Studies of Carbomer Gels Using Rotational Viscometry and Spin Probes

Lyapunov, A. N.; Bezuglaya, Elena; Lyapunov, Nikolay; Kirilyuk, Igor A.

doi:10.1007/s11094-015-1344-3

Cited by 11 publications

(10 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…4. The next step in the substantiation of the choice of API delivery system was research to study the viscoelastic characteristics of the studied gels, which can predict the stability of the dispersed system during storage and the ability to bioadhesion on the skin surface when using them [20][21][22]. The research results are shown in Fig.…”

Section: Research Resultsmentioning

confidence: 99%

Biopharmaceutical and rheometric studies in the development of a gel composition with dimethindene maleate

Popova

Kukhtenko

Bevz

et al. 2021

SR: PS

View full text Add to dashboard Cite

Every year there is an increase in the number of cases of hypersensitivity to bites from various insects. A local allergic reaction to bites occurs within a few minutes and is accompanied by acute pain at the site of the bite, severe itching, hyperemia, the appearance of papules, tissue edema, and sometimes a small-point rash around. Considering the small number of drugs for local therapy of allergic manifestations and the unidirectional nature of their action, it is urgent to develop a drug containing the antihistamine dimethindene maleate and dexpanthenol, which plays the role of an anti-inflammatory, reparative and dermatoprotective substance. The aim. The aim of the study is to substantiate the delivery system of dimethindene maleate and dexpanthenol based on biopharmaceutical and rheometric research methods. Materials and methods. To determine the component composition of the active ingredient delivery system, the type of dimetindene maleate administration was substantiated by studying its solubility. As a delivery system for active pharmaceutical ingredients, hydrogels were considered, which were made using high-molecular compounds of various origins: a natural substance – xanthan gum, a semi-synthetic substance – gyroxypropyl methylcellulose, and a synthetic substance – carbomer. The rate of release of dimethindene maleate from hydrogels was estimated by studying the kinetics of release through a semipermeable membrane. The assessment of the viscoelastic properties of hydrogels was carried out by performing an oscillatory rheometry test, which makes it possible to quantitatively determine the viscous and elastic components, as well as to characterize the bioadhesive properties. Results. Based on the results of studying the solubility of dimethindene maleate in hydrophilic non-aqueous solvents, it was determined that propylene glycol is optimal for ensuring the introduction of a substance into hydrogel bases as a solution. As a result of studying the kinetics of the release of dimethindene maleate from hydrogels, it was found that the use of carbomer as a delivery system provides the release of 28.33 % of dimethindene maleate, xanthan gum – 25 %, hydroxypropyl methylcellulose – 7.33 %. When studying the viscoelastic properties by determining the values of the storage modulus G', the loss modulus G" and the damping (attenuation) factor tg δ, it was found that the carbomer-based hydrogel is a viscoelastic solid, the xanthan gum and hydroxypropyl methylcellulose-based hydrogels are a viscoelastic liquid. Bioadhesion on the surface of the skin during use has the advantage of carbomer hydrogel. Conclusions. Based on the combination of biopharmaceutical and rheometric methods for substantiating the composition of the delivery system for dimetindene maleate and dexpanthenol, it is rational to use carbomer for further pharmacological and microbiological studies

show abstract

Section: Research Resultsmentioning

confidence: 99%

Biopharmaceutical and rheometric studies in the development of a gel composition with dimethindene maleate

Popova

Kukhtenko

Bevz

et al. 2021

SR: PS

View full text Add to dashboard Cite

show abstract

“…У фармації як гелеутворювачі широко використовуються синтетичні високомолекулярні зшиті полімери акрилової кислоти, зокрема карбомери [5]. Компанія «Lubrizol Advanced Materials» випустила на ринок карбомери під назвою Carbopol ® Ultrez, які швидко диспергуються і легко набрякають у воді, що значно полегшує технологічний процес.…”

Section: анотаціяunclassified

“…Компанія «Lubrizol Advanced Materials» випустила на ринок карбомери під назвою Carbopol ® Ultrez, які швидко диспергуються і легко набрякають у воді, що значно полегшує технологічний процес. Карбомери є модифікаторами реологічних властивостей і стабілізаторами гетерогенних дисперсних систем і можуть забезпечити біофармацевтичні властивості гелів і контрольоване вивільнення лікарських речовин із них [5].…”

Section: анотаціяunclassified

Реологічні Дослідження Гелю, Що Містить Водний Витяг З Ксенодерми, Для Місцевого Лікування Опіків

