Current Issue : January - March Volume : 2011 Issue Number : 1 Articles : 17 Articles
The aim of this study was to prepare amoxicillin tri-hydrate (AMXT) granules in the form of single dose (125mg) sachet for pediatric use. A 33 full factorial design to select the best disintigrant, diluent and lubricant, followed by a 23 factorial design for the selection of the optimum excipient concentration as well as the most appropriate techniques for the preparation of drug granules were performed. Finally a complexation study using ßCD (β-cyclodextrin) or HPßCD (Hydroxy propyl β-cyclodextrin) was done. The best formulae obtained from the factorial design, based on the flow ability properties (Angle repose), saturated solubility study and release after 5 minutes from the prepared granules were further investigated after complexation with CD (cyclodextrins). Results showed that optimized amoxicillin tri-hydrate 125 mg sachet in the formation with the composition: 44%Avicel PH101, 1%Mg.Staerate, 5%Ac.Di.Sol and 1:3 AMXT: HPßCD complexation using freeze drying showed an increased solubility and stability of amoxicillin tri-hydrate and thus can be used as a single dose sachet dosage form replacing the currently available drug suspension for pediatric use....
Emerging technological knowledge is leading research into new ventures. Synthetic polymers frequently suffer from the problem of being non-biocompatible, non-biodegradable and expensive. During the past two decades significant advances have been made in the development of natural polymer alone or in combination with synthetic polymeric materials for biomedical applications. Biodegradable polymers are highlighted in their performance in terms of biocompatibility. Therefore in this review we have made an attempt to summaries a role of polymers with potential applicability in medical and pharmaceutical field. Cheap and abundant availability of natural polymers offers an opportunity for its use. Biocomposites with low toxicity can be prepared with natural (collagen) and a synthetic polymer [poly (e-caprolactone)]. In order to overcome biological deficiency and to enhance mechanical characteristics of natural polymers a combination with synthetic polymers or derivatives of natural polymers are utilized. Combination of advantageous properties of natural polymers and hydroxyapatite has been explored in bone defects. It shows application in bacteria preservation. In bio-applications, biocompatibility and/or biodegradability of triglyceride oils play an important role therefore during the 21st century number of polymers are synthesized and evaluated for possibility of utilizing such methods for various applications....
Elimination of unwanted side-effects, especially transfusion-transmitted diseases (HIV and hepatitis) and leucocytes-mediated allosensitisation is an important goal of modern transfusion medicine. The problems and high cost factor involved in collecting and storing human blood and the shortages of blood contributed towards the development of artificial blood. Even though artificial blood does not qualify as perfect red blood cell substitutes but, have many potential clinical and non clinical usages. Artificial blood is designed for the sole purpose of transporting oxygen and carbon dioxide throughout the body. The most promising blood products under development as blood substitutes are perflourocarbons and haemoglobin based oxygen carriers. Perflourocarbons are long chain compounds having oxygen carrying capacity. The haemoglobin based oxygen carrier’s works on haemoglobin’s unique oxygen binding capacity and the lack of blood type antigen. Depending on the type of artificial blood, it can be produced in different ways using synthetic production, chemical isolation, or recombinant biochemical technology....
The free radicals are having much importance in the body and which they lead to cell degradation via different path ways. To avoid the free radical interaction with the cells in the body the spin trapping agents normally nitraso compounds are used to trap them later which they leads to formation of Spin adduct easily excreted by the body. The current research concerned with the cell line analysis to investigate cytotoxicity extent determination by MTT assay. The cell lines initially subjected to the MTT assay to determine the cytotoxicity effect of PBN spin trap on the cell lines...
The objective of the present research work was to formulate and optimize the solid lipid nanoparticles of carvedilol by full factorial design. Solid lipid nanoparticles of carvedilol have been developed to enhance oral bioavailability and sustain release of carvedilol. A 32 factorial design was utilized to optimize the formulation where the concentration of lipid tripalmitin (X1) and concentration of surfactant poloxamer 188 (X2) were taken as independent variables. SLNs were prepared by hot homogenization followed by ultrasonication method. Prepared SLNs were evaluated for morphology, mean particle size, zeta potential and in vitro drug release. The mean particle size and zeta potential values are in range of 50–210 nm and 8 mV respectively. In vitro release studies were performed in phosphate buffer pH 6.8 with 30% PEG 400. Percent of drug released in 5h and 24h, t50% and diffusion exponent were taken as the dependent variables. Polynomial equations and response surface plots were generated for all dependent variables using multiple regression analysis. It was observed that both the factors had significant influence on all dependent variables studied (p<0.05). The results indicating that release of the drug was primarily influenced by concentration of tripalmitin....
