WO2024082230A1 - Use of deslorelin acetate in preparation of drug for regulating sexual cycle of animal - Google Patents
Use of deslorelin acetate in preparation of drug for regulating sexual cycle of animal Download PDFInfo
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- WO2024082230A1 WO2024082230A1 PCT/CN2022/126514 CN2022126514W WO2024082230A1 WO 2024082230 A1 WO2024082230 A1 WO 2024082230A1 CN 2022126514 W CN2022126514 W CN 2022126514W WO 2024082230 A1 WO2024082230 A1 WO 2024082230A1
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/08—Peptides having 5 to 11 amino acids
- A61K38/09—Luteinising hormone-releasing hormone [LHRH], i.e. Gonadotropin-releasing hormone [GnRH]; Related peptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
Definitions
- the invention relates to the field of sexual cycle regulating drugs, and in particular to application of deserorelin acetate in preparing drugs for regulating the sexual cycle of animals.
- the prior art generally monitors the natural sexual cycle of female adult rats by sampling vaginal secretions.
- the vaginal secretions of the rats are taken, and the morphology of the vaginal cell fragments in the secretions is observed, and compared with the characteristics of the secretions of the rats during estrus, so as to determine whether the rats are currently in estrus. If they are in estrus, male rats are arranged for mating; if they are not in estrus, vaginal smears are continuously collected every day, waiting for the animals to enter estrus. Animals that are continuously not in estrus are eliminated.
- the present invention proposes the use of deserorelin acetate in the preparation of drugs for regulating the sexual cycle of animals.
- drugs are used to synchronize the animal cycle and improve the breeding efficiency for adult female rats with sexual cycle disorders.
- the invention provides application of deserorelin acetate in preparing a drug for regulating animal sexual cycle.
- the animal is a rat.
- the medicine is an injection.
- the dosage of deserorelin acetate is 20-40 ⁇ g/mouse.
- the administration dose of deserorelin acetate was 20 ⁇ g/mouse.
- the administration dose of deserorelin acetate was 40 ⁇ g/mouse.
- the drug is administered by injection, and the injection method is any one of subcutaneous injection or intradermal injection, preferably subcutaneous injection.
- the present invention also provides the use of deserorelin acetate as the only active ingredient in the preparation of a medicine for regulating the sexual cycle of animals.
- the present invention also provides a drug for regulating the sexual cycle of animals, wherein deserorelin acetate is the only active ingredient.
- the present invention also provides a method for preparing the drug, comprising the following steps: taking out the storage solution of deserorelin acetate, placing it on ice to completely dissolve it, and using a 1 ml syringe to draw the storage solution of deserorelin acetate for standby use.
- the use of the drug of the present invention does not require daily sampling of each animal, and does not require continuous monitoring of the animal's sexual cycle. Therefore, a large amount of time and labor costs can be saved in large-scale breeding needs.
- the sexual cycle of rats can be determined without relying on the staff's experience in identifying the sexual cycle of animals, thereby achieving the effect of accurate breeding.
- the estrus period of female adult rats can be accurately predicted and breeding can be precisely arranged.
- the conception date of female rats can be controlled, thus saving breeding time and improving breeding efficiency.
- accurate prediction of the estrus period in advance also reserves sufficient time for subsequent gene editing experiment preparations, which helps to improve work efficiency.
- the drug of the present invention is used to regulate the sexual cycle of female rats, and the pregnancy rate of female rats is as high as 100%.
- the administration route of the present invention is simple and easy to learn, and the operator can master it without a lot of practice.
- FIG. 1 is a schematic flow chart of an experimental method proposed in an embodiment of the present invention.
- Desserelin acetate is a structural analogue of LHRH (gonadotropin-releasing hormone) and has similar physiological effects to LHRH in the body.
- Gonadotropin-releasing hormone is a releasing hormone secreted by the hypothalamus, which acts on the pituitary gland to release follicle-stimulating hormone (FSH) and luteinizing hormone (LH).
- FSH and LH act on the ovaries.
- the main function of FSH is to promote the development and maturation of follicles and the secretion of estrogen, while the main function of LH is to promote female ovulation and corpus luteum production, and to promote the secretion of estrogen and progesterone by the corpus luteum. Therefore, additional supplementation of LHRH structural analogues can adjust the sexual cycle of rats.
