Swapnil Sharma | Banasthali University (original) (raw)
Papers by Swapnil Sharma
Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512)
In folk medicine there are various medicinal amalgamation possessing hepatoprotective activity. T... more In folk medicine there are various medicinal amalgamation possessing hepatoprotective activity. This activity is of significance because several toxins cause liver injury. Hence, many pharmaceutical companies are targeting herbal medicines for the treatment of liver abnormalities and towards evolving a safe and effective formulation with desired route of administration. In current review we have focused on the studies showing hepatoprotective effect using marine compounds and plant derived compounds. Liver disorder, a global health problem, usually include acute or chronic hepatitis, heptoses, and cirrhosis. It may be due to toxic chemicals and certain antibiotics. Uncontrolled consumption of alcohol also affects liver in an unhealthy way. To cure liver disorders several formulations of medicinal plants are being used. It is observed that hepatoprotective effect of plant is mostly due to flavonoids, alkaloids, terpenoids, steroids, and glycoside. A single drug cannot be useful for a...
Inorganic Chemistry Communications
Clinical Drug Investigation
Background and Objective Early management of traumatic brain injury (TBI) is essential. We aimed ... more Background and Objective Early management of traumatic brain injury (TBI) is essential. We aimed to evaluate the efficacy of vitamin D over early clinical outcome and serum cytokine levels in patients with moderate to severe brain injury. Methods Thirty-five patients with moderate to severe traumatic brain injury who were admitted to the ICU unit were recruited into the study. Subjects were randomly allocated to a treatment regimen comprising either a one-time oral dose of 120,000 IU (two tablets of 60,000 IU each) of vitamin D (n = 20) or 8 mg of saccharide (two tablets of 4 g each) as placebo (n = 15). The main parameters evaluated included duration of mechanical ventilation and ICU stay, Glasgow Coma Scale (GCS) and cytokine levels (interleukin (IL)-6, tumour necrosis factor (TNF)-α, interferon (IFN)-γ, IL-2). Results The results indicated an improvement in the level of consciousness after 7 days in the vitamin D-treated group compared with placebo. An elevation in GCS score by 3.86 units in the vitamin D-treated group with a 0.19-unit descent in the control group was recorded. Duration of mechanical ventilation was reduced in the vitamin D-treated group compared with the control group (4.7 days vs. 8.2 days, p value 0.0001). A noticeable reduction was recorded in inflammatory biomarkers (cytokines) in the vitamin D-treated group (IL-6 p = 0.08, TNF-α p = 0.02, IL-2 p = 0.36) with notable elevation in IFN-γ (p = 0.65) compared to the control group. Conclusion In the acute phase of moderate to severe traumatic brain injury, vitamin D supplementation plays a vital role and has a favourable effect on the consciousness level of patients. Clinical trial Registry (CTRI) No. CTRI/2019/05/019259.
Current Stem Cell Research & Therapy
Damaged or disabled tissue is life-threatening due to the lack of proper treatment. Many conventi... more Damaged or disabled tissue is life-threatening due to the lack of proper treatment. Many conventional transplantation methods like autograft, iso-graft and allograft are in existence for ages, but they are not sufficient to treat all types of tissue or organ damages. Stem cells, with their unique capabilities like self-renewal and differentiate into various cell types, can be a potential strategy for tissue regeneration. However, the challenges like reproducibility, uncontrolled propagation and differentiation, isolation of specific kinds of cell and tumorigenic nature made these stem cells away from clinical application. Today, various types of stem cells like embryonic, fetal or gestational tissue, mesenchymal and induced-pluripotent stem cells are under investigation for their clinical application. Tissue engineering helps in configuring the stem cells to develop into a desired viable tissue, to use them clinically as a substitute for the conventional method. The use of stem cell...
