Modeling of Hansen's solubility parameters of aripiprazole, ziprasidone, and their impurities: A nonparametric comparison of models for prediction of drug absorption sites

2018 ◽  
Vol 32 (4) ◽  
pp. e2996 ◽  
Author(s):  
Darija Obradović ◽  
Filip Andrić ◽  
Mario Zlatović ◽  
Danica Agbaba
Author(s):  
Ю.И. Цой

Задача получения однородного состава ЛКМ сводится к правильному выбору пленкообразователей и соответствующих растворителей и, в случае необходимости, разбавителей и добавок. На основе положений теории растворимости была проведена оценка совместимости компонентов и стабильности таких систем. Критериями оценки были приняты параметры растворимости и термодинамического взаимодействия. Исследовали совместимость алкидных лаков с аминоформальдегидными смолами в бутаноле, и результаты этих исследований представлены в треугольной фазовой диаграмме. Для оценки совместимости смол по результатам расчета параметров термодинамического взаимодействия были построены спинодали для тройных систем. Как показывает анализ результатов проведенных исследований, даже при большой разности ?? = |?12 – ?13| = 0,2 наблюдается небольшая область несовместимости. С уменьшением разности ?? область несовместимости сужается. При ?23 > ?с область несовместимости расширяется как для ? = 0,2, так и для ?? = 0,1 и ?? = 0. Таким образом, для таких систем на совместимость компонентов, в первую очередь, влияет их взаимодействие между собой – чем оно больше, тем лучше они совместимы. Проведенные исследования показали, что парциальные параметры растворимости, учитывающие природу когезионных сил, более объективно характеризуют растворимость пленкообразующих смол в органических растворителях, чем их общий параметр растворимости. Растворимость пленкообразующих алкидных и этерифицированных аминоформальдегидных смол в органических растворителях обусловлена термодинамическим взаимодействием молекулярных сил различной природы. Стабильность смеси алкидной и этерифицированной аминоформальдегидной смолы в бутаноле обусловлена в большей степени термодинамическим взаимодействием молекулярных сил; при этом степень бутанолизации меламиноформальдегидной смолы оказывает наибольшее влияние на стабильность cистемы. Проведенные исследования по стабильности лакокрасочных смесей из различных пленкообразующих смол на основе рассмотренных критериев оценки могут быть использованы для совершенствования технологии защитно-декоративной отделки древесины. The problem of obtaining a homogeneous composition of the coatings is reduced to the proper selection of film-forming agents, and diluent and, if appropriate, diluents and additives. On the basis of the theory of solubility, we have carried out the assessment of the compatibility of the components and stability of such systems. The evaluation criteria were adopted the parameters of the solubility and thermodynamic interaction. Researched the compatibility with alkyd varnishes aminoformaldehyde resin in butanol, and the results of these studies are presented in the triangular phase diagram. To evaluate the compatibility of the resins according to the results of calculation of thermodynamic parameters of interaction were built spinodal for ternary systems. As the analysis of the results of the studies, even when the difference ??|?12 – ?13| = 0,2 there is a small area of incompatibility. With the decrease of the difference ? ? region incompatibility narrows. When ?23> ?с region incompatibility extends to ?? = 0,2, and for ?? = 0.1 and ?? = 0. Thus, for such systems, compatibility of components, primarily, affects their interaction with each other – the further away it is, the better they are compatible. Studies have shown that the partial solubility parameters, which take into account the nature of cohesive forces, more objectively characterize the solubility of film-forming resins in organic solvents than their total solubility parameter. The solubility and film-forming aminoformaldehyde esterified alkyd resins in organic solvents due to thermodynamic interaction of molecular forces of different nature. Тhe stability of the mixture and aminoformaldehyde esterified alkyd resin in butanol is generated largely by thermodynamic forces of molecular interaction; the degree of butanolate melamine-formaldehyde resin has the greatest effect on the stability of the system. Conducted research on the stability of the paint mixtures of various film-forming resins on the basis of the evaluation criteria can be used to improve the technology of protective and decorative wood finish.


