scholarly journals The impacts of method selectivity and binders on the properties of carbamazepine granules and their applications: A case study

2021 ◽  
Author(s):  
Rahul Shete ◽  
Bhaskar Thorat ◽  
Purnima Amin
Keyword(s):  
Drug Release ◽  
Flow Behavior ◽  
Hydroxypropyl Methylcellulose ◽  
Flow Characteristics ◽  
Spherical Shape ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Binder Ratio ◽  
Hot Melt Granulation

Background: Carbamazepine (CBZ) is a BCS II class drug, having many challenges in solubility, flowability, and compactibility. The study focused on the improvement of solubility, flow behavior, and drug release of carbamazepine. Methods: Low shear granulation (LSG), extrusion spheronization (ES), high shear granulation (HSG), fluid bed granulation (FBG), and hot melt granulation (HMG) methods were employed to prepare CBZ granules. Polyvinylpyrrolidone (PVP) K29/32, PVP K90, and Hydroxypropyl methylcellulose (HPMC) E5 were used as a binder. The drug to binder ratio was maintained in the proportion of 95:5. The nature of granules was analyzed by using X-ray Diffraction and Differential Scanning Calorimetry techniques. A powder flow tester was utilized to study the flow characteristics of the granules. Results: The HMG has successfully converted the crystalline structure of CBZ granules into an amorphous form. Dispersive and distributive mixing in the HMG has achieved better solid dispersion and fast drug release. The ES technique has reported the incompressible nature of the granules. PVP K90 and HPMC E5 were superior binders for imparting strength to the CBZ granules than PVP K29/32. The FBG has exhibited the free-flowing nature of granules due to their uniform and spherical shape. Conclusion: The HMG and FBG were the most effective methods that have remarkably improved drug release, flow properties, and compactibility of CBZ granules.

scholarly journals Enhancement of solubility and dissolution rate of poorly water soluble raloxifene using microwave induced fusion method

2013 ◽  
Vol 49 (3) ◽  
pp. 571-578 ◽  
Author(s):  
Payal Hasmukhlal Patil ◽  
Veena Sailendra Belgamwar ◽  
Pratibha Ramratan Patil ◽  
Sanjay Javerilal Surana
Keyword(s):  
Dissolution Rate ◽  
Hydroxypropyl Methylcellulose ◽  
Microwave Treatment ◽  
Water Soluble ◽  
Fusion Method ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Wetting Properties ◽  
Poorly Soluble ◽  
Poorly Water Soluble

The objective of the present work was to enhance the solubility and dissolution rate of the drug raloxifene HCl (RLX), which is poorly soluble in water. The solubility of RLX was observed to increase with increasing concentration of hydroxypropyl methylcellulose (HPMC E5 LV). The optimized ratio for preparing a solid dispersion (SD) of RLX with HPMC E5 LV using the microwave-induced fusion method was 1:5 w/w. Microwave energy was used to prepare SDs. HPMC E5 LV was used as a hydrophilic carrier to enhance the solubility and dissolution rate of RLX. After microwave treatment, the drug and hydrophilic polymer are fused together, and the drug is converted from the crystalline form into an amorphous form. This was confirmed through scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) studies. These results suggested that the microwave method is a simple and efficient method of preparing SDs. The solubility and dissolution rate of the SDs were increased significantly compared with pure RLX due to the surfactant and wetting properties of HPMC E5 LV and the formation of molecular dispersions of the drug in HPMC E5 LV. It was concluded that the solubility and dissolution rate of RLX are increased significantly when an SD of the drug is prepared using the microwave-induced fusion method.

scholarly journals Preparation, characterization and scale-up of sesamol loaded solid lipid nanoparticles

2012 ◽  
Vol 2 (1) ◽  
pp. 8 ◽  
Author(s):  
Vandita Kakkar ◽  
Indu Pal Kaur
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Scale Up ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Solid Lipid ◽  
Transmission Electron ◽  
The Brain

Sesamol loaded solid lipid nanoparticles (SSLNs) were prepared with the aim of minimizing its distribution to tissues and achieving its targeting to the brain. Three scale-up batches (100x1 L) of S-SLNs were prepared using a microemulsification technique and all parameters were statistically compared with the small batch (1x;10 mL). S-SLNs with a particle size of less than 106 nm with a spherical shape (transmission electron microscopy) were successfully prepared with a total drug content and entrapment efficiency of 94.26±2.71% and 72.57±5.20%, respectively. Differential scanning calorimetry and infrared spectroscopy confirmed the formation of lipidic nanoparticles while powder X-ray diffraction revealed their amorphous profile. S-SLNs were found to be stable for three months at 5±3°C in accordance with International Conference on Harmonisation guidelines. The SLN preparation process was successfully scaled-up to a 100x batch on a laboratory scale. The procedure was easy to perform and allowed reproducible SLN dispersions to be obtained.

