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1.
J Cardiovasc Pharmacol Ther ; 24(6): 499-508, 2019 11.
Article in English | MEDLINE | ID: mdl-31284744

ABSTRACT

The role of oral anticoagulants (OAC) in atrial fibrillation (AF) is well established. However, none of the randomized controlled trials included patients with end-stage renal disease (ESRD) leaving a lack of evidence in this large, challenging and unique patient group. Patients on hemodialysis (HD) with AF have additional risk factors for stroke due to vascular comorbidities, HD treatment, age, and diabetes. Conversely, they are also at increased risk of major bleeding due to uremic platelet impairment. Anticoagulants increase bleeding risk in patients with ESRD and HD up to 10-fold compared with non chronic kidney disease (CKD) patients on warfarin. There are conflicting data and recommendations regarding use of OACs in ESRD which will be reviewed in this article. We conclude by proposing a modified strategy for OAC use in ESRD based on the latest evidence.


Subject(s)
Anticoagulants/administration & dosage , Antithrombins/administration & dosage , Atrial Fibrillation/drug therapy , Kidney Failure, Chronic/physiopathology , Kidney/physiopathology , Stroke/prevention & control , Warfarin/administration & dosage , Administration, Oral , Anticoagulants/adverse effects , Antithrombins/adverse effects , Atrial Fibrillation/diagnosis , Atrial Fibrillation/mortality , Atrial Fibrillation/physiopathology , Clinical Decision-Making , Hemorrhage/chemically induced , Humans , Kidney Failure, Chronic/diagnosis , Kidney Failure, Chronic/mortality , Patient Selection , Practice Guidelines as Topic , Risk Assessment , Risk Factors , Stroke/diagnosis , Stroke/mortality , Stroke/physiopathology , Treatment Outcome , Warfarin/adverse effects
2.
Curr Clin Pharmacol ; 13(2): 128-135, 2018.
Article in English | MEDLINE | ID: mdl-29521214

ABSTRACT

OBJECTIVE: The aim of present research work was to develop a herbal fast disintegrating tablet containing Fagonia schweinfurthii Hadidi dried extract and determining its antihistaminic activity using guinea pig ileum. METHOD: The tablets were formulated by wet granulation technique using three different superdisintegrants (croscarmillose, crospovidone and sodium starch glycolate) at three different levels. The tablets were evaluated for various physical properties like hardness, friability weight variation etc. and various mechanical properties like disintegration time, wetting time to select the best superdisintegrant. The selected superdisintegrant was further used as intra as well as extra granulating agent to develop fast disintegrating tablets of Fagonia schweinfurthii Hadidi dried extract. The optimized formulation was subjected to stability study as per the ICH guidelines. Finally, Ex-vivo antihistaminic study was conducted on guinea pig ileum for optimized formulation and compared with marketed tablet containing cetrizine HCl as API (Stanhist-10, Ranbaxy, Pvt. Ltd). RESULTS: Physical properties of all tablet batches were found to be acceptable and comply with various official specifications. The disintegration time and wetting time of optimized formulation (F'3) were found to be 1.15±0.08 and 0.56±0.04 min respectively. Results of Ex-vivo study showed a comparable histamine inhibition between optimized tablet (15%) and marketed tablet formulation (18.8%) in a dose of 5 µg/ml. CONCLUSION: On the basis of in-vitro and Ex-vivo studies, it was concluded that prepared herbal fast disintegrating tablets were stable and had potent antihistaminic activity.


Subject(s)
Chemistry, Pharmaceutical/methods , Histamine Antagonists/chemistry , Histamine Antagonists/pharmacokinetics , Ileum/drug effects , Plant Preparations/chemistry , Plant Preparations/pharmacokinetics , Animals , Drug Compounding , Guinea Pigs , Hardness , Histamine Antagonists/isolation & purification , Ileum/metabolism , Organ Culture Techniques , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plant Extracts/pharmacokinetics , Plant Preparations/isolation & purification , Solubility , Tablets , Time Factors
3.
J Am Coll Cardiol ; 67(6): 674-683, 2016 Feb 16.
Article in English | MEDLINE | ID: mdl-26868693

