CN1046089C - Antithyroid cream for external application - Google Patents
Antithyroid cream for external application Download PDFInfo
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- CN1046089C CN1046089C CN93111370A CN93111370A CN1046089C CN 1046089 C CN1046089 C CN 1046089C CN 93111370 A CN93111370 A CN 93111370A CN 93111370 A CN93111370 A CN 93111370A CN 1046089 C CN1046089 C CN 1046089C
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- antithyroid
- cream
- thyroid
- hyperthyroidism
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Abstract
The present invention relates to thyroid cream for external application. The thyroid cream contains an antithyroid drug, glucocorticoid and a drug penetration promoting agent and is directly and externally applied on skins at an anterior thyroid part. The thyroid cream directly penetrates skins and enters thyroid to treat hyperthyroidism disease symptom through the drug. The dosage of the used drug is small to quickly control the premonition of hyperthyroidism crisis and quickly correct hyperthyroidism complication. The thyroid cream has the advantages of no hormone side effect and safe use. A patient suffering from hyperthyroidism is treated through the drug of the present invention, relapse rate is very low, and therapeutic effect is good. The drug has the advantages of simple production technique and sufficient raw material and has obvious social benefit and economic benefit.
Description
The present invention relates to treat the thyroid hyperfunction disease disease drug, is about a kind of antithyroid cream for external application medicine.
Thyroid hyperfunction disease disease is that a kind of commonly encountered diseases, frequently-occurring disease, sickness rate are very high, accounts for second in endocrinopathy.Since nineteen forty-three, main antithyroid drug is with imidazoles and Thiourea oral tablet always.This medicament can only partly suppress the activity of thyroid endoperoxidase, to reduce the synthetic of thyroxin, but release synthetic and that be stored in the thyroxin in the thyroid be there is no inhibitory action, just begin to show clinical effectiveness so generally about 2-3 is all behind oral imidazoles medicament.About 1-3 month ability disease controlling.It is synthetic to suppress thyroxin fully, and need take the 100-120mg imidazoles every day approximately, and this dosage toxicity is bigger, can not use.Present conventional oral dose is 30-60mg/ day, and this dosage can only partly suppress the synthetic of thyroxin.For diffuse goiter companion hyperthyroidism, after 1.5～2 years, only there is 50% patient can obtain the persistency alleviation with oral routine dose Drug therapy.
Think that in recent years glucocorticoid has the release that suppresses thyroxin to thyroid, suppress the picked-up of thyroid,, quicken kidney cleaning up iodine to reduce the utilization of thyroid to iodine to reduce the anabolic effect of thyroxin to iodine; Suppress the synthetic and release of throtropin releasing hormone in the hypothalamus, reduce the reaction of hypophysis cerebri throtropin releasing hormone.The excretory thyrotropin of hypophysis is reduced; Suppress the interior thyroxin of body and become the stronger trilute of biological activity; Suppress the reaction of surrounding tissue to thyroxin; Suppress thyroid inner cell immunity and humoral immunization, reduce the generation of thyrotrophin receptor antibody, thereby suppress it thyroid stimulation.However, but the glucocorticoid using dosage is quite big, prolonged application can produce serious whole body and pay effect, and produce a series of complication, as Ke Xing sample syndrome, easily infect, Mental Subnormality, myopathy and myalgia, osteonecrosis and osteomalacia, steroid digestive tract ulcer, diabetes or the like.Therefore in fact can not be used for the treatment of hyperthyroidism at present clinically, oral imidazoles can produce ill effects such as hepatic injury, leucocytes reduction equally
The object of the present invention is to provide a kind of effectively, pay effect little medicament human body to hyperthyroidism treatments.
The antithyroid cream for external application of developing among the present invention, mix by an oil phase component and a water component, contain adrenal gland's glucocorticoid and antithyroid drug in the emulsifiable paste, its constituent content (weight %) is: the distilled water of adrenal gland's glucocorticoid of 1-10,1-20 azone, 11-40 monostearate, 13-60 liquid paraffin, 5-20 vaseline, 5-20 glyceryl monostearate, 1-10 antithyroid drug, 0.1-2.0 sodium lauryl sulphate, 0.1-0.5 triethanolamine, 5-20 propylene glycol and aequum.Said adrenal gland's glucocorticoid can be selected from hydrocortisone, fluocinolone acetonide, dexamethasone, prednisone and andrographolide.Said antithyroid drug is imidazoles and Thiourea, antithyroid drug.Imidazoles wherein can be selected from thiamazole (thiamazole) and carbimazole, and the Thiourea medicine can be selected from propylthiouracil and methylthiouracil:
The compound method of this antithyroid cream for external application is: hydrocortisone, azone, monostearate, liquid paraffin, vaseline, glyceryl monostearate are mixed form oil phase, remainder mixes forms water.Again oil phase and water component are heated to respectively about 70 ℃, under stirring oil phase component are added in the water component, make it fully mix stirring, obtain a kind of oil-in-water type emulsifiable paste all to cooling.
