CN1186659A - Compound smoking-refraining adhesive sheet absorbed through skin - Google Patents
Compound smoking-refraining adhesive sheet absorbed through skin Download PDFInfo
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- CN1186659A CN1186659A CN98111814A CN98111814A CN1186659A CN 1186659 A CN1186659 A CN 1186659A CN 98111814 A CN98111814 A CN 98111814A CN 98111814 A CN98111814 A CN 98111814A CN 1186659 A CN1186659 A CN 1186659A
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Abstract
The present invention is smoking-refraining medicinal preparation and features its special physical shape. The adhesive sheet is one four-layer structure including lining layer, medicine layer, adhesive layer and protecting layer. Its medicine layer contains nicotine or its salt, clonidine or its salt, or Lovastatin or its salt, and medicine osmosis promoter and its adhesive layer may contain local steroid antiphlogistic. The present invention has high smoking-refraining effect and less side effect.
Description
The invention belongs to medicine, be specifically related to contain organic effective ingredient is shaped as feature again with specific physical smoking cessation pharmaceutical product.
Smoking is harmful to your health is people's common recognition.Being cherish life, also is the civilization and the progress of society, gives up the eager desire that craving for tobacco has become numerous smokers.For this reason, smoking cessation with medicine after various oral formulations and ejection preparation, have the 3rd class dosage form-percutaneous absorption patch to appear on the market in recent years again, by widely used both at home and abroad be nicotine percutaneous plaster (Nicotine Transdermal Patch) and clonidine percutaneous plaster (Clonidine Transdermal Patch).The effective ingredient of these two kinds of percutaneous plasters is the one pack system medicine, and use can only accomplish to alleviate the symptom of nicotine withdrawal syndrome separately, promptly only has the effect that alleviates craving for tobacco, is difficult to thoroughly eradicate craving for tobacco, and successful quitting rate is very low.The Chinese invention patent application that it is CN1144088A that there was a publication number on March 5th, 1997 is open, what it was introduced is a kind of Clonidine Patch and the compound method of giving up smoking of nicotine patch, be that Clonidine Patch and nicotine patch are used in a kind of employing simultaneously, the method that control clonidine burst size combines with adjusting nicotine burst size.The essence of the prior art only is the improvement to existing medicine (Clonidine Patch and nicotine patch) using method, rather than the innovation of medicine; It is compared with independent use nicotine patch or Clonidine Patch method, and the smoking cessation effect improves, but its using method is loaded down with trivial details, two medicine rate of release are asynchronous, the course of treatment long (continuing for 5 weeks), application cost height, big to skin irritation, still can not reach best smoking cessation effect.
The objective of the invention is at the deficiencies in the prior art, utilize the synergistic function of multicomponent pharmaceutical, it is better to design a kind of smoking cessation effect, short treating period, pair little, easy to use, the low-cost compound percutaneous absorption adhesive patch of effect.
Realize the object of the invention by the following technical solutions.
Compound smoking-refraining adhesive sheet absorbed through skin of the present invention, include backing layer, drug storehouse layer, adhesion layer and protective layer four-layer structure, drug storehouse layer is a host material with polyisobutylene 200-500mg, include nicotine or its salt 5-120mg (nicotine burst size 5-30mg/d), clonidine or its salt 0.1-6.0mg (clonidine burst size 0.075-0.5mg/d) or lofexidine (Lofexidine) or its salt 0.2-12mg (lofexidine burst size 0.15-1mg/d) and account for the penetrating agent of drug storehouse layer 1%-2% (weight); Adhesion layer is a Polyisobutylene PSA, includes the local steroidal anti-inflammatory drugs 0-2.5mg that uses; Backing layer and protective layer are aluminum-plastic composite membrane, and wherein the silication of protective layer inner face is antiseized.
The active drug composition (principal agent) of compound smoking-refraining adhesive sheet absorbed through skin of the present invention is nicotine or its salt, clonidine or its salt or lofexidine or its salt.Their compound use not only has synergistic function to the smoking cessation effect, and the effect of paying of each medicine also had partial antagonism, for example nicotine has excitation to nervus centralis and cardiovascular system, and clonidine or lofexidine are inhibited to this; Clonidine or lofexidine suppress the secretion of saliva and are directed at thirsty discomfort, and the secretion that nicotine but can saliva stimulating is to offset the former effect of paying.In adhesion layer, add local purpose and be to alleviate the zest of principal agent Transdermal absorption skin with steroidal anti-inflammatory drugs, thereby eliminate the skin irritation reaction of smoking cessation paster, it is an ancillary drug, the most handy fluocinonide (Fluocinonide) or halcinonidedcorten (Halcinonide), or Triamcinolone acetonide acetate (Triamcinolone acetonide).The used Polyisobutylene PSA of polyisobutylene host material that drug storehouse layer is used and adhesion layer all has controlled-release function to principal agent and accessory drugs, skin can slowly be absorbed, to keep effective blood concentration.The most handy Laurel nitrogen of medicine penetrating agent ketone.
