Review on Pharmacoscintigraphy

Pharmacoscintigraphy is a non-invasive technique for determining the fate of drugs after administration into humans. Collecting valuable information through the pharmacoscintigraphyabout absorption and release mechanisms of drugs from formulations, and thus proving to be an invaluable tool in developing newer and more effective formulations. Such studies can be used to determine the behavior of drugs, formulation as well as diagnostic agents that are administered. In this technique, radiolabelled formulations are administered to patients by their intended route of administration. Their transit through the body is monitored using sophisticated imaging cameras. Since the amount of radiotracer that is used is very low, this is a safe, efficient, and accurate method for studying the behavior of drugs in the human body. Preclinical studies of newer drugs have successfully been carried out using the pharmacoscintigraphic technique

Super Porous Hydrogels: A Review

Super porous hydrogels (SPHs) basically developed initially create as a novel drug delivery system to absorb and continue to hold the drugs in the gastric medium which allows absorption in stomach and upper part of the gastrointestinal tract. These systems get swollen in the stomach instantly and in the harsh stomach environment they maintain their integrity, while the pharmaceutical active ingredient is being released. Instant and fast swelling property of hydrogel is based on water absorption through open porous structure by capillary force. SPHs have the poor mechanical strength which has got over by developing the second-generation SPH composites (SPHCs) and the third-generation SPH hybrids (SPHHs). The present review has been focused on the preparation, characterization and application of SPHs

Management of rare and atypical inguinal hernias: our experience at a tertiary care centre

Background: Inguinal hernia is one of the most common surgical conditions operated by the surgeon. The purpose of the study paper was to provide diagnostic and therapeutic resources to deal with certain difficult situations in hernia repair.Methods: A retrospective analysis of 8 rare and atypical inguinal hernias was conducted for a period of 2 years at NRI General Hospital, which includes cases like Loss of domain hernias and hernias with atypical contents; which stood as diagnostic and management challenge to the surgeon.Results: Of the eight very rare and atypical cases operated, no postoperative complications were noted except one which developed a scrotal abscess after one month of discharge.Conclusions: The infrequent encounter with rare and atypical hernias stands a diagnostic challenge to the surgeon. Inguinal hernia repair even-though looks simple yet may sometimes be very difficult.

Development, implementation, and analysis of adverse drug reaction monitoring system in a rural tertiary care teaching hospital in Narketpally, Telangana.

Background: Adverse drug reactions (ADR) are the fourth leading cause of mortality and a great concern in therapeutics. Pharmacovigilance is more important in India as the health care system is inadequate with poor doctor-patient ratio, high incidence of self-medication, and presence of counterfeit drugs. The present study was conducted with the aim of analyzing the pattern of ADR occurring in a rural tertiary care hospital with a newly established pharmacovigilance center and to identify the most frequent ADRs, common drugs implicated and severity of reactions. Methods: A non-interventional observational prospective study was conducted over a year. The red boxes for dropping the filled yellow ADR forms were installed in all the wards and outpatient departments. Additional information and missing data were obtained personally by either consulting the physician or through case sheets. Results: The most common class of drugs implicated in the causation of ADRs was antimicrobials (52%), followed by drugs acting on the central nervous system. The most commonly observed ADRs were dermatological Type B reactions. The majority of the reactions belonged to possible or probable category, but no reaction was categorized as definite. Conclusion: Dermatological reactions are the most common ADR occurring in our hospital and antimicrobials are the most common causative drugs. The reporting rate was adequate, and there is still a need for increasing the awareness and knowledge about ADR reporting system and pharmacovigilance for promoting the safe use of drugs.

Effect of Different Carbon and Nitrogen Sources on Growth and Indole Acetic Acid Production by Rhizobium Species Isolated from Cluster Bean [Cyamopsis tetragonoloba (L.)].

