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1.
The effect of sodium bicarbonate (SB) on the swelling behavior and the sustained release of floating systems was studied with varied proportions of this excipient and metronidazole. Two polymers with different hydration characteristics, Methocel K4M and Carbopol 971P NF, were used to formulate the matrices. Under in vitro dissolution conditions, the addition of SB to metronidazole sustained-release tablets modifies the matrix hydration volume, increasing at the beginning, reaching a maximum, and then declining. Pure Carbopol matrices show a rapid hydration with a limited further effect of the SB and metronidazole loads. Methocel show a significant increase of the apparent hydration volume due to SB addition with no further notable change due to metronidazole load. Increasing the metronidazole load reduces the floating time of Carbopol matrices while no effect on Methocel matrices could be observed within 8 hours dissolution. Matrices show increasing release constant values (k) as the metronidazole load increases. Methocel matrices release the drug 10% to 15% faster than Carbopol matrices. SB increases the cumulative amount of drug released from Methocel but not that releasing from Carbopol. These results are attributed to the intrinsic polymer properties, the barrier effect of CO2 bubbles, and the matrix volume expansion produced after addition of SB.  相似文献   

2.
The sustained release of amoxicillin is desired to be confined to the upper gastrointestinal tract to treat certain kind of infections. In vitro dissolution, at pH 1.2, of amoxicillin sustained release tablets has been studied varying the proportion of Carbopol 971P NF and sodium alginate as well as the ethanol/water proportion in the granulation fluid. Mt, the amount of drug released at time (t) and defined in terms of the total drug released over a long time period (Minf), was described by Mt/Minf = ktn. Matrices with increasing proportions of sodium alginate showed increasing values of the exponent indicative of the release mechanism (n) and increasing release constant values (k). This is attributed to a drop in the coherence of the polymeric matrix with increasing alginate proportions that produces an increasing polymer relaxation and erosion. Decreasing Carbopol 971P NF proportions reduce the amount of dissolved polymer during granulation, producing a lesser obstruction of amoxicillin dissolution. Alginate proportions of 80% produce near zero order release profiles. Granules obtained with increasing ethanol proportions showed increasing release constant values and a minor change in the exponent (n) values. This is considered a result of lower polymer dissolution during granulation that allows a lesser matrix coherence and a greater amoxicillin dissolution. Alginate matrices granulated with different ethanol/water proportions showed no significant changes in the amoxicillin release profile. There is a trend toward increasing floating times with increasing Carbopol 971P NF proportions.  相似文献   

3.
Context: Alternating Current Biosusceptometry is a magnetically method used to characterize drug delivery systems. This work presents a system composed by an automated ACB sensor to acquire magnetic images of floating tablets.

Objective: The purpose of this study was to use an automated Alternating Current Biosusceptometry (ACB) to characterize magnetic floating tablets for controlled drug delivery.

Materials and methods: Floating tablets were prepared with hydroxypropyl methylcellulose (HPMC) as hydrophilic gel material, sodium bicarbonate as gas-generating agent and ferrite as magnetic marker. ACB was used to characterize the floating lag time and the tablet hydration rate, by quantification of the magnetic images to magnetic area. Besides the buoyancy, the floating tablets were evaluated for weight uniformity, hardness, swelling and in vitro drug release.

Results: The optimized tablets were prepared with equal amounts of HPMC and ferrite, and began to float within 4?min, maintaining the flotation during more than 24?h. The data of all physical parameters lied within the pharmacopeial limits. Drug release at 24?h was about 40%.

Conclusions: The ACB results showed that this study provided a new approach for in vitro investigation of controlled-release dosage forms. Moreover, using automated ACB will also be possible to test these parameters in humans allowing to establish an in vitro.in vivo correlation (IVIVC).  相似文献   

4.
The role of β-cyclodextrin (β-CD) on the apparent solubility of theophylline was investigated by the solubility method. Binary systems of theophylline and β-CD were prepared using the dry co-grinding method. Their characterization was performed by differential scanning calorimetry (DSC). The dissolution rate of theophylline and theophylline/β-CD and dissolution studies of matrix tablets prepared from mixtures containing theophylline and ground theophylline were carried out. It can be concluded that β-CD is related to an increase in the apparent solubility and dissolution rate of the drug, promoting improvement on the release of theophylline from matrices manufactured with hydroxypropylmethylcellulose (HPMC). This can be attributed to the amorphous state and the increased wettability of the drug.  相似文献   