With laboratory animal (rat) paster of the present invention and excipient, nicotine patch and Clonidine Patch have been simulation craving for tobacco (nicotine dependence) contrast experiment, its experimental data such as following table:
| Group | Number of rats | Nicotine is intake initiatively | Compare between group | Significant difference | |
| mg/Kg.d | Slip | ||||
| [1] excipient matched group | ????11 | ?0.35±0.12 | ??0％ | [1]∶[2] | P＜0.10 |
| [2] nicotine patch treatment group | ????14 | ?0.25±0.16 | ?27.1％ | [2]∶[4] | P＜0.01 |
| [3] Clonidine Patch treatment group | ????14 | ?0.24±0.10 | ?31.4％ | [3]∶[4] | P＜0.001 |
| [4] patch treatment group of the present invention | ????14 | ?0.10±0.03 | ?71.4％ | [4]∶[1] | P＜0.0001 |
The experiment statistics data can be found out from table, rat is to the active intake of nicotine, with the excipient matched group is benchmark, nicotine patch treatment group reduces 27.1%, Clonidine Patch treatment group reduces by 31.4%, two group of addition and reduces 58.5%, and patch treatment group of the present invention reduces 71.4%, significantly surpass the addition effect of two kinds of folk prescription pasters, prove that compound recipe paster of the present invention has synergistic function; From statistics probability P value, prove compound recipe paster best results of the present invention equally.
Compound smoking-refraining adhesive sheet absorbed through skin of the present invention can make contained nicotine and clonidine or lofexidine discharge synchronously, and two medicine Transdermal absorption can reach valid density simultaneously and bring into play its cooperative effect; Adopt and change a slice subsides usefulness at 24 hours every day, can make and when more pasting new film, keep higher blood drug level, all malaise symptoms that occur in the time of can alleviating smoking cessation, not only quit smoking rate can be higher than two kinds of folk prescription paster use in conjunction, and smoking cessation can foreshorten to about 3 weeks the course of treatment, and expenses for medicine can reduce half.Compound smoking-refraining adhesive sheet absorbed through skin of the present invention compared with prior art has the smoking cessation better effects if, and the effect of paying is littler, and the course of treatment is shorter, expense is lower, use advantages such as easier, is a kind of even more ideal smoking-refraining adhesive sheet absorbed through skin.
Accompanying drawing is the cross-sectional view of compound smoking-refraining adhesive sheet absorbed through skin of the present invention.
Among the figure: 1-backing layer 2-drug storehouse layer 3-adhesion layer 4-protective layer
Embodiment
Example 1, compound smoking-refraining adhesive sheet absorbed through skin A
1) drug storehouse layer: polyisobutylene host material 300mg includes nicotine 30mg, clonidine 0.3mg, Laurel nitrogen ketone 10mg;
2) adhesion layer: Polyisobutylene PSA 200mg includes fluocinonide 0.3mg;
3) backing layer and protective layer are aluminum-plastic composite membrane, and wherein the silication of protective layer inner face is antiseized.
Example 2, compound smoking-refraining adhesive sheet absorbed through skin B
1) drug storehouse layer: polyisobutylene host material 400mg includes nicotine 30mg, lofexidine 0.6mg, Laurel nitrogen ketone 10mg;
2) adhesion layer: Polyisobutylene PSA 200mg includes halcinonidedcorten 1.2mg;
3) backing layer and protective layer (same A)
Example 3, compound smoking-refraining adhesive sheet absorbed through skin C
1) drug storehouse layer: polyisobutylene host material 300mg includes nicotine 30mg, clonidine hydrochloride 0.8mg, Laurel nitrogen ketone 10mg;
2) adhesion layer is a Polyisobutylene PSA;
3) backing layer and protective layer (same A)
Example 4, compound smoking-refraining adhesive sheet absorbed through skin D
1) drug storehouse layer: polyisobutylene host material 400mg includes nicotine tartrate 70mg, lofexidine hydrochlorate 1.8mg, Laurel nitrogen ketone 10mg;
2) adhesion layer (same C)
3) backing layer and protective layer (same A)
Claims (3)
1. compound smoking-refraining adhesive sheet absorbed through skin, comprise backing layer, drug storehouse layer, adhesion layer and protective layer four-layer structure, it is characterized in that: drug storehouse layer is a host material with polyisobutylene 200-500mg, include nicotine or its salt 5-120mg (nicotine burst size 5-30mg/d), clonidine or its salt 0.1-6.0mg (clonidine burst size 0.075-0.5mg/d) or lofexidine or its salt 0.2-12mg (lofexidine burst size 0.15-1mg/d) and account for the penetrating agent of drug storehouse layer 1%-2% (weight); Adhesion layer is a Polyisobutylene PSA, includes the local steroidal anti-inflammatory drugs 0-2.5mg that uses.