Five Rhizobium strains (Cb1, Cb2, Cb3, Cb4 and Cb5) were isolated from root nodules of cluster bean [Cyamopsis tetragonoloba (L.)] on yeast extract mannitol agar (YMA) medium. All the five Rhizobium isolates have shown the Indole Acetic Acid( IAA) production in culture medium supplemented with L-tryptophan. The IAA content in culture supernatant was estimated by using the colorimetric method (13). All the five Rhizobium isolates produced maximum amount of IAA in medium supplemented with 2.5mg/ml Ltryptophan concentration. Production of IAA was maximum at 72h of incubation when bacteria reached the stationary phase. The cultural conditions were optimized for maximum IAA production by using different carbon and nitrogen sources as well as changing the incubation period. Glucose and L-asparagine were found to be the best carbon and nitrogen sources, respectively for maximum IAA production. The cell wall affecting agent, penicillin increased the IAA production up to 77.95% in Cb4, 59.52% in Cb5 and 37.84% in Cb3 isolates, over the control. Among the five isolates studied, isolate Cb4 showed better performance in IAA production.

Modulatory effects of α- linolenic acid on generation of reactive oxygen species in elaidic acid enriched peritoneal macrophages in rats.

Fatty acids are known to influence the ability of macrophages to generate reactive oxygen species (ROS). However the effect of elaidic acid (EA, 18:1 trans fatty acid) on ROS generation is not well studied. Rat peritoneal macrophages were enriched with elaidic acid by incubating the cells with 80 µM EA. The macrophages containing EA generated higher amounts of superoxide anion (O2·-), hydrogen peroxide (H2O2) and nitric oxide (NO˙) by 54, 123 and 237%, respectively as compared to control cells which did not contain EA. To study the competition of other C18 fatty acids with EA macrophages were incubated with EA along with stearic acid (18:0), oleic acid (18:1), linoleic acid (18:2) and α- linolenic acid (ALA, 18:3). ALA significantly reduced the incorporation of EA into macrophage lipids. This also significantly reduced the generation of O2· -, H2O2, NO˙ by macrophages. Studies were also conducted by feeding rats with diet containing partially hydrogenated vegetable fat (PHVF) as a source for EA and linseed oil (LSO) as a source for ALA. The rats were fed AIN-93 diet containing PHVF with 17% EA and incremental amounts of linseed oil for 10 weeks. The peritoneal macrophages from rats fed partially hydrogenated vegetable fat generated higher levels of O2·-, H2O2, NO˙ by 46, 161 and 76% respectively, when compared to rats fed control diets containing ground nut oil. Macrophages from rats fed PHVF with incremental amounts of LSO produced significantly lower levels ROS in a dose dependent manner. Thus ALA reduces the higher levels of ROS generated by macrophages containing EA.

Efficacy of naturopathy and yoga in bronchial asthma.

The aim of the study was to test the efficacy of a one month in-patient naturopathy and yoga programme for patients with asthma. Retrospective data of 159 bronchial asthma patients, undergoing the naturopathy and yoga programme, was analyzed for Forced Vital Capacity, Forced Expiratory Volume at the end of 1 second, Maximum Voluntary Ventilation and Peak Expiratory Flow Rate on admission, 11th day, on discharge and once in three months for three years. The paired sample t test results showed significant increase in the Forced Vital Capacity and Forced Expiratory Volume from the date of admission up to 6th month (P<0.0035) post Bonferroni correction. Maximum Voluntary Ventilation significantly increased from admission till the date of discharge (P<0.0035) and Peak Expiratory Flow Rate significantly increased from admission till the 36th month of follow-up (P<0.0035), post Bonferroni correction. This validated the beneficial effect of combining naturopathy and yoga for the management of bronchial asthma.

Formulation and Evaluation of Oral Elementary Osmotic Pump Tablets of Sumatriptan Succinate.

Aim: In the present study, Sumatriptan succinate was formulated as oral elementary osmotic pump with a zero-order drug release profile. Methodology: The effect of different formulation variables i.e. different types of osmogens, concentrations of osmogen and concentration of coating solution were studied. The in vitro evaluation was carried out in different release media. Result: Highest percentage of drug release was observed at high concentration of mannitol i.e., 1:3 (drug: mannitol). Osmogen with low osmotic pressure (38 atm) showed 71.01% zero-order drug release for 12 hours when compared to that of the osmogen with high osmotic pressure (356 atm) which showed 67.38% of release by zero order. Conclusion: Elementary osmotic pump tablets of Sumatriptan succinate were able to deliver zero-order release up to 12 hours independent of pH of dissolution media and have overcome the problem of chronotherapeutic effect.

Evaluation of the effects of tramadol and diclofenac alone and in combination on post-cesarean pain.

