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Substantiation of the composition and technology for obtaining combined sustained-release tablets for the treatment of hypertension 一种治疗高血压的联合缓释片的合成物及制备工艺的证实
Pub Date : 2023-02-17 DOI: 10.24959/nphj.23.101
T. O. Ponomarenko, D. I. Dmytrievsky, I. O. Kryklyva, V. Hrytsenko
Aim. To develop the composition and technology for obtaining the combined drug of indapamide with enalapril of the prolonged action.Materials and methods. Indapamide and enalapril maleate substances as active components, and polyvinylpyrrolidone, calcium stearate, lactose monohydrate, hydroxypropyl methylcellulose as excipients were used. The pharmaco-technological studies were conducted according to the methods of the State Pharmacopoeia of Ukraine (SPhU).Results and discussion. The pharmaco-technological properties of tablet mixtures and the quality of finished tablets were compared using direct pressing and preliminary wet granulation.Conclusions. It has been found that the use of the method of pre-granulation of the tablet mixture allows obtaining a finished product that fully meets the requirements of the SPhU.
的目标。目的研制吲哚帕胺与依那普利联用的长效药物的组成及制备工艺。材料和方法。以吲达帕胺和马来酸依那普利物质为活性成分,以聚乙烯吡咯烷酮、硬脂酸钙、一水乳糖、羟丙基甲基纤维素为赋形剂。按照乌克兰国家药典(SPhU)的方法进行药理学研究。结果和讨论。比较了直接压片法和湿法初步造粒法制备的混合片剂的药效学性能和成品片剂的质量。研究发现,使用片剂混合物的预造粒方法可以获得完全符合SPhU要求的成品。
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引用次数: 0
Determination of the physical and mechanical indicators of the polymer base and the optimal method of introducing active pharmaceutical ingredients into the base composition 高分子碱的物理力学指标的测定及在碱组合物中引入活性药物成分的最佳方法
Pub Date : 2023-02-17 DOI: 10.24959/nphj.23.111
A. Solomennyi, A. O. Drozdova, L. Davtyan
Treatment of wounds and wound infection remains an urgent medical problem today, especially in conditions of constant hostilities. Hydrogel bandages are quite effective means for local treatment of wounds, which are able to have a complex therapeutic effect and do not require frequent replacement in the process of medical supply to military personnel. Taking into account the relevance of this topic, our research is aimed at developing a hydrogel bandage with lidocaine hydrochloride, ceftriaxone and metronidazole.Aim. To study the physical and mechanical parameters of the polymer base and determine the optimal method for introducing active pharmaceutical ingredients (APIs) into the base composition.Materials and methods. The study materials were APIs (lidocaine hydrochloride, ceftriaxone, metronidazole) and excipients. Physical and mechanical research methods were used in the work.Results and discussion. In order to develop the optimal technology for obtaining the polymer mass and determining technological indicators, we studied the indicators of physical and mechanical properties. Indicators of breaking force and relative elongation depend on such technological characteristics as homogeneity, uniformity of application on the substrate, the absence of air bubbles. It was found that the higher the physical and mechanical parameters, the higher the quality of the polymer mass applied to the substrate. Therefore, after obtaining a homogeneous mass it is necessary to deaerate air bubbles by centrifugation (No. 1-5) at 3000 rpm for 5-10 min. During the study of the ease of application of the polymer mass on the polyethylene terephthalate substrate, it was found that the drying process was affected by the thickness of the layer. It was proven that samples No. 1-5 had a uniform, adhesive layer and could be used for further research. The main technological indicators were the layer thickness of 0.40 mm, the centrifugation time of 5-10 min at 3000 rpm, homogeneity (mixing for 15 min at 36 rpm, an anchor stirrer). It was experimentally found that to obtain a layer thickness of 0.40 mm, it was necessary to apply 0.03 g of the sample per 1 cm2 of the substrate. We proved that polymers in the concentration of 10 % provided the optimal technological indicators. To confirm this, the dependence of the viscosity of the forming solution on the concentration / ratio of polymers was studied. We found that the technological indicators of homogeneity and uniformity directly affected the quality of the resulting product. Taking into account the fact that it was possible to introduce poorly soluble substances into the composition of model samples we conducted an experiment on their sedimentation in a polymer solution. It was found that APIs introduced into the polymer solution had different values of the sedimentation rate (time), which was probably related to the degree of solubility. In addition, the polymer concentration in the forming solutions also affected the s
