Comparative Pharmacokinetic Study and Quantification of Ibuprofen released from Interpenetrating polymer Network Beads of Sodium Carboxymethyl Xanthan and Sodium Alginate (original) (raw)
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Journal of Applied Sciences and Environmental Management, 2017
The work aim at investigating the channeling or modulatory effects of polyethylene glycol (PEG) (MW 4000 and 6000) on drug release from ibuprofen sustained release formulation. Different batches of ibuprofen matrix granules and tablet were prepared by melt granulation using different concentrations of carnauba wax and PEG at different ratios. The granule flow properties and various tablets parameters were evaluated using standard procedures. Drug release kinetics and mechanisms from the tablets were investigated as well as DSC and FTIR drug-excipients compatibility. The granules showed increasingly close packing with increase in the amounts of PEG incorporated. All the tablets did not meet compendial specifications with regard to crushing strength and friability. The release rate and extent of release were found to be influenced by the amount of PEG used as well as the carnauba wax concentration. PEG combination of equal amounts produced the highest release of 91 % in the formulation prepared with 12.20 %w/w of carnauba wax while a 1:2 combination in tablets prepared with 24.40 %w/w of carnauba wax gave a maximum drug release of 83 %. Drug release kinetic and mechanism were most consistent with the Higuchi model hence the release was diffusion mediated. DSC and FTIR studies showed no interactions between ibuprofen and the excipients. Carnauba wax-PEG system can be used successfully as a matrix former to sustain the release of ibuprofen for over 6 h. The studies indicate that the proper balance between a matrix former and a channeling agent can produce a desired drug dissolution profile. © JASEM
Formulation of ibuprofen beads by ionotropic gelation
Iranian Journal of Pharmaceutical Research, 2010
Microencapsulation has become a common technique in the production of controlled release dosage forms. Many results have been reported, concerning the use of alginate beads as controlled release drug formulations. Alginate has a unique gel-forming property in the presence of multivalent cations, in an aqueous medium. Ibuprofen is an excellent analgesic and antipyretic, non-steroidal anti-inflammatory agent with a high therapeutic index. Formulation of ibuprofen in beads could reduce its gastric ...
Journal of Controlled Release, 1999
Controlled-release (CR) matrix tablets of ibuprofen (IBF) and Carbopol® 934P, and blended mixture of Carbopol® 934P and 971P resins, at different drug to polymers ratios, were prepared by the direct compression method. The investigation focuses on the influence of the proportion of the matrix material, and several co-excipients (lactose, microcrystalline cellulose (MCC), and starch) on the mechanism and release rate of the drug from the tablets. In vitro drug release in pH 7.2 phosphate buffer solution appears to occur both by diffusion and a swelling-controlled mechanism, exhibiting either anomalous or Case II type transport. The release process could be described by plotting the fraction released versus time and n fitting data to the simple exponential model: M /M 5kt . The release kinetics were modified when the blended mixtures of tC arbopol® 934P and 971P resins were used as the matrix materials. In general, all of the co-excipients, used in this study, enhanced the release rate of IBF. However, lactose demonstrated slower and more linear release behavior as compared to microcrystalline cellulose or starch. The dissolution T and T values for the three co-excipients were in the order of 50 90 lactose.microcrystalline cellulose.starch. report carbomer matrix tablets showed to 0168-3659 / 99 / $ -see front matter
Brazilian Journal of Pharmaceutical Sciences, 2016
A matrix system was developed that releases ibuprofen (IB) over a 12-hour period and the influence of the polymer type and concentration on the release rate of the drug was evaluated. Tablets containing different concentrations of Carbopol (CP), hydroxypropyl methylcellulose (HPMC), or ethyl cellulose (EC) were prepared using direct compression and the drug content, content uniformity, hardness, friability, dissolution performance, and in vitro release kinetics were examined. Formulated tablets were found to be within acceptable limits for physical and chemical parameters. The release kinetics of the Carbopol®971P 8% formulation showed the best linearity (r 2 =0.977) in fitting zero-order kinetics, suggesting the release rate was time independent. The drug release from tablets containing 8% CP was extended over approximately 18 hours and the release kinetics were nearly linear, suggesting that this system has the potential to maintain constant plasma drug concentrations over 12 hours, which could reduce the frequency of administration and the occurrence of adverse effects associated with repeated administration of conventional IB tablets.
