首页 > 最新文献

RGUHS Journal of Pharmaceutical Sciences最新文献

英文 中文
Development and Evaluation of Floating Bilayer Tablet Containing Combination of Oxethazine and Cefixime Trihydrate 氧乙嗪与三水合头孢克肟复合漂浮双层片的研制与评价
Pub Date : 2023-01-01 DOI: 10.26463/rjps.13_3_3
Raghavendra R, Bhagawati ST, Manjunath K, Irappanavar S
Aim The objective of present work was to formulate and evaluate bilayer tablets of Oxethazine and Cefixime trihydrate developed by direct compression method for effectively treating gastric ulcer and H. pylori infection.Methods The tablets were prepared having immediate release layer of Oxethazine and sustained release layer of Cefixime trihydrate. Sodium starch glycolate was used as super disintegrant for immediate release layer. The bilayer tablets were prepared by direct compression method using HPMC K100 and natural polymers like xanthan gum guar gum karaya gum which release the drug for 12 hours. Pre-compression parameters post-compression parameters and physical characteristics were evaluated for prepared formulations.Results The release of the Oxethazine from the immediate release layer was found to be 94.6plusmn0.02 in 30 minutes. The release of Cefixime trihydrate for the sustained release floating layer was found to be 99.88plusmn0.06 in 12 hours. The data obtained from in vitro release were fitted into the various kinetic models Zero Order Higuchi First Order and Kors MeyerndashPepparsquos Model.Conclusion The bilayer tablets developed offer both immediate release of Oxethazine and sustained release of Cefixime trihydrate. This suggests their potential as a viable option for treating gastric ulcers and H. pylori infections using an innovative dosage form.
目的研制直接加压法制备的奥西嗪-三水合头孢克肟双层片,并对其治疗胃溃疡和幽门螺杆菌感染的疗效进行评价。方法采用氧乙嗪速释层和三水合头孢克肟缓释片。乙醇酸淀粉钠作为快速释放层的强力崩解剂。以HPMC K100为原料,以黄原胶、瓜尔胶、卡拉亚胶等天然聚合物为原料,采用直接加压法制备双层片,缓释时间为12小时。对制备的配方进行了预压缩参数、后压缩参数和物理特性评价。结果立即释放层在30 min内的释放量为94.6±0.02。三水合头孢克肟缓释浮层在12 h内的释放量为99.88±0.06。体外释放数据拟合为零阶Higuchi一阶动力学模型和Kors MeyerndashPepparsquos模型。结论制备的双层片既有奥西嗪的速释,又有三水合头孢克肟的缓释。这表明他们的潜力,作为一个可行的选择,治疗胃溃疡和幽门螺杆菌感染使用一种创新的剂型。
{"title":"Development and Evaluation of Floating Bilayer Tablet Containing Combination of Oxethazine and Cefixime Trihydrate","authors":"Raghavendra R, Bhagawati ST, Manjunath K, Irappanavar S","doi":"10.26463/rjps.13_3_3","DOIUrl":"https://doi.org/10.26463/rjps.13_3_3","url":null,"abstract":"Aim The objective of present work was to formulate and evaluate bilayer tablets of Oxethazine and Cefixime trihydrate developed by direct compression method for effectively treating gastric ulcer and H. pylori infection.Methods The tablets were prepared having immediate release layer of Oxethazine and sustained release layer of Cefixime trihydrate. Sodium starch glycolate was used as super disintegrant for immediate release layer. The bilayer tablets were prepared by direct compression method using HPMC K100 and natural polymers like xanthan gum guar gum karaya gum which release the drug for 12 hours. Pre-compression parameters post-compression parameters and physical characteristics were evaluated for prepared formulations.Results The release of the Oxethazine from the immediate release layer was found to be 94.6plusmn0.02 in 30 minutes. The release of Cefixime trihydrate for the sustained release floating layer was found to be 99.88plusmn0.06 in 12 hours. The data obtained from in vitro release were fitted into the various kinetic models Zero Order Higuchi First Order and Kors MeyerndashPepparsquos Model.Conclusion The bilayer tablets developed offer both immediate release of Oxethazine and sustained release of Cefixime trihydrate. This suggests their potential as a viable option for treating gastric ulcers and H. pylori infections using an innovative dosage form.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"22 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135910422","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
Neuroprotective Metabolites from Endophytic Microbes: A Review 内生微生物的神经保护代谢物:综述
Pub Date : 2023-01-01 DOI: 10.26463/rjps.13_3_6
Vaishali Todkar, Prasanna Habbu, Venkatrao Kulkarni, Smita Madagundi
A progressive loss of functional and structural integrity of the central nervous system leads to neurodegenerative diseases. Neurotoxicity refers to direct or indirect effect of chemicals that disrupt the nervous system. Human beings are grieving from nervous related ailments due increase in the population and aging. Because of the limited capacity of neurons to regenerate there is still no trusted and consistent therapeutic approach available to treat neurodegenerative diseases. Natural compounds have been widely studied as potential neuroprotective agents because of their characteristics of multiple targets and low cytotoxicity. Endophytes could be any organism either bacteria fungi actinomycetes or mycoplasm which reside inside the tissues of plants showing mutualistic relationships without infecting any of the plant cells. Variety of novel secondary metabolites and known analogues of plant metabolites are produced by endophytic microbes. Structurally distinctive and therapeutically active natural products such as flavonoids phenolic acids polyketides terpenoids benzopyranones quinines steroids alkaloids etc. are obtained from endophytes for their potential use in medicine agriculture or industry. Considerable literature is also available on chemically diversified compounds isolated from endophytic fractions possessing neuroprotective activity. The present review emphasizes on promising neuroprotective metabolites isolated from endophytic microbes inhabited in medicinal plants.
