scholarly journals Hollow and Solid Spherical Azithromycin Particles Prepared by Different Spherical Crystallization Technologies for Direct Tableting

Processes ◽  
2019 ◽  
Vol 7 (5) ◽  
pp. 276
Author(s):  
Kui Chen ◽  
Baohong Hou ◽  
Hao Wu ◽  
Xin Huang ◽  
Fei Li ◽  
...  

Many drugs have a propensity for agglomeration, resulting in poor flowability. Spherical crystallization can be used to improve product properties including flowability and particle size. In this work, two methods were developed and utilized to successfully make two kinds of azithromycin spherical particles, namely solid and hollow spheres. The resultant product exhibited regular spherical shape, large particle size, narrow particle size distribution and excellent flowability. The formation mechanism of these different spherical crystals was investigated with the help of a particle vision microscope (PVM). The immersion mechanism and the counter diffusion mechanism were proposed as the formation mechanisms for solid and hollow spheres, respectively. The effects of crystallization parameters on the spherical crystallization processes were investigated systematically. Furthermore, the tablet properties were evaluated to verify that the spherical particles obtained in this work can be directly used for tableting, thus avoiding granulation processes and reducing cost.

Author(s):  
N B Bhagat ◽  
A V Yadav ◽  
P R Mastud ◽  
R A Khutale

In this article we describe the optimizing parameters in the process of spherical crystallisation. Particle engineering of active pharmaceutical agents is an innovative area of research in pharmaceutical industry because of several advantages. Spherical crystallization is one of the particle engineering technique in which drug directly gets crystallized and agglomerated into spherical shape. The spherical crystals can be obtained by different methods like solvent change, Quasi-emulsion droplet, ammonia diffusion and neutralisation. The optimization of process of spherical crystallization is important for obtaining the ideal spherical crystal agglomerates. It includes stirring rate, selection of solvent, pH, temperature etc. which affects on the physico-chemical properties of crystals. These optimizing parameters play its specific role in formation of spherical crystals. Stirring rate affects the shape as well as size of the final agglomerates and solvent selection helps in the formation of maximum amount of agglomerates in the system. The factors like pH and temperature should be maintained in case of drugs which show polymorphism. Apart from this, several others physical phenomenon or parameters like interfacial tension and rate of crystallisation are also important for thorough optimization of process.  


NANO ◽  
2014 ◽  
Vol 09 (02) ◽  
pp. 1450022 ◽  
Author(s):  
XIAOLEI SU ◽  
YONGSHENG TAN ◽  
YAN JIA ◽  
KAILI ZHAO ◽  
JUNBO WANG ◽  
...  

Cu -doped SiC nanopowders have been prepared via combustion synthesis of the silicon and carbon system in a 0.1 MPa nitrogen atmosphere under different reaction time, using copper as the dopant and PTFE as the chemical activator, respectively. X-ray diffraction, scanning electronic microscope and Raman spectra have been used to characterize the phase and morphology of prepared nanopowders. Results indicate that the lattice constant of prepared Cu -doped SiC nanopowder decreases with extending reaction time. The prepared nanopowders have fine spherical particles and narrow particle size distribution and the particle size increases with increasing reaction time. The electric permittivities of prepared Cu -doped SiC nanopowders in the frequency range of 8.2–12.4 GHz have been determined. The real part ε′, imaginary part ε′′ and dielectric loss tgδ of complex permittivity decrease with increasing reaction time. All prepared Cu -doped SiC nanopowder exhibits good microwave absorption property in the frequency range of 8.2–12.4 GHz.


Author(s):  
Van Minh Nguyen ◽  
Tien Hiep Nguyen ◽  
Stanislav V. Gorobinsky

In this work, nanopowders (NP) Co(OH)2 were obtained by chemical precipitation from aqueous solutions of cobalt nitrate Co(NO3)2 and alkali NaOH (10 wt. %) using surfactants: sodium dodecyl sulfate (SDS) and cetylpyridinium chloride (CPC) (0.1 wt. %). It was shown that Co(OH)2 NP with 0.1% SDS is the best quality product, since its dispersion increases more than 2 times compared to the samples with 0.1% CPC and without surfactants. In this case, the Co(OH)2 NP has the form of flakes with an irregular shape and a nanometer size (about 100 nm) with an average thickness of 30 nm. It was found that the average particle size of Co NP obtained by hydrogen reduction of Co(OH)2 NP with 0.1% SDS at 280°C has a maximum on the distribution histogram shifted to the interval 41–50 nm, which is characterized by a narrow particle size distribution and represents spherical particles sintered with each other.


