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 Development of an Oxcarbazepine Solid Dispersion Using Skimmed Milk to Improve the Solubility and Dissolution Profile

2019 ◽  
Vol 11 (05) ◽  
Author(s):  
M. Shah ◽  
D. Patel
Keyword(s):  
Electron Microscopy ◽  
Solid Dispersion ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Infra Red ◽  
Crystalline Nature ◽  
Skimmed Milk ◽  
Scanning Electron

Oxcarbazepine has low solubility and low oral bioavailability, so it’s a challenge to formulate suitable dosage form. In this present investigation, to improve the dissolution rate and solubility, skimmed milk is used as a carrier. Physical mixers were prepared using various drugs to carrier ratio and spray drying technology was used to develop solid dispersion with the carrier. Various techniques were used to characterize the solid dispersion immediately after they were made which includes differential scanning calorimetry, scanning electron microscopy, fourier transform infra- red spectroscopy, X-ray diffraction and in-vitro dissolution profiles. The differential scanning calorimetry thermograms of raw drug indicated of its anhydrous crystalline nature. In thermograms of solid dispersion, the characteristic peak was absent suggesting the change from crystalline nature to amorphous form. X-ray diffraction confirmed those results. X-ray diffraction results of raw drug showed highly intense peak characteristic of its crystalline nature where solid dispersion showed less intense, more diffused peak indicating the change in crystalline form. Fourier transforms infra-red spectroscopy studies showed there was no interaction between drug and carrier. Scanning electron microscopy support the amorphous nature of mixer. The whole formulation showed distinct enhancement in the drug release behavior and solubility. The optimum oxcarbazepine to skimmed milk ratio 1:3 enhances the in-vitro drug release by 3.5 fold and also show distinct increase in solubility. It was concluded that for improvement of solubility of poorly water soluble oxcarbazepine, skimmed milk powder as a carrier can be utilize very well.

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.

The preparation, characterization, structure and dissolution analysis of apremilast solvatomorphs

2017 ◽  
Vol 73 (4) ◽  
pp. 305-313 ◽  
Author(s):  
Yun-Deng Wu ◽  
Xiao-Lei Zhang ◽  
Xiao-Hong Liu ◽  
Jian Xu ◽  
Mei Zhang ◽  
...  
Keyword(s):  
Differential Scanning Calorimetry ◽  
Hydrogen Bonding ◽  
Psoriatic Arthritis ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Dissolution Rates ◽  
X Ray ◽  
Similarity Factor ◽  
Hydrogen Bonding Interactions

Apremilast (AP) {systematic name: (S)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-4-acetamidoisoindoline-1,3-dione} is an inhibitor of phosphodieasterase-4 (PDE4) and is indicated for the treatment of adult patients with active psoriatic arthritis. The ability of AP to form solvates has been investigated and three solvatomorphs of AP, namely, the AP ethyl acetate hemisolvate, C22H24N2O7S·0.5C4H8O2, the AP toluene hemisolvate, C22H24N2O7S·0.5C7H8, and the AP dichloromethane monosolvate, C22H24N2O7S·CH2Cl2, were obtained. The three AP solvatomorphs were characterized by X-ray powder diffraction, thermogravimetric analysis and differential scanning calorimetry. Single-crystal X-ray diffraction was used to analyze the structures, crystal symmetry, packing modes, stoichiometry and hydrogen-bonding interactions of the solvatomorphs. In addition, dissolution analyses were performed to study the dissolution rates of different AP solvatomorph tablets in vitro and to make comparisons with commercial apremilast tablets (produced by Celgene); all three solvatomorphs showed similar dissolution rates and similar values of the similarity factor f2 in a comparison of their dissolution profiles.

scholarly journals Hydrophilic Sugars for Enhancing Dissolution Rate of Cilostazol: Effect of Wet Co-Processing

2020 ◽  
Vol 27 (1) ◽  
pp. 111-120
Author(s):  
Alaa Yosf Bazeed ◽  
Ahmed Nouh ◽  
Ebtessam Ahmed Essa ◽  
Gamal El Maghraby
Keyword(s):  
Aqueous Solubility ◽  
Submicron Particles ◽  
Drug Dissolution ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Swallowing Difficulties ◽  
Fast Disintegrating Tablets

Background: Cilostazol is an anti-platelets drug with considerable antithrombotic effects in vivo. Therefore, it is widely used by elderly patients. However, it suffers from poor bioavailability due to its low aqueous solubility. The objective of this work was to enhance the dissolution of cilostazol with the aim of formulating fast dissolving tablets for geriatrics and those of swallowing difficulties. Methods: Ethanol-assisted co-grinding of cilostazol with sugar-based excipients was adopted. Sucralose and mannitol were used for this purpose as hydrophilic excipient as well as taste improving agents. The obtained products were investigated regarding differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction, scanning electron microscope (SEM) and in vitro drug dissolution. Fast disintegrating tablets were prepared and evaluated. Results: Thermal behavior of the developed products reflected reduced crystallinity, it also suggested possible existence of new crystalline species with sucralose. Eutexia was also suggested for mannitol mixtures, that was supported by X-ray diffraction data. SEM indicated size reduction with the deposition of the drug as submicron particles over the excipient surface. Co-processing markedly improved cilostazol dissolution compared to unprocessed drug. The optimized formulations were successively formulated into fast disintegrating tablets. Conclusion: This investigation introduced the wet grinding strategy with sugar excipients as a platform for the formulation of easy to use tablets with optimum drug release.

