Pharmacotherapy

The aim of the present study was to formulate and evaluate Metformin HCl microspheres to produce a drug delivery system with better pharmaceutical and therapeutic properties. Metformin HCl microspheres were prepared by using ethyl cellulose as a release retardant polymer by solvent evaporation method .Formulations F1, F2 and F3 were prepared using ethyl cellulose in the drug polymer ratio of 1:1, 1:2 and 1:3. A plasticizer (N-dibutyl phthalate) was added in formulations F4,F5 and F6 .The prepared microspheres were evaluated for the parameters like Percentage yield, Particle size analysis, Micromeritic properties like angle of repose, bulk density, tapped density, compressibility index, Hausner’s ratio, melting point determination, drug content estimation, microencapsulation efficiency and in vitro drug release studies. The in vitro release of Metformin HCl was slow and extended over longer period of time. As the concentration of polymer was increased, the drug release was decreased. The drug release was found to be slow in formulations F4, F5 and F6 when compared to F1, F2 and F3. Thus the study clearly indicated a promising potential of sustained release Metformin HCl microspheres containing ethyl cellulose as rate controlling polymer for effectively treating diabetes mellitus.

Résumé/Abstract In 2000, the Society of Critical Care Medicine (SCCM) and the American College of Clinical Pharmacy (ACCP) published a position paper that defined critical care pharmacy services as fundamental, desirable, and optimal. A task force was developed ...

Peptic ulcer is a disorder of the upper gastrointestinal tract that is caused by gastric acid. There are various chemical agents available for the treatment of peptic ulcers, but claim serious side effects. Herbal drugs are preferred over chemical agents due to their relatively less toxicity, better acceptability and better compatibility with human body. Lesser adverse effects, economical, effective and easy availability. The present research has been carried out to investigate antiulcer activity of Hydroalcoholic leaf extract of Pisonia grandis R.Br (HEPG) using Indomethacin induced gastric ulcer and Pylorus ligation induced gastric ulcer in wistar rats. Ulcer score, ulcer index and number of ulcers were determined for indomethacin and pylorus ligation induced gastric ulcers. Antiulcer effect of Pisonia grandis R.Br (HEPG) was compared with standard drug omepprazole (20mg/kg). These observations helped us to conclude that Hydroalcoholic leaf extract of Pisonia grandis R.Br had significant antiulcer properties.

Coronary artery bypass grafting (CABG) is an established revascularization procedure for the treatment of advanced atherothrombotic coronary artery disease.1 The National Center for Health Statistics estimated that 427,000 procedures were performed on 249,000 patients in the ...

La enfermedad de Parkinson fue descrita por primera vez en el año 1817 por el médico inglés James Parkinson, en su “Ensayo sobre la parálisis agitante”, donde sistematizaba las descripciones clínicas de una serie de pacientes, que se caracterizaban por presentar un temblor continuo en estado de reposo, con rigidez muscular, adopción de posturas anormales y una notable lentitud en sus movimientos de carácter voluntario (bradicinesia). Todos estos síntomas comenzaban a desarrollarse entre los 50 y los 60 años de edad, y no parecían afectar a los sentidos ni a la inteligencia de las personas. Actualmente se sabe que los pacientes presentan una disminución muy importante del contenido de dopamina en el estriado, lo cual es principal responsable de la aparición de los síntomas motores característicos de la enfermedad, como temblor, bradicinesia y rigidez muscular; y también de algunos no motores, como depresión, ansiedad y trastornos del sueño y autonómicos, que pueden preceder al desarrollo de la enfermedad en varios años. En estadios avanzados pueden existir también alteraciones de la postura y del equilibrio. La oficina de farmacia es el establecimiento sanitario adecuado para formar a los pacientes parkinsonianos y promover una educación sanitaria que permita mejorar el uso de los tratamientos y prevenir los problemas relacionados con los mismos.

A novel is ligand namely 5,5'-(6-(4-methoxyphenoxy)-1,3,5-triazine-2,4-diyl)bis (azanediyl)diquinolin-8-ol (PBDQ-6)  has been prepared and characterized. This ligand was characterized by IR, 1H-NMR, and elemental analysis. Coordination polymers of this bis-ligand (NBDQ) were prepared with Cu(II), Ni(II), Co(II), Mn(II), and Zn(II) metal ions. All of these coordination polymers were characterized by elemental analyses, IR spectral and diffuse reflectance spectral studies. The thermal stability was evaluated by thermo gravimetric analyses (TGA). In addition, all of the coordination polymers have been characterized by their magnetic susceptibilities. All the novel synthesized compounds were screened for their antibacterial and antifungal activities.