伤口和伤口感染的治疗今天仍然是一个紧迫的医疗问题,特别是在持续敌对行动的情况下。水凝胶绷带是一种非常有效的局部伤口治疗手段,治疗效果复杂,在向军事人员提供医疗用品的过程中不需要频繁更换。考虑到本课题的相关性,我们的研究旨在开发一种含有盐酸利多卡因、头孢曲松和甲硝唑的水凝胶绷带。研究高分子碱的物理力学参数,确定在碱组合物中引入活性药物成分的最佳方法。材料和方法。研究材料为原料药(盐酸利多卡因、头孢曲松、甲硝唑)和辅料。这项工作采用了物理和机械的研究方法。结果和讨论。为了制定最佳的聚合物质量获取工艺和工艺指标的确定,对其物理力学性能指标进行了研究。断裂力和相对伸长率的指标取决于诸如均匀性、基材上的均匀性、无气泡等技术特性。结果表明,物理力学参数越高,所得到的聚合物质量越高。因此,在获得均匀质量后,需要在3000 rpm下离心(No. 1-5)使气泡脱氧5-10 min。在研究聚合物质量在聚对苯二甲酸乙二醇酯底物上的应用便利性时,发现干燥过程受层厚的影响。结果表明,1-5号样品具有均匀的粘接层,可用于进一步研究。主要工艺指标为层厚0.40 mm, 3000rpm离心时间5- 10min,均匀性(36rpm搅拌15min,锚定搅拌器)。实验发现,要获得0.40 mm的层厚,每1 cm2的衬底必须施加0.03 g的样品。实验证明,聚合物浓度为10%时的工艺指标最优。为了证实这一点,研究了成型溶液粘度与聚合物浓度比的关系。我们发现,均匀性和均匀性的技术指标直接影响到最终产品的质量。考虑到有可能将难溶性物质引入模型样品的组成,我们对它们在聚合物溶液中的沉积进行了实验。研究发现,引入聚合物溶液的原料药具有不同的沉降速率(时间)值,这可能与溶解度有关。此外,成型溶液中聚合物的浓度也会影响原料药的沉降速率。黏度越高,原料药颗粒沉降越慢。在研究过程中发现,满意的物理力学参数指标可以保证聚合物量产工艺的质量,是选择聚合物包衣以获得具有麻醉、抗菌、抗菌作用的水凝胶的基础。确定的主要技术指标为层厚(0.40 mm)、离心时间(3000转/分钟,5-10分钟)、均匀性(36转/分钟,搅拌15分钟)。所得结果将用于开发盐酸利多卡因、头孢曲松和甲硝唑的药物组合物及其制造工艺。
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引用次数: 0
Peculiarities of the filtration process of liposomal emulsion for the production of eye drops based on a peptide complex 以肽复合物为基础的滴眼液用脂质体乳剂过滤过程的特点
Pub Date : 2023-02-17 DOI: 10.24959/nphj.23.102
Ye. M. Kruglov, G. I. Borshchevskiy
Liposomes are increasingly being studied and implemented as drug delivery systems in the form of eye drops. An important stage in the production of a liposomal preparation in the form of eye drops is the stage of sterilization filtration before filling the medicinal product into a container for final dosage. It is assumed that liposome components interact with the membrane and clog it due to their unique physicochemical properties. Therefore, a deeper understanding of the sterilization filtration of liposomes is needed to make appropriate decisions regarding the choice of filters for sterilization.Resistance and permeability values calculated from the Darcy equation are well suited for comparing different filter membranes or process parameters.Aim. To substantiate the choice of optimal brands of filter membranes and parameters of the liposomal emulsion filtration process for the production of eye drops based on a peptide complex.Materials and methods. The study object was a liposomal emulsion for the production of eye drops based on a peptide complex. A prepared liposomal emulsion of eye drops based on a peptide complex and membrane filters of various brands were used for filtration. Filtration tests were performed on a Zero-T scaling unit manufactured by Sartorius, Germany. For all measurements, the filtrate weight was controlled using a balance. Filtration experiments were evaluated using Zero-T 2.0 software from Sartorius Stedim Biotech, Germany. At the first stage, the recorded data of the results was saved to a file. Based on the data obtained using the Excel table processor, the filtration flow J°, the initial resistance of the membrane R°zag and the throughput Ṽ were calculated according to the calculated measurement time: the beginning of T10 % and the end of T80 %.Results and discussion. According to the results obtained, the optimal brands of sterilizing membranes were determined; it was shown that by increasing the pressure drop, the volumetric throughput was significantly improved by more than 18 times (from 0.7 to 4.1 bar), and in another experiment – by more than 10 times (from 0.3 to 2.1 bar). In addition, the benefit of using a higher pressure drop to filter liposomes through various sterilizing membranes was shown.Conclusions. The obtained values of the initial resistance of the membrane showed that the geometrical aspects and properties of the material of the Supor® (Pall) and Sartopore 2® (Sartorius) membrane brands have a lower ability to block the membrane during filtration and provide the filtration resource due to greater throughput. It has been also shown that the use of a higher pressure drop increases the productivity of the process.
脂质体以滴眼液的形式被越来越多地研究和实施作为药物输送系统。在生产滴眼液形式的脂质体制剂的一个重要阶段是在将药品填充到最终剂量的容器之前的灭菌过滤阶段。据推测,脂质体成分与膜相互作用,并堵塞它由于其独特的物理化学性质。因此,需要更深入地了解脂质体的灭菌过滤,以便在选择灭菌过滤器时做出适当的决定。由达西方程计算出的电阻和渗透率值非常适合于比较不同的过滤膜或工艺参数。为了确定最佳滤膜品牌的选择和基于肽复合物的滴眼液的脂质体乳化过滤工艺参数。材料和方法。研究对象是一种以肽复合物为基础的用于生产滴眼液的脂质体乳液。以多肽复合物为基础制备滴眼液脂质体乳液,并用不同品牌的膜过滤器进行过滤。过滤试验在德国Sartorius公司生产的Zero-T标度装置上进行。对于所有测量,滤液重量使用天平控制。过滤实验采用德国Sartorius Stedim Biotech公司的Zero-T 2.0软件进行评价。在第一阶段,将记录的结果数据保存到文件中。根据Excel表格处理器获得的数据,根据计算出的测量时间:t10%开始和t80%结束,计算出过滤流量J°、膜的初始阻力R°zag和吞吐量Ṽ。结果和讨论。根据所得结果,确定了灭菌膜的最佳品牌;结果表明,通过增加压降,体积吞吐量显着提高了18倍以上(从0.7到4.1 bar),在另一项实验中-提高了10倍以上(从0.3到2.1 bar)。此外,还显示了用较高的压降过滤脂质体通过各种灭菌膜的好处。所获得的膜的初始阻力值表明,Supor®(Pall)和Sartopore 2®(Sartorius)膜品牌的材料的几何方面和性能在过滤过程中阻塞膜的能力较低,并且由于更高的吞吐量而提供过滤资源。还表明,使用较高的压降可以提高工艺的生产率。
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引用次数: 0
Experience of work as an extemporal pharmacy and providing the population with medicines under the conditions of the martial law 作为临时药房的工作经验,在戒严令的情况下为民众提供药品
Pub Date : 2022-11-07 DOI: 10.24959/nphj.22.97
N. I. Shtuchna, L. Vyshnevska
