scholarly journals Preparation and Evaluation of Release Formulation of γ-Oryzanol/Algae Oil Self-Emulsified with Alginate Beads

Marine Drugs ◽  
2019 ◽  
Vol 17 (3) ◽  
pp. 156 ◽  
Author(s):  
Kai-Min Yang ◽  
Po-Yuan Chiang
Keyword(s):  
In Vitro Release ◽  
Bimodal Distribution ◽  
Alginate Beads ◽  
Controlled Delivery ◽  
Simulated Intestinal Fluid ◽  
Release Formulation ◽  
Emulsion Droplets ◽  
Algae Oil ◽  
Preparation And Evaluation

Self-emulsion improves solubility and bioavailability for γ-oryzanol/algae oil, and alginate beads can be used as controlled release carriers. In this study, self-emulsified alginate beads (SEABs) were prepared with different weight ratios of self-emulsion treatment (5%, 10%, 15%, 20%, and 30%) with alginate. We found that the microstructure with a surfactant of SEABs had a different appearance with alginate-based beads. The encapsulation of γ-oryzanol corresponded with the self-emulsion/alginate ratio, which was 98.93~60.20% with a different formulation of SEABs. During in vitro release, SEABs had the gastric protection of γ-oryzanol/algae oil, because γ-oryzanol and emulsion were not released in the simulated stomach fluid. When the SEABs were transferred to a simulation of the small intestine, they quickly began to swell and dissolve, releasing a higher content of the emulsion. We observed that the emulsion that formed had a bimodal distribution in the simulated intestinal fluid as a result of the hydrogel and emulsion droplets, leading to the formation of large aggregates. These results suggested that γ-oryzanol encapsulation within alginate beads via emulsification combined with gelation can serve as an effective controlled delivery system.

Controlled release of indomethacin from crosslinked alginate beads

e-Polymers ◽  
2008 ◽  
Vol 8 (1) ◽  
Author(s):  
Murat Inal ◽  
Mustafa Yiğitoğlu ◽  
Nuran Işiklan
Keyword(s):  
Sodium Alginate ◽  
Exposure Time ◽  
Alginate Bead ◽  
In Vitro Release ◽  
Alginate Beads ◽  
Simulated Gastric Fluid ◽  
Scanning Calorimetry ◽  
Simulated Intestinal Fluid ◽  
Release Data

AbstractBeads of the sodium alginate (NaAlg) were prepared by dropping aqueous sodium alginate (NaAlg) into glutaraldehyde (GA) as a crosslinker and HCl as a catalyst mixture solution. Beads prepared were used to deliver a model non-steroid, anti-inflammatory drug, indomethacin (IM). The beads were characterized with Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). Chemical stability of the IM after encapsulation into beads was confirmed by FTIR. SEM photograph indicated that alginate bead has spherical shape and rough surface. Preparation conditions of the beads were optimized by considering the percentage of entrapment efficiency, swelling capacity of the beads, particle size and their release data. In vitro release studies were performed in simulated gastric fluid (pH 1.2) for the initial 2 h, followed by simulated intestinal fluid (pH 7.4) for 4 h. Effects of variables such as, GA concentration, exposure time to GA, drug/polymer (d/p) ratio and percentage of HCl on the release of the IM were investigated. It was observed that, IM release from the beads decreased with increasing GA concentration, exposure time to GA, d/p ratio and percentage of HCl. The highest cumulative IM release obtained at the end of 6 h was 68% for alginate beads which were prepared with 0.5% HCl. On the other hand the least cumulative IM release obtained was to be 20 % for alginate beads which were prepared with 30 min exposure time to GA. In order to understand the crosslinking of the polymeric matrix, the molar mass between crosslinks were calculated using the swelling parameters. It was also found from the swelling experiments that swelling degree of the beads increases with increase in the temperature. The release data have been fitted to an empirical equation to estimate the kinetic parameters. The diffusion coefficient was also calculated for the transport of the drug through the polymeric beads. Values of these parameters were found to be consistent with the release data.

scholarly journals Preparation and Evaluation of Controlled Release Calcium Alginate Beads Containing Mefenamic Acid

2019 ◽  
pp. 9-16
Keyword(s):  
Mefenamic Acid ◽  
Calcium Alginate ◽  
In Vitro Release ◽  
Alginate Beads ◽  
Release Profile ◽  
Calcium Alginate Beads ◽  
Eudragit S100 ◽  
Percentage Yield ◽  
Preparation And Evaluation

The present study was designed to investigate the effects of different variables on the release profile of mefenamic acid from calcium alginate beads formulated using modified emulsification method. Five formulations of beads (F1-F5) with different drug: polymer ratios were prepared in which the amount of drug (1g) was kept constant and the amount of calcium alginate was increased from 1 up to 5g. All the formulated beads were evaluated for percentage yield, entrapped efficiency and in vitro release profile at pH 1.2 and 7.2 dissolution media. For further minimize the release of drug from calcium alginate beads, the selected formulation F3 beads were coated separately with 3% and 6% Eudragit S100 solution using dipping method. The coated beads (F6 and F7) minimized the release of drug both in pH 1.2 and 7.2. The study confirms significant effects of two variables, drug:polymer ratio and coating on the release of drug from beads which can be effectively utilized to control the release from prepared calcium alginate formulations.