PURPOSE: The aim of the study was to formulate different proportion of Lamivudine: Methocel K15M with mannitol formulations, in order to investigation the effect of polymer proportion and diluent (mannitol and avicel) on the drug release mechanism. Lamivudine, an anti-HIV agent, was used as a model drug to evaluate its release characteristics from different matrices. METHOD: Matrix tablets of Lamivudine were prepared by direct compression process using methocel K15M CR polymer mannitol and avicel as filler. In vitro release studies were performed using US Pharmacopeia type 1 apparatus (basket method) in 900 ml of pH 1.2 and pH 6.8 phosphate buffer at 100 rpm for 8 hours. Scanning Electron Microscopy (SEM) was used to evaluate and surface properties of the matrices. Drug release was analyzed according to their kinetic models. A One-way analysis of variance (ANOVA) was used to interpret the result. RESULTS: Statistically significant differences were found among the drug release profile from different formulations. Higher proportion of polymeric content (30% of the total tablet weight) in the matrix, release was extended > 8 hours due to increased tortuosity and decreased porosity. At lower proportion of polymeric content (10% of the total tablet weight), the rate of drug release was elevated. Two formulations showed drug release is more controlled. The release mechanism was explored and explained with zero order, first order, Higuchi and Korsmeyer and Hixon-Crowell equations. CONCLUSION: The release kinetics was found to be governed by the type and content of the excipients (polymer or filler, mannitol). By suitable modulation could be developed controlled delivery of such type of drug....
Extended release capsules provides prolonged periods of drug in plasma levels there by reduce dosing frequency and improve patient compliance. Acetazolamide is a carbonic anhydrase inhibitor used in the treatment and management of cardiac oedema, glaucoma etc. Acetazolamide ER capsules provide prolonged action to inhibit aqueous humor secretion for 18 to 24 hours after each dose, whereas conventional tablets act for only 8 to 12 hours. Acetazolamide ER capsules were formulated using methocel K4M premium CR Hydroxy Propyl Methyl Cellulose (HPMC), methocel E10M premium CR HPMC, ethocel 10EP and ethocel 100 EP as matrixing agents. Acetazolamide capsules were prepared by direct filling method. Granules of acetazolamide were formulated by wet granulation method and filled into capsules by using hand filling capsule machine. Lubricated blend (granules) of acetazolamide was evaluated for bulk density, tapped density, % compressibility index and hausner’s ratio. Formulated capsules were evaluated for uniformity of weight, assay, in-vitro drug release studies and stability studies. Inclusion of ethocel 10EP and ethocel 100EP failed to control the release of drug, but inclusion of methocel K4M and methocel E10M the rate of drug release was controlled. The release profile was excellent and the burst release observed from the capsules containing pure drug (75.3%) at the end of first hour was overcome with methocel K4M and methocel E10M. It is concluded that the desired drug release pattern can be obtained by using methocel K4M premium CR HPMC compared to ethocel grades. The drug release followed first order kinetics and controlled by diffusion mechanism. The drug release was affected by concentration of methocel K4M premium CR HPMC....
The aim of the present investigation was to prepare and evaluate ofloxacin controlled release subgingival films using biodegradable calcium alginate prepared in situ. The equipment necessary for the present investigation was fabricated and employed for casting of sodium alginate subgingival films. Subgingival films of drug:polymer (10:90, 25:75, 50:50 and 75:25) were prepared using solvent casting method. A 10%w/v CaCl2 solution was used for converting sodium alginate into calcium alginate and gelation of the films. As polymer concentration is increased the smoothness of the films increased. The thickness of films varied from 135±0.5 to 292±1.3μm which is well below the recommended thickness (<300 µm) of the subgingival films. The average weight of the films was found to be between 15.32±1.04 and 22.07 ±0.49 mg. The percentage of drug content ranged from 41.64±0.41to 58.22±0.41%. The low values may be due to loss of drug during treatment with CaCl2 solution. In vitro release studies showed that all the films had an initial burst release for the first 8 h, followed by controlled release of ofloxacin (>3.0 µg/ml) up to 120 h which is sufficient to inhibit the growth of the micro-organisms. The rate of drug release was inversely proportional to polymer concentration in the formulations. The low K1 and ‘r’ values obtained may be due to biphasic drug release pattern. The formulations did not fit into Higuchi equation because of low values of <0.640846which indicate that the drug release might be due to diffusion only in second phase of dissolution. All the films have shown to have integrity even after 5 days of dissolution studies. The formulations O1 and O2 which contain 90 and 75%w/w of polymer could be employed for controlled delivery of ofloxacin for 5 days in subgingival infections. Calcium alginate, being a biodegradable polymer is a good choice in the present study....
