scholarly journals Lignin and Cellulose Blends as Pharmaceutical Excipient for Tablet Manufacturing via Direct Compression

Biomolecules ◽  
2019 ◽  
Vol 9 (9) ◽  
pp. 423 ◽  
Author(s):  
Domínguez-Robles ◽  
Stewart ◽  
Rendl ◽  
González ◽  
Donnelly ◽  
...  
Keyword(s):  
Drug Loading ◽  
Antioxidant Properties ◽  
Maximum Amount ◽  
Release Profile ◽  
Direct Compression ◽  
Compression Force ◽  
Crushing Strength ◽  
Pharmaceutical Excipient ◽  
Tablet Manufacturing ◽  
Model Drug

Extensive efforts are being made to find alternative uses for lignin (LIG). In the present work the use of this biopolymer as excipient to prepare tablets was studied. For this purpose, LIG was combined with microcrystalline cellulose (MCC) and used as excipients to prepare directly compressed tablets containing a model drug, tetracycline (TC). The excipients contained different concentrations of LIG: 100%, 75%, 50%, 25% and 0% (w/w). Two different compression forces were used (two and five tonnes). When formulations were prepared using LIG as the only excipient, tablets were formed, but they showed lower densities and crushing strength than the ones obtained with only MCC or LIG/MCC blends. Moreover, tablets prepared using five tonnes of compression force showed TC releases ranging from 40% to 70% of the drug loading. On the other hand, the tablets prepared using two tonnes of compression force showed a faster and more efficient TC release, between 60% and 90%. The presence of LIG in the tablets modified significantly the release profile and the maximum amount of TC released. Finally, a DPPH (2,2-diphenyl-1-picrylhydrozyl) assay was performed to confirm that the presence of LIG provided antioxidant properties to the formulations. Accordingly, LIG has potential as a pharmaceutical excipient.

scholarly journals Effect of a co-processed excipient on the disintegration and drug release profile of ibuprofen tablets

Bio-Research ◽  
2020 ◽  
Vol 18 (1) ◽  
Author(s):  
BB Mohammed ◽  
EJ John ◽  
NK Ajuji
Keyword(s):  
Drug Release ◽  
Release Profile ◽  
Angle Of Repose ◽  
Oral Dosage ◽  
Direct Compression ◽  
Drug Release Profile ◽  
Disintegration Time ◽  
Crushing Strength ◽  
Tablet Properties ◽  
Spray Dried

Tablets at present, remain the most preferred oral dosage form because of many advantages they offer to formulators as well as physicians and patients. The objective of this work was to determine the effect of co-processing on the disintegration and drug-release profile of ibuprofen tablets prepared from a co-processed excipient. The co-processed excipient (CE) containing lactose, gelatin and mucin in the ratio 90:9:1 was prepared using co-fusion. The excipient was evaluated for its physicochemical properties and then used to formulate tablets with the addition of a disintegrant by direct compression. The tablets were evaluated for their tablet properties and compared with tablets prepared with cellactose- 80® (CEL) and spray dried lactose® (SDL) and a physical mix (PM) of the co-processed ingredient. Results from evaluation of CE showed that flow rate, angle of repose, Carr’s index and Hausner’s ratio were 5.28 g/sec, 20.30o, 23.75 % and 1.31, respectively. Tablets prepared with CE had friability (0%), crushing strength (5.25) KgF, disintegration time (3 mins) and T50% (2 mins). For CEL, friability (0.4 %), crushing strength (7.25) KgF, disintegration time (1 min) and T50% (2 mins); SDL, friability (1.57 %), crushing strength (7.50) KgF, disintegration time (4 mins) and T50% (2 mins) and PM, friability (2.38 %), crushing strength (5.00) KgF, disintegration time (1 min) and T50% (2 mins). In conclusion, the disintegration time and drug release profile for CE was not superior but compared favorably with CEL, SDL and PM.  

