技术领域technical field
本发明涉及近视治疗领域，具体涉及一种前列腺素F2α受体激动剂在制备抑制近视药物上的应用及其使用方法。The invention relates to the field of myopia treatment, in particular to the application of a prostaglandin F2alpha receptor agonist in the preparation of myopia-suppressing medicine and its application method.
背景技术Background technique
前列腺素PGF2α是一种内源性激素，眼内有其受体FP的表达，现有技术中，前列腺素PGF2α作为影响及治疗青光眼的药物使用，其中治疗青光眼用的药物包括Latanoprost、travoprost、bimatoprost、unoprostone等，经眼内酶分解产生前列腺素F2α类似物，通过结合F2α受体FP，改变睫状肌张力，使小梁网细胞释放金属基质蛋白酶，消化睫状肌的“细胞外基质”，使组织疏松，细胞间隙增大，增加房水流出。Prostaglandin PGF2α is an endogenous hormone, and its receptor FP is expressed in the eye. In the prior art, prostaglandin PGF2α is used as a drug for affecting and treating glaucoma, wherein the drugs for treating glaucoma include Latanoprost, Travoprost, bimatoprost, unoprostone, etc., are decomposed by intraocular enzymes to produce prostaglandin F2α analogues. By binding to F2α receptor FP, they can change the tension of ciliary muscle, make trabecular meshwork cells release metal matrix protease, and digest ciliary muscle The "extracellular matrix" of the tissue loosens the intercellular space and increases the outflow of aqueous humor.
而现有的关于前列腺素与近视的研究中，到目前为止尚无发现有前列腺素F2α受体激动剂在制备抑制近视的作用报道。因此，我们猜想，可以通过调节眼内前列腺素F2α水平，从而达到干预近视发生发展的目的。However, in the existing research on prostaglandins and myopia, so far there is no report on the effect of prostaglandin F2α receptor agonists on inhibiting myopia. Therefore, we guess that the purpose of intervening the occurrence and development of myopia can be achieved by regulating the level of prostaglandin F2α in the eye.
发明内容Contents of the invention
为了解决现有技术的不足，本发明提供了一种前列腺素F2α受体激动剂在制备抑制近视药物上的应用及其使用方法。In order to solve the deficiencies in the prior art, the present invention provides an application of a prostaglandin F2α receptor agonist in the preparation of a medicine for inhibiting myopia and a use method thereof.
本发明采用的技术解决方案是：一种前列腺素F2α受体激动剂在制备抑制近视药物上的应用。The technical solution adopted in the present invention is: the application of a prostaglandin F2alpha receptor agonist in the preparation of medicines for inhibiting myopia.
所述的前列腺素F2α受体激动剂为拉坦前列腺素 。The prostaglandin F2alpha receptor agonist is latanoprost.
所述的前列腺素F2α受体激动剂为拉坦前列腺素游离酸。The prostaglandin F2alpha receptor agonist is latanoprost free acid.
所述的拉坦前列腺素游离酸在抑制近视上的用量为1-5μg／day。The dosage of the latanoprost free acid for inhibiting myopia is 1-5 μg/day.
所述的拉坦前列腺素游离酸在抑制近视上的用量为3μg／day。The dosage of the latanoprost free acid for inhibiting myopia is 3 μg/day.
一种所述的前列腺素F2α受体激动剂的使用方法，包括以下步骤：患眼结膜下注射浓度为30ug/ml的拉坦前列腺素游离酸100ul，连续注射4周。A method for using the prostaglandin F2α receptor agonist comprises the following steps: subconjunctival injection of 100 ul of latanoprost free acid with a concentration of 30 ug/ml in the affected eye, and continuous injection for 4 weeks.
本发明的有益效果是：本发明提供了一种前列腺素F2α受体激动剂在制备抑制近视药物上的应用及其使用方法，通过应用前列腺素F2α受体激动剂拉坦前列腺素游离酸，升从而升高眼内前列腺素F2α，从而抑制形觉剥夺引起的玻璃体腔延长及眼轴延长，稳定多巴胺D2受体在近视中的作用，Aripiprazole抑制了形觉剥夺性近视过程中的玻璃体腔以及眼轴的延长，从而抑制近视进展的作用。The beneficial effect of the present invention is: the present invention provides a prostaglandin F2α receptor agonist in the preparation of the application of myopia inhibitors and its use method, by using the prostaglandin F2α receptor agonist latanoprost Free acid, so as to increase prostaglandin F2α in the eye, thereby inhibiting the elongation of the vitreous cavity and eye axis caused by form deprivation, and stabilizing the role of dopamine D2 receptors in myopia. Aripiprazole inhibits the process of form deprivation myopia The vitreous cavity in the eye and the extension of the eye axis can inhibit the progression of myopia.
附图说明Description of drawings
图1是实验眼和对侧眼屈光度差值图。Figure 1 is a diagram of the diopter difference between the experimental eye and the fellow eye.
