Drug development & registration最新文献

{"title":"Phase I Pharmacokinetics Study of Oral Administration of Esperavir® (INN: Molnupiravir) (LLC \"PROMOMED RUS\", Russia)","authors":"T. N. Komarov, N. Bagaeva, K. K. Karnakova, K. Zaslavskaya, P. A. Bely, I. Shohin","doi":"10.33380/2305-2066-2024-13-1-1644","DOIUrl":"https://doi.org/10.33380/2305-2066-2024-13-1-1644","url":null,"abstract":"Introduction. The pandemic of the new coronavirus infection COVID-19 (Coronavirus Disease 2019) was caused by a single-stranded RNA virus SARS-CoV-2 (Severe acute respiratory syndrome-related coronavirus 2). Molnupiravir is an antiviral drug with activity against RNA viruses including SARS-CoV-2. Molnupiravir exerts the antiviral effect by introducing copy errors during viral RNA replication – by that the replication of SARS-CoV-2 inhibits. For oral administration of molnupiravir the drug Esperavir® has been registered in Russia.Aim. The aim is pharmacokinetics study of Esperavir®, capsules 200 mg (the manufacturer is JSC \"Biokhimic\", LLC \"PROMOMED RUS\", Russia, as registration certificate holder) by a single dose (800 mg) and multiple doses oral administration (800 mg twice a day with a gap of 12 hours between doses) in healthy volunteers in a phase I pharmacokinetics study, comparison the obtained data of pharmacokinetic parameters with the literature data.Materials and methods. The clinical and analytical phases of the pharmacokinetic study as well as pharmacokinetic analyses have been performed as a part of a clinical trial of the drug Esperavir®, capsules 200 mg (the manufacturer is JSC \"Biokhimic\", LLC \"PROMOMED RUS\", Russia, as registration certificate holder). Chromatographic separation and detection by Nexera XR high-performance liquid chromatograph with triple quadrupole tandem mass spectrometry LCMS-8040 (Shimadzu Corporation, Japan). The pharmacokinetic parameters were calculated with the Boomer pharmacokinetic analysis add-in for Microsoft Excel (Department of Pharmacokinetics and Drug Metabolism, Allergan, Irvine, CA 92606, USA). Descriptive pharmacokinetic statistics were calculated with Microsoft Excel (Microsoft Corporation, USA).Results and discussion. Pharmacokinetic parameters for cohort 1 (800 mg single dose of Esperavir®) and for cohort 2 (800 mg of Esperavir® twice a day with a gap of 12 hours between doses) were calculated. Averaged pharmacokinetic profiles of mean NHC concentrations over time in linear and log-linear scales were plotted. The geometric mean of Cmax and T1/2, the median, minimum and maximum of Tmax showed the comparability of the obtained data after a single dose administration of 800 mg of Esperavir® and the available literature data.Conclusion. According to the concentrations from the analytical phase of the pharmacokinetic study the pharmacokinetic parameters were calculated, averaged pharmacokinetic profiles in linear and log-linear scales were plotted after a single dose and multiple doses of the drug Esperavir®, capsules (the manufacturer is JSC \"Biokhimic\", LLC \"PROMOMED RUS\", Russia, as registration certificate holder). The comparability of the obtained data and the available literature data was shown. The results justified the study of the subsequent phases of clinical trials of Esperavir®.","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"167 ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140451523","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}

{"title":"The Effect of Individual Compounds from Rubus chamaemoruson Hemostasis in vitro","authors":"V. Luzhanin, A. Samorodov, A. K. Whaley, A. Whaley, G. P. Yakovlev, I. A. Samylina","doi":"10.33380/2305-2066-2024-13-1-1566","DOIUrl":"https://doi.org/10.33380/2305-2066-2024-13-1-1566","url":null,"abstract":"Introduction. One of the key tasks of the pharmaceutical industry is the search for new promising compounds – potential drug candidates. Natural objects, especially plants, have long been rich sources of new molecules and are widely used in the global food and pharmaceutical industries. Cloudberry (Rubus chamaemorus L.) is a perennial herb from the Rosaceae family. The fruits and leaves of R. chamaemorus contain a wide variety of polyphenolic secondary metabolites – hydrolysable/condensed tannins and flavonoids. Extracts enriched by polyphenols showed significant antiproliferative activity and inhibition of cell growth, and also induce cell apoptosis. As a result of our