ABSTRACT

BACKGROUND: Radiofrequency catheter ablation is used to treat recurrent ventricular tachycardia (VT). OBJECTIVES: This study evaluated long-term safety and effectiveness of radiofrequency catheter ablation using an open-irrigated catheter. METHODS: Patients with sustained monomorphic ventricular tachycardia associated with coronary disease were analyzed for cardiovascular-specific adverse events within 7 days of treatment, hospitalization duration, 6-month sustained monomorphic ventricular tachycardia recurrence, quality of life measured by the Hospital Anxiety and Depression Scale, long-term (1-, 2-, and 3-year) survival, symptomatic VT control, and amiodarone use. RESULTS: Overall, 249 patients, mean age 67.4 years, were enrolled. The cardiovascular-specific adverse events rate was 3.9% (9 of 233) with no strokes. Noninducibility of targeted VT was achieved in 75.9% of patients. Post-ablation median hospitalization was 2 days. At 6 months, 62.0% (114 of 184) of patients had no sustained monomorphic ventricular tachycardia recurrence; the proportion of patients with implantable cardioverter-defibrillator shocks decreased from 81.2% to 26.8% (p < 0.0001); the frequency of VT in implantable cardioverter-defibrillator patients with recurrences was reduced by ≥50% in 63.8% of patients; and the proportion with normal Hospital Anxiety and Depression Scale scores increased from 48.8% to 69.1% (p < 0.001). Patient-reported VT remained steady for 1, 2, and 3 years at 22.7%, 29.8%, and 24.1%, respectively. Amiodarone use and hospitalization decreased from 55% and 77.2% pre-ablation to 23.3% and 30.7%, 18.5% and 36.7%, 17.7% and 31.3% at 1, 2, and 3 years, respectively. CONCLUSIONS: Radiofrequency catheter ablation reduced implantable cardioverter-defibrillator shocks and VT episodes and improved quality of life at 6 months. A steady 3-year nonrecurrence rate with reduced amiodarone use and hospitalizations indicate improved long-term outcomes. (NaviStar ThermoCool Catheter for Endocardial RF Ablation in Patients With Ventricular Tachycardia [THERMOCOOL VT]; NCT00412607).


Subject(s)
Catheter Ablation/methods , Heart Rate/physiology , Tachycardia, Ventricular/surgery , Adult , Aged , Aged, 80 and over , Catheter Ablation/instrumentation , Device Approval , Equipment Design , Female , Follow-Up Studies , Humans , Male , Middle Aged , Prospective Studies , Quality of Life , Recurrence , Retrospective Studies , Tachycardia, Ventricular/physiopathology , Therapeutic Irrigation/methods , Time Factors , Treatment Outcome
4.
Springerplus ; 4: 96, 2015.
Article in English | MEDLINE | ID: mdl-25763306

ABSTRACT

UNLABELLED: Whether sex affects the acute phase of myocardial ischemia in experimental animal models is currently being debated. Our purpose was to determine if sex influences either the incidence or severity of reperfusion-induced arrhythmias resulting from a brief coronary occlusion. Male and female Sprague-Dawley rats were assigned to the study. Anesthetized animals were subjected to a 5-minute coronary artery occlusion followed by 5 minutes of reperfusion. Mortality differed by sex: 10/27 (37%) of males died due to VT/VF while only 1/16 females (6%) died due to VT/VF (p = 0.033). Quantitative analysis of the electrocardiogram was performed on data acquired from 17 male and 15 female survivors. Analysis showed no other significant differences in ventricular arrhythmias between the two groups. CONCLUSION: Lethal reperfusion-induced arrhythmias led to a higher mortality in male rats versus female rats. Among survivors there was no difference in any other arrhythmic parameters measured.

5.
Article in English | MEDLINE | ID: mdl-25403255

ABSTRACT

The mutual prodrugs of aceclofenac with various naturally available antioxidants; menthol, thymol, eugenol, guiacol and vanillin have been synthesized by the DCC coupling method, purified and characterized by spectral data, as well as, partition coefficient, solubility and hydrolytic studies. The title compounds have more lipophilic character as compared to the parent moieties and good stability in acidic environment, which is prerequisite for the oral absorption of the drug. Under gastric as well as intestinal pH conditions these prodrugs showed variable susceptibility towards hydrolysis. The synthesized derivatives were evaluated for antiinflammatory, analgesic activities and ulcerogenic potential. Prodrug showed improved solubility in organic solvents, which implies lipophilic character of ester prodrugs and were also found to be chemically stable in acidic environment. The aceclofenac mutual prodrugs showed improved analgesic and anti-inflammatory activities with reduced ulcerogenicity.


