This paper describes preparation and characterization of beads of alginate and psyllium containing probiotic bacteria of Lactobacillus acidophilus DMSZ20079. Twelve different formulations containing alginate (ALG) and alginate-psyllium (ALG-PSL) were prepared using extrusion technique. The prepared beads were characterized in terms of size, morphology and surface properties, encapsulation efficiency, viabilities in acid (pH 1.8, 2 hours) and bile (0.5% w/v, 2 hours) conditions, and release in simulated colon pH conditions. The results showed that spherical beads with narrow size distribution ranging from 1.59 ± 0.04 to 1.67 ± 0.09 mm for ALG and from 1.61 ± 0.06 to 1.80 ± 0.07 mm for ALG-PSL with encapsulation efficiency higher than 98% were achieved. Furthermore, addition of PSL into ALG enhanced the integrity of prepared beads in comparison with ALG formulations. The results indicated that incorporation of PSL into alginate beads improved viability of the bacteria in acidic conditions as well as bile conditions. Also, stimulating effect of PSL on the probiotic bacteria was observed through 20-hour incubation in simulated colonic pH solution. According to our in vitro studies, PSL can be a suitable polymer candidate for partial substitution with ALG for probiotic coating.

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Naproxen was crystallized from acetone-water in the presence of different concentrations of hydroxypropylcellulose (HPC). Naproxen particles recrystallized in the presence of HPC exhibited an obvious improvement in their packing, flow, and mechanical properties compared to naproxen recrystallized in the absence of the polymer (control particles). The results showed that the particle size distributions of the treated samples were broader than those obtained when HPC was absent. The agglomerates produced in the presence of 0.25% HPC displayed superior flow characteristics (displaying both a low angle of repose and Carr index) in comparison to samples produced in the presence of other concentrations of HPC. This was attributed to the spherical shape and smooth surface, since the area of contact in the powder bed for spherical agglomerates was smaller than that for other crystal shapes. However it was found that the tensile strength of tablets with the particles isolated in the presence of 1% HPC was increased to a greater extent than tablets produced using the spherical particles. Generally, the tensile strengths of the tablets increased with increasing concentrations of HPC present in the crystallization medium. Differential scanning calorimetry (DSC) and X-ray powder diffraction studies showed that naproxen particles, crystallized in the presence of HPC did not undergo structural modifications.

Abstract. Microparticles of naproxen with Eudragit L100 and Aerosil were prepared by the emulsion solvent diffusion method in order to avoid local gastrointestinal irritation, one of the major side effects of nonsteroidal anti-inflammatory drugs after oral ingestion. The process of preparation involved the use of ethanol as good solvent, dichloromethane as a bridging liquid, water as poor solvent, Aerosil as antiadhesion agent, and sodium dodecyl sulfate to aid in the dispersion of the drug and excipients into the poor solvent. The obtained microparticles were evaluated for micromeritic properties, yield, encapsulation efficiency, drug physical state, and drug release properties. The influence of formulation factors and preparation condition (polymer/naproxen ratio, Aerosil/polymer ratio, and the initial difference of temperature between the solvent and nonsolvent) on the properties of the microparticles were also examined. The resultant microparticles were finely spherical and uniform with high incorporation efficiency (>79%) and yield (>71%). The incorporation efficiency was enhanced with increasing the ratio of excipients to drug and the initial difference of temperature between the solvent and nonsolvent. The mean diameter of the microparticles was influenced by all of the manufacturing parameters. Studies carried out to characterize the micromeritic properties of formulations, such as flowability and packability, showed that microparticles were suitable for further pharmaceutical manipulation (e.g., capsule filling). Drug release studies of the microparticles confirmed the gastroresistance, and mathematical studies showed that the drug released followed a Hixon and Crowell kinetic. These microparticles represent a simple method for the preparation of drug-loaded enteric microparticles with desired micromeritic properties and gastroresistance release.

The purpose of this research was to obtain directly compressible agglomerates of naproxen containing disintegrant by spherical crystallization technique. Acetone-water containing hydroxypropyl celloluse (HPC) and disintegrant was used as the crystallization system. In this study croscarmellose sodium (Ac-Di-Sol) was employed as disintegrant. The agglomerates were characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (XRPD), and scanning electron microscopy and were evaluated for flow, packing and tableting properties and drug release. The growth of particle size and the spherical form of the agglomerates resulted in formation of products with good flow and packing properties. The improved compaction properties of the agglomerated crystals were due to their fragmentation occurred during compression. DSC and XRPD studies showed that naproxen particles, crystallized in the presence of HPC and Ac-Di-Sol did not undergo structural modifications. The dissolution rate of naproxen from tablets made of naproxen-(Ac-Di-Sol) agglomerates was enhanced significantly because of including the disintegrant in to the particles. This was attributed to an increase in the surface area of the practically water insoluble drug is exposed to the dissolution medium. In conclusion the spherical crystallization technique developed in this study is suitable for obtaining agglomerates of drug with disintegrant.

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This study deals with the spherical crystallization process by the spherical agglomeration mechanism to obtain agglomerates with improved physicomechanical properties. The effect of temperature and speed of agitation on the micromeritic, mechanical and dissolution behavior of the agglomerates were investigated in order to make the link between the variables and properties of the agglomerates. Primary properties of the agglomerates were also evaluated by powder X-ray diffraction (XRPD) and differential scanning calorimetry (DSC). The mean particle size, flowability, bulk density and drug release of the agglomerates were found to be affected by either of the two variables, but there is no significant influence found on the compactibility properties. Hence, both variables must be fixed to obtained dense and well-shaped agglomerates adequate for direct tableting. XRPD and DSC results showed that during the agglomeration process, carbamazepine Form III changed to Form I.