scholarly journals Basic studies on preparations and drug release properties of w/o/w type multiple emulsions as carriers of water-soluble drugs. The use of lipiodol-soybean oil mixture for oily phase.

1994 ◽  
Vol 9 (1) ◽  
pp. 31-36 ◽  
Author(s):  
Hideaki Ohkouchi ◽  
Masahiro Nakano
Keyword(s):  
Drug Release ◽  
Soybean Oil ◽  
Water Soluble ◽  
Multiple Emulsions ◽  
Water Soluble Drugs ◽  
Basic Studies

Improved Dissolution Properties of Ketoconazole through Application of Liquisolid Techniques

2015 ◽  
Vol 8 (4) ◽  
pp. 3053-3059
Author(s):  
Sudarshan Singh ◽  
S S Shyale ◽  
H G Sandip
Keyword(s):  
Drug Release ◽  
Immediate Release ◽  
Water Soluble ◽  
Wet Granulation ◽  
Wetting Properties ◽  
Enhanced Dissolution ◽  
Water Soluble Drug ◽  
Drug Concentrations ◽  
Water Soluble Drugs ◽  
Liquisolid Compacts

In present investigation liquisolid compact technique is investigated as a tool for enhanced dissolution of poorly water-soluble drug Ketoconazole. The liquisolid tablets were formulated with liquid medications, namely Propylene Glycol (PG) drug concentrations, 60% w/w, 70% w/w and 80% w/w. Avicel pH102 was used as a carrier material, Aerosil 200 as a coating material and Sodium starch glycollate as a super-disintegrant. Quality control tests, such as uniformity of tablet weight, uniformity of drug content, tablet hardness, friability test, disintegration and dissolution tests were performed to evaluate prepared tablets. For further confirmation of results the liquisolid compacts were evaluated by XRD and FTIR studies to prove that, solubility of Ketoconazole has been increased by liquisolid compact technique. From the results obtained, it was be speculated that such systems exhibit enhanced drug release profiles due to increased wetting properties and surface of drug available for dissolution. As liquisolid compacts demonstrated significantly higher drug release rates, in PG as compared to directly compressible tablets and conventional wet granulation, we lead to conclusion that it could be a promising strategy in improving the dissolution of poor water soluble drugs and formulating immediate release solid dosage forms.  

Mesoporous Silica Molecular Sieve based Nanocarriers: Transpiring Drug Dissolution Research

2017 ◽  
Vol 23 (3) ◽  
pp. 467-480 ◽  
Author(s):  
Satyanarayan Pattnaik ◽  
Kamla Pathak
Keyword(s):  
Drug Release ◽  
Mesoporous Silica ◽  
Molecular Sieves ◽  
Release Kinetics ◽  
Drug Loading ◽  
Scale Up ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Water Soluble Drugs ◽  
Loading Methods

Background: Improvement of oral bioavailability through enhancement of dissolution for poorly soluble drugs has been a very promising approach. Recently, mesoporous silica based molecular sieves have demonstrated excellent properties to enhance the dissolution velocity of poorly water-soluble drugs. Description: Current research in this area is focused on investigating the factors influencing the drug release from these carriers, the kinetics of drug release and manufacturing approaches to scale-up production for commercial manufacture. Conclusion: This comprehensive review provides an overview of different methods adopted for synthesis of mesoporous materials, influence of processing factors on properties of these materials and drug loading methods. The drug release kinetics from mesoporous silica systems, the manufacturability and stability of these formulations are reviewed. Finally, the safety and biocompatibility issues related to these silica based materials are discussed.

scholarly journals Cyclodextrin Complex Formation with Water-Soluble Drugs: Conclusions from Isothermal Titration Calorimetry and Molecular Modeling

2021 ◽  
Vol 22 (7) ◽  
Author(s):  
Karim S. Shalaby ◽  
Muhammad I. Ismail ◽  
Alf Lamprecht
Keyword(s):  
Molecular Modeling ◽  
Complex Formation ◽  
Drug Release ◽  
Binding Affinity ◽  
Isothermal Titration Calorimetry ◽  
Water Soluble ◽  
Titration Calorimetry ◽  
Cyclodextrin Complex ◽  
Water Soluble Drugs

