CN100502817C - A composite intrauterine device using copper salts as copper ion source - Google Patents

A composite intrauterine device using copper salts as copper ion source Download PDF

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CN100502817C
CN100502817C CNB2007100513642A CN200710051364A CN100502817C CN 100502817 C CN100502817 C CN 100502817C CN B2007100513642 A CNB2007100513642 A CN B2007100513642A CN 200710051364 A CN200710051364 A CN 200710051364A CN 100502817 C CN100502817 C CN 100502817C
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copper
mantoquita
composite
iud
active substance
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CN101006949A (en
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谢长生
蔡水洲
夏先平
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Huazhong University of Science and Technology
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Huazhong University of Science and Technology
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Abstract

The invention discloses a composite uterine pregnant contraceptive device based on copper salt as copper ion source, which is characterized by the following: adopting base material and active material to form kinds of shape through thermo plasticity or heat solidity; setting the weight quantity of active material at 0.5-50% corresponding to IUD; setting the base material as low-density polyethylene or silicon rubber; selecting active material from one kind of copper salt or copper salt and sulphanilamide haemostatic drug and steroid hormone contraceptive pill; reducing a series of hemorrhagic and pain on the clinic; avoiding the damage of active oxygen for uterus.

Description

A kind of is the composite intrauterine device of copper ion source with the mantoquita
Technical field
The present invention relates to a kind of women's long-acting contraception birth control utensil, being specially a kind of is the composite intrauterine device of copper ion source with the water solublity mantoquita, and it can load mantoquita or Combined Loading mantoquita, anti-inflammation hemostasia medicine or steroid hormonal contraceptive separately.
Technical background
Intrauterine device Intrauterine Device (IUD) is a kind of safe, effective, economic, reversible and easy contraceptive device, also is one of global most popular method.IUD is divided into inertia and active two big classes.Inertia IUD is replaced by copper IUD fully owing to its contraceptive effect difference.Copper IUD mainly contains two types: copper-loaded IUD (Cu-IUD) and hormonal contraceptive medicine slow release IUD.It is good that Cu-IUD has a contraceptive effect, continuously service time long, the cost performance height has advantages such as reversibility, thereby it is maximum to become current research, uses the widest a kind of IUD.
Traditional copper-loaded IUD shows some inherent drawbacks in the use in more than 30 years: (1) copper-loaded in effective conversion ratio of copper ion lower; (2) insert the copper ion release of human body initial stage and present the violent release phenomenon; (3) the copper ion rate of release can not be regulated and control; (4) metallic copper directly contacts with endometrium, and copper surface can become more and more coarse and deposit a large amount of deposit damage endometrium; (5) elemental copper oxidation in uterine cavity produces the generation that is attended by active oxygen in the process of copper ion all the time, and active oxygen has problems such as damaging action to the uterus.These drawbacks easily to user bring hemorrhage, come off, side effect such as menoxenia and pelvic inflammatory disease.Therefore, how to eliminate or alleviate various side effect that IUD brings, impel more reproduction age women to be ready to accept and to adopt IUD to practise contraception, become relevant difficult problem that presses for solution of scientific worker.
With elemental copper granule (copper nano particles, copper micron particle) is that the polymer matrix composite intrauterine device of copper ion source can address the above problem well, but be attended by the generation of active oxygen in the process of elemental copper oxidation generation copper ion in uterine cavity all the time, and active oxygen there is damaging action to the uterus.
Summary of the invention
The purpose of this invention is to provide a kind of is the composite intrauterine device of copper ion source with the mantoquita, this birth control apparatus has been expanded the copper ion source of cupric IUD, eliminated the active oxygen that produces in the corrosion process of elemental copper, avoided active oxygen the infringement of uterine cavity and the variation that therefore causes the uterine cavity environment; Simplify the preparation technology of existing naked copper structure I UD simultaneously, can guarantee to alleviate under its contraceptive effect prerequisite the side effect such as hemorrhage and pain that existing naked copper structure I UD exists clinically.
Provided by the invention a kind of be the composite intrauterine device of copper ion source with the mantoquita, this birth control apparatus is made of matrix material and active substance, the percentage by weight of active substance is the 0.5-50% of gross weight, and wherein, matrix material is low density polyethylene (LDPE) or silicone rubber; Active substance is that water solublity mantoquita or water solublity mantoquita add a kind of of anti-inflammation hemostasia medicine or steroid hormonal contraceptive.Described mantoquita is CuCl 2, CuSO 4Perhaps Cu (NO 3) 2When adopting mantoquita and anti-inflammation hemostasia medicine as active substance, the percentage by weight of anti-inflammation hemostasia medicine is 0.5~40% of an active substance gross weight; When adopting mantoquita and steroid hormonal contraceptive as active substance, the percentage by weight of steroid hormonal contraceptive is the 0.5-50% of active substance gross weight.
As prioritization scheme of the present invention, steroid hormonal contraceptive is megestrol, methylnorethindron or levonorgestrel.
With respect to naked copper structure I UD, composite IUD provided by the invention has following unique advantage:
(1) composite IUD is directly dissolved to produce by mantoquita in uterine fluid and has the contraceptive efficacy copper ion, does not have oxidizing process to take place, thereby can not produce the active oxygen that the uterus is had damaging action.And elemental copper in the oxidized generation copper ion, produces the active oxygen that the uterus is had detrimental effect among the naked copper structure I UD in uterine fluid.
