CN107468676A - A kind of medicinal for tranquilizing mind based on Desflurane - Google Patents
A kind of medicinal for tranquilizing mind based on Desflurane Download PDFInfo
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- DPYMFVXJLLWWEU-UHFFFAOYSA-N desflurane Chemical compound FC(F)OC(F)C(F)(F)F DPYMFVXJLLWWEU-UHFFFAOYSA-N 0.000 title claims abstract description 81
- 229960003537 desflurane Drugs 0.000 title claims abstract description 80
- 230000002936 tranquilizing effect Effects 0.000 title claims abstract description 43
- 239000003204 tranquilizing agent Substances 0.000 claims abstract description 44
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A—HUMAN NECESSITIES
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Abstract
本发明涉及到一种基于地氟烷的镇静安神药,包括药物和药物载体,所述药物为地氟烷。所述药物载体包括吸水材料和外壳;所述吸水材料用于承载地氟烷;所述外壳用于包覆吸水材料,用于避免地氟烷挥发;所述外壳上设置有开口,用于治疗过程中从开口处挥发地氟烷,开口上设置有封口装置。本发明提供的基于地氟烷的镇静安神药为一种通过呼吸方式接受药物的吸入型药,其镇静安神速度快、副作用小,而且该药起效后消退快,不会影响药品使用者正常的生活和工作。此外所述基于地氟烷的镇静安神药的生物转化率极低,对肝肾毒性极低或没有,适用于肝肾疾病患者。而且所述基于地氟烷的镇静安神药对血流动力和心率的影响极小,适用于接受心脏手术的患者。
The invention relates to a desflurane-based sedative and tranquilizer, which includes a drug and a drug carrier, and the drug is desflurane. The drug carrier includes a water-absorbing material and a shell; the water-absorbing material is used to carry desflurane; the shell is used to cover the water-absorbing material to prevent desflurane from volatilizing; the shell is provided with an opening for treating During the process, desflurane is volatilized from the opening, and a sealing device is arranged on the opening. The desflurane-based sedative and tranquilizer medicine provided by the present invention is an inhaled medicine that accepts the medicine through breathing. life and work. In addition, the desflurane-based sedative and tranquilizer has an extremely low biotransformation rate, and has extremely low or no liver and kidney toxicity, and is suitable for patients with liver and kidney diseases. Moreover, the desflurane-based sedative and tranquilizer has minimal impact on blood flow and heart rate, and is suitable for patients undergoing heart surgery.
Description
技术领域technical field
本发明涉及医药领域,尤其是一种基于地氟烷的镇静安神药。The invention relates to the field of medicine, in particular to a desflurane-based sedative and tranquilizer.
背景技术Background technique
随着生活节奏的逐步加快,当前经常被失眠焦虑症困扰的人群逐渐增多。而目前市面上针对失眠焦虑症通常采用口服安定类药物来进行缓解,但是安定类药物具有时间滞后性,会导致服用者白天嗜睡、乏力、精神萎靡等;更为严重的是,患有睡眠性呼吸暂停症的失眠者,因安眠药可延长呼吸暂停的时间,以致可能发生猝死;同时存在有些病人不适宜使用口服安定药或者注射安定剂的问题;而且口服安定类药物的生物转化率较高,对于肝肾疾病患者或接受心脏手术的患者不适用。With the gradual acceleration of the pace of life, the number of people who are often troubled by insomnia and anxiety is gradually increasing. At present, insomnia and anxiety are usually relieved by oral stable drugs on the market, but stable drugs have a time lag, which will cause drowsiness, fatigue, listlessness, etc. during the day; For insomniacs with apnea, because sleeping pills can prolong the time of apnea, sudden death may occur; at the same time, some patients are not suitable for taking oral tranquilizers or injecting tranquilizers; and the biotransformation rate of oral tranquilizers is relatively high. Not for use in patients with liver or kidney disease or those undergoing cardiac surgery.
