scholarly journals Solid state characterization, solid dispersions, solubility enhancement, drug dissolution and drug release

2017 ◽  
Vol 22 (1) ◽  
pp. 1-1 ◽  
Author(s):  
Raid Alany
Keyword(s):  
Solid State ◽  
Drug Release ◽  
Solid Dispersions ◽  
Solubility Enhancement ◽  
Drug Dissolution ◽  
Solid State Characterization

scholarly journals Different BCS Class II Drug-Gelucire Solid Dispersions Prepared by Spray Congealing: Evaluation of Solid State Properties and In Vitro Performances

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 548 ◽  
Author(s):  
Serena Bertoni ◽  
Beatrice Albertini ◽  
Nadia Passerini
Keyword(s):  
Solid State ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Class Ii ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Crystalline Solid ◽  
Dissolution Behavior ◽  
Bcs Class Ii

Delivery of poorly water soluble active pharmaceutical ingredients (APIs) by semi-crystalline solid dispersions prepared by spray congealing in form of microparticles (MPs) is an emerging method to increase their oral bioavailability. In this study, solid dispersions based on hydrophilic Gelucires® (Gelucire® 50/13 and Gelucire® 48/16 in different ratio) of three BCS class II model compounds (carbamazepine, CBZ, tolbutamide, TBM, and cinnarizine, CIN) having different physicochemical properties (logP, pKa, Tm) were produced by spray congealing process. The obtained MPs were investigated in terms of morphology, particles size, drug content, solid state properties, drug-carrier interactions, solubility, and dissolution performances. The solid-state characterization showed that the properties of the incorporated drug had a profound influence on the structure of the obtained solid dispersion: CBZ recrystallized in a different polymorphic form, TBM crystallinity was significantly reduced as a result of specific interactions with the carrier, while smaller crystals were observed in case of CIN. The in vitro tests suggested that the drug solubility was mainly influenced by carrier composition, while the drug dissolution behavior was affected by the API solid state in the MPs after the spray congealing process. Among the tested APIs, TBM-Gelucire dispersions showed the highest enhancement in drug dissolution as a result of the reduced drug crystallinity.

scholarly journals Solid-state characterization of Felodipine–Soluplus amorphous solid dispersions

2015 ◽  
Vol 42 (3) ◽  
pp. 485-496 ◽  
Author(s):  
Jiannan Lu ◽  
Kristina Cuellar ◽  
Nathan I. Hammer ◽  
Seongbong Jo ◽  
Andreas Gryczke ◽  
...  
Keyword(s):  
Solid State ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Amorphous Solid Dispersions ◽  
Solid State Characterization

scholarly journals Cocrystallization of Etodolac: Prediction of Cocrystallization, Synthesis, Solid State Characterization And In Vitro Drug Release

2016 ◽  
Vol 21 (24530) ◽  
pp. 78-88 ◽  
Author(s):  
Dipak D Gadade ◽  
Sanjay S Pekamwar ◽  
Swaroop R Lahoti ◽  
Santosh D Patni ◽  
Mahesh C Sarode
Keyword(s):  
Solid State ◽  
Drug Release ◽  
In Vitro Drug Release ◽  
Solid State Characterization

scholarly journals Solid-State Characterization and Dissolution Properties of Meloxicam–Moringa Coagulant–PVP Ternary Solid Dispersions

2013 ◽  
Vol 14 (2) ◽  
pp. 569-577 ◽  
Author(s):  
Suhail B. Noolkar ◽  
Namdeo R. Jadhav ◽  
Santosh A. Bhende ◽  
Suresh G. Killedar
Keyword(s):  
Solid State ◽  
Solid Dispersions ◽  
Dissolution Properties ◽  
Ternary Solid Dispersions ◽  
Solid State Characterization

scholarly journals Comparison of Different Solubility Enhancement Techniques for Clopidogrel

2021 ◽  
Vol 69 (1) ◽  
Author(s):  
Degala. Vishwanayani ◽  
Dr. P.Tripura Sundari
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solubility Enhancement ◽  
Solvent Evaporation ◽  
Cyclodextrin Complexes ◽  
Drug Content ◽  
Beta Cyclodextrin ◽  
Peg 4000 ◽  
Release Studies

The present study is aimed to formulate and evaluate various formulations to enhance the solubility of poorly aqueous soluble drug Clopidogrel. For this we have selected different techniques like solid dispersion, Nanosuspension and cyclodextrin complexes. As a part of it we prepared solid dispersions of drug employing PVPk30 and PEG 4000. Beta cyclodextrin complexes are prepared by kneading and solvent evaporation methods. Whereas nanosuspension are prepared by employing polaxomer as polymer. The prepared formulations were evaluated for drug Content and drug release studies.

