scholarly journals SPHERICAL CRYSTALLIZATION A NOVEL APPROACH FOR SOLUBILITY AND DISSOLUTION ENHANCEMENT OF SIMVASTATIN

Author(s):  
Rakesh Kumar Mishra

Simvastatin is commonly used antihyperlipidemic in the treatment of hypercholesterolemia and dyslipidemia. As evidenced form the scientific investigation, it is reported for its lower solubility and poor dissolution rate. The aim of the present investigation was to develop simvastatin spherical agglomerates to improve its solubility and dissolution characteristics by spherical agglomeration method. The crystallization media used was methanol, water and chloroform as bridging liquid and PVP K-30 as a polymer. The process variables such as amount and type of (bridging liquid and polymer), stirring speed and stirring time were optimized and reported. The spherical agglomerates were further subjected for determination of % drug content, particle size analysis, solubility and dissolution rate. The agglomerates were also characterized by Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FTIR), and X-ray Powder Diffraction (XRD) analysis and affirmed. Among the entire parameters spherical agglomerates obtained with methanol (7ml), water (50ml), chloroform (1.5ml) and PVP K-30 (0.5%) showed improvement in solubility and dissolution rate in comparison with pure drug. The spherical agglomerates showed significant improvement in dissolution from a value of 25.53% for pure simvastatin to 91.31% of spherical agglomerate. The spherical agglomerates of optimized batch were directly compressed and dissolution profile was compared with marketed tablet. Such a technique can successfully be employed to improve solubility and dissolution characteristic of poorly soluble drugs.

2019 ◽  
Vol 10 (3) ◽  
pp. 2290-2299 ◽  
Author(s):  
Manoj K ◽  
Seenivasan P ◽  
Arul K ◽  
Senthil kumar M

Polymer Enriched Bridging liquid is a novel approach for enhancing the flow characteristics, properties, solubility and dissolution of poorly water-soluble drugs. is an orally effective II receptor antagonist used extensively for the effective management of hypertension. is a poorly water-soluble drug and an ideal candidate for this approach. PVPK30 is used as the hydrophilic polymer. Various formulations were prepared with the addition of PVPK30 in the bridging liquid by Polymer Enriched Bridging Liquid Technique (PEBL). The preparations were subjected to particle size analysis, characteristics, FTIR, differential scanning (DSC) and Scanning Electron microscopic analysis. The crystal agglomerates were found to be spherical in nature with excellent flow characteristics. The of the pure drug was found to be decreased without any drug-polymer interaction. The saturation solubility studies showed that the optimized formulation STP04 showed 30.695 folds increase in solubility in water and 29.462 folds enhancement in pH 7.5 phosphate buffer. The in drug release studies also confirmed the enhancement in dissolution rate. The stability of the prepared aggregates was determined by accelerated stability studies. The addition of polymer in the bridging liquid during crystallization stage improved the effective incorporation of the hydrophilic polymer in the aggregates. Polymer Enriched Bridging Liquid technique can be considered as an ideal technique for solubility and dissolution enhancement.


1970 ◽  
Vol 4 (1) ◽  
pp. 1-8 ◽  
Author(s):  
Parthasarathi Keshavarao Kulkarni ◽  
Mudit Dixit ◽  
Achin Jain

Naproxen, an anti-inflammatory drug, exhibits poor water solubility and flow properties. Spherical agglomerates were prepared by solvent change method. Solvent composition for spherical agglomeration was determined by constructing ternary diagram. Crystallization medium used for spherical agglomerates of naproxen consisted of tetra-hydro-furan (good solvent); water (poor solvent); isopropyl acetate (bridging liquid) in the ratio of 29:61:10, respectively. Spherical agglomerates were characterized by differential scanning calorimetry, infrared spectroscopy, X-ray diffractometry and scanning electron microscopy. Micromeritic and dissolution behavior studies were carried out. Process variables such as amount of bridging liquid, stirring time and duration of stirring were optimized. Dissolution profile of the spherical agglomerates was compared with pure sample and recrystallized sample. Spherical agglomerates exhibited decreased crystallinity and improved micromeritic properties. The dissolution of the spherical agglomerates was not improved compared with pure sample because the dissolution of naproxen dependent on particle size or surface area.   Key words: Spherical agglomerates; Naproxen; Crystallinity; Dissolution.DOI: http://dx.doi.org/10.3329/sjps.v4i1.8860 SJPS 2011; 4(1): 1-8


