aeruginosa, Escherichia coli and pneumonia bar
Infection of burn that bacterium etc. cause, septicemia, infection in respiratory system, urinary system infection contamination, gall-bladder infection of biliary tract
And soft tissue severe infections etc..
TOB currently mainly has the formulations such as eye drops, oral formulations, injection to supply Clinical practice, due to
Oral formulations is easily generated first pass effect toxic to liver cell in the gastrointestinal tract, and injection is easily in injection site
Produce pain and lump, and access times are many, easily make patient produce psychological burden.
Traditional black plaster uses inconvenience, and skin irritation is big, and allergic reaction is many.And transdermal drug delivery system tool
There is administration time length, avoid first pass effect, the bad reaction reducing medicine and the advantage such as easy to use, be one
Plant more satisfactory form of administration.Matrix-type transdermal absorbable preparation about TOB does not also have research at present.
Summary of the invention
The present invention is to solve that existing TOB uses inconvenience, the shortcoming of targeting difference, invented appropriate cloth mould
Element matrix-type transdermal absorbable preparation.
The invention provides a kind of pharmaceutical preparation, including TOB.
The invention provides a kind of transdermal absorption formulation, including TOB.
The invention provides a kind of TOB transdermal absorption formulation, including storage layer, adhesive-layer, back sheet
With protective layer four part, storage layer includes that TOB 11-15 part, framework material 50-54 part, infiltration promote
Enter agent 9-12 part and other 1-25 parts.Preferably TOB 12 parts, framework material 52 parts, penetration enhancer 11
Part and pressure sensitive adhesive 1 part.
The preparation method of TOB transdermal absorption formulation is: medicine and penetration enhancer are dispersed in bone
In frame material, it is then placed within the mould fixed or on clean glass plate, plastic film mulch, is dried, demoulding,
Put in reinforcing patch, add up-protective layer and get final product.
Preferably, transdermal absorption formulation of the present invention constitute be followed successively by back sheet, adhesive-layer, storage layer,
Adhesive-layer, storage layer, adherent layer；Or back sheet, adhesive-layer, storage layer, adhesive-layer, adherent layer；Or
Back sheet, adhesive-layer, storage layer, adherent layer；
Described framework material is polyvinyl chloride or polyvinyl alcohol or polyacrylic resin；
Possibly together with penetration enhancer in described storage layer, penetration enhancer be poloxamer, urea, borneol,
N-N-ethyl pyrrole N ketone, sldium lauryl sulfate or oleic acid or their mixture；
Applicants have unexpectedly found that the specific penetration enhancer of employing, and add a small amount of serine, energy wherein
Enough it is obviously enhanced Transdermal absorption effect.Preferably, serine, N-N-ethyl pyrrole N ketone and laruyl alcohol sulfuric acid are used
The composition of sodium is as penetration enhancer, and the part by weight of three is 1:4:6.
Described back sheet and adhesive-layer are reinforcing patch；
Described adhesive-layer surface is additionally provided with adherent layer, and adherent layer is separate paper.Protective layer is separate paper.
Embodiment 1
Including storage layer, adhesive-layer, back sheet and protective layer four part, wherein the drug storehouse layer of storage layer includes
Drug storehouse layer 1 and drug storehouse layer 2 two-layer, drug storehouse layer 1 consist of TOB 6g, polyvinyl chloride 52g, serine
0.5g, N-N-ethyl pyrrole N ketone 2g, sldium lauryl sulfate 4g；Drug storehouse layer 2 consist of TOB 6g, pressure-sensitive
Glue 1g, serine 0.5g, N-N-ethyl pyrrole N ketone 2g, sldium lauryl sulfate 2g；Adhesive-layer includes pressure sensitive adhesive 3g.
Other compositions of the present embodiment are water.Preferably, above-mentioned 1 " g " represents 1 gram.
Preparation method is: after being dissolved by the medicine TOB water in drug storehouse layer 1, with polyvinyl chloride, silk ammonia
Acid, N-N-ethyl pyrrole N ketone, sldium lauryl sulfate mix, and are placed on the glass plate of clean flat smooth,
Making into a film, 60-80 DEG C is dried, demoulding.Pressure sensitive adhesive and thickener are mixed, plastic film mulch on separate paper,
It is dried, as reinforcing patch.By the TOB in medicine layer 2, pressure sensitive adhesive and serine, N-N-ethyl pyrrole N ketone,
Sldium lauryl sulfate mixes, and heats deaeration, is placed in the mould being lined with separate paper, plastic film mulch, removes mould
Tool, is dried 2 hours under the conditions of 80 DEG C, and the film in medicine layer 1 is pasted on the reinforcing patch removing separate paper
On (back sheet), medicine layer 1 and 2 is pasted together by adhesive-layer.Back sheet is pasted on the protection layer,
Cut into 5*6cm2Paster.Every square centimeter of content of dispersion is 0.20-0.30mg.