中枢神经系统功能和结构完整性的逐渐丧失导致神经退行性疾病。神经毒性是指化学物质对神经系统的直接或间接影响。由于人口增长和老龄化,人类正为与神经有关的疾病而悲伤。由于神经元的再生能力有限,目前还没有可靠和一致的治疗方法来治疗神经退行性疾病。天然化合物由于具有多靶点和低细胞毒性的特点,作为潜在的神经保护剂被广泛研究。内生菌可以是存在于植物组织内的任何生物体,细菌、真菌、放线菌或支原体,它们表现出共生关系,而不感染任何植物细胞。多种新的次生代谢物和已知的植物代谢物类似物是由内生微生物产生的。从内生菌中获得结构独特且具有治疗活性的天然产物,如黄酮类、酚酸、多酮类、萜类、苯并吡喃酮类、奎宁类、类固醇、生物碱等,在医药、农业或工业中具有潜在的用途。相当多的文献也可从具有神经保护活性的内生植物馏分中分离出化学多样化的化合物。本文综述了从药用植物内生微生物中分离出的具有神经保护作用的代谢物。
{"title":"Neuroprotective Metabolites from Endophytic Microbes: A Review","authors":"Vaishali Todkar, Prasanna Habbu, Venkatrao Kulkarni, Smita Madagundi","doi":"10.26463/rjps.13_3_6","DOIUrl":"https://doi.org/10.26463/rjps.13_3_6","url":null,"abstract":"A progressive loss of functional and structural integrity of the central nervous system leads to neurodegenerative diseases. Neurotoxicity refers to direct or indirect effect of chemicals that disrupt the nervous system. Human beings are grieving from nervous related ailments due increase in the population and aging. Because of the limited capacity of neurons to regenerate there is still no trusted and consistent therapeutic approach available to treat neurodegenerative diseases. Natural compounds have been widely studied as potential neuroprotective agents because of their characteristics of multiple targets and low cytotoxicity. Endophytes could be any organism either bacteria fungi actinomycetes or mycoplasm which reside inside the tissues of plants showing mutualistic relationships without infecting any of the plant cells. Variety of novel secondary metabolites and known analogues of plant metabolites are produced by endophytic microbes. Structurally distinctive and therapeutically active natural products such as flavonoids phenolic acids polyketides terpenoids benzopyranones quinines steroids alkaloids etc. are obtained from endophytes for their potential use in medicine agriculture or industry. Considerable literature is also available on chemically diversified compounds isolated from endophytic fractions possessing neuroprotective activity. The present review emphasizes on promising neuroprotective metabolites isolated from endophytic microbes inhabited in medicinal plants.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"75 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135910417","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
A Case Study on Tubercular Cavernous Sinus Syndrome 结节海绵窦综合征1例研究
Pub Date : 2023-01-01 DOI: 10.26463/rjps.13_3_1
Megha S Arali, Syed Khaleel Ahmed, Nagarjuna Damarla
Tubercular cavernous sinus syndrome is a rare condition of extra-pulmonary tuberculosis EPTB in which cavernous sinus involvement is observed. Cavernous sinus is a venous structure that holds and protects pituitary gland on one side and temporal lobe on other side. CSS is mainly characterized by multiple cranial neuropathies which is effected by various etiologies. This is a case report of tubercular cavernous sinus syndrome admitted to hospital with chief complaints of fever headache drooping of eyelids altered sensorium with disorientation and fever that reduced over next 3 to 4 days but headache was still persisting due to the damage to the cranial nerves. Based on these symptoms they underwent clinical examination which revealed hypotension elevated CRP levels and MRI suggestive of acute dural venous sinus thrombosis involving superior sagittal sinus and bilateral bulky cavernous sinus with transverse T2 hypo intensity in right transverse sagittal superior sagittal and internal jugular vein IJV. Granulomatous etiology indicated tubercular cavernous sinus syndrome. For this treatment was initiated with anti-tubercular drug therapy with vitamin supplements and anticoagulants. EPTB remains a significant health problem in developing countries. Prevalence of EPTB is increasing over the last several years globally.