Aim. To highlight the expediency of reviving extemporaneous formulations as a necessary condition for fully providing the population of Ukraine with individualized medicinal products that can be also used in conditions of the martial law and emergency situations.Materials and methods. Publications and our own research of the activities of pharmacy No. 80 in Slovyansk, Donetsk region, with extemporaneous compounding of medicines were used. The following methods were used in the work: system analysis, synthesis, own observations and generalization of data.Results and discussion. From a professional point of view, medicinal products extemporaneously manufactured are a unique attribute of pharmacy practice, which reflects the professional status of pharmacists, particularly hospital pharmacists. Despite a significant reduction in the range and quantity of pharmacy-made medicines in pharmacies, they continue to retain important functions (medical, therapeutic, social). During the period from February 24, 2022 to March 9, 2022, sale volumes of the most popular medicines increased significantly. Suspensions for external use were in the greatest demand, in particular, the universal white lotion doubled in dispensing (from 4 to 8 bottles per day), as well as sedative drugs (Quarter’s mixture) – more than five times (from 2 to 13 bottles day). The number of powders (with different dosages of captopril, verospiron, furosemide, anaprilin, euthyrox, etc.) for children in one order could befrom 30-50 doses to 90-120 doses, and one child sometimes had 2-3 names of prescribed medicines, i.e. the number of doses of the daily compounding of powders reached 200-300 pieces for one consumer.Conclusions. Today, an important task of domestic pharmacy is not only to preserve extemporaneous formulations, but also to improve them and develop new magistral formulas using professional recommendations and professional advice.
的目标。强调恢复临时配方的便宜性,作为向乌克兰人民充分提供个性化医疗产品的必要条件,这些产品也可在戒严和紧急情况下使用。材料和方法。出版物和我们自己对顿涅茨克地区斯洛夫扬斯克第80号药房的活动进行的研究使用了临时合成药物。在工作中采用了系统分析、综合、自己观察和数据推广的方法。结果和讨论。从专业角度看,临时生产的药品是药学实践的一种独特属性,它反映了药师特别是医院药师的专业地位。尽管药店生产的药品的范围和数量大大减少,但它们继续保持重要的功能(医疗、治疗和社会)。在2022年2月24日至3月9日期间,最受欢迎的药品销量显著增加。外用悬浮液的需求量最大,特别是通用白色洗液的配药量翻了一番(从每天4瓶增加到8瓶),镇静药物(Quarter的混合物)的配药量增加了五倍以上(从每天2瓶增加到13瓶)。儿童单单配用粉剂(卡托普利、维罗螺隆、呋塞米、阿那普利林、促甲状腺素等不同剂量)的数量可达30-50剂至90-120剂,一个儿童有时有2-3个处方名称,即一个消费者每日配用粉剂的剂量可达200-300片。如今,国内药房的一项重要任务不仅是保留即席配方,而且要利用专业建议和专业意见对其进行改进和开发新的地方配方。
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引用次数: 1
Biopharmaceutical and microbiological research of fennel fruit infusions 茴香浸剂的生物制药及微生物学研究
Pub Date : 2022-11-07 DOI: 10.24959/nphj.22.96
O. M. Fylypyuk, L. Vyshnevska
Aim. To develop and study physico-chemical, pharmaco-technological, pharmacognostic and microbiological quality indicators of infusions obtained by extraction of the plant raw material of fennel fruits of different degrees of grinding and from different types of packaging.Materials and methods. The study objects were model samples of fennel fruits of different degrees of grinding and water extracts obtained on their basis and from different types of packaging. Water extracts were prepared according to the SPhU method and the patient information leaflet on fennel fruits. The study of pH of solutions, extractives, identification of the main biologically active substances (BAS), and microbiological purity of water extracts were performed by the SPhU methods; the quantitative determination of the essential oil was conducted by direct alkalimetric titration with 0.01 mol/l NaOH solution in the presence of methylene blue and phenolphthalein indicators according to the Guidelines of the Ministry of Health of Ukraine.Results and discussion. Extractives in model samples of infusions obtained from filter bags vary from 0.43 to 0.48 % without filter bags (samples 1, 3, 5, 7) – from 0.52 to 0.55 %, and its amount is the lowest in sample 9 – 0.37 %. However, the essential oil content is the highest in sample 9, these are whole fennel fruits from the pack (0.15 %); slightly higher indicators are in model samples without filter bags (samples 2, 4, 6, 8). The pH value is slightly higher in infusions obtained from filter bags than without them (in the range of 6.61-6.70 and 6.22-6.25, respectively). However, the infusion obtained from a nylon pyramid bag (sample 7) had a pH value close to infusions obtained from the fennel medicinal raw material without packaging (6.25). The presence of infusions of anethole and terpenoids in model samples has been proven by thin layer chromatography. The microbiological studies conducted have shown that the use of the method of making water extracts from the patient information leaflet allows obtaining conditionally sterile infusions. Conclusions. The indicators studied (transparency, color, odor, taste, extractives, identification and quantitative determination of BAS) can be used in the analysis of water extracts from the medicinal plant raw material produced in filter bags.
