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ABSTRACT

The objective of the study is to formulate and evaluate Delayed Release tablets and to develop a pharmaceutically stable, cost effective and quality improved formulation. The prime intension is to delay the release of drug which is inactivated by the stomach contents.Methacrylicacid copolymer (EudragitL30D55) was used as a enteric coating material in the formulation and mannitol is used as diluent and Crospovidone as super disintegrant and povidone(PVP K-30) as binder in different proportions and varying the compositions of sub coating and enteric coating using sicovit yellow ,titanium dioxide and eudragit .The core tablets were prepared by dry granulation method. Stability study is carried out for 2 months at 25°C; 60% RH: and 40°C; 75%RH, according to ICH guidelines. The tablets were tested for acid release during the stability period and confirmed that results were found with in the limits.

Key Words:- Esomeprazole, Eudragit, H1.inhibitor, Relative humidity.

ABSTRACT

The aim of this research wok is to formulate and evaluate Cefixime Trihydrate solid dispersions system by using the different techniques. This will increase the solubility of the drug or Cefixime Trihydrate and give the immediate release of the drug from the formulations. The main objective is to formulate a drug product as immediate release oral solid dosage form of Cefixime Trihydrate solid dispersion system which is considered to be stable, robust quality and enhanced dissolution rate. To optimize the method of manufacture by formulate the Cefixime Trihydrate solid dispersion system by various techniques like Physical mixing, Co-grinding, Kneading and solvent evaporation techniques. The disintegrating agent used in the present study is Croscarmellose sodium. To study the dissolution of Cefixime Trihydrate solid dispersion system by using the Physical mixing, Co-grinding, Kneading and solvent evaporation techniques, Optimization of formula. Among the four different techniques used for preparation o solid dispersions solvent evaporation technique has shown the increase in dissolution rate that is the Trail-5 was found to have a faster solubility and dissolution property which was prepared by using Croscarmellose sodium as a disintegrant in the ratio of 1:1.

Key Words:- Solid dispersions, Solubility, Dissolution rate, Cefixime Trihydrate, Croscarmellose sodium.

ABSTRACT

The combination of liquid chromatography and mass spectrometry (LC–MS) is a powerful analytical tool and is widely applied in these days. The use of LC-MS is increasing and is proven to be useful in many areas of drug discovery like identification of lead molecule, identification of impurities and study of pharmacokinetic and metabolism profiles. High-throughput LC-MS-systems are used in the “accelerated drug discovery” process studies. The current developments in liquid chromatography-mass spectrometry (LC-MS) and its applications to the drug discovery process are reviewed in the present article.

Key Words:- Liquid Chromatography(LC), Mass Spectroscopy, Drug discovery.

ABSTRACT Prior studies suggested that nano particle drug delivery might improve the therapeutic response to anticancer drugs and allow the simultaneous monitoring of drug uptake by tumours. Cancer nano therapeutics are rapidly progressing and are being implemented to solve several limitations of conventional drug delivery systems such as nonspecific bio distribution and targeting, lack of water solubility, poor oral bioavailability, and low therapeutic indices. To improve the bio distribution of cancer drugs, nano particles have been designed for optimal size and surface characteristics to increase their circulation time in the bloodstream. They are also able to carry their loaded active drugs to cancer cells by selectively using the unique pathophysiology of tumours, such as their enhanced permeability and retention effect and the tumor microenvironment. In addition to this passive targeting mechanism, active targeting strategies using ligands or antibodies directed against selected tumor targets amplify the specificity of these therapeutic nano particles. Drug resistance, another obstacle that impedes the efficacy of both molecularly targeted and conventional chemotherapeutic agents, might also be overcome, or at least reduced, using nano particles. Nano particles have the ability to accumulate in cells without being recognized by P-glycoprotein, one of the main mediators of multidrug resistance, resulting in the increased intracellular concentration of drugs. Multifunctional and multiplex nano particles are now being actively investigated and are on the horizon as the next generation of nano particles, facilitating personalized and tailored cancer treatment. Targeting methotrexate increased its antitumor activity and markedly decreased its toxicity, allowing therapeutic responses not possible with a free drug. Key Words:- Nano particles, Drug delivery, Targeting, Drug release.

