CN115177750A - Application of conjugated polymer in preparation of thyroid disease radiotherapy drug - Google Patents
Application of conjugated polymer in preparation of thyroid disease radiotherapy drug Download PDFInfo
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- CN115177750A CN115177750A CN202210711531.6A CN202210711531A CN115177750A CN 115177750 A CN115177750 A CN 115177750A CN 202210711531 A CN202210711531 A CN 202210711531A CN 115177750 A CN115177750 A CN 115177750A
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- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
- A61P5/16—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
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Abstract
The invention relates to application of a conjugated polymer in preparation of a thyroid disease radiotherapy drug, and belongs to the technical field of tumor treatment. The iodine-131 conjugated polymer disclosed by the invention has a conjugated carbon chain as a main chain and a radioactive isotope of iodine as a side chain 131 I, which are enriched in vivo by thyroid-specific uptake, thereby specifically treating thyroid diseases such as thyroid cancer, hyperthyroidism (hyperthyroidism). The structure of the iodine isotope conjugated polymer nanofiber determines that the iodine isotope conjugated polymer nanofiber is enriched and retained at a focus part after being absorbed by thyroid tissue, increases the specific killing of the focus part, reduces the damage to other tissues at non-focus parts, and can reduce the total damageBody 131 The dosage of the radiation therapy improves the curative effect and reduces the side effect.
Description
Technical Field
The invention belongs to the technical field of tumor treatment, and particularly relates to an application of a conjugated polymer in preparation of a thyroid disease radioactive therapeutic drug, in particular to an application of an iodine-131 conjugated polymer in preparation of a thyroid disease radioactive therapeutic drug.
Background
Iodine-131 is a radioactive isotope of elemental iodine, an artificial radionuclide (nuclear fission product), and has the symbol I-131 and a half-life of 8.02 days. Iodine-131 is a very effective and extremely safe method (also known as "non-open surgery treatment") for treating thyroid diseases because iodine-131 can be highly selectively taken in (iodine 131 is almost only taken in by thyroid gland) and concentrated in thyroid tissues, and the maximum range of beta rays emitted by iodine 131 is only 3.63mm, and the average range of beta rays is 0.48mm, so that the treatment effect of beta rays on thyroid gland is strong, and the influence on tissues around thyroid gland and other organs is extremely small. However, free iodine is absorbed and then has a short metabolic cycle, and is easily excreted through the kidney, so that sufficient radiotherapy effect on the focus part cannot be achieved. How the thyroid targeting effect based on iodine-131 further improves the long-term retention of the iodine-131 in the thyroid part is the key of the iodine-131 used for the radiation therapy of thyroid diseases.
Disclosure of Invention
The invention solves the technical problems that the metabolic cycle is short after iodine-131 is ingested by thyroid gland, the focus can not be fully radiotreated, and multiple times of administration are needed in the prior art, and provides a conjugated polymer containing iodine-131, wherein the main chain of the conjugated polymer is a Polydiacetylene (PDA) carbon chain, and the side chain only contains an iodine-131 substituent group, so that the conjugated polymer can be enriched at the focus part of the thyroid gland and can be retained for a long time.
According to the purpose of the invention, the application of conjugated carbon-iodine polymer for preparing the radioactive therapeutic medicine for thyroid diseases is provided, and iodine atoms in the conjugated carbon-iodine polymer have radioactive isotopes 131 I。
Preferably, the structural formula of the conjugated carbon-iodine polymer comprises a structure shown in formula 1:
preferably, the conjugated carbon-iodine polymer has a structural formula shown in formula I or formula II:
preferably, the conjugated carbon-iodine polymer is prepared by 131 And I, realizing thyroid disease radiotherapy by virtue of radioactivity.
Preferably, the thyroid disease is thyroid cancer or hyperthyroidism.
Generally, compared with the prior art, the technical scheme conceived by the invention mainly has the following technical advantages:
(1) The invention provides a conjugated polymer containing iodine-131, wherein the main chain of the conjugated polymer is a polydiacetylene carbon chain, and the side chain only contains iodine-131 substituent groups, so that the conjugated polymer can be enriched in thyroid lesion sites and can be retained for a long time.
(2) The iodine-131 conjugated polymer is of a nanofiber structure, can specifically target thyroid lesion tissues, and can be kept in the lesion tissues for long-time retention treatment.
(3) The iodine-131 conjugated polymer of the invention has high iodine content, and can improve iodine radiotherapy and synchronously perform iodine-based CT imaging, thereby realizing the monitoring of the iodine-131 treatment process.
(4) The iodine-131 conjugated polymer has a good enrichment effect on thyroid lesion tissues, is long in effective retention time, and can realize a better treatment effect at a lower dosage by combining CT imaging tracking.
(5) The iodine isotope conjugated polymer has short radiation distance, only produces radiotherapy effect on the thyroid gland focus part, and has little damage to other tissues.
(6) Preferably, the iodine-131 conjugated polymer can be applied to thyroid cancer, hyperthyroidism and other thyroid diseases.
(7) The iodine content of the conjugated carbon iodine polymer is up to 84 percent, and iodine-131 has good radiotherapy.
Drawings
FIG. 1 is a scanning electron microscope image of iodine-131 conjugated carbon-iodine polymer provided by the present invention.
Fig. 2 is a CT image of the iodine-131 conjugated carbon-iodine polymer in vivo.
FIG. 3 is a CT time-dependent metabolism chart of the iodine-131 conjugated carbon-iodine polymer in vivo.
Detailed Description
In order to make the objects, technical solutions and advantages of the present invention more apparent, the present invention is described in further detail below with reference to the accompanying drawings and embodiments. It should be understood that the specific embodiments described herein are merely illustrative of the invention and are not intended to limit the invention. In addition, the technical features involved in the embodiments of the present invention described below may be combined with each other as long as they do not conflict with each other.