- the invention uses a method of subcutaneously injecting desserelin acetate into female adult rats through the neck skin to adjust the sexual cycle of female rats. After 72 hours of the injection, mating with male rats can successfully conceive.
- Drug Desorelin acetate/gonadorelin acetate.
- Dissolution method Dissolve in sterile water for injection, pay attention to aseptic operation.
- Test animals Female adult rats
- Injection dose 20 ⁇ g (0.05 ml)
- Test animals Female adult rats
- Injection dose 40 ⁇ g (0.1 ml)
- Test animals Female adult rats
- Injection dose 40 ⁇ g (0.1 ml)
- Test animals Female adult rats
- Injection method intraperitoneal injection
- Injection dose 40 ⁇ g (0.1 ml)
- Test animals Female adult rats
- Injection dose 40 ⁇ g (0.1 ml)
- Test animals Female adult rats
- Example 1 The results showed that one of the three rats in Example 1 became pregnant, with a pregnancy rate of 33.3%; all of the five rats in Example 2 became pregnant, with a pregnancy rate of 100%; one of the four rats in Example 3 became pregnant, with a pregnancy rate of 25%; none of the three rats injected intraperitoneally in Example 5 became pregnant, with a pregnancy rate of 0.
- Examples 2-4 injected the same dose of the drug, but the injection method was different.
- the results showed that subcutaneous injection was better than intradermal injection, and intraperitoneal injection had no effect.
- the injection method was the same, both were subcutaneous injections, but the drug dosage was different, indicating that 40 ⁇ g/rat was better than 20 ⁇ g/rat.
- the above results show that desserelin acetate, as a drug for regulating the sexual cycle of rats, can achieve a 100% pregnancy rate in rats by subcutaneous injection and a dose of 40 ⁇ g/rat.
- Example 2 The same volume of drug and solvent were injected subcutaneously, and the pregnancy rates of the control group (Comparative Example 1) and the experimental group (Example 2) were compared.
- the pregnancy rate of Example 2 was 100%, and all 5 rats were pregnant.
- the pregnancy rate of Comparative Example 1 was 0, which ruled out the influence of the experimental operation on the pregnancy rate of rats.
- deserorelin acetate As a small polypeptide molecule, deserorelin acetate is very easy to be degraded. If taken orally, it is decomposed into amino acids by digestive enzymes in the small intestine, loses its structural similarity with Gnrh, and thus loses its function. Injection can ensure that the molecular structure of the drug is not destroyed and maintains its activity; and for subcutaneous injection, this injection route does not release the drug into the blood in one go, so it has a certain sustained release effect, and the drug effect is most obvious. Therefore, deserorelin acetate of the present invention is preferably administered by subcutaneous injection as a drug for regulating sexual cycles. As a drug, it is not necessary to add excipients, pay attention to the dilution method and solvent, timely subpackage and strictly store at low temperature, and prohibit repeated freezing and thawing.
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- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Endocrinology (AREA)
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- Animal Behavior & Ethology (AREA)
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Abstract
The present invention provides a use of deslorelin acetate in preparation of a drug for adjusting a sexual cycle of an animal. The animal is a rat, and the drug is an injection, preferably administered by subcutaneous injection. By using the drug of the present invention, there is no need to sample each animal every day, which allows for significant time cost savings and labor cost savings, and the sexual cycle of the rat can be determined without depending on staff's experience in identifying the sexual cycle of the animal, so as to achieve the effect of accurate breeding, and for a sexual cycle disorder of the adult female rat, the cycle of the animal is synchronized and the breeding efficiency is improved by using the drug, and the conception rate of the female rat is as high as 100%.
Description
本发明涉及性周期调节药物领域，特别涉及醋酸德舍瑞林在制备调节动物的性周期药物中的应用。The invention relates to the field of sexual cycle regulating drugs, and in particular to application of deserorelin acetate in preparing drugs for regulating the sexual cycle of animals.
雌性成年大鼠遇到应激会发生性周期紊乱，周期紊乱期间不接受配种，从而繁殖能力下降；而调节雌性大鼠性周期可以快速使雌性大鼠处于发情期，且能控制发情期时间，在发情时间内与雄性成年大鼠配种，则可达到精准配种的效果，配种成功即可进行下一步基因编辑实验或者满足扩大繁殖需求。When female adult rats encounter stress, their sexual cycle will be disrupted, and they will not accept mating during the disordered cycle, which will reduce their reproductive capacity. However, regulating the sexual cycle of female rats can quickly put female rats into estrus and control the duration of the estrus period. When they are mated with male adult rats during the estrus period, the effect of precise breeding can be achieved. If the mating is successful, the next step of gene editing experiments can be carried out or the needs of expanding reproduction can be met.