previous phytochemical research of R. chamaemorus leaves, five polyphenolic secondary metabolites belonging to the classes of tannins and flavonoids were isolated and characterized.Aim. Screening of previously isolated from R. chamaemorus individual compounds for the hemostasis system in vitro and identification of the most promising compounds for subsequent pharmaceutical development.Materials and methods. Experiments under in vitro conditions were performed on the blood of healthy male donors. The research of the effect on platelet aggregation was carried out according to the Born method on an AT-02 aggregometer (LLC \"SPF \"Medtech\", Russia). Determination of anticoagulant activity was carried out by conventional clotting tests on a Solar CGL 2110 turbidimetric hemocoagulometer (CJSC \"SOLAR\", Russia). Cytofluorimetric analysis was performed on a NovoCyte instrument (Agilent Technologies, USA).Result and discussion. The influence of the isolated compounds 1–5 on the parameters of activation, platelet aggregation and the coagulation component of hemostasis was studied. At a concentration of 1.0 mg/ml, compounds 1–5 did not affect the fibrinogen concentration and prothrombin time. Compounds 1, 3 and 5 completely suppressed platelet activation at the studied concentrations. Compounds 1 and 3 showed antiaggregation activity comparible to the values of acetylsalicylic acid and are contained in all aqueous and alcoholic extracts of R. сhamaemorus leaves; their quantitative content varies depending on the extraction conditions.Conclusion. Thus, as a result of the screening of individual compounds 1–5 isolated from the leaves of R. chamaemorus their antiaggregating and anticoagulation properties were established. Compounds 1 (4-O-α-L-arabinofuranosylellagic acid) and 3 (quercetin-3-O-β-D-glucuronide) showed antiaggregation activity comparible to that of acetylsalicylic acid, and are the most promising of the studied series of compounds for the subsequent pharmaceutical development of new antiplatelet agents.","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"58 31","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139844445","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}

{"title":"Comparative Evaluation of the Diuretic Activity of Infusions of Four Species of the Genus Astragalus (Astragalus L.) in the Experiment","authors":"U. A. Matvienko, A. Karetnikova, N. Durnova","doi":"10.33380/2305-2066-2024-13-1-1461","DOIUrl":"https://doi.org/10.33380/2305-2066-2024-13-1-1461","url":null,"abstract":"Introduction. Astragalus L. is the largest genus of the Fabaceae family and one of the largest genera of vascular plants on Earth. The official type of raw material included in the 7th edition of the European Pharmacopoeia is Radix Astragali – the dried root of Astragalus membranaceus (Fisch.) Bunge and Astragalus mongholicus Bunge. Extracts obtained from astragalus root have anti-inflammatory, immunostimulatory, antioxidant, diuretic effects. In traditional medicine, the herb of Astragalus dasyanthus Pall. is actively used. An infusion of the herb of Astragali dasyanthi has sedative, hypotensive and diuretic effects. However, the raw material is not official and is not included in the list of plant raw materials of the State Pharmacopoeia of the Russian Federation of the XIV edition. Promising species of the genus Astragalus L. can be not Astragalus membranaceus (Fisch.) Bunge and Astragalus dasyanthus Pall., but also other species, for example, Astragalus varius S.G. Gmel., Astragalus testiculatus Pall., Astragalus henningii (Stev.) Klok., which are widespread in the Saratov region. In view of the available data on the presence of the herb of Astragalus dasyanthus Pall. and Astragalus membranaceus (Fisch.) Bunge of the diuretic effect, it is of interest to study the diuresis of extracts from the herb of other species of the genus Astragalus L.Aim. To study the diuretic activity of infusions from the herb of four types of astragalus: Astragalus dasyanthus, Astragalus varius, Astragalus testiculatus, Astragalus henningii in 4- and 24-hour experiments on male rats.Materials and methods. The study of the diuretic activity of aqueous extracts from the herb of four types of Astragalus was performed on 42 white male rats, which were divided into 6 experimental and control groups of 6 animals. Aqueous extracts from Astragalus herb were prepared in the ratio of raw material-extractant 