结核性海绵窦综合征是一种罕见的肺外结核性EPTB,其中海绵窦受累。海绵窦是一种静脉结构,它的一侧是脑垂体,另一侧是颞叶。CSS的主要特征是多种病因影响的多发性颅脑神经病变。本文报告一例结核性海绵窦综合征患者入院,主诉为发热、头痛、眼睑下垂、感觉改变、定向障碍和发热,在接下来的3至4天内发热减轻,但由于颅神经损伤,头痛仍持续存在。基于这些症状,他们接受了临床检查,发现低血压,CRP水平升高,MRI提示急性硬脑膜静脉窦血栓形成,累及上矢状窦和双侧笨重的海绵窦,右侧横矢状、上矢状和颈内静脉IJV的横向T2低强度。肉芽肿的病因提示结核性海绵窦综合征。这种治疗开始于抗结核药物治疗,包括维生素补充剂和抗凝血剂。EPTB仍然是发展中国家的一个重大健康问题。在过去几年中,EPTB的流行在全球呈上升趋势。
{"title":"A Case Study on Tubercular Cavernous Sinus Syndrome","authors":"Megha S Arali, Syed Khaleel Ahmed, Nagarjuna Damarla","doi":"10.26463/rjps.13_3_1","DOIUrl":"https://doi.org/10.26463/rjps.13_3_1","url":null,"abstract":"Tubercular cavernous sinus syndrome is a rare condition of extra-pulmonary tuberculosis EPTB in which cavernous sinus involvement is observed. Cavernous sinus is a venous structure that holds and protects pituitary gland on one side and temporal lobe on other side. CSS is mainly characterized by multiple cranial neuropathies which is effected by various etiologies. This is a case report of tubercular cavernous sinus syndrome admitted to hospital with chief complaints of fever headache drooping of eyelids altered sensorium with disorientation and fever that reduced over next 3 to 4 days but headache was still persisting due to the damage to the cranial nerves. Based on these symptoms they underwent clinical examination which revealed hypotension elevated CRP levels and MRI suggestive of acute dural venous sinus thrombosis involving superior sagittal sinus and bilateral bulky cavernous sinus with transverse T2 hypo intensity in right transverse sagittal superior sagittal and internal jugular vein IJV. Granulomatous etiology indicated tubercular cavernous sinus syndrome. For this treatment was initiated with anti-tubercular drug therapy with vitamin supplements and anticoagulants. EPTB remains a significant health problem in developing countries. Prevalence of EPTB is increasing over the last several years globally.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"9 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135910421","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
Navigating Uncharted Waters: A Vision for our Pharmacy Journal 导航未知水域:我们的药学杂志的愿景
Pub Date : 2023-01-01 DOI: 10.26463/rjps.13_3_2
Dr. Satheesh Babu B K
None
{"title":"Navigating Uncharted Waters: A Vision for our Pharmacy Journal","authors":"Dr. Satheesh Babu B K","doi":"10.26463/rjps.13_3_2","DOIUrl":"https://doi.org/10.26463/rjps.13_3_2","url":null,"abstract":"<jats:p xml:lang=\"en\">None</jats:p>","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"62 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135911277","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
Advances of Niosomes as a Targeted Drug Delivery Syste 纳米体作为靶向给药系统的研究进展
Pub Date : 2023-01-01 DOI: 10.26463/rjps.13_3_7
K Pooja, S B Shirsand
Due to a lack of effective treatment factor or drug delivery systems many diseases go untreated especially when side effects and toxicities are the main cause of concern. Consequently we chose novel drug delivery system. The structure of niosomes is made up of three moieties hydrophilic amphiphilic and lipophilic which can accommodate several drug molecules with a wide range of solubilities. Niosomes are preferred over liposomes because of the non-ionic surfactants higher stability lower cost and ease of storage compared to phospholipids. Surfactants do not require any particular handling or storage conditions. Niosomes act as a controlled and targeted drug delivery system that reduces toxicity and increases drug penetration into target tissues. The review article focused on several ideas including advantages and disadvantages of niosomal preparations niosome characteristics and its application.