Subject(s)
Analgesics/chemical synthesis , Analgesics/pharmacology , Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Anti-Inflammatory Agents/chemical synthesis , Anti-Inflammatory Agents/pharmacology , Diclofenac/analogs & derivatives , Prodrugs/chemical synthesis , Prodrugs/pharmacology , Acetic Acid , Analgesics/toxicity , Animals , Anti-Inflammatory Agents/toxicity , Anti-Inflammatory Agents, Non-Steroidal/toxicity , Carrageenan , Diclofenac/chemical synthesis , Diclofenac/pharmacology , Diclofenac/toxicity , Disease Models, Animal , Drug Design , Drug Stability , Edema/chemically induced , Edema/prevention & control , Female , Hydrogen-Ion Concentration , Hydrolysis , Kinetics , Male , Mice , Pain/chemically induced , Pain/prevention & control , Prodrugs/toxicity , Rats, Wistar , Risk Assessment , Solubility , Stomach Ulcer/chemically induced , Stomach Ulcer/pathology
6.
Pak J Pharm Sci ; 27(5): 1175-82, 2014 Sep.
Article in English | MEDLINE | ID: mdl-25176375

ABSTRACT

This study was designed to perform the physicochemical and phytochemical standardization with HPTLC fingerprinting of Nigella sativa seeds in order to establish the standard pharmacognostical parameters of this miracle herb. Different parameters like extractive values; total ash value, acid insoluble ash value and water soluble ash value, moisture content, loss on drying, pH values of Nigella sativa seeds were performed. Preliminary phytochemical screening was done to detect different phytoconstituents by using the Harborne's phytochemical methods. Quantification of phenolic and flavonoid contents, determination of pesticides residues, aflatoxin and heavy metals were also carried out. HPTLC fingerprinting of methanolic extract was performed using CAMAG-HPTLC system connected with win CAT software. Preliminary phytochemical screening of the extracts in different solvent revealed the presence of carbohydrates, phenolic compounds, flavonoids, alkaloids, proteins, saponins, lipids, sterols and tannins. Total flavonoid and phenolic contents in methanolic extract was found to be 1.4 mg/gm and 9.8 mg/gm extract respectively. Concentrations of heavy metals were found within acceptable limits. Pesticides residues and aflatoxins were not detected. The physicochemical and phytochemical standards along with HPTLC fingerprint profile established as an outcome of this research may be utilized as substantial data for identification, purification and standardization of Nigella sativa seeds.


Subject(s)
Chromatography, Thin Layer/methods , Nigella/chemistry , Aflatoxins/analysis , Flavonoids/analysis , Metals, Heavy/analysis , Pesticide Residues/analysis , Plant Extracts/analysis , Seeds/chemistry
7.
Pharm Biol ; 52(6): 745-9, 2014 Jun.
Article in English | MEDLINE | ID: mdl-24417586

ABSTRACT

CONTEXT: Many synthetic antidiabetic components show toxic and/or mutagenic effects. Hence, attention has been given to naturally occurring antidiabetic components. Identification of effective antidiabetic components from plants origin is an ideal strategy for new drug development. The fresh root, bark, and leaves of Salvadora persica L. (Salvadoraceae) have been used in folk medicine for the treatment of a wide range of medical problems such as cough, asthma, scurvy, piles, rheumatism, leprosy, and gonorrhea disorders. OBJECTIVE: The S. persica root extract was investigated for the reduction of the risk of diabetes in diabetic rats. MATERIAL AND METHODS: The hydro-alcoholic root extract, 200 and 400 mg/kg, was fed to streptozotocin-induced diabetic rats for 21 d. Blood serum glucose, lipid profile, body weight, and food intake were monitored at 0, 7, 14, and 21 d after induction of diabetes. RESULTS: S. persica hydro-alcoholic root extract was not toxic at doses up to 1200 mg/kg. Significant reduction of blood glucose and lipid profile in diabetic rats treated with 400 mg/kg hydro-alcoholic root extract after 21 d versus diabetic control and glibenclamide-treated rats. The glibenclamide and root extract-treated group's peak values of blood glucose significantly decreased from 281.50 to 106 mg/dL and 285.50 to 150.25 mg/dL, respectively. Hence, in this study, observations showed that root hydro-alcoholic reduced the blood glucose level in diabetic rats but values did not return to normal controls. CONCLUSION: The research suggests that the root extract was significantly effective when compared with control and standard in the treatment of hyperlipidemia and hyperglycemia in diabetic rats. Therefore, it may be beneficial to diabetic patients.