Present study elaborates on development and evaluation of floating–pulsatile drug delivery system intended for chronotherapy in hypertension. Novel floating–pulsatile concept was applied to increase the gastric residence of the dosage form having lag phase followed by a burst release. To overcome limitations of various approaches for imparting buoyancy, we generated the system, which consisted of three different parts, a core tablet containing the active ingredient, an outer shell and a top cover buoyant layer. The coated tablet consists in a drug-containing core, coated by a hydrophilic polymer, which is responsible for a lag phase and their by of pulsatile release. The floating layer was optimized using different concentration of Methoce1 K100M and sodium bicarbonate, which provides buoyancy to increase the retention of the oral dosage form in the stomach. The effect of the different hydrophilic polymer with different viscosity grade and their combination in different ratios on the lag time and drug release was investigated. Developed formulations were evaluated for their buoyancy and dissolution. The results showed that the drug release after certain lag time was mainly due to the erosion of the dry coated layer. Floating time was controlled by the quantity and composition of the buoyant layer....
Hyaluronan (Hyaluronic acid or HA), is a polyanionic polysaccharide that consists of N-acetyl-D-glucosamine and β-glucoronic acid these being linked together through alternating 1, 4 and 1, 3 glycosidic bonds. The chemical and physicochemical properties of HA and its physiological role in humans, together with its versatile properties, such as its biocompatibility, non-immunogenicity, biodegradability and viscoelasticity, have proved that it is an ideal biomaterial for cosmetic, medical and pharmaceutical applications. HA is a polyanionic polymer that can form complexes with drugs and stabilize drug formulations. HA’s viscoelastic matrix can act as a strong biocompatible support material. A relatively simple chemical structure allows HA to be further modified to create a wide range of possible drug delivery carriers. The purpose of this review is to describe briefly the physical and chemical properties of HA together with some details of its pharmaceutical uses with emphasis on this more recent Trans dermal application....
This technique facilitates the movement of ions across a membrane under the influence of an externally applied electric potential difference, is one of the most promising physical skin penetration enhancing method. The rationale behind using this technique is the capability of this method to increase the systemic delivery of high molecular weight compounds with controlled input kinetics and minimum inter-subject variability, which is otherwise achieved only when parentral route of administration is used. Recently, good permeation of larger peptides like insulin has been achieved through this technique in combination with chemical enhancers. This review briefly describes the factors which affect Iontophoretic drug delivery and summarizes the studies conducted recently using this technique in order to achieve higher systemic absorption of the drugs having low passive diffusion otherwise. The effect of permeation enhancers (chemical enhancers) on Iontophoretic flux of drugs has also been described. Present review also provides an insight into reverse Iontophorosis. Various parameters which affect the transdermal absorption of drugs through Iontophorosis like drug concentration, polarity of drugs, pH of donor solution, presence of co-ions, ionic strength, electrode polarity etc. have also been reviewed in detail....
In this review, the formation, characterization, properties and applications of nano-emulsions are reviewed and summarized. Nanoemulsions are submicron sized emulsions that are under extensive investigation as drug carriers for improving the delivery of therapeutic agents. Nanoemulsions are the thermodynamically stable isotropic system in which two immiscible liquid (water and oil) are mixed to form a single phase by means of an appropriate surfactants. Due to their small droplet size nano-emulsions possess stability against sedimentation or creaming with Ostwald ripening forming the main mechanism of nanoemulsion breakdown. Nanoemulsion droplet sizes fall typically in the range of 20-200nm. Diameter and surface properties of droplets of nanoemulsion plays an important role in the biological behavior of the formulation. Nanoemulsion show great promise for the future of cosmetics, diagnostics, drug therapies, and biotechnologies. The main application of nanoemulsions is the preparation of nanoparticles using a polymerizable monomer as the disperse phase (the so-called miniemulsion polymerization method) where nanoemulsion droplets act as nanoreactors. Another interesting application which is experiencing an active development is the use of nanoemulsions as formulations, namely for controlled drug delivery and targeting....