由于缺乏有效的治疗因素或药物输送系统,许多疾病得不到治疗,特别是当副作用和毒性是主要引起关注的时候。因此,我们选择了新型给药系统。乳质体的结构由亲水、亲两、亲脂三大部分组成,可容纳多种溶解度较大的药物分子。乳质体比脂质体更受欢迎,因为与磷脂相比,乳质体的非离子表面活性剂具有更高的稳定性、更低的成本和更易于储存。表面活性剂不需要任何特殊的处理或储存条件。Niosomes是一种受控的靶向药物传递系统,可降低毒性并增加药物对靶组织的渗透。本文综述了乳质体制剂的优缺点、乳质体的特性及其应用。
{"title":"Advances of Niosomes as a Targeted Drug Delivery Syste","authors":"K Pooja, S B Shirsand","doi":"10.26463/rjps.13_3_7","DOIUrl":"https://doi.org/10.26463/rjps.13_3_7","url":null,"abstract":"Due to a lack of effective treatment factor or drug delivery systems many diseases go untreated especially when side effects and toxicities are the main cause of concern. Consequently we chose novel drug delivery system. The structure of niosomes is made up of three moieties hydrophilic amphiphilic and lipophilic which can accommodate several drug molecules with a wide range of solubilities. Niosomes are preferred over liposomes because of the non-ionic surfactants higher stability lower cost and ease of storage compared to phospholipids. Surfactants do not require any particular handling or storage conditions. Niosomes act as a controlled and targeted drug delivery system that reduces toxicity and increases drug penetration into target tissues. The review article focused on several ideas including advantages and disadvantages of niosomal preparations niosome characteristics and its application.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"22 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135910413","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 Dendrimer-5-Flurouracil and Folic acid Conjugation for the Treatment of Colon Cancer via Target Drug Delivery 树突状分子-5-氟尿嘧啶与叶酸偶联靶向给药治疗结肠癌的研究进展
Pub Date : 2023-01-01 DOI: 10.26463/rjps.13_3_5
Haribabu T, Selva Kumar K, Manjunatha PM
Background Cancer cells are also known as carcinoma sarcoma melanoma lyphoma and leukemia. The ability of the bodys immune cells to recognise and eliminate newly formed cells when there arent many of them is probably more crucial to the development of cancer than the conversion of a normal cell into a malignant cell. Colonic epithelial cells which line the lumen of the organ and replace themselves every five days from a stem cell population found at the base of colonic epithelial cell crypts are the source of colon cancers.Aim To develop a Dendrimer of 5-Flurouracil and Folic acid conjugate for the treatment of colon cancer via target drug delivery.Methods The dendrimers of 5-Flurouracil and Folic acid conjugate were developed involving the following steps- formulation of dendrimer of antineoplastic drugs dendrimer Acylated Dendrimer characterization of compounds and in ndash vivo anti - cancer activity.Results On 7th and 14th a significant decrease in WBC increase in RBC and increase in Haemoglobin was observed compared to Cancer control.Conclusion It has been concluded that cancer induction in mice Groups I II III results in decreased RBC and Hb levels along with an increase in WBC count. Treatment with drugs restores the abnormal hematopoietic system parameters to normal levels in cancer-bearing mice.