Subject(s)
Diabetes Mellitus, Experimental/drug therapy , Hyperlipidemias/drug therapy , Hypoglycemic Agents/therapeutic use , Hypolipidemic Agents/therapeutic use , Plant Extracts/therapeutic use , Salvadoraceae , Animals , Blood Glucose/drug effects , Blood Glucose/metabolism , Diabetes Mellitus, Experimental/blood , Diabetes Mellitus, Experimental/chemically induced , Hyperlipidemias/blood , Hypoglycemic Agents/isolation & purification , Hypoglycemic Agents/pharmacology , Hypolipidemic Agents/isolation & purification , Hypolipidemic Agents/pharmacology , Plant Extracts/isolation & purification , Plant Extracts/pharmacology , Plant Roots , Rats , Rats, Wistar , Streptozocin/toxicity , Treatment Outcome
8.
Europace ; 16(7): 1007-14, 2014 Jul.
Article in English | MEDLINE | ID: mdl-24446509

ABSTRACT

AIMS: The step-wise approach to catheter ablation for persistent atrial fibrillation (AF) requires considerable substrate modification targeting at complex fractionated atrial electrograms (CFAEs) in addition to pulmonary vein (PV) isolation. An alternative strategy that minimizes the amount of ablation would be desirable. The aim of this study was to investigate whether the use of pre-procedural amiodarone affects: (i) the amount of ablation required to achieve procedural success, and (ii) long-term outcomes. METHODS AND RESULTS: We studied 121 consecutive patients with persistent AF who underwent catheter ablation. The patients were divided into two groups: Group 1, amiodarone (n = 31); Group 2, other antiarrhythmic drugs or rate control (n = 90). All the patients underwent a step-wise ablation procedure beginning with PV isolation, then proceeding with ablation of the CFAEs and linear lesions until sinus rhythm was achieved. Mean left atrial cycle length of AF (AFCL) was recorded at each step. The number of CFAE ablation sites was recorded. The number of CFAE sites in Group 1 was significantly less than that in Group 2 (P = 0.0121). The AFCLs after each step in Group 1 were significantly longer than those in Group 2. The procedure time and the radiofrequency time of CFAE ablation in Group 1 were significantly shorter than that in Group 2 (P = 0.0276 and P = 0.0458, respectively). There was no significant difference between the two groups in early and long-term outcomes. CONCLUSION: Use of pre-procedural amiodarone prolongs AFCL during catheter ablation and reduces the number of CFAE sites requiring ablation to achieve procedural success while maintaining equivalent long-term results.


Subject(s)
Amiodarone/therapeutic use , Anti-Arrhythmia Agents/therapeutic use , Atrial Fibrillation/therapy , Catheter Ablation , Operative Time , Pulmonary Veins/drug effects , Aged , Amiodarone/adverse effects , Anti-Arrhythmia Agents/adverse effects , Atrial Fibrillation/diagnosis , Atrial Fibrillation/physiopathology , Catheter Ablation/adverse effects , Combined Modality Therapy , Electrophysiologic Techniques, Cardiac , Female , Humans , Male , Middle Aged , Pulmonary Veins/physiopathology , Retrospective Studies , Time Factors , Treatment Outcome
9.
Drug Dev Ind Pharm ; 40(4): 568-76, 2014 Apr.
Article in English | MEDLINE | ID: mdl-23547761

ABSTRACT

UNLABELLED: Abstract Context: The vesicles based on skin lipid have a drug localization effect and its main lipid, ceramide provides protective and regenerative effects while oleic acid (OA) is a penetration enhancer, however, it causes slight irritation, so we have formulated formulation incorporating both of these to develop a transdermal formulation for better permeation. OBJECTIVE: Present study investigated the preparation and characterization of physicochemical properties and permeation of nanovesicles of ceramide-2 containing OA and palmitic acid (PA) respectively and a commercial gel. MATERIALS AND METHODS: The vesicles were made using ceramide 2, cholesterol (Chol), cholesteryl sulfate (CS) and OA or PA, respectively, using film hydration method. The vesicles were characterized for physicochemical properties, ex vivo permeation using human skin and pharmacokinetic parameters and anti-inflammatory activity in rats. RESULTS: The vesicles showed size at 102-125 nm while PDI was 0.11-0.13 and negative zeta potential. OV-3 showed highest entrapment efficiency. The drug fluxes were 92.02 and 8.920 µg/cm(2)/h, respectively, for OV-3 and PV-1. The Cmax were 7.91 and 4.01 µg/ml at 4 and 6 h for OV-3 (2.5 mg) and PV-1 (10 mg), respectively. OV-3 and PV-1 showed 98.8% and 77.36% edema inhibition, respectively, at 3 h. DISCUSSION: Both formulations showed similar physical parameters and different permeation since OA get incorporated in vesicles and increases its permeability and ceramide makes sure that vesicles can rapidly traverse the stratum corneum. CONCLUSION: OV-3 containing 3% OA showed optimum physical parameters and good permeation with maximum anti-inflammatory activity.


