Pub Date : 2019-05-31DOI: 10.37285/ijpsn.2019.12.3.2
Y. Brhane, Tesfaye Gabriel, T. Adane, Yemisrach Negash, H. Mulugeta, M. Ayele
Tuberculosis (TB) is a contagious infectious illness caused by species having a place with the Mycobacterium tuberculosis complex. The clinical management of tuberculosis still remains a difficult task. Treatment of TB with anti-tubercular drugs becomes the only option available. Hence, the goals of treatment are ensure cure without relapse, prevent death, impede transmission, and prevent emergence of drug resistant strains. This review describes the latest developments and innovative drug delivery strategies for treatment of TB in order to improve the therapeutic efficacy and reduce toxic effect of anti-tubercular agents and enhance patient compliance with concomitant decrease in drug interaction. Among different novel drug delivery systems Niosomes, Liposomes, Dendrimers, Cyclodextrins, Microencapsulation, Alginates and Hydrogels have been described as new drug delivery strategies of anti-tubercular agents.
{"title":"Recent Developments and Novel Drug Delivery Strategies for the Treatment of Tuberculosis","authors":"Y. Brhane, Tesfaye Gabriel, T. Adane, Yemisrach Negash, H. Mulugeta, M. Ayele","doi":"10.37285/ijpsn.2019.12.3.2","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.3.2","url":null,"abstract":"Tuberculosis (TB) is a contagious infectious illness caused by species having a place with the Mycobacterium tuberculosis complex. The clinical management of tuberculosis still remains a difficult task. Treatment of TB with anti-tubercular drugs becomes the only option available. Hence, the goals of treatment are ensure cure without relapse, prevent death, impede transmission, and prevent emergence of drug resistant strains. This review describes the latest developments and innovative drug delivery strategies for treatment of TB in order to improve the therapeutic efficacy and reduce toxic effect of anti-tubercular agents and enhance patient compliance with concomitant decrease in drug interaction. Among different novel drug delivery systems Niosomes, Liposomes, Dendrimers, Cyclodextrins, Microencapsulation, Alginates and Hydrogels have been described as new drug delivery strategies of anti-tubercular agents. ","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"45 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78567227","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}
Pub Date : 2019-05-31DOI: 10.37285/ijpsn.2019.12.3.3
K. Agrawal, Nitin Agrawal, J. Gupta, Tripanshu Gupta
The aim of the present study was to investigate the in-vitro anti-diabetic activity of aqueous and methanolic extract of dried pericarp (Shell) of Juglans regia L. The preliminary qualitative phytochemical screening was also undertaken to reveal the presence of Phyto-constituents in the extracts. Phytochemical screening of aqueous extract shows the presence of polyphenols, flavanoids, cardiac glycosides, carbohydrates and reducing sugar while methanolic extract show the presence of alkaloids, polyphenols, cardiac glycosides, carbohydrates and reducing sugar. Pharmacological evaluation of Juglans regia was performed by α-amylase inhibition assay method. Percentage inhibition of α amylase at dose of 50mg/mL, 100 mg/mL and 150 mg/mL of aqueous and methanolic extract was found to be 33.33, 66.67, 93.34 and 32.27, 59.64, 90.74 respectively. Among the extracts the aqueous extract showed highest activity as compared to control and methanolic extract.