癌细胞也被称为癌、肉瘤、黑色素瘤、淋巴瘤和白血病。人体免疫细胞在新形成的细胞数量不多的情况下识别并清除它们的能力,可能比正常细胞转化为恶性细胞对癌症的发展更为重要。结肠上皮细胞排列在器官的管腔内,每五天从结肠上皮细胞隐窝底部的干细胞群中替换一次,这是结肠癌的来源。目的研制一种5-氟尿嘧啶-叶酸缀合物树状大分子靶向给药治疗结肠癌。方法对5-氟尿嘧啶和叶酸缀合物进行树状大分子的制备、抗肿瘤药物树状大分子的酰基化、化合物树状大分子的表征和体内抗癌活性的研究。结果与对照组相比,第7、14天WBC明显下降,RBC升高,血红蛋白升高。结论:ⅰ组和ⅲ组小鼠肿瘤诱导导致红细胞和血红蛋白水平降低,白细胞计数增加。药物治疗可使患癌小鼠的异常造血系统参数恢复到正常水平。
{"title":"Development of Dendrimer-5-Flurouracil and Folic acid Conjugation for the Treatment of Colon Cancer via Target Drug Delivery","authors":"Haribabu T, Selva Kumar K, Manjunatha PM","doi":"10.26463/rjps.13_3_5","DOIUrl":"https://doi.org/10.26463/rjps.13_3_5","url":null,"abstract":"Background Cancer cells are also known as carcinoma sarcoma melanoma lyphoma and leukemia. The ability of the bodys immune cells to recognise and eliminate newly formed cells when there arent many of them is probably more crucial to the development of cancer than the conversion of a normal cell into a malignant cell. Colonic epithelial cells which line the lumen of the organ and replace themselves every five days from a stem cell population found at the base of colonic epithelial cell crypts are the source of colon cancers.Aim To develop a Dendrimer of 5-Flurouracil and Folic acid conjugate for the treatment of colon cancer via target drug delivery.Methods The dendrimers of 5-Flurouracil and Folic acid conjugate were developed involving the following steps- formulation of dendrimer of antineoplastic drugs dendrimer Acylated Dendrimer characterization of compounds and in ndash vivo anti - cancer activity.Results On 7th and 14th a significant decrease in WBC increase in RBC and increase in Haemoglobin was observed compared to Cancer control.Conclusion It has been concluded that cancer induction in mice Groups I II III results in decreased RBC and Hb levels along with an increase in WBC count. Treatment with drugs restores the abnormal hematopoietic system parameters to normal levels in cancer-bearing mice.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"13 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135910415","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
Amide Codrug Approach: Synthesis and Biopharmaceutical Evaluation of Nonsteroidal Anti-Inflammatory Drug and Calcium Channel Blocker Conjugates 酰胺共药方法:非甾体抗炎药和钙通道阻滞剂缀合物的合成和生物制药评价
Pub Date : 2023-01-01 DOI: 10.26463/rjps.13_3_4
Anjali Nayak, Paramita Das, Amit Kumar Das
Background and Aim Geriatric patients often suffer from osteoarthritis and hypertension comorbidity. The codrugs approach was shown to be an effective strategy for targeting diseases synergistically hence improving the quality of life of patients. The present study aimed to synthesize various Nonsteroidal Anti-inflammatory Drugs NSAIDs and Calcium channel blocker CCB Co-drugs and biopharmaceutical study to eliminate the adverse gastrointestinal effects of the NSAIDs to treat comorbid conditions in geriatric patients with significant reduction of polypharmacy.Methods Various conjugates were synthesized by a one-pot amidation reaction of Amlodipine with various NSAIDs. Further characterization by melting point TLC Fourier transform infrared nuclear magnetic resonance and mass spectroscopy followed by solubility partition coefficient and hydrolysis study in SGF and SIF.Results The synthesized codrugs satisfied the structural criteria of the proposed plan. From the biopharmaceutical and hydrolysis study it was observed that the co-drugs underwent significant hydrolysis in SIF pH 7.4 and have showed delayed onset of action with respect to the standard drugs. The delayed onset may be due to the hydrolysis of amide linkage followed by the release of the prodrug which finally releases the active drug.Conclusion The findings illuminated the codrugs pros and cons aiding optimization and development. This research advances amide-based mutual prodrugs and their use in pharmaceutical research. The outcome of this exploration confirmed that the described co-drug can offer desirable safety and therapeutic benefits. Hence these conjugates could be considered for further development.