1:10, all obtained infusions met the requirements for these dosage forms according to the General Pharmacopoeia of the State Fund of the Russian Federation of the XIV edition. Aqueous extracts were administered to animals intragastrically through an umbrella at a dose of 100 mg/kg. During the experiment were collected 4-hour and 24-hour portions of urine. The comparison drug in the 4-hour experiment was furosemide at a dose of 1 mg/kg, and in the 24-hour experiment, hydrochlorothiazide at a dose of 20 mg/kg. Results and discussion. As a result of the experiment, the diuretic effect of the infusion of the herb of Astragalus dasyanthus both in the 4-hour experiment and in the 24-hour experiment. Also in both experiments, the most pronounced diuretic effect was found in the infusion of the herb of Astragalus henningii at a dose of 100 mg/kg compared with herb infusions Astragalus dasyanthus, Astragalus varius. Diuretic effect Astragalus henningii exceeded the diuretic activity of furosemide at a dose of 1 mg/kg, while a comparable effect was observed with hydrochlorothiazide ","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"17 17","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139782364","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}

{"title":"Comparative Evaluation of the Diuretic Activity of Infusions of Four Species of the Genus Astragalus (Astragalus L.) in the Experiment","authors":"U. A. Matvienko, A. Karetnikova, N. Durnova","doi":"10.33380/2305-2066-2024-13-1-1461","DOIUrl":"https://doi.org/10.33380/2305-2066-2024-13-1-1461","url":null,"abstract":"Introduction. Astragalus L. is the largest genus of the Fabaceae family and one of the largest genera of vascular plants on Earth. The official type of raw material included in the 7th edition of the European Pharmacopoeia is Radix Astragali – the dried root of Astragalus membranaceus (Fisch.) Bunge and Astragalus mongholicus Bunge. Extracts obtained from astragalus root have anti-inflammatory, immunostimulatory, antioxidant, diuretic effects. In traditional medicine, the herb of Astragalus dasyanthus Pall. is actively used. An infusion of the herb of Astragali dasyanthi has sedative, hypotensive and diuretic effects. However, the raw material is not official and is not included in the list of plant raw materials of the State Pharmacopoeia of the Russian Federation of the XIV edition. Promising species of the genus Astragalus L. can be not Astragalus membranaceus (Fisch.) Bunge and Astragalus dasyanthus Pall., but also other species, for example, Astragalus varius S.G. Gmel., Astragalus testiculatus Pall., Astragalus henningii (Stev.) Klok., which are widespread in the Saratov region. In view of the available data on the presence of the herb of Astragalus dasyanthus Pall. and Astragalus membranaceus (Fisch.) Bunge of the diuretic effect, it is of interest to study the diuresis of extracts from the herb of other species of the genus Astragalus L.Aim. To study the diuretic activity of infusions from the herb of four types of astragalus: Astragalus dasyanthus, Astragalus varius, Astragalus testiculatus, Astragalus henningii in 4- and 24-hour experiments on male rats.Materials and methods. The study of the diuretic activity of aqueous extracts from the herb of four types of Astragalus was performed on 42 white male rats, which were divided into 6 experimental and control groups of 6 animals. Aqueous extracts from Astragalus herb were prepared in the ratio of raw material-extractant 1:10, all obtained infusions met the requirements for these dosage forms according to the General Pharmacopoeia of the State Fund of the Russian Federation of the XIV edition. Aqueous extracts were administered to animals intragastrically through an umbrella at a dose of 100 mg/kg. During the experiment were collected 4-hour and 24-hour portions of urine. The comparison drug in the 4-hour experiment was furosemide at a dose of 1 mg/kg, and in the 24-hour experiment, hydrochlorothiazide at a dose of 20 mg/kg. Results and discussion. As a result of the experiment, the diuretic effect of the infusion of the herb of Astragalus dasyanthus both in the 4-hour experiment and in the 24-hour experiment. Also in both experiments, the most pronounced diuretic effect was found in the infusion of the herb of Astragalus henningii at a dose of 100 mg/kg compared with herb infusions Astragalus dasyanthus, Astragalus varius. Diuretic effect Astragalus henningii exceeded the diuretic activity of furosemide at a dose of 1 mg/kg, while a comparable effect was observed with hydrochlorothiazide ","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"136 ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139842122","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}