JPC – Journal of Planar Chromatography – Modern TLC
Oriental Pharmacy and Experimental Medicine
Treatment of cognitive disorders is a challenging task in neurology since long time. Crataegus ox... more Treatment of cognitive disorders is a challenging task in neurology since long time. Crataegus oxyacantha, also known as hawthorn belongs to family Rosaceae grew in colder areas and is one of the most widely used herb for the treatment of heart disorders. Traditionally Crataegus oxyacantha has also been used to treat Alzheimer disease, nervousness, stress, pain, and sleep disorders. In this study nootropic activity of petroleum ether, chloroform and methanol extract of Crataegus oxyacantha leaves was assessed using elevated plus maze model. Scopolamine (1 mg/kg) was used as amnesia-inducing agent and piracetam (120 mg/ kg) as standard nootropic drug. On the last day of the experiment, biochemical parameters like acetylcholinesterase, lipid peroxidase, and superoxide dismutase were measured in brain homogenate.EffectofCrataegusoxyacanthaonmonoamines mediated behaviour was assessed through lithium-induced head twitches and haloperidol-induced catalepsy model in rats. Among all three extracts, methanol extract of Crataegus oxyacantha caused the highest reduction in transfer latency time significantly as measured on the 7th and 14th day and on 8th and 15th day on elevated maze and also decreased acetylcholinesterase and lipid peroxidase level and increased superoxide dismutase content as compared to scopolamine group. Methanol extract of Crataegus oxyacantha (200 mg/kg and 400 mg/kg) decreased number of head twitches and duration of catalepsy in rats significantly compared to vehicle-treated group. So our study showed promising effect of Crataegus oxyacantha in enhancing learning and memory due to the presence of certain phytoconstituents.
Journal of Herbs, Spices & Medicinal Plants
The nephroprotective activity of hydro-alcoholic (HAEAM) and ethyl acetate (EAEAM) extracts of Ae... more The nephroprotective activity of hydro-alcoholic (HAEAM) and ethyl acetate (EAEAM) extracts of Aegle marmelos leaves were evaluated against nephrotoxicity induced by cisplatin (CP), a widely used chemotherapeutic agent in cancer therapy. Wistar rats were treated with CP (6 mg.kg-1 ; i.p.). Treatment groups received the same dose of CP, along with HAEAM and EAEAM (200 and 400 mg. kg-1) orally for 5 d. Blood urea nitrogen (BUN), serum creatinine, and antioxidant enzymes were estimated in renal tissues. EAEAM exhibited minimum IC 50 values 6.13 ± 1.05, 67.34 ± 1.7, 59.7 ± 3.9, and 49.17 ± 2.19 μg.mL-1. EAEAM (400 mg.kg-1) decreased the creatinine levels from 2.29 ± 0.387 to 0.96 ± 0.095 mg.dL-1 and BUN from 92.06 ± 7.949 to 38.18 ± 5.686 mg.dL-1 and restored the activities of renal antioxidant enzymes, decreased the lipid peroxidasde (LPO) levels from 158.70 ± 3.542 to 106.91 ± 5.876 nM.g-1 , and increased superoxide dismutase (SOD) levels from 12.59 ± 0.463 to 29.95 ± 5.222 U.g-1 , glutathione (GSH) from 0.24 ± 0.029 to 0.57 ± 0.048 μM.g-1 , and catalase (CAT) from 1.14 ± 0.067 to 3.27 ± 0.296 U.mg-1).
Alzheimer’s disease (AD), the most widespread cause of dementia is delineated by progressive cogn... more Alzheimer’s disease (AD), the most widespread cause of dementia is delineated by progressive cognitive impairment in the elderly people. During its progression, N-Methyl-D-Aspartate receptor antagonists are known to play a key role in the mechanisms of learning and memory. Extensive side effects alongside other effects on learning and memory have limited the therapeutic significance of various blockers and antagonists of the NMDA receptor. In this study, we identify potential compounds targeted against NMDA. In order to reveal the essential structural features for NMDA receptor, three-dimensional pharmacophore models are constructed based on a set of known NMDA inhibitors. This is followed by virtual screening which results in novel chemical compounds having the potential to inhibit NMDA. The lead compounds are then subjected to molecular docking and assessed by a scoring function, which results in two compounds with high Libdock scores. These compounds also show interactions with i...