The using method of antithyroid cream for external application II of the present invention is: emulsifiable paste II evenly is coated on the skin at thyroid position, throat, each consumption is 0.3 gram, and beginning is early, middle and late respectively once every day, treats the hyperthyroidism transference cure or disappears T substantially
3, T
4, VT
3, FT
3, FT
4Reduce to normal 1-2 after week, change into sooner or later respectively once, reuse changes the I emulsifiable paste that does not contain the hydrogenation cortisone into after 2 weeks, keep treatment once a day.
For showing progressive of the present invention, with emulsifiable paste II of the present invention the swollen companion of 52 routine diffusivity first shapes hyperthyroidism (GD) patient being made thyroid position, throat skin is coated with to use instead after the control of the applying treatment state of an illness and does not contain the coating of hydrogenation cortisone emulsifiable paste I throat and keep treatment, and random packet 52 examples are with the thiamazole of oral conventional therapy dosage, add 40 milligrams of hydrocortisone every days in the state of an illness control phase, the state of an illness control back hydrocortisone of stopping using.Organize I in contrast with this, pay effect with the ill effect and the poison of paired observation medicine, do clinical observation in the Shandong Prov. Hospital simultaneously, be a year and a half two groups the course of treatment, observed mean time is 17.63 ± 9.43 months.Have 19 examples to finish the back drug withdrawal the course of treatment in every group and observe, observed mean time is 10.70 ± 4.56 months, and two groups of comparing results see the following form.
The state of an illness treatment group matched group I hyperthyroidism state of an illness begins the time of alleviating (my god) 5.4 ± 4.2 29.4 ± 13.8 hyperthyroidism state of an illness complete obiteration times (my god) 24.2 ± 14.6 75.9 ± 36.6 thyroid and dwindles obviously that incidence rate (%) 61.5 38.5 vessel of thyroid noises alleviate or disappearance incidence rate (%) 90.4 40.4T
3, T
4Be down to normal, (my god) 12.6 ± 8.9 58.1 ± 28.8 hyperthyroidisms incidence repeatedly, (%) 9.6 30.8 medicine hypothyroidism incidences, (%) 9.6 32.7 stop recurrence rate behind the medicine, (%) the comprehensive disease incidence of 5.8 26.9 Ke Xing samples, (%) 0 11.5 cause that blood pressure increases incidence, (%) 0 7.7 cause that blood sugar increases incidence, (%) 0 36.5 liver lesion induced by drugs evil 0 7.7
Experimental result shows that its effect obviously is better than matched group I with emulsifiable paste II treatment hyperthyroidism of the present invention, does not almost have bad pair of effect and medicine poison and pays effect, and to the critical patient that some can not be oral, can control the critical disease million of hyperthyroidism rapidly.
Also with random packet 52 examples, be coated with applying treatment in addition with the antithyroid cream for external application I that does not contain the hydrogenation cortisone, as second matched group, its therapeutic effect of clinical contrast observation, two groups comparing result sees the following form.
The state of an illness treatment group control Group II hyperthyroidism state of an illness begins the time of alleviating (my god) 5.4 ± 4.2 20.1 ± 16.1 hyperthyroidisms performances extinction time (my god) 24.2 ± 14.6 64.4 ± 51.2 thyroid and obviously reduces incidence rate (%) 61.5 17.3 vessel of thyroid noises and alleviate incidence rate 90.4 32.7
(%) T
3, T
4Transfer to normal time (my god) 12.6 ± 8.9 31.7 ± 22.7
Clinical trial shows that hydrocortisone and thiamazole have good synergism in the hyperthyroidism treatment, improve the therapeutic effect to hyperthyroidism.
The several examples of following reuse further specify the present invention. component example one example dihydro cortisone 5 gram/FAs/0.5 gram azone 5 grams 5 gram monostearates 11 grams 11 gram atoleines 15 grams 15 gram vaseline 5 grams 5 gram glycerin monostearates 5 grams 5 gram propylthiouracils/5 gram methimazoles, 5 gram/lauryl sodium sulfate, 0.5 gram 0.5 restrains 41.5 milliliters 46 milliliters of 5 milliliter of 5 ml waters of 2 milliliters of 2 milliliters of propane diols of triethanolamine
The several examples of following reuse further specify effect of the present invention, do the hyperthyroidism treatment by above-mentioned using method.
Example 1, * *, 52 years old, the severe hyperthyroid patient, concurrent hyperthyroid heart disease, quick atrial fibrillation, the III degree is heart failure whole-heartedly, the invalid hyperthyroidism crisis tendency that occurs of oral a large amount of methylthiouracil two weeks.With emulsifiable paste II of the present invention number treatment tendency performance disappearance after 7 days.
Example 2, * * *, 62 years old, the patient merged hyperthyroid heart disease of ZANG-organs and coronary heart disease, and persistence atrial fibrillation, pneumonia, medicine cause leukopenia to 2.2～2.7 * 10
939 ℃ of/L body temperature, heart rate 140 times/minute.Under can not the situation of oral methylthiouracil, with emulsifiable paste II external application for curing of the present invention, the state of an illness be obviously improved in the 10th day, and heart rate is reduced to 76 times/minute, the 14th day T
3, T
4Reduce to normally, leukocyte rose to 5.2 * 10 in the 25th day
9/ L, the state of an illness was clearly better and leaves hospital in the 42nd day.Followed up a case by regular visits to 26 months, and can participate in labor in general, do not have the recurrence disease.