2021 ◽  
Vol 14 (5) ◽  
pp. 397
Author(s):  
Carlos Benavent ◽  
Carlos Torrado-Salmerón ◽  
Santiago Torrado-Santiago

The aim of this study was to improve the treatment of Candida albicans biofilms through the use of nystatin solid dispersions developed using maltodextrins as a hyperosmotic carrier. Characterization studies by differential scanning calorimetry, X-ray diffraction, dissolution studies, and particle size analysis were performed to evaluate changes in nystatin crystallinity. Antifungal activity and anti-biofilm efficacy were assessed by microbiological techniques. The results for nystatin solid dispersions showed that the enhancement of antifungal activity may be related to the high proportions of maltodextrins. Anti-biofilm assays showed a significant reduction (more than 80%) on biofilm formation with SD-N:MD [1:6] compared to the nystatin reference suspension. The elaboration process and physicochemical properties of SD-N:MD [1:6] could be a promising strategy for treatment of Candida biofilms.


INDIAN DRUGS ◽  
2021 ◽  
Vol 57 (11) ◽  
pp. 22-26
Author(s):  
Manisha Dhere ◽  
◽  
Arti Majumdar ◽  
Neelesh Malviya

In the present research, newly developed complex with sodium caprylate was investigated for solubility and dissolution enhancement of eluxadoline. Complexes were prepared in different ratios by solvent evaporation method and characterised solubility study, Infrared spectroscopy (IR), Diffrential scanning calorimetry (DSC), X-Ray Diffraction (XRD), drug content analysis and in vitro Drug release. The solubility and dissolution rate revealed most suitable ratio of eluxadoline and sodium caprylate (1:4). The IR, DSC and X-RD data also confirmed the results. It was concluded that complex prepared with (1:4 drug:sodium caprylate ratio) using solvent evaporation method showed significant improvement in solubility and drug dissolution.


1986 ◽  
Vol 17 (3) ◽  
pp. 530-536 ◽  
Author(s):  
Ephraim F. Aharonson ◽  
Nir Karasikov ◽  
Moshe Roitberg ◽  
Joseph Shamir

2011 ◽  
Vol 317-319 ◽  
pp. 185-188 ◽  
Author(s):  
Pornsak Sriamornsak ◽  
Srisuda Kontong ◽  
Yotsanan Weerapol ◽  
Jurairat Nunthanid ◽  
Srisagul Sungthongjeen ◽  
...  

The aim of this study was to manufacture the ternary solid dispersions composed of nifedipine, Eudragit® E and adsorbent. Dissolution enhancement of nifedipine was also investigated. The inert solid carriers were added in the mixtures of nifedipine and Eudragit® E at varying ratios. The physicochemical properties of ternary systems, compared to physical mixtures, were analyzed using powder x-ray diffraction (PXRD) and differential scanning calorimetry (DSC). The dissolution of nifedipine from ternary systems was compared to the drug alone. The influence of drug:polymer: adsorbent ratio and type of adsorbent on the dissolution rate of the drug was also evaluated. The PXRD and DSC results of the systems with high amount of polymer showed that the drug was present in an amorphous form. On the other hand, the diffraction patterns and DSC thermograms of the physical mixtures revealed that to some extent the drug was present in a crystalline form. The results from this study demonstrated that an improvement in dissolution rate of nifedipine with Eudragit® E and adsorbents was obtained.


2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Y. Eshovo Apeji ◽  
IY. Muhammad ◽  
A. Kehinde Olowosulu ◽  
G. Owoicho Okpanachi ◽  
A. Rukayat Oyi

Abstract Diluents are essential components of a tablet formulation. The type of diluent used in a formulation influences the quality of tablets produced from that formulation. The aim of this study was to evaluate the tableting properties of co-processed excipients (C-PEs) incorporated as diluents in tablet formulation by wet granulation. Metronidazole tablets were prepared by wet granulation incorporating different diluents that were either single component excipients (SCEs) (lactose and microcrystalline cellulose) or C-PEs (Ludipress®, StarLac®, Prosolv® and AVICEL®HFE). The granules obtained for each formulation were evaluated for particle size analysis, flow properties and compression properties. Tablets weighing 500 mg were compressed from the metronidazole granules on a Single Station Tablet Press using a 12 mm punch and die tooling system. The tablets were kept for 24 h post-production, and the properties of weight uniformity, thickness, tensile strength, friability, disintegration time and dissolution profile evaluated subsequently. Results of granule properties showed that variations in parameters evaluated was as a result of differences in the type and composition of diluent used in formulation. Compactibility and tabletability profile of metronidazole granules revealed a better performance with granules processed with C-PE based diluents compared to SCE-based diluents. Tablets formulated with C-PEs as diluents were uniform in tablet weight, disintegrated faster and yielded a faster drug release compared to tablet formulations containing SCEs as diluent. This study reveals the performance advantage of C-PEs as diluents in tablets manufactured by wet granulation and highlights the importance of rational selection of excipients during tablet formulation.