的目标。开发和研究不同粉碎程度、不同包装的茴香植物原料提取浸剂的理化、药理学、生药学和微生物学质量指标。材料和方法。研究对象是在茴香不同研磨程度的基础上,采用不同包装方式获得的茴香模型样品和水提取物。根据SPhU法和茴香患者资料制备茴香水提取物。采用SPhU法对溶液pH、提取液、主要生物活性物质(BAS)鉴定和水提取液微生物纯度进行研究;根据乌克兰卫生部的指南,在亚甲基蓝和酚酞指示剂存在的情况下,用0.01 mol/l NaOH溶液直接碱滴定法对精油进行定量测定。结果和讨论。在没有过滤袋的情况下(样品1、3、5、7),从0.43%到0.48%(样品1、3、5、7)的模型样品中,萃取物的含量从0.52%到0.55%不等,在样品9中,萃取物的含量最低,为0.37%。然而,样品9中精油含量最高,这些是整包茴香果(0.15%);未使用滤袋的模型样品(样品2、4、6、8)各项指标略高。使用滤袋的样品pH值略高于未使用滤袋的样品(分别为6.61 ~ 6.70和6.22 ~ 6.25)。然而,从尼龙金字塔袋(样品7)中获得的输注液的pH值接近于从未包装的茴香药用原料中获得的输注液(6.25)。薄层色谱法证实了模型样品中存在茴香醚和萜类化合物。所进行的微生物学研究表明,使用从患者信息小册子中提取水的方法可以获得有条件的无菌输液。结论。所研究的指标(透明度、颜色、气味、味道、萃取物、BAS的鉴别和定量测定)可用于药用植物原料滤袋水提物的分析。
{"title":"Biopharmaceutical and microbiological research of fennel fruit infusions","authors":"O. M. Fylypyuk, L. Vyshnevska","doi":"10.24959/nphj.22.96","DOIUrl":"https://doi.org/10.24959/nphj.22.96","url":null,"abstract":"Aim. To develop and study physico-chemical, pharmaco-technological, pharmacognostic and microbiological quality indicators of infusions obtained by extraction of the plant raw material of fennel fruits of different degrees of grinding and from different types of packaging.\u0000Materials and methods. The study objects were model samples of fennel fruits of different degrees of grinding and water extracts obtained on their basis and from different types of packaging. Water extracts were prepared according to the SPhU method and the patient information leaflet on fennel fruits. The study of pH of solutions, extractives, identification of the main biologically active substances (BAS), and microbiological purity of water extracts were performed by the SPhU methods; the quantitative determination of the essential oil was conducted by direct alkalimetric titration with 0.01 mol/l NaOH solution in the presence of methylene blue and phenolphthalein indicators according to the Guidelines of the Ministry of Health of Ukraine.\u0000Results and discussion. Extractives in model samples of infusions obtained from filter bags vary from 0.43 to 0.48 % without filter bags (samples 1, 3, 5, 7) – from 0.52 to 0.55 %, and its amount is the lowest in sample 9 – 0.37 %. However, the essential oil content is the highest in sample 9, these are whole fennel fruits from the pack (0.15 %); slightly higher indicators are in model samples without filter bags (samples 2, 4, 6, 8). The pH value is slightly higher in infusions obtained from filter bags than without them (in the range of 6.61-6.70 and 6.22-6.25, respectively). However, the infusion obtained from a nylon pyramid bag (sample 7) had a pH value close to infusions obtained from the fennel medicinal raw material without packaging (6.25). The presence of infusions of anethole and terpenoids in model samples has been proven by thin layer chromatography. The microbiological studies conducted have shown that the use of the method of making water extracts from the patient information leaflet allows obtaining conditionally sterile infusions.\u0000 Conclusions. The indicators studied (transparency, color, odor, taste, extractives, identification and quantitative determination of BAS) can be used in the analysis of water extracts from the medicinal plant raw material produced in filter bags.","PeriodicalId":19221,"journal":{"name":"News of Pharmacy","volume":"36 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85145140","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The substantiation of the composition of a medical pencil for the prevention and treatment of diseases of the skin and the red border of the lips 一种用于预防和治疗皮肤疾病和唇红边的医用铅笔的组合物的确证
Pub Date : 2022-11-07 DOI: 10.24959/nphj.22.95
T. Nesteruk, N. Polovko
Aim. To substantiate the composition of the product for the prevention and treatment of diseases of the skin and the red border of the lips in the form of a medical pencil.Materials and methods. When developing the composition of a medical pencil the study objects were samples containing corn oil or the oil extract from a mixture of the medicinal plant raw material, cocoa butter, such waxes as beeswax, carnauba, candelilla, and lanolin, paraffin in various ratios, as well as the mango extract. The medical pencilcomposition was substantiated based on the results of determining the organoleptic, sensory (consumer) and physicochemical properties (melting point, hardness, spreadability and adhesion (stickiness) of the smear).Results and discussion. The results of the study shown that the hardness and melting point of pencils increased with an increase in the content of sealants, primarily beeswax and carnauba wax, and paraffin. An increase in the content of these components reduced the spreadability and adhesion of the base. Cocoa butter and lanonin in thecomposition of the base improved the adhesion and spreadability of the pencil, but did not provide the necessary hardness of the product. Based on the results of the study of physico-chemical and consumer properties, the bases, which included the mango extract and the oil extract from a mixture of the medicinal plant raw material (sage leaves,eucalyptus leaves, marigold flowers, chamomile flowers), were chosen. It was shown that the introduction of extracts slightly increased the melting point and hardness of the base and reduced the spreadability of the pencil.Сonclusions. Based on the results of studying the melting point, hardness, spreadability and adhesion the composition of the wax-fat base has been chosen. The effect of the oil extract of a mixture of the medicinal plant raw material and the mango extract on the properties of the pencil base has been determined. According to the results of our research, the composition of a medical pencil for the prevention and treatment of infectious and inflammatory diseases of the skin and the red border of the lips has been proposed. It contains cocoa butter – 10 %, beeswax – 10 %, lanolin – 5 %, carnauba wax – 3 %, candelilla wax – 7 %, the mango extract – 5 % and the oil extract of a mixture of the medicinal plant raw material – up to 100.0.