Letters in Drug Design & Discovery
Background: Alzheimer’s disease is a medical condition with detrimental brain health. It is major... more Background: Alzheimer’s disease is a medical condition with detrimental brain health. It is majorly diagnosed in aging individuals plaque in β) characterized by accumulated Amyloidal beta (A 1 BACE) 1 secretase APP cleavage enzyme βneurological areas. The ) is the target of choice that can be exploited to find drugs against Alzheimer’s disease. Methods: A series of BACE-1 inhibitors with reported binding constant were considered for the development of a feature based pharmacophore model. Results: The good correlation coefficient (r=0.91) and RMSD of 0.93 was observed with 30 compounds in training set. The model was validated internally (r2test=0.76) as well as externally by Fischer validation. The pharmacophore based virtual screening retrieved compounds that were docked and biologically evaluated. Conclusion: The three structurally diverse molecules were tested by in-vitro method. The pyridine derivative with highest fit value (6.9) exhibited IC50 value of 2.70 µM and thus was foun...
Oriental Pharmacy and Experimental Medicine
Journal of Microencapsulation
International Journal of Polymeric Materials and Polymeric Biomaterials
Journal of Microbiological Methods
Journal of Traditional and Complementary Medicine
Current Computer-Aided Drug Design
Background: : Rho-kinase is an essential downstream target of GTP-binding protein RhoA, and plays... more Background: : Rho-kinase is an essential downstream target of GTP-binding protein RhoA, and plays a crucial role in the calcium-sensitization pathway. Rho-kinase pathway is critically involved in phosphorylation state of myosin light chain, leading to increased contraction of smooth muscles. Inhibition of this pathway has turned out to be a promising target for several indications such as cardiovascular diseases, glaucoma and inflammatory diseases. Methods:: The present work focuses on a division-based 2D quantitative structure-activity relationship (QSAR) analysis along with a docking study to predict structural features that may be essential for the enhancement of selectivity and potency of the target compounds. Furthermore, a set of indoles and azaindoles were also projected based on the regression equation as novel developments. Molecular docking was applied for exploring the binding sites of the newly predicted set of compounds with the receptor. Results: : Results of the docke...
International Journal of PharmTech Research
Background: Immediate release formulation of Hydrochlorothiazide is available in market. Cmax ach... more Background: Immediate release formulation of Hydrochlorothiazide is available in market. Cmax achieved at 2 h, duration of action persist for 6-12 h, resulting in multiple dosing to maintain plasma concentration and in vivo activity. Objective: The objective of research work was to design modified release tablets of Hydrochlorothiazide 25 mg with the intention of once a day dosing. Cmax will achieve after 10 to 12 h of administration. This controlled release will constantly induce diuretic activity for whole night and day especially during early morning hours, resulting in decreased blood volume, reduced cardiac output and controlled blood pressure. When patient awakes up in morning, blood pressure will be comparatively low thus reducing the frequency of cardiac arrest.Method: Here an attempt has been made to kinetically calculate required in-vitro dissolution profile by deconvolution method using Wagner-nelson equation. Plasma concentration time profile of immediate release tablet 12.5 mg is available in literature and that of modified release formulation 25 mg is calculated such that Area under curve of modified release tablet matches with that of two immediate release tablets of 12.5 mg along with Cmax and Kel, thus meeting the criteria for bio-equivalency. Tmax will be delayed from 2 h to approximately 10 h. Results: In-vivo dissolution profile is calculated from the equation of "fraction of drug absorbed". Perfect IVIVC is matched when value of slope is 1, intercept is 0 and correlation coefficient (R 2) 0.99. Conclusion: This in-vitro profile will be used further to develop modified release formulation.
Scientific reports, Jan 2, 2018
In view of the role of sEH (soluble epoxide hydrolase) in hypertension, we have developed a rigor... more In view of the role of sEH (soluble epoxide hydrolase) in hypertension, we have developed a rigorously validated pharmacophore model containing one HBA (Hydrogen Bond Acceptor), two HY (Hydrophobic) and one RA (Ring Aromatic) features. The model was used as a query to search the NCI (National Cancer Institute) and Maybridge database leading to retrieval of many compounds which were sorted on the basis of predicted activity, fit value and Lipinski's violation. The selected compounds were docked into the active site of enzyme soluble epoxide hydrolase. Potential interactions were observed between the features of the identified hits and the amino acids present in the docking site. The three selected compounds were subjected to in vitro evaluation using enzyme- based assay and the isolated rat aortic model followed by cytotoxicity studies. The results demonstrate that the identified compounds are potent, safe and novel soluble epoxide hydrolase inhibitors.