图2是实验眼和对侧眼玻璃体腔深度差值图。Figure 2 is a diagram of the difference in depth of the vitreous cavity between the experimental eye and the fellow eye.
图3是实验眼和对侧眼眼轴长度差值图。Figure 3 is a diagram of the difference in axial length between the experimental eye and the fellow eye.
图4是实验眼和对侧眼眼内压差值图。Figure 4 is a diagram of the intraocular pressure difference between the experimental eye and the fellow eye.
附图中，“差值”指实验眼与对侧眼屈光度或眼轴参数的差值；溶剂组和给药组之间比较采用独立样本T检验：“*” 表示P< 0.05。In the accompanying drawings, "difference" refers to the difference in diopter or eye axis parameters between the experimental eye and the fellow eye; the comparison between the solvent group and the drug treatment group uses an independent sample T test: "*" means P<0.05.
具体实施方式detailed description
实施例Example11
实验动物为3周龄英国种短毛三色豚鼠。采用面罩法进行单眼形觉剥夺（FD），并对形觉剥夺眼给予PGF2α类似物拉坦前列腺素游离酸（LAT-FA）结膜下注射，从而升高眼内PGF2α作用。动物随机分为2组：形觉剥夺+溶剂对照组（FD+DMSO），形觉剥夺+药物组（FD+ 30μg/ml LAT-FA 100ul）组。每天上午9点进行结膜下注射药物，连续注射4周，对侧眼不做处理。分别于实验前、给药2周、给药4周用红外偏心摄影验光仪（EIR）测量屈光度、A超（11MHz）测量玻璃体腔深度和眼轴长度等眼轴参数、用TonoVet TV01眼压计检测眼内压。The experimental animals were 3-week-old British short-haired tricolor guinea pigs. Monocular form deprivation (FD) was performed by mask method, and subconjunctival injection of PGF2α analogue latanoprost free acid (LAT-FA) was given to form deprived eyes, so as to increase the intraocular PGF2α effect. Animals were randomly divided into two groups: form deprivation + solvent control group (FD+DMSO), form deprivation + drug group (FD+ 30μg/ml LAT-FA 100ul) group. Subconjunctival injections were performed at 9 am every day for 4 consecutive weeks, and the fellow eye was left untreated. Before the experiment, 2 weeks after administration, and 4 weeks after administration, the diopter was measured with infrared eccentric photography refractometer (EIR), the axial parameters such as vitreous cavity depth and axial length were measured with A-ultrasound (11MHz), and the TonoVet TV01 tonometer was used to measure the diopter. Check intraocular pressure.
实施例Example22
实验动物为3周龄英国种短毛三色豚鼠。采用面罩法进行单眼形觉剥夺（FD），并对形觉剥夺眼给予PGF2α类似物拉坦前列腺素游离酸（LAT-FA）结膜下注射，从而升高眼内PGF2α作用。动物随机分为2组：形觉剥夺+溶剂对照组（FD+DMSO），形觉剥夺+药物组（FD+ 1μg LAT-FA）组。每天上午9点进行结膜下注射药物，连续注射4周，对侧眼不做处理。分别于实验前、给药2周、给药4周用红外偏心摄影验光仪（EIR）测量屈光度、A超（11MHz）测量玻璃体腔深度和眼轴长度等眼轴参数、用TonoVet TV01眼压计检测眼内压。The experimental animals were 3-week-old British short-haired tricolor guinea pigs. Monocular form deprivation (FD) was performed by mask method, and subconjunctival injection of PGF2α analogue latanoprost free acid (LAT-FA) was given to form deprived eyes, so as to increase the intraocular PGF2α effect. Animals were randomly divided into two groups: form deprivation + solvent control group (FD+DMSO), form deprivation + drug group (FD+ 1μg LAT-FA) group. Subconjunctival injections were performed at 9 am every day for 4 consecutive weeks, and the fellow eye was left untreated. Before the experiment, 2 weeks after administration, and 4 weeks after administration, the diopter was measured with infrared eccentric photography refractometer (EIR), the axial parameters such as vitreous cavity depth and axial length were measured with A-ultrasound (11MHz), and the TonoVet TV01 tonometer was used to measure the diopter. Check intraocular pressure.