scholarly journals FORMULATION ANDCHARACTERIZATION OF OLANZEPINELOADED MUCOADHESIVE MICROSPHERES

2017 ◽  
Vol 10 (4) ◽  
pp. 249
Author(s):  
Madhuri T Deshmukh ◽  
Shrinivas K Mohite
Keyword(s):  
Fourier Transforms ◽  
Crosslinking Agent ◽  
Entrapment Efficiency ◽  
Ionic Gelation ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Model Stability ◽  
X Ray ◽  
Mucoadhesive Microsphere

Objective: The objective of this research was to formulate and evaluate olanzapine (OLE) mucoadhesive microsphere prepared using carbopol and sodium combination. OLE having extensive hepatic first pass metabolism and low bioavailability problem, determined the need for the development of sustained release formulation.Methods: OLE mucoadhesive microspheres were prepared by ionic gelation method. OLE mucoadhesive microspheres were prepared byionic gelation method by using calcium chloride as crosslinking agent. The OLE mucoadhesive microsphere was characterized by particle sizemeasurement, process yield, morphology of microsphere, drug entrapment efficiency, mucoadhesion test, differential scanning calorimetry, powder X-ray diffraction, Fourier transforms infrared (FTIR) study and in-vitro drug release.Results: The OLE mucoadhesive microsphere having mean particle size ranged from 546.0 µm to 554.3 µm, and the entrapment efficiencies ranged from 73% to 96%. All the olanzapine (OLE) microsphere batches showed good in-vitro mucoadhesive property ranging from 75.89% to 96.47% and in the in-vitro wash off test ranging from 68.12% to 81.3%. FTIR studies indicated the no drug-polymer interactions in the ideal formulation F9. Therewere no compatibility issues, and the crystallinity of OLE was found to be reduced shoeing less intense peak in prepared mucoadhesive microspheres, which were confirmed by differential scanning calorimeter and X-ray diffraction studies. Among different formulations, the OLE microspheres of batch F9 had shown the optimum percent drug entrapment of microspheres. Release pattern of OLE from F9 microspheres batch followed Higuchi kinetic model. Stability studies were carried out for F9 formulation at 4°C/ambient, 25±2°C/60±5%, 40±2°C/75±5% relative humidity revealed that the drug entrapment, mucoadhesive behavior, and drug release were within permissible limits.Conclusion: The results obtained in this work demonstrate the use of carbopol and sodium alginate polymer for preparation of mucoadhesive microsphere.Keywords: Ionic gelation method, Gastroretentive delivery, Mucoadhesive microsphere, Carbopol.

Beta-Cyclodextrin and Maltodextrin Based Solid Dispersion of Meloxicam to Enhance the Solubility of Meloxicam; Formulation and In-vitro Evaluation

2019 ◽  
Vol 41 (1) ◽  
pp. 133-133
Author(s):  
Muhammad Zaman Muhammad Zaman ◽  
Muhammad Hanif Muhammad Hanif ◽  
Syed Saeed Ul Hassan Syed Saeed Ul Hassan ◽  
Javed Iqbal and Muhammad Ahmad Shehzad Javed Iqbal and Muhammad Ahmad Shehzad
Keyword(s):  
Solid Dispersion ◽  
X Ray Diffraction ◽  
Flow Properties ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
X Ray ◽  
Beta Cyclodextrin ◽  
Release Studies ◽  
Pure Drug

The purpose of the current study was to enhance the solubility of the meloxicam (MLX) by preparing complex with β-Cyclodextrin (CD) and maltodextrin (MD). Dextrins have the ability to capture the drug inside their cavities without forming any chemical bonding. Three (3) formulations, each of solid dispersion (SD) and physical mixture (PM) were prepared by using different drug to polymer ratios (1:4, 1:6 and 1:8) followed by evaluation for micromeritic properties, drug contents, and in vitro drug release studies, scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and x-ray diffraction (XRD) studies. Chemical compatibility of the ingredients was evaluated by using Fourier transform infrared spectroscopy (FTIR). Results of conducted studies exposed excellent flow properties of SDs as well as prepared PMs, with reasonable amount of loaded drug, i.e. andgt;90%. SEM showed a bit irregular surface while XRD suggested crystalline behavior of pure drug, which was masked after its conversion into SDs and PMs based on dextrins. Solubility of the MLX was increased significantly form its initial extent of solubility i.e. 12.5 and#181;g/ml in pure form to 786.72 and#181;g/ml in the form of SD (pandlt;0.05), advocating suitability of materials and methods for solubility enhancement of MLX.