Above clinical test results shows that the present invention has following advantage:
1, because emulsifiable paste of the present invention can be applied on the skin at thyroid position, throat medicine outward directly sees through skin and enter in the thyroid, the control hyperthyroidism state of an illness is fast, can control the hyperthyroidism crisis omen rapidly, and can correct the hyperthyroidism complication rapidly.
2, drug use dosage is little, the human body whole body is not had the medicine poison pay effect, does not also have hormone and pays effect, makes glucocorticoid be used for the treatment of hyperthyroidism and becomes a reality.
3, by method of the present invention treatment hyperthyroidism, hyperthyroidism incidence rate and relapse rate repeatedly is starkly lower than conventional oral drug therapy method.
The present invention has improved the hyperthyroidism therapeutic effect for hyperthyroid patient provides a kind of not only convenient but also economical new curative and method, alleviate patient's misery, this drug manufacture technology is simple, the raw material abundance, have obvious social and economic benefit, be worthy of popularization.
Claims (4)
1, a kind of antithyroid cream for external application, comprise an oil phase component and a water component, it is characterized in that containing in the emulsifiable paste adrenal gland's glucocorticoid and antithyroid drug, its component content (weight %) is adrenal gland's glucocorticoid of 1-10, the 1-20 azone, the 11-40 monostearate, the 13-60 liquid paraffin, 5-20 vaseline, the 5-20 glyceryl monostearate, 1-10 antithyroid drug, 0.1-2.0 sodium lauryl sulphate, 0.1-0.5 triethanolamine, the distilled water of 5-20 propylene glycol and aequum.
2, according to the described antithyroid cream for external application of claim 1, it is characterized in that said adrenal gland's glucocorticoid, can from hydrocortisone, fluocinolone acetonide, dexamethasone, prednisone and andrographolide, select.
3, according to the described antithyroid cream for external application of claim 1, it is characterized in that said antithyroid drug is imidazoles and Thiourea antithyroid drug, said imidazoles antithyroid drug can be selected from thiamazole and carbimazole, and said Thiourea antithyroid drug can be selected from propylthiouracil and methylthiouracil.
4, according to the compound method of the described antithyroid cream for external application of claim 1, be adrenal gland's glucocorticoid, azone, monostearate, liquid paraffin, vaseline, glyceryl monostearate to be mixed form oil phase, remainder mixes forms water, oil phase component and water component are heated to respectively about 70 ℃, stir down oil phase component is added in the water component, fully mix to cooling, obtain a kind of oil-in-water type emulsifiable paste.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN93111370A CN1046089C (en) | 1993-07-24 | 1993-07-24 | Antithyroid cream for external application |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN93111370A CN1046089C (en) | 1993-07-24 | 1993-07-24 | Antithyroid cream for external application |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1085079A CN1085079A (en) | 1994-04-13 |
| CN1046089C true CN1046089C (en) | 1999-11-03 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN93111370A Expired - Fee Related CN1046089C (en) | 1993-07-24 | 1993-07-24 | Antithyroid cream for external application |
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| CN (1) | CN1046089C (en) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100406063C (en) * | 2005-05-18 | 2008-07-30 | 陈凌 | External-applied ointment used for treating thyropathy, and its prepn. method |
| NZ552816A (en) * | 2007-01-24 | 2009-05-31 | Bomac Research Ltd | Formulation for transdermal administration of antihyperthyroid drug comprising a penetration enhancer selected from oleic acid, d-limonene, pyrrolidones, a C2-C8 alcohol, glycol ethers, triacetin and combinations thereof |
| CN102631312A (en) * | 2011-02-09 | 2012-08-15 | 张蔚 | Compound antithyroid gel for external application and preparation method thereof |
| WO2015172769A2 (en) | 2014-05-13 | 2015-11-19 | Dendropharm Gmbh | Formulations for treatment of hyperthyroidism |
| CN104117066B (en) | 2014-07-16 | 2016-03-02 | 陈凌 | The preparation method of external-applied ointment used for treating thyropathy |
-
1993
- 1993-07-24 CN CN93111370A patent/CN1046089C/en not_active Expired - Fee Related
Non-Patent Citations (3)
| Title |
|---|
| 福建医药杂志，11(6) 1989.11.1 陈兆樵，甲状腺局部注射配合小剂量他巴唑治疗甲状腺机能的疗效观察 * |
| 药剂学第2版 1987.5.1 奚念朱，顾学裘，人民卫生出版社 * |
| 药剂学第2版 1987.5.1 奚念朱，顾学裘，人民卫生出版社;福建医药杂志，11(6) 1989.11.1 陈兆樵，甲状腺局部注射配合小剂量他巴唑治疗甲状腺机能的疗效观察 * |
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| Publication number | Publication date |
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| CN1085079A (en) | 1994-04-13 |
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Granted publication date: 19991103 |