ABSTRACT

Lectin was isolated from Adathoda vasica leaves. The galactose specific lectin from Adathoda vasica leaves was purified by 80 % ammonium sulphate precipitation, followed by dialysis against 50 mM Tris HCl pH (7.6) and sephadex G-100 column (16 mm dia m x 22 cm) chromatography. The Flow rate of 1.5 mL 12min−1 fraction showed hemagglutinating activity against on rabbit 4% erythrocytes. The A. vasica lectin pH dependent assays showed best hemagglutinating activity at pH 5.0–7.0; being decreased at acidic/ alkaline conditions and by EDTA treatment. A.vasica lectin is a tetramer at pH 7.2 and a dimer at pH 4.0. Human erythrocytes from ABO system, cow, sheep, Goat, mice, rabbit, big were collected and titrated against Adathoda vasica lectin result confirmed that the rabbit erythrocyte specificity for AVL. The results for molecular mass determinations were about 20 kDa. This new methodology is useful and easy, with low costs, for lectin purification in large amounts.

Key Words:- Lectin isolation, Lectin purification, Protein purification.

ABSTRACT

The studies on Clinical comparison of the efficacy and safety of Bimatoprost/Timolol combination and Travoprost/Timolol combination in glaucoma patients were carried out in a Vasan Eye Care Hospital located at Tiruchirappalli. The hospital is unique and well known for its services, to people who come from all over the district and various parts of the country. This study was designed to compare the efficacy and safety of Bimatoprost/Timolol combination and Travoprost/Timolol combination in glaucoma patients. This study included 30 glaucoma patients, based on the inclusion and exclusion criteria. From the selected 30 patients, 15 patients were treated with Bimatoprost/Timolol combination (Group A) and remaining 15 patients were treated with Travoprost/Timolol combination (Group B). In this study initial readings were considered as base, First Review values taken at the end of 2nd week and the Second Review values taken at the end of 6th week. Bimatoprost/Timolol combination and Travoprost/Timolol combination does not have any effect on Visual acuity, Pupil size, Blood pressure and Pulse rate. The present study concluded that, adverse drug reactions of Travoprost/Timolol combination were less than the Bimatoprost/Timolol combination. Further, the pharmacoeconomic study (cost effective analysis) revealed that Bimatoprost/Timolol combination is cost effective than Travoprost/Timolol combination. Due to the patient counseling, the patient’s knowledge about glaucoma, its drug usage and patient compliance is improved.

Key Words:- Glaucoma, Bimatoprost/Timolol, Travoprost/Timolol, Adverse Drug Reactions.

ABSTRACT

A simple and precise RP-HPLC method was developed for the determination of related substances in Rosuvastatin calcium tablet dosage form. The chromatographic separation was achieved on an kromosil C18 250x4.6mm (5microns) column with mobile phase contain the gradient mixture of the solvent (Water:A:C:N:Methanol:Triethylamine) in the ratio of 450:250:350:1. The eluted compounds were monitored at248nm and the run time was 60 min. the development method separates (two) unknown impurities and rosuvastatin calcium from each other. The calibration curve were linear in the range between 50-200% with correlation coefficient 0.996 and 0.999, %recovery studies were found to be 99.8 and 99.6 for impurity I and II. The development and validated RP-HPLC method is applied for identification of eluted unknown impurities of Rosuvastatin calcium.

Key Words:- Rosuvastatin calcium, RP-HPLC, Method validation, Impurities.

ABSTRACT

Colon targeting system is used for both local and systemic delivery of drugs. It is also a potential site for systemic delivery of therapeutic proteins and peptides, oligonucleotides and vaccines. It is an alternative system for the orally administrated drugs that pass through GIT which presents several formidable barriers to drug delivery. Treatment could be more effective if it is possible for drug to be directly administered to colon there by dose and systemic side effects can be reduced. To achieve successful colonic delivery, a drug needs to be protected from absorption and /or the environment of the upper gastrointestinal tract (GIT) and then be abruptly released into the proximal colon, which is considered the optimum site for colon-targeted delivery of drugs. Colon targeting is naturally of value for the treatment of diseases of colon such as Crohn\'s diseases, ulcerative colitis, colorectal cancer and amoebiasis. This review mainly concentrates on primary and novel approaches to target the colon. Primary approaches include pH Dependent, Time-Dependent Delivery, Microbially Triggered Drug Delivery to colon and novel approaches include Pressure Controlled Drug-Delivery Systems, Novel Colon Targeted Delivery System (CODESTM), Osmotic Controlled Drug Delivery (ORDS-CT), Bioadhesive systems and Multiparticulate Systems. These novel approaches are unique in terms of achieving in vivo site specificity and feasibility of manufacturing processes.