现有技术一般通过阴道分泌物采样监测雌性成年大鼠自然性周期。取大鼠阴道分泌物，观察分泌物里的阴道细胞残片形态，对照大鼠发情期分泌物特点，从而判断大鼠当下是否处于发情期，如处于发情期则安排雄性大鼠配种；如不处于发情期，则继续每日采样阴道涂片，等待动物进入发情期。持续不发情的动物则予以淘汰。但是这个方法存在诸多缺点：(1)每只动物每天进行阴道涂片采样，工作量大，不适用于规模繁殖；(2)需依赖经验判断大鼠是否处于发情期，因此工作人员需要具备一定的辨别经验才可做出准确判断；(3)对于性周期紊乱的大鼠需一直监测，不能预测其发情时间，因此配种效率低下，导致实验周期过长。因此出于精准配种需要，目前亟需一种针对成年雌性大鼠性周期紊乱、同步动物性周期、提高配种效率的药物。The prior art generally monitors the natural sexual cycle of female adult rats by sampling vaginal secretions. The vaginal secretions of the rats are taken, and the morphology of the vaginal cell fragments in the secretions is observed, and compared with the characteristics of the secretions of the rats during estrus, so as to determine whether the rats are currently in estrus. If they are in estrus, male rats are arranged for mating; if they are not in estrus, vaginal smears are continuously collected every day, waiting for the animals to enter estrus. Animals that are continuously not in estrus are eliminated. However, this method has many disadvantages: (1) Vaginal smear sampling is performed on each animal every day, which is a large workload and is not suitable for large-scale breeding; (2) It is necessary to rely on experience to determine whether the rats are in estrus, so the staff needs to have certain identification experience to make an accurate judgment; (3) Rats with disordered sexual cycles need to be monitored all the time, and their estrus time cannot be predicted, so the mating efficiency is low, resulting in a long experimental cycle. Therefore, for the purpose of accurate mating, there is an urgent need for a drug that can treat disordered sexual cycles of adult female rats, synchronize animal sexual cycles, and improve mating efficiency.
发明内容Summary of the invention
针对现有技术中的缺陷，本发明提出了醋酸德舍瑞林在制备调节动物 的性周期药物中的应用，出于精准配种需要，针对成年雌性大鼠性周期紊乱，利用药物同步动物周期，提高配种效率。In view of the defects in the prior art, the present invention proposes the use of deserorelin acetate in the preparation of drugs for regulating the sexual cycle of animals. For the purpose of accurate breeding, drugs are used to synchronize the animal cycle and improve the breeding efficiency for adult female rats with sexual cycle disorders.
本发明提供醋酸德舍瑞林在制备调节的动物性周期药物中的应用。The invention provides application of deserorelin acetate in preparing a drug for regulating animal sexual cycle.
进一步的，所述动物为大鼠。Furthermore, the animal is a rat.
进一步的，所述药物为注射剂。Furthermore, the medicine is an injection.
进一步的，醋酸德舍瑞林的给药剂量为20～40μg/鼠。Furthermore, the dosage of deserorelin acetate is 20-40 μg/mouse.
进一步的，醋酸德舍瑞林的给药剂量为20μg/鼠。Furthermore, the administration dose of deserorelin acetate was 20 μg/mouse.
进一步的，醋酸德舍瑞林的给药剂量为40μg/鼠。Furthermore, the administration dose of deserorelin acetate was 40 μg/mouse.
进一步的，所述药物通过注射进行给药，所述注射方式为皮下注射或皮内注射中的任意一种，优选为皮下注射。Furthermore, the drug is administered by injection, and the injection method is any one of subcutaneous injection or intradermal injection, preferably subcutaneous injection.
本发明还提供醋酸德舍瑞林作为唯一活性成份在制备调节动物的性周期的药物中的应用。The present invention also provides the use of deserorelin acetate as the only active ingredient in the preparation of a medicine for regulating the sexual cycle of animals.