Carvedilol (BCS Class II drug) is a nonselective β-adrenergic blocking agent with α1-blocking activity and it is mainly used in the management of hypertension. Carvedilol has been found to form inclusion complexes with β-Cyclodextrins. The present study was undertaken to determine a suitable method for preparing Carvedilol- β-Cyclodextrin inclusion complexes. Carvedilol- β-Cyclodextrin inclusion complexes were prepared at a molar ratio of 1:1, 1:2 and 1:3 by physical mixing, kneading and solvent evaporation methods. In vitro dissolution studies were carried out in 0.1N HCl. All the methods of preparation of complexes were found to be useful in increasing the solubility of Carvedilol except solvent evaporation method where the rise in solubility is not significant. Kneading method at both 1:2 and 1:3 molar ratios was found to be equally effective in improving the solubility of Carvedilol. In vitro dissolution study data indicated that inclusion complexes prepared by kneading method in 1:2 molar ratios were suitable for improving the solubility of Carvedilol....
Current study was undertaken to improve the solubility of glibenclamide, a poorly water soluble drug. Physical mixtures, kneading mixtures or solid dispersions were prepared using shatavari as solubility enhancer at 1:1, 1:3, 1:5, 1:7 & 1:9 drug to carrier weight ratio. The resulting systems were subjected to solubility analysis and in vitro dissolution studies. X-ray diffraction, Infrared Fourier Transform Spectroscopy (FTIR) and differential scanning calorimetry were used to characterize the resulting systems. The solid dispersions of glibenclamide with drug carrier ratio at 1:9 showed superior dissolution rate of 46.05 % when compared with pure drug (3.27 %). This impressive improvement in dissolution is attributed to lower energy required for the dissolution due to amorphous form of the drug, glibenclamide....
A multiple unit floating drug delivery system based on gas formation technique was developed, in order to prolong the gastric residence time& to increase the overall bioavailability of the dosage form. Pioglitazone is a thiazolidinedione antidiabetic agent that depends on the presence of insulin for its mechanism of action .The drug is having short biological half life (3 to 7 hrs); hence it is suitable for formulating floating microcapsules. Floating microcapsules of pioglitazone were prepared by orifice ionic gelation technique by dispersing the drug together with sodium carbonate in an aqueous solution of sodium alginate and then dripping the dispersion into an acidified solution of calcium chloride. The CO2 developed from the reaction of carbonate salts with acid, caused the desired buoyancy to float beads on the dissolution fluids. In the present work, the effect of concentration of sodium alginate,CaCl2,acetic acid & sodium carbonate, volume of curing solution and curing time on drug entrapment efficiency & in vitro release of pioglitazone was studied with a view to develop floating microcapsules for pioglitazone. Formulated microcapsules were evaluated for floating lag time, total floating time, % drug entrapped and in-vitro drug release. The drug entrapment efficiencies were in the range of 44-95.7%. The microcapsules formulated using 35 % w/v sodium alginate, 1.5% v/v acetic acid, 500 mg sodium carbonate, 50 ml of 10% w/v calcium chloride with curing time 60 min yielded the drug release up to 10 hrs and showed entrapment efficiency up to 93%....
The present research aims at synthesis of diclofenac amino compounds, their corneal transport through mammalian cornea and characterization of screened compound. Four diclofenac amino acid compounds were synthesized named as Diclofenac Glycine compound (DGC), diclofenac histidine compound (DHC), diclofenac Arginine compound (DAC) and diclofenac lysine compound (DLC) and screened for in-vitro corneal transport through excised goat cornea using modified franz diffusion cell and also compared with 0.1% w/v diclofenac sodium aqueous solution (DS). DAC showed maximum transport through cornea. It was further characterized for physical properties, melting point, TLC, FTIR, DSC and XRD. The results suggested during synthesis process diclofenac free acid reacts with arginine and formed a complex having differed properties. The compound thus formed showed better permeation across cornea as compared to DS and physical mixture of diclofeanac and arginine and seems to show active transport phenomenon. Formation of amino acid compound of the diclofenac showed better permeability as compared to its corresponding salt....
A fullerene is also allotrope of carbon molecule composed entirely of carbon, in the form of a hollow sphere, ellipsoid, or tube Fullerenes may be classified in two different catagories: Exohedral (inside the cage) and Endohedral(outside the cage). Fullerenes are soluble in organic solvent such as benzene, toluene and chloroform. Fullerenes are useful in various allergic reactions, MRI contrast agent and water purification. Researchers have found that water-soluble derivates of fullerenes inhibit the HIV-1 protease (enzyme responsible for the development of the virus) and are therefore useful in fighting the HIV virus that leads to AIDS....
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