背景与目的老年患者常并发骨关节炎和高血压。联合用药方法被证明是一种有效的策略,可以协同靶向疾病,从而改善患者的生活质量。本研究旨在合成多种非甾体类抗炎药NSAIDs与钙通道阻滞剂CCB联合用药及生物制药研究,以消除NSAIDs对胃肠道的不良反应,治疗老年患者合并症,显著减少多药治疗。方法将氨氯地平与多种非甾体抗炎药一锅酰胺化反应合成多种缀合物。通过熔点TLC傅里叶变换红外核磁共振和质谱进一步表征SGF和SIF的溶解度分配系数和水解研究。结果所合成的共药符合所提出方案的结构标准。从生物制药和水解研究中可以观察到,联合药物在SIF pH 7.4时发生了显著的水解,并且相对于标准药物表现出延迟起效。延迟发作可能是由于酰胺键的水解,随后释放前药,最后释放活性药物。结论研究结果阐明了复方药物的优缺点,有助于优化和开发。本研究促进了酰胺基互前药及其在药学研究中的应用。这一探索的结果证实了所描述的联合药物可以提供理想的安全性和治疗效益。因此,这些共轭物可以考虑进一步发展。
{"title":"Amide Codrug Approach: Synthesis and Biopharmaceutical Evaluation of Nonsteroidal Anti-Inflammatory Drug and Calcium Channel Blocker Conjugates","authors":"Anjali Nayak, Paramita Das, Amit Kumar Das","doi":"10.26463/rjps.13_3_4","DOIUrl":"https://doi.org/10.26463/rjps.13_3_4","url":null,"abstract":"Background and Aim Geriatric patients often suffer from osteoarthritis and hypertension comorbidity. The codrugs approach was shown to be an effective strategy for targeting diseases synergistically hence improving the quality of life of patients. The present study aimed to synthesize various Nonsteroidal Anti-inflammatory Drugs NSAIDs and Calcium channel blocker CCB Co-drugs and biopharmaceutical study to eliminate the adverse gastrointestinal effects of the NSAIDs to treat comorbid conditions in geriatric patients with significant reduction of polypharmacy.Methods Various conjugates were synthesized by a one-pot amidation reaction of Amlodipine with various NSAIDs. Further characterization by melting point TLC Fourier transform infrared nuclear magnetic resonance and mass spectroscopy followed by solubility partition coefficient and hydrolysis study in SGF and SIF.Results The synthesized codrugs satisfied the structural criteria of the proposed plan. From the biopharmaceutical and hydrolysis study it was observed that the co-drugs underwent significant hydrolysis in SIF pH 7.4 and have showed delayed onset of action with respect to the standard drugs. The delayed onset may be due to the hydrolysis of amide linkage followed by the release of the prodrug which finally releases the active drug.Conclusion The findings illuminated the codrugs pros and cons aiding optimization and development. This research advances amide-based mutual prodrugs and their use in pharmaceutical research. The outcome of this exploration confirmed that the described co-drug can offer desirable safety and therapeutic benefits. Hence these conjugates could be considered for further development.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"64 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135912888","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
A Review on Vaginal Drug Delivery System 阴道给药系统研究进展
Pub Date : 2015-02-14 DOI: 10.5530/RJPS.2014.4.3
Arshad Khan, C. Saha
Purpose: This review article has been written with a purpose to collate both conventional and novel vaginal drug delivery systems, highlighting the need and advantages of the novel vaginal drug delivery systems. This article will benefit the researchers working in the field of vaginal drug delivery with information about the current research being done in this area. Approach: The unique anatomy and physiology of the vagina is briefly described and then the various conventional and novel drug delivery systems such as vaginal films, vaginal rings, vaginal microspheres, vaginal liposomes, vaginal mucoadhesive caplets, vaginal mini tablets, and vaginal nanofibres are discussed. Research studies focusing on the novel vaginal drug delivery and their findings have also been reported. Findings: The novel vaginal drug delivery systems offer various advantages such as improved mucoadhesion, targeted drug delivery, prolonged drug delivery, improved stability and less frequency of dosing. Conclusion: Traditionally, intravaginal drug delivery has been restricted to delivery of anti infectives to the local vaginal cavity. With the rediscovery of the vaginal route as a potential route for the delivery of therapeutically important molecules, such as microbicides, novel vaginal drug delivery systems are being investigated. These novel systems would enhance the delivery of many drugs offering better therapeutic outcomes.