{"title":"Antidiabetic Activity of Aqueous and Methanolic Extract of Dried Pericarp (Shell) of Juglans Regia L.","authors":"K. Agrawal, Nitin Agrawal, J. Gupta, Tripanshu Gupta","doi":"10.37285/ijpsn.2019.12.3.3","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.3.3","url":null,"abstract":"The aim of the present study was to investigate the in-vitro anti-diabetic activity of aqueous and methanolic extract of dried pericarp (Shell) of Juglans regia L. The preliminary qualitative phytochemical screening was also undertaken to reveal the presence of Phyto-constituents in the extracts. Phytochemical screening of aqueous extract shows the presence of polyphenols, flavanoids, cardiac glycosides, carbohydrates and reducing sugar while methanolic extract show the presence of alkaloids, polyphenols, cardiac glycosides, carbohydrates and reducing sugar. Pharmacological evaluation of Juglans regia was performed by α-amylase inhibition assay method. Percentage inhibition of α amylase at dose of 50mg/mL, 100 mg/mL and 150 mg/mL of aqueous and methanolic extract was found to be 33.33, 66.67, 93.34 and 32.27, 59.64, 90.74 respectively. Among the extracts the aqueous extract showed highest activity as compared to control and methanolic extract.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"9 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81146507","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}
Pub Date : 2019-05-31DOI: 10.37285/ijpsn.2018.11.3.1
M. Misra, Aashu Gupta, Kritika Nayak
This review describes current nanotechnology-based delivery systems for ocular targeting. Amongst all the drug delivery systems existing today, ocular drug delivery is one such delivery approach which is having great endeavours due to the challenges faced by it. Many new as well as exciting treatment options have emerged in this field. The major cause behind development of new treatment alternatives in this field are the limitations raised by the conventional approaches. Currently, researchers are working on development of novel nano techniques to overcome these challenges. The major hurdle is associated with the complicated anatomy and physiology of eye having various static (cornea, conjunctiva, retinal pigmental epithelium) as well as dynamic barriers (blood aqueous barrier, blood retinal barrier) which reduce the overall bioavailability of the drugs. These membranous and fluidic barriers make drug delivery to eye a very challenging task. Hence, current research focuses on developing a system, which is least invasive and able to surpass ocular barriers to maintain sufficient drug levels within the ocular tissue. Nanotechnology based delivery systems play a vital role in this. Many vesicular as well as particulate systems are attempted for the same for anterior as well as posterior segment targeting which can easily overcome limitations of conventional drug delivery systems. Current momentum and ongoing research in this field holds a significant level of promise towards development of improved therapies for treating vision related ailments.
{"title":"Nanotechnology-based Strategies for Ocular Drug Delivery Systems","authors":"M. Misra, Aashu Gupta, Kritika Nayak","doi":"10.37285/ijpsn.2018.11.3.1","DOIUrl":"https://doi.org/10.37285/ijpsn.2018.11.3.1","url":null,"abstract":"This review describes current nanotechnology-based delivery systems for ocular targeting. Amongst all the drug delivery systems existing today, ocular drug delivery is one such delivery approach which is having great endeavours due to the challenges faced by it. Many new as well as exciting treatment options have emerged in this field. The major cause behind development of new treatment alternatives in this field are the limitations raised by the conventional approaches. Currently, researchers are working on development of novel nano techniques to overcome these challenges. The major hurdle is associated with the complicated anatomy and physiology of eye having various static (cornea, conjunctiva, retinal pigmental epithelium) as well as dynamic barriers (blood aqueous barrier, blood retinal barrier) which reduce the overall bioavailability of the drugs. These membranous and fluidic barriers make drug delivery to eye a very challenging task. Hence, current research focuses on developing a system, which is least invasive and able to surpass ocular barriers to maintain sufficient drug levels within the ocular tissue. Nanotechnology based delivery systems play a vital role in this. Many vesicular as well as particulate systems are attempted for the same for anterior as well as posterior segment targeting which can easily overcome limitations of conventional drug delivery systems. Current momentum and ongoing research in this field holds a significant level of promise towards development of improved therapies for treating vision related ailments. \u0000 ","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"15 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89262812","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}
Pub Date : 2019-05-31DOI: 10.37285/ijpsn.2019.12.3.5
P. Nerkar, Vaishali Badjuar, Pradyumna P. Ige, H. Mahajan, Sameer Ansari
This manuscript describes the development and validation of a simple, isocratic, and accurate reversed-phase HPLC method for the assay of tramadol in bulk powder form and tablet formulations. The chromato-graphic separation was achieved on an Qualisil BDS C18 (250 mm x 4.6mm, 5μm) column using acetonitrile: methanol: phosphate buffer pH 3.4 adjusted with orthophosphoric acid: (20:10:70, v/v) as a mobile phase, at a flow rate of 1 mL/min and detection at 271 nm. The linear range for tramadol were 2.0 to 10 μg/mL was obtained with correlation coefficients ≥ 0.999. The retention time was found to be 4.47 min for tramadol that was subjected to stress conditions, such as hydrolysis, oxidation, photolysis and thermal degradation, and the stressed samples were analyzed using the above methodology. The method was validated for the precision, accuracy, linearity and robustness. The developed stability-indicating method for tramadol was validated as per ICH guidelines.