Pharmacy Education, 2022
Introduction: Ibuprofen is a non-steriodal anti-inflammatory drug which shows low bioavailability. For gel preparations it is important to increase the release rate of ibuprofen by using solid dispersion systems. Objective: To obtain the optimum release rate of ibuprofen-PEG 6000 solid dispersion from gel, by optimising the gelling agent and the penetrating enhancers. Method: Determination of gelling agent was carried out by comparing the ibuprofen release flux. The gel formulation with the best release flux will be used in the determination of penetrating enhancer to obtain the optimum release flux, by using a two-factor factorial design. Result: HPMC showed the highest release flux (339.5 g/cm 2 min). The results showed an increase in the release flux (489.4 g/cm 2 min) in the optimum formula with 39.9% propylene glycol and 3.3% isopropyl myristate. Conclusion: The increase in the ibuprofen solid dispersion release flux has been carried out using HPMC, and propylene glycol-isopropyl myristate as a penetrating enhancer. Wisudyaningsih & Ameliana Effect of gelling agent and penetration enhancer on Ibuprofen-PEG 6000 Pharmacy Education 22(2) 55-59 56 This study aimed to obtain the best gelling agent and determine the combination of isopropyl myristate and propylene glycol that provided the optimum in-vitro release rate of ibuprofen solid dispersion from a gel preparation using a factorial design.
Journal of Controlled Release, 1998
In order to assess the potential of carbopol 974P-NF as matrix material in hydrophilic matrix tablets containing a slightly ® water-soluble drug, ibuprofen (IBF), controlled release matrix tablets of ibuprofen and carbopol 974P-NF, at different drug to polymer ratios, were prepared by the direct compression method. The influence of the concentration of the matrix material ® (carbopol 974P) and several co-excipients (lactose, microcrystalline cellulose, and starch) on the release rate of the drug was investigated. An in vitro dissolution test in pH 7.2 phosphate buffer solution showed that drug release from all the ® formulations containing carbopol 974P was considerably prolonged in concentration-dependent manners. Increasing the ® amount of carbopol 974P in tablets resulted in a reduction in the drug release rate and a linearization of the drug release curve. When the influence of the co-excipients on the release of the drug was examined, all of the co-excipients used in this study enhanced the release rate of IBF. However, lactose demonstrated slower and more linear release behavior as compared in microcrystalline cellulose or starch. The dissolution T and T values for the three co-excipients were in the order of 50 90 lactose.microcrystalline cellulose.starch.
Evaluation of the Release Profiles of Ibuprofen Formulated.pdf
Purpose: To investigate the sustained release characteristics of ibuprofen lipospheres made from Capra hircus (GF) and carnauba wax (CW) in comparison with conventional granules as standard. Methods: Ibuprofen (90 g) and the lipid (30 g) were prepared by melt dispersion technique. Conventional granules of ibuprofen were prepared with starch mucilage, 20% w/v. Resulting lipospheres were characterized with respect to sizes, flow property, bulk and tap densities, encapsulated in hard gelatin capsules and evaluated for drug release profiles. Results: Dissolution profile for lipospheres were a maximum drug release of 97% in 1 hr (conventional granules), 23% in 4 hr (GF), 60% in 2 hr (CW) and 40% in admixtures of fats (GC). Admixing the fats enhanced flow properties of the lipospheres. Inclusion of a surfactant enhanced the release profiles from the lipospheres. Conclusion: Formulation of ibuprofen into lipospheres modified the release profile, which has implications in the formulation of...