发明内容Contents of the invention
本发明的目的在于提供一种基于地氟烷的镇静安神药,改善目前安定类药物在缓解失眠、焦虑、烦躁等一些精神类疾病过程中存在的一些弊端。The object of the present invention is to provide a desflurane-based sedative and tranquilizer, which can improve some disadvantages of current tranquilizers in relieving insomnia, anxiety, irritability and other mental diseases.
本发明解决的第一个问题是提供一种起效快、消退也快,且对于肝肾疾病患者或接受心脏手术的患者仍然适用的镇定安神药;为此,本发明实施例提供了以下技术方案:The first problem solved by the present invention is to provide a sedative and tranquilizer that has a quick onset and disappears quickly, and is still applicable to patients with liver and kidney diseases or patients undergoing heart surgery; for this reason, the embodiments of the present invention provide the following technologies plan:
一种基于地氟烷的镇静安神药,包括药物和药物载体,所述药物为地氟烷。A sedative and tranquilizer based on desflurane, comprising a drug and a drug carrier, the drug is desflurane.
所述镇静安神药的药物采用地氟烷,主要是因为与其他吸入性麻醉药相比,地氟烷起效速度最快、药性作用完毕后消退也最快,因此不会产生时间滞后性而影响患者正常的生活和工作。而且地氟烷的生物转化率最低,仅为0.017%,对肝、肾毒性极低或没有,适用于肝肾疾病患者。且地氟烷麻醉时,患者的血流动力稳定,无心率失常发生,适用于接受心脏手术的患者。Desflurane is used as the sedative and tranquilizer, mainly because compared with other inhalation anesthetics, desflurane has the fastest onset speed and the fastest disappearance after the drug properties are finished, so it will not produce time lag and Affect the normal life and work of patients. Moreover, the biotransformation rate of desflurane is the lowest, only 0.017%, and has very low or no toxicity to the liver and kidney, and is suitable for patients with liver and kidney diseases. And when desflurane is anesthetized, the patient's hemodynamics is stable and no arrhythmia occurs, which is suitable for patients undergoing cardiac surgery.
本发明解决的第二个问题是,在地氟烷为液体制剂时,如何实现地氟烷在不使用时的存储问题及在使用时的挥发问题,为此,本发明实施例提供了以下技术方案:The second problem to be solved by the present invention is how to realize the storage problem of desflurane when it is not in use and the problem of volatilization when it is used when desflurane is a liquid preparation. For this reason, the embodiment of the present invention provides the following technology plan:
所述药物载体包括吸水材料层和外壳,所述地氟烷为液体制剂;所述吸水材料层用于承载地氟烷;所述外壳用于包覆吸水材料;所述外壳上设置有开口,用于挥发地氟烷,开口上设置有封口装置。The drug carrier includes a water-absorbing material layer and a shell, the desflurane is a liquid preparation; the water-absorbing material layer is used to carry desflurane; the shell is used to cover the water-absorbing material; the shell is provided with an opening, It is used to volatilize desflurane, and the opening is provided with a sealing device.
优选地,所述外壳呈胶囊状,其长度为1-2CM。Preferably, the shell is in the shape of a capsule with a length of 1-2CM.
本发明解决的第三个问题是,如何避免地氟烷的过度挥发,避免浪费,为此本发明实施例提供了以下技术方案:The third problem solved by the present invention is how to avoid excessive volatilization of desflurane and avoid waste. For this reason, the embodiments of the present invention provide the following technical solutions:
所述开口的长度为0.5-1CM,宽度为0.5-1CM。The length of the opening is 0.5-1CM, and the width is 0.5-1CM.
优选地,所述制作吸水材料层的材料为棉、无纺布、纸浆,或以上材料的复合物所形成的高分子聚合物。Preferably, the material for making the water-absorbing material layer is cotton, non-woven fabric, pulp, or a polymer formed by a composite of the above materials.
优选的,所述封口装置为封口盖。但不局限于此,所述封口装置还可以有其他多种选择,例如撕拉型封条等。Preferably, the sealing device is a sealing cap. But not limited thereto, the sealing device can also have other options, such as tear-off seals and the like.
