ABSTRACT
Abstract The study is aimed to develop a monolithic controlled matrix transdermal patches containing Metoclopramide as a model drug by solvent casting method. Eudragit L100, Polyvinylpyrrolidone K-30, and Methylcellulose were used in different ratios and Polyethylene glycol 400 added as a plasticizer. Resulting patches were evaluated for their physicochemical characters like organoleptic characters, weight variation, folding endurance, thickness, swelling index, flatness, drug content, swelling index, percentage erosion, moisture content, water vapor transmission rate and moisture uptake. Formed patches were also evaluated through Fourier transform spectroscopy (FT-IR), X-ray diffraction (XRD), Differential Scanning calorimetry (DSC) and Scanning Electron Microscopy (SEM). Results of SEM unveiled smooth surface of drug-loaded patches. In-vitro dissolution studies were conducted by using dissolution medium phosphate buffer saline pH 7.4. Effect of natural permeation enhancers was elucidated on two optimized formulations (Z4 and Z9). Different concentrations (5%-10 %) of permeation enhancers i.e. Olive oil, Castor oil and Eucalyptus oil were evaluated on Franz diffusion cell using excised abdominal rat skin. Z4-O2 (Olive oil 10%) had enhanced sustain effect and flux value (310.72) close to the desired flux value. Z4-O2 followed Higuchi release model (R2= 0.9833) with non-fickian diffusion release mechanism (n=0.612)
Subject(s)
Spectrum Analysis/methods , Oils, Volatile/analysis , Metoclopramide/agonists , X-Ray Diffraction/instrumentation , Calorimetry, Differential Scanning/methods , Microscopy, Electron, Scanning/methodsABSTRACT
Losartan potassium is a water soluble antihypertensive agent with short half-life. Controlling its release will improvepatient compliance. The benefit will be extended for geriatric patients if the developed system was liquid. The objectiveof this work was to develop controlled release oral liquid losartan potassium. This employed a combination of in situgelation and coating drug particles with pH-dependent polymer (Eudragit® L100). Solid dispersion (SD) prepared at1:1, 1:1.5, and 1:2 drug : polymer ratios, respectively. Sodium alginate solution was loaded with either pure drug orSD, in presence and absence of 1% w/v chitosan. These systems were evaluated for the drug release using continuouspH variation study. Alginate formulation with pure drug underwent in situ gelation in the gastric conditions but lost thegelling strength in the intestinal phase with burst drug release. Loading the formulation with SD resulted in controlleddrug release both in the gastric and intestinal phases. Increasing eudragit concentration in SD decreased the drugreleased with total release efficiency of 62.1%, 53.0%, and 41.7%. Incorporation of chitosan at reduced further drugrelease rate reaching 21% at the higher eudragit concentration. The study provided the formulator with a range of oralliquid formulations for controlled release of losartan potassium.
ABSTRACT
The present study was aimed at preparation of transdermal patches of tizanidine HCl, evaluation of the effect of polymers on in vitro release pattern of the drug, and the effect of permeation enhancers on the penetration of the drug through the rabbit skin. Various proportions of hydrophilic (HPMC) and hydrophobic (Eudragit L-100) polymers were used with PEG 400 as film-forming agent, and Span 20 or DMSO as permeation enhancer. The formulations were assessed for physicochemical characteristics and in vitro drug release studies using USP paddle over disc method in phosphate buffered saline (pH 7.4) at 32.0±1°C. On the basis of in vitro studies and physicochemical evaluations, S03-A and S04-A were selected at Eudragit : HPMC ratios of 8 : 2 and 7 : 3, respectively, for further ex vivo analysis. The effects of different concentrations of Span 20 and DMSO were evaluated on excised rabbit skin using Franz diffusion cell. Cumulative drug permeation, flux, permeability coefficient, target flux, and enhancement ratio were calculated and compared with the control formulations. Kinetic models and Tukey's multiple comparison test were applied to evaluate the drug release patterns. Formulation SB03-PE containing Eudragit L-100:HPMC (7:3) with Span 20 (15% w/w) produced the highest enhancement in drug permeation, and followed zero order kinetic model with super case-II drug release mechanism.
Subject(s)
Animals , Rabbits , Transdermal Patch/classification , Transdermal Patch/supply & distribution , In Vitro Techniques , Pharmaceutical Preparations/analysis , Hydrophobic and Hydrophilic Interactions , Drug Liberation/drug effectsABSTRACT
Omeprazole (OMZ) is a weak base proton pump inhibitor and it can be easily broken down in the acidic location before reaching to the small intestine where it is absorbed. Therefore, the main aim of this investigation is to protect the drug in the stomach environment with the object of exhibiting 100% drug release at the site of absorption. Prior to coating all the capsules were filled with API and other suitable excipients then placed on to the lab model conventional coating pan. Two different polymers such as (HPMC) and Eudragit L 100 were selected for this study. First, the pre coating solution (HPMC) was employed after drying enteric coating solution (Eudragit L 100) was applied under suitable coating parameter finally over coating solution of (HPMC) was applied and kept for drying. Different coating thickness ranges from 38.33 to 89.75% was observed by Scanning electron microscopy and tested for acid uptake test, disintegration and dissolution tests in pH 1.2 HCl media for 2 hours and pH 6.8 phosphate buffer solution. Less coating thickness capsules were allowed to penetrate the acid and the capsules were ruptured in an acid environment, therefore early drug release was occurred in acid media. Whereas capsules with high coating thickness of 89μm were not allowed acid to penetrate this indicates that the drug could be protected from degradation in the gastric environment.