Subject(s)
Ceramides/chemistry , Diclofenac/administration & dosage , Drug Delivery Systems , Excipients/chemistry , Administration, Cutaneous , Animals , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Chemistry, Pharmaceutical/methods , Diclofenac/pharmacokinetics , Diclofenac/pharmacology , Disease Models, Animal , Humans , Inflammation/drug therapy , Inflammation/pathology , Male , Nanoparticles , Oleic Acid/chemistry , Palmitic Acid/chemistry , Particle Size , Rats , Rats, Wistar , Skin Absorption
10.
Pharm Biol ; 52(3): 298-307, 2014 Mar.
Article in English | MEDLINE | ID: mdl-24107271

ABSTRACT

CONTEXT: Desmostachya bipinnata (L.) Stapf [Gramineae (Poaceae)] has been traditionally used to treat various disorders such as asthma, kidney stone, diarrhea, wound healing, etc. OBJECTIVE: The present study involves pharmacognostic, botanical, and preliminary phytochemical examination of various plant parts and powders of D. bipinnata. MATERIALS AND METHODS: Leaves, stem, roots, underground and aerial part powders were microscopically examined. Pharmacognostic standardization parameters were determined as per the WHO guidelines. Parameters, including extractive value in different solvents, ash values, and loss on drying, were determined. Preliminary phytochemical studies, fluorescence analysis, and chromatographic profiling were performed for the correct identification of this crude drug and some of its phytoconstituents. RESULTS: Microscopical studies showed various characteristic features including, collateral vascular bundle, bundle sheath cells, and bulliform cells in leaf, conjoint, collateral and closed vascular bundles, and sclerenchymatous sheath in stem; and silica bodies in root. Phytochemical screening and chromatographic profile of aerial plant parts revealed the presence of alkaloids, tannins, flavonoids, steroids, glycosides, and coumarins. Underground plants parts indicated the presence of glycosides, steroids, flavonoids, coumarins, and alkaloids. DISCUSSION AND CONCLUSION: The results of the performed studies are helpful in correct identification, characterisation of D. bipinnata. Preliminary phytochemical studies and chromatographic profiling may be helpful in further isolation and purification of lead compounds from different extracts.


Subject(s)
Plant Extracts/chemistry , Poaceae/chemistry , Chromatography/methods , Guidelines as Topic , Microscopy , Plant Components, Aerial , Plant Extracts/isolation & purification , Plant Roots , World Health Organization
11.
Artif Cells Nanomed Biotechnol ; 42(5): 323-30, 2014 Oct.
Article in English | MEDLINE | ID: mdl-23944163

ABSTRACT

CONTEXT: Ibuprofen is an important NSAID, however, it can cause GI disturbances when given orally, and employment of transdermal route will require permeation enhancer causing skin injury. OBJECTIVE: Drug-loaded nanovesicles of ceramide-2, cholesterol, palmitic acid, and cholesteryl sulfate (ICVG) were formulated and analyzed for physicochemical and permeation properties. MATERIALS AND METHOD: Vesicles were formulated using film hydration method and physicochemical parameters, in vitro drug release, and stability were assessed. Further, nanovesicle gels were evaluated against plain gel containing drug (CG) for ex vivo/in vivo drug permeation and anti-inflammatory activity. RESULTS: The developed formulations showed optimal physicochemical profile and ICV-1 gave 97.24% drug release. Drug permeation was between 17.32 and 33.12 µg/cm(2) for ICVG formulations and 0.27 µg/cm(2) for CG. ICVG-1 and CG showed Cmax of 9.6 and 0.7 µg/ml at 8 and 4 h. ICVG-1 showed 19.9 times higher AUC than CG. Edema inhibition was 57.98% during initial hours by ICVG-1. DISCUSSION: Ratio of ceramide 2 and palmitic acid plays a critical role in drug permeation through stratum corneum. The stability and protective effect of the formulations were due to ceramide content. CONCLUSION: The composition has an important role in physicochemical properties and drug permeation thereby generating an optimum formulation.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/metabolism , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Ceramides/chemistry , Chemical Phenomena , Ibuprofen/metabolism , Ibuprofen/pharmacology , Nanostructures/chemistry , Administration, Cutaneous , Animals , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Chemistry, Pharmaceutical , Drug Liberation , Humans , Ibuprofen/administration & dosage , Ibuprofen/chemistry , Male , Membranes, Artificial , Permeability , Rats , Skin/metabolism
12.
Pharm Dev Technol ; 19(1): 48-54, 2014 Feb.
Article in English | MEDLINE | ID: mdl-23281714