本发明解决的第四个问题是,如何实现镇静安神药的固定,为此本发明实施例提供了以下技术方案:The fourth problem solved by the present invention is how to realize the fixation of the sedative and tranquilizer, for which the embodiment of the present invention provides the following technical solutions:
所述外壳的外表面设置有条形的涂胶和与涂胶对应的离型纸。进一步地,所述涂胶区域的长度为1-2CM,宽度为0.5-1CM。The outer surface of the shell is provided with a strip of glue and a release paper corresponding to the glue. Further, the glue-coated area has a length of 1-2CM and a width of 0.5-1CM.
优选地,所述涂胶为生物胶或者有机硅凝胶。该药品为吸入型药品,患者需撕掉离型纸,将所述镇静安神药贴在面部对应鼻孔的位置,所述镇静安神药即可发挥治疗作用。Preferably, the glue is biological glue or silicone gel. The medicine is an inhalation medicine, and the patient needs to tear off the release paper, and stick the sedative and tranquilizer on the face corresponding to the nostril, and the sedative and tranquilizer can exert a therapeutic effect.
优选地,所述地氟烷的剂量为1-10ml。所述地氟烷的剂量为1-5ml。这里将该药品设置成两种型号,主要考虑到药物使用群体的身体状况,为保护使用者不会被过度镇静,对于身体强健的年轻人使用剂量为1-10ml的药品,而对于儿童或者身体较虚弱的老人使用剂量为1-5ml的药品。Preferably, the dose of desflurane is 1-10ml. The dosage of said desflurane is 1-5ml. Here, the drug is set into two types, mainly considering the physical condition of the drug user group. In order to protect the user from being over-sedated, a drug with a dose of 1-10ml is used for healthy young people, while for children or Weaker elderly people use the drug in doses of 1-5 ml.
由于采用了上述技术方案,本发明提供的基于地氟烷的镇静安神药具有以下有益效果:Due to the above-mentioned technical scheme, the desflurane-based sedative and tranquilizer provided by the present invention has the following beneficial effects:
1)所述镇静安神药的药物采用地氟烷,所述地氟烷镇静/催眠速度快,消退也快,不会因滞留药效而影响药品使用者正常的生活和工作。地氟烷的生物转化率仅为0.017%,对肝肾毒性极低或没有,适用于肝肾疾病患者。而且地氟烷对血流动力和心率的影响极小,适用于接受心脏手术的患者。1) Desflurane is used as the sedative and tranquilizer. The desflurane has a fast sedative/hypnotic speed and disappears quickly, and will not affect the normal life and work of the drug user due to the retention of the drug effect. The biotransformation rate of desflurane is only 0.017%, with very low or no toxicity to the liver and kidney, and is suitable for patients with liver and kidney diseases. Moreover, desflurane has minimal impact on blood flow and heart rate, and is suitable for patients undergoing cardiac surgery.
2)所述镇静安神药为通过呼吸方式接受药物的吸入型药,尤其能够解决患者不适宜服用口服药或者注射药剂的问题,能够避免患者因口服药或者注射药带来的痛苦。2) The sedative and tranquilizer medicine is an inhalation medicine that accepts medicine through breathing, especially can solve the problem that patients are not suitable for taking oral medicine or injection medicine, and can avoid the pain caused by oral medicine or injection medicine for patients.
附图说明Description of drawings
图1为基于地氟烷的镇静安神药的俯视图。Figure 1 is a top view of a desflurane-based sedative-tranquilizer.
图2为基于地氟烷的镇静安神药的正视图。Figure 2 is a front view of a desflurane-based sedative-tranquilizer.
图中标记:外壳1、开口2和涂胶3。Marks in the figure: shell 1, opening 2 and glue coating 3.
具体实施方式detailed description
下面结合试验例及具体实施方式对本发明作进一步的详细描述。The present invention will be further described in detail below in conjunction with test examples and specific embodiments.
地氟烷,化学名称:1,2,2,2-四氟乙基二氟甲基醚。Desflurane, chemical name: 1,2,2,2-tetrafluoroethyl difluoromethyl ether.