Effect of Modified Hydroxypropyl Tapioca Starch and Percentage of Drug Loading on Physical Property of Paracetamol Tablet

2020 ◽  
Vol 859 ◽  
pp. 3-8
Author(s):  
Vipaluk Patomchaiviwat ◽  
Sontaya Limmatvapirat ◽  
Chaisai Sirisapaya ◽  
Rohanee Kolae ◽  
Kulmanee Anantakul ◽  
...  
Keyword(s):  
Drug Loading ◽  
Physical Property ◽  
High Hardness ◽  
Direct Compression ◽  
Compression Method ◽  
Disintegration Time ◽  
Tapioca Starch ◽  
Drug Concentrations ◽  
Model Drug ◽  
Better Than

The objective of this study was to investigate the effect of modified hydroxypropyl tapioca starch (HPTS) and % drug loading on physical property of tablet. Paracetamol was used as model drug because of its poor compressibility. The filler ability of modified HPTS such as hydroxyl propyl oxidized tapioca starch (HPOTS), hydroxyl propyl crosslinked tapioca starch (HPCTS) and pregelatinized tapioca starch (PTS) were evaluated and compared with the commercial starch (Starch 1500®). Tablets were prepared by direct compression method and the percent drug loading were 15, 30, 45, 60, 75%. For modified HPTS, the hardness of the tablets tended to decrease when the concentration of paracetamol increased. At drug concentrations of 15-30%, HPOTS exhibited good performance of tablet as indicated by the high hardness, low friability and acceptable disintegration time. The obtained results were better than HPTS and comparable to Starch 1500®. Moreover, the results revealed that tablet containing PTS provided the highest hardness and prolonged disintegration time (>30 min) while tablet containing HPCTS showed rapid disintegration time (<2 min). Therefore, modified HPTS disclosed promising properties for application as tablet filler

scholarly journals On the Drug-Loading Capacity of Pectin Powder for Direct Compression

2012 ◽  
Vol 13 (2) ◽  
pp. 601-604
Author(s):  
Ingunn Tho ◽  
Katharina Picker-Freyer ◽  
Linda Salbu ◽  
Annette Bauer-Brandl
Keyword(s):  
Drug Loading ◽  
Direct Compression ◽  
Loading Capacity

scholarly journals Contrasting the crospovidones functionality as excipients for direct compression

2015 ◽  
Vol 51 (1) ◽  
pp. 155-171 ◽  
Author(s):  
Daniel García Ramírez ◽  
Leopoldo Villafuerte Robles
Keyword(s):  
Drug Product ◽  
Absolute Number ◽  
Powder Flow ◽  
Direct Compression ◽  
Flow Properties ◽  
Technological Performance ◽  
A Value ◽  
Tablet Disintegration ◽  
Input Variables ◽  
Model Drug

Specific values of technological properties of excipients allow the establishment of numerical parameters to define and compare their functionality. This study investigates the functionality of Polyplasdones XL and XL10. Parameters studied included tablet disintegration profiles, compactibility profiles and powder flow. The results allowed the establishment of quantitative surrogate functionalities of technological performance, such as absolute number, and as a value relative to the known microcrystalline cellulose type 102. Moreover, the establishment of an explicit functionality to improve the technological performance of two diluents and a model drug was investigated, as was setting up of these functionalities, as quantitative values, to determine the input variables of each material and its probable functionality in a drug product. Disintegration times of pure Polyplasdone XL and its admixtures were around half that of Polyplasdone XL10. The improvement in tablet compactibility was 25-50% greater for Polyplasdone XL10 than Polyplasdone XL. Crospovidones proportions of up to 10% have little effect on the flow properties of other powders, although pure Polyplasdone XL10 and its admixtures display compressibility indexes about 20% greater than Polyplasdone XL. The observed results are in line with a smaller particle size of Polyplasdone XL10 compared to Polyplasdone XL.

scholarly journals Synthesis and Characterization of Stearic Acid-Beclomethasone Dipropionate Conjugates with the Potential for Improving Loading Capacity in Lipid-based Nanoparticles

2021 ◽  
Author(s):  
Shishuai Dang ◽  
Zhengwei Huang ◽  
Ying Huang ◽  
Xin Pan ◽  
Chuanbin Wu
Keyword(s):  
Drug Delivery ◽  
Stearic Acid ◽  
Beclomethasone Dipropionate ◽  
Drug Loading ◽  
Pulmonary Delivery ◽  
Dynamics Simulation ◽  
Loading Capacity ◽  
Technology Platform ◽  
New Type ◽  
Model Drug