Vons¹,

Melnyk²,

Hroshovyi³

et al. 2019

ФЧ

View full text Add to dashboard Cite

Мета роботи. Дослідження реологічних (тиксотропних) властивостей розробленого гелю та встановлення впливу температури на його стабільність. Матеріали і методи. Об’єктом дослідження обрано гель для місцевого лікування опіків на основі зшитого кополімеру акрилової кислоти – карбомеру Carbopol® Ultrez 21, що містить водний витяг із ксенодерми та лідокаїну гідрохлорид. Реологічні властивості досліджували на ротаційному віскозиметрі «Rheomat-30». Досліджували такі характеристики гелю, як напруга зсуву, динамічна в’язкість і механічну стабільність. Результати й обговорення. Для визначення типу течії, наявності тиксотропних властивостей і механічної стабільності гелю досліджено реограми його текучості. Під час експериментів встановлено, що досліджуваний гель є неньютонівською рідиною та має пластичний тип текучості, що характеризує його як структуровану дисперсну систему. Наявність тиксотропних властивостей у досліджуваному гелі характеризує задовільну здатність до екструзії з туб і намазування. Висновки. Визначено залежність реологічних властивостей, зокрема, структурної в’язкості досліджуваного гелю від температури. Розраховані значення механічної стабільності гелю дозволяють спрогнозувати стабільність препарату впродовж передбачуваного терміну його придатності.

show abstract

“…It was previously shown that the formation of gels with carbomers which were characterized by plastic flow behaviour and high apparent viscosity did not cause an increase in the viscosity of the gel dispersion medium. Dissolved in the gel base spin probes remained in a state of rapid isotropic rotation; that could be a prerequisite for the rapid release of dissolved active substances from such gels [3]. However, during those experiments the effect of this factor on the release of active substances was not studied.…”

Section: Introductionmentioning

confidence: 99%

“…Also it was shown that the interaction of the spin probe 4-amino-TEMPO and carboxylate anions of carbomers caused an increase in the rotational correlation time (τ -1 ) of this spin probe in the gels within a certain pH range. This interaction can affect the release of active substances with amino groups in the molecules, or prevent their introduction into formulations of gels based on carbomers [3]. However, that article does not contain any results of studies with other polymers, such as hypromellose (HPMC), which molecules do not possess reactive carboxylate anions.…”

Section: Introductionmentioning

confidence: 99%

Study of factors affecting the in vitro release of diclofenac sodium from hypromelose-based gels

Bezuglaya

Ivashchenko

Lyapunov

et al. 2021

SR: PS

View full text Add to dashboard Cite

The aim of our study was to identify factors affecting the in vitro release of diclofenac sodium (DS) from hypromellose-based gels (HPMC). Materials and methods. Gels with HPMC and liquids without HPMC were studied by viscosity-rotating viscometer method and spin probe electron paramagnetic resonance spectroscopy. Rheograms were used to determine the flow behavior and the apparent viscosity, and the EPR spectra were used to determine the rotational correlation time (τ–1) of the dissolved spin probes. The in vitro release tests were performed using vertical diffusion cells according to a validated procedure. The assay of DS and isopropyl alcohol (IPA) in the receptor medium was performed by high performance liquid chromatography (HPLC) and gas chromatography (GC) according to validated procedures, and the water content was determined using semi-micro method. Results. The apparent viscosity of the gels increased with increasing HPMC content and depended on the HPMC grade. The high apparent viscosity of the gels did not affect the values of τ–1 of the dissolved spin probes. In viscous gels and Newtonian fluids, the composition of which corresponded to the dispersion medium of gels, the values of τ–1 were identical and were in the range of rapid rotation, which is a prerequisite for similar and rapid release of the dissolved substances from gels and liquids. It was shown that the HPMC-based gel and Newtonian liquid without HPMC in terms of in vitro release parameters DS and IPA were equivalent. During in vitro testing the release of dissolved DS increased with increasing its concentration in the gel and depended on the dispersed state of DS. When the content of IPA was changed from 45.0 % to 22.5 %, the water absorption by the gel and the release of IPA decreased, and the release of DS increased, which was due to the decrease in the solubility of DS in the gel. Conclusions. HPMC, which provided high apparent viscosity of the gels, did not affect the value of τ–1 of the dissolved spin probes and the in vitro release of DS from the gels. The gel and Newtonian liquid were equivalent in terms of in vitro release of DS and IPA. The release of DS altered proportionally with the concentration of DS and depended on its dispersed state. As the content of IPA decreased, the release of IPA decreased, but the release of DS increased because of the decrease in the solubility of the DS in the gel

show abstract

Studies of Carbomer Gels Using Rotational Viscometry and Spin Probes

Cited by 11 publications

References 0 publications

Biopharmaceutical and rheometric studies in the development of a gel composition with dimethindene maleate

Biopharmaceutical and rheometric studies in the development of a gel composition with dimethindene maleate

Реологічні Дослідження Гелю, Що Містить Водний Витяг З Ксенодерми, Для Місцевого Лікування Опіків

Study of factors affecting the in vitro release of diclofenac sodium from hypromelose-based gels

Contact Info

Product

Resources

About