5.
Cellulose derivatives are the most frequently used polymers in formulations of pharmaceutical products for controlled drug delivery. The main aim of the present work was to evaluate the effect of different cellulose substitutions on the release rate of ibuprofen (IBP) from hydrophilic matrix tablets. Thus, the release mechanism of IBP with methylcellulose (MC25), hydroxypropylcellulose (HPC), and hydroxypropylmethylcellulose (HPMC K15M or K100M) was studied. In addition, the influence of the diluents lactose monohydrate (LAC) and β-cyclodextrin (β-CD) was evaluated. Distinct test formulations were prepared containing: 57.14% of IBP, 20.00% of polymer, 20.29% of diluent, 1.71% of talc lubricants, and 0.86% of magnesium stearate as lubricants. Although non-negligible drug-excipient interactions were detected from DSC studies, these were found not to constitute an incompatibility effect. Tablets were examined for their drug content, weight uniformity, hardness, thickness, tensile strength, friability, porosity, swelling, and dissolution performance. Polymers MC25 and HPC were found to be unsuitable for the preparation of this kind of solid dosage form, while HPMC K15M and K100M showed to be advantageous. Dissolution parameters such as the area under the dissolution curve (AUC), the dissolution efficiency (DE20 h), dissolution time (t 50%), and mean dissolution time (MDT) were calculated for all the formulations, and the highest MDT values were obtained with HPMC indicating that a higher value of MDT signifies a higher drug retarding ability of the polymer and vice-versa. The analysis of the drug release data was performed in the light of distinct kinetic mathematical models—Kosmeyer-Peppas, Higuchi, zero-, and first-order. The release process was also found to be slightly influenced by the kind of diluent used.  相似文献   

6.
In the present study, investigation of the possibility of interaction of verapamil hydrochloride with Carbopol 934P using differential scanning calorimetric analysis and Fourier transform infrared analysis was performed. The effect of the drug-to-polymer ratio, the electrolyte concentration, and the pH of the medium on the extent of interaction of the drug with the polymer using 23 factorial design was investigated. The study also investigated the effect of this interaction on the rate of water uptake of the matrix or the rate of release of verapamil hydrochloride from the swelling polymer matrix. Results revealed that the drug-to-polymer ratio had the most influential effect on both the extent of interaction between the drug and the polymer and the rate of water uptake of the polymer matrix. On the other hand, the pH of the medium had the most significant effect on the rate of drug release. Interaction of the tertiary amine nitrogen of the drug with the anionic carboxyl group on the polymer, forming an insoluble complex, reduced the rate of drug release. This interaction also led to neutralization of the carboxyl group and suppression of the electrostatic repulsion between the anionic groups, which reduced the uncoiling and chain relaxation of the polymer and consequently decreased the swelling of the matrix. The application of the designed experiment allowed the quantification of the effect of each of the studied variables on the investigated responses through the calculation of their coefficient in the response surface equation and checking of their significance.  相似文献   

7.
The purpose of this study was to apply the optimization method incorporating artificial neural network (ANN) using pH-independent release of weakly basic drug, carvedilol from HPMC-based matrix formulation. Because of weakly basic nature of carvedilol, drug shows pH-dependent solubility. The enteric polymer EUDRAGIT L100 was added formulations to overcome pH-dependent solubility of carvedilol. Effects of the Hydroxypropylmethyl cellulose (HPMC) K4M and EUDRAGIT L100 amount on drug release were investigated. For this purpose 13 kinds of formulations were prepared at three different levels of each variables. The optimization of the formulation was evaluated by using ANN method. Two formulation parameters, the amounts of HPMC K4M and Eudragit L100 at three levels (?1, 0, 1) were selected as independent/input variables. In-vitro dissolution sampling times at twelve different time points were selected as dependent/output variables. By using experimental dissolution results and amount of HPMC K4M and EUDRAGIT L100, percentage of dissolved carvedilol was predicted by ANN. Similarity factor (f2) between predicted and experimentally observed profile was calculated and f2 value was found 76.33. This value showed that there was no difference between predicted and experimentally observed drug release profile. As a result of these experiments, it was found that ANNs can be successfully used to optimize controlled release drug delivery systems.  相似文献   