{"title":"Development and Validation of Stability-indicating Reverse Phase HPLC Assay for Tramadol in Bulk and Tablet Formulations","authors":"P. Nerkar, Vaishali Badjuar, Pradyumna P. Ige, H. Mahajan, Sameer Ansari","doi":"10.37285/ijpsn.2019.12.3.5","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.3.5","url":null,"abstract":"This manuscript describes the development and validation of a simple, isocratic, and accurate reversed-phase HPLC method for the assay of tramadol in bulk powder form and tablet formulations. The chromato-graphic separation was achieved on an Qualisil BDS C18 (250 mm x 4.6mm, 5μm) column using acetonitrile: methanol: phosphate buffer pH 3.4 adjusted with orthophosphoric acid: (20:10:70, v/v) as a mobile phase, at a flow rate of 1 mL/min and detection at 271 nm. The linear range for tramadol were 2.0 to 10 μg/mL was obtained with correlation coefficients ≥ 0.999. The retention time was found to be 4.47 min for tramadol that was subjected to stress conditions, such as hydrolysis, oxidation, photolysis and thermal degradation, and the stressed samples were analyzed using the above methodology. The method was validated for the precision, accuracy, linearity and robustness. The developed stability-indicating method for tramadol was validated as per ICH guidelines.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"501 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85639332","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}
Pub Date : 2019-05-31DOI: 10.37285/ijpsn.2019.12.3.1
R. Parhi, Divya Supriya N
Transdermal drug delivery (TDD) provides an attractive and alternative drug delivery when compared to oral and other drug delivery as the former route offers several advantages like avoiding pre-systemic first pass metabolism of administered drugs, patient compliance, and avoiding gastric irritation. However, stratum corneum (SC), the upper most layer of skin, limits the permeation of number of drugs because of its barrier property. To breach or bypass this barrier, two approaches namely: chemical and physical are generally used. Physical approaches seem to be better as it does not involve the use of chemicals in the formulations, which could interact, with other component of formulations and more importantly may cause reversible damage to the skin. Microneedle technique is one of the most advanced physical techniques, which can easily by-pass, the SC and allow the drug to reach viable epidermis directly. The needles used in microneedle techniques are in hundreds of micron length range and when applied on skin generally produce little or no pain. The objective of this review is mainly focused on types of microneedles, various materials and fabrication techniques used in the preparation of microneedles. Furthermore, various techniques used in the application of microneedles and mechanism of action are described. In addition, this review also describes commercial products, patents on microneedle technology and recent works carried out on microneedles research and safety aspects of microneedles.
{"title":"Review of Microneedle based Transdermal Drug Delivery Systems","authors":"R. Parhi, Divya Supriya N","doi":"10.37285/ijpsn.2019.12.3.1","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.3.1","url":null,"abstract":"Transdermal drug delivery (TDD) provides an attractive and alternative drug delivery when compared to oral and other drug delivery as the former route offers several advantages like avoiding pre-systemic first pass metabolism of administered drugs, patient compliance, and avoiding gastric irritation. However, stratum corneum (SC), the upper most layer of skin, limits the permeation of number of drugs because of its barrier property. To breach or bypass this barrier, two approaches namely: chemical and physical are generally used. Physical approaches seem to be better as it does not involve the use of chemicals in the formulations, which could interact, with other component of formulations and more importantly may cause reversible damage to the skin. Microneedle technique is one of the most advanced physical techniques, which can easily by-pass, the SC and allow the drug to reach viable epidermis directly. The needles used in microneedle techniques are in hundreds of micron length range and when applied on skin generally produce little or no pain. The objective of this review is mainly focused on types of microneedles, various materials and fabrication techniques used in the preparation of microneedles. Furthermore, various techniques used in the application of microneedles and mechanism of action are described. In addition, this review also describes commercial products, patents on microneedle technology and recent works carried out on microneedles research and safety aspects of microneedles.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"86 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90625197","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}
Amarjit Salunke Salunke, Neeraj Upamanyu, Alka Singh, A. Jaiswal
The convenient and recent drug delivery system always likely to have some ideal and unique characters, particularly for safety, desired actions, accurate delivery, enrich with a therapeutic index with minimal adverse occurrence. In this regard, Nano sponges serve as a recent advance new drug delivery. Many researchers are attracted and concerned on Nano sponges presently. The present twofold objective of the review clarifies why Nano sponges are recent and advanced delivery system along with challenges related to solubility, stability and controlled release of Nano sponge and proven techniques to overcome. Since the nano-sized drug free carriers are recently formulated and suggested for drug delivery, which can be loaded with the numerous drugs, hence dealing with an appropriate technique for drug release is the need of the present time. This article states the most convenient method for drug release, and at concluding part gives awareness on recent work done and result obtained on Nano sponge worldwide along with the unique summary on the US granted patents for Nano sponges. Thus, a complete scenario on recent work, methods for evaluations, unique and multiple characters of Nano sponge has been discussed and summarized.