scholarly journals Development and In-Vitro Evaluation of pH Responsive Polymeric Nano Hydrogel Carrier System for Gastro-Protective Delivery of Naproxen Sodium

2019 ◽  
Vol 2019 ◽  
pp. 1-13
Author(s):  
Rai Muhammad Sarfraz ◽  
Muhammad Rouf Akram ◽  
Muhammad Rizwan Ali ◽  
Asif Mahmood ◽  
Muhammad Usman Khan ◽  
...  
Keyword(s):  
Drug Release ◽  
Naproxen Sodium ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Gravimetric Analysis ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Swelling Behaviour ◽  
X Ray

Current research work was carried out for gastro-protective delivery of naproxen sodium. Polyethylene glycol-g-poly (methacrylic acid) nanogels was developed through free radical polymerization technique. Formulation was characterized for swelling behaviour, entrapment efficiency, Fourier transform infrared (FTIR) spectroscopy, Differential scanning calorimetry (DSC), and Thermal Gravimetric Analysis (TGA), Powder X-ray diffraction (PXRD), Zeta size distribution, and Zeta potential measurements, and in-vitro drug release. pH dependent swelling was observed with maximum drug release at higher pH. PXRD studies confirmed the conversion of loaded drug from crystalline to amorphous form while Zeta size measurement showed size reduction. On the basis of these results it was concluded that prepared nanogels proved an effective tool for gastro-protective delivery of naproxen sodium.

scholarly journals High Throughput Screening and Characterization Methods of Jordanian Oil Shale as a Case Study

Energies ◽  
2019 ◽  
Vol 12 (16) ◽  
pp. 3148 ◽  
Author(s):  
Ziad Abu El-Rub ◽  
Joanna Kujawa ◽  
Esra’a Albarahmieh ◽  
Nafisah Al-Rifai ◽  
Fathieh Qaimari ◽  
...  
Keyword(s):  
High Throughput Screening ◽  
Oil Shale ◽  
Analytical Techniques ◽  
Economic Feasibility ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Characterization Methods ◽  
X Ray ◽  
Hydrogen Mass

Oil shale is an important possible solution to the problem of energy in Jordan. To explore the technical and the economic feasibility of oil shale deposits, numerous samples are analyzed using the standard Fischer Assay (FA) method. However, it would be useful to develop faster, cheaper, and reliable methods for determining the oil content of oil shale. Therefore, the aim of this work was to propose and investigate rapid analytical techniques for the screening of oil shale deposits and to correlate them with the FA method. The Omari deposit located east of Jordan was selected as a case study for analysis using thermogravimetric analysis (TGA) coupled with Fourier-transform infrared (FTIR), differential scanning calorimetry (DSC), elemental analysis, X-ray fluorescence (XRF), X-ray diffraction (XRD), scanning electron microscopy (SEM), and energy-dispersive X-ray (EDX) analysis. Results obtained from the TGA method were linearly correlated with FA with high regression factor (R2 = 0.99); a quadratic correlation (R2 = 0.98) was maintained between the FA and the elemental hydrogen mass content, and a quadratic correlation (R2 = 0.97) was found between the FA and the aliphatic hydrocarbons (FTIR peak at 2927 cm−1) produced in the pyrolysis zone. Although other techniques were less correlated, further investigation might lead to better results. Subsequently, these correlated techniques can be a practical alternative to the conventional FA method when, in particular, specific correlation is made for each deposit.

Fabrication and characterization of smart karaya gum/sodium alginate semi-IPN microbeads for controlled release of D-penicillamine drug

2020 ◽  
pp. 096739112090447
Author(s):  
O Sreekanth Reddy ◽  
MCS Subha ◽  
T Jithendra ◽  
C Madhavi ◽  
K Chowdoji Rao
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Polymerization Reaction ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Drug Release Kinetics ◽  
Swelling Capacity ◽  
Release Data ◽  
Karaya Gum

This article reports the fabrication of pH-sensitive microbeads from sodium alginate (SA) and modified karaya gum (KG). KG was modified by graft copolymerization using 2-hydroxyethyl methacrylate (2-HEMA) through in situ free radical polymerization reaction. The graft copolymer was blended with SA to develop microbeads by a simple ionotropic gelation technique. The microbeads were characterized by Fourier transform infrared spectroscopy, X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, and scanning electron microscopy. The effect of %HEMA and polymer blend ratio on the swelling capacity was investigated. Drug release kinetics of the microbeads was investigated under both pH 7.4 and pH 1.2 at 37°C. The drug release kinetics was analyzed by evaluating the release data using different kinetic models.