实施例Example33
实验动物为3周龄英国种短毛三色豚鼠。采用面罩法进行单眼形觉剥夺（FD），并对形觉剥夺眼给予PGF2α类似物拉坦前列腺素游离酸（LAT-FA）结膜下注射，从而升高眼内PGF2α作用。动物随机分为2组：形觉剥夺+溶剂对照组（FD+DMSO），形觉剥夺+药物组（FD+ 5μg LAT-FA）组。每天上午9点进行结膜下注射药物，连续注射4周，对侧眼不做处理。分别于实验前、给药2周、给药4周用红外偏心摄影验光仪（EIR）测量屈光度、A超（11MHz）测量玻璃体腔深度和眼轴长度等眼轴参数、用TonoVet TV01眼压计检测眼内压。The experimental animals were 3-week-old British short-haired tricolor guinea pigs. Monocular form deprivation (FD) was performed by mask method, and subconjunctival injection of PGF2α analogue latanoprost free acid (LAT-FA) was given to form deprived eyes, so as to increase the intraocular PGF2α effect. Animals were randomly divided into two groups: form deprivation + solvent control group (FD+DMSO), form deprivation + drug group (FD+ 5μg LAT-FA) group. Subconjunctival injections were performed at 9 am every day for 4 consecutive weeks, and the fellow eye was left untreated. Before the experiment, 2 weeks after administration, and 4 weeks after administration, the diopter was measured with infrared eccentric photography refractometer (EIR), the axial parameters such as vitreous cavity depth and axial length were measured with A-ultrasound (11MHz), and the TonoVet TV01 tonometer was used to measure the diopter. Check intraocular pressure.
比较实验前后测量参数，发现给药组的形觉剥夺眼，屈光近视程度和玻璃体腔及眼轴延长程度均小于形觉剥夺溶剂组，和溶剂对照组比较具有统计学意义。因此，结膜下注射LAT-FA升高眼内PGF2α的作用可以抑制豚鼠形觉剥夺性近视的进展。Comparing the measured parameters before and after the experiment, it was found that the degree of refractive myopia, vitreous cavity and eye axis extension of the form deprived eyes of the drug treatment group were smaller than those of the form deprivation solvent group, which was statistically significant compared with the solvent control group. Therefore, subconjunctival injection of LAT-FA to elevate intraocular PGF2α can inhibit the progression of form deprivation myopia in guinea pigs.
由图1可知，实验4周后，形觉剥夺注射LAT-FA与形觉剥夺注射溶剂组相比近视形成量明显减少，说明LAT-FA能抑制形觉剥夺性近视的进展。It can be seen from Figure 1 that after 4 weeks of the experiment, the amount of myopia formed by the form deprivation injection of LAT-FA was significantly reduced compared with the form deprivation injection vehicle group, indicating that LAT-FA can inhibit the progression of form deprivation myopia.
由图2可知，实验4周后，给药组玻璃体腔延长与溶剂组相比相对较小，说明LAT-FA能抑制形觉剥夺引起的玻璃体腔延长。It can be seen from Figure 2 that after 4 weeks of the experiment, the extension of the vitreous cavity in the administration group was relatively smaller than that in the solvent group, indicating that LAT-FA can inhibit the extension of the vitreous cavity caused by form deprivation.
由图3可知，实验4周后，给药组眼轴延长与溶剂组相比相对较小，说明LAT-FA能抑制形觉剥夺引起的眼轴延长。It can be seen from Figure 3 that after 4 weeks of the experiment, the ocular axis extension of the administration group was relatively smaller than that of the solvent group, indicating that LAT-FA can inhibit the ocular axis extension caused by form deprivation.
由图4可知，实验4周后，给药组与溶剂组相比眼内压没有显著变化，说明LAT-FA并未影响眼内压，该剂量为安全剂量。It can be seen from Figure 4 that after 4 weeks of the experiment, the intraocular pressure of the administration group had no significant change compared with the solvent group, indicating that LAT-FA did not affect the intraocular pressure, and this dose is a safe dose.
上述实验，证明利用前列腺素PGF2α类似物LAT-FA升高眼内PGF2α的作用，可明显起到抑制近视进展的作用。The above experiments prove that the use of prostaglandin PGF2α analogue LAT-FA to increase intraocular PGF2α can significantly inhibit the progression of myopia.
以上所述仅是本发明的优选实施方式，本发明的保护范围并不仅局限于上述实施例，凡属于本发明思路下的技术方案均属于本发明的保护范围。应当指出，对于本技术领域的普通技术人员来说，在不脱离本发明原理前提下的若干改进和润饰，这些改进和润饰也应视为本发明的保护范围。The above descriptions are only preferred implementations of the present invention, and the protection scope of the present invention is not limited to the above-mentioned embodiments, and all technical solutions under the idea of the present invention belong to the protection scope of the present invention. It should be pointed out that for those skilled in the art, some improvements and modifications without departing from the principles of the present invention should also be regarded as the protection scope of the present invention.
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610323246.1ACN105998030A (en) | 2016-05-17 | 2016-05-17 | Application of a prostaglandin F2α receptor agonist in the preparation of medicines for inhibiting myopia and its application method |
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610323246.1ACN105998030A (en) | 2016-05-17 | 2016-05-17 | Application of a prostaglandin F2α receptor agonist in the preparation of medicines for inhibiting myopia and its application method |
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| CN105998030Atrue CN105998030A (en) | 2016-10-12 |
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610323246.1APendingCN105998030A (en) | 2016-05-17 | 2016-05-17 | Application of a prostaglandin F2α receptor agonist in the preparation of medicines for inhibiting myopia and its application method |
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| RJ01 | Rejection of invention patent application after publication | Application publication date:20161012 | |
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