{"title":"Nano Sponges","authors":"Amarjit Salunke Salunke, Neeraj Upamanyu, Alka Singh, A. Jaiswal","doi":"10.1002/9783527341009","DOIUrl":"https://doi.org/10.1002/9783527341009","url":null,"abstract":"The convenient and recent drug delivery system always likely to have some ideal and unique characters, particularly for safety, desired actions, accurate delivery, enrich with a therapeutic index with minimal adverse occurrence. In this regard, Nano sponges serve as a recent advance new drug delivery. Many researchers are attracted and concerned on Nano sponges presently. The present twofold objective of the review clarifies why Nano sponges are recent and advanced delivery system along with challenges related to solubility, stability and controlled release of Nano sponge and proven techniques to overcome. Since the nano-sized drug free carriers are recently formulated and suggested for drug delivery, which can be loaded with the numerous drugs, hence dealing with an appropriate technique for drug release is the need of the present time. This article states the most convenient method for drug release, and at concluding part gives awareness on recent work done and result obtained on Nano sponge worldwide along with the unique summary on the US granted patents for Nano sponges. Thus, a complete scenario on recent work, methods for evaluations, unique and multiple characters of Nano sponge has been discussed and summarized.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"83 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72915115","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}
Pub Date : 2019-03-31DOI: 10.37285/ijpsn.2019.12.2.1
N. Dudhipala
This article describes the current state and future perspectives of solid lipid nanoparticles for achieving high delivery of drugs with greater therapeutic outcomes. The oral route is the most preferred route of administration for majority of drugs. Problems such as poor solubility or chemical stability in the environment of the gastrointestinal tract, poor permeability through the biological membranes or sensitivity to metabolism are well known to result in the rejection of potential drug candidates as oral delivery products. Hence, lipid-based drug delivery systems have been proposed as a means of bypassing the resistant chemical or physical barriers associated with poorly absorbed drugs. Solid lipid nanoparticles (SLNs) can be an attractive one option for oral drug delivery vehicles as they hold tremendous potential to improve the oral bioavailability of drugs, concomitant reduction of drug toxicity and stability of drug in both GIT and plasma. SLNs are in submicron size range and are made of biocompatible and biodegradable materials capable of incorporating both lipophilic and hydrophilic drugs. SLNs are considered as substitute to other colloidal drug systems and are being used as controlled and targeted delivery systems. The SNL technology has greatly revolutionized the delivery systems for poorly soluble drugs. This article describes the methodologies used for preparation and characterization of SNLs. It outlined the development of stable solid lipid nanoparticles by different techniques. Further, it describes the current status of pharmacokinetic and pharmaco-dynamic studies reported on SLN systems. Finally, it provides a brief outlook on current marketed preparation and the future scope of SLN technology.
