Current Issue : July-September Volume : 2015 Issue Number : 3 Articles : 8 Articles
Nanofibers with diameters in the nanometer range have attracted for designing of drug delivery systems due to large surface areas per unit mass, porosity, low density so we can applied in advance application such as controlled drug delivery systems. Nanofibers are an exciting class of material produced using an innovative manufacturing process technology. Hence, nanofibers are considered for use as sensors, air and liquid filtration, energy storage, composite, aerospace, battery separators etc. Nanofibers also produced from natural or synthetic polymers on the basis of their desired properties. Although there are many methods of fabricating nanofibers, electrospinning is the most versatile process. The fabricated nanofibers are characterized by geometrical characterization including scanning electron microscopy, transmission electron microscopy, Atomic force microscopy then chemical characterization, particle size, drug entrapment in nanofibers through conventional techniques and instruments. The fabricated nanofibers can be used in novel drug delivery as a platform to load desired drug....
The objective of present work was to formulate floating pulsatile microspheres of ivabradine hydrochloride intended for chronopharmacotherapy of angina pectoris. Floating pulsatile concept was applied to increase the gastric residence of the dosage form having a lag phase during floating in acidic medium followed by burst release in basic medium. These microspheres were prepared by non aqueous solvent evaporation technique using Eudragit S100 which is a pH dependent polymer that gets solubilized at pH 7 and above. Ivabradine hydrochloride is categorized as If channel antagonist, water soluble drug and was selected as model drug for treatment of angina pectoris which rely on circadian rhythm. Moreover it has short half life (2 hours), it undergoes extensive first pass metabolism. All these factors contribute to formulate ivabradine hydrochloride as floating pulsatile microspheres. These microspheres were evaluated for micromeritic properties, particle size, entrapment efficiency, in-vitro floating ability, drug release and kinetics of microspheres. The optimized formulation exhibited good entrapment efficiency, flow properties, floating property and released the drug at right time by maintaining required lag phase and followed first order kinetics....
The aim of the present investigation was to formulate and evaluate stable ketoconazole organogel preparation to increase the solubility of ketoconazole and release the drug for prolonged period of time. Ketoconazole was dissolved in clove oil. The required amount of the tween 80 and PEG 400 was added to the clove oil containing propyl paraben. Subsequently, water containing methyl paraben was added drop-by-drop to the organogelator solution with constant stirring on magnetic stirrer until there was a formation of clear microemulsion. Carbopol 934 was used as a gelling phase, slowly mixed with microemulsion in 1:1 ratio with constant and uniform stirring to get milky white homogeneous organogel. Formulated organogels were evaluated for their physical appearance, pH, viscosity, globule size, drug content, spreadability, extrudability, in-vitro and ex-vivo drug release, antifungal activity and stability. Organogel carrying ketoconazole showed good physical appearance, acceptable skin pH (6 - 6.8), non-newtonian pseudoplastic system, drug content (99.68�±0.19), globule size (572 nm), spreadability (21.67�±0.034 gm.cm/sec), good extrudability, in-vitro release (98.75�±0.32 %), ex-vivo release (73.45�±0.86 %) for optimized batch. Skin irritation study did not showed any irritation reaction and possess a good anti-fungal activity. The optimized batch OG3 showed better drug release as compared to marketed cream. Similarly ex-vivo release of formulation showed better drug release through mice skin as compared with marketed cream (KT CURE). The formulations followed zero order kinetic model followed by higuchi mechanism. Thus, results of the current study clearly indicated a promising potential of the ketoconazole organogel as an alternative to the conventional dosage form....
Azithromycin Dihydrate is an antibiotic useful for the treatment of bacterial infections. It is a BCS class II drug and its bioavailability is about 40-45%. The present aim of this formulation was to formulate solid self-emulsifying drug delivery system to improve the solubility and bioavailability of azithromycin dihydrate. The liquid (SEDDS) consisted of clove oil as oil phase, tween 20 as surfactant and ethanol as co-surfactant. Oil, surfactant and co-surfactant were selected on the basis of solubilization capacity of drug and emulsification ability of surfactant and co-surfactants. The formulations were optimized by constructing the pseudo-ternary phase diagram. The liquid formulation was solidified by adsorption technique, using magnesium hydroxide as solid carrier. There are many techniques to convert liquid SMEDDS to solid, but an adsorption technique is simple and economic. Drug releases from S-SMEDDS were found to be significantly higher as compared with that of plain azithromycin dihydrate. Study concluded that S-SMEDDS can effectively formulated by adsorption technique with enhanced dissolution rate and concomitantly bioavailability....