The preparation of the conjugated carbon-iodine polymer in the invention can be referred to the invention patent with the publication number of CN 114149569A.
Example 1
The iodine-131 conjugated carbon iodine polymer shown in formula I has a conjugated carbon chain as a main chain and a radioactive isotope of iodine as a side chain 131 I, the iodine content is up to 84 percent. It is a nanofibrous structure (fig. 1) observed by scanning electron microscopy, generally distributed in the same direction overall. Iodine is a trace element necessary for human body, and is also a main raw material for synthesizing thyroid hormone. The physiological function of iodine is mainly to promote the growth and development of the organism and the differentiation of tissues by playing a role after thyroid hormone is synthesized by thyroid gland. Iodine has a dense and inseparable relationship with thyroid gland, and as is well understood, iodine is a synthetic thyroid hormoneThe thyroid gland is a "factory" for synthesizing thyroid hormone, which is a derivative of amino acid and is classified into two major groups, T3T4, and the T3T4 is an amino acid bonded with 3 or 4 iodine atoms. For this reason, our body, after absorbing iodine, concentrates toward the thyroid to synthesize hormones. The normal thyroid can enrich and take up 15% -45% of iodine within 24 hours, if the area is iodine-deficient, the demand of thyroid hormone of the body is increased, and the iodine-taking capability of the thyroid can be enhanced to 80%. After the iodine-131 conjugated carbon iodine polymer shown in the formula I is injected into a rat body, the enrichment and metabolism processes of the iodine-131 conjugated carbon iodine polymer in the body can be observed through CT imaging, and besides the target thyroid part, other much ingested iodine is smoothly discharged in the form of urine through the kidney (figure 2), so that no additional damage is caused to other tissues. For the in vivo circulating metabolism of the iodine-131 conjugated carbon iodine polymer, the iodine-131 conjugated carbon iodine polymer is enriched at a target position in the long circulation of blood in vivo, and the distribution of iodine in vivo can be tracked through CT in the whole process, and finally the required effect is verified (figure 3). The following are radioactive isotopes whose side chains are iodine 131 The structural formula of the conjugated carbon iodine polymer of I:
it will be understood by those skilled in the art that the foregoing is only a preferred embodiment of the present invention, and is not intended to limit the invention, and that any modification, equivalent replacement, or improvement made within the spirit and principle of the present invention should be included in the scope of the present invention.
Claims (5)
1. The application of the conjugated carbon iodine polymer in preparing the medicines for treating thyroid diseases by radioactive emission is characterized in that iodine atoms in the conjugated carbon iodine polymer have radioactive isotopes 131 I。
2. The use of claim 1, wherein the conjugated carbon iodine polymer has a structural formula comprising the structure of formula 1:
3. the use of claim 2, wherein the conjugated carbon-iodine polymer has a formula of formula i or formula ii:
4. use according to any one of claims 1 to 3, wherein the conjugated carbon-iodine polymer is prepared by reacting a conjugated carbon-iodine polymer with a base 131 And I, realizing thyroid disease radiotherapy by virtue of radioactive action.
5. The use of any one of claims 1 to 3, wherein the thyroid disorder is thyroid cancer or hyperthyroidism.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202210711531.6A CN115177750A (en) | 2022-06-22 | 2022-06-22 | Application of conjugated polymer in preparation of thyroid disease radiotherapy drug |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202210711531.6A CN115177750A (en) | 2022-06-22 | 2022-06-22 | Application of conjugated polymer in preparation of thyroid disease radiotherapy drug |
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| Publication Number | Publication Date |
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| CN115177750A true CN115177750A (en) | 2022-10-14 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN202210711531.6A Pending CN115177750A (en) | 2022-06-22 | 2022-06-22 | Application of conjugated polymer in preparation of thyroid disease radiotherapy drug |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB333946A (en) * | 1929-05-25 | 1930-08-25 | Ig Farbenindustrie Ag | Process for the manufacture of chlorine and bromine derivatives of compounds of the acetylene series |
| CN106344939A (en) * | 2016-09-29 | 2017-01-25 | 四川大学华西医院 | Preparation method and application of radioiodinated biodegradable chitosan-collagen composite microsphere medicine |
| CN112641924A (en) * | 2020-12-29 | 2021-04-13 | 黑龙江中医药大学 | Medicine for treating thyroid cancer and preparation method and application thereof |
| CN114149569A (en) * | 2021-11-30 | 2022-03-08 | 华中科技大学 | Conjugated carbon-iodine polymer, preparation and application thereof in preparing positioning marker |
-
2022
- 2022-06-22 CN CN202210711531.6A patent/CN115177750A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB333946A (en) * | 1929-05-25 | 1930-08-25 | Ig Farbenindustrie Ag | Process for the manufacture of chlorine and bromine derivatives of compounds of the acetylene series |
| CN106344939A (en) * | 2016-09-29 | 2017-01-25 | 四川大学华西医院 | Preparation method and application of radioiodinated biodegradable chitosan-collagen composite microsphere medicine |
| CN112641924A (en) * | 2020-12-29 | 2021-04-13 | 黑龙江中医药大学 | Medicine for treating thyroid cancer and preparation method and application thereof |
| CN114149569A (en) * | 2021-11-30 | 2022-03-08 | 华中科技大学 | Conjugated carbon-iodine polymer, preparation and application thereof in preparing positioning marker |
Non-Patent Citations (1)
| Title |
|---|
| AIWU SUN ET AL: "Preparation of Poly(diiododiacetylene),an Ordered Conjugated Polymer of Carbon and Iodine", 《SCIENCE》 * |
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