的目标。以医疗铅笔的形式证实该产品的成分,用于预防和治疗皮肤疾病和嘴唇的红边。材料和方法。在研制医用铅笔的成分时,研究对象是含有玉米油或药用植物原料、可可脂、蜂蜡、巴西棕榈、小烛花、羊毛脂、石蜡等各种比例的蜡的混合物的油提取物以及芒果提取物的样品。根据测定药膏的感官、感官(消费者)和理化性质(熔点、硬度、涂抹性和粘附性)的结果,确定了医用铅笔的成分。结果和讨论。研究结果表明,铅笔的硬度和熔点随着密封剂(主要是蜂蜡、巴西棕榈蜡和石蜡)含量的增加而增加。这些成分含量的增加会降低基材的涂抹性和附着力。可可脂和羊毛蛋白的基础成分提高了铅笔的附着力和涂抹性,但没有提供必要的产品硬度。根据理化性质和消费特性的研究结果,选择了包括芒果提取物和药用植物原料(鼠尾草叶、桉树叶、万寿菊花、洋甘菊花)混合物的油提取物的基础。结果表明,提取物的加入使基体的熔点和硬度略有提高,但降低了pencil.Сonclusions的涂抹性。通过对蜡脂基的熔点、硬度、涂覆性和附着力的研究,确定了蜡脂基的组成。测定了药用植物原料和芒果提取物的混合物的油提取物对铅笔底座性能的影响。根据我们的研究结果,提出了一种用于预防和治疗皮肤和嘴唇红边感染性和炎症性疾病的医用铅笔的成分。它含有10%的可可脂、10%的蜂蜡、5%的羊毛脂、3%的巴西棕榈蜡、7%的小烛花蜡、5%的芒果提取物和高达100.0%的药用植物原料混合物的油提取物。
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引用次数: 0
The anticonvulsant effect of digoxin on basic models of primary generalized seizures does not depend on the route of administration 地高辛对原发性全身性癫痫基本模型的抗惊厥作用不依赖于给药途径
Pub Date : 2022-11-07 DOI: 10.24959/nphj.22.98
V. Tsyvunin, S. Shtrygol’, M. V. Mishchenko, D. Shtrygol’
Improving the prevention and treatment of epilepsy is one of the urgent tasks. Based on the available data on the anticonvulsant activity of the cardiac glycoside digoxin, it is advisable to compare the anticonvulsant effect of the drug by different routes of administration in the experiment.Aim. To determine the impact of the route of administration on the anticonvulsant effect of the cardiac glycoside digoxin on basic models of primary generalized seizures induced by pentylenetetrazol and maximal electric shock.Materials and methods. Two basic models were used: the model of primary generalized convulsions induced in mice by pentylenetetrazol (80 mg/kg subcutaneously) and maximal electric shock (current strength – 50 mA, frequency – 50 Hz, 0.2 sec corneally). Digoxin was administered in the dose of 0.8 mg/kg (about 1/10 LD50) 30 min before modeling seizures in the stomach and subcutaneously. Standard parameters of convulsive syndrome severity and mortality were recorded.Results and discussion. In both seizure models, the anticonvulsant effect of digoxin was little dependent on the route of administration. In the pentylenetetrazole-induced model, with both routes of administration, lethality tended to decrease; when administered intragastrically, digoxin statistically significantly reduced the number of clonic-tonic seizures per 1 mouse, the number of animals with the most severe tonic seizures, and the duration of the convulsive period; when administered subcutaneously, it significantly increased the latent period of seizures and reduced the number of animals with tonic seizures. In the model of maximal electric shock, digoxin reduced seizure severity andlethality almost equally by both routes of administration (by 55 % with the intragastric administration and by 67.5 % with the subcutaneous administration). In both models, there were no statistically significant differences in the course of seizures in both routes of the digoxin administration. With subcutaneous administration, the anticonvulsant effect was somewhat more pronounced at the level of a weak tendency.Conclusions. The anticonvulsant effect of digoxin when administered intragastrically and subcutaneously in mice with models of pentylenetetrazole-induced seizures and maximal electric shock is practically independent of the routeof administration. Digoxin has a pronounced anticonvulsant effect on the model of electrically induced seizures, and a moderate effect on the model of pentylenetetrazole seizures.