2020 ◽  
pp. 089270572096215
Author(s):  
Maryam Ataeefard ◽  
Mohammad Mahdi Salehi

The main element of electrophotographic (EP) printing and copying devices is a polymeric composite called toner and one of the most significant components of toner composite is an iron oxide (magnetite). Magnetite, which is applied as a colorant and additive for toner is the main mineral able to develop an electrical charge on the printing procedure. Although there are several ways to produce magnetite, given the dearth of resources and environmental aspect, it is safer to practice recycling and greener method. In the present study, an encouraging way to reuse the magnetite particles as a byproduct of the preparation of micro silica in the concrete industry was described. The obtained magnetite was then utilized as the charge control agent to produce magnetite/carbon black/styrene co-butyl acrylate composite microspheres by green emulsion aggregation method, which is used as toner in the printing procedure. Characterization of toner and recovered magnetite was done by X-ray Powder Diffraction (XRD), Atomic Gradient Force Magnetometry (AGFM), Particle Size Analysis (PSA), Differential Scanning Calorimetry (DSC), and Scanning Electron Microscopy with Energy Dispersive X-Ray (SEM-EDX). The results supported the fact that the produced toner composite by recycled waste magnetite show suitable characteristics comparing to an industrial toner.


2011 ◽  
Vol 61 (4) ◽  
pp. 391-402 ◽  
Author(s):  
Lim Lyn ◽  
Huan Sze ◽  
Adhiyaman Rajendran ◽  
Gorajana Adinarayana ◽  
Kamal Dua ◽  
...  

Crystal modifications and dissolution rate of piroxicam Piroxicam is a nonsteroidal anti-inflammatory drug with low aqueous solubility which exhibits polymorphism. The present study was carried out to develop polymorphs of piroxicam with enhanced solubility and dissolution rate by the crystal modification technique using different solvent mixtures prepared with PEG 4000 and PVP K30. Physicochemical characteristics of the modified crystal forms of piroxicam were investigated by X-ray powder diffractometry, FT-IR spectrophotometry and differential scanning calorimetry. Dissolution and solubility profiles of each modified crystal form were studied and compared with pure piroxicam. Solvent evaporation method (method I) produced both needle and cubic shaped crystals. Slow crystallization from ethanol with addition of PEG 4000 or PVP K30 at room temperature (method II) produced cubic crystal forms. Needle forms produced by method I improved dissolution but not solubility. Cubic crystals produced by method I had a dissolution profile similar to that of untreated piroxicam but showed better solubility than untreated piroxicam. Cubic shaped crystals produced by method II showed improved dissolution, without a significant change in solubility. Based on the XRPD results, modified piroxicam crystals obtained by method I from acetone/benzene were cube shaped, which correlates well with the FTIR spectrum; modified needle forms obtained from ethanol/methanol and ethanol/acetone showed a slight shift of FTIR peak that may be attributed to differences in the internal structure or conformation.


2011 ◽  
Vol 311-313 ◽  
pp. 96-100
Author(s):  
Jian Li Cheng ◽  
Cun Zhou ◽  
Hao Peng ◽  
Huan Wang ◽  
Yu Sun

Two kind of polyimide/silica nanocomposites which were recorded poly(amic acid)/ silica(PAA/SiO2) and SiO2in poly(amic acid) ammonium salt(PAS/SiO2) respectively, have been prepared for different methods. The size of SiO2in PAA/SiO2and PAS/SiO2are measured by Particle size analysis and the average particle size are 377nm and 53.7nm. Transmission electron microscopy(TEM) images of PAS/ SiO2confirm that the size of particles are ranged from 40 to 80nm. The stuctures of samples have been characterized by FT-IR spectra. The thermal stability of PAA/SiO2and PAS/SiO2are studied by thermogravimetric analysis (TGA) and the thermal behaviors were investigated by differential scanning calorimetry (DSC) in this paper. It is shown that PAA/SiO2have slightly better thermal properties than that of PAS/SiO2. The results obtained from Instron universal strength tester present the water-solube PAS/SiO2own the excellent mechanical prperties as same as PAA/SiO2.


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