Current Issue : July - September Volume : 2014 Issue Number : 3 Articles : 9 Articles
The objective of this research was to improve the trans-tympanic invasive delivery of ciprofloxacin, a synthetic fluoroquinolone antibiotic, to the middle ear, attempting to treat acute otitis media (AOM) ototopically. In order to achieve this goal, ciprofloxacin spanlastics were prepared by thin film hydration (TFH) technique, using several edge activators (EAs). The prepared vesicles were evaluated with respect to their entrapment efficiencies (EE %) in order to select an optimal formulation, which was subjected to further investigations (measuring the particle size (PS), polydispersity index (PDI), zeta potential (ZP), deformability index (DI), in-vitro release and ex-vivo permeation). Results revealed that the optimal formulation (composed of Span 60 and Brij 35 as an EA at weight ratio of 80: 20) showed EE % of 51.81 %, PS of 287.55 nm, PDI of 0.47, ZP of - 24.35 mV and DI of 3.90 g. in addition, it exhibited high ex-vivo drug flux through ear skin when relative to the marketed product (Ciprocin® drops). Accordingly, spanlastics could be a promising approach for improving trans-tympanic delivery....
Carvedilol is an antihypertensive drug used for management of hypertension. It has short half-life and less oral bioavailability due to first pass metabolism. Hence, it required frequent dosing. The present study was aimed to formulate reservoir-type patch of carvedilol and establishment of correlation between ex-vivo and in-vivo drug release. Transdermal patches of carvedilol were prepared to sustain the drug release and to improve the bioavailability of drug and for patient compliance. Reservoir-type transdermal formulations were prepared by varying the amount of eudragit RL 100 and eudragit RS 100 employing solvent casting method. A 32 full factorial design was applied to check the effect of eudragit-RL 100 (X1) and eudragit RS 100 (X2) on the responses i.e. tensile strength, percentage drug released in 20 hr (Q20) and diffusion coefficient (n) as dependent variables. In-vitro release data were fitted to various models to ascertain the kinetic of drug release batch F1 was considered optimised batch and it was subjected to ex-vivo study and in-vivo study. The bioavailability studies in wistar rats indicated that the carvedilol loaded transdermal patches provided steady-state plasma concentration and improved bioavailability in comparison to oral administration. Area under the curve from time 0 to t (AUC0–t) values of in-vivo data to the ex-vivo cumulative amounts delivered were compared and level A correlation was observed....
Atenolol nasal microspheres were prepared by using the emulsion cross linking technique. As the drug atenolol has 6-\r\n7 hrs half life it was formulated in the form of sustained release. Chitosan was used as polymer. Different cross linking agent\r\nglutaraldehyde and sodium tripolyphosphate were used in the preparations of microspheres. Among them sodium\r\ntripolyphosphate was found to be the better choice as the cross linking agent to attain the optimum result. Among the ratios\r\nprepared 1:3 ratio of core:coat is found to be the best ratio. The best formulation was selected on the basis of % entrapment\r\nefficiency and in-vitro drug release studies....
Diabetes mellitus, being one of the most prevalent disease in India, generally accompanied with major complications like heart attack, cardiomyopathy, stroke and peripheral vascular disease. These conditions account for most morbidity and mortality among middle-aged and older people. Cardiovascular disease is the leading cause of death in individuals with type 2 diabetes. The low compliance and high cost are the major hindrance blocks for multiple drug therapy. The main objective of this research work was to develop optimized bilayer tablets of metformin HCl and amlodipine besilate as twice a day formulation to overcome the problems associated with multiple drug therapy. The drug choice for type-2 diabetes mellitus was metformin HCl and for prevention of diabetes associated CVS complications was amlodipine besilate. The formulations of tablets were prepared by using three matrix forming polymers such as HPMC K15M and HPMC K100M for SR tablets and two super disintegrating agents such as crospovidone and croscarmellose sodium. Various formulation batches were prepared by applying 32 factorial designs for both SR layer and IR layer. Bilayer tablets were prepared from optimized SR and IR layer and then extensively evaluated for in-vitro release behavior for 12 hr. The current investigation concluded that metformin HCl and amlodipine besilate can be incorporated in bilayer tablets, which may successfully improve patient compliance by reducing dose....
The objective of the present research work was formulation and evaluation of sublingual film containing nanoparticles of prochlorperazine maleate to get quick disintegration for rapid release and onset of action in the treatment of chemotherapy induced nausea and vomiting. For dissolution rate enhancement, nanosuspension of prochlorperazine maleate was prepared using high speed homogenizer. This nanosuspension was casted in the petridish. HPMC E 5-LV and SDS were used as a stabilizer in nanosuspension. HPMC E 5-LV used as film forming polymer and PEG 400 used as a plasticizer. Nanosuspensions were evaluated for parameters like particle size, PdI and zeta potential. Sublingual films were evaluated for physical characterizations, thickness, surface pH, disintegration time, tensile strength, folding endurance, drug content, in-vitro drug release, ex-vivo permeation study and taste masking study. In this research, release profile depends on the concentration HPMC E-5 LV. 32 factorial design was applied to check the effect of concentration of HPMC E-5 LV (X1) and PEG 400 (X2) on the dependent variable i.e. % in-vitro drug release Y1, disintegration time (sec) Y2 and tensile strength Y3. ANOVA was performed for dependent variables. From D.O.E 9.0.1 software F5 concluded as optimized batch which contains HPMC E 5-LV (250 mg) and PEG 400 (20% w/w of HPMC E 5-LV). The studies indicating that dissolution rate increase by film containing nanoparticle of drug and quick disintegrating film can efficiently be formulated of prochlorperazine maleate by using solvent casting technique....