ABSTRACT

CONTEXT: Transdermal formulations contain permeation enhancer which causes skin damage. Ceramide 2 is natural lipid found in stratum corneum (SC). OBJECTIVE: Drug-loaded nanovesicles of ceramide-2, cholesterol, palmitic acid, cholesteryl sulfate were formulated and analyzed for physical and biological properties. Diclofenac was used as a model drug. MATERIALS AND METHOD: The vesicles were prepared using the film hydration method and characterized for physical parameters, in vitro drug release, accelerated stability studies and formulated into gel. Respective gels were compared with a commercial formulation (CEG) and plain carbopol gel (CG) containing drug for ex vivo, in vivo drug permeation and anti-inflammatory activity. RESULTS: The vesicles were stable with optimum physical parameters. DCG-1 showed 92.89% in vitro drug release. Ceramide vesicles showed drug release between 18 and 25 µg/cm(2) whereas CG and CEG released 0.33 and 1.35 µg/cm(2) drug, respectively. DCG-1 and CEG showed corresponding Cmax at 6 and 4 h, respectively. DCG-1 showed six times AUC than CEG. DCG-1 inhibited edema by 86.37% by 4th hour of application. DISCUSSION: The presence of ceramide 2 specifically promotes the drug permeation through SC and dermis and also contribute towards stability and non-irritancy. CONCLUSION: The composition of the nanovesicle played an important role in physical properties and drug permeation.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Ceramides/chemistry , Diclofenac/administration & dosage , Nanocapsules/chemistry , Skin Absorption , Administration, Cutaneous , Animals , Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Cholesterol/chemistry , Cholesterol Esters/chemistry , Diclofenac/pharmacokinetics , Diclofenac/pharmacology , Male , Palmitic Acid/chemistry , Rats , Rats, Wistar , Skin/drug effects , Skin/metabolism , Skin Irritancy Tests
13.
Artif Cells Nanomed Biotechnol ; 42(5): 296-301, 2014 Oct.
Article in English | MEDLINE | ID: mdl-23865793

ABSTRACT

Lipid vesicles are an important drug carrier which can serve for controlled delivery of drugs; however, these vesicles are quite unstable at ambient temperature and require stringent storage condition. Present work was done to develop a stable vesicular system for drug delivery. Vesicles of ceramide-2, cholesterol, cholesterol sulfate, and palmitic acid were prepared and compared with phosphatidylcholine vesicles for physicochemical parameters and accelerated stability. Diclofenac sodium was used as a model drug. Based on physicochemical parameter and in vitro release PCV-3 and CV-3 were selected for further studies in three different accelerated stability conditions. PCV-3 showed moderate changes at 4°C but was severely affected at 25°C and 40°C. CV-3 showed stable characteristics at 4°C and 25°C whereas at 40°C, CV-3 showed signs of slight modification owing to moisture absorption. Based on the study, CV-3 containing highest content of palmitic acid was found to be most stable.


Subject(s)
Liposomes/chemistry , Nanostructures/chemistry , Chemistry, Pharmaceutical , Diclofenac/chemistry , Drug Liberation , Drug Stability , Phosphatidylcholines/chemistry
14.
Am Heart J ; 166(2): 381-387.e8, 2013 Aug.
Article in English | MEDLINE | ID: mdl-23895823

ABSTRACT

BACKGROUND: The Atrial Fibrillation Effect on QualiTy of Life (AFEQT) questionnaire is a novel quality of life (QOL) measure previously shown to be valid, reliable, and sensitive to clinical change in patients with atrial fibrillation (AF). The clinical relevance of a given change in the score is not known. The most useful "anchor" for a measure of meaningful change in QOL is patient-reported magnitude of change. OBJECTIVE: The aim of this study was to define the interpretability of changes in the AFEQT score from the patients' perspective. METHODS: With the use of the original validation study of AFEQT, in which 210 patients completed the questionnaire at baseline and at 3 months, we estimated the AFEQT score corresponding to a meaningful improvement in QOL using the patients' assessments of global change in QOL, AF symptoms from the Atrial Fibrillation Severity Scale (AFSS), and physicians' assessment of global QOL over the 3 months, as anchors. RESULTS: In patients with a moderate improvement in global QOL, the AFEQT scores increased from 51.9 ± 21.8 to 70.8 ± 17.4 (an increase of 18.9 ± 20.7), compared with an increase of 6.9 ± 16.9 units in patients with "unimportant change" in global QOL. Physicians' global assessment yielded a similar change in AFEQT score corresponding to a moderate change in global QOL (21.3 ± 20.2 units). Patients with moderate improvement in AF symptom severity using the AFSS scale had an increase of 17.9 ± 11.8 units on the AFEQT scale. A change in 19 units in the AFEQT score corresponded to a 0.9 SD unit change or greater than a minimal important difference from a distribution based method. CONCLUSIONS: A meaningful improvement in QOL in patients with AF can be measured from a change in the AFEQT score. These results can assist in monitoring patient progress and interpreting the effects of interventions in patients with AF.