8.
In vitro dissolution of metronidazole from sustained release floating tablets was studied with varied proportions of sodium bicarbonate (SB) and Pharmatose DCL 11. Two polymers with different hydration characteristics, Methocel K4M and Carbopol 971P NF, were used to formulate the matrices. The variables studied include the matrices' release profile, hydration volume, and floating behavior. All Methocel matrices floated more than 8 h with SB proportions up to 24%, while Carbopol matrices floated more than 8 h with SB proportions only up to 12%. Matrices' hydration increased with time until reaching a peak and declining thereafter. Methocel matrices showed greater hydration volumes and greater drug dissolution compared to Carbopol matrices. After adding increasing quantities of Pharmatose to matrices containing 12% SB, hydration volume decreased while dissolution increased. These results were attributed to water-filled pores that formed following the Pharmatose dissolution and to reduced polymer proportions. Carbopol matrices showed greater susceptibility to the added Pharmatose, becoming more erodible and releasing higher quantities of metronidazole. The greater Carbopol susceptibility to added Pharmatose was attributed to its faster hydration. Methocel matrices hydrate rapidly only at the surface, delaying hydration and Pharmatose dissolution.  相似文献   

9.
This study discusses the effect of formulation composition on the physical characteristics and drug release behavior of controlled-release formulations made by roller compaction. The authors used mixture experimental design to study the effect of formulation components using diclofenac sodium as the model drug substance and varying relative amounts of microcrystalline cellulose (Avicel), hydroxypropyl methylcellulose (HPMC), and glyceryl behenate (Compritol). Dissolution studies revealed very little variability in drug release. The t70 values for the 13 formulations were found to vary between 260 and 550 min. A reduced cubic model was found to best fit the t70 data and gave an adjusted r-square of 0.9406. Each of the linear terms, the interaction terms between Compritol and Avicel and between all three of the tested factors were found to be significant. The longest release times were observed for formulations having higher concentrations of HPMC or Compritol. Tablets with higher concentrations of Avicel showed reduced ability to retard the release of the drug from the tablet matrix. Crushing strength showed systematic dependence on the formulation factors and could be modeled using a reduced quadratic model. The crushing strength values were highest at high concentrations of Avicel, while tablets with a high level of Compritol showed the lowest values. A predicted optimum formulation was derived by a numerical, multiresponse optimization technique. The validity of the model for predicting physical attributes of the product was also verified by experiment. The observed responses from the calculated optimum formulation were in very close agreement with values predicted by the model. The utility of a mixture experimental design for selecting formulation components of a roller compacted product was demonstrated. These simple statistical tools can allow a formulator to rationally select levels of various components in a formulation, improve the quality of products, and develop more robust processes.  相似文献   

10.
The objective of this study was to design and evaluate azilsartan osmotic pump tablets. Preformulation properties of azilsartan were investigated for formulation design. Azilsartan osmotic pump tablets were prepared by incorporation of drug in the core and subsequent coating with cellulose acetate and polyethylene glycol 4000 as semi-permeable membrane, then drilled an orifice at the center of one side. The influence of different cores, compositions of semipermeable membrane and orifice diameter on azilsartan release were evaluated. The formulation of core tablet was optimized by orthogonal design and the release profiles of various formulations were evaluated by similarity factor (f2). The optimal formulation achieved to deliver azilsartan at an approximate zero-order up to 14?h. The pharmacokinetic study was performed in beagle dogs. The azilsartan osmotic pump tablets exhibited less fluctuation in blood concentration and higher bioavailability compared to immediate-release tablets. Moreover, there was a good correlation between the in vitro dissolution and in vivo absorption of the tablets. In summary, azilsartan osmotic pump tablets presented controlled release in vitro, high bioavailability in vivo and a good in vitro-in vivo correlation.  相似文献   