The objective of present study was to formulate and evaluate ambroxol hydrochloride sustained release pellet by extrusion spheronization technique for minimize fluctuation in plasma drug concentration with better patient compliance. Sustained release pellets prepared using xanthan gum and guar gum in different concentration. In 32 factorial designs xanthan gum (X1) and guar gum (X2) were selected as independent variables and drug release in two hrs (Q2) (Y1) and Q12 (Y2) were dependent variables. All formulations were evaluated for angle of repose, bulk density, tapped density, carr’s index, % friability, % yield, drug content and drug release. Optimized formulation was evaluated for one month stability study. The optimization study indicates that % drug release in 2 hrs (Q2) and in 12 hrs (Q12) depends on concentration of xanthan gum and guar gum. Regression analysis and analysis of variance were performed for dependent variables. Formulation F4 containing 5% of xanthan gum and 15% of guar gum was optimized. It showed 32.79% drug release in two hrs and 98.67% drug release at 12 hr. The studies indicate that the sustained release pellets can be efficiently formulated for ambroxol hydrochloride by extrusion spheronization. The optimized formulation was subjected to stability studies for one month at 40°C temperature with RH 75±5% and showed there was no significant change in drug content, physicochemical parameters and release pattern....
Gastroretentive drug delivery systems have shown to be of better significance in controlling release rate for drug having site specific absorption. The purpose study was to develop an optimized dual retard floating tablet of amlodipine besylate and atenolol using optimization technique. Dual retard floating tablet comprised of two layers, i.e immediate release layer of amlodipine besylate and sustained release layer of atenolol. Immediate release layer comprised of different superdisintegrant like sodium starch glycolate, cross carmellose sodium and kyron T-314. Formulation containing 4% Kyron T-314 as a superdisintegrating agent was selected as optimized formulation which release 99.86% of amlodipine besylate within 30 min. Sustained release layer comprised of different polymers like HPMC K4m, HPMC K15M and HPMC K100M. Formulation containing 10% HPMC K100M was selected as optimized which release 90% of drug within 12 hours. Gas generating approach was used for floating purpose. A 32 factorial design was employed in formulating the GRFDDS with conc. of HPMC K100M (X1) and sodium bicarbonate (X2) as independent variables while xanthan gum was added to maintain matrix integrity. FLT, Q15, T50, T75 and Q360 were selected as dependent variables. The granules were characterized by FTIR and DSC studies. There was no incompatibility observed between them. There was no significant change observed after following ICH stability guideline....
The aim of this study was to produce gliclazide loaded eudragit® L100-55 microparticles by coacervation technique in order to achieve pH responsive drug release using hydroxypropyl methycellulose (HPMC) as stabilizer and Poloxamer 407 as surfactant. The effect of enteric polymer: HPMC ratio on properties of microparticles was investigated with regard to particle size distribution, morphology, yield, encapsulation efficiency, in-vitro drug release profiles and interaction between gliclazide and eudragit® L100-55. Average % drug entrapment efficiency was seen in all microparticles. Particle diameter increased when the enteric polymer content was higher relative to HPMC. In-vitro dissolution studies demonstrated that the drug release from the microparticles was dependent upon enteric polymer: HPMC ratio and particle size distribution. At the ratio of at least 3:1 of enteric polymer: HPMC, drug release was suppressed most significantly in low pH (hydrochloric acid as medium) while rapid drug release was observed in pH 7.4....
Genipin crosslinked gelatin microspheres of gliclazide were developed through simple coacervation phase-separation method. Effect of drug: polymer ratio (gliclazide: gelatin ratio and concentration of genipin) on swelling index (%), drug release at t50 (min.) and particle size (µm) were optimized using 32 factorial design. The swelling index was within the range of 90.8±0.10 to 326.8±0.12%. The in-vitro drug release (t50) from the microspheres (151.23±0.30 to 605.52±0.31 over 12 h (720 min.)) was followed controlled release (Higuchi) pattern (r2 = 0.933 to 0.992) with super case-II transport mechanism. The average particle size of microspheres was within 16.25 to 28.5 µm. The microspheres were also characterized by SEM, XRD, DSC and FTIR. The % yield, drug loading and entrapment efficiency were also influence by drug: polymer ratio. These data demonstrate that drug release rates from gelatin microspheres may be sustained and extended by controlling the degree of crosslinking with genipin....
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