本发明还提供一种调节动物的性周期的药物，所述药物中醋酸德舍瑞林作为唯一活性成份。The present invention also provides a drug for regulating the sexual cycle of animals, wherein deserorelin acetate is the only active ingredient.
本发明还提供所述药物的制备方法，包括如下步骤：取出醋酸得舍瑞林储存液，置于冰上溶解完全，以1ml注射器吸取醋酸得舍瑞林储存液，备用。The present invention also provides a method for preparing the drug, comprising the following steps: taking out the storage solution of deserorelin acetate, placing it on ice to completely dissolve it, and using a 1 ml syringe to draw the storage solution of deserorelin acetate for standby use.
综上，与现有技术相比，本发明达到了以下技术效果：In summary, compared with the prior art, the present invention achieves the following technical effects:
(1)使用本发明的药物，不需要对每只动物每天采样，不需要持续监测动物性周期，因此在规模化繁殖需求中，可大量节省时间成本和人力成本。(1) The use of the drug of the present invention does not require daily sampling of each animal, and does not require continuous monitoring of the animal's sexual cycle. Therefore, a large amount of time and labor costs can be saved in large-scale breeding needs.
(2)不依赖于工作人员对动物的性周期辨别经验即可判断大鼠性周期，达到精准繁殖的效果。(2) The sexual cycle of rats can be determined without relying on the staff's experience in identifying the sexual cycle of animals, thereby achieving the effect of accurate breeding.
(3)按照标准操作流程操作，可以精准预测雌性成年大鼠发情期，精 准安排配种，雌性大鼠受孕日期可控，因此可以节约配种时间，提高配种效率，同时提前准确预测发情期也为后续基因编辑实验准备工作预留出充分时间，有助于提高工作效率。(3) By following the standard operating procedures, the estrus period of female adult rats can be accurately predicted and breeding can be precisely arranged. The conception date of female rats can be controlled, thus saving breeding time and improving breeding efficiency. At the same time, accurate prediction of the estrus period in advance also reserves sufficient time for subsequent gene editing experiment preparations, which helps to improve work efficiency.
(4)使用本发明的药物对雌性大鼠性周期进行调控，雌性大鼠受孕率高达100％。(4) The drug of the present invention is used to regulate the sexual cycle of female rats, and the pregnancy rate of female rats is as high as 100%.
(5)本发明给药途径简单易学，操作者无需大量练习即可掌握。(5) The administration route of the present invention is simple and easy to learn, and the operator can master it without a lot of practice.
为了更清楚地说明本发明实施例的技术方案，下面将对实施例中所需要使用的附图作简单地介绍，应当理解，以下附图仅示出了本发明的某些实施例，因此不应被看作是对范围的限定，对于本领域普通技术人员来讲，在不付出创造性劳动的前提下，还可以根据这些附图获得其他相关的附图。In order to more clearly illustrate the technical solutions of the embodiments of the present invention, the drawings required for use in the embodiments are briefly introduced below. It should be understood that the following drawings only show certain embodiments of the present invention and therefore should not be regarded as limiting the scope. For ordinary technicians in this field, other related drawings can be obtained based on these drawings without creative work.
图1为本发明实施例提出的实验方法的流程示意图。FIG. 1 is a schematic flow chart of an experimental method proposed in an embodiment of the present invention.
为了使本技术领域的人员更好地理解本发明方案，下面将结合本发明实施例中的附图，对本发明实施例中的技术方案进行清楚、完整地描述，显然，所描述的实施例仅仅是本发明一部分的实施例，而不是全部的实施例。基于本发明中的实施例，本领域普通技术人员在没有做出创造性劳动的前提下所获得的所有其他实施例，都应当属于本发明保护的范围。In order to enable those skilled in the art to better understand the scheme of the present invention, the technical scheme in the embodiments of the present invention will be clearly and completely described below in conjunction with the drawings in the embodiments of the present invention. Obviously, the described embodiments are only part of the embodiments of the present invention, not all of the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without creative work should fall within the scope of protection of the present invention.