(2) composite IUD has greatly simplified the preparation technology of existing cupric IUD, can disposable machine-shaping obtains the copper IUD of various forms.And existing cupric IUD usually earlier becomes material preparations such as polyethylene supports such as T type, is twining copper wire on the transverse arm of the both sides of support and on the trailing arm or is inlaying copper sheathing then, and perhaps suit contains the release pipe of steroid hormonal contraceptive on trailing arm.
(3) composite IUD has avoided the phenomenon that naked copper structure I UD has to take out in advance because of the corrosion spalling or the fracture of its copper wire or copper sheathing, composite IUD is controlled release matrix with the polymer, copper ion discharges because of following long-term, the steadily release of " stripping controlled release " rule, and the phenomenon of taking out in advance because of fracture can not take place.And then avoided lower abdomen discomfort that naked copper structure I UD brought even pain, through side effect such as blood volume showed increased.
What (4) contact with endometrium behind the composite IUD implant into body has only biocompatibility low density polyethylene (LDPE) preferably, has avoided naked copper structure I UD because of its copper surface corrosion roughening and CaCO fully 3Form aggravation such as calculus at its surface aggregation to the abnormal inflammatory that stimulation and damage caused of endometrial tissue and side-effect problem such as hemorrhage.
(5) composite IUD can carry out controlled release release to copper ion, can regulate the rate of release of copper ion when guaranteeing service life.This point naked copper structure I UD has no idea to accomplish.
With respect to being the intrauterine device of copper ion source with elemental copper (comprising block copper, copper nano-particle and copper micron particle), it with the mantoquita copper ion source that the polymer matrix composite intrauterine device of copper ion source has not only been expanded cupric IUD, and can guarantee significantly to alleviate under the excellent contraceptive effect prerequisite a series of side effect such as hemorrhage and pain that existing cupric IUD exists clinically equally, avoided the oxidation of elemental copper and the active oxygen that generates to the damage in uterus.
Description of drawings
Fig. 1 is the composite inner structural representation of composite IUD of the present invention; Black representation polymer matrix among the figure, white point representative is based on the active substance of mantoquita (comprise in anti-inflammation hemostasia medicine and the steroid hormonal contraceptive one or both);
Fig. 2 is the rate of release sketch map of copper ion among the anhydrous cupric chloride polymer composites IUD of the present invention.
The specific embodiment
Considering that the active substance that really plays contraceptive efficacy is a copper ion, is that the polymer matrix composite intrauterine device of copper ion source directly dissolves the generation copper ion with the mantoquita in uterine cavity, and this process does not produce active oxygen.Therefore mantoquita is that the polymer matrix composite intrauterine device of copper ion source not only has the advantage that elemental copper particulate polymers based composites intrauterine device is had, but also can avoid the damaging action of active oxygen to the uterus.This uterine cavity environment that neither changes has to reach the desirable substitute that the IUD of contraceptive effect preferably will become existing naked copper IUD.Therefore, we to have developed this be the composite intrauterine device of copper ion source with the mantoquita.
A kind of among the present invention is that the composite IUD of copper ion source is made of matrix material and active substance with the mantoquita, and the percentage by weight of active substance is the 0.5-50% of gross weight, and matrix material is low density polyethylene (LDPE) or silicone rubber; Active substance is that mantoquita or mantoquita add a kind of of anti-inflammation hemostasia medicine or steroid hormonal contraceptive.Mantoquita is with anhydrous CuCl 2, anhydrous CuSO 4And Cu (NO 3) 2Etc. water miscible be main, especially with anhydrous CuCl 2Be the best.
When above-mentioned composite IUD adopted mantoquita and anti-inflammation hemostasia medicine as active substance, the percentage by weight of anti-inflammation hemostasia medicine was the 0.5-40% of active substance gross weight.
When above-mentioned composite IUD adopted mantoquita and steroid hormonal contraceptive as active substance, the percentage by weight of steroid hormonal contraceptive was the 0.5-50% of active substance gross weight.
By above-mentioned requirements with matrix material with after active substance mixes, adopt the thermoplastic processing method time processing of routines such as injection moulding to become various forms, promptly obtaining the present invention a kind of is the polymer matrix composite IUD of copper ion source with the mantoquita, and the representative configuration of birth control apparatus is γ type, T type, Y type and V-type etc.
As shown in Figure 1, polymeric matrix is the polymer matrix composite IUD of copper ion source with the mantoquita with constituting a kind of as the mantoquita of active substance, anti-inflammation hemostasia medicine and steroid hormonal contraceptive, and the rate of release of active substance is rule as shown in Figure 2 among this composite IUD.
The present invention is further illustrated below in conjunction with example.Low density polyethylene (LDPE) and silicone rubber related among the embodiment are medical grade, and mantoquita, anti-inflammation hemostasia medicine and steroid hormonal contraceptive are analytical pure.
Embodiment 1
Take by weighing 25g CuCl 2Superfines, 25g medical grade low density polyethylene (LDPE) (LDPE) adopt methods such as premix, blend, pressure injection or injection moulding, prepare the composite IUD of γ type.
Embodiment 2-27 all adopts method preparation similar to Example 1, and the constituent of wherein prepared composite IUD is as shown in table 1.
The constituent of composite IUD among each embodiment of table 1
Figure C200710051364D00061
Adopt low density polyethylene (LDPE) obviously to be better than adopting the technique effect of silicone rubber as base material as the technique effect of base material, therefore preferred matrix material is a low density polyethylene (LDPE).Mantoquita is with CuCl 2, CuSO 4And Cu (NO 3) 2Deng being main, especially with CuCl 2Be the best.Steroid hormonal contraceptive can adopt existing various progestogen.Because the fusing point of megestrol, methylnorethindron and levonorgestrel etc. is higher than the heat processing and forming temperature of composite IUD, therefore the steroid hormonal contraceptive that preferably uses is megestrol, methylnorethindron and levonorgestrel etc.

