Santosh

In the present study, an attempt was made to prepare and evaluate matrix tablets of Ondansetron HCl using HPMC, EC and Eudragit for Sustained release of Ondansetron HCl. The matrix tablets were prepared by wet granulation method. All the formulations are evaluated for the Hardness, Friability, Weight variation, Drug Content, In-Vitro Drug Release. The weight variation and drug contents of all the tablets were found to be uniform with the low SD values. The FTIR study indicated that the drug is stable in the formulations. The prepared matrix tablets were capable of releasing the drug for 12 hours depending upon the formulation variables. The tablets prepared with HPMC and Eudragit combination have shown higher drug release Drug release mechanism followed non-Fickian transport from both the polymers matrices. The drug released from the formulation is depends on the concentration of the polymers.

Oxalis corniculata Linn. (Oxalidaceae) is one of the important medicinal plants used traditionally for the treatment of fever, pain and inflammation. The present study was aimed to screen antipyretic activity of petroleum ether, chloroform, ethyl acetate, methanol extracts and β-sitosterol isolated from petroleum ether extract of Oxalis corniculata Linn. The leaves of Oxalis corniculata Linn. was used for successive extraction with increasing polarity solvents. Petroleum ether extract was selected for activity-guided fractionation to isolate β-sitosterol due to its better efficacy than other extracts. Antipyretic activity was done by yeast induced pyrexia method. All the extracts were screened at the dose of 100 mg/kg, i.p. and isolated β-sitosterol was screened at the dose of 10 and 20 mg/kg. The result showed that after five hour of petroleum ether extract (100 mg/kg) administration significant inhibition of pyrexia up to 89.5% was observed. Isolated β-sitosterol 10 and 20 mg/kg, i.p. showed promising antipyretic activity with inhibition of pyrexia by 91.23 and 94.41% respectively. Results are compared with standard drug paracetamol (50 mg/kg i.p.). Thus the present pharmacological screening provides support for the folklore claim of antipyretic activity of Oxalis corniculata Linn.

Creature models are urgent for comprehension the system of neuropathic painand improvement of powerful treatment for its ideal administration. A battery of neuropathic torment models has been produced to reproduce the clinical agony conditions with different etiology. The present audit thoroughly examines the procedure, behavioural adjustments, limits, and focal points of around 40 diverse creature models of neuropathic pain alongside their changes. Improvement of these models has helped tremendously in understanding the interminable pain and underlying fringe and focal pathogenic instruments. Moreover, scrutinize has brought about the improvement of new helpful operators for neuropathic agony administration, and the preclinical information acquired utilizing these creature models have been progressively meant powerful torment administration in clinical setup likewise. As every creature model has been made with particular strategy and results have a tendency to change to a great extent with the slight progressions identified with strategy, along these lines, it is vital that information from distinctive models ought to be accounted for and deciphered in the connection of the particular torment model.

Thiophene a five member heterocycles had been found with enormous biological activities with the suitable modifications in the structure. The present review is an attempt made to direct the attention of the researchers towards the thiopene ring for the development of newer chemical entities which are quite useful in the treatment of various life threatening diseases and disorders This review article covers the most active thiopene derivatives that have shown considerable biological actions such as antimicrobial, anti-inflammatory. This review also discusses the structure-activity relationship of the most potent compounds. It can act as an important tool for medicinal chemists to develop newer compounds possessing thiopene moiety that could be better agents in terms of efficacy and safety

A well developed and validated RP – HPLC method by UV- detection was used for the determination of Gatifloxacin in human plasma with metronidazole as internal standard. Solid phase extraction was involved in the process. The drug and the internal standard were eluted under isocratic mode using a 150 X 4.6 mm i.d, 5 µm Phenomenex ODS 2 C18 column. The mobile phase composed of a mixture of 5:95 % v/v methanol and 20mM mixed phosphate buffer (pH 3.5± 0.05) at a flow rate of 1.4 mL/Minute. The detection wave length of the detector was 268 nm. A volume of  50 µL was injected and the runtime of the method was 9 minutes. The method showed good linearity in the range of  50.1 to 7000.9 ng/mL. The recovery of gatifloxacin was 92.42 % with a standard deviation of 1.533 and recovery of internal standard was 87.6 %. The LOD of Gatifloxacin was 50.1 ng/mL. Matrix effects were not observed.