scholarly journals Preparation and Characterisation of Nobiletin-Loaded Nanostructured Lipid Carriers

2017 ◽  
Vol 2017 ◽  
pp. 1-10 ◽  
Author(s):  
Wei Huang ◽  
Huating Dou ◽  
Houjiu Wu ◽  
Zhigao Sun ◽  
Hua Wang ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Chemical Interaction ◽  
Amorphous State ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carriers ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Lipid Mixture ◽  
Food Response

The objective of this manuscript was to investigate and optimise the potential of nanostructured lipid carriers (NLCs) as a carrier system for nobiletin (NOB), which was prepared by high-pressure homogenisation method. Additionally, this study was focused on the application of NOB-loaded NLC (NOB-NLC) in functional food. Response surface method with a three-level Box–Behnken design was validated through analysis of variance, and the robustness of the design was confirmed through the correspondence between the values measured in the experiments and the predicted ones. Properties of the prepared NOB-NLC, such as Z-average, polydispersity, entrapment efficiency, zeta potential, morphology, and crystallinity, were investigated. NOB-NLC exhibited a spherical shape with a diameter of 112.27 ± 5.33 nm, zeta potential of −35.1 ± 2.94 mV, a polydispersity index of 0.251 ± 0.058, and an EE of 81.06%  ±  6.02%. Results from X-ray diffraction and differential scanning calorimetry of NOB-NLC reviewed that the NOB crystal might be converted to an amorphous state. Fourier transform infrared spectroscopic analysis demonstrated that chemical interaction was absent between the compound and lipid mixture in NOB-NLC.

scholarly journals DEVELOPMENT AND CHARACTERIZATION OF MUCOADHESIVE MICROSPHERE-LOADED INTRANASAL GEL OF VENLAFAXINE HYDROCHLORIDE

2016 ◽  
Vol 9 (9) ◽  
pp. 139
Author(s):  
Kritika Saikia ◽  
Bhupen Kalita ◽  
Banasmita Kalita
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Entrapment Efficiency ◽  
Sustained Drug Release ◽  
Scanning Calorimetry ◽  
Venlafaxine Hydrochloride ◽  
Gel Formulations ◽  
Carbopol 934P ◽  
Mucoadhesive Microsphere

ABSTRACTObjective: The main objective of the present work is to develop and characterize a novel mucoadhesive intranasal microsphere gel formulation ofdrug venlafaxine to control the drug release through nasal mucosa and reach the target site with minimal side effect. The objectives of the studyare (1) formulation of mucoadhesive microspheres, (2) evaluation of mucoadhesive microspheres, (3) formulation of mucoadhesive microsphereloadednasal gel, (4) and evaluation of nasal gel.Methods: Preparation of chitosan microsphere: The chitosan microspheres were prepared by emulsion cross-linking method. Preparation ofmicrosphere-loaded gel: The nasal gels with varying concentrations of Carbopol 934P were prepared by dispersing required quantity of Carbopol inrequired quantity of distilled water with continuous stirring and kept overnight for complete hydration. The gel was then modified by the addition ofvarying proportion of hydroxypropyl methylcellulose (HPMC) K4M.Results: The prepared microspheres were evaluated for size distribution, surface morphology by scanning electron microscopy, entrapment efficiency,compatibility by Fourier transform infrared spectroscopy, and differential scanning calorimetry. Entrapment efficiency of all formulations was foundmore than 70%. Microsphere formulation containing drug and polymer in the ratio of 1:2.5 was found to be optimized. Optimized microsphereformulation was then incorporated in gel prepared using Carbopol 934P and HPMC. Prepared gel formulations were studied for viscosity, spreadability,and in-vitro drug release in simulated nasal conditions. Viscosity of the optimized batch of gel was recorded at 1056 centipoise. Drug release wasprolonged for the microsphere-in-gel formulations compared to the microspheres alone. For the optimized batch of gel, cumulative drug release of85.67% was found after 8 hrs.Conclusion: The results suggest that venlafaxine hydrochloride mucoadhesive microsphere-loaded nasal gel would give sustained drug release andsuperior bioavailability in the brain sites.Keywords: Venlafaxine, Chitosan, Mucoadhesive, Microsphere, Nasal gel.

scholarly journals UNSUCCESSFUL DELIVERY OF TETRANDRINE FROM COLON-TARGETED DOSAGE FORMS COMPRISING ALGINATE/HYDROXYPROPYL METHYLCELLULOSE AND ALGINATE–CHITOSAN BEADS

