Current Issue : July - September Volume : 2016 Issue Number : 3 Articles : 5 Articles
The present work deals with the development and characterization of lercanidipine hydrochloride pulsatile drug delivery system for chronomodulated therapy for improvement in therapeutic index and efficacy of lercanidipine HCl. The basic design consists of an insoluble hard gelatin capsule body, filled with eudragit coated chitosan microcapsules of lercanidipine HCl and sealed with a hydrogel plug. The entire device was enteric coated with cellulose acetate phthalate, so that the variability in gastric emptying time can be overcome and a colon-specific release can be achieved. The lercanidipine hydrochloride chitosan microspheres were prepared by emulsion cross linking method in four batches A, B, C, D by varying drug to polymer ratio and evaluated for the particle size, drug content and in-vitro release profile. From the obtained results; two better formulations were selected and enteric coated with Eudragit S-100 and Eudragit L-100 in the ratios of 1:2 by solvent evaporation method. These two enteric coated formulations were selected for further fabrication of pulsatile capsule. Different hydrogel polymers were used as plugs, to maintain a suitable lag period and it was found that the drug release was controlled by the proportion of polymers used. In-vitro release studies of pulsatile device revealed that, increasing the hydrophilic polymer content resulted in delayed release of lercanidipine HCl from microcapsules. The mechanism of drug release was found to be Korsmeyer-Peppas model for optimized formulations. FT-IR and DSC studies revealed the absence of any drug-excipients interaction. Stabilitystudies carried out on optimised microspheres showed that the microspheres remained stable during the stability period without any significant changes in their physico-chemical properties....
The aim of this research was formulation and evaluation of mucoadhesive buccal tablet of ivabradine hydrochloride for the treatment of stable angina pectoris. Ivabradine hydrochloride is an anti-anginal drug used in the symptomatic management of stable angina pectoris. It has absolute bioavailability only 40% due to extensive hepatic first pass metabolism. Mucoadhesive buccal drug delivery system will avoid first pass metabolism due to which bioavailability of drug may be improved. The drug loss will be decreased in GI tract by minimizing dissolution of drug into the saliva by designing “core in cup” design. Identification and compatibility study of drug and excipients were carried out using melting point, FTIR and DSC studies. Ivabradine hydrochloride showed λmax at 286 nm in phosphate buffer pH 6.8 and linearity was 0.9997. Core tablet was prepared with the combination of HPMC K4M and polycarbophil. Ethyl cellulose was used as a backing layer, found to be providing the desired release. Results of pre compressional and post compressional were found to be within the limits. Varying the amount of HPMC K4M and amount of polycarbophil have significant effect on mucoadhesive strength (Y1), % drug release at 6 hour (Y2) and % swelling index (Y3). Optimized batch shows Mucoadhesive strength (0.317 N), % drug release at 6 hour (96.06 %) and % swelling index (33.52 %) is desired in case of buccal drug delivery. The ivabradine hydrochloride mucoadhesive tablet is a promising approach for the effective treatment of stable angina pectoris as it provides sustained drug release....