醋酸得舍瑞林是LHRH(促性腺激素释放激素)的结构类似物，在体内与LHRH有类似的生理作用。促性腺激素释放激素是下丘脑分泌的释放激素，作用于垂体，使垂体释放卵泡刺激素(FSH)和黄体生成素(LH),FSH和LH作用于卵巢。FSH的主要作用是促进卵泡发育、成熟以及分泌雌激素，而LH的作用主要是促进雌性排卵和黄体生成，促使黄体分泌雌激素和孕激素，因此，额外补充LHRH结构类似物可调整大鼠性周期。Desserelin acetate is a structural analogue of LHRH (gonadotropin-releasing hormone) and has similar physiological effects to LHRH in the body. Gonadotropin-releasing hormone is a releasing hormone secreted by the hypothalamus, which acts on the pituitary gland to release follicle-stimulating hormone (FSH) and luteinizing hormone (LH). FSH and LH act on the ovaries. The main function of FSH is to promote the development and maturation of follicles and the secretion of estrogen, while the main function of LH is to promote female ovulation and corpus luteum production, and to promote the secretion of estrogen and progesterone by the corpus luteum. Therefore, additional supplementation of LHRH structural analogues can adjust the sexual cycle of rats.
本发明采用雌性成年大鼠经颈部皮肤皮下注射醋酸德舍瑞林的方法调整雌性大鼠性周期，注射72小时过后，与雄鼠配种，即可成功受孕。The invention uses a method of subcutaneously injecting desserelin acetate into female adult rats through the neck skin to adjust the sexual cycle of female rats. After 72 hours of the injection, mating with male rats can successfully conceive.
实验方法：experimental method:
醋酸得舍瑞林/醋酸戈那瑞林储存液配制Preparation of Deserelin Acetate/Gonadorelin Acetate Stock Solution
药品：醋酸得舍瑞林/醋酸戈那瑞林。Drug: Desorelin acetate/gonadorelin acetate.
品牌：碧云天。Brand: Biyuntian.
Catalog NO:P9068。Catalog NO:P9068.
CAS号：57773-65-6。CAS number: 57773-65-6.
规格：1mg。Specification: 1mg.
状态：粉末。State: Powder.
溶解方法：灭菌注射用水溶解，注意无菌操作。Dissolution method: Dissolve in sterile water for injection, pay attention to aseptic operation.
储存浓度：400μg/ml。Stock concentration: 400 μg/ml.
储存条件：分装于-80℃储存，3个月内使用完毕。Storage conditions: Store at -80℃ in aliquots and use within 3 months.
提前半小时从冰箱中取出醋酸得舍瑞林/醋酸戈那瑞林储存液，置于冰上溶解完全，以1ml注射器吸取适量醋酸得舍瑞林/醋酸戈那瑞林储存液，将药物注射入大鼠体内。注射结束放大鼠回居家笼，按照日常动物管理进行即可，注射结束72小时后与一只雄性大鼠配种，隔天早晨检查雌性大鼠阴道栓，镜检见精子，即判断受孕，统计受孕大鼠的数量，计算受孕率。Take out the storage solution of deserelin acetate/gonadorelin acetate from the refrigerator half an hour in advance, place it on ice to dissolve completely, draw an appropriate amount of deserelin acetate/gonadorelin acetate storage solution with a 1ml syringe, and inject the drug into the rat. After the injection, put the rat back to the home cage and follow the daily animal management. 72 hours after the injection, mate with a male rat. Check the vaginal plug of the female rat the next morning. If sperm is seen under the microscope, it is judged that the rat is pregnant. Count the number of pregnant rats and calculate the pregnancy rate.