Subject(s)
Atrial Fibrillation , Quality of Life , Surveys and Questionnaires , Aged , Female , Humans , Male , Middle Aged , Socioeconomic Factors
15.
J Res Pharm Pract ; 2(3): 123-9, 2013 Jul.
Article in English | MEDLINE | ID: mdl-24991619

ABSTRACT

OBJECTIVE: The main objective of this study was to assess the effects of pharmaceutical care interventions in patients with essential hypertension in Lakshmi Pat Singhania Institute of Cardiology, Kanpur, India. METHODS: The study was carried out from July 2010 to August 2011. Pharmaceutical care was provided for 54 patients (intervention group) which was comprised of the patient education, the prescription assistance and the life style modifications and motivation for health. Then the clinical outcome as well as health related quality of life (HRQOL) were compared with the control group (48 patients) in which the pharmaceutical care was not provided. Furthermore, the effect of pharmaceutical care intervention on HRQOL was assessed using Short Form-36 (SF-36), a general health related quality of life questionnaire used to evaluate the QOL of patients. Blood pressure (BP) measurements and QOL survey was performed at baseline and at the follow-up session. FINDINGS: The difference between blood pressure readings from the baseline to the second follow-up was significant for systolic [(P = 0.0001), 12.24 mmHg] and diastolic BP [(P = 0.001), 5.17 mmHg] in the intervention group. The questionnaire used to evaluate the QOL of patients also showed improvement in the mean score for intervention group. CONCLUSION: Results from our study showed that applying pharmaceutical care to hypertensive patients can help in the control of these patients' blood pressure, and consequently lower the risk that hypertension poses in cardiovascular disease. Successful implementation of pharmaceutical care has the potential to increase patients' satisfaction with their pharmacists' activities and may increase patients' expectations that pharmacists will work on their behalf to assist them with their healthcare needs.

16.
J Cardiovasc Electrophysiol ; 23(12): 1374-83, 2012 Dec.
Article in English | MEDLINE | ID: mdl-23134527

ABSTRACT

INTRODUCTION: The effect of remote ischemic preconditioning (RIPC) on arrhythmias in in vivo models is unknown. Our purpose was to determine effects of both acute and delayed RIPC on arrhythmias. METHODS AND RESULTS: In the acute protocol anesthetized open chest rats were exposed to 5 minutes of proximal left coronary artery occlusion (CAO) and 10 minutes of reperfusion. Rats were either untreated (ischemia/reperfusion, IR group, n = 17) or received RIPC (n = 14) with 5 minutes bilateral femoral occlusions followed by 5 minutes of reperfusion times 3, started 30 minutes before CAO. At reperfusion, onset of ventricular tachycardia (VT) was delayed in RIPC group (25.7 seconds) versus IR (8.8 seconds; P = 0.04). Number of episodes of VT was 17.0 in IR versus 3.0 in the RIPC group (P = 0.01) and duration of VT was 54.1 seconds in IR versus 4.9 seconds in RIPC (P = 0.019). Number of ventricular premature complexes (VPC) was 26.0 in IR and 10.0 in RIPC rats (P = 0.04). Levels of reperfusion injury salvage kinases (RISK), that is, phospho-Akt and phospho-p70S6 in the risk area of IR and RIPC hearts were similarly higher compared to the nonischemic areas both at 1 and 10 minutes into reperfusion. Delayed RIPC was induced on day 1 and on day 2, myocardial IR was induced. Delayed RIPC did not affect VT or VPC. CONCLUSION: Acute RIPC of the lower limbs induced a powerful delay in/and reduction in IR induced ventricular arrhythmias, but without evoking the RISK pathway; a late protective phase of RIPC on arrhythmias did not occur.