2018 ◽  
Vol 10 (1) ◽  
pp. 396
Author(s):  
Raditya Iswandana ◽  
Metah Putri Mutia ◽  
Farahia Khairina Widyaningrum
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
Dosage Forms ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Chitosan Beads ◽  
X Ray ◽  
Moisture Contents ◽  
Ph Conditions ◽  
Upper Gastrointestinal

Objective: The objective of this study was to optimize the formulations of antifibrotic tetrandrine beads using alginate and various concentrations ofhydroxypropyl methylcellulose (HPMC) and chitosan.Methods: Beads were formulated with six (F1–F6) concentrations of polymer and were then characterized using scanning electron microscopy,differential scanning calorimetry, and X-ray diffraction; these beads were used for measurements of moisture contents, swelling, and in vitro drugrelease.Results: Beads with the highest concentrations of HPMC and chitosan produced the highest entrapment efficiencies of 49.83% and 50.71%,respectively. Moreover, drug release under stomach conditions (HCl pH 1.2 medium) was restricted to 75.01%, 61.01%, 51.86%, 74.84%, 66.00%,and 41.63% with increasing HPMC and chitosan concentrations (F1–F6, respectively).Conclusion: Beads of all formulations showed inadequate retention of tetrandrine under pH conditions of the upper gastrointestinal tract and wouldlikely be unsuccessful as colon-targeted dosage forms.

scholarly journals Novel Solid Dispersions of Naphthoquinone Using Different Polymers for Improvement of Antichagasic Activity

Pharmaceutics ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 1136
Author(s):  
Verônica da Silva Oliveira ◽  
Elen Diana Dantas ◽  
Anna Thereza de Sousa Queiroz ◽  
Johny Wysllas de Freitas Oliveira ◽  
Marcelo de Sousa da Silva ◽  
...  
Keyword(s):  
Biological Activities ◽  
Solid Dispersions ◽  
Hydroxypropyl Methylcellulose ◽  
Chemical Characterization ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Rotary Evaporation ◽  
A Value ◽  
Low Solubility

IVS320 (3a,10b-dihydro-1H-cyclopenta[b]naphtho[2,3-d]furan-5,10-dione) is a naphthoquinone that has low solubility in aqueous medium, a physical behavior that limits its biological activities, considering that compounds from this class have several activities. In this work, solid dispersions (SDs) prepared between IVS320 and polymers hydroxypropyl methylcellulose (HPMC), polyethylene glycol (PEG), and polyvinylpyrrolidone (PVP) were developed using physical mixture (PM), kneading (KN), and rotary evaporation (RE) methods. Dispersions were investigated using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetry (TG), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). In addition, in vitro antiparasitic activity in Trypanosoma cruzi Y strains was evaluated. Physical-chemical characterization demonstrated the formation of SDs through the interaction of IVS320 with polymeric matrices. SDs of IVS320-polymer presented a significant potentiation of antichagasic activity, with inhibitory growth around 62% (IVS320-HPMC/RE), 55% (IVS320-PEG/RE), and 85% (IVS320-PVP/RE), while pure IVS320 showed a value of 48% for the highest concentrations evaluated (50 µg/mL).

scholarly journals Spherical crystals of celecoxib to improve solubility, dissolution rate and micromeritic properties

2007 ◽  
Vol 57 (2) ◽  
pp. 173-184 ◽  
Author(s):  
Venkadari Gupta ◽  
Srinivas Mutalik ◽  
Madhobhai Patel ◽  
Girish Jani
Keyword(s):  
Dissolution Rate ◽  
Spherical Shape ◽  
Aqueous Solubility ◽  
Spectroscopic Studies ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Acetone Water ◽  
Ir Spectroscopic ◽  
Spherical Crystals

Spherical crystals of celecoxib to improve solubility, dissolution rate and micromeritic propertiesCelecoxib spherical agglomerates were prepared with polyvinylpyrrolidone (PVP) using acetone, water and chloroform as solvent, non-solvent and bridging liquid, respectively. The agglomerates were characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD), IR spectroscopic studies and scanning electron microscopy (SEM). The IR spectroscopy and DSC results indicated the absence of any interactions between drug and additives. XRD studies showed a decrease in crystallinity in agglomerates. The crystals exhibited significantly improved micromeritic properties compared to pure drug. The loading efficiency (% or mg drug per 100 mg crystals) was in the range of 93.9 ± 2.3 and 97.3 ± 1.3% (n = 3) with all formulations. The aqueous solubility and dissolution rate of the drug from crystals was significantly (p < 0.05) increased (nearly two times). The solubility andin vitrodrug release rates increased with an increase in PVP concentration (from 2.5 to 10%). The SEM studies showed that the crystal posseses a good spherical shape with smooth and regular surface.

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