<p>Lipid-based nanoparticles (LBNs) are a new type of nanoparticulate drug delivery system, which have been gradually shown broad prospects in pulmonary drug delivery systems. However, the main disadvantage of these LBNs for inhalable drugs with limited lipophilicity is the low encapsulation capacity. Herein, this study anticipates establishing a technology platform to improve the loading capacity of low lipophilicity drugs in LBNs, for the therapy of lung diseases. A proof-of-concept was carried out using Beclomethasone dipropionate (BDP) as a model drug. BDP was conjugated with stearic acid (SA), a kind of the lipid matrix for LBN. The conjugate was characterized and the interactions between the conjugate and SA were investigated by molecular dynamics simulation. It is expected that the drug loading capacity of weak-lipophilic drugs in LBN can be increased by establishing the technology platform, and the application of LBNs in pulmonary delivery can be broadened.</p>

Synthesis, characterization and formulation of sodium calcium silicate bioceramic for drug delivery applications

2016 ◽  
Vol 23 (4) ◽  
pp. 375-380
Author(s):  
P. Manohar Reddy ◽  
Ravy Lakshmi ◽  
Febin Prabhu Dass ◽  
Swamiappan Sasikumar
Keyword(s):  
Drug Delivery ◽  
Calcium Silicate ◽  
Release Kinetics ◽  
Release Profile ◽  
Apatite Formation ◽  
X Ray Diffraction ◽  
Drug Release Profile ◽  
Sodium Calcium ◽  
Calcium Magnesium ◽  
Model Drug

AbstractSodium calcium silicate (Na2CaSiO4) is a bioactive silicate with Na2O, CaO and SiO2 as its basic components, which is similar to that of the composition of bioactive glasses. In the present study, pure sodium calcium silicate was synthesized by rapid combustion technique, and the synthesized sample was characterized by powder X-ray diffraction to check the phase purity. The scaffolds were prepared by varying the ratio of sodium calcium silicate and polyvinyl alcohol, and the apatite-formation ability of the scaffolds was examined by soaking them in a simulated body fluid. The results revealed the formation of hydroxyapatite on the surface of the scaffold after 5 days, which is found to be rapid when compared with the bioactivity of the calcium silicates and calcium magnesium silicates. The scaffolds were also loaded with ciprofloxacin as a model drug and analyzed for its drug release profile using UV spectrophotometer. The release profile did not vary with the change in bioceramic-to-biopolymer ratio, and 60% of the drug was released in 10 days, which is within the appreciable range for a targeted drug delivery system. Moreover, the experimental and simulated values of the release kinetics were compared by applying the existing mathematical model.

Ceftizoxime Loaded ZnO/L-Cysteine Based an Advanced Nanocarrier Drug for Growth Inhibition of Salmonella Typhimurium

2021 ◽  
Author(s):  
Md. Sadek Bacchu ◽  
Md. Romzan Ali ◽  
Md. Ali Ahasan Setu ◽  
Selina Akter ◽  
Md. Zaved Hossain Khan
Keyword(s):  
Drug Loading ◽  
Hollow Spheres ◽  
Antibacterial Properties ◽  
Trisodium Citrate ◽  
Release Profile ◽  
Attenuated Total Reflection ◽  
Diffusion Method ◽  
Dilution Method ◽  
Agar Disc ◽  
Serovar Typhimurium

Abstract L-Cysteine coated zinc oxide (ZnO) nano hollow spheres were prepared as a potent drug delivery agent to eradicate Salmonella enterica serovar Typhimurium (S. typhimurium). The ZnO nano hollow spheres were synthesized by following the environmentally-friendly trisodium citrate assisted method and L-Cysteine (L-Cys) conjugate with its surface. ZnO/L-Cys@CFX nanocarrier drug has been fabricated by incorporating ceftizoxime with L-Cys coated ZnO nano hollow spheres and characterized using different techniques such as scanning electron microscope (SEM), attenuated total reflection Fourier transform infrared (ATR-FTIR), and X-ray diffraction (XRD) etc. Furthermore, the drug-loading and encapsulation efficiency at different pH levels was measured using UV-vis spectrometer and optimized. A control and gradual manner of pH-sensitive release profile was found after investigating the release profile of CFX from the carrier drug. The antibacterial activity of ZnO/L-Cys@CFX and CFX were evaluated through the agar disc diffusion method and the broth dilution method, which indicate the antibacterial properties of antibiotics enhance after conjugating. Surprisingly, the ZnO/L-Cys@CFX exhibits a minimum inhibitory concentration (MIC) of 5µg/ml against S. typhimurium is lower than CFX (20µg/ml) itself. These results indicate the nanocarrier can reduce the amount of CFX dosed to eradicate S. typhimurium.