Systematic management models such as anticoagulation clinics have emerged in order to optimize warfarin effectiveness and to minimize related complications. Most of these models are structured so that patients come to a clinic for in-person testing and evaluation, thus making this model of care difficult to access and time consuming for many patients. The emergence of portable instruments for measuring anticoagulant effect in capillary whole blood made it possible for patients receiving warfarin to self-monitor the effect of their anticoagulant therapy. Self-monitoring empowers patients, offers the advantage of more frequent monitoring, and increases patient convenience by allowing testing at home and avoiding the need for frequent laboratory and clinic visits. Self-monitoring can entail patient self-testing (PST) and/or patient self-management (PSM). Several studies have evaluated and shown the benefit of both PST and PSM models of care when compared with either routine medical care or anticoagulation clinic management of anticoagulation therapy. Self-monitoring (PSM and/or PST) of anticoagulation results in lower thromboembolic events, lower mortality, and no increase in major bleeding when compared with standard care. Despite favorable results and enhanced patient convenience, the adoption of self-monitoring into clinical practice in the United States has been limited, especially in higher risk, disadvantaged populations. Although the emergence of a multitude of novel oral anticoagulants will permit clinicians to better individualize anticoagulant therapy options by choosing the optimum regimen based on individual patient characteristics, it is also expected that traditional agents will continue to play a role in a significant subset of patients. For those patients treated with traditional anticoagulants such as warfarin, future models of care will entail patient-centered management such as PST and PSM. The incorporation of technology (i.e., Web-based expert systems) is expected to further improve the outcomes realized by PST and PSM. Further studies are needed to explore factors that influence the adoption of self-monitoring in the United States and to evaluate the feasibility and implementation in real-life clinical settings.

With the continuing evolution of pharmacy as a clinical profession, the need to prepare well-trained clinicians beyond the knowledge gained from a doctor of pharmacy degree program is magnified. Such training is afforded by pharmacy residency programs, which have expanded from hospital sites to practice settings as diverse as managed care organizations and public health departments. Although the resident benefits

To assess the effect of health literacy on drug adherence in the context of a pharmacist-based intervention for patients with heart failure. Post hoc analysis of a randomized controlled trial. Inner-city ambulatory care practice affiliated with an academic medical center. The original trial enrolled 314 patients with heart failure who were aged 50 years or older and were taking at least one cardiovascular drug for heart failure; 122 patients received the pharmacist intervention (patient education, therapeutic monitoring, and communication with primary care providers), and 192 patients received usual care (regular follow-up with primary care providers). We analyzed the results of 281 patients who had available health literacy and adherence data. Drug adherence was assessed over 9 months using electronic prescription container monitors on cardiovascular drugs. Health literacy was assessed using the Short Test of Functional Health Literacy in Adults (scores range from 0-36, with an ade...

A  simple,  fast  and  accurate  method  has  been  developed  for  the  estimation of  benzene content  in  Lovastatin  by  Gas  Chromatography.  The analysis was carried out on Perkin Elmer Clarus 600 GC-HS Chromatograph. The column used was DB-624 30m X 0.32 mm X 1.8 µm fused silica analytical column (6%  cyanopropylphenyl  94 %  dimethylpolysiloxane  as  a stationary  phase).The  detector  used  was  FID  detector.

A 55-year-old Caucasian man was receiving warfarin therapy after undergoing aortic valve replacement. His international normalized ratio (INR) was stabilized with warfarin 95 mg/week for 5 weeks. Commencement of a low-carbohydrate, high-protein diet resulted in a series of subtherapeutic INRs that led to a 16% increase in the dosage requirement to maintain therapeutic INRs. After the patient discontinued the diet, his INR increased, and several dosage reductions were required until his INR stabilized with his original dosage of 95 mg/week. Two additional case reports have described a possible interaction between warfarin and a high-protein diet. The potential for increased dietary protein intake to raise serum albumin levels and/or cytochrome P450 activity has been postulated as mechanisms for the resulting decrease in INRs. Given the available animal and human data that demonstrate alterations in drug metabolism in the presence of altered dietary protein intake, an increase in warfarin metabolism due to cytochrome P450 activation appears to be the most likely cause. In addition to the previously reported cases, this case indicates a potential interaction between warfarin and a high-protein diet. Because of the popularity of high-protein diets and because of the risks associated with inadequate or excessive warfarin anticoagulation, patients and health care providers should be aware of this interaction to ensure appropriate monitoring when warranted.