加强对癫痫的预防和治疗是当务之急。根据心脏糖苷地高辛抗惊厥活性的现有资料,在实验中比较不同给药途径对心脏糖苷地高辛的抗惊厥作用是可取的。目的探讨心糖苷地高辛给药方式对戊四唑和最大电击致原发性全发性癫痫基本模型抗惊厥作用的影响。材料和方法。采用两种基本模型:戊四唑(80 mg/kg皮下注射)致小鼠原发性全身惊厥模型和最大电击(电流强度- 50 mA,频率- 50 Hz,角膜0.2秒)模型。地高辛以0.8 mg/kg(约1/10 LD50)的剂量在模拟癫痫发作前30分钟胃内和皮下给药。记录惊厥综合征严重程度和死亡率的标准参数。结果和讨论。在两种癫痫模型中,地高辛的抗惊厥作用对给药途径的依赖性很小。在戊四唑致大鼠模型中,两种给药方式均有降低死亡率的趋势;地高辛灌胃后,每1只小鼠的阵挛性强直性癫痫发作次数、发生最严重强直性癫痫发作的动物数量和惊厥持续时间均显著减少;皮下给药时,显著增加癫痫发作潜伏期,减少强直性癫痫发作的动物数量。在最大电击模型中,地高辛在两种给药方式下降低癫痫发作的严重程度和死亡率几乎相同(胃内给药55%,皮下给药67.5%)。在两种模型中,地高辛两种给药方式在癫痫发作过程中没有统计学上的显著差异。皮下给药时,抗惊厥作用在弱倾向水平上更为明显。地高辛的抗惊厥作用在戊四唑诱导的癫痫发作和最大电击模型小鼠的胃内和皮下给药实际上与给药途径无关。地高辛对电致癫痫发作模型有明显的抗惊厥作用,对戊四唑癫痫发作模型有中等作用。
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引用次数: 0
The morphological and anatomical study of Wisteria sinensis leaves 紫藤叶的形态解剖研究
Pub Date : 2022-10-08 DOI: 10.24959/nphj.22.90
O. Demeshko, V. Kovalev, O. V. Krivoruchko, S. V. Kovalev, S. I. Stepanova
Chinese wisteria (Wisteria sinensis), Glycine chinensis, is a genus of treelike deciduous lianas from the legume family (Fabaceae). In natural conditions, Glycine chinensis is found in the subtropical forests of China, Korea and Japan. Nowadays, the plant is widely cultivated in European countries. Leaves of the plant exhibit the antioxidant,cytostatic effect, flowers inhibit the growth of tubercle bacilli. The seeds are used in Chinese medicine to treat cardiovascular diseases and as a diuretic.Aim. To study macro- and microscopic features of Chinese wisteria leaves for standardization of the medicinal plant raw material and development of the quality control method.Materials and methods. The study object was the leaves of Chinese wisteria harvested in the period of mass flowering in the Kyiv region and the Autonomous Republic of Crimea. The morphological features were studied visually. Preparations from the leaf surface were prepared according to conventional methods.Results and discussion. The main morphological and anatomical features of Chinese wisteria leaves have been determined. Macroscopic features include complex unpaired leaves that have a common petiole and its continuation – rachis, on which there are five pairs of opposite leaves and one apical one. The leaves are large, do not have a toothed edge, pubescent at first, but eventually become smooth; microscopic signs are the dorso-ventral type of theleaf blade structure. The epidermis is covered with a cuticle. The cells of the upper epidermis are parenchymal, slightly convoluted, with evenly thickened membranes. Above the vein, the cells are prosenchymal, elongated along the vein. The lower epidermis is represented by cells of various shapes, parenchymal or having a somewhat elongated shape, sinuous-walled, polygonal. Stomata are frequent and oval. The stomatal apparatus is of anisocyte type. There are numerous hairs along the central vein and on the petiole. The petiole of the leaf has a rounded shape. In the center there is a single conductive bundle surrounded by parenchymal cells. The epidermis consists of small erect cells. There are numerous simple unicellular hairs. The cross-section of the rachis has an oval-triangular shape, the tubercles are ribshaped. Stomata are present.Conclusions. As a result of the studies, the main macroscopic and microscopic features of Chinese wisteria leaves have been determined; they will be used to standardize the medicinal plant raw material and develop the quality control method.
中国紫藤(wisteria sinensis), Glycine chinensis,是豆科(蚕豆科)的一个树状落叶藤本植物属。在自然条件下,甘氨酸生长于中国、韩国和日本的亚热带森林。如今,这种植物在欧洲国家被广泛种植。叶子的植物表现出抗氧化,抑制细胞生长的效果,花抑制结节杆菌的生长。其种子在中医中用于治疗心血管疾病和作为利尿剂。研究紫藤叶的宏观和微观特征,为药用植物原料的标准化和质量控制方法的建立提供依据。材料和方法。研究对象是在基辅地区和克里米亚自治共和国大量开花期间收获的中国紫藤叶子。目视观察其形态特征。根据常规方法从叶表面制备制剂。结果和讨论。确定了紫藤叶的主要形态和解剖特征。宏观特征包括复杂的未成对叶片,具有共同的叶柄及其延续轴,其上有5对相对的叶片和1对顶部叶片。叶子大,没有齿状边缘,起初被短柔毛,但最终变得光滑;显微镜下表现为叶片结构的背-腹型。表皮被角质层覆盖。上表皮细胞实质,微卷曲,膜均匀增厚。在静脉上方,细胞呈前皮层,沿静脉拉长。下表皮由各种形状的细胞组成,有的是实质的,有的是细长的,壁呈弯曲状,呈多边形。气孔频繁,卵圆形。气孔器为异角细胞型。沿中央脉和叶柄上有许多毛。叶柄呈圆形。中央有一个被实质细胞包围的导电束。表皮由小的直立细胞组成。有许多简单的单细胞毛发。脊柱横截面呈卵三角形,结节呈肋状。有气孔。研究结果确定了紫藤叶的主要宏观和微观特征;将用于药用植物原料的标准化和质量控制方法的制定。