scholarly journals Preparation and evaluation of novel galantamine hydrobromide sustained-release capsule

2016 ◽  
Vol 11 ◽  
pp. S82-S91 ◽  
Author(s):  
Shuoye Yang
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
In Vitro Study ◽  
Release Process ◽  
Release Formulation ◽  
Sustained Release Formulation ◽  
Promising Alternative ◽  
Release Studies ◽  
Preparation And Evaluation

In present study, a novel galantamine hydrobromide sustained-release capsule was prepared with the extrusion-spheronization method and the optimized preparative formulation. The release studies were performed using marketed capsules (Razadyne ER) as a reference and data were analyzed in terms of cumulative release amounts as a function of time. Furthermore, fiber-optic real time detection was adopted to monitor the release process. Results demonstrated that our developed formulation had superior properties, worked better as sustained-release carriers and lasted longer time to release compared with the marketed product. The in vitro release characteristics of different batches of preparations were quite similar with each other, the total release proportions of galantamine hydrobromide from sustained-release capsules reached higher than 90% within 12 hours. Similar factors f2 of two preparations were all higher than 50, the release profile of drugs from capsules fitted to Higuchi model with the equation of Q% = 0.2681t1/2 + 0.0684 (r = 0.9966). Pharmacokinetics profile and parameters in beagle dogs after oral administration also revealed the superior release performances of new capsules being consistent with the in vitro study. The developed sustained-release formulation may be a promising alternative dosage form for treatment of related diseases. 

Formulation and Evaluation of Ophthalmic Antibacterial Gels and Comparison of Different Polymers Using Factorial Design

2020 ◽  
Vol 3 (3) ◽  
pp. 01-07
Author(s):  
Alka Ahuja
Keyword(s):  
Factorial Design ◽  
Drug Delivery Systems ◽  
In Vitro Release ◽  
Hydroxypropyl Cellulose ◽  
Eye Drops ◽  
Eye Infections ◽  
Preparation And Evaluation ◽  
Vitro Release ◽  
Ophthalmic Solutions

Different formulations for the treatment of eye infections are usually administered in the form of conventional ocular drug delivery systems which are topical eye drops or ointments (1). Typically ophthalmic bioavailabilities of only 1–10% are achieved due to the short precorneal residence time of ophthalmic solutions. (2) The preparation and evaluation of gel containing antibiotic azithromycin combined with different polymers like Carbopol, sodium alginate and Hydroxypropyl cellulose (HPC) was done and assessed to find out which polymer could best be used in preparing ophthalmic gels for this antibiotic using factorial design. Since the efficacy of these gels is dependent on factors like viscosity and pH, the polymers in these gels were also examined for different parameters such as pH, in vitro release, permeation and microbiological evaluation.

scholarly journals Preparation and Evaluation of Intravaginal Ring Containing Drospirenone

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
Ying Zhang ◽  
Chun-Xiao Li ◽  
Mei-Ying Ning ◽  
Xue-Yan Duan ◽  
Ying Liu
Keyword(s):  
Light Exposure ◽  
In Vitro Release ◽  
Tissue Level ◽  
Strong Light ◽  
Reservoir System ◽  
The Matrix ◽  
Reservoir Type ◽  
Preparation And Evaluation ◽  
Effective Contraceptive

In the present study, we investigated the feasibility of the vaginal administration of drospirenone silicone IVR. The in vitro release characteristics of matrix-type and reservoir-type IVR were compared under sink conditions in 21 days. At the same time, API excipients compatibility and preformulation study was performed by HPLC, IR, and DSC methods. Biocompatibility of reservoir system was evaluated by tolerability on tissue level in rats. It was found that, under strong light exposure, high temperature, and high humidity conditions, drospirenone and excipients had no significant interactions. The daily release of reservoir-type IVR was about 0.5 mg/d sustaining 21 days, which significantly decreased the burst effect compared with the matrix system. When drospirenone was modified by the PVPk30 in the reservoir system formulation, the daily release rate increased to 1.0 mg/d sustaining 21 days. The cumulative release of reservoir-type IVR was fitted to zero release equation. In addition, biocompatibility of drospirenone IVR system in this dosage is safe. It is feasibility feasibile to further developed for safe, convenient, and effective contraceptive drug delivery with reduced dosing interval.

scholarly journals Development of coated beads for oral controlled delivery of cefaclor: In vitro evaluation