11.
The objective was to investigate the potential of polymer molecular weight (MW) and polymer blends for the control of drug release from in situ gelling nasal inserts prepared by lyophilization of solutions of model drugs (oxymetazoline HCl, diprophyllin) and polymers. Drug release, polymer solution viscosity, water uptake and mass loss, mechanical properties, and bioadhesion potential were measured. Sonication was effective to reduce the viscosity/polymer MW of carrageenan solutions. Nasal inserts prepared from sonicated carrageenan showed an insignificant reduction in water uptake with sonication time and no disintegration of the gel matrix. In contrast, inserts of different MW Na-alginates revealed a reduced water uptake and an increased mass loss with lower MW. Inserts prepared from carrageenan/low MW Na-alginate blends took up more water at a higher low MW Na-alginate content. Sonicated carrageenan inserts released oxymetazoline HCl independent of the sonication time and diprophyllin with only a slight reduction in the release rate. Release of both drugs from Na-alginate inserts was slow from high MW inserts because no insert dissolution occurred. Increasing the Na-alginate content of inserts prepared from polymer blends accelerated the drug release enabling release rates over a broad range. The bioadhesion potential of Na-alginate inserts was strongly reduced for the low MW grades because of dissolution of the inserts. Xanthan gum and Carbopol 971 blended with Na-alginate formed inserts with poor bioadhesion. The use of polymer blends to control the drug release from nasal inserts was superior to the use of polymers of different MW.  相似文献   

12.
Purpose: To investigate the physical stability and drug release-related properties of the aqueous polymer dispersions Kollicoat® SR 30 D and Aquacoat® ECD (an ethylcellulose-based dispersion) in the presence water-soluble polymers (pore formers) with special attention to the potential flocculation of the polymer dispersions. Methods: A precise characterization of the flocculation phenomena in undiluted samples was monitored with turbidimetric measurements using the Turbiscan Lab-Expert. Theophylline or propranolol HCl drug-layered pellets were coated with Kollicoat® SR 30 D and Aquacoat® ECD by the addition of water-soluble polymers polyvinyl pyrrolidone (Kollidon® 30 and 90 F), polyvinyl alcohol–polyethylene glycol graft copolymer (Kollicoat® IR), and hydroxypropyl methylcellulose (Pharmacoat® 603 or 606) in a fluidized bed coater Glatt GPCG-1 and drug release was performed according to UPS paddle method. Results: Stable dispersions were obtained with both Kollicoat® SR 30 D (a polyvinyl acetate-based dispersion) and Aquacoat® ECD with up to 50% hydrophilic pore formers polyvinyl alcohol-polyethylene glycol graft copolymer (Kollicoat® IR) and polyvinyl pyrrolidone (Kollidon® 30). In general, Kollicoat® SR 30 D was more stable against flocculation than Aquacoat® ECD. Stable dispersions were also obtained with higher amounts of water-soluble polymer or by reducing the concentration of the polymer dispersion. Flocculated dispersions resulted in porous films and, thus, in a sharp increase in drug release. Conclusions: Kollicoat® SR 30 D was more resistant to flocculation upon addition of water-soluble polymers than Aquacoat® ECD. The continuous adjustment of drug release from Kollicoat® SR 30-coated pellets was possible with Kollicoat® IR amounts over a broad range.  相似文献   

13.
For various molecular ratios ranging between 0% and 30%, the effect of Crab Shell Particles (CSP) on the thermal and thermomechanical properties of polybenzoxazine has been studied. The high contents of CaCO3 particles in CSP clearly improve both the thermomechanical and thermal properties of the polybenzoxazine corresponding to a gain in storage modulus and glass transition temperature of 137% and 25%, respectively, at 30% CSP loading. Thermal analysis reveals that the polybenzoxazine matrix filled with CSP also increases the initial decomposition temperatures and the char yield of composites which reaches 49% at maximum CSP content.  相似文献   

