scholarly journals Insight into the Formation of Glimepiride Nanocrystals by Wet Media Milling

Pharmaceutics ◽  
2020 ◽  
Vol 12 (1) ◽  
pp. 53 ◽  
Author(s):  
Djordje Medarević ◽  
Svetlana Ibrić ◽  
Elisavet Vardaka ◽  
Miodrag Mitrić ◽  
Ioannis Nikolakakis ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Spray Drying ◽  
Lattice Energy ◽  
Superior Performance ◽  
Dissolution Enhancement ◽  
Polymorphic Transformations ◽  
Topology Analysis ◽  
Media Milling ◽  
Ft Ir ◽  
Insight Into

Nanocrystal formation for the dissolution enhancement of glimepiride was attempted by wet media milling. Different stabilizers were tested and the obtained nanosuspensions were solidified by spray drying in presence of mannitol, and characterized regarding their redispersibility by dynamic light scattering, physicochemical properties by differential scanning calorimetry (DSC), FT-IR spectroscopy, powder X-ray diffraction (PXRD), and scanning electron microcopy (SEM), as well as dissolution rate. Lattice energy frameworks combined with topology analysis were used in order to gain insight into the mechanisms of particle fracture. It was found that nanosuspensions with narrow size distribution can be obtained in presence of poloxamer 188, HPC-SL and Pharmacoat® 603 stabilizers, with poloxamer giving poor redispersibility due to melting and sticking of nanocrystals during spray drying. DSC and FT-IR studies showed that glimepiride does not undergo polymorphic transformations during processing, and that the milling process induces changes in the hydrogen bonding patterns of glimepiride crystals. Lattice energy framework and topology analysis revealed the existence of a possible slip plane on the (101) surface, which was experimentally verified by PXRD analysis. Dissolution testing proved the superior performance of nanocrystals, and emphasized the important influence of the stabilizer on the dissolution rate of the nanocrystals.

Formulation and Characterization of Glimepiride Nanoparticles for Dissolution Enhancement

2020 ◽  
Vol 10 (5) ◽  
pp. 649-663
Author(s):  
Reena Siwach ◽  
Parijat Pandey ◽  
Harish Dureja
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Oral Absorption ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Class Ii ◽  
Dissolution Enhancement ◽  
In Vitro Drug Release ◽  
Bcs Class Ii

Background: The rate-limiting step in the oral absorption of BCS class II drugs is dissolution. Their low solubility is one of the major obstacles in the process of drug development. Dissolution rate can be increased by decreasing the particle size to the nano range, eventually leading to increased bioavailability. Objective: : In the present study, glimepiride loaded nanoparticles were prepared to enhance the dissolution rate. The aim of the work was to examine the effect of polymer-drug ratio, solvent-antisolvent ratio and speed of mixing on in vitro release of glimepiride. Methods: Glimepiride is an antidiabetic drug belonging to the BCS class II drugs. The polymeric nanoparticles were formulated according to Box-Behnken Design (BBD) using nanoprecipitation technique. The prepared nanoparticles were evaluated for in vitro drug release, loading capacity, entrapment efficiency, and percentage yield. Result: It was found that NP-8 has maximum in vitro drug release and was selected as an optimized batch. Analysis of Variance (ANOVA) was applied to the in vitro drug release to study the fitness and significance of the model. The batch NP-8 showed 70.34 ± 1.09% in vitro drug release in 0.1 N methanolic HCl and 92.02 ± 1.87% drug release in phosphate buffer pH 7.8. The release data revealed that the nanoparticles followed zero order kinetics. Conclusion: The study revealed that the incorporation of glimepiride into gelucire 50/13 resulted in enhanced dissolution rate.

