Superior Dissolution Behavior and Bioavailability of Pharmaceutical Cocrystals and Recent Regulatory Issues

(1) Background: Pharmaceutical cocrystals have attracted remarkable interest and have been successfully used to enhance the absorption of poorly water-soluble drugs. However, supersaturable cocrystals are sometimes thermodynamically unstable, and the solubility advantages present a risk of precipitation because of the solution-mediated phase transformation (SMPT). Additives such as surfactants and polymers could sustain the supersaturation state successfully, but the effect needs insightful understanding. The aim of the present study was to investigate the roles of surfactants and polymers in the dissolution-supersaturation-precipitation (DSP) behavior of cocrystals. (2) Methods: Five surfactants (SDS, Poloxamer 188, Poloxamer 407, Cremophor RH 40, polysorbate 80) and five polymers (PVP K30, PVPVA 64, HPC, HPMC E5, CMC-Na) were selected as additives. Tecovirimat-4-hydroxybenzoic (TEC-HBA) cocrystals were chosen as a model cocrystal. The TEC-HBA cocrystals were first designed and verified by PXRD, DSC, SEM, and FTIR. The effects of surfactants and polymers on the solubility and dissolution of TEC-HBA cocrystals under sink and nonsink conditions were then investigated. (3) Results: Both the surfactants and polymers showed significant dissolution enhancement effects, and most of the polymers were more effective than the surfactants, according to the longer Tmax and higher Cmax. These results demonstrate that the dissolution behavior of cocrystals might be achieved by the maintained supersaturation effect of the additives. Interestingly, we found a linear relationship between the solubility and Cmax of the dissolution curve for surfactants, while no similar phenomena were found in solutions with polymer. (4) Conclusions: The present study provides a basis for additive selection and a framework for understanding the behavior of supersaturable cocrystals in solution.

Download Full-text

283. Differences in Dissolution Behavior in a Phagolysosomal Simulant Fluid for Single-Component and Multicomponent Beryllium Materials Associated with Beryllium Sensitization and Chronic Beryllium Disease

10.3320/1.2758747 ◽

2005 ◽

Author(s):

A. Stefaniak ◽

G. Day ◽

M. Hoover ◽

P. Breysse ◽

R. Scripsick

Keyword(s):

Single Component ◽

Dissolution Behavior ◽

Chronic Beryllium Disease ◽

Beryllium Disease ◽

Beryllium Sensitization

Download Full-text

Dissolution Behavior of an Amorphous Solid Dispersion in Surfactant Containing Media

10.26226/morressier.57ea3d6ad462b8028d88e2d5 ◽

2016 ◽

Author(s):

Guangyu Ma

Keyword(s):

Solid Dispersion ◽

Amorphous Solid ◽

Amorphous Solid Dispersion ◽

Dissolution Behavior

Download Full-text

Regulatory Issues in Pakistan Telecommunication

The Pakistan Development Review ◽

10.30541/v37i4iipp.873-882 ◽

1998 ◽

Vol 37 (4II) ◽

pp. 873-882 ◽

Cited By ~ 1

Author(s):

Sarfaraz Khan Quershi

Keyword(s):

National Economy ◽

Cost Effective ◽

Market Forces ◽

Global Trends ◽

Regulatory Issues ◽

Competitive Price ◽

Modern Services ◽

A Company ◽

Telecom Infrastructure

Growth in telecom infrastructure and provision of modern telecom services to consumers at a cost based tariff helps growth of national economy. Modern telecoms serve as the engine of growth of national economy. Following the global trends of liberalisation and deregulation in telecoms monopolies which have thus far been providing inefficient communication at a greedily high tariffs are falling apart. Mergers in telecoms are not for increasing the size of the monopoly but to provide more efficient and cost effective services to the consumers. In Pakistan the erstwhile T&T department played a needful role at its time. Conversion of the department into a corporation and then into a company were steps necessary for following the global trends. Need now is to continue this trend further, eliminate the monopolistic approach by allowing more players in the field thus permitting the market forces to decide the provision of better quality of modern services at competitive price.

Download Full-text

Solving the Problem of Silicon Dioxide Melting Based on Deviation Model

Non-Metallic Material Science ◽

10.30564/omms.v2i1.1653 ◽

2020 ◽

Vol 2 (1) ◽

Author(s):

Yuhan Sun

Keyword(s):

Silicon Dioxide ◽

Blast Furnace Slag ◽

Melting Process ◽

Melting Rate ◽

Dissolution Behavior ◽

Characteristic Parameters ◽

Contour Feature ◽

Time Periods ◽

Main Component ◽

Furnace Slag

Abstract: In order to reveal the dissolution behavior of iron tailings in blast furnace slag, we studied the main component of silica in iron tailings. First, edge contour features need to be established to represent the melting process of silica. We choose shape, perimeter, area and generalized radius as objects. By independently analyzing the influence of these four indexes on the melting rate, the area and shape were selected as the characteristic parameters of the edge contour of the silica particles. Then, the actual melting rate of the silica is estimated by the edge contour feature index. Finally, we can calculate the melting rate of the first second of three time periods of 0.00010312mm3/s，0.0002399mm3/s，0.0000538mm3/s.

Download Full-text