In this paper an attempt is made to prepare IPN beads of the drug by taking alginate solution in combination with a polymer (PVA/Kennel powder /Guar gum). The prepared copolymer solution is dropped in to 2% CaCl2. The beads are hardened by cross linking with a common cross-linking agent, glutaraldehyde. The beads are characterized by Fourier transform infra-red spectroscopy and scanning electron microscopy. Additionally quality control tests such as swelling index, bead water uptake, entrapment efficiency and drug release studies are performed. The extent of cross-linking is studied in terms of the size and release characteristics of the beads. Most of the formulations indicated erosion based release pattern. The size of the beads ranged from 250 to 400 µm. The entrapment efficiency of the formulation ranged from 73.6% to 94.50%.  

The present investigation has been undertaken with aim to formulation and evaluation of etoricoxib gel with different gelling agent and different penetration enhancer. Etoricoxib is highly selective cyclooxygenase-2 (COX-2) inhibitor. In this present study gel with carbopol, HPMC and Na-CMC as gelling agent prepared with different penetration enhancer like propyl glycol, oleic acid. Menthol oil. Formulation were evaluated for pH, stability study, spreadibilty, extrudabilty, bioadhesive (ex-vivo), skin irritation, viscosity, appearance and In-vitro drug diffusion. The formulation of Etoricoxib topical gel was prepared using carbopol, HPMC and Na-cmc in three batches A, B and C. With the consideration of all formulation characteristic and parameter we selected batch-A formulation for further study of anti-inflammatory and anti-analgesic activity. It was concluded that the Etoricoxib gel formulation containing carbopol with increase concentration of propyl glycol 10% and 2% oleic acid (OA) was suitable for topical application and it shows comparable result with market product and shows much better result of formulation, anti-inflammatory and anti-analgesic activity.

The aim of this study was to prepare Diclofenac potassium (DP) microspheres by using Double Emulsion-solvent evaporation method with ethyl cellulose (EC) and Eudragit polymers. An attempt was made to formulate a sustained release dosage form of diclofenac potassium, to minimize frequent dosing as well as reducing or eliminating local side effects by avoiding the drug release in the upper gastro-intestinal tract Poly vinyl alcohol containing 2% (w/w) span 80 was the external phase and polymer -drug solution was the internal phase. EC and Eudragit were used to encapsulate diclofenac potassium. By using different formulation variables, six different formulations (F1, F2, F3, F4, F5, & F6) were prepared. The resulting microspheres obtained, were more spherical in shape and showed more entrapment efficiency. The size of the microspheres varied between 346-695 μm and as high as 96.24% loading efficiency for Eudragit and 82.34% for EC was obtained. In vitro release study was carried out in 0.1 N hydrochloric acid solution (pH 1.2) for first 2 hours followed by in phosphate buffer solution (pH 6.8) for next 4 hours. After first 2 hours of dissolution in 0.1 N hydrochloric acid, EC microspheres released 23% of drug and Eudragit released 7% of drug. The formulations were found to be effective in providing controlled release of drug for a longer period of time.

Conventionally, drugs are released in an instant or absolute manner. Nevertheless, in current days, Pulsatile Drug Release Systems (PDRS) are gaining upward attention. Pulsatile delivery is defined as the rapid and transient release of certain amounts of drug molecules within a short time period immediately after a predetermined off-release period, i.e., lag time. PDRS can be classified in single and multiple pulse systems. This system provides spatial and temporal delivery of the drug. These systems are designed according to the circadian rhythm or biological clock of the body. These deliver the drug at the right time and at the right place and in the right amount thus increasing patient compliance. Pulsatile systems are beneficial for drugs where night time dosing is required, such as anti-asthmatic and anti-arrhythmic drugs where the disease severity is time dependent. This concept has several advantages, notably maximum therapeutic benefit, minimum harm, improved patient convenience and compliance. Pharmacists must realize the need to develop and dispense such medications having potential therapeutic benefit. The current article focuses on the diseases requiring PDDS, methodologies involved for the existing systems, and PDDS product currently available in the market.

QSAR analysis on a set of heterocyclic derivatives for antifungal activity was performed by using multiple regression procedure. The activity contribution of these compounds was determined from regression equation and the validation procedure to analyze the predictive ability of QSAR model was described. High agreement between experimental and predicted inhibitory values was obtained. The results of this study indicate that the parameter has a significant effect on antifungal activity of this class of compounds, thus simplifying design of new biologically active molecules.