Current clinical pharmacology, Jan 25, 2018
Computer has wide applicability in many field, and in pharmaceutical science the computer play a ... more Computer has wide applicability in many field, and in pharmaceutical science the computer play a crucial role as a commander of all the theoretical aspects and provide a workbench to improve the overall quality system of the pharmaceutical research and development. The aim of this article is to provide computational approach in development of the many booming technology of computer software in the field of clinical pharmacokinetics. The computational technique practiced by clinical pharmacist and scientist with the applied knowledge and skills of dealing with clinical pharmacokinetics problems, which can be applied in routine clinical practices. Methods used to distinguish the pharmacokinetics (PK) and pharmacodynamics (PD) analysis software has evolved greatly in recent years, allowing users to focus on analysis. Clinical pharmacokinetics software like Population pharmacokinetics, Individual pharmacokinetics, ADME pharmacokinetics, in - silico pharmacokinetics like WinNonlin, SAS, ...
Journal of Heterocyclic Chemistry
Therapeutic drug monitoring, Jan 6, 2018
Therapeutic drug monitoring (TDM) of anti-epileptic drugs provides a valid clinical tool in optim... more Therapeutic drug monitoring (TDM) of anti-epileptic drugs provides a valid clinical tool in optimization of overall therapy. However, TDM is challenging due to the high biological samples (plasma/blood) storage/shipment costs and the limited availability of laboratories providing TDM services. Sampling in the form of dry plasma spot (DPS) or dry blood spot (DBS) is a suitable alternative to overcome these issues. An improved, simple, rapid, and stability indicating method for quantification of pregabalin in human plasma and DPS has been developed and validated. Analyses were performed on liquid chromatography tandem mass spectrometer under positive ionization mode of electrospray interface. Pregabain-d4 was used as internal standard, and the chromatographic separations were performed on Poroshell 120 EC-C18 column using an isocratic mobile phase flow rate of 1 mL/min. Stability of pregabalin in DPS was evaluated under simulated real-time conditions. Extraction procedures from plasma...
Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512)
In folk medicine there are various medicinal amalgamation possessing hepatoprotective activity. T... more In folk medicine there are various medicinal amalgamation possessing hepatoprotective activity. This activity is of significance because several toxins cause liver injury. Hence, many pharmaceutical companies are targeting herbal medicines for the treatment of liver abnormalities and towards evolving a safe and effective formulation with desired route of administration. In current review we have focused on the studies showing hepatoprotective effect using marine compounds and plant derived compounds. Liver disorder, a global health problem, usually include acute or chronic hepatitis, heptoses, and cirrhosis. It may be due to toxic chemicals and certain antibiotics. Uncontrolled consumption of alcohol also affects liver in an unhealthy way. To cure liver disorders several formulations of medicinal plants are being used. It is observed that hepatoprotective effect of plant is mostly due to flavonoids, alkaloids, terpenoids, steroids, and glycoside. A single drug cannot be useful for a...
Inorganic Chemistry Communications
Clinical Drug Investigation
Background and Objective Early management of traumatic brain injury (TBI) is essential. We aimed ... more Background and Objective Early management of traumatic brain injury (TBI) is essential. We aimed to evaluate the efficacy of vitamin D over early clinical outcome and serum cytokine levels in patients with moderate to severe brain injury. Methods Thirty-five patients with moderate to severe traumatic brain injury who were admitted to the ICU unit were recruited into the study. Subjects were randomly allocated to a treatment regimen comprising either a one-time oral dose of 120,000 IU (two tablets of 60,000 IU each) of vitamin D (n = 20) or 8 mg of saccharide (two tablets of 4 g each) as placebo (n = 15). The main parameters evaluated included duration of mechanical ventilation and ICU stay, Glasgow Coma Scale (GCS) and cytokine levels (interleukin (IL)-6, tumour necrosis factor (TNF)-α, interferon (IFN)-γ, IL-2). Results The results indicated an improvement in the level of consciousness after 7 days in the vitamin D-treated group compared with placebo. An elevation in GCS score by 3.86 units in the vitamin D-treated group with a 0.19-unit descent in the control group was recorded. Duration of mechanical ventilation was reduced in the vitamin D-treated group compared with the control group (4.7 days vs. 8.2 days, p value 0.0001). A noticeable reduction was recorded in inflammatory biomarkers (cytokines) in the vitamin D-treated group (IL-6 p = 0.08, TNF-α p = 0.02, IL-2 p = 0.36) with notable elevation in IFN-γ (p = 0.65) compared to the control group. Conclusion In the acute phase of moderate to severe traumatic brain injury, vitamin D supplementation plays a vital role and has a favourable effect on the consciousness level of patients. Clinical trial Registry (CTRI) No. CTRI/2019/05/019259.
