Cocrystals of Propylthiouracil and Nutraceuticals toward Sustained-Release: Design, Structure Analysis, and Solid-State Characterization

2021 ◽  
Vol 21 (2) ◽  
pp. 1202-1217
Author(s):  
Yuntian Xiao ◽  
Ling Zhou ◽  
Hongxun Hao ◽  
Ying Bao ◽  
Qiuxiang Yin ◽  
...  
Keyword(s):  
Solid State ◽  
Sustained Release ◽  
Structure Analysis ◽  
Design Structure ◽  
Solid State Characterization

Development of Sustained Release Oseltamivir Phosphate Dry Powder Inhaler: In-Vitro Characterization and In-Vivo Toxicological Studies

2020 ◽  
Vol 17 (8) ◽  
pp. 703-710 ◽  
Author(s):  
Harshal Sahastrabudhe ◽  
Prathmesh Kenjale ◽  
Varsha Pokharkar
Keyword(s):  
Solid State ◽  
Sustained Release ◽  
Spray Drying ◽  
Burst Release ◽  
Upper Respiratory Tract ◽  
Dry Powder ◽  
Oseltamivir Phosphate ◽  
Solid State Characterization

Background: Oseltamivir Phosphate (OP) is an ethyl ester prodrug prescribed for the treatment of influenza virus infection. Current marketed formulations of OP have been observed to be supplemented with an adverse effect during post-marketing surveillance. These prerequisites are sufficed by developing a sustained release Dry Powder for Inhalation (DPI). Objectives: The objective of the present study was to develop OP-DPI by an innovative formulation approach comprising of Immediate (IR) and Sustained (SR) Release portions. Methods: DPI formulation comprising IR and SR portions were prepared by spray drying technique using Hydroxy Propyl Methyl Cellulose (HPMC) as the rate-controlling polymer for SR portion. The spray-dried product was further characterized for various pharmaco-technical, in-vitro and in-vivo parameters. Results: OP-DPI showed a burst release of 49% within 15 min further sustaining the drug release up to 9 hrs. The in-vitro aerodynamic performance of OP-DPI showed maximum deposition at stage 3 and Fine Particle Dose (FPD) of 1.08 mg indicating deposition in the upper respiratory tract. Solid-state characterization by DSC and XRD indicated the partial amorphization of OP due to spray drying. In-vivo toxicological examination revealed no sign of inflammation, indicating the safety of the developed formulation. Accelerated stability study as per ICH guidelines displayed no significant change in the solid-state characterization and drug-related performance of OP-DPI. Conclusion: Prepared novel and scalable OP-DPI may have the potential to overcome the problems associated with existing marketed dosage forms of OP. Further, localized drug delivery of the antiviral drug through the pulmonary route might be clinically beneficial in controlling the viral proliferation.

Intermolecular Interactions and Solubility Behavior of Multicomponent Crystal Forms of 2,4-dichlorophenoxyacetic acid: Design, Structure Analysis, and Solid-State Characterization

CrystEngComm ◽  
2021 ◽  
Author(s):  
Lan Fang ◽  
Yun tian Xiao ◽  
Chengtian Zhang ◽  
Zhenguo Gao ◽  
Songgu Wu ◽  
...  
Keyword(s):  
Solid State ◽  
Plant Growth ◽  
Growth Regulator ◽  
Plant Growth Regulator ◽  
Dichlorophenoxyacetic Acid ◽  
Crystal Forms ◽  
Solubility Behavior ◽  
Design Structure ◽  
2,4 Dichlorophenoxyacetic Acid ◽  
Solid State Characterization

2,4-dichlorophenoxyacetic acid (2,4-D) is a kind of plant growth regulator which exhibits hormesis effects at low dosages, while high dosages adversely affect the exposed organisms and act as herbicide. The...