14.
Two grades of commercial purity (CP) titanium (grades 2 and 4) were processed using equal-channel angular extrusion (ECAE) at 300 °C and 450 °C, respectively. The processing temperatures were the minimum temperatures at which eight pass ECAE could be performed without any shear-localization. The coarse-grained (CG) microstructures of as-received grade-2 and grade-4 CP-Ti, with average grain sizes of 110 μm and 70 μm, respectively, were refined down to sub-micron levels with a mean grain size of about 300 nm for both grades after 8 ECAE passes. The ultrafine-grained (UFG) microstructures led to substantial enhancement in strength for both grades. The grade-2 sample showed a more than two fold increase in yield strength (σy), from 307 MPa for the as-received one to about 620 MPa for the processed samples. The grade-4 CP-Ti exhibited a relatively smaller increase in strength due to the higher processing temperature, and it showed about 50% increase in σy after eight pass ECAE, from 531 to 758 MPa. These strength levels were obtained with high ductility levels of 21% and 25% for UFG grade-2 and grade-4 Ti, respectively. These improvements in mechanical properties are attributed to the substantially refined grain size and increased dislocation density. Grade-4 Ti is stronger than grade-2 because of the higher oxygen content. The higher ductility and significantly higher strain hardening capability of UFG grade-4 Ti, in spite of the similar grain size and microstructure with UFG grade-2 Ti, is also due to the higher impurity content, probably resulting in a higher dislocation storage capability during room temperature deformation, and thus, higher strain hardening capacity. Such properties make UFG grade-4 Ti comparable to the commercial Ti-6Al-4V alloy for biomedical applications without negative effects of the alloying elements on biocompatibility.  相似文献   

15.
The effect of fiber, matrix and interface properties on the in-plane shear response of carbon-fiber reinforced epoxy laminates was studied by means of a combination of experiments and numerical simulations. Two cross-ply laminates with the same epoxy matrix and different carbon fibers (high-strength and high-modulus) were tested in shear until failure according to ASTM standard D7078, and the progressive development of damage was assessed by optical microscopy in samples tested up to different strains. The composite behavior was also simulated through computational micromechanics, which was able to account for the effect of the constituent properties (fiber, matrix and interface) on the macroscopic shear response. The influence of matrix, fiber and interface properties on each region and on the overall composite behavior was assessed from the experimental results and the numerical simulations. After the initial elastic region, the shear behavior presented two different regions, the first one controlled by matrix yielding and the second one by the elastic deformation of the fibers. It was found that in-plane shear behavior of cross-ply laminates was controlled by the matrix yield strength and the interface strength and was independent of the fiber properties.  相似文献   

16.
In this study, AA 6013 aluminum plates were butt‐welded with friction stir welding via pin offset technique. Macrostructural observations revealed that kissing bonds, originated from the broken oxide layers, were found to occur in the welded joints. The fracture location of welded joints after tensile tests was found to be outside the joint area, revealing that kissing bonds which were formed in the stir zone exhibited no detrimental effect on the mechanical properties of joints. Microstructural observations revealed that phases belonging to Mg2Si, Al4Cu2Mg8Si7 and Al(MnFe)Si were observed in the x‐ray diffraction pattern of friction stir welded joints. The highest tensile strength with a value of 206 MPa was achieved with the process parameters of 1.5 mm pin offset towards the advancing side and 500 min?1 tool rotational speed, leading the ratio of tensile strength of joint to ultimate tensile strength of base metal, also known as joint efficiency, to reach 74 %.  相似文献   

17.
《Advanced Powder Technology》2021,32(10):3826-3844
Mechanical milling presents an effective solution in producing a homogenous structure for composites. The present study focused on the production of 0.5 wt% yttria nanoparticle reinforced 7075 aluminum alloy composite in order to examine the effects of yttria dispersion and interfacial bonding by ball milling technique. The 7075 aluminum alloy powders and yttria were mechanically alloyed with different milling times. The milled composites powders were then consolidated with the help of hot pressing. Hardness, density, and tensile tests were carried out for characterizing the mechanical properties of the composite. The milled powder and the microstructural evolution of the composites were analyzed utilizing scanning and transmission electron microscopy. A striking enhancement of 164% and 90% in hardness and ultimate tensile strength, respectively, were found compared with the reference 7075 aluminum alloy fabricated with the same producing history. The origins of the observed increase in hardness and strength were discussed within the strengthening mechanisms' framework.  相似文献   

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