{"title":"The Effect of Individual Compounds from Rubus chamaemoruson Hemostasis in vitro","authors":"V. Luzhanin, A. Samorodov, A. K. Whaley, A. Whaley, G. P. Yakovlev, I. A. Samylina","doi":"10.33380/2305-2066-2024-13-1-1566","DOIUrl":"https://doi.org/10.33380/2305-2066-2024-13-1-1566","url":null,"abstract":"Introduction. One of the key tasks of the pharmaceutical industry is the search for new promising compounds – potential drug candidates. Natural objects, especially plants, have long been rich sources of new molecules and are widely used in the global food and pharmaceutical industries. Cloudberry (Rubus chamaemorus L.) is a perennial herb from the Rosaceae family. The fruits and leaves of R. chamaemorus contain a wide variety of polyphenolic secondary metabolites – hydrolysable/condensed tannins and flavonoids. Extracts enriched by polyphenols showed significant antiproliferative activity and inhibition of cell growth, and also induce cell apoptosis. As a result of our previous phytochemical research of R. chamaemorus leaves, five polyphenolic secondary metabolites belonging to the classes of tannins and flavonoids were isolated and characterized.Aim. Screening of previously isolated from R. chamaemorus individual compounds for the hemostasis system in vitro and identification of the most promising compounds for subsequent pharmaceutical development.Materials and methods. Experiments under in vitro conditions were performed on the blood of healthy male donors. The research of the effect on platelet aggregation was carried out according to the Born method on an AT-02 aggregometer (LLC \"SPF \"Medtech\", Russia). Determination of anticoagulant activity was carried out by conventional clotting tests on a Solar CGL 2110 turbidimetric hemocoagulometer (CJSC \"SOLAR\", Russia). Cytofluorimetric analysis was performed on a NovoCyte instrument (Agilent Technologies, USA).Result and discussion. The influence of the isolated compounds 1–5 on the parameters of activation, platelet aggregation and the coagulation component of hemostasis was studied. At a concentration of 1.0 mg/ml, compounds 1–5 did not affect the fibrinogen concentration and prothrombin time. Compounds 1, 3 and 5 completely suppressed platelet activation at the studied concentrations. Compounds 1 and 3 showed antiaggregation activity comparible to the values of acetylsalicylic acid and are contained in all aqueous and alcoholic extracts of R. сhamaemorus leaves; their quantitative content varies depending on the extraction conditions.Conclusion. Thus, as a result of the screening of individual compounds 1–5 isolated from the leaves of R. chamaemorus their antiaggregating and anticoagulation properties were established. Compounds 1 (4-O-α-L-arabinofuranosylellagic acid) and 3 (quercetin-3-O-β-D-glucuronide) showed antiaggregation activity comparible to that of acetylsalicylic acid, and are the most promising of the studied series of compounds for the subsequent pharmaceutical development of new antiplatelet agents.","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"76 26","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139784687","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}

{"title":"Relevance of the Development of Dental In situ Implant for Post-resection Therapy (Review)","authors":"M. V. Pomytkina, E. Bakhrushina, P. Sakharova, P. D. Konogorova, N. Demina","doi":"10.33380/2305-2066-2024-13-1-1462","DOIUrl":"https://doi.org/10.33380/2305-2066-2024-13-1-1462","url":null,"abstract":"Introduction. The problem of pain relief after surgery is relevant in modern dentistry, as pain control is an important part of treatment. In addition to anesthesia, there are other problems of post-resection therapy such as bleeding from the wound and inflammation. Modern dental practice does not have a targeted delivery system or a medical product with analgesic, anti-inflammatory, anesthetic or hemostatic action, which ensures high adherence of patients to the ongoing post-resection therapy.Text. To solve this problem, it can be proposed to develop an in situ implant – a dosage form that is formed directly