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This study aims to develop semisolid pharmaceutical forms for the topical administration of mometasone furoate.

Obtaining orodispersible tablets (ODT) containing substances from the second Biopharmaceutical Class has raised concerns as the dissolution test is challenging. This study aimed to select suitable excipients for developing orodispersible tablets containing cannabidiol (CBD) by direct compression method. No similar studies were found in the literature. Excipients from different classes were characterized using the SeDeM-ODT tool: fillers – lactose (LCT) and microcrystalline cellulose (CelMC), sweeteners – sorbitol (SRB) and mannitol (MNT), disintegrants – sodium starch glycolate (SSG), sodium croscarmellose (CCS), soy polysaccharides (Emcosoy® – EMCS) and two co-processed excipients (Prosolv®-ODT G2 – PODTG2 and Prosolv® EasyTab sp – PETsp). Drug compatibility with excipients in binary mixtures (1:1) was verified by Differential Scanning Calorimetry (DSC) and Fourier Transform-Infrared (FTIR) spectroscopy. Using the SeDeM-ODT expert system, the fillers and the co-processed excipients showed good properties regarding compressibility and disintegration behavior. Also, the DSC and FTIR results showed that small or no interactions between the CBD and the excipients took place. [ABSTRACT FROM AUTHOR]

One class of cosmetic compounds that have raised interest of many experts is peptides. The search for ingredients with good biocompatibility and bioactivity has led to the use of peptides in cosmetic products. Peptides are novel active ingredients that improve collagen synthesis, enhance skin cell proliferation, or decrease inflammation. Based on their mechanism of action, they can be classified into signal peptides, carrier peptides, neurotransmitter inhibitor peptides, and enzyme inhibitor peptides. This review focuses on the main types of peptides and their application in the cosmetic field, underlining their main limitations. One of the most significant drawbacks of cosmetic peptides is their poor permeability through membranes, which limits their delivery and effectiveness. As a result, this review follows the methods used for improving permeability through the stratum corneum. Increasing peptide bioavailability and stability for enhanced delivery to the desired site of action and visible effects have become central points for the latest research due to their promising features. For this purpose, several methods have been identified and described. Physical techniques include thermal ablation (radiofrequency and laser), electrical methods (electroporation, iontophoresis), mechanical approach (microneedles), and ultrasounds. As an alternative, innovative formulations have been developed in nano-systems such as liposomes, niosomes, ethosomes, nanoemulsions, and other nanomaterials to reduce skin irritation and improve product effectiveness. The purpose of this review is to provide the latest information regarding these noteworthy molecules and the reasoning behind their use in cosmetic formulations.

Background/objectives: The search for novel ways of providing treatment also targets the development of formulations used in drug delivery. Among the important characteristics of pharmaceutical gels are their ability to penetrate membranes, their capability to offer rapid response, and their capacity to avoid the hepatic metabolization route followed by many drugs. Bigels combine the advantages of both hydrogels and oleogels, creating a biphasic system that might improve the solubility of amiodarone in water, which is otherwise poorly soluble. This study aimed to succeed in formulating stable amiodarone hydrochloride bigels (coded from ABG1-ABG6) destined for atrial application and evaluating them from a pharmacotechnical perspective., Methods: Three of the six initial formulations presented stability and underwent studies of spreadability, rheology, drug content, textural properties, and microbiological activity. A statistical analysis was performed on penetrometry and drug assay data., Results: The spreadability varied from 1734.07 mm 2 (ABG1) to 2163.85 mm 2 (ABG6), while the drug concentration ranged between 1.35 and 1.49% ( w / w ). The textural profile analysis highlighted superior hardness, cohesiveness, and resilience for ABG6 and higher adhesion for ABG2. Both presented pseudoplastic thixotropic behavior, while a plastic thixotropic flow was registered in the case of ABG1., Conclusions: All three bigels are suitable for amiodarone incorporation; however, the influence of the type of ingredients chosen on the texture and properties of the formulations was reflected in the data gathered upon evaluation.

Background and Aims: The individualization of cosmetic products or personalized dermatology preparations are in great demand at the present time., Methods: 24 emulsifying cream bases were proposed which were prepared by the classical, automatic and semi-automatic methods, respectively, and the physical stability resulted from the three types of homogenization was taken into account. Texture parameters were also studied for the most stable cream bases in the preformulation stage and the t - statistical test was applied. In order to choose the most optimal preservative, the effectiveness of the NipaEster solution 0.1%, Cosgard and Euxyl ® PE 9010 was tested on the strains of Staphylococcus aureus , Pseudomonas aeruginosa , and Candida albicans ., Results: 9 cream bases were stable through all the preparation methods used, and preservation was achieved with Euxyl ® PE 9010. Following the texture parameters, significant differences were observed for the same formula in the case of choosing a different preparation method., Conclusions: Formulas F1, with methyl glucose sesquistearate as emulsifier, F8, with cetearyl glucosite as emulsifier, and F14, with Ceteareth-20 can be used as cream bases for customized products.