Background: Post-cesarean pain is a common cause of acute pain in the obstetrics. Pain in the postoperative period is an important impediment to recovery from surgery and anesthesia. This study was conducted to evaluate the efficacy of postoperative analgesia and incidence of side-effects of centrally acting drug tramadol with peripherally acting drug diclofenac alone and in combination in patients undergoing elective cesarean delivery under spinal anesthesia. Methods: The study population of 90 patients was randomly divided into three groups of 30 each to receive the following treatments: tramadol (Group T), diclofenac (Group D), tramadol and diclofenac at reduced doses (Group TD). Results: Combination of tramadol and diclofenac produced significantly early analgesia in comparison to tramadol or diclofenac alone and decrease in the incidence of side-effects. Conclusion: We conclude that a multimodal approach to post-cesarean management with a combination of tramadol and diclofenac produced better analgesia than individual drugs and a reduction in the side-effects. Such a combination approach to relieve pain is more effective and advantageous.

Preparation and Evaluation of Novel Expandable Drug Delivery System.

Aims: The purpose of this research is to develop a novel expandable gastroretentive dosage form (GRDF), based on unfolding mechanism. It consists of a drug loaded bilayer polymeric film, folded into a hard gelatin capsule. Gastric retention is achieved due to unfolding of the dosage form within 15-20 min. Furosemide is selected as the drug candidate for this work. Due to its narrow absorption window, Furosemide has to be administered to the upper parts of the intestine in order to maintain sustained therapeutic levels. This may be achieved by a GRDF. Methodology: Films were prepared by solvent-casting technique using Ethyl cellulose, HPMC E15 and Eudragit RLPO as polymers and dibutyl phthalate as the plasticizer in both layers. The film with zigzag folding in the capsule was shown to unfold in the gastric juice and provide drug release up to 12 h in the acidic medium. The films were evaluated for weight & thickness variation, mechanical properties, in vitro drug release and unfolding behavior based on the mechanical shape memory of polymers. Absence of drug polymer interaction and uniform drug dispersion in the polymeric layers was revealed by DSC, XRD studies and SEM. The GRDF location in the gastrointestinal tract was determined by X-ray studies. Results: X-ray studies revealed that the GRDF is retained in the stomach up to 6± 0.5 h in fasting condition and 8 h in fed state. Conclusion: The polymers used in the development of GRDFs were safe and proper combination of these polymers will yield a novel expandable GRDF with good in vitro drug release in acidic media, mechanical properties, and unfolding behaviour. These outcomes demonstrate that the GRDF may be used to improve furosemide therapy and can be applied to extend the absorption of other narrow absorption window drugs that require continuous input.

Enhanced Bioavailability of Nimodipine from Bioadhesive Buccal Bilayered Patches in Human Volunteers.

Aims: The objective of the present study was to develop a bioadhesive bilayered buccal patch of Nimodipine (15 mg) using Eudragit Rs 100 as secondary layer and a primary layer with Hydroxy propyl methyl cellulose and Hydroxy propyl cellulose JF. Methodology: Bilayered buccal patches were prepared by solvent casting technique. The absence of physiochemical interactions between NMDP and the polymer were investigated by differential scanning calorimetry (DSC). Bilayered buccal patches of NMDP were evaluated for in vitro drug permeation through porcine buccal membrane, in vitro drug release, moisture absorption, surface pH, mechanical properties and in vitro bioadhesion. Results: The results indicated that suitable bioadhesive bilayered buccal patches with desired permeability could be prepared. The bioavailability study was performed in healthy humans in a crossover experimental design. Bioavailability studies revealed that nimodipine possessed good buccal absorption. The relative bioavailability of the optimized buccal patch was found to be 205% in comparison to 30 mg marketed oral tablet. The formulation CC3 showed 68.84 ± 1.4% release and 46.85 ± 5.1% of drug permeated through porcine buccal membrane in 4 hr. A good correlation was seen between percentage in vitro release the extent of bioavailability for nimodine buccal patch. Conclusion: An improvement of bioavailability was obtained by buccal route to the extent of 2.05 times higher than that of oral route for NMDP. Hence, the development of a bioadhesive bilayered buccal patch for NMDP might be a promising one, as the necessary dose of drug could be decreased, resulting less side effects. Good ex vivo - in vivo correlation was obtained for NMDP.