2007 ◽  
Vol 342-343 ◽  
pp. 477-480
Author(s):  
Xi Ming Pu ◽  
Yun Qing Kang ◽  
Ai Zheng Chen ◽  
Li Liao ◽  
Guang Fu Yin

5-Fluorouracil-poly(L-lactide) (5-Fu-PLLA) microspheres have been co-precipitated in a process namely solution-enhanced dispersion by supercritical CO2 (SEDS). First, the 5-Fu is successfully micronized and then used to produce the 5-Fu-PLLA microspheres. The 5-Fu-PLLA microspheres synthesized in the SEDS process exhibited a rather spherical shape, smooth surface, and a narrow particle size distribution, where it ranged from 531 nm to 1280 nm, with a mean particle size of 793 nm. The dichloromethane residue in the 5-Fu-PLLA microspheres is 46 ppm. The average drug load of the 5-Fu-PLLA microspheres is 12.7%. The results of this study indicate that the SEDS process is an effective technique to co-precipitate 5-Fu and PLLA as composite microspheres.


Author(s):  
Harish Singh Dhami ◽  
Koushik Viswanathan

Abstract Grinding swarf is conventionally of secondary interest to the process engineer. However, it has long been recognized that it is a useful indicator of process performance — the exact particle morphologies occurring in the swarf contain a wealth of information about the abrasive-workpiece interaction mechanics. In this work, we study the generation of perfectly spherical particles when grinding two plain carbon steels and a grade of stainless steel with an alumina wheel. Similar particles have also been reported in the wear community and several possible formation mechanisms have been discussed including chip curl resulting from electronic charge distributions; melting due to local flash temperatures in the grinding zone; and repeated abrasive wear of the workpiece surface. We postulate that the particles are likely formed as a result of an oxidation-melting-solidification route with small grinding chips. We present spectroscopy and X-ray diffraction data in support of this hypothesis — significant oxygen content, in the form of Fe3O4 was detected on the surface of the spheres. Electron micrographs also show remarkably robust dendrite-like structures on the surface of the particles, indicative of rapid solidification from the melt. Motivated by these results, we present model calculations to support our hypothesis. We first evaluate the initial temperature of chips exiting the grinding zone using a three-way heat partition model for dry grinding. An upper bound for the chip temperature is ∼ 600°C, well-below the melting point for the metal. Next, we show that the oxidation kinetics at this elevated temperature are such that the formation of a thin oxide layer (∼ 2μm) on the surface of an initially curled up chip, with size ∼ 50 μm comparable to the observed spheres, is enough to melt the entire chip on a timescale of 10−6 seconds. Surface tension then brings the molten chip into a perfectly spherical shape, followed by rapid solidification. We present a preliminary calculation of this solidification process, using a coupled heat conduction model along with a moving interphase interface. By making suitable approximations, we derive an ordinary differential equation describing the temporal evolution of the interface location. Coupling the interface velocity with a Mullins-Sekerka type instability analysis, we argue that solidification of these drops likely starts from a nucleated core in the drop interior, resulting in dendrite-type patterns on the outer surface. Our work is a preliminary attempt to put decades old observations of grinding swarf on a firm quantitative footing. The experimental evidence and related analysis presented here make a strong case for the oxidation-melting-solidification hypothesis for the formation of spherical particles in grinding swarf.


2019 ◽  
Vol 97 ◽  
pp. 05034
Author(s):  
Liudmila Volgina ◽  
Anastasiia Romanova

The paper studies impact of determining the diameter of solid particles on the calculation of the hydraulic particle size in the water flow. The relevance of the topic is also connected with the use of calculation of hydraulic size in hydraulic engineering in forecasting: downstream erosion, the formation of shoals, canals, bottom spillages, etc. Most of the empirical formulas for calculating the hydraulic particle size are applicable to spherical particles. However, the nature of the solid particles rarely has a spherical shape. The aim of this work is to investigate experimentally the dependence of the hydraulic size of the diameter of the solid particles. Different approaches to determining the diameter solid particles are analyzed, as for non-spherical particles finding the diameter is an independent and complex problem. For the experimental research solid particles of different shapes and sizes were used. The diameter is included in the empirical formulas for hydraulic size linearly, and to the power of 2 or 0.5. Therefore, the dependence of the experimental hydraulic size on the diameter was correlated with the corresponding functions. The shape of the particle significantly affects the value of the hydraulic size and depends on the diameter to the power of (0.5).


2007 ◽  
Vol 336-338 ◽  
pp. 477-480
Author(s):  
Wei Hua Pu ◽  
Xiang Ming He ◽  
Guo Yun Zhang ◽  
Chang Yin Jiang ◽  
Chun Rong Wan ◽  
...  