Allantoin possesses numerous beneficial properties for the skin, like anti-irritant effects, wound healing, skin hydration, and epithelization. In this paper, we investigated a suitable preparation method for an allantoin hydrogel using the Semi-Solid Control Diagram (SSCD) method and characterized its rheological and consistency behavior. To accomplish this, xanthan gum (XG) was selected as a model gelling agent. Briefly, four hydrogels were prepared, two without allantoin (coded M01 and M02) and two with allantoin (M1 and M2). Similarly, the formulations were either prepared through magnetic stirring (M01 and M1) or homogenization in a mortar (M02 and M2). The prepared hydrogels were evaluated using the SSCD for specific parameters and indexes. The Good Quality Index (GQI) shows a higher value for the formulation, M1 = 6.27, compared to M2 = 5.45. This result is also underlined by the value of M01 = 6.45, which is higher than M02 = 6.38. Considering the consistency, the formulation M01 possessed the highest spreadability, followed by M02 and then the allantoin hydrogels M1 and M2. The rheological behavior had a thixotropic pseudoplastic flow for all the formulations. The use of SSCD pictographs outlined the rheological properties that need improvement, the method that is suitable to prepare the allantoin hydrogels, and the influence of the allantoin suspended in the XG hydrogel.

Community pharmacy has evolved a lot in recent years in terms of pharmaceutical services and marketing policies applied in Romania. This study aimed to evaluate the degree of patient satisfaction in community pharmacies in Iași, Romania correlated with the frequency of returning to the pharmacy, level of education, gender, and stress level at the time when the pharmacist dispenses the medication. A total of 30 community pharmacies were involved, and in a period of three months, they issued questionnaires to patients. 722 patients responded, and to verify the first research hypothesis, the Pearson correlation was applied. Statistical analysis revealed that there is a negative, medium-level, and significant correlation between the level of satisfaction with pharmaceutical services and the frequency of visits to the pharmacy, r = -0.342, p < 0.0001. There is also a significant, negative correlation of low intensity between the level of satisfaction with pharmaceutical services and patient status, r = -0.202, p < 0.0001. The degree of patient satisfaction is influenced by the quality of the basic pharmaceutical service offered, by the frequency of visits to the pharmacy, by the level of stress, and by social class.

The main objective of this study consists in establishing the influence of the intergranular superdisintegrant on the specific properties of drotaverine hydrochloride fast-dissolving granules (DROT-FDGs) and orodispersible tablets (DROT-ODTs). The orodispersible tablets were obtained by the compression of the FDGs and excipient mixture with an eccentric tableting machine. To develop DROT-ODTs, two types of superdisintegrant excipients in different concentrations (water-soluble soy polysaccharides (SSP) (1%, 5%) and water-insoluble soy polysaccharides-Emcosoy ® STS IP (EMCS) (1%, 3%, 5%)) were used, resulting in five formulations (D1-D5). The DROT-FDGs and the DROT-ODTs were subjected to pharmacotechnical and analytical evaluation. All the orodispersible tablets obtained respect the quality requirements in terms of friability (less than 1%), crushing strength (ranging between 52 N for D2 and 125.5 N for D3), and disintegration time (<180 s). The in vitro release of drotaverine from ODTs showed that all formulations presented amounts of active substance released greater than 85% at 10 min. The main objective, developing 30 mg DROT-ODTs for children aged between 6 and 12 years by incorporating the API in FDGs, was successfully achieved.

This study aimed to develop caffeine (CAF) orodispersible films (ODFs) and verify the effects of different percentages of film-forming agent and hydrotropic substances (citric acid-CA or sodium benzoate-SB) on various film properties. Hydroxypropyl methylcellulose E 5 (HPMC E 5) orodispersible films were prepared using the solvent casting method. Four CAF-ODF formulations were prepared and coded as CAF1 (8% HPMC E 5, CAF), CAF2 (8% HPMC E 5 and CAF:CA-1:1), CAF3 (9% HPMC E 5 and CAF:CA-1:1), and CAF4 (9% HPMC E 5 and CAF:SB-1:1). The CAF-ODFs were evaluated in terms of disintegration time, folding endurance, thickness, uniformity of mass, CAF content, thickness-normalized tensile strength, adhesiveness, dissolution, and pH. Thin, opaque, and slightly white CAF-ODFs were obtained. All the formulations developed exhibited disintegration times less than 3 min. The dissolution test revealed that CAF1, CAF2, and CAF3 exhibited concentrations of active pharmaceutical ingredients (APIs) released at 30 min that were close to 100%, whilst CAF4 showed a faster dissolution behaviour (100% of the CAF was released at 5 min). Thin polymeric films containing 10 mg of CAF/surface area (3.14 cm 2 ) were prepared.