at the injection site, in the alveolar socket. Targeted delivery system has advantages: no need to use a medical dressing material; no risk of secondary contamination; dosing accuracy and target delivery to the lesion locus; high mucoadhesion to the site of application; the duration of the active ingredient release and others. The purpose of the review is to substantiate the possibility and relevance of developing a new in situ implant system for use in dental post-resection practice. The study was conducted on the main databases of publications (Scopus, Web of Science, PubMed and others), and patent search database on materials published from 2000 to the present. The study describes the currently existing in situ systems for dental problems, which could be a prototype of systems for delivering an anesthetic directly to the tooth socket, the polymers used to create them and the possibility of releasing drugs, and also characterizes existing drugs for the pain relief (applied both locally and for systemic action), in comparison with in situ systems, which have certain advantages and great potential for development.Conclusion. Based on the results of the work, a conclusion about the possibility of pharmaceutical development of dental in situ implants was made, and the most promising polymers for phase transition in the alveolar socket were identified.","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"16 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139870760","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}

{"title":"HPLC-UV Analysis of Flavonoid Glycosides in the Herb of Astragalus (A. dasyanthus, A. varius, A. testiculatus, A. henningii), Growing in the Volga Region","authors":"U. A. Matvienko, N. A. Durnova, A. Poluyanov, N. V. Bobkova, G. Ramenskaya","doi":"10.33380/2305-2066-2024-13-1-1623","DOIUrl":"https://doi.org/10.33380/2305-2066-2024-13-1-1623","url":null,"abstract":"Introduction. The search for new promising sources of biologically active substances is one of the tasks of modern pharmacognosy. Among the huge variety of species of the genus Astragalus L., only a few of them have been studied. In addition, none of them is included in the current edition of the State Pharmacopoeia of the Russian Federation. In our opinion, the study of four species of this genus of Astragalus L. (A. dasyanthus, A. varius, A. testiculatus, A. henningii) growing in the Volga region is of interest.Aim. Study of the glycoside composition of flavonoids in the astragalus herb of four species (A. dasyanthus, A. varius, A. testiculatus, A. henningii) by HPLC-UV using external standards.Materials and methods. The material was samples of astragalus grass (A. dasyanthus, A. varius, A. testiculatus, A. henningii), collected on the territory of the Saratov region in accordance with the basic rules of collection and preparation and dried to an air-dry state. Aqueous-alcoholic extracts (1 : 50) were analyzed. Qualitative and quantitative analysis of flavonoid glycosides was carried out on an Agilent 1260 chromatograph (Agilent Technologies, USA) equipped with a diode array detector, manual sample injection (Agilent G1328C manual injector, Agilent Technologies USA) and an Agilent Open Lab CDS system for collecting and processing chromatographic data. The elution gradient was selected individually using 0.1 % phosphoric acid/acetonitrile solution as solvents. Compounds were identified by retention times and UV spectra of reference standards (RS). The quantitative content of each detected component was expressed in mg/g of dry raw material. All studies were repeated five times, the results were statistically processed using MS Exсel 2010.Results and discussion. The chromatographic profiles of aqueous-alcoholic extracts from the herbs of four types of astragalus were studied. Differences were found in both the qualitative composition and quantitative content of flavonoid glycosides in the grass of the analyzed species. The largest number of compounds was found in the herb of A. varius (6 compounds), 4 compounds were identified in the herb of A. dasyanthus and A. henningii, and 3 compounds were identified in the herb of A. testiculatus. The dominant components in the herb of A. henningii are orientin and rutin, in the herb of A. testiculatus and A. varius it is cynaroside, and in A. dasyanthus it is rutin.Conclusion. A HPLC-UV method was developed for determining the quantitative content of flavonoid glycosides in extracts from the herbs of four species of astragalus (A. dasyanthus, A. varius, A. testiculatus, A. henningii) and the chromatographic profiles of the analyzed samples were studied.","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"6 24","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139811153","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}