Rizatriptan (RZT) is a potent anti migraine drug having agonist activity at the 5-hydroxytryptamine (5-HT) 1B and 5-HT 1D receptor used in treatment of migraine. In the present study, an attempt has been made to prepare fast dissolving film of RZT using eudragit E PO as a taste masking agent and film forming polymer. Various grades of HPMC 5 cp, 15 cp and 50 cp were selected as film former for immediate release of drug for this study. PEG 400 and glycerin were used as plasticizer. Film is prepared by solvent casting/evaporation technique and prepared film was evaluated for various parameters like thickness, folding endurance, disintegration test taste acceptability, tensile strength and drug release study. Mouth dissolving film containing RZT showed all the properties such as tensile strength, % percentage elongation, in-vitro disintegration and in-vitro dissolution characteristics within the limit without any type of imperfection. Drug release profile showed 100% within 10 min. The immediate drug release profile indicates that it could be successfully used to cure migraine attack without need of water for immediate release of drug. The mouth dissolving films was found superior in palatability and patient convenience than the tablets. It is suitable for pediatrics and elderly patients due to its convenience....
The purpose of the present study was to develop oro‐dispersible tablet containing rizatriptan benzoate using natural, synthetic and ion exchange resin superdisintegrants. Migraine is a common headache disorder that imposes a substantial burden on both the individual patient and society. Typically, migraines are intense with >80% of patients describing their pain as severe. Rizatriptan benzoate is a potent and selective 5-HT1B/1D receptor agonist and is effective for the treatment of acute migraine. Conventional rizatriptan benzoate tablets available in market are not suitable where quick onset of action is required, the enzymatic degradation in the gastrointestinal tract and first-pass metabolism in the liver can be avoided. Thus, mouth dissolving tablets can potentially achieve high bioavailability and rapid onset of desirable action in a convenient manner. To provide the patients with the most conventional mode of administration, there was a need to develop rapidly disintegrating dosage form, particularly one that disintegrates and dissolves/disperses in saliva and can be administered without need of water. Hence orodispersible tablet was formulated by direct compression that can be administered orally to get rapid onset of action. A total 9 batches (F1-F9) were formulated using three categories of superdisintegrants viz. natural, synthetic and ion exchange resin in three different concentrations. To mask the bitter taste of drug, aspartame is added as sweetener. The tablets were prepared by direct compression technique. Thickness, hardness, friability, weight variation, disintegration test, in-vitro dissolution study and uniformity of content were evaluated for each formulation and found satisfactory. Natural superdisintegrants, gives a rapid disintegration and high release as compared to synthetic superdisintegrants in formulation of orally disintegrating tablet of rizatriptan. The drug release of the optimized batch (F6) obtained was 95.6% within 15 min which is higher than the marketed conventional tablet. Optimized batch is evaluated for masking of bitter taste using E-tongue....
In the modern day the mucoadhesive drug delivery systems have gained popularity for the various reasons. The highly permeable buccal mucosal membrane attracting many researchers to explore the possibilities administering drugs via buccal mucosa to get better bioavailability by avoiding first pass hepatic metabolism. Buccal dosage forms are mainly used to reduce the overall dose of drug and thus the dose related side effects can be reduced. Various dosage forms like tablets, films, patches, wafers, semisolid gels and lozenges are developed by using different mucoadhesive polymers. The dosage forms can be evaluated by properties like physical properties, mucoadhesive strength, tensile strength, swelling index, folding endurance, in-vitro drug diffusion and dissolution studies. Number of buccal formulations have been developed and are being marketed across the world....
The main objective of present study was prepation of Zaltoprofen loaded gelatin nanoparticles (Z-GNP) by nanoprecipitation to sustained release of Zaltoprofen from its nanoparticulate carriers. The zaltoprofen loaded gelatin nanoparticles (Z-GNP) were prepared by nanoprecipitation method. (Z-GNP) were characterized by particle size, entrapment efficiency, drug loading, yield of nanoparticles, Qualitative determination of crosslinking efficiency, Scanning electron microscopy(SEM), differential scanning calorimetry (DSC), in–vitro drug release studies, fourier transform infrared (FT-IR) spectroscopy. The particle size, entrapment efficiency and drug loading of (Z-GNP) of optimized formulation (GN 5) was found to be 352 nm, 73.11%, 27.19% respectively. In-vitro drug release in phosphate buffer saline (pH 7.4) was maximum (63.45%) in 48 hrs. and shows sustained release action. Glutaradehyde used to cross-link the gelatin nanoparticles and Qualitative determination of crosslinking efficiency by Potentiometric titration. The principle parameters studied for its optimum conditions were the ratio of drug, surfactant and polymer was found to be 0.48:32:1. The pluronic F-127 used to prevent aggregation of gelatin nanoparticles generally observed in previous two step desolvation method. The result of DSC and FTIR were compared with reference gives no chemical interaction and stability of zaltoprofen in gelatin nanoparticles. It can be confirmed that, the drug (Zaltoporfen) release from gelatin nanoparticles was sustained in 7.4 pH buffer....
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