It is Possible to Achieve Tablets with Good Tabletability from Solid Dispersions – the Case of the High Dose Drug Gemfibrozil

2020 ◽  
Vol 17 ◽  
Author(s):  
Eduarda Rocha Bigogno ◽  
Luciano Soares ◽  
Matheus Henrique Ruela Mews ◽  
Melissa Zétola ◽  
Giovana Carolina Bazzo ◽  
...  
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Croscarmellose Sodium ◽  
Poorly Water Soluble

Background: Solid dispersions (SDs) have been extensively used to increase dissolution of poorly water-soluble drugs. However, there are few studies exploring SDs properties that must be considered during tablet development, like tabletability. Poorly water-soluble drugs with poor compression properties and high therapeutic doses, like gemfibrozil, are an additional challenge in the production of SDs-based tablets. Objective: This study evaluates the applicability of SDs to improve both tabletability and dissolution rate of gemfibrozil. A SD-based tablet formulation was also proposed. Method: SDs were prepared by ball milling, using hydroxypropyl methylcellulose (HPMC) as carrier, according to a 23 factorial design. The formulation variables were: gemfibrozil:HPMC ratio, milling speed, and milling time. The response in the factorial analysis was the tensile strength of the compacted SDs. Dissolution rate and solid-state characterization of SDs were also performed. Results: SDs showed simultaneous drug dissolution enhancement and improved tabletability when compared to corresponding physical mixtures and gemfibrozil. The main variable influencing drug dissolution and tabletability was the gemfibrozil:HPMC ratio. Tablets containing gemfibrozil-HPMC-SD (1:0.250 w/w) and croscarmellose sodium showed fast and complete drug release while those containing the same SD and sodium starch glycolate exhibited poor drug release due to their prolonged disintegration time. Conclusion: SDs proved to be effective for simultaneously improving tabletability and dissolution profile of gemfibrozil. Tablets containing gemfibrozil-HPMC-SD and croscarmellose sodium as disintegrating agent showed improved drug release and good mechanical strength, demonstrating the potential of HPMC-based SDs to simultaneously overcome the poor dissolution and tabletability properties of this drug.

scholarly journals Physicochemical characterization and in vitro dissolution behavior of olanzapine-mannitol solid dispersions

2012 ◽  
Vol 48 (2) ◽  
pp. 243-255 ◽  
Author(s):  
Venkateskumar Krishnamoorthy ◽  
Suchandrasen ◽  
Verma Priya Ranjan Prasad
Keyword(s):  
Solid State ◽  
Solid Dispersions ◽  
In Vitro Dissolution ◽  
Dissolution Behavior ◽  
Phase Solubility ◽  
Permeation Studies ◽  
Ft Ir ◽  
Solubility Studies ◽  
Solid State Characterization

The objective of the present work is to study the dissolution behavior of olanzapine from its solid dispersions with mannitol. Solid dispersions were prepared by melt dispersion method and characterized by phase solubility studies, drug content and in vitro dissolution studies. The best releasing dispersions were selected from release data, dissolution parameters and their release profiles. Solid state characterization techniques like Fourier transform infrared (FT-IR) spectroscopy, X-ray diffractometry, differential scanning calorimetry, near-infrared and Raman spectroscopy were used to characterize the drug in selected dispersions. The dispersions were also evaluated by wettability studies and permeation studies. The results of phase solubility studies and the thermodynamic parameters indicated the spontaneity and solubilization effect of the carrier. The release study results showed greater improvement of drug release from solid dispersions compared to pure drug, and the release was found to increase with an increase in carrier content. The possible mechanism for increased release rate from dispersions may be attributed to solubilization effect of the carrier, change in crystal quality, phase transition from crystalline to amorphous state, prevention of agglomeration or aggregation of drug particles, change in surface hydrophobicity of the drug, and increased wettability and dispersability of the drug in dissolution medium. The suggested reasons for increased release rate from dispersions were found to be well supported by results of solid state characterization, wettability and permeation studies. The absence of any interaction between the drug and the carrier was also proved by FT-IR analysis.

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