Current Stem Cell Research & Therapy
Damaged or disabled tissue is life-threatening due to the lack of proper treatment. Many conventi... more Damaged or disabled tissue is life-threatening due to the lack of proper treatment. Many conventional transplantation methods like autograft, iso-graft and allograft are in existence for ages, but they are not sufficient to treat all types of tissue or organ damages. Stem cells, with their unique capabilities like self-renewal and differentiate into various cell types, can be a potential strategy for tissue regeneration. However, the challenges like reproducibility, uncontrolled propagation and differentiation, isolation of specific kinds of cell and tumorigenic nature made these stem cells away from clinical application. Today, various types of stem cells like embryonic, fetal or gestational tissue, mesenchymal and induced-pluripotent stem cells are under investigation for their clinical application. Tissue engineering helps in configuring the stem cells to develop into a desired viable tissue, to use them clinically as a substitute for the conventional method. The use of stem cell...
JPC – Journal of Planar Chromatography – Modern TLC
Oriental Pharmacy and Experimental Medicine
Treatment of cognitive disorders is a challenging task in neurology since long time. Crataegus ox... more Treatment of cognitive disorders is a challenging task in neurology since long time. Crataegus oxyacantha, also known as hawthorn belongs to family Rosaceae grew in colder areas and is one of the most widely used herb for the treatment of heart disorders. Traditionally Crataegus oxyacantha has also been used to treat Alzheimer disease, nervousness, stress, pain, and sleep disorders. In this study nootropic activity of petroleum ether, chloroform and methanol extract of Crataegus oxyacantha leaves was assessed using elevated plus maze model. Scopolamine (1 mg/kg) was used as amnesia-inducing agent and piracetam (120 mg/ kg) as standard nootropic drug. On the last day of the experiment, biochemical parameters like acetylcholinesterase, lipid peroxidase, and superoxide dismutase were measured in brain homogenate.EffectofCrataegusoxyacanthaonmonoamines mediated behaviour was assessed through lithium-induced head twitches and haloperidol-induced catalepsy model in rats. Among all three extracts, methanol extract of Crataegus oxyacantha caused the highest reduction in transfer latency time significantly as measured on the 7th and 14th day and on 8th and 15th day on elevated maze and also decreased acetylcholinesterase and lipid peroxidase level and increased superoxide dismutase content as compared to scopolamine group. Methanol extract of Crataegus oxyacantha (200 mg/kg and 400 mg/kg) decreased number of head twitches and duration of catalepsy in rats significantly compared to vehicle-treated group. So our study showed promising effect of Crataegus oxyacantha in enhancing learning and memory due to the presence of certain phytoconstituents.