结构式:Structural formula:
分子式:C3H2F6OMolecular formula: C3H2F6O
分子量:168.04Molecular weight: 168.04
理化特性:卤代吸入性全身麻醉剂,无色透明;标准大气压下,沸点为22.8℃,22℃时饱和蒸气压为663.75mmHg;理化和生物性质稳定,室温下,临床使用浓度的地氟烷不燃烧、不爆炸;血/气分配系数为0.42,脂肪/血分配系数为27。Physical and chemical properties: Halogenated inhalational general anesthetic, colorless and transparent; under standard atmospheric pressure, the boiling point is 22.8°C, and the saturated vapor pressure at 22°C is 663.75mmHg; the physical, chemical and biological properties are stable. Combustion, no explosion; blood/gas partition coefficient is 0.42, fat/blood partition coefficient is 27.
药理特点:地氟烷的血/气分配系数为0.42,在现有的吸入麻醉药中最小,麻醉诱导和苏醒均很迅速。地氟烷具有显著的肌松作用,可以引起剂量相关性神经-肌肉传递减少。地氟烷在体内几乎无分解代谢,生物转化率仅为异氟烷的1/10(异氟烷的代谢率为0.17%),是已知体内生物转化率最低的吸入麻醉药,对肝、肾的毒性极低或没有。Pharmacological characteristics: The blood/air partition coefficient of desflurane is 0.42, which is the smallest among the existing inhalational anesthetics, and the induction and recovery of anesthesia are very rapid. Desflurane has a significant muscle relaxant effect, which can cause a dose-related decrease in neuromuscular transmission. Desflurane has almost no catabolism in the body, and its biotransformation rate is only 1/10 of that of isoflurane (the metabolic rate of isoflurane is 0.17%). It is an inhalation anesthetic with the lowest known biotransformation rate in the body. Renal toxicity is minimal or nonexistent.
鉴于地氟烷的特点,可以将其用于治疗失眠证,发挥其催眠镇静快速、生物转化率极低、不影响血流动力和心率的特点,为失眠人群,特别是为肝肾疾病患者或接受心脏手术患者改善睡眠发挥作用。In view of the characteristics of desflurane, it can be used for the treatment of insomnia syndrome, and its characteristics of rapid hypnotic sedation, extremely low biotransformation rate, and no influence on blood flow and heart rate are suitable for people with insomnia, especially for patients with liver and kidney diseases or Improved sleep plays a role in patients undergoing heart surgery.
作为一种应用的举例,将地氟烷与适合的载体配合,制作成一种基于地氟烷的镇静安神药物,用于治疗失眠证。As an application example, desflurane is combined with a suitable carrier to make a desflurane-based sedative and tranquilizer drug for treating insomnia.
请参阅图1和图2,图1和图2仅仅是一个示意性的结构展示,不代表镇静安生药的具体结构。如图1和图2所示的一种基于地氟烷的镇静安神药,包括药物和药物载体,所述药物为地氟烷。所述镇静安神药的药物采用地氟烷,主要是因为地氟烷起效比较快、作用完毕后消退也快,因此不会产生时间后滞性而影响患者正常的生活和工作,同时地氟烷的生物转化率仅为0.017%,对肝肾毒性极低或没有,适用于肝肾疾病患者。而且地氟烷对血流动力和心率的影响极小,适用于接受心脏手术的患者。Please refer to Figure 1 and Figure 2, Figure 1 and Figure 2 are only a schematic structure display, and do not represent the specific structure of the sedative drug. As shown in Figure 1 and Figure 2, a desflurane-based sedative and tranquilizer comprises a drug and a drug carrier, and the drug is desflurane. Desflurane is used as the sedative and tranquilizer drug, mainly because desflurane has a quicker onset of effect and disappears quickly after the effect is completed, so it will not produce time lag and affect the normal life and work of the patient. The biotransformation rate of alkane is only 0.017%, and the toxicity to liver and kidney is extremely low or not, and it is suitable for patients with liver and kidney diseases. Moreover, desflurane has minimal impact on blood flow and heart rate, and is suitable for patients undergoing cardiac surgery.