Carvedilol is an antihypertensive drug use for management of Hypertension. It has the half-life of 6 hr and oral bioavailability of 25% due to first pass metabolism. The total daily dose of Carvedilol is 25 mg, hence it required frequent dosing. Transdermal patches of Carvedilol were prepared for sustained release and improve bioavailability of drug and patient compliance. Different formulations were prepared by varying the amount of HPMC-K4M and Eudragit RS-100 by solvent casting method. The prepared formulations were evaluated for various parameters like thickness, tensile strength, folding endurance, % elongation, % moisture content, % moisture uptake, % drug content, In-vitro drug release, In-vitro permeation and skin irritation study. A 32 full factorial design was applied to check the effect of varying the amount of Eudragit-RS 100 (X1) and amount of HPMC-K4M (X2) on the responses i.e. tensile strength and percentage drug released in 20 hr (Q20) as dependent variables. Regression analysis and analysis of variance were performed for dependent variables. In-vitro release data were fitted to various models to ascertain kinetic of drug release. The best selected formulation is subjected to in-vitro skin permeation and skin irritation study. Batch F7 was considered optimum batch which contained 400 mg of Eudragit RS-100 and 600 mg of HPMC-K4M, showed release 95.73% up to 24 hr and was more similar to Zero order release kinetics (r2=0.982). Batch F7 showed flux of 125.8 μg/cm2/h, hence the patch area of 1.33 cm2 would be expected to deliver targeted flux of 83.72μg/cm2/h.

A new simple, accurate, precise and reproducible Ion chromatography method has been developed for the estimation of Methane sulfonic acid in Busulfan injectable dosage. The method which is developed is also validated in complete compliance with the current regulatory guidelines by using well developed analytical method validation techniques and tools which comprises with the analytical method validation parameters like Linearity, LOD and LOQ determination, Accuracy, Method precision, Specificity, System suitability, Robustness, Ruggedness etc. by adopting the current method the linearity obtained is near to 0.999 and thus this shows that the method is capable to give a good detector response, the recovery calculated was within the range of 85% to 115% of the specification limits.

The purpose of this study was to evaluate the possibility of taste masking of Levocetirizine dihydrochloride (L-CTZ) by means of inclusion complexation and ion exchange resin. Initially an attempt was given to mask the bitter taste of the drug by inclusion complexation with β-Cyclodextrin using kneading method. But from gustatory evaluation, it was found that β-Cyclodextrin was not proven good for effective taste masking. So, another attempt was given to mask bitter taste of Levocetrizine diHCl by Kyron T-114 (weak cation exchange resin). It is a water-insoluble, high molecular weight, cross linked polymer of methacrylic acid. Kyron T-114 is inexpensive and this method is simple, rapid and cost-effective method for taste masking. Ion exchange resin complex was prepared by the batch technique and various parameters viz. resin activation, drug: resin ratio, pH, temperature, swelling time and stirring time were optimized to successfully formulate the tasteless Drug Resin Complex (DRC). Maximum drug loading was obtained when the resin was activated by acid treatment, with 1:3 drug: resin ratio, soaked in water for 90 min. and stirred with the drug for 240 minutes, pH maintained 5.5 and temperature maintained 30áµ’C. Complexation was confirmed by FT-IR and DSC study. The drug resin complex was evaluated for taste in-vitro and in-vivo evaluation. The volunteers rated the complexes as tasteless and agreeable. Drug release from DRC in salivary pH was insufficient to impart bitter taste. Complete drug release was observed at gastric 0.1 N HCl (pH 1.2). Formulation of drug resin complex was confirmed by FT-IR and DSC studies.