The objective of this research work was to formulate and evaluate PEO WSR 301 bucco-adhesive tablet in combination with carbopol 934p for controlled release of sumatriptan succinate. To bypass high hepatic first pass metabolism, unidirectional bucco-adhesive tablet was selected as dosage form for the experimental work. Initially preliminary trials were carried out for the selection of excipients and their relative quantity for incorporation in the dosage form. From the results, polyethylene oxide-PEO WSR 301 (mucoadhesive polymer) and Carbopol 934p (control release) were selected as a suitable excipients for experimentation. Composition of the mucoadhesive tablet was optimized using 32 full factorial design where amount of PEO WSR 301 (X1) and amount of carbopol 934p (X2) were taken as independent variables and mucoadhesive strength, drug release at 6 hour and % swelling index taken as response variables. The formulations of design batches were characterized for post compression parameters like weight variation, hardness, thickness, friability, drug content, swelling index, ex-vivo mucoadhesive strength, surface pH, drug release at 6 hr., ex-vivo residence time and curve fitting analysis. The optimized formulation was obtained using Minitab software based on desirability value. Characterization of optimized batch was carried out by ex-vivo permeation study. From the results of meting point, DSC and FTIR study the drug and its compatibility with other excipients was confirmed. λmax of sumatriptan succinate was found to be 227 nm and linearity was 0.9995. Mucoadhesive strength and swelling index were in range of 0.25-0.43 N and 45-50 % respectively. Drug release at 6 hr. was in the range of 87-95%. The bucco-adhesive tablets of sumatriptan succinate provides good concept to bypass the extensive hepatic first-pass metabolism. Formulated tablet using PEO-WSR 301 and carbopol 934p showed good mucoadhesion, release profile, swelling index and permeation behavior. The sumatriptan succinate unidirectional bucco-adhesive tablet is a promising approach for the effective treatment of disease as it provides control drug release in 6 hr....
Solubility is an essential factor for drug effectiveness, independent of the route of administration. Poorly soluble drugs are often a challenging task for formulators in the industry. Conventional approaches for enhancement of solubility have limited applicability, especially when the drugs are poorly soluble simultaneously in aqueous and in non‐aqueous media. Drug nanosuspensions emerged as one promising solution for delivering such poorly soluble drugs. A pharmaceutical nanosuspension is defined as very finely colloid, biphasic, dispersed, solid drug particles in an aqueous vehicle, bearing size below 1 µm, without any matrix material, stabilized by surfactants and polymers prepared by suitable methods for drug delivery applications, through various routes of administration like oral, parenteral, ocular and pulmonary routes. Scaling down to nanoparticles enhances drug aqueous solubility, bioavailability and thus therapeutic efficacy by increasing drug surface area that comes into contact with biological media. These are simple to prepare and bear several beneficial aspects intended to improve in-vivo performances i.e. pharmacokinetics, pharmacodynamics, safety and targeted delivery which are discussed in this review. The present review also describes formulation criteria, different preparation methods with their merits and demerits, characterization techniques and achievements of nanosuspension in drug delivery system. Additionally, transformation of nanocrystals to final formulations and future trends of nanocrystals have also been described in this review article....
The aim of the current study was to develop self-nanoemulsifying systems (SNES) of enalapril (EN) in an attempt to improve the solubility of the sparingly soluble drug, enalapril and enhance its in-vitro release. The solubility of EN in oily phases, surfactants and cosurfactants was determined to identify the components of SNES. The SNES of EN were prepared using the oils; oleic acid, capryol 90 and labrafil M1944CS, the sufactants; tween 80 and labrasol and the co-surfactant; Transcutol HP. Pseudo-ternary phase diagrams were constructed to identify the self-emulsifying regions and to optimize emulsifier to co-emulsifier ratio and the concentration of oil. The nanoemulsion regions in the diagrams are plotted and the wider region indicated the better self-emulsification efficiency. Systems which include tween 80 and labrasol showed highest self-emulsification region when used with transcutol HP in concentration ratio (2:1). However increasing the surfactant to co-surfactant ratio to be (3:1) mostly didn’t increase the self-emulsification region. So Sys.1, Sys.2, Sys.3, Sys.4, Sys.5 and Sys.6 which contain surfactant and co-surfactant in ratio 2:1 were chosen for completing this study. The prepared SNES (Sys.1, Sys. 2, Sys.3, Sys.4, Sys.5 and Sys.6) were evaluated for their drug content, in-vitro drug release, emulsification time, dispersibility, droplet size, zeta potential and morphological study of the SNES globules. The physicochemical compatibility studies of EN and its physical mixture with different materials used in SNES preparation were carried out using DSC and FTIR analysis. It can be concluded that the optimal SNES formulae (Sys.1, Sys.3 and Sys.5) had nanometer charged particle size (10.32 to 70.65), clear appearance in dispersibility test and they released drug more than (99%) within one minute....
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