Journal of Herbs, Spices & Medicinal Plants
The nephroprotective activity of hydro-alcoholic (HAEAM) and ethyl acetate (EAEAM) extracts of Ae... more The nephroprotective activity of hydro-alcoholic (HAEAM) and ethyl acetate (EAEAM) extracts of Aegle marmelos leaves were evaluated against nephrotoxicity induced by cisplatin (CP), a widely used chemotherapeutic agent in cancer therapy. Wistar rats were treated with CP (6 mg.kg-1 ; i.p.). Treatment groups received the same dose of CP, along with HAEAM and EAEAM (200 and 400 mg. kg-1) orally for 5 d. Blood urea nitrogen (BUN), serum creatinine, and antioxidant enzymes were estimated in renal tissues. EAEAM exhibited minimum IC 50 values 6.13 ± 1.05, 67.34 ± 1.7, 59.7 ± 3.9, and 49.17 ± 2.19 μg.mL-1. EAEAM (400 mg.kg-1) decreased the creatinine levels from 2.29 ± 0.387 to 0.96 ± 0.095 mg.dL-1 and BUN from 92.06 ± 7.949 to 38.18 ± 5.686 mg.dL-1 and restored the activities of renal antioxidant enzymes, decreased the lipid peroxidasde (LPO) levels from 158.70 ± 3.542 to 106.91 ± 5.876 nM.g-1 , and increased superoxide dismutase (SOD) levels from 12.59 ± 0.463 to 29.95 ± 5.222 U.g-1 , glutathione (GSH) from 0.24 ± 0.029 to 0.57 ± 0.048 μM.g-1 , and catalase (CAT) from 1.14 ± 0.067 to 3.27 ± 0.296 U.mg-1).
Alzheimer’s disease (AD), the most widespread cause of dementia is delineated by progressive cogn... more Alzheimer’s disease (AD), the most widespread cause of dementia is delineated by progressive cognitive impairment in the elderly people. During its progression, N-Methyl-D-Aspartate receptor antagonists are known to play a key role in the mechanisms of learning and memory. Extensive side effects alongside other effects on learning and memory have limited the therapeutic significance of various blockers and antagonists of the NMDA receptor. In this study, we identify potential compounds targeted against NMDA. In order to reveal the essential structural features for NMDA receptor, three-dimensional pharmacophore models are constructed based on a set of known NMDA inhibitors. This is followed by virtual screening which results in novel chemical compounds having the potential to inhibit NMDA. The lead compounds are then subjected to molecular docking and assessed by a scoring function, which results in two compounds with high Libdock scores. These compounds also show interactions with i...
Letters in Drug Design & Discovery
Background: Alzheimer’s disease is a medical condition with detrimental brain health. It is major... more Background: Alzheimer’s disease is a medical condition with detrimental brain health. It is majorly diagnosed in aging individuals plaque in β) characterized by accumulated Amyloidal beta (A 1 BACE) 1 secretase APP cleavage enzyme βneurological areas. The ) is the target of choice that can be exploited to find drugs against Alzheimer’s disease. Methods: A series of BACE-1 inhibitors with reported binding constant were considered for the development of a feature based pharmacophore model. Results: The good correlation coefficient (r=0.91) and RMSD of 0.93 was observed with 30 compounds in training set. The model was validated internally (r2test=0.76) as well as externally by Fischer validation. The pharmacophore based virtual screening retrieved compounds that were docked and biologically evaluated. Conclusion: The three structurally diverse molecules were tested by in-vitro method. The pyridine derivative with highest fit value (6.9) exhibited IC50 value of 2.70 µM and thus was foun...
Oriental Pharmacy and Experimental Medicine
Journal of Microencapsulation
International Journal of Polymeric Materials and Polymeric Biomaterials
Journal of Microbiological Methods
Journal of Traditional and Complementary Medicine
Current Computer-Aided Drug Design
Background: : Rho-kinase is an essential downstream target of GTP-binding protein RhoA, and plays... more Background: : Rho-kinase is an essential downstream target of GTP-binding protein RhoA, and plays a crucial role in the calcium-sensitization pathway. Rho-kinase pathway is critically involved in phosphorylation state of myosin light chain, leading to increased contraction of smooth muscles. Inhibition of this pathway has turned out to be a promising target for several indications such as cardiovascular diseases, glaucoma and inflammatory diseases. Methods:: The present work focuses on a division-based 2D quantitative structure-activity relationship (QSAR) analysis along with a docking study to predict structural features that may be essential for the enhancement of selectivity and potency of the target compounds. Furthermore, a set of indoles and azaindoles were also projected based on the regression equation as novel developments. Molecular docking was applied for exploring the binding sites of the newly predicted set of compounds with the receptor. Results: : Results of the docke...