Influence of emulsification mode, stirring speed and volume on ibuprofen-loaded PLGA microparticles

2021 ◽  
Vol 70 (1) ◽  
pp. 32-40
Author(s):  
Holická Martina ◽  
Muselík Jan ◽  
Kubová Kateřina ◽  
Deáková Veronika ◽  
Pavloková Sylvie ◽  
...  
Keyword(s):  
Aqueous Phase ◽  
Drug Loading ◽  
Particle Morphology ◽  
Laser Diffraction ◽  
Size Reduction ◽  
Emulsion System ◽  
Solvent Evaporation Method ◽  
Particle Size Reduction ◽  
Acid Copolymer ◽  
Model Drug

Microparticles based on biodegradable synthetic lactic acid and glycolic acid copolymer (PLGA) were successfully prepared by the solvent evaporation method. Ibuprofen was chosen as the model drug. Various formulation and process parameters have been used to prepare each sample with emphasis on size reduction. The effect of the emulsification method (direct emulsification or emulsification using an ULTRA-TURRAX or a NE-1000 dispenser), the volume of the aqueous phase (200, 800 ml) and the stirring speed of the emulsion system (600, 1000 rpm) on the characteristic properties of microparticles, such as encapsulation efficiency, drug loading and particle morphology, was observed. The resulting microparticles were evaluated by optical microscopy or laser diffraction and the dissolution test was performed. It was found that the sample prepared by direct emulsification with 800 ml of an aqueous phase at 600 rpm provided the most favorable results, meanwhile the emulsification pre-step using a homogenizer caused promising particle size reduction. Gradual emulsification was evaluated as inapplicable due to great losses.

Integrated modeling of a continuous direct compression tablet manufacturing process: A production scale case study

2019 ◽  
Vol 354 ◽  
pp. 199-210 ◽  
Author(s):  
S.C. Galbraith ◽  
B. Cha ◽  
Z. Huang ◽  
S. Park ◽  
H. Liu ◽  
...  
Keyword(s):  
Manufacturing Process ◽  
Integrated Modeling ◽  
Direct Compression ◽  
Production Scale ◽  
Tablet Manufacturing

scholarly journals Formulation of Nanomicelles to Improve the Solubility and the Oral Absorption of Silymarin

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1688 ◽  
Author(s):  
Vieri Piazzini ◽  
Mario D’Ambrosio ◽  
Cristina Luceri ◽  
Lorenzo Cinci ◽  
Elisa Landucci ◽  
...  
Keyword(s):  
Encapsulation Efficiency ◽  
Oral Absorption ◽  
Drug Loading ◽  
Antioxidant Properties ◽  
Aqueous Solubility ◽  
Average Diameter ◽  
Critical Micellar Concentration ◽  
Polydispersity Index ◽  
Vitamin E Tpgs

Two novel nanomicellar formulations were developed to improve the poor aqueous solubility and the oral absorption of silymarin. Polymeric nanomicelles made of Soluplus and mixed nanomicelles combining Soluplus with d-α-tocopherol polyethylene glycol 1000 succinate (vitamin E TPGS) were prepared using the thin film method. Physicochemical parameters were investigated, in particular the average diameter, the homogeneity (expressed as polydispersity index), the zeta potential, the morphology, the encapsulation efficiency, the drug loading, the critical micellar concentration and the cloud point. The sizes of ~60 nm, the narrow size distribution (polydispersity index ≤0.1) and the encapsulation efficiency >92% indicated the high affinity between silymarin and the core of the nanomicelles. Solubility studies demonstrated that the solubility of silymarin increased by ~6-fold when loaded into nanomicelles. Furthermore, the physical and chemical parameters of SLM-loaded formulations stored at room temperature and in refrigerated conditions (4 °C) were monitored over three months. In vitro stability and release studies in media miming the physiological conditions were also performed. In addition, both formulations did not alter the antioxidant properties of silymarin as evidenced by the 1,1-Diphenyl-2-picrylhydrazyl radical (DPPH) assay. The potential of the nanomicelles to increase the intestinal absorption of silymarin was firstly investigated by the parallel artificial membrane permeability assay. Subsequently, transport studies employing Caco-2 cell line demonstrated that mixed nanomicelles statistically enhanced the permeability of silymarin compared to polymeric nanomicelles and unformulated extract. Finally, the uptake studies indicated that both nanomicellar formulations entered into Caco-2 cells via energy-dependent mechanisms.

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