Claims (2)

1, a kind of is the composite intrauterine device of copper ion source with the mantoquita, it is characterized in that: this birth control apparatus is made of matrix material and active substance, the percentage by weight of active substance is the 0.5-50% of gross weight, and wherein, matrix material is low density polyethylene (LDPE) or silicone rubber; Active substance is the mixture of mantoquita, mantoquita and anti-inflammation hemostasia medicine or the mixture of mantoquita and steroid hormonal contraceptive;
Described mantoquita is CuCl 2, CuSO 4Perhaps Cu (NO 3) 2
When active substance was the mixture of mantoquita and anti-inflammation hemostasia medicine, the percentage by weight of anti-inflammation hemostasia medicine was the 0.5-40% of active substance gross weight;
When active substance was the mixture of mantoquita and steroid hormonal contraceptive, the percentage by weight of steroid hormonal contraceptive was the 0.5-50% of active substance gross weight.
2, composite intrauterine device according to claim 1 is characterized in that: described steroid hormonal contraceptive is megestrol, methylnorethindron or levonorgestrel.
CNB2007100513642A 2007-01-24 2007-01-24 A composite intrauterine device using copper salts as copper ion source Expired - Fee Related CN100502817C (en)

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CN103446629B (en) * 2013-08-28 2015-08-19 中国科学院理化技术研究所 anti-infection material for intrauterine device and preparation method thereof

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3803308A (en) * 1968-09-18 1974-04-09 Searle & Co Method of contraception with a soluble non-toxic copper or zinc compound
US3934580A (en) * 1973-11-09 1976-01-27 Apamed Anstalt Chemically acting intra-uterine device
US4040417A (en) * 1970-12-01 1977-08-09 G. D. Searle & Co. Intrauterine device
WO1985004798A1 (en) * 1984-04-19 1985-11-07 University Of Queensland Contraceptive methods and delivery systems therefore
CN1349397A (en) * 1999-05-07 2002-05-15 德克·怀尔德米尔斯克 Intrauterine contraception with less side effects
CN1440819A (en) * 2003-04-02 2003-09-10 华中科技大学 Nano composite material for intrauterine birth control device
CN1666724A (en) * 2005-04-06 2005-09-14 华中科技大学 Drug-carrying intrauterine device without holding bracket made of nanometer composite material

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3803308A (en) * 1968-09-18 1974-04-09 Searle & Co Method of contraception with a soluble non-toxic copper or zinc compound
US4040417A (en) * 1970-12-01 1977-08-09 G. D. Searle & Co. Intrauterine device
US3934580A (en) * 1973-11-09 1976-01-27 Apamed Anstalt Chemically acting intra-uterine device
WO1985004798A1 (en) * 1984-04-19 1985-11-07 University Of Queensland Contraceptive methods and delivery systems therefore
CN1349397A (en) * 1999-05-07 2002-05-15 德克·怀尔德米尔斯克 Intrauterine contraception with less side effects
CN1440819A (en) * 2003-04-02 2003-09-10 华中科技大学 Nano composite material for intrauterine birth control device
CN1666724A (en) * 2005-04-06 2005-09-14 华中科技大学 Drug-carrying intrauterine device without holding bracket made of nanometer composite material

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