为了便于地氟烷的盛放以及挥发,所述药物载体包括吸水材料和外壳1,所述吸水材料用于承载地氟烷,所述外壳1用于包覆吸水材料,所述外壳1上设置有开口2,分布于吸水材料上的地氟烷可以从开口2处挥发。开口2上设置有封口装置,使用时将封口装置打开,使用完毕后再利用封口装置封闭开口2。In order to facilitate the storage and volatilization of desflurane, the drug carrier includes a water-absorbing material and a shell 1, the water-absorbing material is used to carry desflurane, and the shell 1 is used to cover the water-absorbing material, and the shell 1 is provided with There is an opening 2, and the desflurane distributed on the water-absorbing material can volatilize from the opening 2. The opening 2 is provided with a sealing device, the sealing device is opened during use, and the opening 2 is closed by the sealing device after use.
考虑到地氟烷的沸点低,仅为22.8℃。所以利用地氟烷制备的镇静安神药在未使用期间,建议冷藏保存。Considering that the boiling point of desflurane is low, only 22.8°C. Therefore, it is recommended to keep the sedative and tranquilizer prepared by desflurane in cold storage when not in use.
作为举例,所述封口装置选用封口盖。但不局限于此,所述封口装置还可以有其他多种选择,例如撕拉型封条等。As an example, the sealing device is a sealing cap. But not limited thereto, the sealing device can also have other options, such as tear-off seals and the like.
作为举例,制作吸水材料的材料优选为棉、无纺布、纸浆,或以上材料的复合物所形成的高分子聚合物,对异氟烷的承载效果好。但不局限于此,所述制作吸水材料的材料还可以有其他多种选择。As an example, the material for making the water-absorbing material is preferably cotton, non-woven fabric, pulp, or a polymer formed by a composite of the above materials, which has a good bearing effect on isoflurane. But not limited thereto, the material for making the water-absorbing material can also have other choices.
外壳1的结构可以有多种形状,作为应用举例,所述外壳1呈胶囊状,其长度为1-2CM。将所述镇静安神药放置在患者的鼻孔处可以增强对地氟烷的吸收,增强治疗效果,因此,在使用时首选将镇静安神药放置在患者的鼻孔处。通过将胶囊状结构设计为1-2CM,一方面可以有效地控制地氟烷的挥发量;另一方面也可以保证镇静安神药在放置在患者鼻孔处时,不会因外壳过大而影响患者正常呼吸。The structure of the shell 1 can have various shapes. As an application example, the shell 1 is in the shape of a capsule with a length of 1-2 cm. Placing the sedative and tranquilizer at the patient's nostrils can enhance the absorption of desflurane and enhance the therapeutic effect. Therefore, it is preferred to place the sedative and tranquilizer at the patient's nostrils during use. By designing the capsule structure to be 1-2 cm, on the one hand, the volatilization of desflurane can be effectively controlled; on the other hand, it can also ensure that the sedative and tranquilizer will not affect the patient due to the large shell when it is placed in the patient's nostril Breathe normally.
开口2的作用是使地氟烷挥发出来,以被人体吸收。通过设置开口2的尺寸可以控制单位时间内地氟烷的挥发量。作为较优的实施方式的举例,开口2的长度为0.5-1CM,宽度为0.5-1CM。经过研究试验,经过此种尺寸的开口2挥发的地氟烷,不仅对于患者治疗失眠效果好,而且不至于使地氟烷过多挥发进入人体以外的空气中,减少地氟烷的浪费。The function of the opening 2 is to volatilize the desflurane to be absorbed by the human body. The volatilization amount of desflurane per unit time can be controlled by setting the size of the opening 2 . As an example of a preferred embodiment, the length of the opening 2 is 0.5-1CM, and the width is 0.5-1CM. After research and experimentation, the desflurane volatilized through the opening 2 of this size not only has a good effect on treating insomnia for patients, but also prevents the desflurane from volatilizing too much into the air outside the human body, reducing the waste of desflurane.
