In modern neurology, the main component of successful treatment of cerebrovascular pathology is pharmacotherapy. At the same time, the arsenal of effective medicines of evidence-based medicine in this area is quite limited. Vinpocetine (Cavinton) is one of the drugs that effectively selectively corrects cerebral perfusion. The use of alternative ways of absorption of vinpocetine (rectal and nasal) in certain soft application dosage forms will allow to significantly increase the bioavailability of the medicinal substance, reduce the level of adverse reactions from its use and expand the pharmacotherapeutic arsenal of domestic effective neuroprotective drugs. Taking into account the above, the employees of the Department of Medicines Technology of Zaporizhzhia State Medical University, on the basis of complex physical-chemical, pharmacotechnological, rheological and biopharmaceutical research, proposed rational formulations and technologies of two new soft application dosage forms of vinpocetine – rectal suppositories on a lipophilic basis and nasal cream on an emulsion basis for the therapy of arterial hypertension of II–III stages with cerebrovascular complications, reduction of the manifestation of neurological and/or mental symptoms in various forms of cerebral blood circulation insufficiency, consequences of a stroke, transient ischemic attack, etc. The aim of the work is to study the specific activity of the proposed innovative application dosage forms of vinpocetine. Materials and methods. Nasal ointment containing 0.5 % vinpocetine on an emulsion basis and rectal suppositories with vinpocetine 0.01 g on a lipophilic carrier were used as the object of preclinical studies, which ensure optimal release of the active pharmaceutical ingredient. The study of the specific activity of the developed medicinal forms of vinpocetine was carried out on a model of acute cerebrovascular accident of the type of ischemic stroke. Vinpocetin tablets (Astrapharm, Ukraine), which are used in neurological practice quite effectively and over a long period of time, were used as a comparison drug. Results. The comparative results showed that the appointment of all studied drugs led to an increase in motor activity. In addition, the administration of medicinal forms of vinpocetine reduced the development of cognitive and cognitive disorders after acute disorders of cerebral blood circulation. It was found that the highest result was shown by the group of animals that received a course of vinpocetine intranasally. In the groups of animals that received vinpocetine for 4 days, markers of oxidative stress – aldehyde phenylhydrazones and ketone phenylhydrazones – were significantly reduced. The highest activity was demonstrated by the pharmaceutical form of vinpocetin, which was used intranasally for 4 days. The introduction of dosage forms of vinpocetine exerted an energizing effect, which was expressed in an increase in the level of macroergic phosphates. Evidently, vinpocetine has a direct positive effect on the three-carbon sections of the Krebs cycle and increases the production of adenosine triphosphate (ATP). At the same time, the vinpocetine nasal cream applied intranasally for 4 days demonstrated the greatest energizing activity. Conclusions. Preclinical studies of the developed application soft medicines with vinpocetine on the model of acute cerebrovascular accident type ischemic stroke experimentally confirmed the expressed neuroprotective activity of rectal suppositories and nasal cream with vinpocetine and it was found that the effectiveness of therapy with these application medicinal forms is demonstrably higher than that in comparison with oral tablet means.
The external treatment of seborrheic dermatitis of the scalp depends on the withdrawal of clinical symptoms and the complaints the patient made to the doctor. At present Ukrainian dermatology has several dozen pharmacotherapeutic products in this direction, with dominating medicines of ketoconazole, zinc pyrition, and their combinations. They are characterized by the short-term or weak effect, associated with the pathogenic microorganisms’ resistance against the background of long-term use of biologically active substances which are their active parts. One way to solve the problem is using the drugs with new highly active pharmaceutical ingredients. Employees of the Department of Technology of Medications of the Zaporizhzhia State Medical University proposed the composition of a new applicate semisolid dosage form of pirocton olamine based on complex physical-chemical, pharmacotechnological, biopharmaceutical, and rheological investigations – topical ointment on the hydrophilic base in combination with resin-free naphthalene for external use in the complex etiotropic treatment of seborrheic dermatitis of the scalp. The aim of this work is to study the specific activity of the combined ointment with pirocton olamine and resin-free naphthalene on a hydrophilic vehicle. Materials and methods. As the object of preclinical studies used experimental ointment containing 1 % piroctone olamine and 5 % resin-free naphthalene on the base of sodium carboxymethylcellulose glycerogel, providing optimum release of active pharmaceutical ingredients from the vehicle, and appropriate placebo semisolid dosage form. The study of the specific activity of the developed ointment under the conditional name “Oktonaf” was carried out by evaluating its antimicrobial, anti-inflammatory, and antioxidant effects given the foreseeable therapeutic focus and the literature on the spectrum of biological activity of active substances. The anti-inflammatory and antioxidant action of the proposed composition was evaluated by the allergic contact dermatitis model. As a reference drug cream “Psoricap” (KMP, Ukraine), which has long been applied in dermatological practice was used. Results of comparative microbiological studies proved that composite anti-seborrheic ointment with piroctone olamine and resin-free naphthalene by the antibacterial effect in relation to the size of the growth delay zones for Staphylococcus aureus and Escherichia coli (gram-positive and gram-negative microorganisms) slightly exceeds the effective dermatological medication reference cream “Psoricap”. At the same time, the antimycotic activity of experimental ointment in relation to Candida albicans practically does not differ from the same reference drug. A study of antioxidant and anti-inflammatory activity of the developed piroctone olamine ointment on a hydrophilic basis using the model of allergic contact dermatitis revealed that its level reliably was exceed the efficacy of topical reference medication “Psoricap”. Conclusions. Obtained data of a spectrum of specific activity of a combined ointment with piroctone olamine and resin-free naphthalene can predict the high clinical value of the proposed drug for practical domestic dermatology.
Diuretics increase the volume of urine and sodium excretion, and therefore are often used to remove excess fluid from the body during various diseases, including hypertension, heart and kidney failure, nephrotic syndrome, cirrhosis, etc. Until now, a wide range of diuretics is known, but none of them is completely safe and has a number of side effects. The aim of the work is to investigate the diuretic activity of 1,2,4-triazole derivatives containing fluorophenyl substituents at the fifth position of the 1,2,4-triazole fragment, as well as to establish the relationship between “chemical structure and diuretic action” among derivatives 1,2,4-triazole. Materials and methods. To study the effect on kidney function, six groups of animals with seven rats each were used. When studying water diuresis, rats were kept on a constant diet with free access to water. Before water loading (5 % of body weight), rats were fasted for 2 hours without food and water. Since all tested compounds were insoluble in water, they were administered orally as an aqueous suspension stabilized with Tween-80. The compounds were administered at a dose of 1/10 LD50. Results. The diuretic activity of 28 new compounds of a number of substituted 1,2,4-triazole-3-thiols, which according to their chemical structure belong to different classes of compounds, was investigated. Conclusions. Analysis of the results of diuretic activity indicates that there are a number of compounds whose activity is higher than hypothiazide, as well as a compound that exceeds the activity of furosemide.
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