{"title":"A Comprehensive Review on Solid Lipid Nanoparticles as Delivery Vehicle for Enhanced Pharmacokinetic and Pharmacodynamic Activity of Poorly Soluble Drugs","authors":"N. Dudhipala","doi":"10.37285/ijpsn.2019.12.2.1","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.2.1","url":null,"abstract":"This article describes the current state and future perspectives of solid lipid nanoparticles for achieving high delivery of drugs with greater therapeutic outcomes. The oral route is the most preferred route of administration for majority of drugs. Problems such as poor solubility or chemical stability in the environment of the gastrointestinal tract, poor permeability through the biological membranes or sensitivity to metabolism are well known to result in the rejection of potential drug candidates as oral delivery products. Hence, lipid-based drug delivery systems have been proposed as a means of bypassing the resistant chemical or physical barriers associated with poorly absorbed drugs. Solid lipid nanoparticles (SLNs) can be an attractive one option for oral drug delivery vehicles as they hold tremendous potential to improve the oral bioavailability of drugs, concomitant reduction of drug toxicity and stability of drug in both GIT and plasma. SLNs are in submicron size range and are made of biocompatible and biodegradable materials capable of incorporating both lipophilic and hydrophilic drugs. SLNs are considered as substitute to other colloidal drug systems and are being used as controlled and targeted delivery systems. The SNL technology has greatly revolutionized the delivery systems for poorly soluble drugs. This article describes the methodologies used for preparation and characterization of SNLs. It outlined the development of stable solid lipid nanoparticles by different techniques. Further, it describes the current status of pharmacokinetic and pharmaco-dynamic studies reported on SLN systems. Finally, it provides a brief outlook on current marketed preparation and the future scope of SLN technology.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"27 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82237817","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}
Pub Date : 2019-03-31DOI: 10.37285/ijpsn.2019.12.2.8
Kamar Shayah, Abduljalil Ghrewati, Y. Mohammad, I. Hadid
Genetic variations in drug metabolizing hepatic CYP2C9 gene determine the optimal dose for many drugs including anticoagulants such as warfarin. Here we sought to detect the frequency distribution of genetic variations of CYP2C9 gene and to determine its potential role in the control of warfarin dose in Syrian patients. The study included 125 patients with high risk of thrombosis of adults who visited the Heart Disease & Surgery Hospital (HDSH) and Aleppo University Hospital (AUH) and treated with warfarin as oral anticoagulant therapy, and the dose-corrected by the international normalized ratio (INR) at least three months ago. Genomic DNA was extracted from blood samples, and genotype analysis for CYP2C9*2 and CYP2C9*3 variant alleles was done by polymerase chain reaction-restriction fragment length polymorphism assay (PCR-RFLP). Data were analyzed using SPSS version 20. The results obtained in this study suggest that Genotype frequency distribution of CYP2C9*2 and CYP2C9*3 variant alleles was found to be different from other populations and has significant effect on warfarin dose requirement (p<0.05). It is concluded that there is a need to include CYP2C9 genetic variations detection tests in the warfarin dosing algorithm, as this has an important role in reducing serious hemorrhagic complications, especially in patients with the CYP2C9*2/*2 and CYP2C9*3/*3 homozygous mutant genotypes.
药物代谢肝脏CYP2C9基因的遗传变异决定了包括华法林等抗凝剂在内的许多药物的最佳剂量。在这里，我们试图检测CYP2C9基因遗传变异的频率分布，并确定其在叙利亚患者华法林剂量控制中的潜在作用。该研究纳入125例血栓形成高风险的成人患者，这些患者就诊于心脏病和外科医院(HDSH)和阿勒颇大学医院(AUH)，接受华法林作为口服抗凝治疗，并至少在三个月前按国际标准化比例(INR)进行剂量校正。提取血样中基因组DNA，采用聚合酶链反应-限制性片段长度多态性法(PCR-RFLP)对CYP2C9*2和CYP2C9*3变异等位基因进行基因型分析。数据分析采用SPSS version 20。本研究结果表明，CYP2C9*2和CYP2C9*3变异等位基因的基因型频率分布与其他人群不同，对华法林剂量需用量有显著影响(p<0.05)。因此，有必要在华法林给药方案中纳入CYP2C9基因变异检测试验，因为这对减少严重出血并发症具有重要作用，特别是对于CYP2C9*2/*2和CYP2C9*3/*3纯合突变基因型患者。