实施例1Example 1
受试动物：雌性成年大鼠Test animals: Female adult rats
器械：1ml注射针Instrument: 1ml injection needle
药物：醋酸得舍瑞林注射液(400μg/ml)Drug: Desserelin acetate injection (400 μg/ml)
注射方式：皮下注射Injection method: Subcutaneous injection
注射剂量：20μg(0.05ml)Injection dose: 20 μg (0.05 ml)
实施例2Example 2
受试动物：雌性成年大鼠Test animals: Female adult rats
器械：1ml注射针Instrument: 1ml injection needle
药物：醋酸得舍瑞林注射液(400μg/ml)Drug: Desserelin acetate injection (400 μg/ml)
注射方式：皮下注射Injection method: Subcutaneous injection
注射剂量：40μg(0.1ml)Injection dose: 40 μg (0.1 ml)
实施例3Example 3
受试动物：雌性成年大鼠Test animals: Female adult rats
器械：1ml注射针Instrument: 1ml injection needle
药物：醋酸得舍瑞林注射液(400μg/ml)Drug: Desserelin acetate injection (400 μg/ml)
注射方式：皮内注射Injection method: Intradermal injection
注射剂量：40μg(0.1ml)Injection dose: 40 μg (0.1 ml)
实施例4Example 4
受试动物：雌性成年大鼠Test animals: Female adult rats
器械：1ml注射针Instrument: 1ml injection needle
药物：醋酸得舍瑞林注射液(400μg/ml)Drug: Desserelin acetate injection (400 μg/ml)
注射方式：腹腔注射Injection method: intraperitoneal injection
注射剂量：40μg(0.1ml)Injection dose: 40 μg (0.1 ml)
实施例5Example 5
受试动物：雌性成年大鼠Test animals: Female adult rats
器械：1ml注射针Instrument: 1ml injection needle
药物：醋酸戈那瑞林注射液(400μg/ml)Drug: Gonadorelin acetate injection (400 μg/ml)
注射方式：皮下注射Injection method: Subcutaneous injection
注射剂量：40μg(0.1ml)Injection dose: 40 μg (0.1 ml)
对比例1Comparative Example 1
受试动物：雌性成年大鼠Test animals: Female adult rats
器械：1ml注射针Instrument: 1ml injection needle
药物：灭菌注射用水Drug: Sterile water for injection
注射方式：皮下注射Injection method: Subcutaneous injection
注射剂量：0.1mlInjection dose: 0.1ml
大鼠的受孕率结果如表1所示：The results of pregnancy rate of rats are shown in Table 1:
表1Table 1
结果显示，实施例1的3只大鼠受孕1只，受孕率为33.3％；实施例2的5只大鼠全部受孕，受孕率为100％，实施例3的4只大鼠有1只受孕，受孕率为25％；实施例5采用腹腔注射的3只大鼠全部没有受孕，受孕率为0。实施例2-4注射相同剂量的药物，只是注射方式不同，结果表明皮下注射的效果优于皮内注射，腹腔注射没有效果。实施例1和实施例2相比，注射方式相同，均为皮下注射，只是药物剂量不同，说明40μg/鼠比20μg/鼠的效果更好。以上结果表明，醋酸德舍瑞林作为调节大鼠性周期的药物，采用皮下注射的方式和40μg/鼠的剂量，能够使大鼠的受孕率达到100％。The results showed that one of the three rats in Example 1 became pregnant, with a pregnancy rate of 33.3%; all of the five rats in Example 2 became pregnant, with a pregnancy rate of 100%; one of the four rats in Example 3 became pregnant, with a pregnancy rate of 25%; none of the three rats injected intraperitoneally in Example 5 became pregnant, with a pregnancy rate of 0. Examples 2-4 injected the same dose of the drug, but the injection method was different. The results showed that subcutaneous injection was better than intradermal injection, and intraperitoneal injection had no effect. Compared with Example 1 and Example 2, the injection method was the same, both were subcutaneous injections, but the drug dosage was different, indicating that 40μg/rat was better than 20μg/rat. The above results show that desserelin acetate, as a drug for regulating the sexual cycle of rats, can achieve a 100% pregnancy rate in rats by subcutaneous injection and a dose of 40μg/rat.
以皮下注射方式，注射相同体积的药物和溶剂，对比对照组(对比例1)和实验组(实施例2)受孕率，实施例2的受孕率是100％，5只大鼠全部 受孕，对比例1的受孕率是0，由此可以排除实验操作对大鼠受孕率的影响。The same volume of drug and solvent were injected subcutaneously, and the pregnancy rates of the control group (Comparative Example 1) and the experimental group (Example 2) were compared. The pregnancy rate of Example 2 was 100%, and all 5 rats were pregnant. The pregnancy rate of Comparative Example 1 was 0, which ruled out the influence of the experimental operation on the pregnancy rate of rats.