{"title":"HPLC-UV Analysis of Flavonoid Glycosides in the Herb of Astragalus (A. dasyanthus, A. varius, A. testiculatus, A. henningii), Growing in the Volga Region","authors":"U. A. Matvienko, N. A. Durnova, A. Poluyanov, N. V. Bobkova, G. Ramenskaya","doi":"10.33380/2305-2066-2024-13-1-1623","DOIUrl":"https://doi.org/10.33380/2305-2066-2024-13-1-1623","url":null,"abstract":"Introduction. The search for new promising sources of biologically active substances is one of the tasks of modern pharmacognosy. Among the huge variety of species of the genus Astragalus L., only a few of them have been studied. In addition, none of them is included in the current edition of the State Pharmacopoeia of the Russian Federation. In our opinion, the study of four species of this genus of Astragalus L. (A. dasyanthus, A. varius, A. testiculatus, A. henningii) growing in the Volga region is of interest.Aim. Study of the glycoside composition of flavonoids in the astragalus herb of four species (A. dasyanthus, A. varius, A. testiculatus, A. henningii) by HPLC-UV using external standards.Materials and methods. The material was samples of astragalus grass (A. dasyanthus, A. varius, A. testiculatus, A. henningii), collected on the territory of the Saratov region in accordance with the basic rules of collection and preparation and dried to an air-dry state. Aqueous-alcoholic extracts (1 : 50) were analyzed. Qualitative and quantitative analysis of flavonoid glycosides was carried out on an Agilent 1260 chromatograph (Agilent Technologies, USA) equipped with a diode array detector, manual sample injection (Agilent G1328C manual injector, Agilent Technologies USA) and an Agilent Open Lab CDS system for collecting and processing chromatographic data. The elution gradient was selected individually using 0.1 % phosphoric acid/acetonitrile solution as solvents. Compounds were identified by retention times and UV spectra of reference standards (RS). The quantitative content of each detected component was expressed in mg/g of dry raw material. All studies were repeated five times, the results were statistically processed using MS Exсel 2010.Results and discussion. The chromatographic profiles of aqueous-alcoholic extracts from the herbs of four types of astragalus were studied. Differences were found in both the qualitative composition and quantitative content of flavonoid glycosides in the grass of the analyzed species. The largest number of compounds was found in the herb of A. varius (6 compounds), 4 compounds were identified in the herb of A. dasyanthus and A. henningii, and 3 compounds were identified in the herb of A. testiculatus. The dominant components in the herb of A. henningii are orientin and rutin, in the herb of A. testiculatus and A. varius it is cynaroside, and in A. dasyanthus it is rutin.Conclusion. A HPLC-UV method was developed for determining the quantitative content of flavonoid glycosides in extracts from the herbs of four species of astragalus (A. dasyanthus, A. varius, A. testiculatus, A. henningii) and the chromatographic profiles of the analyzed samples were studied.","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"2 3","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139870979","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}

{"title":"Relevance of the Development of Dental In situ Implant for Post-resection Therapy (Review)","authors":"M. V. Pomytkina, E. Bakhrushina, P. Sakharova, P. D. Konogorova, N. Demina","doi":"10.33380/2305-2066-2024-13-1-1462","DOIUrl":"https://doi.org/10.33380/2305-2066-2024-13-1-1462","url":null,"abstract":"Introduction. The problem of pain relief after surgery is relevant in modern dentistry, as pain control is an important part of treatment. In addition to anesthesia, there are other problems of post-resection therapy such as bleeding from the wound and inflammation. Modern dental practice does not have a targeted delivery system or a medical product with analgesic, anti-inflammatory, anesthetic or hemostatic action, which ensures high adherence of