Subject(s)
Heart Rate , Heart Ventricles/physiopathology , Ischemic Preconditioning/methods , Myocardial Reperfusion Injury/complications , Myocardial Reperfusion Injury/physiopathology , Ventricular Fibrillation/etiology , Ventricular Fibrillation/physiopathology , Animals , Female , Myocardial Reperfusion Injury/prevention & control , Rats , Rats, Sprague-Dawley , Treatment Outcome , Ventricular Fibrillation/prevention & control
17.
J Ayurveda Integr Med ; 3(2): 80-4, 2012 Apr.
Article in English | MEDLINE | ID: mdl-22707864

ABSTRACT

BACKGROUND: Strychnos nux-vomica, commonly known as kuchla, contains strychnine and brucine as main constituents. Minor alkaloids present in the seeds are protostrychnine, vomicine, n-oxystrychnine, pseudostrychnine, isostrychnine, chlorogenic acid, and a glycoside. Seeds are used traditionally to treat diabetes, asthma, aphrodisiac and to improve appetite. OBJECTIVE: The present study was aimed to evaluate the various pharmacognostical characters and antidiabetic activity of S. nux-vomica seed. MATERIALS AND METHODS: Pharmacognostical characters were performed as per the WHO guideline. Extraction was carried out in petroleum ether, chloroform, alcohol, hydroalcoholic, aqueous, and phytochemical constituents present in extracts were detected by different chemical tests. Among these extracts hydroalcoholic, aqueous extracts were evaluated for antidiabetic activity on the basis of extractive yield and phytoconstituents, in alloxan-induced diabetic rats using gliclazide as standard. RESULTS: Various analytical values of S. nux-vomica extract were established. Phytoconstituents present in S. nux-vomica extracts were detected. CONCLUSION: S. nux-vomica extracts show antihyperglycemic activity in experimental animals.

18.
Anc Sci Life ; 31(3): 132-6, 2012 Jan.
Article in English | MEDLINE | ID: mdl-23284220

ABSTRACT

This study was carried out to investigate the antioxidant and free radical scavenging activity of methanolic extract of Madhuca indica bark in varios systems. DPPH radical, superoxide anion radical, nitric oxide radical, hydroxyl radical, lipid peroxidation, and total phenolic content assays were carried out to evaluate the antioxidant potential of the extract. The percentage inhibition of 40 µg/ml concentration of MMI in DPPH radical scavenging model was found as 74.1%. The scavenging of nitric oxide by the plant extract was concentration dependent and IC(50) value of rutin was found to be 161.7 µg/ml. MMI elicited significant and concentration-dependent superoxide radical scavenging effect with MMI as well as standard curcumin, which exhibited IC(50) values of 38.1 and 5.84 µg/ml, respectively. MMI demonstrated significant scavenging activity of OH(-) radical generated from Fe(2+)-ascorbate-EDTA-H(2)O(2) in a concentration-dependent manner. The extract showed a significant dose-dependent free radical scavenging activity in all the models. The extract showed the presence of high phenolic content corresponding to 98.48 µg equivalent of gallic acid and the antioxidant activity could be attributed to this.

19.
Indian J Crit Care Med ; 15(3): 173-5, 2011 Jul.
Article in English | MEDLINE | ID: mdl-22013310

ABSTRACT

Stevens-Johnson syndrome (SJS) is a rare immunologic reaction that may involve skin or various mucosal surfaces. The etiology may range from multiple pharmacologic agents to viral infections. Associated findings can range from minimal skin and mucosal involvement to extensive dermal exfoliation, nephritis, lymphadenopathy, hepatitis, and multiple serologic abnormalities. We report a female patient of 38 years with a history of drug allergy who was administered oxcarbazepine for the management of right partial bronchial seizure due to left parasagittal mass lesion following which she developed papular rashes all over the body and diagnosed as SJS. Although carbamazepine (CBZ) is the most common cause of SJS, a new anticonvulsant, oxcarbazepine, which is structurally related to CBZ, has been shown to induce SJS.

20.
J Young Pharm ; 3(3): 226-31, 2011 Jul.
Article in English | MEDLINE | ID: mdl-21897663

ABSTRACT

Natural compounds still play an increasingly important role in many areas of research and development. Their structural diversity is enhanced by the synthetic potential of combinatorial chemistry. Fractionation and separation of samples obtained from nature remain time-consuming, tedious and extremely expensive even though the assays for testing these samples have become faster and more cost-effective thanks to advanced high-throughput screening (HTS) processes. Today, sepbox is the standard technology used for separating compounds from natural resources. Fractionations and separation of samples obtained from nature remain very difficult. Automation of sample preparation therefore has great economic potential. The unique sepbox concept allows processing sample automatically and will make up to 30 times faster than by using a conventional process.

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