由于镇静安神药放置在鼻孔处使用可以增强吸收效果,因此在使用时,为了便于镇静安神药固定在鼻孔处,作为较优的实施方式,外壳1的外表面设置有条形的涂胶3和与涂胶3对应的离型纸。本镇静安神药为吸入型药品,容易理解地,涂胶3和开口2分别位于外壳1的两个相邻的面,使用时,患者需要将所述镇静安神药外壳涂胶上的离型纸撕掉,将涂胶面贴在面部人中的位置,此时外壳1上开口2的位置正对于鼻孔,开口2上撕拉型封条撕掉后外壳内的地氟烷便开始挥发,同时挥发的地氟烷会随着患者的吸气动作进入到患者体内。Since the sedative and tranquilizer is placed in the nostrils and used to enhance the absorption effect, in order to facilitate the sedative and tranquilizer to be fixed at the nostrils during use, as a preferred embodiment, the outer surface of the shell 1 is provided with strips of glue 3 and Release paper corresponding to glue 3. The sedative and tranquilizer is an inhalation drug. It is easy to understand that the glue 3 and the opening 2 are respectively located on two adjacent surfaces of the shell 1. During use, the patient needs to glue the release paper on the shell of the sedative and tranquilizer. Tear it off, and stick the glued surface on the middle of the face. At this time, the position of the opening 2 on the shell 1 is facing the nostrils. After the tear-off seal on the opening 2 is torn off, the desflurane in the shell will start to volatilize and volatilize at the same time. The desflurane will enter the patient's body with the patient's inhalation action.
涂胶的面积可以根据外壳的尺寸来确定,例如涂胶3长度为1-2CM,宽度为0.5-1CM。涂胶3可以为生物胶或者有机硅凝胶,既能保障粘贴性,又不至于对人体造成伤害。The glued area can be determined according to the size of the shell, for example, the glued 3 has a length of 1-2CM and a width of 0.5-1CM. The glue 3 can be biological glue or silicone gel, which can not only ensure the adhesiveness, but also avoid causing harm to the human body.
所述镇静安神药作为单剂量药品使用,即使用一次后就要丢弃,因此为了充分利用药物,避免地氟烷的浪费,需要控制地氟烷的计量,使得地氟烷刚好被患者吸收用于镇静安神。自然地,针对于不同的患者地氟烷的使用剂量不同,例如身体虚弱的老年人的使用量少于身体强壮的年轻人。经过研究,本实施例中列举了两种规格的地氟烷剂量,其中一种是地氟烷的剂量为1-10ml,另一种是地氟烷的剂量为1-5ml,为保护使用者不会被过度镇静,以及避免药物浪费,对于身体强健的年轻人适用于剂量为1-10ml的药品,而对于身体较虚弱的老人则适用于剂量为1-5ml的药品。为了便于区分两个规格的镇静安神药,在生产过程中,可以将外壳设置为大、小两种规格,也可以通过对外壳着以不同颜色进行区分。The sedative and tranquilizer is used as a single-dose medicine, and it will be discarded after one use. Therefore, in order to make full use of the medicine and avoid the waste of desflurane, it is necessary to control the dosage of desflurane so that the desflurane is just absorbed by the patient. Calm down. Naturally, the dosage of desflurane is different for different patients, for example, the dosage of frail elderly people is less than that of healthy young people. After research, this example lists two dosages of desflurane, one of which is 1-10ml of desflurane, and the other is 1-5ml of desflurane, in order to protect users To prevent excessive sedation and to avoid drug waste, it is suitable for healthy young people with a dose of 1-10ml, and for the weaker elderly, it is suitable for a dose of 1-5ml. In order to facilitate the distinction between the two specifications of sedative and tranquilizers, during the production process, the shell can be set in two sizes, large and small, or it can be distinguished by wearing different colors on the shell.
以上所述,仅为本发明的较佳实施例,但本发明的保护范围不局限于此,任何熟悉本技术方案的技术人员在本发明揭露的技术范围内,对以上实例进行简单修改、同等变换,均涵盖在本发明的保护范围内。The above description is only a preferred embodiment of the present invention, but the scope of protection of the present invention is not limited thereto. Any skilled person who is familiar with the technical solution can simply modify the above examples within the technical scope disclosed in the present invention, and make equivalent Transformations are all covered within the protection scope of the present invention.
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