scholarly journals IMPROVEMENT OF DISSOLUTION RATE OF VALSARTAN BY SOLID DISPERSION SYSTEM USING D(−) MANNITOL

2017 ◽  
Vol 10 (3) ◽  
pp. 288 ◽  
Author(s):  
Erizal Zaini ◽  
Salman Umar ◽  
Nurhidayah Nurhidayah
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
In Vitro Dissolution ◽  
Type I ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Dispersion System ◽  
Grinding Technique

ABSTRACTObjective: To improve dissolution rate of valsartan from solid dispersion system of valsartan and D(−) mannitol using co-grinding approach.Methods: Valsartan solid dispersion with different ratio of D(−) mannitol (1:1; 1:3 and 1: 5) were prepared by co-grinding method. Solid statecharacterization of the solid dispersion system was evaluated in term of crystallographic properties (powder X-ray diffraction), thermal behavior(differential scanning calorimetry [DSC]) and morphology (scanning electron microscope). The profile of dissolution rate was examined using USPdissolution apparatus type I at a temperature of 37±0.5°C.Results: Based on thermal analysis DSC and powder X-ray diffraction analysis, valsartan was transformed from semicrystalline phase to amorphousstate as indicated by the disappearance of its melting endothermic peaks and the characteristic diffraction peaks. The in vitro dissolution rate studyrevealed that all solid dispersion system showed significant increase in dissolution rate compared with the intact valsartan.Conclusion: Solid dispersion of valsartan with D(−) mannitol prepared by co-grinding technique has successfully improved the dissolution ratecompared with intact valsartan.Keywords: Valsartan, D(−) mannitol, Solid dispersion, Co-grinding, Dissolution rate.

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 Design and Evaluation of Voriconazole Loaded Solid Lipid Nanoparticles for Ophthalmic Application

2016 ◽  
Vol 2016 ◽  
pp. 1-11 ◽  
Author(s):  
Anubha Khare ◽  
Inderbir Singh ◽  
Pravin Pawar ◽  
Kanchan Grover
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Tween 80 ◽  
Lipid Nanoparticles ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Release Agent ◽  
X Ray ◽  
Corneal Hydration ◽  
Solid Lipid

Voriconazole is a second-generation antifungal agent with excellent broad spectrum of antifungal activity commercially available for oral and intravenous administration. Systemic administration of voriconazole is associated with side effects including visual and hepatic abnormalities. This study assessed the feasibility of using solid lipid nanoparticles for ocular delivery of voriconazole adopting stearic acid as lipidic material, tween 80 as a stabilizer, and Carbopol 934 as controlled release agent and for increasing the precorneal residence time in eye. The systems were prepared using two different methods, that is, ultrasonication method and microemulsion technique. The results indicated that the larger particle size of SLNs was found with microemulsion technique (308±3.52 nm to 343±3.51) compared to SLN prepared with ultrasonication method (234±3.52 nm to 288±4.58 nm). The polydispersity index values were less than 0.3 for all formulations and zeta potential of the prepared formulations by these two methods varied from −22.71±0.63 mV to −28.86±0.58 mV. Powder X-ray diffraction and differential scanning calorimetry indicated decrease in crystallinity of drug. The in vitro release study and the SLN formulations prepared with ultrasonication method demonstrated sustained release up to 12 hours. This study demonstrated that SLN prepared by ultrasonication method is more suitable than microemulsion technique without causing any significant effect on corneal hydration level.

scholarly journals Two Novel Palbociclib-Resorcinol and Palbociclib-Orcinol Cocrystals with Enhanced Solubility and Dissolution Rate

Pharmaceutics ◽  
2021 ◽  
Vol 14 (1) ◽  
pp. 23
Author(s):  
Chenxin Duan ◽  
Wenwen Liu ◽  
Yunwen Tao ◽  
Feifei Liang ◽  
Yanming Chen ◽  
...  
Keyword(s):  
Water Solubility ◽  
Cancer Drug ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Dissolution Rates ◽  
Intrinsic Dissolution ◽  
X Ray ◽  
Enhanced Solubility

Palbociclib (PAL) is an effective anti-breast cancer drug, but its use has been partly restricted due to poor bioavailability (resulting from extremely low water solubility) and serious adverse reactions. In this study, two cocrystals of PAL with resorcinol (RES) or orcinol (ORC) were prepared by evaporation crystallization to enhance their solubility. The cocrystals were characterized by single crystal X-ray diffraction, Hirshfeld surface analysis, powder X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, Fourier transform infrared and scanning electron microscopy. The intrinsic dissolution rates of the PAL cocrystals were determined in three different dissolution media (pH 1.0, pH 4.5 and pH 6.8), and both cocrystals showed improved dissolution rates at pH 1.0 and pH 6.8 in comparison to the parent drug. In addition, the cocrystals increased the solubility of PAL at pH 6.8 by 2–3 times and showed good stabilities in both the accelerated stability testing and stress testing. The PAL-RES cocrystal also exhibited an improved relative bioavailability (1.24 times) than PAL in vivo pharmacokinetics in rats. Moreover, the in vitro cytotoxicity assay of PAL-RES showed an increased IC50 value for normal cells, suggesting a better biosafety profile than PAL. Co-crystallization may represent a promising strategy for improving the physicochemical properties of PAL with better pharmacokinetics.

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