目的:这篇综述文章的目的是整理传统和新型阴道给药系统,强调新型阴道给药系统的需求和优势。这篇文章将有利于研究人员在阴道给药领域的工作与信息,目前正在做的研究在这一领域。方法:简要描述了阴道独特的解剖学和生理学,然后讨论了各种传统的和新型的药物输送系统,如阴道膜、阴道环、阴道微球、阴道脂质体、阴道黏附胶囊、阴道迷你片和阴道纳米纤维。关于新型阴道给药的研究及其结果也有报道。结果:新型阴道给药系统具有改善黏附、靶向给药、延长给药时间、提高稳定性和减少给药频率等优点。结论:传统上,阴道内给药仅限于局部阴道内给药。随着阴道途径作为一种潜在的治疗重要分子(如杀微生物剂)输送途径的重新发现,新的阴道给药系统正在被研究。这些新系统将增强许多药物的输送,提供更好的治疗效果。
{"title":"A Review on Vaginal Drug Delivery System","authors":"Arshad Khan, C. Saha","doi":"10.5530/RJPS.2014.4.3","DOIUrl":"https://doi.org/10.5530/RJPS.2014.4.3","url":null,"abstract":"Purpose: This review article has been written with a purpose to collate both conventional and novel vaginal drug delivery systems, highlighting the need and advantages of the novel vaginal drug delivery systems. This article will benefit the researchers working in the field of vaginal drug delivery with information about the current research being done in this area. Approach: The unique anatomy and physiology of the vagina is briefly described and then the various conventional and novel drug delivery systems such as vaginal films, vaginal rings, vaginal microspheres, vaginal liposomes, vaginal mucoadhesive caplets, vaginal mini tablets, and vaginal nanofibres are discussed. Research studies focusing on the novel vaginal drug delivery and their findings have also been reported. Findings: The novel vaginal drug delivery systems offer various advantages such as improved mucoadhesion, targeted drug delivery, prolonged drug delivery, improved stability and less frequency of dosing. Conclusion: Traditionally, intravaginal drug delivery has been restricted to delivery of anti infectives to the local vaginal cavity. With the rediscovery of the vaginal route as a potential route for the delivery of therapeutically important molecules, such as microbicides, novel vaginal drug delivery systems are being investigated. These novel systems would enhance the delivery of many drugs offering better therapeutic outcomes.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"36 1","pages":"142-147"},"PeriodicalIF":0.0,"publicationDate":"2015-02-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88185381","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: 5
Safety of Therapies demands intensive post marketing surveillance 治疗的安全性需要在上市后进行严格的监督
Pub Date : 2015-02-14 DOI: 10.5530/RJPS.2014.4.1
R. Thakur
{"title":"Safety of Therapies demands intensive post marketing surveillance","authors":"R. Thakur","doi":"10.5530/RJPS.2014.4.1","DOIUrl":"https://doi.org/10.5530/RJPS.2014.4.1","url":null,"abstract":"","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"7 1","pages":"125-127"},"PeriodicalIF":0.0,"publicationDate":"2015-02-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86483093","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
Microemulsion Based Transdermal Drug Delivery of Labetalol 基于微乳液的拉贝他洛尔经皮给药研究
Pub Date : 2015-02-14 DOI: 10.5530/RJPS.2014.4.4
B. P. Rao, P. Sahithi, Beny Baby, S. Rajarajan, K. Ramesh
Purpose: The purpose of the research was to formulate Microemulsion based transdermal drug delivery for a poorly soluble and low bioavailable drug, labetalol, an antihypertensive agent. Methodology: Based on solubility studies Isopropyl myristate, Tween 80 and 1,2-propylene glycol were selected as Oil, Surfactant and Co-surfactant respectively. Pseudo ternary phase studies were carried out. The optimum concentrations for labetalol microemulsion based on phase diagram and thermodynamic stability evaluation were found to be Isopropyl myristate (6.66% w/w), Mixture (36.66% w/w) of 1 part of Tween 80, 15 parts of 1,2-propylene glycol and remaining water. The labetalol microemulsions were prepared by phase titration method. Findings: The globule size, zeta potential, viscosity, in vitro and ex vivo release for the best formulation was found to be 9.826 nm, -15.96 mV, 0.8872 cP, 92.61% and 71.045% respectively. Permeation studies of labetalol microemulsions were performed through rat skin. The steady state flux (J ss ) was determined and found to be 4.912 mgcm −2 h −1 . Conclusion: Based on the responses labetalol microemulsion shows a potential drug delivery system with good stability and release profile.