Key Words:- Colon drug delivery, Drug targeting, approaches, biodegradable polymers.

ABSTRACT

Conventional drug delivery systems have little control over their drug release and almost no control over the effective concentration at the target site. This kind of dosing pattern may result in constantly changing, unpredictable plasma concentrations. Drugs can be delivered in a controlled pattern over a long period of time by the process of osmosis. Osmotic devices are the most promising strategy based systems for controlled drug delivery. They are the most reliable controlled drug delivery systems and could be employed as oral drug delivery systems. The present review is concerned with the study of drug release systems which are tablets coated with walls of controlled porosity. When these systems are exposed to water, low levels of water soluble additive is leached from polymeric material i.e. semi permeable membrane and drug releases in a controlled manner over an extended period of time. Drug delivery from this system is not influenced by the different physiological factors within the gut lumen and the release characteristics can be predicted easily from the known properties of the drug and the dosage form. In this paper, various types of osmotically controlled drug delivery systems and the basic components of controlled porosity osmotic pump tablets have been discussed briefly. In osmotic delivery systems, osmotic pressure provides the driving force for drug release. Increasing pressure inside the dosage form from water incursion causes the drug to release from the system.

Key Words:- Osmosis, Osmotic pressure, Osmogen, Semi permeable membrane, Osmotic pumps.

ABSTRACT

The present study was designed to develop a simple, validated UV-Spectrophotometric method and a RP-HPLC method for the analysis of Metaxalone in bulk and pharmaceutical dosage forms. The fast and reliable UV-Spectrophotometric Method was carried out using the values measured at 280 nm in methanol for Metaxalone. Calibration graph was constructed at the wavelength of determination was linear in the concentration range of using 40-200 μg/ml for Metaxalone and the correlation coefficient was found to be 0.9998. Precision study showed that the % RSD was within the range of acceptable limits (< 2), and the % Recovery was found to be in the range of 98.24 % - 100.97 %. The LOD and LOD were found to be 0.301404286 g/mL and 0.913346321 g/mL respectively. A precise and accurate RP-HPLC method was developed by isocratic operation of mobile phase. The best stationary phase was determined as C18 column, 5 μm, 250 mm × 4.6 mm. Mobile phase was optimized to obtain a fast and selective separation of the drug. Flow rate was 1.00 mL/min, Wavelength was set at 210 nm and the volume of each injection was 20 μL. An isocratic Phosphate buffer (pH 5): Acetonitrile: Methanol mobile phase at the ratio of 40:40:20 gave the best separation and resolution. The proposed methods were accurate, precise, sensitive, and linear over a wide range of concentration of Metaxalone. The developed methods have been validated as per ICH guidelines. The validated methods were successfully applied to the determination of Metaxalone in bulk and pharmaceutical dosage forms.

Key Words:- Metaxalone, UV-Spectrophotometric, RP-HPLC, ICH guidelines.

ABSTRACT

Patients receiving a large number of medications are more prone to drug related problems (DRPs). This is especially true for nephrology patients who are prescribed an average of eight medications per day. The complexity of drug therapy can lead to confusion, non compliance, interaction and adverse effects. Nephrology patients are known to be dependent on a large number of medications in view of the severity of the disease. Therefore, this study was performed to evaluate the incidence of DRPs, types of drugs involved, drug risk ratio and risk factors for nephrology patients. The study was performed using the PCNE criteria for identifying DRPs. It was carried out prospectively in a local tertiary hospital. A total of 70 patients were recruited in the study, of which 45 (64.3%) patients reported at least one DRP. There was a total of 118 DRPs reported with a rate of 1.7 DRP per patient. The most common DRP reported based on the PCNE classification was ‘drug use problem’ (n=57/118, 48.3%) and ‘adverse reaction’ (n=39/118, 33.1%). The most common class of drugs involved were antianemia (n=23/118, 19.5%), mineral supplements (n=12/118, 10.2%) and lipid modifying agents (n=12/118, 10.2%). The drugs with the highest drug risk ratio were corticosteroid (0.5), lipid modifying agents (0.32) and antianaemia (0.32). Interestingly, risk factors of DRPs were gender (RR=0.105, p=0.030) and number of drugs prescribed (RR=0.130, p=0.015). This work presents the importance of providing appropriate support for nephrology patients to ensure reduced risk of DRPs.

Key Words:- Drug related problems, Nephrology, Medication.