International Journal of PharmTech Research
Background: Immediate release formulation of Hydrochlorothiazide is available in market. Cmax ach... more Background: Immediate release formulation of Hydrochlorothiazide is available in market. Cmax achieved at 2 h, duration of action persist for 6-12 h, resulting in multiple dosing to maintain plasma concentration and in vivo activity. Objective: The objective of research work was to design modified release tablets of Hydrochlorothiazide 25 mg with the intention of once a day dosing. Cmax will achieve after 10 to 12 h of administration. This controlled release will constantly induce diuretic activity for whole night and day especially during early morning hours, resulting in decreased blood volume, reduced cardiac output and controlled blood pressure. When patient awakes up in morning, blood pressure will be comparatively low thus reducing the frequency of cardiac arrest.Method: Here an attempt has been made to kinetically calculate required in-vitro dissolution profile by deconvolution method using Wagner-nelson equation. Plasma concentration time profile of immediate release tablet 12.5 mg is available in literature and that of modified release formulation 25 mg is calculated such that Area under curve of modified release tablet matches with that of two immediate release tablets of 12.5 mg along with Cmax and Kel, thus meeting the criteria for bio-equivalency. Tmax will be delayed from 2 h to approximately 10 h. Results: In-vivo dissolution profile is calculated from the equation of "fraction of drug absorbed". Perfect IVIVC is matched when value of slope is 1, intercept is 0 and correlation coefficient (R 2) 0.99. Conclusion: This in-vitro profile will be used further to develop modified release formulation.
Scientific reports, Jan 2, 2018
In view of the role of sEH (soluble epoxide hydrolase) in hypertension, we have developed a rigor... more In view of the role of sEH (soluble epoxide hydrolase) in hypertension, we have developed a rigorously validated pharmacophore model containing one HBA (Hydrogen Bond Acceptor), two HY (Hydrophobic) and one RA (Ring Aromatic) features. The model was used as a query to search the NCI (National Cancer Institute) and Maybridge database leading to retrieval of many compounds which were sorted on the basis of predicted activity, fit value and Lipinski's violation. The selected compounds were docked into the active site of enzyme soluble epoxide hydrolase. Potential interactions were observed between the features of the identified hits and the amino acids present in the docking site. The three selected compounds were subjected to in vitro evaluation using enzyme- based assay and the isolated rat aortic model followed by cytotoxicity studies. The results demonstrate that the identified compounds are potent, safe and novel soluble epoxide hydrolase inhibitors.
Current clinical pharmacology, Jan 25, 2018
Computer has wide applicability in many field, and in pharmaceutical science the computer play a ... more Computer has wide applicability in many field, and in pharmaceutical science the computer play a crucial role as a commander of all the theoretical aspects and provide a workbench to improve the overall quality system of the pharmaceutical research and development. The aim of this article is to provide computational approach in development of the many booming technology of computer software in the field of clinical pharmacokinetics. The computational technique practiced by clinical pharmacist and scientist with the applied knowledge and skills of dealing with clinical pharmacokinetics problems, which can be applied in routine clinical practices. Methods used to distinguish the pharmacokinetics (PK) and pharmacodynamics (PD) analysis software has evolved greatly in recent years, allowing users to focus on analysis. Clinical pharmacokinetics software like Population pharmacokinetics, Individual pharmacokinetics, ADME pharmacokinetics, in - silico pharmacokinetics like WinNonlin, SAS, ...
Journal of Heterocyclic Chemistry
Therapeutic drug monitoring, Jan 6, 2018
Therapeutic drug monitoring (TDM) of anti-epileptic drugs provides a valid clinical tool in optim... more Therapeutic drug monitoring (TDM) of anti-epileptic drugs provides a valid clinical tool in optimization of overall therapy. However, TDM is challenging due to the high biological samples (plasma/blood) storage/shipment costs and the limited availability of laboratories providing TDM services. Sampling in the form of dry plasma spot (DPS) or dry blood spot (DBS) is a suitable alternative to overcome these issues. An improved, simple, rapid, and stability indicating method for quantification of pregabalin in human plasma and DPS has been developed and validated. Analyses were performed on liquid chromatography tandem mass spectrometer under positive ionization mode of electrospray interface. Pregabain-d4 was used as internal standard, and the chromatographic separations were performed on Poroshell 120 EC-C18 column using an isocratic mobile phase flow rate of 1 mL/min. Stability of pregabalin in DPS was evaluated under simulated real-time conditions. Extraction procedures from plasma...