The development of semisolid formulations, gels in particular, has raised the attention of scientists more and more over the last decades. Because of their biocompatibility, hydrophilic nature, and capacity of absorbing large quantities of water, hydrogels are still one of the most promising pharmaceutical formulations in the pharmaceutical industry. The purpose of this study is to develop an optimal formulation capable of incorporating a water-poorly soluble active ingredient such as miconazole used in the treatment of fungal infections with Candida albicans and Candida parapsilosis . A D-optimal design was applied to study the relationship between the formulation parameter and the gel characteristics. The independent parameters used in this study were the Carbopol 940 concentration (the polymer used to obtain the gel matrix), the sodium hydroxide amount, and the presence/absence of miconazole. Ten different dependent parameters (Y1-Y10) were evaluated (penetrometry, spreadability, viscosity, and tangential tension at 1 and 11 levels of speed whilst destructuring and during the reorganization of the gel matrix). The consistency of the gels ranged from 23.2 mm (GO2) to 29.6 mm (GM5). The least spreadable gel was GO7 (1384 mm 2 ), whilst the gel that presented the best spreadability was GO1 (3525 mm 2 ). The viscosity and the tangential stress at the selected levels (1 and 11) varied due to the different compositions of the proposed gels. The gels were also tested for drug content and antifungal activity. All determinations had satisfying results; the drug content was within limits accepted by Ph. Eur. 10 and all formulations containing miconazole exhibited antifungal activity. An optimal formulation with miconazole was attained, consisting of 0.84% Carbopol 940 and 0.32% sodium hydroxide.

Orodispersible tablets (ODTs) are pharmaceutical formulations used to obtain fast therapeutic effects, usually recommended for geriatric and pediatric patients due to their improved compliance, bioavailability, ease of administration, and good palatability. This study aimed to develop ODTs with cannabidiol (CBD) phytocannabinoid extracted from Cannabis sativa used in the treatment of Lennox-Gastaut and Dravet syndromes. The tablets were obtained using an eccentric tableting machine and 9 mm punches. To develop CBD ODTs, the following parameters were varied: the Poloxamer 407 concentration (0 and 10%), the type of co-processed excipient (Prosolv ® ODT G2-PODTG2 and Prosolv ® EasyTab sp-PETsp), and the type of superdisintegrant (Croscarmellose-CCS, and Soy Polysaccharides-Emcosoy ® -EMCS), resulting in eleven formulations (O1-O11). The following dependent parameters were evaluated: friability, disintegration time, crushing strength, and the CBD dissolution at 1, 3, 5, 10, 15, and 30 min. The dependent parameters were verified according to European Pharmacopoeia (Ph. Eur.) requirements. All the tablets obtained were in accordance with quality requirements in terms of friability (less than 1%), and disintegration time (less than 180 s). The crushing strength was between 19 N and 80 N. Regarding the dissolution test, only four formulations exhibited an amount of CBD released higher than 80% at 30 min. Taking into consideration the results obtained and using the Modde 13.1 software, an optimal formulation was developed (O12), which respected the quality criteria chosen (friability 0.23%, crushing strength of 37 N, a disintegration time of 27 s, and the target amount of CBD released in 30 min of 99.3 ± 6%).

This study aims to develop new antifungal dermal films based on their mechanical properties (elongation, adhesion, behaviour towards vapour moisture) and the in vitro availability of miconazole nitrate, used as a pharmaceutical active ingredient in various concentrations. The three polymeric films prepared were translucent or shiny, with the surface of 63.585 cm², 0.20⁻0.30 mm thickness, and content of miconazole nitrate of 3.931 or 15.726 mg·cm². The mechanical resistance and elongation tests demonstrated that the two films based on hydroxyethyl cellulose (HEC) polymer were more elastic than the one prepared with hydroxypropyl methylcellulose (HPMC). The vapour water absorption and vapour water loss capacity of the films revealed that the HPMC film did not dry very well in the process of preparation by the evaporation of the solvent technique, unlike the HEC films that jellified more evenly in water and had higher drying capacity at 40 °C. The in vitro availability of miconazole nitrate from dermal films was evaluated using the Franz diffusion cell method, through a synthetic membrane (Ø 25 mm × 0.45 µm) and acceptor media with pH 7.4 (phosphate buffer and sodium lauryl sulphate 0.045%), resulting a release rate of up to 70%.

Aim: The development of a new pellets formulation which is able to modulate the release of metoprolol tartrate, an active pharmaceutical ingredient very soluble in water and therefore very difficult to process., Materials and Methods: Two types of different viscosity grade hydroxypropyl methylcellulose (Methocel K100; HPMC 15.000) and Eudragit NE30D are used as prolonged drug release agents, thus resulting in three formulations which have been prepared in form of pellets, in a conventional coating pan. The obtained pellets are characterized and compared in terms of: particles size distribution, drug loading efficiency, drug content and kinetic of in vitro drug release., Results: Lower amounts of Eudragit NE30D (7.5%) determine more uniform size distributions of particles. Drug content and charging efficiency is higher in case of fractions ranging in size from 0.80 to 1.25 mm. The combination of HPMC 15000 with 10% Eudragit NE30D leads to a prolongation for a period of 11.5 hours of metoprolol tartrate release. Release kinetics analysis was performed by fitting the in vitro release profile with different kinetic models., Conclusions: It was developed a pellets formulation that release in vitro the metoprolol tartrate in an extended mode, with Korsmeyer-Peppas kinetic-type.