CN1234350C - Estrogen plaster used in cavity or duct - Google Patents
Estrogen plaster used in cavity or duct Download PDFInfo
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- CN1234350C CN1234350C CN 01126268 CN01126268A CN1234350C CN 1234350 C CN1234350 C CN 1234350C CN 01126268 CN01126268 CN 01126268 CN 01126268 A CN01126268 A CN 01126268A CN 1234350 C CN1234350 C CN 1234350C
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- estrogen
- plaster
- silicone rubber
- plaster according
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Abstract
The present invention relates to an estrogen plaster used in cavities or ducts, which is composed of a macromolecular adhesive layer (1), a medicine containing layer (2) using macromolecular materials as a carrier, and a controlled release membrane (3) made of macromolecular materials. The estrogen plaster can be adhered to a vaginal ring and an intrauterine device to slowly release oestrogens or a selective oestrogens antagonist in minute quantities, and a great amount of long-term systemic side reaction of oestrogens can be avoided. The present invention has the advantages of simple and convenient removal and placement, etc.
Description
Technical field
The present invention relates to a kind of estrogen long-acting slow-release preparation, more particularly relate to the estrogen plaster of using on pessary or the intrauterine device.
Background technology
The progestogen long-acting slow-release preparation of simple property commonly used has subdermal implants, pessary, intrauterine device etc. at present, when using this class progestogen long-acting slow-release preparation, the side reaction that progestogen cause can appear in the people of significant proportion, as long-time, the side reactions such as drop is hemorrhage, menostaxis or amenorrhea that cause because of the confusion of the menstrual cycle, thereby the clinical use and the market share of these medicines have been hindered.Often stop using progestin preparation when running into this class side reaction at present clinically, or allow more oral estrogen preparations of user or anti symptom treatment.Although oral estrogen has better curative effect to the above-mentioned side reaction that overcomes progestogen and cause, the dosage of oral estrogen is bigger than normal, and the cycle is long.For a long time, use the people of progestogen long-acting slow-release preparation just to wish have the minimum estrogen slow releasing preparation of a kind of side effect own to reduce or eliminate the side effect that progestin preparation brings simultaneously very much.
Though do not use progestin preparation for some, need the crowd of complementing estrogen really, oral estrogen the systemic side effect that estrogen causes occurs sometimes because dosage is bigger than normal.So also be sought after the little slow release estrogen plaster of a kind of systemic side effects.
Summary of the invention
The present invention is intended to research and develop out a kind of preparation, and it can overcome side effect, adopts the plaster on local pessary or the intrauterine device, slowly discharges estrogen, directly acts on the target tissue organ.
An object of the present invention is to provide a kind of systemic side effects few, use simple, have the pessary of slow releasing function or an estrogen plaster on the intrauterine device.
The objective of the invention is to realize by following design: estrogen plaster on a kind of pessary or the intrauterine device, by being followed successively by (1) macromolecule glue adhesion coating; (2) with the macromolecular material be the medicated layer of carrier; (3) release-controlled film of macromolecular material formation is formed.
Description of drawings
Fig. 1 is the profile of plaster of the present invention.
The specific embodiment
The thickness of macromolecule glue adhesion coating 1 is 0.05-0.5mm among Fig. 1; The medicated layer thickness that with the macromolecular material is carrier is 0.1-2mm, and the thickness of release-controlled film 3 is 0.1-2mm.
Wherein said macromolecule glue adhesion coating (1) is made of the product-morotik series pressure sensitive adhesive of U.S. morton company.
The medicated layer (2) that with the macromolecular material is carrier comprises medicine and carrier, the weight ratio of its Chinese medicine and carrier is 0.05: 1-0.5: 1, described carrier is the macromolecular material that is selected from room temperature vulcanized silicone rubber (RTV), addition vulcanization or cryogenic vulcanization silicone rubber (LTV), silicone rubber, EVA, acrylate polymer, described medicine is selected from estrogens, selective estrogen class medicine, as the derivant of estradiol, estriol, ethinylestradiol and all kinds of estrogenic corresponding esters.