{"title":"Role of Genetic Variations in the CYP2C9 Gene in Determining the Optimal Dose of Warfarin in a Group of Syrian Patients","authors":"Kamar Shayah, Abduljalil Ghrewati, Y. Mohammad, I. Hadid","doi":"10.37285/ijpsn.2019.12.2.8","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.2.8","url":null,"abstract":"Genetic variations in drug metabolizing hepatic CYP2C9 gene determine the optimal dose for many drugs including anticoagulants such as warfarin. Here we sought to detect the frequency distribution of genetic variations of CYP2C9 gene and to determine its potential role in the control of warfarin dose in Syrian patients. The study included 125 patients with high risk of thrombosis of adults who visited the Heart Disease & Surgery Hospital (HDSH) and Aleppo University Hospital (AUH) and treated with warfarin as oral anticoagulant therapy, and the dose-corrected by the international normalized ratio (INR) at least three months ago. Genomic DNA was extracted from blood samples, and genotype analysis for CYP2C9*2 and CYP2C9*3 variant alleles was done by polymerase chain reaction-restriction fragment length polymorphism assay (PCR-RFLP). Data were analyzed using SPSS version 20. The results obtained in this study suggest that Genotype frequency distribution of CYP2C9*2 and CYP2C9*3 variant alleles was found to be different from other populations and has significant effect on warfarin dose requirement (p<0.05). It is concluded that there is a need to include CYP2C9 genetic variations detection tests in the warfarin dosing algorithm, as this has an important role in reducing serious hemorrhagic complications, especially in patients with the CYP2C9*2/*2 and CYP2C9*3/*3 homozygous mutant genotypes. ","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"31 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75772805","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}
Pub Date : 2019-03-31DOI: 10.37285/ijpsn.2019.12.2.7
Sandhya Pamu, S SubrahmanyamC.V., Patnaik K. S. K. Rao
An oral dosage form containing gastro-retentive floating tablets forms a stomach-specific drug delivery system for the treatment of hypertension. Valsartan belongs to the BCS class II (poo Classification System). It is desirable to improve the extent of bioavailability (23%). The objective of the present study was to apply design of experiment to optimize floating drug delivery of valsartan by employing 22 factorial design. Improvement of the aqueous solubility of valsartan was done by solid dispersions using hot melt extrusion technique. Plasdone S630 copovidone is a variable carrier and drug to carrier ratio of 1:2 was optimized. Valsartan floating tablets were prepared by employing factorial design (22), where HPMC K15M (X1) and pregelatinized starch (X2) were independent variables and drug dissolution was the dependent parameter (Y1) to prepare matrix tablets. The factorial analysis, steepest ascent method was utilized for obtaining optimized formulation. In vitro evaluation, In vivo radiographic study and biopharmaceutical analysis in rabbits for valsartan optimized formulation (FT-5). Floating lag time (FLT) for valsartan optimized formulation (FT-5) was 15 s and total floating time (TFT) of the tablets was about 33 h, which was satisfactory. A four-point (1 h, 4 h, 8 h and 16 h) dissolution analysis gave satisfactory dissolution profile up to 24 h. The release kinetics of valsartan optimized formulation (FT-5) followed zero order and the release mechanism was found to be Korsemeyer Peppas model, i.e. swelling type. The dissolution efficiency for valsartan floating tablets was 1190.89% against the marketed formulation of 39.77%. The accelerated stability profile of valsartan optimized formulation (FT-5) was evaluated in terms of drug content and percent cumulative dissolution of valsartan in 24 h, in a 6 months study. In vivo X-ray image study for valsartan optimized formulation (FT-5) indicated the presence of intact tablet up to 12 h in gastric region of rabbit. The biopharmaceutical analysis in rabbits was conducted for valsartan optimized formulation (FT-5). The HPLC method was established and validated for the in vivo analysis. The Cmax was 453.2 ng/mL compared to that of the marketed tablets (522.4 ng/mL). The mean residence time (MRT) for the valsartan optimized formulation (FT-5) was 14.82 h as against 4 h for marketed tablet. The relative bioavailability of valsartan optimized formulation (FT-5) was 650% higher than the marketed tablet. To overcome the poor bioavailability of valsartan, it was suitably modified using hot-melt extrusion for improving therapeutic outcome. In conclusion, gastro-retentive drug delivery system is an excellent approach for improving the bioavailability of valsartan.