2. according to the described compound smoking-refraining adhesive sheet absorbed through skin of claim 1, it is characterized in that preferably Laurel nitrogen ketone of penetrating agent that drug storehouse layer includes; The part that adhesion layer includes is with steroidal anti-inflammatory drugs preferably fluocinonide or halcinonidedcorten, or Triamcinolone acetonide acetate.
3. according to the described compound smoking-refraining adhesive sheet absorbed through skin of claim 1, it is characterized in that backing layer and protective layer are aluminum-plastic composite membrane, wherein the silication of protective layer inner face is antiseized.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN98111814A CN1186659A (en) | 1998-01-09 | 1998-01-09 | Compound smoking-refraining adhesive sheet absorbed through skin |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN98111814A CN1186659A (en) | 1998-01-09 | 1998-01-09 | Compound smoking-refraining adhesive sheet absorbed through skin |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1186659A true CN1186659A (en) | 1998-07-08 |
Family
ID=5221702
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN98111814A Pending CN1186659A (en) | 1998-01-09 | 1998-01-09 | Compound smoking-refraining adhesive sheet absorbed through skin |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1186659A (en) |
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011128810A1 (en) * | 2010-04-14 | 2011-10-20 | Centre National De La Recherche Scientifique | Statins for the prevention or treatment of drug addictions |
| WO2013072763A2 (en) * | 2011-11-16 | 2013-05-23 | Nometics Inc. | Non-sensitizing transdermal clonidine patch |
| WO2014053081A1 (en) * | 2012-10-01 | 2014-04-10 | The Hong Kong University Of Science And Technology | Design and manufacture of nonelectronic, active-infusion patch and device for transdermal delivery across skin |
| CN103933018A (en) * | 2013-01-18 | 2014-07-23 | 江苏康倍得药业有限公司 | Transdermal drug delivery system |
| CN104305516A (en) * | 2014-08-25 | 2015-01-28 | 上海烟草集团有限责任公司 | Patch type smokeless tobacco product for oral cavity |
| CN105311002A (en) * | 2015-10-22 | 2016-02-10 | 安徽一灵药业有限公司 | Preparation method of clonidine controlled-release patch |
| CN106723371A (en) * | 2016-12-13 | 2017-05-31 | 河南中烟工业有限责任公司 | A kind of self-heating cigarette substitute and preparation method thereof |
| CN112618617A (en) * | 2021-01-05 | 2021-04-09 | 鹤壁市星银凯丰科技有限公司 | A patch containing coffee powder and its preparation method |
-
1998
- 1998-01-09 CN CN98111814A patent/CN1186659A/en active Pending
Cited By (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2958850A1 (en) * | 2010-04-14 | 2011-10-21 | Centre Nat Rech Scient | DRUGS FOR THE PREVENTION OR TREATMENT OF ADDICTIONS TO DRUGS |
| US20130109712A1 (en) * | 2010-04-14 | 2013-05-02 | Universite De Poitiers | Statins for the Prevention or Treatment of Drug Addictions |
| WO2011128810A1 (en) * | 2010-04-14 | 2011-10-20 | Centre National De La Recherche Scientifique | Statins for the prevention or treatment of drug addictions |
| WO2013072763A2 (en) * | 2011-11-16 | 2013-05-23 | Nometics Inc. | Non-sensitizing transdermal clonidine patch |
| WO2013072763A3 (en) * | 2011-11-16 | 2013-08-15 | Nometics Inc. | Non-sensitizing transdermal clonidine patch |
| CN105073102A (en) * | 2012-10-01 | 2015-11-18 | 香港科技大学 | Design and fabrication of non-electronic active injection patches and devices for transdermal drug delivery |
| WO2014053081A1 (en) * | 2012-10-01 | 2014-04-10 | The Hong Kong University Of Science And Technology | Design and manufacture of nonelectronic, active-infusion patch and device for transdermal delivery across skin |
| US10548854B2 (en) | 2012-10-01 | 2020-02-04 | The Hong Kong University Of Science And Technology | Manufacture of nonelectronic, active-infusion patch and device for transdermal delivery across skin |
| CN103933018A (en) * | 2013-01-18 | 2014-07-23 | 江苏康倍得药业有限公司 | Transdermal drug delivery system |
| CN104305516B (en) * | 2014-08-25 | 2016-08-31 | 上海烟草集团有限责任公司 | The SMD smoke-free tobacco product in a kind of oral cavity |
| CN104305516A (en) * | 2014-08-25 | 2015-01-28 | 上海烟草集团有限责任公司 | Patch type smokeless tobacco product for oral cavity |
| CN105311002A (en) * | 2015-10-22 | 2016-02-10 | 安徽一灵药业有限公司 | Preparation method of clonidine controlled-release patch |
| CN106723371A (en) * | 2016-12-13 | 2017-05-31 | 河南中烟工业有限责任公司 | A kind of self-heating cigarette substitute and preparation method thereof |
| CN112618617A (en) * | 2021-01-05 | 2021-04-09 | 鹤壁市星银凯丰科技有限公司 | A patch containing coffee powder and its preparation method |
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