Macromolecular material in the release-controlled film (3) is a Dow corning Q7-4750 silicone rubber.
Plaster is preferably long to be 10-20mm, and wide is the rectangle of 0.5-10mm.
Plaster of the present invention is preparation like this:
Weight ratio with medicine and carrier is 0.05: 1-0.5: 1 ratio takes by weighing said medicine and macromolecular material, with it mixing after, be pressed into thick 0.1-2mm by mould, long 10-20mm, the thin slice of wide 0.5-10mm, 100 ℃ of following dry heat vulcanizations, be tiled on the glass plate then, apply the above-mentioned macromolecule material film of 0.01-0.2mm thickness, behind hot air drying, reverse side is coated the above-mentioned macromolecule glue adhesion coating that thickness is 0.01-0.2mm thickness.
To further describe the present invention according to specific embodiment below.
Embodiment 1
Take by weighing silicone rubber (trade name: LS-4100, Shanghai Rubber Products Insitute) 0.5 gram, estradiol 50mg, with it mixing after, be pressed into thick 0.5mm by mould, long 12mm, the thin slice of wide 2mm, in 100 ℃, standby behind 10 minutes dry heat vulcanizations.
Overlay on the glass plate the above-mentioned thin slice that obtains is flat, coat 0.01mm Dow corning Q7-4750 silicon rubber film, behind the hot air drying, reverse side is coated morotik pressure sensitive adhesive (U.S. morton company product).
Take by weighing silicone rubber (trade name: 110-2, Shanghai Rubber Products Insitute) 0.2 gram, Damiano Tommasi phenol 20mg, with it mixing after, be pressed into thick 1mm by mould, long 13mm, the thin slice of wide 3mm, in 100 ℃, standby behind 10 minutes dry heat vulcanizations.
Overlay on the glass plate the above-mentioned thin slice that obtains is flat, coat 0.01mm Dow corning Q7-4750 silicon rubber film, behind the hot air drying, reverse side is coated morotik pressure sensitive adhesive (U.S. morton company product).
Take by weighing silicone rubber (trade name: 110-2, Shanghai Rubber Products Insitute) and EVA (ethylene-vinyl acetate copolymer) and mix pellet 0.5 gram, estradiol 10mg, with it mixing after, be pressed into thick 1mm by mould, long 13mm, the thin slice of wide 2mm, in 100 ℃, standby behind 10 minutes dry heat vulcanizations.
Overlay on the glass plate the above-mentioned thin slice that obtains is flat, coat 0.01mm Dow corning Q7-4750 silicon rubber film, behind the hot air drying, reverse side is coated morotik pressure sensitive adhesive (U.S. morton company product).
Embodiment 4
Take by weighing EVA pellet (ethylene-vinyl acetate copolymer) 0.6 gram, estradiol 10mg, measure 3 milliliters of chloroform, with it mixing after, cast in mould inner pressure and make thick 0.2mm, long 13mm, the thin slice of wide 2mm, standby after xeothermic 2 hours in 50 ℃.
Overlay on the glass plate the above-mentioned thin slice that obtains is flat, coat 0.01mm Dow corning Q7-4750 silicon rubber film, behind the hot air drying, reverse side is coated morotik pressure sensitive adhesive (U.S. morton company product).
Embodiment 5
Get polypropylene (granularity 50-200 μ m) 0.5 gram, estradiol 30mg, measure 2 milliliters in acetone, with it mixing after, be pressed into thick 0.3mm by mould, long 10mm, the thin slice of wide 2mm, in 100 ℃, standby behind 10 minutes dry heat vulcanizations.
Overlay on the glass plate the above-mentioned thin slice that obtains is flat, coat 0.01mm Dow corning Q7-4750 silicon rubber film, behind the hot air drying, reverse side is coated morotik pressure sensitive adhesive (U.S. morton company product).
Plaster of the present invention has following characteristics:
1. be the medicine plaster that contains of drug release carrier with the macromolecular material, sticking to can slow, micro-release estrogen or selective estrogen antagonist on pessary, the intrauterine device.