Pressure sensitive adhesive and thickener selected by the present invention are the conventional use of pressure sensitive adhesive of field of pharmaceutical preparations and thickening
Agent, preferably pressure sensitive adhesive are polyisobutene class pressure sensitive adhesive, specifically, are high molecular weight polyisobutylene (the equal molecules of number
Amount is 120,000～250,000, viscosity average molecular weigh 300,000～1,200,000).Thickener is carbomer.
Comparative example 1
The present embodiment includes storage layer, adhesive-layer, back sheet and protective layer four part, the wherein medicine of storage layer
Storehouse layer includes TOB 12g, polyvinyl chloride 52g, N-N-ethyl pyrrole N ketone 5g, sldium lauryl sulfate 6g, pressure
Quick glue 1g；Adhesive-layer includes pressure sensitive adhesive 3g.Other compositions are water.Every square centimeter of content of dispersion is
0.20-0.30mg。
Preparation method is with embodiment 1.
Comparative example 2
The present embodiment includes storage layer, adhesive-layer, back sheet and protective layer four part, the wherein medicine of storage layer
Storehouse layer includes TOB 12g, polyvinyl alcohol 52g, poloxamer 11g, pressure sensitive adhesive 1g；Adhesive-layer includes pressure
Quick glue 3g.Other compositions are water.Every square centimeter of content of dispersion is 0.20-0.30mg.
Preparation method is with embodiment 1.
Comparative example 3
The present embodiment includes storage layer, adhesive-layer, back sheet and protective layer four part, the wherein medicine of storage layer
Storehouse layer includes TOB 12g, polyvinyl chloride 52g, N-N-ethyl pyrrole N ketone 11g, pressure sensitive adhesive 1g；Adhesive-layer bag
Include pressure sensitive adhesive 3g.Other compositions are water.Every square centimeter of content of dispersion is 0.20-0.30mg.
Preparation method is with embodiment 1.
Comparative example 4
The present embodiment includes storage layer, adhesive-layer, back sheet and protective layer four part, the wherein medicine of storage layer
Storehouse layer includes TOB 12g, polyvinylpyrrolidone 55g, azone 4g, urea 2g, pressure sensitive adhesive 1g；Viscous
Glue-line includes pressure sensitive adhesive 3g.Other compositions are water.Every square centimeter of content of dispersion is 0.20-0.30mg.
Preparation method is with embodiment 1.
Comparative example 5
The present embodiment includes storage layer, adhesive-layer, back sheet and protective layer four part, the wherein medicine of storage layer
Storehouse layer includes TOB 10g, polyvinyl chloride 55g, serine 5g, N-N-ethyl pyrrole N ketone 2g, laruyl alcohol sulphur
Acid sodium 4g, pressure sensitive adhesive 1g；Adhesive-layer includes pressure sensitive adhesive 3g.Other compositions are water.Every square centimeter of content of dispersion
For 0.20-0.30mg.
Preparation method is with embodiment 1.
Illustrating: the auxiliary material used relative to embodiment 1 and consumption, following comparative example has made following amendment:
The penetration enhancer of comparative example 1 does not use serine；
Comparative example 2 uses poloxamer as penetration enhancer；
Comparative example 3 only uses N-N-ethyl pyrrole N ketone as penetration enhancer；
Comparative example 4 uses polyvinylpyrrolidone as framework material, uses azone and urea as infiltration
Accelerator；
Comparative example 5 changes each Ingredient Amount.
The unit of weight that above-described embodiment 1 is used with comparative example 1-5 is identical, and i.e. 1 " part " represents identical
Weight.Preferably, 1 " part " represents 1 gram.
The permeation test in vitro of TOB transdermal absorption formulation
1. skin treatment peels off the skin of abdomen of the 24h mouse that lost hair or feathers, and removes subcutaneous fat, uses physiological saline
Clean and soak, put 4 DEG C of Refrigerator stores standby.