{"title":"Formulation of Gastro-retentive Floating Tablets of Valsartan by 2 power 2 Factorial Designs: In vitro and In vivo Evaluations","authors":"Sandhya Pamu, S SubrahmanyamC.V., Patnaik K. S. K. Rao","doi":"10.37285/ijpsn.2019.12.2.7","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.2.7","url":null,"abstract":"An oral dosage form containing gastro-retentive floating tablets forms a stomach-specific drug delivery system for the treatment of hypertension. Valsartan belongs to the BCS class II (poo Classification System). It is desirable to improve the extent of bioavailability (23%). The objective of the present study was to apply design of experiment to optimize floating drug delivery of valsartan by employing 22 factorial design. Improvement of the aqueous solubility of valsartan was done by solid dispersions using hot melt extrusion technique. Plasdone S630 copovidone is a variable carrier and drug to carrier ratio of 1:2 was optimized. Valsartan floating tablets were prepared by employing factorial design (22), where HPMC K15M (X1) and pregelatinized starch (X2) were independent variables and drug dissolution was the dependent parameter (Y1) to prepare matrix tablets. The factorial analysis, steepest ascent method was utilized for obtaining optimized formulation. In vitro evaluation, In vivo radiographic study and biopharmaceutical analysis in rabbits for valsartan optimized formulation (FT-5). Floating lag time (FLT) for valsartan optimized formulation (FT-5) was 15 s and total floating time (TFT) of the tablets was about 33 h, which was satisfactory. A four-point (1 h, 4 h, 8 h and 16 h) dissolution analysis gave satisfactory dissolution profile up to 24 h. The release kinetics of valsartan optimized formulation (FT-5) followed zero order and the release mechanism was found to be Korsemeyer Peppas model, i.e. swelling type. The dissolution efficiency for valsartan floating tablets was 1190.89% against the marketed formulation of 39.77%. The accelerated stability profile of valsartan optimized formulation (FT-5) was evaluated in terms of drug content and percent cumulative dissolution of valsartan in 24 h, in a 6 months study. In vivo X-ray image study for valsartan optimized formulation (FT-5) indicated the presence of intact tablet up to 12 h in gastric region of rabbit. The biopharmaceutical analysis in rabbits was conducted for valsartan optimized formulation (FT-5). The HPLC method was established and validated for the in vivo analysis. The Cmax was 453.2 ng/mL compared to that of the marketed tablets (522.4 ng/mL). The mean residence time (MRT) for the valsartan optimized formulation (FT-5) was 14.82 h as against 4 h for marketed tablet. The relative bioavailability of valsartan optimized formulation (FT-5) was 650% higher than the marketed tablet. To overcome the poor bioavailability of valsartan, it was suitably modified using hot-melt extrusion for improving therapeutic outcome. In conclusion, gastro-retentive drug delivery system is an excellent approach for improving the bioavailability of valsartan. \u0000 ","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"56 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75698262","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}
Pub Date : 2019-03-31DOI: 10.37285/ijpsn.2019.12.2.2
M. Kulshreshtha, Pragati Srivastava, D. Panjwani
This review article describes the role of hormones, microvascular complications, pharmacological and non-pharmacological treatments and precautions of diabetes therapy. Diabetes mellitus (DM) is a chronic, lifelong condition that affects ability to use the energy found in food. According to World Health Organization (WHO), it is estimated 422 million adults are suffered with DM up to latest 2016 data. It occurs throughout the world but is more common in the more developed countries. Increase in prevalence is occurring in low- and middle-income countries including in Asia and Africa, where most patients will probably be found by 2030. The WHO estimates that diabetes resulted in 1.5 million deaths in 2012, making it the 8th leading cause of death. We summarized the published scientific data and new development in the field of diabetes with a search of PubMed, Google scholar, med know and other online resources. Various hormones play an important role in which insulin has a more importance in DM. Pharmacological treatment included various side effects while herbal drugs are found to be safe. Diet and exercise are the excellent key points to cure the disease. Avoid high sugar diet and various foods whose sugar levels are high should be avoided at the age 40. Overall, better knowledge, balanced life style, and daily exercise are the excellent treatment of diabetes and effective glucose control.
{"title":"Endocrine and Therapeutic Basis of Diabetes Mellitus Therapy","authors":"M. Kulshreshtha, Pragati Srivastava, D. Panjwani","doi":"10.37285/ijpsn.2019.12.2.2","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.2.2","url":null,"abstract":"\u0000This review article describes the role of hormones, microvascular complications, pharmacological and non-pharmacological treatments and precautions of diabetes therapy. Diabetes mellitus (DM) is a chronic, lifelong condition that affects ability to use the energy found in food. According to World Health Organization (WHO), it is estimated 422 million adults are suffered with DM up to latest 2016 data. It occurs throughout the world but is more common in the more developed countries. Increase in prevalence is occurring in low- and middle-income countries including in Asia and Africa, where most patients will probably be found by 2030. The WHO estimates that diabetes resulted in 1.5 million deaths in 2012, making it the 8th leading cause of death. We summarized the published scientific data and new development in the field of diabetes with a search of PubMed, Google scholar, med know and other online resources. Various hormones play an important role in which insulin has a more importance in DM. Pharmacological treatment included various side effects while herbal drugs are found to be safe. Diet and exercise are the excellent key points to cure the disease. Avoid high sugar diet and various foods whose sugar levels are high should be avoided at the age 40. Overall, better knowledge, balanced life style, and daily exercise are the excellent treatment of diabetes and effective glucose control. ","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"2 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75531438","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}
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