{"title":"The morphological and anatomical study of Wisteria sinensis leaves","authors":"O. Demeshko, V. Kovalev, O. V. Krivoruchko, S. V. Kovalev, S. I. Stepanova","doi":"10.24959/nphj.22.90","DOIUrl":"https://doi.org/10.24959/nphj.22.90","url":null,"abstract":"Chinese wisteria (Wisteria sinensis), Glycine chinensis, is a genus of treelike deciduous lianas from the legume family (Fabaceae). In natural conditions, Glycine chinensis is found in the subtropical forests of China, Korea and Japan. Nowadays, the plant is widely cultivated in European countries. Leaves of the plant exhibit the antioxidant,cytostatic effect, flowers inhibit the growth of tubercle bacilli. The seeds are used in Chinese medicine to treat cardiovascular diseases and as a diuretic.\u0000Aim. To study macro- and microscopic features of Chinese wisteria leaves for standardization of the medicinal plant raw material and development of the quality control method.\u0000Materials and methods. The study object was the leaves of Chinese wisteria harvested in the period of mass flowering in the Kyiv region and the Autonomous Republic of Crimea. The morphological features were studied visually. Preparations from the leaf surface were prepared according to conventional methods.\u0000Results and discussion. The main morphological and anatomical features of Chinese wisteria leaves have been determined. Macroscopic features include complex unpaired leaves that have a common petiole and its continuation – rachis, on which there are five pairs of opposite leaves and one apical one. The leaves are large, do not have a toothed edge, pubescent at first, but eventually become smooth; microscopic signs are the dorso-ventral type of theleaf blade structure. The epidermis is covered with a cuticle. The cells of the upper epidermis are parenchymal, slightly convoluted, with evenly thickened membranes. Above the vein, the cells are prosenchymal, elongated along the vein. The lower epidermis is represented by cells of various shapes, parenchymal or having a somewhat elongated shape, sinuous-walled, polygonal. Stomata are frequent and oval. The stomatal apparatus is of anisocyte type. There are numerous hairs along the central vein and on the petiole. The petiole of the leaf has a rounded shape. In the center there is a single conductive bundle surrounded by parenchymal cells. The epidermis consists of small erect cells. There are numerous simple unicellular hairs. The cross-section of the rachis has an oval-triangular shape, the tubercles are ribshaped. Stomata are present.\u0000Conclusions. As a result of the studies, the main macroscopic and microscopic features of Chinese wisteria leaves have been determined; they will be used to standardize the medicinal plant raw material and develop the quality control method.","PeriodicalId":19221,"journal":{"name":"News of Pharmacy","volume":"32 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75482826","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Development of the adhesive composition for the transdermal therapeutic system with the anti-inflammatory action 具有抗炎作用的透皮治疗系统用黏附组合物的研制
Pub Date : 2022-10-03 DOI: 10.24959/nphj.22.92
A. Olefir, L. Vyshnevska
Aim. To develop the content of the adhesive composition, being one of the stages in developing the transdermal therapeutic system with the anti-inflammatory action.Materials and methods. Using organoleptic research methods, the properties affecting the process of applying the adhesive to the base and subsequently to the quality of the finished product were studied. Color, consistency and homogeneity were determined visually, and the features of applying the mass to the base were recorded. To determine the optimal temperature and drying time, drying was performed in a thermostat at a temperature of 60 to 120 ºС for 5-15 min.Results and discussion. Compositions based on a mixture of hydrogels with a hydrophobic silicone adhesive had a very thick consistency, which made it difficult to apply them to the base and led to significant weight losses during application. Instead, compositions based on a mixture of the aesilonum-aerosil base with a hydrophobic silicone adhesive had too liquid consistency. Adjusting the amount of aesilonum-4 we obtained a composition with satisfactory consistent properties, which distributed over the base in a uniform thin layer. When studying the effect of enhancers on the properties of the adhesive composition it was found that the addition of oleic acid and dimethyl sulfoxide diluted themass and prevented uniform application to the base, the addition of isopropyl myristate slightly diluted the mass, while the addition of propylene glycol did not affect the properties of the composition at all. Therefore, propylene glycol could be used as an enhancer. When setting the extension mode, the optimal one was determined to be 120 ºС for 5 min.Conclusions. The content of the adhesive composition has been developed. The composition includes: polysiloxane – 5.0, H-polysiloxane – 5.0, aerosil – 0.35, aesilonum-4 – 1.0, propylene glycol – 1.0. It has satisfactory consistency and organoleptic properties. It has been found that the optimal drying mode of the hydrophobic adhesive composition is 120 ºС for 5 min.