Formulation and Evaluation of Gastroretentive Floating Tablets of Domperidone Maleate.

The low bioavailability (15%) and good solubility of Domperidone Maleate in acidic pH following oral administration favours development of a gastro retentive formulation. Gastroretentive floating matrix tablets of Domperidone Maleate were successfully prepared with hydrophilic polymers like HPMC K4M, HPMC K15M and HPMC K100M. From the Preformulation studies for drug excipients compatibility it was observed that there was no compatability problem with the excipients used in study. The drug release from most of the formulations follows fickian diffusion. From in-vivo X-ray studies, it was clearly observed that the floating tablets showed a gastric residence of nearly 4.5 hrs in fed state.

Preparation of activated kaza’s carbons from bio-materials and their characterization.

Prepared three different activated carbons from parts of three different bio-materials viz., Phaseolus trilobus, Leucena leucocephala and Casuarina collected from agricultural field. In the present study phsicochemical and surface characterstics of these prepared carbons have been discussed. For surface characterization FTIR and EDAX methods were used.

Localization of mycobacteral smegmatis adenosine deaminase.

The study was carried out to check the localization of M.smegmatic adenosine deaminase for its metabolic and clinical importance. The separation and washing of the membrane was done by using refrigerated high-speed centrifuge. The high activity was observed in crude extract while low activity in first washing of the membrane but after second washing there was no enzyme activity seen. Culture media also does not show any enzyme activity. Thus M.smegmatic adenosine deaminase may be a cytosolic enzyme and it does not excreted in to the surrounding media.

An evaluation of the color stability of tooth-colored restorative materials after bleaching using CIELAB color technique.

AIMS AND OBJECTIVE: The aim of this laboratory study was to evaluate the effect of three home bleaching agents: Vivastyle Paint On, Vivastyle, and Opalascence PF on the color stability of the microfilled composite Durafill, the nanofilled composite Filtek Z 350, and the glass ionomer cement Fuji II. MATERIALS AND METHODS: There were 3 groups in this study (n=40)-Group I: durafill, Group II: Filtek Z 350, and Group III: Fuji II. Each group was further subdivided into 4 subgroups (n=10), Subgroup A: bleaching with Vivastyle Paint On, Subgroup B: bleaching with Vivastyle, Subgroup C: bleaching with Opalascence PF, and Subgroup D: control specimens stored in distilled water. Bleaching was carried out following the manufacturer's instructions for a period of 14 days. At the end of the bleaching regimen, the specimens were tested for color change using the CIELAB technique and a reflectance spectrophotometer. RESULTS: The data was subjected to statistical analysis. A Kruskal-Wallis variance analysis and Mann Whitney U test were done to determine the significant color change of the restorative materials. All restorative materials demonstrated a significantly higher color change (DeltaE) with Vivastyle (P < 0.0001). The mean color change of GIC (11.4 +/- 0.3) was the highest among the materials followed by Durafill (7.5 +/- 0.1). Filtek z 350 (0.3 +/- 0.1) showed the least color change with all the bleaching agents. CONCLUSION: Glass ionomer cement showed the highest color change followed by the microfilled composite. The nanofilled composite was found to be highly stable in terms of color.

Evaluation of target concentration intervention strategy of gentamicin therapy in a malnourished patient population of south India.

BACKGROUND & OBJECTIVE: Aminoglycoside antibiotics, especially gentamicin, are widely used in suspected Gram-negative infections in India. Therapeutic drug monitoring is not commonly used for this drug in our population. We evaluated the target concentration intervention (TCI) strategy of gentamicin therapy in a predominantly malnourished patient population with lower respiratory tract infection in south India. METHODS: Patients who were prescribed gentamicin for suspected lower respiratory tract infection were randomized to any of the three groups, viz., control (CG), once daily dosing (ODD), and pharmacokinetic dosing (TCI) groups. Diagnosis was initially done by clinical evaluation and confirmed radiologically. Patients in CG received 80 mg gentamycin twice daily, ODD group received 160 mg once daily, and TCI groups received 160 mg once daily initially followed by dose revision based on serum drug levels. Blood samples were collected at peak and trough levels and assayed for gentamicin concentration. Dose adjustment was done in TCI group whereas the other groups received standard doses. Efficacy and safety were evaluated as outcome measures. RESULTS: Of the 52 patients included initially in the study, 43 (CG 20, ODD 12, TCI 11) completed the study. The doses administered to the study subjects were less than those prescribed in standard textbooks and guidelines. Patients in TCI group had their gentamicin doses revised upwardly to a dose of 4.3+/-0.6 mg/kg to achieve a peak gentamicin concentration of 12 to 15 microg/ml. Both ODD and TCI groups showed significant improvements in outcomes studied over the control group. INTERPRETATION & CONCLUSION: The results of our study indicated that once daily dosing of gentamycin was superior to multiple daily dosing in treating the lower respiratory tract infection in the study population. All patients in the ODD and TCI groups achieved satisfactory serum drug concentrations at administered doses (160 mg/day for ODD and <or= 200 mg/day for TCI group). In our study, target concentration intervention did not significantly improve the therapy outcomes. Since the study sample is small further research may be needed.