2013 ◽  
Vol 63 (1) ◽  
pp. 31-44 ◽  
Author(s):  
Bazigha K. Abdul ◽  
Sahar A. Fahmy
Keyword(s):  
Antimicrobial Activity ◽  
Controlled Release ◽  
Dosage Form ◽  
Size Range ◽  
Alginate Beads ◽  
Controlled Delivery ◽  
Peg 400 ◽  
Maximum Value ◽  
Plasma Profile

The aim of the present study was to develop and characterize coated chitosan-alginate beads containing cefaclor as a controlled release delivery system. Coated cefaclor beads were prepared by solvent evaporation techniques. Beads were found to be intact and spherical in shape. Their size range was 1.05 to 2.06. The loading efficiency showed maximum value when the concentration of cefaclor, chitosan and PEG 400 was 10 % (m/V), 0.5 % (m/V) and 2 % (V/V), respectively. Best retardation of cefaclor release from chitosan-alginate beads was achieved by coating with 15 % of shellac in formula F19. A significant antimicrobial activity (p < 0.05) against Staphylococcus aureus and Klebsiella pneumoniae was observed for formula F19 compared to the standard antibiotic disc. Furthermore, the simulated plasma profile showed the superiority of F19 in sustaining drug release for more than 12 h. Therefore, shellac coated chitosan-alginate beads could be considered a successful controlled release oral cefaclor dosage form.

scholarly journals DEVELOPMENT AND COMPARISON OF ORALLY INHALABLE SUSTAINED RELEASE FORMULATIONS FOR THREE RESPIRATORY DRUGS FOR ASTHMA

2016 ◽  
Vol 12 (25) ◽  
pp. 5679-5699
Author(s):  
K.Sathish Kumar ◽  
C. Kumaresan ◽  
R. Anantharaj
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Solvent Evaporation Method ◽  
Release Formulation ◽  
Sustained Release Formulation ◽  
Montelukast Sodium ◽  
Ambroxol Hydrochloride ◽  
Vitro Release ◽  
Respiratory Drugs

The present work was designed to develop and compare orally inhalable sustained release formulation for salbutamol sulphate (SS), ambroxol hydrochloride (AH) and montelukast sodium (MS).The emulsion solvent evaporation method was used to prepare microparticles with the polymers. The prepared polymer encapsulated microparticles were blended with carrier inhalable lactose and filled in size 3 hard empty gelatin capsule. Formulations T1-T9 were prepared with 1:1 ratio of PLGA (50:50), PLGA (75:25) and Eudragit RS100. The formulation T1 prepared with SS:PLGA (50:50) produces best result when compared with other formulations T2-T9. Formulation T1 gives in vitro release 91.23% at 12 h and having particle size of microparticles (D0.5 µm) 1.94±0.6 and respiratory fraction 34.9± 2.59 %.

scholarly journals IN VITRO RELEASE STUDIES OF CARBAMAZEPINE TABLETS AND BENZOYL METRONIDAZOLE SUSPENSIONS USING THE FLOW-THROUGH CELL APPARATUS AND SIMULATED GASTROINTESTINAL FLUIDS

2017 ◽  
Vol 9 (4) ◽  
pp. 54 ◽  
Author(s):  
Jose Raul Medina ◽  
Jonathan Hernandez ◽  
Marcela Hurtado
Keyword(s):  
In Vitro Release ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Dissolution Time ◽  
Intestinal Fluid ◽  
Simulated Intestinal Fluid ◽  
Release Studies ◽  
Flow Through ◽  
Vitro Release

Objective: To characterize the in vitro release of carbamazepine tablets and benzoyl metronidazole suspensions using the flow-through cell apparatus and simulated gastrointestinal fluids.Methods: Tegretol® tablets, Flagyl® suspension, and generic formulations of each were tested. Release studies were performed using an automated flow-through cell apparatus. Simulated gastric fluid (with and without pepsin) and simulated intestinal fluid (without pancreatin) at 16 ml/min and fasted state simulated intestinal fluid at 8 ml/min, all at 37.0±0.5 °C, were used as dissolution media. The quantity of dissolved carbamazepine and benzoyl metronidazole was determined at 5-min intervals until 60 min at 285 and 278 nm, respectively. Percentage dissolved at 60 min, mean dissolution time, dissolution efficiency values, and t10%, t25%, t50% and t63.2% were calculated. Mean values for all parameters were compared between the reference and generic formulations using Studentʼs t-test. Dissolution data were fitted to different kinetic models.Results: Simulated gastric fluid without pepsin showed no discriminative capability for carbamazepine tablets. Significant differences were observed between the reference and generic formulations for almost all parameters (*P<0.05). In some cases, the logistic model best described the in vitro release of both drugs.Conclusion: Using an apparatus and media that best simulates the gastrointestinal environment, we identified differences in the rate and extent of dissolution of both drugs that could help to optimise the design of interchangeable formulations. Based on the physicochemical characteristics of carbamazepine and benzoyl metronidazole and the conditions in which the formulations were tested, these differences could be of clinical relevance. 

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