Crystal structure and lattice energetics of 10-methylacridinium halides

2000 ◽  
Vol 53 (8) ◽  
pp. 627 ◽  
Author(s):  
Piotr Storoniak ◽  
Karol Krzyminski ◽  
Pawel Dokurno ◽  
Antoni Konitz ◽  
Jerzy Blazejowski
Keyword(s):  
Crystal Lattice ◽  
Lattice Energy ◽  
Enthalpies Of Formation ◽  
Triclinic Space Group ◽  
X Ray ◽  
Molecular Arrangement ◽  
Van Der Waals Contacts ◽  
Chloride Monohydrate ◽  
Insight Into

The crystal structures of 10-methylacridinium chloride monohydrate, bromide monohydrate and iodide were determined by X-ray analysis. The compounds crystallize in the triclinic space group, P¯1, with 2 molecules in the unit cell. The molecular arrangement in the crystals revealed that hydrogen bonds (in hydrates) and van der Waals contacts play a significant part in intermolecular interactions. To discover their nature, contributions to the crystal lattice energy arising from electrostatic (the most important since the compounds form ionic crystals), dispersive and repulsive interactions were calculated. Enthalpies of formation of the salts, their stability and susceptibility to decomposition could be predicted from a combination of crystal lattice energies with values of other thermochemical characteristics obtained theoretically or taken from the literature. The role of water in the stabilization of the crystal lattice of the hydrates is also explained. The information gathered has given an insight into the features and behaviour of compounds which can be regarded as models of a large group of aromatic quaternary nitrogen salts.

AN ENHANCEMENT OF SOLUBILITY OF PIOGLITAZONE HYDROCHLORIDE USING LIQUISOLID TECHNIQUE

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (06) ◽  
pp. 36-39
Author(s):  
S Deshmane ◽  
◽  
K Gandhi ◽  
S. Nagpure ◽  
A. Sawant ◽  
...  
Keyword(s):  
Mathematical Model ◽  
Drug Release ◽  
Dissolution Rate ◽  
In Vivo Study ◽  
Dimethyl Acetamide ◽  
Volatile Liquid ◽  
Ft Ir ◽  
Ir Study

The new mathematical model was developed by studying angle of slide using N, N-dimethyl acetamide, non-volatile liquid vehicle and prepared liquisolid tablets, in which the different concentrations of non-volatile liquid adsorbed over carrier and coating material separately. Both DSC and FT-IR study showed better compatibility and stability. The optimized formulation showed higher drug release during in-vitro and in-vivo study against conventional and marketed preparation. The present work concludes that N, N-dimethyl acetamide enhanced the solubility of pioglitazone HCl with higher dissolution rate through liquisolid technique.

scholarly journals Systematic Finite-Temperature Reduction of Crystal Energy Landscapes.

2020 ◽  
Author(s):  
Nicholas Francia ◽  
Louise S. Price ◽  
Jonas Nyman ◽  
Sarah (Sally) Price ◽  
Matteo Salvalaglio
Keyword(s):  
Molecular Dynamics ◽  
Finite Temperature ◽  
Structure Prediction ◽  
Lattice Energy ◽  
Biased Sampling ◽  
Energy Landscapes ◽  
Polymorphic Transformations ◽  
Temperature And Pressure ◽  
Dynamics Simulations ◽  
The Impact

<p>Crystal structure prediction methods are prone to overestimate the number of potential polymorphs of organic molecules. In this work, we aim to reduce the overprediction by systematically applying molecular dynamics simulations and biased sampling methods to cluster subsets of structures that can easily interconvert at finite temperature and pressure. Following this approach, we rationally reduce the number of predicted putative polymorphs in CSP-generated crystal energy landscapes. This uses an unsupervised clustering approach to analyze independent finite-temperature molecular dynamics trajectories and hence identify a representative structure of each cluster of distinct lattice energy minima that are effectively equivalent at finite temperature and pressure. Biased simulations are used to reduce the impact of limited sampling time and to estimate the work associated with polymorphic transformations. We demonstrate the proposed systematic approach by studying the polymorphs of urea and succinic acid, reducing an initial set of over 100 energetically plausible CSP structures to 12 and 27 respectively, including the experimentally known polymorphs. The simulations also indicate the types of disorder and stacking errors that may occur in real structures.<br></p>

Controllable synthesis of Mo2C with different morphology and application to electrocatalytic hydrogen evolution reaction

2021 ◽  
Author(s):  
He-qiang Chang ◽  
Guo-Hua Zhang ◽  
Kuo-Chih Chou
Keyword(s):  
Hydrogen Evolution ◽  
Hydrogen Evolution Reaction ◽  
Structural Design ◽  
Superior Performance ◽  
Controllable Synthesis ◽  
Nitridation Reaction ◽  
Special Surface ◽  
One Step ◽  
The One ◽  
Insight Into