Designer insulins regimens in clinical practice--pilot multicenter Indian study.

BACKGROUND: Newer insulin analogues viz., premix insulin analogue (biphasic insulin aspart) and insulin glargine are now available in India. A multicenter all-India study was done to document the patient profile and responses to these analogues in routine clinical practice. METHODS: The study was conducted prospectively at 4 diabetes care clinics in different regions of India and collected data on the use of either of the two regimens A. Premix insulin analogue given twice-daily B. Basal-bolus analogue regimen (insulin aspart with every meal and insulin glargine once-a-day at bedtime). The centers collected all data at 3 time-points--baseline, 4 weeks later and end of 12 weeks. The study measures were FPG (fasting plasma glucose), PPPG (postprandial plasma glucose), HbA1c and insulin dose. FPG and PPPG were recorded at each of the three time points. HbA1c was recorded at baseline and end of study. Safety was assessed based on reported adverse drug reactions and occurrence of hypoglycaemias. RESULTS: Data of 145 patients was available for analysis (n=114 on premix insulin analogue and n=31 on basal-bolus analogue regimen). Baseline demography was comparable in the two groups. Both the regimens lowered all blood glucose parameters including HbA1c significantly as compared to baseline. However, the premix insulin analogue fared better than the basal-bolus regimen in lowering HbA1c (1.58 vs. 1.16% respectively; p<0.05). Also 41% more patients in the premix group could achieve target HbA1c of < 7% at the end of study. The mean insulin dose was lower with the premix analogue group at the end of 12 weeks. There was no significant difference between the two groups in terms of change in body weight. No major hypoglycaemias were reported and the percentage of patients experiencing a minor episode was lower with the premix analogue than the basal-bolus regimen both at 4 and 12 weeks (11.4 vs. 35.48%; 16.7 vs. 58.06% respectively). No adverse drug reactions were reported throughout the study. CONCLUSION: We conclude that both premix analogue administered twice a day and four times a day basal bolus regimen appear to be a convenient, safe and effective way of initiating insulin therapy in people with type-2 diabetes. The premix analogues achieves target better than the basal bolus regimen as has better compliance.

Comparison of target concentration intervention strategy with conventional dosing of digoxin.

Digoxin is a widely used drug in patients with congestive heart failure. The present study compared the quality of life of congestive heart failure patients on one year follow-up period with two different dosing of digoxin (5/7 therapy and 7/7 therapy in whom the target serum digoxin concentration is maintained). Quality of life significantly improved in intervention group thus emphasizing the need for continuous dosing of digoxin based on target concentration.

Effect of lead on Na+, K(+)-ATPase activity in Penaeus indicus postlarvae.

In vivo effect of lead on Na, K(+)-ATPase was studied in plasma membrane/mitochondrial fraction of P. indicus post-larvae (PL), exposed to 30 days to a sublethal concentration (1.44 ppm) of lead. A significant (P < 0.05) decrease in the enzyme activity was observed for exposed PL with respect to their controls at different intervals except 24hr. Further the substrate (ATP) and ion (Na+ and K+)-dependent kinetics of Na+, K(+)-ATPase was studied with the plasma membrane/mitochondrial fractions of control and 30 days exposed PL. The apparent KM and V(max). values were calculated to determine the nature of inhibition. Both the control and exposed PL showed almost the same apparent KM values in the presence of different substrate or ion concentrations indicating that lead interacts with the enzyme at a different binding site.