Development and Characterization of LBG-PVA Interpenetrating Networks Incorporating Gliclazide for Sustained Release

2020 ◽  
Vol 15 ◽  
Author(s):  
Ashish Katoch ◽  
Manju Nagpal ◽  
Malkiet Kaur ◽  
Manjinder Singh ◽  
Geeta Aggarwal ◽  
...  
Keyword(s):  
Solid State ◽  
Sustained Release ◽  
Half Life ◽  
Solid State Nmr ◽  
Oral Dosage ◽  
Cross Linking ◽  
Interpenetrating Networks ◽  
Dsc Studies ◽  
Biological Half Life ◽  
Percentage Yield

Background: Controlled oral dosage forms have always been preferred for drugs with variable absorption, and short biological half life and frequent dosing. The prime goal with sustained release systems is to maintain uniform therapeutic blood levels for longer periods of time. Interpenetrating networks (IPNs) have been evidenced as uniform sustained release systems. In current study, polyvinyl alcohol (PVA) and locust bean gum (LBG) based IPNs were developed for the oral sustained release drug delivery of gliclazide (shows variable absorption). Method: The IPNs were synthesized by emulsion cross-linking method using glutaraldehyde (GA) as a cross linking agent. Gliclazide is a potential second generation, short-acting sulfonylurea oral hypoglycemic agent is having a short biological half-life (2-4 h), variable absorption and poor oral bioavailability. Various batches of IPNs were formulated by varying LBG: PVA ratio and evaluated for percentage yield, drug entrapment efficiency (DEE), swelling properties and in vitro drug release studies. Further characterizations were done by Fourier Transform Infrared Spectroscopy (FTIR), C13 Solid state NMR, X-Ray diffraction study (XRD), Scanning electron microscopy (SEM), and Differential scanning microscopy (DSC) studies. Results: The percentage yield, drug entrapment and equilibrium swelling was observed to be dependent on PVA-LBG ratio and GA amount. Sustained release of drug was observed in all IPN formulations (approx 59 - 86% in 8 h in various batches) with variable release kinetics. SEM studies revealed the regular structures of IPNs. FTIR, XRD, C13 Solid state NMR and DSC studies proposed that drug was successfully incorporated into the formed IPNs. Conclusion: IPNs of LBG and PVA can be used as a promising carrier with uniform sustained release characteristics.

Triazole-tethered ferrocene-quinoline conjugates: solid-state structure analysis, electrochemistry and theoretical calculations

2021 ◽  
Author(s):  
Senka Djaković ◽  
Silvija Maračić ◽  
Jasmina Lapić ◽  
Eduard Kovalski ◽  
Alexander Hildebrandt ◽  
...  
Keyword(s):  
Solid State ◽  
Structure Analysis ◽  
Theoretical Calculations ◽  
State Structure ◽  
Solid State Structure

Solid-State Characterization of Amorphous and Mesomorphous Calcium Ketoprofen

2010 ◽  
Vol 99 (9) ◽  
pp. 3684-3697 ◽  
Author(s):  
Faraj Atassi ◽  
Chen Mao ◽  
Ahmad S. Masadeh ◽  
Stephen R. Byrn
Keyword(s):  
Solid State ◽  
Solid State Characterization

Microwave assisted synthesis and solid-state characterization of lithocholyl amides of isomeric aminopyridines

Steroids ◽  
2011 ◽  
Vol 76 (3) ◽  
pp. 261-268 ◽  
Author(s):  
Kari V. Ahonen ◽  
Manu K. Lahtinen ◽  
Arto M. Valkonen ◽  
Martin Dračínský ◽  
Erkki T. Kolehmainen
Keyword(s):  
Solid State ◽  
Microwave Assisted Synthesis ◽  
Microwave Assisted ◽  
Solid State Characterization

A silver complex with ibuprofen: Synthesis, solid state characterization, DFT calculations and antibacterial assays

2013 ◽  
Vol 1049 ◽  
pp. 1-6 ◽  
Author(s):  
Irlene Maria Pereira e Silva ◽  
Daniel de Moraes Profirio ◽  
Raphael Enoque Ferraz de Paiva ◽  
Marcelo Lancellotti ◽  
André Luiz Barboza Formiga ◽  
...  
Keyword(s):  
Solid State ◽  
Dft Calculations ◽  
Silver Complex ◽  
Solid State Characterization
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