Structural and Physicochemical Studies of Olopatadine Hydrochloride Conformational Polymorphs

Łaszcz, Marta; Trzcińska, Kinga; Witkowska, Anna; Ciesielska, Agnieszka; Badowska-Rosłonek, Katarzyna; Kuziak, Krzysztof

doi:10.1016/j.xphs.2016.05.031

Cited by 8 publications

(7 citation statements)

References 23 publications

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“…The more stable form of the API should always be used to avoid transformations during manufacture, delivery, or storage that could ultimately affect the properties of the drug and lead to undesirable therapeutic consequences [39]. The same difference in melting point was observed for polymorphs of various APIs described by Laszcz et al and in the work of Machado Viana et al [36,40]. When comparing different series of GML-3 substances (Form I) with Form II, it can be concluded that the change in the melting point is explained not by fluctuations in the size of particles and crystals in the samples but by the presence of another polymorphic form of API (Figure 5a).…”

Section: Micronization By the Ress Methodsmentioning

confidence: 64%

Section: Micronization By the Ress Methodsmentioning

confidence: 73%

“…Since this entails a change in the bioavailability and toxicity of the drug, there are several rules described in the guidance of the International Conference on Harmonization Q6A by Decision Tree No. 4, describing the requirements for controlling the behavior of the API in the solid state [36]. According to the European Pharmacopoeia, 57% of APIs can form hydrates, 20% form solvates, and about 58% are polymorphs [37,38].…”

Section: Introductionmentioning

confidence: 99%

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Modeling of the Aqueous Solubility of N-butyl-N-methyl-1-phenylpyrrolo[1,2-a] pyrazine-3-carboxamide: From Micronization to Creation of Amorphous–Crystalline Composites with a Polymer

Markeev,

Tishkov,

Vorobei

et al. 2023

Polymers

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N-butyl-N-methyl-1-phenylpyrrole[1,2-a] pyrazine-3-carboxamide (GML-3) is a potential candidate for combination drug therapy due to its anxiolytic and antidepressant activity. The anxiolytic activity of GML-3 is comparable to diazepam. The antidepressant activity of GML-3 is comparable to amitriptyline. GML-3 is an 18 kDa mitochondrial translocator protein (TSPO) ligand and is devoid of most of the side effects of diazepam, which makes the research on the creation of drugs based on it promising. However, its low water solubility and tendency to agglomerate prevented its release. This research aimed to study the effect of dry grinding, the rapid expansion of a supercritical solution (RESS), and the eutectic mixture (composite) of GML-3 with polyvinylpyrrolidone (PVP) on the particle size, dissolution rate, and lattice retention of GML-3. The use of supercritical CO2 in the RESS method was promising in terms of particle size reduction, resulting in a reduction in the particle size of GML-3 to 20–40 nm with a 430-fold increase in dissolution rate. However, in addition to particle size reduction after RESS, GML-3 began to show signs of a polymorphism phenomenon, which was also studied in this article. It was found that coarse grinding reduced particle size by a factor of 2 but did not significantly affect solubility or crystal structure. Co-milling with the polymer made it possible to level the effect of the appearance of a residual electrostatic charge on the particles, as in the case of grinding, and the increased solubility in the resulting mechanical mixtures of GML-3 with the polymer may also indicate the dissolving properties of polymers (an increase in 400–800 times). The best result in terms of GML-3 solubility was demonstrated by the resulting GML-3:PVP composite at a ratio of 1:4, which made it possible to achieve a solubility of about 80% active pharmaceutical ingredient (API) within an hour with an increase in the dissolution rate by 1600 times. Thus, the creation of composites is the most effective method for improving the solubility of GML-3, superior to micronization.

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Section: Micronization By the Ress Methodsmentioning

confidence: 64%

Section: Micronization By the Ress Methodsmentioning

confidence: 73%

Section: Introductionmentioning

confidence: 99%

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Modeling of the Aqueous Solubility of N-butyl-N-methyl-1-phenylpyrrolo[1,2-a] pyrazine-3-carboxamide: From Micronization to Creation of Amorphous–Crystalline Composites with a Polymer

Markeev,

Tishkov,

Vorobei

et al. 2023

Polymers

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“…26 in 2016 while studying structural and physicochemical studies of Olopatadine HCl conformational polymorphs. 26…”

Section: Discussionmentioning

confidence: 99%

Fabrication and evaluation of Olopatadine hydrochloride ocular inserts

Qureshi

Iqbal

Hussain

et al. 2020

Journal of Plastic Film & Sheeting

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Development of the novel delivery provides optimal drug delivery via facilitated transcorneal penetration and ultimately improved retention time in eye. The present study was to fabricate and evaluate the performance of ocular inserts of Olopatadine hydrochloride by consuming polymers such as hydroxypropyl methylcellulose, gelatin, and chitosan at various concentrations with different plasticizers using solvent casting technique. Prepared formulations were evaluated for thickness, weight variations, drug content, surface pH, swelling studies, and in vitro drug release. Fourier transform infrared spectroscopy studies showed that interaction occurred between polymer and drug, and successful drug entrapment occurred in the matrix. All formulations showed excellent film-forming capacity with good thickness and weight uniformity. Folding endurance proved that the inserts were soft, elastic, and flexible. Chitosan-based ocular inserts showed greater swelling index as compared to gelatin and hydroxypropyl methylcellulose inserts. In vitro studies showed prolonged drug release and followed zero-order kinetic model and non-Fickian drug release.

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“…Solubility measured after 5 h stirring in pure water at 25 and 35 °C showed that form II is 1.5 and 1.4 times more soluble than form I, respectively (ŁASZCZ et al, 2016).…”

mentioning

confidence: 94%

Polymorph screening and solubility characterization of lercanidipine hydrochloride

Repin¹

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Structural and Physicochemical Studies of Olopatadine Hydrochloride Conformational Polymorphs

Cited by 8 publications

References 23 publications

Modeling of the Aqueous Solubility of N-butyl-N-methyl-1-phenylpyrrolo[1,2-a] pyrazine-3-carboxamide: From Micronization to Creation of Amorphous–Crystalline Composites with a Polymer

Modeling of the Aqueous Solubility of N-butyl-N-methyl-1-phenylpyrrolo[1,2-a] pyrazine-3-carboxamide: From Micronization to Creation of Amorphous–Crystalline Composites with a Polymer

Fabrication and evaluation of Olopatadine hydrochloride ocular inserts

Polymorph screening and solubility characterization of lercanidipine hydrochloride

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