醋酸得舍瑞林作为多肽小分子，极容易被降解，若通过口服，则在小肠中被消化酶分解为氨基酸，失去与Gnrh的结构相似性，因此失去功能。注射可以保证药物分子结构不被破坏，保持活性；且对皮下注射来说，此注射途径并非一次性释放药物进入血液，因此起到一定缓释效果，药物作用发挥最明显。因此本发明的醋酸得舍瑞林作为调节性周期的药物，优选以皮下注射的方式给药。作为药物不需要添加辅料，注意稀释方式和溶剂，及时分装并严格低温保存，并禁止反复冻融。As a small polypeptide molecule, deserorelin acetate is very easy to be degraded. If taken orally, it is decomposed into amino acids by digestive enzymes in the small intestine, loses its structural similarity with Gnrh, and thus loses its function. Injection can ensure that the molecular structure of the drug is not destroyed and maintains its activity; and for subcutaneous injection, this injection route does not release the drug into the blood in one go, so it has a certain sustained release effect, and the drug effect is most obvious. Therefore, deserorelin acetate of the present invention is preferably administered by subcutaneous injection as a drug for regulating sexual cycles. As a drug, it is not necessary to add excipients, pay attention to the dilution method and solvent, timely subpackage and strictly store at low temperature, and prohibit repeated freezing and thawing.
以上所述仅为本发明的较佳实施例，并不用以限制本发明，凡在本发明的精神和原则之内，所作的任何修改、等同替换、改进等，均应包含在本发明的保护范围之内。The above description is only a preferred embodiment of the present invention and is not intended to limit the present invention. Any modifications, equivalent substitutions, improvements, etc. made within the spirit and principle of the present invention should be included in the protection scope of the present invention.
Claims (10)
- 醋酸德舍瑞林在制备调节动物的性周期药物中的应用。Use of deserorelin acetate in the preparation of drugs for regulating the sexual cycle of animals.
- 根据权利要求1所述的应用，其特征在于，所述动物为大鼠。The use according to claim 1, characterized in that the animal is a rat.
- 根据权利要求1所述的应用，其特征在于，所述药物为注射剂。The use according to claim 1 is characterized in that the medicine is an injection.
- 根据权利要求1所述的应用，其特征在于，醋酸德舍瑞林的给药剂量为20～40μg/鼠。The use according to claim 1, characterized in that the dosage of deserorelin acetate is 20 to 40 μg/mouse.
- 根据权利要求1所述的应用，其特征在于，醋酸德舍瑞林的给药剂量为20μg/鼠。The use according to claim 1, characterized in that the dosage of deserorelin acetate is 20 μg/mouse.
- 根据权利要求1所述的应用，其特征在于，醋酸德舍瑞林的给药剂量为40μg/鼠。The use according to claim 1, characterized in that the dosage of deserorelin acetate is 40 μg/mouse.
- 根据权利要求1所述的应用，其特征在于，所述药物通过注射进行给药，所述注射方式为皮下注射或皮内注射中的任意一种，优选为皮下注射。The use according to claim 1 is characterized in that the drug is administered by injection, and the injection method is any one of subcutaneous injection or intradermal injection, preferably subcutaneous injection.
- 根据权利要求1所述的应用，其特征在于，醋酸德舍瑞林作为唯一活性成份在制备调节动物的性周期药物中的应用。The use according to claim 1 is characterized in that deserorelin acetate is used as the sole active ingredient in the preparation of a drug for regulating the sexual cycle of animals.
- 一种调节动物的性周期的药物，其特征在于，所述药物中醋酸德舍瑞林作为唯一活性成份。A drug for regulating the sexual cycle of animals, characterized in that deserorelin acetate is the only active ingredient in the drug.
- 权利要求9所述药物的制备方法，其特征在于，包括如下步骤：The method for preparing the drug according to claim 9, characterized in that it comprises the following steps:取出醋酸得舍瑞林储存液，置于冰上溶解完全，以1ml注射器吸取醋酸得舍瑞林储存液，备用。Take out the serrelin acetate storage solution, place it on ice to dissolve completely, and use a 1 ml syringe to draw up the serrelin acetate storage solution for later use.
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| US20050130894A1 (en) * | 2003-10-03 | 2005-06-16 | Thorn Bioscience Llc | Process for the synchronization of ovulation for timed breeding without heat detection |
| CN111202837A (en) * | 2018-11-22 | 2020-05-29 | 中国农业大学 | A preparation for controlling ovulation of equine animal and method for controlling ovulation |
| US20200376002A1 (en) * | 2019-05-30 | 2020-12-03 | Applied Technologies Consultants Inc. | Injectable Hormone Formulations for Estrous Cycle Control in Mammals, its Manufacturing Process, Estrous Cycle Control and Puberty Triggering Methods, and Pregnancy Enhancement in Mammals |
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