2020 ◽  
Vol 15 ◽  
Author(s):  
Diksha Sharma ◽  
Deepak Sharma

Background: Gliclazide (GLZ) belongs to the second-generation of sulphonylureas, is a drug of choice for the management of type II DM. It belongs to BCS Class II. The major site of drug absorption for GLZ is the stomach; it displayed variation in the drug absorption rate and bioavailability due to the shorter gastric retention time. Floating mechanism performance gets affected when the gastric fluid level not sufficiently higher, which ultimately obstructs the floating behavior, which is the major limitation of reported formulations. This limitation can get over by folded the film into the capsule shell that dissolved in gastric fluid and film swell/expands to dimensions higher than pylorus sphincter (12mm), thus prevents its evacuation. Objective: To explore the floating mechanism in the designing of films along with a tendency to expand by swelling and unfolding by utilizing a mixture of hydrophilic and hydrophobic polymer to achieve the controlled drug delivery and prolonged gastric retention of drug. Methods: The gastroretentive floating films were formulated by the solvent casting technique using 32 full factorial design and subjected to in vitro evaluation parameters, drug-excipient compatibility, X-ray diffraction and accelerated stability study. Results: The pre-formulation study established the purity and identification of drug. FTIR study confirmed no drug excipient interaction. F3, F6, and F9 were optimized based on in vitro floating characteristics, swelling/expanding ability, and unfolding time study. All developed formulations were unfolded within 14-22 min after capsule disintegration. The F3 was selected as final formulation as its ability to control the release of drug for 24 hrs followed by Zero-order kinetics having super case 2 transport. XRD confirmed the amorphousness of drug within formulation. The stability study results revealed that formulation was quite stable at extreme storage condition. Conclusion: The developed novel formulation has a good potential for the effective management and treatment of Diabetes Mellitus.


1992 ◽  
Vol 62 (9) ◽  
pp. 535-546 ◽  
Author(s):  
Philip E. Slade ◽  
Debra N. Hild

The surface energies of spin finishes adsorbed onto synthetic fibers are a major factor in determining the processing capabilities of these fibers. They also play a key role in determining how wettable the fibers are by other materials that may be applied to yarn or fabrics in later stages of processing, such as dyes, sizes, or anti-soiling agents. We have applied several homologous series of nonionic surfactants, which can be used as spin finish emulsifiers, to nylon 66 fibers and determined the polar, dispersion, and total surface energies of these adsorbed materials. We also propose a relationship between the measured surface energies and the calculated Hansen fractional solubility parameters.


2006 ◽  
Vol 6 (9) ◽  
pp. 2959-2966 ◽  
Author(s):  
Na Zhang ◽  
Qineng Ping ◽  
Guihua Huang ◽  
Xiuzhen Han ◽  
Yanna Cheng ◽  
...  

Wheat germ agglutinin (WGA) modified liposomes and solid lipid nanoparticles (SLNs) were evaluated for improving intestinal absorption of insulin. In an in situ local intestinal perfusion experiment, formulations containing 100 IU/kg insulin were administered to the duodenum, jejunum, and ileum of fasted rats. As hypothesized, ileum was the best intestinal location for the absorption of insulin-containing liposomes. Serum insulin concentrations decreased for the various formulations in different absorption sites according to the following trends: Duodenum > ileum > jejunum for WGA-modified insulin-containing liposomes; duodenum > jejunum > ileum for WGA-modified insulin-containing SLNs; ileum > jejunum > duodenum for insulin-containing liposomes; ileum > duodenum > jejunum for insulin-containing SLNs; and duodenum ≥ ileum > jejunum for aqueous solution of insulin. These results imply that the nanoparticle type and delivery site were important factors with respect to increasing the bioavailability of insulin following oral administration. The proteolytic degradation as well as the epithelial permeability were primary determinants influcing insulin mucosal absorption.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 272
Author(s):  
Arik Dahan ◽  
Isabel González-Álvarez

The gastrointestinal tract (GIT) can be broadly divided into several regions: the stomach, the small intestine (which is subdivided to duodenum, jejunum, and ileum), and the colon. The conditions and environment in each of these segments, and even within the segment, are dependent on many factors, e.g., the surrounding pH, fluid composition, transporters expression, metabolic enzymes activity, tight junction resistance, different morphology along the GIT, variable intestinal mucosal cell differentiation, changes in drug concentration (in cases of carrier-mediated transport), thickness and types of mucus, and resident microflora. Each of these variables, alone or in combination with others, can fundamentally alter the solubility/dissolution, the intestinal permeability, and the overall absorption of various drugs. This is the underlying mechanistic basis of regional-dependent intestinal drug absorption, which has led to many attempts to deliver drugs to specific regions throughout the GIT, aiming to optimize drug absorption, bioavailability, pharmacokinetics, and/or pharmacodynamics. In this Editorial we provide an overview of the Special Issue "Regional Intestinal Drug Absorption: Biopharmaceutics and Drug Formulation". The objective of this Special Issue is to highlight the current progress and to provide an overview of the latest developments in the field of regional-dependent intestinal drug absorption and delivery, as well as pointing out the unmet needs of the field.


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