Journal of Controlled Release, 1999
Controlled-release (CR) matrix tablets of ibuprofen (IBF) and Carbopol® 934P, and blended mixture of Carbopol® 934P and 971P resins, at different drug to polymers ratios, were prepared by the direct compression method. The investigation focuses on the influence of the proportion of the matrix material, and several co-excipients (lactose, microcrystalline cellulose (MCC), and starch) on the mechanism and release rate of the drug from the tablets. In vitro drug release in pH 7.2 phosphate buffer solution appears to occur both by diffusion and a swelling-controlled mechanism, exhibiting either anomalous or Case II type transport. The release process could be described by plotting the fraction released versus time and n fitting data to the simple exponential model: M /M 5kt . The release kinetics were modified when the blended mixtures of tC arbopol® 934P and 971P resins were used as the matrix materials. In general, all of the co-excipients, used in this study, enhanced the release rate of IBF. However, lactose demonstrated slower and more linear release behavior as compared to microcrystalline cellulose or starch. The dissolution T and T values for the three co-excipients were in the order of 50 90 lactose.microcrystalline cellulose.starch. report carbomer matrix tablets showed to 0168-3659 / 99 / $ -see front matter
International Journal of pharma and Bio Sciences, 2019
The goal of any drug delivery system is to provide a therapeutic amount of drug to the proper site in the body to achieve promptly and then maintain the desired drug concentration. The drug-delivery system should deliver drug at a rate dictated by the needs of the body over a specified period of treatment. A number of systems containing hydrophobic and waxes were fabricated with drugs in to dosage forms with the aim of sustaining drug levels and hence drug action for an extended period of time. 3 Sustained release Sustained release systems include any drug delivery system that achieves low release of drug over an extended period of time sustained drug action at a determined rate by maintaining a relatively constant, effective drug level in the body with concomitant minimization of undesirable side effects. Site specific targeting In site specific targeting, the target is adjacent to or in the diseased organ or tissue. 2. Embedding the drug in a matrix 3. Coating the drug or dosage form containing the drug 4. Forming complexes of the drug with materials such as ion exchange resins. Partition coefficient and molecular size Partition coefficient and molecular size influence not only the permeation of a drug across the biological membranes, but also diffusion across or through a rate-controlling membrane or matrix. Drugs with extremely high partition coefficient (i.e., very oil-soluble) readily penetrate the membranes but unable to proceed further, while drugs with excessive aqueous solubility, i.e., low oil/water partition coefficients cannot penetrates the membranes. A balance in the partition coefficient is needed to give an optimum flux for permeation through the biological rate controlling members. Biological half-life The usual goal of an oral sustained release product is to maintain therapeutic blood levels over an extended period. To achieve this, drug must enter the circulation at approximately the same rate at which it is eliminated. The elimination rate is quantitatively described by the half-life(t1/2). Each drug has its own characteristic elimination rate, which is the sum of all elimination process, including metabolism, urinary excretion, and all other processes that permanently remove drug from the blood stream. Therapeutic compounds with short half-lives are excellent for sustained release preparations, since this can reduce dosing frequency. However, this is limited, in that drugs with very short half-lives may require excessively large Distribution The distribution of drugs into tissues can be an important factor in the overall drug elimination kinetics since it not only lowers the concentration of circulating drug but it also can be rate limiting in its equilibration with blood and extra cellular fluid. In the bound portion of a drug can be considered inactive and unable to cross membranes. Encapsulation dissolution control These methods generally involve coating individual particles or granules of drug with a slowly dissolving material. The coated particles can be compressed directly into tablets as in space tabs or placed in capsules as in the spanule products. Matrix dissolution control The reduced drug solubility plus larger particle size can be used to modify available rates. There is an upper restriction on the size of particles one can employ for the oralzoute while the low solubility approach will produce a changing dissolution are as the area for dissolution decrease. An alternate Reservoir devices In this system, a water insoluble polymeric material encloses a core of drug .Drug will partition in to the membrane and exchange with the fluid surrounding the particle or tablet. Additional drug will enter the membrane. Diffuse to the periphery, and exchange with surrounding media. 11 As important parameter in above equation is the partition coefficient which is defined as the concentration of drug in membrane over all concentration drug in the core. If the partition coefficient is high. The core will depleted of drug in a short time so that zero order release will be observed only over short segment of the time course of drug release. 10 1.5.3. Diffusion and dissolution controlled systems: The main feature is that the drug core is enclosed with a partially soluble membrane. Dissolution of part of the membrane allows for diffusion of the continued drug through pores is the polymer coat. The release profile of drug from this type of product can be described by the following equation: Release rate = AD(C1-C2)/1 important to the rate of diffusion, In addition, the amount of solvent in the matrix of the resin, as well as the structural rigidity of the resin, i.e. cross-linking, also influences the drug diffusion rate. For this reason, the porosity of the resin and the size of the bead of particle must be carefully controlled during the formulation process. 11 Drug release is triggered by penetration of eluting media into the matrix dissolving the drug, thereby creating channels through which diffusion takes place. A High tortuosity means that the effective average diffusion path is large. The porosity items takes in to account the space available for drug dissolution; an Higuchi' equation: Q = K2t ½ (3) Where Q is the amount of drug release at time t, and k 2 is the diffusion rate constant. 12 SOLID DISPERSION The term solid dispersion refers to a group of solid products consisting of at least two components, generally a hydrophilic matrix and a hydrophobic drug. ➢ Particles with higher porosity ➢ Drugs in amorphous state. Disadvantages of solid dispersion Though they increase the bio-availability of the drugs by increasing the solubility, their commercial use has been limited primarily because of • Recently, a method of measurement of viscosity of dissolution medium as the polymer dissolves from the solid dispersion as used to know the amount of drug release. This is Micro viscometry techniques(MVT). 20 Figure 2: Schematic representation of the bioavailability enhancement of poorly water soluble drug by solid dispersion technique. 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