scholarly journals Dissolution Media for In Vitro Testing of Water-Insoluble Drugs: Effect of Surfactant Purity and Electrolyte on In Vitro Dissolution of Carbamazepine in Aqueous Solutions of Sodium Lauryl Sulfate

1997 ◽  
Vol 86 (3) ◽  
pp. 384-388 ◽  
Author(s):  
John R. Crison ◽  
Norman D. Weiner ◽  
Gordon L. Amidon
Author(s):  
KOMESMUNEEBORIRAK PHOJANA ◽  
WERAWATGANONE PORNPEN ◽  
MUANGSIRI WALAISIRI

Objective: At present, the nail preparation to cure onychomycosis, caused by non-dermatophyte molds, is not commercially available in Thailand. The physical and chemical stability of amphotericin B (AmB) extemporaneous preparations in the presence of 30% dimethyl sulfoxide (DMSO) and their in vitro nail permeation was evaluated. Methods: AmB extemporaneous preparations in the presence of 30% DMSO were prepared from a commercial sterile injection product, and cream or hydrophilic ointment. Physical stability was tested at 30°C for 2 months, or using 6 heating-cooling cycles. The chemical stability and in vitro nail permeation of AmB content were analyzed using high-performance liquid chromatography (HPLC). In vitro nail permeation was performed by applying 3.5 mg/mm2 of the tested formulation on nail clippings for 5 consecutive days. Results: The AmB cream and ointment extemporaneous preparations containing 30% DMSO, a permeation enhancer, were homogeneous and pale yellow to yellow cream or ointment. The AmB ointment was stable for up to 60 days. The ointment preparation allows in vitro penetration through nails up to 14.17 μg/cm2. The ointment preparation allows significantly better penetration through than the cream preparation due to the presence of DMSO, sodium lauryl sulfate (SLS), and water in the ointment preparation. Conclusion: The AmB extemporaneous ointment was successfully compounded from a commercial sterile injection product with a beyond-use date of 60 days. The ointment preparation is currently under further investigation for in vivo efficacy.


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


2014 ◽  
Vol 48 (5) ◽  
pp. 343-345 ◽  
Author(s):  
D. A. Shutov ◽  
E. O. Ol’khova ◽  
A. N. Kostyleva ◽  
E. S. Bobkova

2010 ◽  
Vol 2010 ◽  
pp. 1-7 ◽  
Author(s):  
M. A. Abdl-Rahman ◽  
F. A. R. Sawiress ◽  
A. M. Abd El-Aty

The aim of the current study was to evaluate the effect of sodium lauryl sulfate-fumaric acid coupled addition onin vitromethangenesis and rumen fermentation. Evaluation was carried out usingin vitrogas production technique. Ruminal contents were collected from five steers immediately after slaughtering and used for preparation of inoculums of mixed rumen microorganisms. Rumen fluid was then mixed with the basal diet of steers and used to generate four treatments, negative control (no additives), sodium lauryl sulfate (SLS) treated, fumaric acid treated, and SLS-fumaric acid coupled addition treated. The results revealed that, relative to control, efficiency in reduction of methanogenesis was as follows: coupled addition > SLS-addition > fumaric acid addition. Both SLS-addition and SLS-fumaric acid coupled addition demonstrated a decremental effect on ammonia nitrogen (–), total short chain volatile fatty acids (SCVFAs) concentrations and the amount of substrate degraded, and an increment effect on microbial mass and microbial yield (). Nevertheless, fumaric acid did not alter any of the previously mentioned parameters but induced a decremental effect on –. Furthermore, both fumaric acid and SLS-fumaric acid coupled addition increased propionate at the expense of acetate and butyrate, while, defaunation increased acetate at the expense of propionate and butyrate. The pH value was decreased by all treatments relative to control, while, cellulase activity did not differ by different treatments. The current study can be promising strategies for suppressing ruminal methane emissions and improving ruminants feed efficiency.


2017 ◽  
Vol 532 (1) ◽  
pp. 519-527 ◽  
Author(s):  
Mareike Probst ◽  
Martin Schmidt ◽  
Katharina Tietz ◽  
Sandra Klein ◽  
Werner Weitschies ◽  
...  

Molecules ◽  
2018 ◽  
Vol 23 (7) ◽  
pp. 1716 ◽  
Author(s):  
Francesca Sansone ◽  
Tiziana Esposito ◽  
Maria Lauro ◽  
Patrizia Picerno ◽  
Teresa Mencherini ◽  
...  

Many natural compounds having antioxidant and anti-inflammatory activity are a potential target for new therapies against chronic inflammatory syndromes. The oral administration of functional herbal supplements may become a prevention strategy or therapy adjuvant for susceptible patients. A case study is our milk thistle (Silybum marianum) extract rich in silymarin complex. A water-soluble microencapsulated powder system was developed by a spray drying technique to improve the poor silymarin bioactivity after oral administration. Sodium carboxymethylcellulose (NaCMC) was employed as coating/swelling polymer matrix and sodium lauryl sulfate (SLS) as the surfactant (1:1:0.05 w/w/w). A H2O/EtOH/acetone (50/15/35 v/v/v) solvent system was used as liquid feed. The microsystems were capable of improving the in vitro dissolution and permeation rates, suggesting an enhancement of bioactivity after oral administration. The microsystems protect the antioxidant activity of silymarin after harsh storage conditions period and do not affect the anti-inflammatory properties of the raw extract (efficient already at lower concentrations of 0.312 mg/mL) to reduce dendritic cells (DCs) inflammatory cytokine secretion after lipopolysaccharide administration. This approach allows managing particle size, surface properties and release of bioactive agents improving the bioactivity of a herbal supplement and is also possibly applicable to many other similar natural products.


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