的目标。开发具有抗炎作用的经皮治疗系统的黏附组合物的含量是开发该系统的一个阶段。材料和方法。采用感官研究方法,研究了影响胶粘剂在基材上的应用过程以及随后对成品质量的性能。视觉上确定颜色、一致性和均匀性,并记录将质量应用于基础的特征。为了确定最佳温度和干燥时间,在温度为60 ~ 120ºС的恒温器中干燥5-15分钟。结果和讨论。基于水凝胶与疏水性硅酮粘合剂混合物的组合物具有非常厚的稠度,这使得它们难以应用于基础,并且在应用过程中导致显着的重量损失。相反,基于aesilonum-aerosil基和疏水性硅酮粘合剂的混合物的组合物具有太大的液体稠度。通过调整aesilonum-4的用量,我们得到了一种具有满意一致性的组合物,它以均匀的薄层分布在基体上。在研究增强剂对粘合剂组合物性能的影响时,发现油酸和二甲基亚砜的加入稀释了质量,不能均匀地涂在基体上,肉豆酸异丙酯的加入稍微稀释了质量,而丙二醇的加入对组合物的性能没有影响。因此,丙二醇可以作为增强剂。在设定拉伸方式时,确定最佳拉伸方式为120ºС,拉伸时间为5 min。研究了胶粘剂组合物的含量。该组合物包括:聚硅氧烷- 5.0、h -聚硅氧烷- 5.0、气相油- 0.35、埃西隆-4 - 1.0、丙二醇- 1.0。它具有令人满意的一致性和感官特性。研究发现疏水胶粘剂组合物的最佳干燥方式为120ºС,干燥5 min。
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引用次数: 0
Determination of ionization constants for sequinidazole in aqueous solutions and mixtures of water with isopropanol, acetonitrile and ethanol 异丙醇、乙腈和乙醇水溶液和水混合物中甲咪唑电离常数的测定
Pub Date : 2022-02-21 DOI: 10.24959/nphj.22.85
Z. Shovkova, O. Tkachenko, I. Seniuk
Seknidazole is a drug from the 5-nitroimidazole group with a number of side-effects. This drug is virtually unexplored from the point of view of chemico-toxicological analysis (CTA). Therefore, the development of a set of methods for the detection and quantification of secnidazole in biological fluids for use in CTA is an urgent task.Aim. To study the acid-base equilibrium of secnidazole in aqueous solutions and mixtures of water with amphiphilic solvents and determine the corresponding ionization constants.Materials and methods. Spectrophotometric measurements were performed using a SPEKOL®1500 single-beam spectrophotometer. An EV-74 ionomer was used to control the pH of the solutions. Seknidazole solutions in the concentrationof 1000 μg/ml were used in the experiment.Results and discussion.  Absorption spectra of secnidazole in water and mixtures of water and amphiphilic solvents in the pH range studied showed four isobestic points characterizing two protolytic equilibria (equilibrium 1 – 240 and 295 nm, equilibrium 2 – 261 and 297 nm). The position of the isobestic points of equilibrium 2 fluctuated in the range ± 3 nm; it was due to the presence of tautomeric transformations for the molecular form of secnidazole.Conclusions. The acid-base equilibria of secnidazole in aqueous solutions and mixtures of water with amphiphilic solvents have been studied. It has been shown that in a strongly alkaline medium there is an anionic form of secnidazole R–, with further decrease in the pH value the molecular form HR appears, in a strongly acidic medium the final product – a protonated form H2R+ – is formed. The ionization constant 1 has been determined for aqueous solutions of secnidazole, mixtures of water with isopropanol, acetonitrile and ethanol. It is impossible to determine the equilibrium constant 2 by the method specified.
塞克硝唑是一种5-硝基咪唑类药物,有许多副作用。从化学毒理学分析(CTA)的角度来看,这种药物实际上是未开发的。因此,开发一套用于CTA的生物液中塞硝唑的检测和定量方法是一项紧迫的任务。研究塞克硝唑在水溶液及水与两亲性溶剂混合物中的酸碱平衡,并测定其电离常数。材料和方法。使用SPEKOL®1500单光束分光光度计进行分光光度测量。采用EV-74离子单体控制溶液的pH。实验采用浓度为1000 μg/ml的塞克硝唑溶液。结果和讨论。在所研究的pH范围内,塞克硝唑在水和水-两亲性溶剂混合物中的吸收光谱显示出4个等容点,表征了两个原水解平衡(平衡1 - 240和295 nm,平衡2 - 261和297 nm)。平衡2等肥胖点的位置在±3nm范围内波动;这是由于塞克硝唑的分子形式发生了互变异构转化。研究了塞克硝唑在水溶液和水与两亲性溶剂的混合物中的酸碱平衡。结果表明,在强碱性介质中,塞克硝唑R -存在阴离子形式,随着pH值的进一步降低,分子形式HR出现,在强酸性介质中,最终产物形成质子化形式H2R+。测定了塞尼唑水溶液、水与异丙醇、乙腈和乙醇的混合物的电离常数1。用规定的方法测定平衡常数是不可能的。
{"title":"Determination of ionization constants for sequinidazole in aqueous solutions and mixtures of water with isopropanol, acetonitrile and ethanol","authors":"Z. Shovkova, O. Tkachenko, I. Seniuk","doi":"10.24959/nphj.22.85","DOIUrl":"https://doi.org/10.24959/nphj.22.85","url":null,"abstract":"Seknidazole is a drug from the 5-nitroimidazole group with a number of side-effects. This drug is virtually unexplored from the point of view of chemico-toxicological analysis (CTA). Therefore, the development of a set of methods for the detection and quantification of secnidazole in biological fluids for use in CTA is an urgent task.\u0000Aim. To study the acid-base equilibrium of secnidazole in aqueous solutions and mixtures of water with amphiphilic solvents and determine the corresponding ionization constants.\u0000Materials and methods. Spectrophotometric measurements were performed using a SPEKOL®1500 single-beam spectrophotometer. An EV-74 ionomer was used to control the pH of the solutions. Seknidazole solutions in the concentrationof 1000 μg/ml were used in the experiment.\u0000Results and discussion.  Absorption spectra of secnidazole in water and mixtures of water and amphiphilic solvents in the pH range studied showed four isobestic points characterizing two protolytic equilibria (equilibrium 1 – 240 and 295 nm, equilibrium 2 – 261 and 297 nm). The position of the isobestic points of equilibrium 2 fluctuated in the range ± 3 nm; it was due to the presence of tautomeric transformations for the molecular form of secnidazole.\u0000Conclusions. The acid-base equilibria of secnidazole in aqueous solutions and mixtures of water with amphiphilic solvents have been studied. It has been shown that in a strongly alkaline medium there is an anionic form of secnidazole R–, with further decrease in the pH value the molecular form HR appears, in a strongly acidic medium the final product – a protonated form H2R+ – is formed. The ionization constant 1 has been determined for aqueous solutions of secnidazole, mixtures of water with isopropanol, acetonitrile and ethanol. It is impossible to determine the equilibrium constant 2 by the method specified.","PeriodicalId":19221,"journal":{"name":"News of Pharmacy","volume":"182 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-02-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85733763","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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