AbstractCyclodextrin (CD) complexes are frequently used for enhancing the solubility or absorption of poorly water-soluble drugs. On the contrary, little is known about their complex formation with water-soluble drugs. Here, we have studied the interaction between 2-hydroxypropyl β-CD (HPβCD) and three water-soluble drugs, namely naloxone (NX), oxycodone (OC), and tramadol (TR), by isothermal titration calorimetry (ITC) combined with molecular modeling in view of the potential impact on drug release. The results showed that the complex formation of HPβCD with all three drugs occurs spontaneously. The complexes formed with NX and OC were found to be 2NX:1HPβCD and 3OC:2HPβCD, respectively. TR was found to form 2 complexes with HPβCD; of 1:2 and 1:1 complexation ratios. The binding of HPβCD to NX was greater than to OC due to the higher hydrophobicity of the structure of the former. Moreover, the binding affinity of HPβCD to TR was higher than to OC, which indicated the effect of the higher flexibility of the guest in increasing the binding affinity. In vitro drug release experiments from the various complexes revealed a significant impact of the stoichiometry of the complex on the release profiles. Accordingly, the co-administration of cyclodextrins with water-soluble drugs should be closely monitored, as it may result in unintentional complex formation that can potentially impact the drugs’ gastrointestinal absorption.

Effects of Mucoadhesive Polymers on Released Particles and Drug Release in Solid Lipid Particle-Based Buccal Tablets

2020 ◽  
Vol 21 ◽  
Author(s):  
Thuy T.H. Phan ◽  
Phuong H.L. Tran ◽  
Thao T.D. Tran
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Critical Role ◽  
Water Soluble ◽  
Buccal Delivery ◽  
Solid Lipid ◽  
Mucoadhesive Polymers ◽  
Buccal Drug Delivery ◽  
Lipid Particle ◽  
Water Soluble Drugs

Background: Mucoadhesive polymers play a critical role in controlled release tablets for buccal drug delivery. Objective: This research aimed to investigate the characterization and mechanisms of solid lipid particle-based tablets with different mucoadhesive polymers for buccal delivery. Methods: Prednisolone (PSL)-loaded solid lipid particles (SLPs) were conventionally prepared by ultrasonication. The freeze-drying method was used to convert the SLP suspension into a solid dosage form for buccal delivery by using mucoadhesive polymers. Results: All formulations showed over 80% drug release after 6 h, which followed immediate and sustained release patterns depending on the SLP type. However, the different polymers in the formulations resulted in different mucoadhesion times and drug release and drug permeability profiles. HPMC 4000 showed higher drug permeation (3327 μg vs. 2589 μg after 6 h) but a shorter mucoadhesion time than Carbopol (197 min vs. 361 min). In addition, surface morphology, swelling and erosion, particle size and zeta potential were also noted for the different mechanisms for buccal tablet design with different controlled release profiles. Conclusion: The results of this work indicate a good strategy for the selection of mucoadhesive polymers for SLP-based tablets in improving the bioavailability of poorly water-soluble drugs.

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 Osmotic drug delivery system of valsartan

2019 ◽  
Vol 1 (2) ◽  
pp. 43-52
Author(s):  
Syed mujtaba pasha ◽  
Syed abid ali ◽  
Omair sohail ahmed ◽  
Omer wasiq ◽  
Mohammed mukaram ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Release Rate ◽  
Water Soluble ◽  
Hydrophilic Polymers ◽  
The Core ◽  
Drug Molecules ◽  
Water Soluble Drug ◽  
Water Soluble Drugs ◽  
Amitriptyline Hydrochloride

The objective of this study is to design and evaluate a new EOP called swellable elementary osmotic pump (SEOP) of the freely water soluble drug, amitriptyline hydrochloride (1 g /mL) by adding water swellable polymers in the core. The hydrophilic polymers included in the core retard the highly water soluble drug by producing hydrogel within the core, which may restrict and delay the solvent contact with drug molecules and may increase the diffusional length of the solvent to achieve a constant release rate. Thus, this technology can be exploited to achieve constant drug release at predetermined rate especially for highly water soluble drugs.

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