2. the skin handled well is lain in Franz diffusion cell by penetrating absorption, fixing, gives to coyote hole
Giving embodiment 1 and comparative example's 1-5 paster, receiving liquid is physiological saline 6mL, and magnetic stirrer makes mouse
Skin contacts with accepting liquid level, under the conditions of 39 DEG C ± 0.1 DEG C, continuously stirs, and after sample-adding, 7h respectively takes continuously
Sample 2mL, for the mensuration of TOB transdermal amount.Physiological saline 2mL is added after every sub-sampling.Sample is with 0.45
After μm filtering with microporous membrane, taking 20 μ L and carry out HPLC mensuration, replication 3 times, records peak area and calculating contains
Amount.
Accumulative transdermal penetration amount M of different sample points is calculated as follows:
M=CnV+ΣN-1i=1CiVi
In formula, M is accumulative transdermal penetration amount；CnFor sampling the concentration of liquid during each sample point；V is reception tank volume；
CiConcentration for each sample point sampling liquid；ViFor sample volume.
TOB total amount in TOB transdermal penetration rate=TOB transdermal penetration amount × 100%/paster
The results are shown in Table 1.
Control group: include storage layer, adhesive-layer, back sheet and protective layer four part, the wherein medicine of storage layer
Storehouse layer includes TOB 12 parts, polyvinyl chloride 52 parts, pressure sensitive adhesive 1 part；Adhesive-layer includes pressure sensitive adhesive 3 parts.
Other compositions are water.Preparation method is with embodiment 1.
TOB transdermal penetration rate is referred to as TOB transmitance by table 1.
Table 1
From the data in table 1, it can be seen that in comparative example 1-5, TOB transmitance is far below embodiment 1, when 7h
In embodiment 1, TOB transmitance is 84%, and in comparative example 1-5, TOB transmitance is all less than
50%, there is significant difference.As can be seen here, the TOB transdermal absorption formulation choosing that the present invention is claimed
Auxiliary material and consumption be all specific, its effect is the most beat all good.Either auxiliary material type change is also
It is that supplementary product consumption change all can substantially reduce Transdermal absorption effect.
Claims (1)
1. a TOB transdermal absorption formulation, it is characterised in that include storage layer, adhesive-layer, back sheet and
Protective layer four part, storage layer includes TOB 12 parts, framework material 52 parts, penetration enhancer 11 parts
With pressure sensitive adhesive 1 part, by weight, wherein in storage layer, framework material is polyvinyl chloride, and penetration enhancer is silk
Propylhomoserin, N-N-ethyl pyrrole N ketone and the composition of sldium lauryl sulfate, and the part by weight of three is 1:4:6.
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| CN201410484374.5A CN104208042B (en) | 2014-09-19 | 2014-09-19 | A kind of transdermal absorption formulation |
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| CN201410484374.5A CN104208042B (en) | 2014-09-19 | 2014-09-19 | A kind of transdermal absorption formulation |
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| CN104208042B true CN104208042B (en) | 2016-08-31 |
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| CN106509652B (en) * | 2016-11-08 | 2021-02-02 | 雅安职业技术学院 | Method for preparing diced pork in pot by microwave heating sterilization |
| CN107233333A (en) * | 2017-06-12 | 2017-10-10 | 重庆安格龙翔医药科技有限公司 | A kind of epinastine hydrochloride transdermal patch and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002032459A2 (en) * | 2000-10-17 | 2002-04-25 | Massachusetts Institute Of Technology | Method of increasing the efficacy of antibiotics by complexing with cyclodextrins |
| CN1969971A (en) * | 2006-12-01 | 2007-05-30 | 哈尔滨商业大学 | Transdermal absorption formulation of total alkaloid of common monkshood root and preparation process thereof |
| CN102014886A (en) * | 2008-03-07 | 2011-04-13 | Lectec公司 | Hand sanitizing patch |
-
2014
- 2014-09-19 CN CN201410484374.5A patent/CN104208042B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002032459A2 (en) * | 2000-10-17 | 2002-04-25 | Massachusetts Institute Of Technology | Method of increasing the efficacy of antibiotics by complexing with cyclodextrins |
| CN1969971A (en) * | 2006-12-01 | 2007-05-30 | 哈尔滨商业大学 | Transdermal absorption formulation of total alkaloid of common monkshood root and preparation process thereof |
| CN102014886A (en) * | 2008-03-07 | 2011-04-13 | Lectec公司 | Hand sanitizing patch |
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| CN104208042A (en) | 2014-12-17 |
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