ABSTRACT
The present study was an attempt to formulate and evaluate enteric coated tablets for Ilaprazole to reduce the gastrointestinal tract side effects. Four formulations of core tablets were prepared and one who shows rapid disintegration (near around three minutes) was selected for enteric coating. Ilaprazole which have an irritant effect on the stomach can be coated with a substance that will only dissolve in the small intestine. Enteric coat was optimized using two different polymers such as HPMCP 50 and Eudragit L 100 in different concentrations. The prepared tablets were evaluated in terms of their pre-compression parameters, physical characteristics and in-vitro release study. 2.5% seal coating on core tablets was optimized and 9% enteric coating on seal coated tablets was performed using HPMC P 50 (60%), triethyl citrate (10%) and IPA:DCM (60:40) which gives the highest dissolution release profile and f2 value.
ABSTRACT
Objective: To prepare the baicalin-Eudragit L100-55 (EL) enteric coated solid dispersion and to investigate the feasibility of this baicalin preparation. Methods: Baicalin-EL enteric coated solid dispersion was prepared by using solvent evaporation method. The microscopic structure and physicochemical properties of solid dispersion were analyzed using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray powder diffraction (XRD), and infrared vibrational spectra (IR). And its in vitro release was also investigated. Results: DSC and XRD analyses suggested that baicalin may be present in enteric coated solid dispersion as amorphous substance. IR results indicated the presence of interactions between baicalin and EL. The in vitro release showed the accumulated dissolution rate of baicalin was less than 3% in artificial pH 1.2 dilute hydrochloric acid solution for 2 h, but an accumulated dissolution rate exceeding 90% in pH 6.8 phosphate buffer solution for 2 h when baicalin-EL ratio reached 1:6. Conclusion: Baicalin-EL enteric coated solid dispersion prepared could release drug rapidly and increase local drug concentration and then improve the oral absorption of baicalin.
ABSTRACT
The present study was an attempt to formulate and evaluate enteric coated tablets for Ilaprazole to reduce the gastrointestinal tract side effects. Four formulations of core tablets were prepared and one who shows rapid disintegration (near around three minutes) was selected for enteric coating. Ilaprazole which have an irritant effect on the stomach can be coated with a substance that will only dissolve in the small intestine. Enteric coat was optimized using two different polymers such as HPMCP 50 and Eudragit L 100 in different concentrations. The prepared tablets were evaluated in terms of their pre-compression parameters, physical characteristics and in-vitro release study. 2.5% seal coating on core tablets was optimized and 9% enteric coating on seal coated tablets was performed using HPMC P 50 (60%), triethyl citrate (10%) and IPA:DCM (60:40) which gives the highest dissolution release profile and f2 value.
ABSTRACT
Dry suspension is commercial dry mixtures that require addition of water at the time of dispensing. The major consequence of the bitter taste is to restrict greatly the further development of oral preparations and clinical applications of these drugs. People wish to take effective drugs that have a nice taste can be administered easily. Accordingly, it is important to mask the unpalatable taste of a drug in order to improve the product quality. The solvent evaporation process is used for microencapsulation which is carried out in a liquid manufacturing vehicle. Eudragit L100 is used as taste masking agent. FT-IR study shows that there is no significant interactions occurring between drug and excipients. The suspension prepared was evaluated for various parameters like sedimentation volume, degree of flocculation, drug content and In-vitro dissolution time. All the parameters were found to be within limits. When the results were compared with marketed preparation suspension was found to be better with respect to marketed preparation.
ABSTRACT
OBJECTIVE: To investigate the properties of polyacrylic: resin Eudragit L100-Eudragit S100 (mixed at ratio of 1:4) free film and its various influencing factors. METHODS: The free film was prepared by casting method,and its solubility parameter, intrinsic viscosity, tensile strength and permeability were determined. The optimal solvent and plaslicizer were screened. RESULTS: The tensile strength of the film prepared by ethanol was maximum, and the permeability of the free film made using acetone was the highest, therefore ethanol was the optimal solvent. Plasticizer could decrease the tensile strength and increase the permeability of free film,and diethyl phthalate was the optimal plasticizer. CONCLUSION: The present investigation might be helpful for screening coating formulation and optimizing coating process.