Abstract In order to evaluate the effect of precursors and synthesis strategies on catalytic ability of Mo2C in the hydrogen evolution reaction (HER), four kinds of Mo2C were synthesized using two kinds of MoO3 by two strategies. Compared with the one-step direct carbonization strategy, Mo2C with a large special surface area and a better performance could be synthesized by the two-step strategy composed of a nitridation reaction and a carbonization reaction. Additionally, the as-prepared porous Mo2C nanobelts (NBs) exhibit good electrocatalytic performance with a small overpotential of 165 mV (0.5 M H2SO4) and 124 mV (1 M KOH) at 10 mA cm-2, as well as a Tafel slope of 58 mV dec-1 (0.5 M H2SO4) and 59 mV dec-1 (1 M KOH). The excellent catalytic activity is ascribed to the nano crystallites and porous structure. What’s more, the belt structure also facilitates the charge transport in the materials during the electrocatalytic HER process. Therefore, the two-step strategy provides a new insight into the structural design with superior performance for electrocatalytic HER.

COMPLEX OF ELUXADOLINE WITH SODIUM CAPRYLATE FOR IMPROVED SOLUBILITY AND DISSOLUTION RATE

INDIAN DRUGS ◽  
2021 ◽  
Vol 57 (11) ◽  
pp. 22-26
Author(s):  
Manisha Dhere ◽  
◽  
Arti Majumdar ◽  
Neelesh Malviya
Keyword(s):  
Dissolution Rate ◽  
Solvent Evaporation ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Solvent Evaporation Method ◽  
Scanning Calorimetry ◽  
Evaporation Method ◽  
Solubility Study ◽  
Sodium Caprylate

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.

scholarly journals DESIGN AND DEVELOPMENT OF NOVEL DRUG DELIVERY SYSTEM USING HERBAL MEDICINE TO TREAT ALZHEIMER’S DISEASE

2019 ◽  
pp. 202-210
Author(s):  
RAMA RAO NADENDLA ◽  
LAKSHMI SWAPNA SAI ◽  
NIHITHA SANKA ◽  
SANTHI PRIYA NAGAM
Keyword(s):  
Particle Size ◽  
Spray Drying ◽  
Herbal Extracts ◽  
Natural Polymer ◽  
Herbal Formulation ◽  
Behavioral Studies ◽  
Ft Ir ◽  
Novel Drug Delivery System ◽  
Novel Drug ◽  
Spray Dried

Objective: The present study was focused to design an herbal formulation for the treatment of Alzheimer’s disease (AD) to develop the formulation using various techniques such as spray drying, centrifugation, and lyophilization and to conduct behavioral studies to evaluate the activity of the herbal formulation. Methods: Formulation contains herbal extracts such as curcumin, guggul, and ashwagandha. To develop this formulation, various techniques such as spray drying, centrifugation, and lyophilization were employed along with a natural polymer chitosan in various combinations of excipient. Preformulation studies such as solubility of herbal extracts and Fourier transmission infrared spectroscopy (FT-IR) studies for compatibility of the natural polymer with herbal extracts were studied. The formulation was characterized by tests such as particle size determination using optical microscopy, surface morphological evaluation using scanning electron microscopy (SEM), and behavioral testing by Morris water maze test using diazepam-induced amnesia method. Results: The particle size varied from 12.27 μ for normal chitosan to 3.59 μ for spray-dried chitosan. In the same way, the particle of normal formulation (12.9 μ) was about 4–5 times larger than that of spray-dried formulation (2.7 μ). The SEM images showed no proper morphology for chitosan, round surface with wrinkles for spray-dried chitosan, improper structures for normal formulation, and rounded smooth surface for spray-dried formulation. Significant p value was shown when the spray-dried test formulation was tested using diazepam-induced amnesia method. The transfer latency was noted on the 8th day and after 24 h of intraperitoneal administration of diazepam for the test group. Conclusion: In the present research study, an attempt was made to design and develop a novel drug delivery system using herbal medicine to treat AD. FT-IR compatibility study was carried out using the selected polymer and the herbal extracts using novel spray-drying techniques; behavioral studies were also done.

Sign in / Sign up

Export Citation Format

Share Document