Water-Insoluble Drugs and Their Pharmacokinetic Behaviors

Author(s):  
Honghui Zhou
Keyword(s):  
Author(s):  
J M Shah ◽  
N.H Shah ◽  
Hadiya P D

Pharmaceutical technology has developed various newer modes of novel drug delivery aspects. Modifications in the previously existing drug delivery methods have led to various newly innovated technologies serving as a safe and effective means of improvement over the existing ones. Novasome technology is one of the new innovations of liposomes which have solved many of the problems related to liposomal drug delivery system. It offers a seven bilayer membrane which has the ability to incorporate both water soluble and insoluble drugs. It has an excellent entrapment efficiency which provides better medication. Formulation of novasomes is achieved in a high shear device. Due to its numerous advantages, novasomes have been used extensively in various fields like cosmetics, chemical, personal care, foods, pharmaceuticals and agrochemicals.


2003 ◽  
Vol 51 (1) ◽  
pp. 15-19 ◽  
Author(s):  
Masako Kajihara ◽  
Toshihiko Sugie ◽  
Hiroo Maeda ◽  
Akihiko Sano ◽  
Keiji Fujioka ◽  
...  

2021 ◽  
Vol 28 ◽  
Author(s):  
Bei He ◽  
Xinxin Liu ◽  
Shi Qi ◽  
Run Zheng ◽  
Minmin Chang ◽  
...  

Background: Cellulose, huge reserves of natural polymers, have been widely applied in pharmaceutical and biomedicine fields due to its good biocompatibility, biodegradability, non-toxicity and excellent mechanical properties. At present, water-resistant metal-based and petroleum-based materials applied in medical field exists obvious problems of poor biocompatibility and high cost. Therefore, water-resistant cellulose-based materials with good biocompatibility and low price will become an attractive alternative. This review aims to summarize the preparation of water-resistant cellulose-based materials and their potential application in pharmaceutical and biomedical in recent years. Methods: Common hydrophobic treatments of cellulose fibers or paper were overviewed. The preparation, properties and applications of water-resistant cellulose-based materials in the pharmaceutical and biomedical fields were summarized. Results: Common hydrophobic treatments of cellulose fibers or paper were divided into chemical modification (graft polymerization, crosslinking, solution casting or dip-coating), physico-chemical surface modifications (plasma treatments, surface patterning, electrostatic spraying and electrowetting) and physical processing (electrostatic spinning, SAS process and 3D EHD printing). These hydrophobically processed cellulose fibers or paper could be prepared into various water-resistant cellulose-based materials and applied in pharmaceutical excipients, drug-loaded amphiphilic micelles, drug-loaded composite fibers, hydrophobic biocomposite film/coatings and paper-based detectors. They presented excellent water resistance and biocompatibility, low cytotoxicity and high drug loading ability, and stable drug release rate, etc., which could be used for water-insoluble drugs carriers, wound dressings, and medical testing equipment. Conclusion: Currently, water-resistant cellulose-based materials were mainly applied in water-insoluble drugs delivery carriers, wound dressing and medical diagnosis and presented great application prospects. However, the contradiction between hydrophobicity and mechanical properties of these reported water-resistant cellulose-based materials limited their wider application in biomedicine such as tissue engineering. In the future, attention will be focused on the higher hydrophobicity of water-resistant cellulose-based materials with excellent mechanical properties. In addition, clinical medical research of water-resistant cellulose-based materials should be strengthened.


1970 ◽  
Vol 6 (1) ◽  
pp. 25-36 ◽  
Author(s):  
RP Patel ◽  
MM Patel

Several attempts have been made to improve the solubility of water insoluble drugs. Over the years, inclusion complexation of drugs with ?-cyclodextrin has emerged as a viable attempt to improve the dissolution of water insoluble drugs. The aim of the present work was to improve the dissolution rate of lovastatin, a water insoluble drug, by inclusion complexation with ?-cyclodextrin. The stoichiometric ratio determined by phase solubility analysis for inclusion complexation of lovastatin with ?-cyclodextrin was 1:1. The solubility of lovastatin increased with increasing amount of ?-cyclodextrin in water. Gibbs free energy (?Gtr°) values were all negative, indicating the spontaneous nature of lovastatin solubilization. Complexes of lovastatin were prepared with ?-cyclodextrin by various methods such as kneading, coevaporation and physical mixing. The complexes were characterized by Fourier-transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), and X-ray diffraction (XRD) patterns. These studies indicated the inclusion of lovastatin in the cavity of ?-cyclodextrin. The complexation resulted in a marked improvement in the solubility of lovastatin. The complex prepared by kneading method showed fastest and highest in vitro dissolution rate compared to the tablets of pure of lovastatin. Physical mixture of ?-cyclodextrin/lovastatin also showed significant improvement in the dissolution rate compared to pure lovastatin. Mean dissolution time (MDT) of lovastatin decreased significantly after preparation of complexes and physical mixture of lovastatin with ?-cyclodextrin. Similarity factor (f2) indicated significant difference between the release profiles of lovastatin from complexes and from pure lovastatin. Key words: Lovastatin, ?-cyclodextrin, inclusion complexation, in vitro dissolution studies. Dhaka Univ. J. Pharm. Sci. 6(1): 25-36, 2007 (June) The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website


Author(s):  
Sanjay Jain ◽  
R. K. Maheshwari ◽  
R. K. Nema ◽  
Indrajeet Singhvi

Objective: Commonly used organic solvents for spectrophotometric analysis of water insoluble drugs are methanol, ethanol, chloroform, benzene, toluene etc. The main drawbacks of organic solvents include high cost, toxicity, and pollution. Organic solvents have numerous adverse effects caused by single exposure like dermatitis, headache, drowsiness, nausea, eye irritation and long term exposure causes serious effects such as neurological disorder, chronic renal failure, and liver damage. They should be replaced by other ecofriendly alternative sources.Methods: The present study is an attempt to show that solid can also be used to act as solvent precluding the use of organic solvents. A simple, safe and sensitive method of spectrophotometric determination of diazepam obeyed beers law in the concentration range of 5-25 mcg/ml at 306 nm.Results: The results of analyses have been validated statistically for Linearity, accuracy, precision, LOD and LOQ. The results of validation parameters also indicated that proposed method was found to be accurate, precise, reproducible, sensitive, and suitable for routine quality control analysis for estimation of diazepam in bulk drug and solid dosage formulation.Conclusion: A rapid, simple, and non toxic UV spectrophotometric method has been developed for the determination and quantification of diazepam. The present method also validated as per ICH guidelines for linearity, precision, accuracy.


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