A novel process was proposed for preparing spinel LiMn2O4 with spherical particles from cheap materials of MnSO4, NaOH, NH3•H2O and LiOH. Its successful preparation started with a carefully controlled crystallization of Mn3O4, leading to the spherical shape of its particles and a high tap density. The mixture of Mn3O4 and LiOH was sintered to produce LiMn2O4 with spherical particle size retention. The spherical particles of spinel LiMn2O4 were of excellent fluidity and dispersivity, and had tap density as high as 2.14 g cm-3 and the initial discharge capacity reaching 128 mAh g-1. Its 15th cycle capacity kept to be 125 mAh g-1.


2012 ◽  
Vol 531-532 ◽  
pp. 226-229
Author(s):  
Xing Wu Zou ◽  
Shu Xuan Wang ◽  
Zhan Shou Yang ◽  
Mi Xiang Qi ◽  
Shu Ya Wang

A new synthetic technology of Strontium carbonate with high gravity is introduced in this paper. We got ultrafine SrCO3 powders with Sr(NO3)2 and NaCO3 or CO2 as raw material by high gravity method. We studied flows, the rotating speed, additives and CO2 as the reactants on the morphology of strontium carbonate. The results show that the presence of additive-free, we got rod-like structure of strontium carbonate. Added EDTA, we got a good dispersion of spherical particles of narrow particle size distribution. The presence of EDTA, the average particle size of spherical particles decreases with the speed increases. CO2 alternative Na2CO3 as the reactants, the presence of additive-free, we got the bundle structure of strontium carbonate. The presence of EDTA, we got spherical particles, but the particle dispersion is not well, gathered together.


Author(s):  
Nisha Patel ◽  
Hitesh A Patel

In this study, we sought to improve the dissolution characteristics of a poorly water-soluble BCS class IV drug canaglifozin, by preparing nanosuspension using media milling method. A Plackett–Burman screening design was employed to screen the significant formulation and process variables. A total of 12 experiment were generated by design expert trial version 12 for screening 5 independent variables namely the amount of stabilizer in mg (X1), stirring time in hr (X2), amt of Zirconium oxide beads in gm (X3), amount of drug in mg (X4) and stirring speed in rpm (X5) while mean particle size in nm (Y1) and drug release in 10 min. were selected as the response variables. All the regression models yielded a good fit with high determination coefficient and F value. The Pareto chart depicted that all the independent variables except the amount of canaglifozin had a significant effect (p<0.001) on the response variables. The mathematical model for mean particle size generated from the regression analysis was given by mean particle size = +636.48889 -1.28267 amt of stabilizer(X1) -4.20417 stirring time (X2) -7.58333 amt of ZrO2 beads(X3) -0.105556 amt of drug(X4) -0.245167 stirring speed(X5) (R2=0.9484, F ratio=22.07, p<0.001). Prepared canaglifozin nanosuspension exemplified a significant improvement (p<0.05) in the release as compared to pure canaglifozin and marketed tablet with the optimum formulation releasing almost 80% drug within first 10min. Optimized nanosuspension showed spherical shape with surface oriented stabilizer molecules and a mean particle diameter of 120.5 nm. There was no change in crystalline nature after formulation and it was found to be chemically stable with high drug content.


2020 ◽  
Vol 14 (3) ◽  
pp. 210-224
Author(s):  
Gayatri Patel ◽  
Bindu K.N. Yadav

Background: The purpose of this study was to formulate, characterize and in-vitro cytotoxicity of 5-Fluorouracil loaded controlled release nanoparticles for the treatment of skin cancer. The patents on nanoparticles (US8414926B1), (US61654404A), (WO2007150075A3) etc. helped in the selection polymers and method for the preparation of nanoparticles. Methods: In the present study nanoparticles were prepared by simple ionic gelation method using various concentrations of chitosan and sodium tripolyphosphate (TPP). Several process and formulation parameters were screened and optimized using 25-2 fractional factorial design. The prepared nanoparticles were evaluated for particle size, shape, charge, entrapment efficiency, crosslinking mechanism and drug release study. Results: The optimized 5-Fluorouracil loaded nanoparticle were found with particle size of of 320±2.1 nm, entrapment efficiency of 85.12%± 1.1% and Zeta potential of 29mv±1mv. Scanning electron microscopy and dynamic light scattering technique revealed spherical particles with uniform size. The invitro release profile showed controlled release up to 24 hr. Further study was carried using A375 basal cell carcinoma cell-line to elucidate the mechanism of its cytotoxicity by MTT assay. Conclusion: These results demonstrate that the possibility of delivering 5-Fluorouracil to skin with enhanced encapsulation efficiency indicating effectiveness of the formulation for treatment of basal cell carcinoma type of skin cancer.


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