目的:为低生物利用度、难溶性降压药拉贝他洛尔制备微乳剂经皮给药方法。方法:通过对肉豆酸异丙酯的溶解度研究,选择Tween 80和1,2-丙二醇分别作为油脂、表面活性剂和助表面活性剂。进行了伪三元相研究。通过相图分析和热力学稳定性评价,得出拉贝他洛尔微乳液的最佳制备浓度为肉豆酸异丙酯(6.66% w/w)、t80 1份、2-丙二醇15份和剩余水的混合物(36.66% w/w)。采用相滴定法制备拉贝他洛尔微乳。结果:最佳配方的微球粒径为9.826 nm, zeta电位为-15.96 mV,黏度为0.8872 cP,体外释放度为92.61%,体外释放度为71.045%。研究了拉贝他洛尔微乳在大鼠皮肤中的渗透作用。测定稳态通量(jss)为4.912 mgcm−2 h−1。结论:拉贝他洛尔微乳具有良好的稳定性和释放特性,是一种潜在的给药系统。
{"title":"Microemulsion Based Transdermal Drug Delivery of Labetalol","authors":"B. P. Rao, P. Sahithi, Beny Baby, S. Rajarajan, K. Ramesh","doi":"10.5530/RJPS.2014.4.4","DOIUrl":"https://doi.org/10.5530/RJPS.2014.4.4","url":null,"abstract":"Purpose: The purpose of the research was to formulate Microemulsion based transdermal drug delivery for a poorly soluble and low bioavailable drug, labetalol, an antihypertensive agent. Methodology: Based on solubility studies Isopropyl myristate, Tween 80 and 1,2-propylene glycol were selected as Oil, Surfactant and Co-surfactant respectively. Pseudo ternary phase studies were carried out. The optimum concentrations for labetalol microemulsion based on phase diagram and thermodynamic stability evaluation were found to be Isopropyl myristate (6.66% w/w), Mixture (36.66% w/w) of 1 part of Tween 80, 15 parts of 1,2-propylene glycol and remaining water. The labetalol microemulsions were prepared by phase titration method. Findings: The globule size, zeta potential, viscosity, in vitro and ex vivo release for the best formulation was found to be 9.826 nm, -15.96 mV, 0.8872 cP, 92.61% and 71.045% respectively. Permeation studies of labetalol microemulsions were performed through rat skin. The steady state flux (J ss ) was determined and found to be 4.912 mgcm −2 h −1 . Conclusion: Based on the responses labetalol microemulsion shows a potential drug delivery system with good stability and release profile.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"23 1","pages":"148-155"},"PeriodicalIF":0.0,"publicationDate":"2015-02-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79407809","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: 1
期刊
RGUHS Journal of Pharmaceutical Sciences
全部 Acc. Chem. Res. ACS Applied Bio Materials ACS Appl. Electron. Mater. ACS Appl. Energy Mater. ACS Appl. Mater. Interfaces ACS Appl. Nano Mater. ACS Appl. Polym. Mater. ACS BIOMATER-SCI ENG ACS Catal. ACS Cent. Sci. ACS Chem. Biol. ACS Chemical Health & Safety ACS Chem. Neurosci. ACS Comb. Sci. ACS Earth Space Chem. ACS Energy Lett. ACS Infect. Dis. ACS Macro Lett. ACS Mater. Lett. ACS Med. Chem. Lett. ACS Nano ACS Omega ACS Photonics ACS Sens. ACS Sustainable Chem. Eng. ACS Synth. Biol. Anal. Chem. BIOCHEMISTRY-US Bioconjugate Chem. BIOMACROMOLECULES Chem. Res. Toxicol. Chem. Rev. Chem. Mater. CRYST GROWTH DES ENERG FUEL Environ. Sci. Technol. Environ. Sci. Technol. Lett. Eur. J. Inorg. Chem. IND ENG CHEM RES Inorg. Chem. J. Agric. Food. Chem. J. Chem. Eng. Data J. Chem. Educ. J. Chem. Inf. Model. J. Chem. Theory Comput. J. Med. Chem. J. Nat. Prod. J PROTEOME RES J. Am. Chem. Soc. LANGMUIR MACROMOLECULES Mol. Pharmaceutics Nano Lett. Org. Lett. ORG PROCESS RES DEV ORGANOMETALLICS J. Org. Chem. J. Phys. Chem. J. Phys. Chem. A J. Phys. Chem. B J. Phys. Chem. C J. Phys. Chem. Lett. Analyst Anal. Methods Biomater. Sci. Catal. Sci. Technol. Chem. Commun. Chem. Soc. Rev. CHEM EDUC RES PRACT CRYSTENGCOMM Dalton Trans. Energy Environ. Sci. ENVIRON SCI-NANO ENVIRON SCI-PROC IMP ENVIRON SCI-WAT RES Faraday Discuss. Food Funct. Green Chem. Inorg. Chem. Front. Integr. Biol. J. Anal. At. Spectrom. J. Mater. Chem. A J. Mater. Chem. B J. Mater. Chem. C Lab Chip Mater. Chem. Front. Mater. Horiz. MEDCHEMCOMM Metallomics Mol. Biosyst. Mol. Syst. Des. Eng. Nanoscale Nanoscale Horiz. Nat. Prod. Rep. New J. Chem. Org. Biomol. Chem. Org. Chem. Front. PHOTOCH PHOTOBIO SCI PCCP Polym. Chem.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1