2. plaster can be according to medication person's needs, voluntarily or select to use 1-6 cycle under physician guidance, obtain correction until the menstrual function disorder.
3. plaster adopts short-term, stage, micro medicine to discharge, and local the use avoided the long-term a large amount of systemic side effects of estrogen.
4. plaster is with the non cohesive gel form, goes, puts easy, do not influence the pessary and the IUD of original use.
Clinical implementation example 1
The plaster of embodiment 1 preparation is attached on the pessary of pastille not, suffers from climacteric syndrome women because of estrogen deficiency, 56 years old, after one week, the symptom of original climacteric syndrome, disappear in succession as hectic fever, cardiac disorder, urinary tract infection etc., use continuously to reach 5 months, to keep curative effect.
Clinical implementation example 2
With the plaster cut growth 12.6mm of embodiment 3 preparations, wide 1mm, the plaster of thick 0.2mm is attached on the pessary.Drop is hemorrhage to reach for 2 weeks to one patient because of using behind the megestrol intrauterine contraceptive loop after the menstruation in two months, used after the above-mentioned pessary three days, and the drop stopped bleeding was used 3 months altogether, and it is normal that menstruation keeps always.
Claims (8)
1. the estrogen plaster of using on pessary or the intrauterine device is by being followed successively by macromolecule glue adhesion coating (1); With the macromolecular material is the medicated layer (2) of carrier; Form with the release-controlled film (3) that macromolecular material constitutes, the thickness of wherein said macromolecule glue adhesion coating (1) is 0.01-0.2mm, and the thickness of described medicated layer (2) is 0.1-2mm, and the thickness of release-controlled film (3) is 0.01-0.2mm.
2. plaster according to claim 1, the macromolecule carrier of wherein said medicated layer is selected from silicone rubber, ethylene-vinyl acetate copolymer, acrylate polymer.
3. plaster according to claim 2, wherein said silicone rubber are selected from room temperature vulcanized silicone rubber or addition vulcanization or cryogenic vulcanization silicone rubber.
4. plaster according to claim 1, wherein said release-controlled film is made of Dow corning Q7-4750 silicone rubber.
5. plaster according to claim 1, the medicine of wherein said medicated layer is selected from estrogen.
6. plaster according to claim 5, wherein said medicine are estradiol, estriol, ethinylestradiol or its corresponding esters.
7. the application of plaster according to claim 1 on the preparation pessary.
8. the application of plaster according to claim 1 on the preparation intrauterine device.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 01126268 CN1234350C (en) | 2001-07-18 | 2001-07-18 | Estrogen plaster used in cavity or duct |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 01126268 CN1234350C (en) | 2001-07-18 | 2001-07-18 | Estrogen plaster used in cavity or duct |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1397274A CN1397274A (en) | 2003-02-19 |
| CN1234350C true CN1234350C (en) | 2006-01-04 |
Family
ID=4666290
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 01126268 Expired - Fee Related CN1234350C (en) | 2001-07-18 | 2001-07-18 | Estrogen plaster used in cavity or duct |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1234350C (en) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101695589B (en) * | 2009-10-22 | 2013-03-20 | 华中科技大学 | Sandwich layer slow-release birth control material |
| EP2566877A4 (en) * | 2010-05-05 | 2013-10-09 | Teva Womens Health Inc | Methods of reducing symptoms in subjects using single dosage forms with tapering release rates |
| CN102861374B (en) * | 2011-07-08 | 2014-06-25 | 上海市计划生育科学研究所 | Pessulum capable of steadily releasing medicine |
| ES2930330T3 (en) * | 2018-04-19 | 2022-12-12 | Yipurun Shanghai Biotechnology Co Ltd | Elastic membrane having a function of reactivation of the endometrial basal layer in a uterine cavity and preparation method of the elastic membrane |
| CN110624137B (en) * | 2019-10-28 | 2022-07-01 | 易浦润（上海）生物技术有限公司 | Uterine stent |
-
2001
- 2001-07-18 CN CN 01126268 patent/CN1234350C/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| CN1397274A (en) | 2003-02-19 |
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| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20060104 Termination date: 20170718 |