patients to the ongoing post-resection therapy.Text. To solve this problem, it can be proposed to develop an in situ implant – a dosage form that is formed directly at the injection site, in the alveolar socket. Targeted delivery system has advantages: no need to use a medical dressing material; no risk of secondary contamination; dosing accuracy and target delivery to the lesion locus; high mucoadhesion to the site of application; the duration of the active ingredient release and others. The purpose of the review is to substantiate the possibility and relevance of developing a new in situ implant system for use in dental post-resection practice. The study was conducted on the main databases of publications (Scopus, Web of Science, PubMed and others), and patent search database on materials published from 2000 to the present. The study describes the currently existing in situ systems for dental problems, which could be a prototype of systems for delivering an anesthetic directly to the tooth socket, the polymers used to create them and the possibility of releasing drugs, and also characterizes existing drugs for the pain relief (applied both locally and for systemic action), in comparison with in situ systems, which have certain advantages and great potential for development.Conclusion. Based on the results of the work, a conclusion about the possibility of pharmaceutical development of dental in situ implants was made, and the most promising polymers for phase transition in the alveolar socket were identified.","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"35 3","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139811131","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}

{"title":"Comparative Study of Free Amino Acid Profiles in Underground Organs of Several Species of the Genus Rumex During Different Phases of the Vegetation Cycle","authors":"A. Poluyanov, U. A. Matvienko, A. Y. Sokolova, A. E. Savelyeva, N. A. Durnova, N. V. Bobkova","doi":"10.33380/2305-2066-2024-13-1-1719","DOIUrl":"https://doi.org/10.33380/2305-2066-2024-13-1-1719","url":null,"abstract":"Introduction. Amino acids (AA), the primary metabolites in plants, play a crucial role in various physiological processes, including the synthesis of phenolic compounds. Drug products and dietary supplements made from medicinal plants can become a rich source of both nonessential and essential amino acids. High levels of free amino acids found in herbal raw material often indicate the presence of biotic and abiotic stress in the plants. Therefore, understanding the dynamics of bioactive compound accumulation in plants throughout their phenological phases of development is critical to optimizing their potential health benefits.Aim. To compare qualitative composition and dynamics of AA accumulation in the underground organs of four representatives of the Rumex genus: R. confertus, R. crispus L., R. obtusifolius L., R. aquaticus L. of three different vegetative phases.Materials and methods. Water extracts from underground organs of the studied plants were analyzed using two different methods for qualitative and quantitative analysis. Extracts were applied to the chromatographic plates TLS Silica gel 60 F254 (Merk, Germany) 20 × 20 cm with a micro-syringe (LLC \"Tsvet\", Russia). After elution, the plates were treated with a 2 % ninhydrin solution. Quantitative analysis was carried out using the SF-2000 spectrophotometer (LLC \"OKB Spectr\", Russia).Results and discussion. The amino acid profile of the underground organs of R. confertus, R. crispus L., R. obtusifolius L., R. aquaticus L. during three vegetative phases was determined using the TLC method; the quantitative analysis performed using spectrophotometry.Conclusion. The most diverse amino acid (AA) profiles were found in the withering phase in all Rumex species, with up to 9 amino adsorption zones. In contrast, the least diverse AA profiles were observed in the flowering phase, ranging from 2 to 4 adsorption zones. The quantitative content of AA was lowest in the flowering phase, increased during the regrowth phase, and peaked in the withering phase. However, R. crispus L. showed an unusual pattern, with the highest quantitative content of AA detected in the regrowth phase.","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"39 8","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140488171","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}