The objective of present study was to develop pharmaceutically elegant and stable enteric coated tablet formulation for highly unstable drug in acidic environment using pH dependent polymers. Omeprazole is a specific and non-competitive inhibitor of the enzyme H+/K+-ATPase. It is unstable in conditions of low pH and required protection from the effects of gastric acid when given orally so it is formulated in the form of enteric coated dosage forms. The core tablets were prepared by direct compression method using different concentration of crospovidone as a super disintegrant. Formulations showing less disintegration time were first subcoated with HPMC 15 cps upto 3% weight gain, followed by enteric coating with Eudragit L 100, Eudragit L 100-55 and Cellulose acetate phthalate. Pre and post compression evaluation of core and coated tablets were carried out. In vitro drug release studies were conducted in acidic and basic media to determine the appropriate coating ratio. All batches enteric coated with 8% weight gain of three polymers showed stable coating in 0.1 N HCl for 2 hours. Formulated batch F11 with 7% weight gain of Eudragit L 100-55 showed stable coating in 0.1 N HCl and had shown complete drug release in phosphate buffer pH 6.8. The prepared enteric coated tablets exhibited good physical and chemical stability, when subjected to accelerated stability studies. Further, when compared to marketed formulation (OPT tablet 20 mg Omeprazole), the prepared enteric coated tablets showed excellent similarities with marketed product (with respect to drug content, disintegration time and drug release) thereby establishing bioequivalence with marketed product.

Impurity profiling is the process of acquiring and evaluating data that establishes biological safety of an individual impurity. Impurity is considered as any other organic material, besides the drug substance, or ingredients, arise out of synthesis or unwanted chemicals that remains with API’s. The control of impurities is currently a critical issue to the pharmaceutical industry. International Conference on Harmonization (ICH) formulated guidelines regarding the control of impurities. Various regulatory authorities like ICH, USFDA, Canadian Drug and Health Agency are emphasizing on the purity requirements and the identification of impurities in Active Pharmaceutical Ingredient’s (API’s). Identification of impurities is done by TLC, HPLC, The advent of hyphenated techniques has revolutionized impurity profiling, by not only separation but structural elucidation of impurities as well. The most exploited techniques, for impurity profiling of drugs are LC-MS-MS, LC-NMR, LC-NMR- MS, GC-MS, and LC-MS.

A straightforward, efficient and more sustainable solvent-free method has been developed for the synthesis of benzimidazole derivatives to achieve yields that were comparable to or better than, those in conventional media. It is noteworthy that the reaction was exclusively carried out in Zinc chloride catalysis system, rendering the methodology highly valuable from both environment and economic points of view. The various benzimidazoles were synthesized by the reaction of o-phenylenediamine with different types of aldehydes and characterized by their Physical constant, FT-IR Spectra, 1H NMR Spectra and LCMS. The excellent chemo selectivity, mild reaction condition, short reaction times and excellent yield made the best method then other methods.

An accurate, precise, simple and economical High Performance Liquid Chromatographic method for the Estimation of Bortezomib in its lyophilized dosage form has been developed. The method developed is Reverse Phase High Performance Liquid Chromatographic method using Hypersil BDS C18 column (Length: 150 mm, Diameter: 4.6mm, Particle size: 5μ) with a simple 0.1 % TFA buffer and Acetonitrile mixed in the proportion of 20:80v/v as a mobile phase, and Methanol: Water (90:10) as a diluent. The method so developed was validated in compliance with the regulatory guidelines by using well developed analytical method validation tool which comprises with the analytical method validation parameters like Linearity, Accuracy, Method precision, Specificity with forced degradation, System suitability, Robustness and Ruggedness. The results obtained were well within the acceptance criteria.

Quality by Design (QbD) refers to a holistic approach towards drug development. The purpose of research was to implement quality by design to study prospective process validation of 4 mg Salbutamol Sulphate Tablets with risk-based approach. Validation is one of the important steps in achieving and maintaining the quality of the final product. Quality Target Product Profile, Critical Quality Attributes, Critical Process Parameters, Design Space and control strategy are identified with the help of Quality Risk Management. Three initial batches of same size, method, equipment was taken for process validation. The critical parameters involved in sifting, dry mixing, preparation of granulating solution, wet mixing, drying, sizing, lubrication, compression were identified and evaluated. The formulation properties of three initial batches of process validated tablets are compared with the marketed products of Salbutamol Sulphate Tablets (Astahlin tab and Salbetol tab). Results obtained with this process validation data provides high degree of assurance that manufacturing process produces product meeting its predetermined specifications and quality attributes. The output of process validation can be used to increase productivity, its consistent quality and decreasing the need for processing and market complaints.

A lo largo del capítulo recordaremos los aspectos más relevantes de la farmacología de los fármacos antiparasitarios, haciendo especial énfasis en la localización de sus efectos en el ciclo biológico del parásito, así como en el resto de características farmacocinéticas, farmacodinámicas y toxicológicas.