Development of soft dosage forms of pyrimidine derivatives based on carbopols

2021 ◽  
pp. 36-41
Author(s):  
Maria Boldina ◽  
Viktoriya Grikh ◽  
Alina Gubanova ◽  
Maxim Stantsov ◽  
Anna Kozlova
Keyword(s):  
Side Effects ◽  
Solid Phase ◽  
Skin Barrier ◽  
Dosage Forms ◽  
Pharmaceutical Market ◽  
Ease Of Use ◽  
Gelling Agent ◽  
Structural Element ◽  
Pharmaceutical Substance ◽  
Pharmaceutical Substances

In the process of improving the technology for obtaining and expanding the range of dosage forms of known pharmaceutical substances, an important aspect is to reduce side effects and ensure ease of use. At the same time, medicines should provide the most important properties of pharmaceutical substances, namely, their most rapid and complete release from the base of the dosage form and penetration into the target organ, which should serve as factors in justifying formulations and technologies of effective and safe medicines [3, 4]. Due to the lesser manifestation of side effects and ease of use, soft dosage forms (gels, ointments) are among the most demanded dosage forms on the modern pharmaceutical market. The trend towards replacing hydrophobic bases in soft dosage forms with hydrophilic ones has been traced in pharmacy for quite a long time, since gels provide higher efficiency in application due to better penetration of pharmaceutical substances through the skin barrier relative to hydrophobic ointments. The presence of a polymer-gelling agent in gels determines not only the rheological properties of medicines, but also allows a highly dispersed solid phase of a pharmaceutical substance to be included in the network structure of a polymer and to maintain the dispersion of a pharmaceutical substance poorly soluble in water during storage. Methyluracil, also known as dioxomethyltetrahydropyrimidine, is a derivative of pyrimidine, a structural element of nucleic acids and is used in the treatment of diseases of various etiologies, mainly to improve the course of regeneration in damaged tissues. A significant disadvantage of methyluracil is its low solubility in water, which significantly affects the degree of release of the pharmaceutical substance from the base of the drug [1]. Due to the lack of methyluracil gels on the pharmaceutical market, their development using acrylic acid derivatives in order to improve the biopharmaceutical properties of a pharmaceutical substance is an important problem in pharmacy.

Assortment Analysis And Comparative Characteristics Of The Results Of Registration Of Sedative Drugs In The Republic Of Uzbekistan

2021 ◽  
Vol 03 (07) ◽  
pp. 77-91
Author(s):  
Firuza Alisherovna Umarova ◽  
◽  
Kamal Saidakbarovich Rizaev ◽  
Nemat Kayumovich Olimov ◽  
Zaynab Enverovna Sidametova ◽  
...  
Keyword(s):  
Medicinal Product ◽  
Raw Materials ◽  
Dosage Forms ◽  
Pharmaceutical Market ◽  
Joint Stock Company ◽  
Stock Company ◽  
Dry Extract ◽  
The Republic ◽  
Sedative Drugs

Analysis of the assortment of sedatives registered in the Republic of Uzbekistan showed that sedatives are represented on the pharmaceutical market of the country by such dosage forms as drops, solutions, tinctures, syrups, medicinal herbal raw materials, capsules and tablets. Considering that sedatives registered in the form of a substance, with the exception of the dry extract of Leoglycyrfl produced by “Uzkimyofarm”, there are practically no names of S.K. Islambekov in the Joint Stock Company. In this regard, we consider it expedient to create a new sedative medicinal product of herbal origin in the form of a substance and obtain dosage forms based on it.

VASODILATORS FOR THE TREATMENT OF CARDIAC DISEASES (С01D) ON THE PHARMACEUTICAL MARKET OF THE REPUBLIC OF BELARUS

2021 ◽  
Vol 92 (2) ◽  
pp. 33-39
Author(s):  
S. E. Rzheussky ◽  
◽  
P. S. Varabei ◽  
Keyword(s):  
Side Effects ◽  
Domestic Market ◽  
Pharmaceutical Market ◽  
Isosorbide Mononitrate ◽  
Cardiac Diseases ◽  
Bcg Matrix ◽  
The Matrix ◽  
The Republic ◽  
Marketing Information

The article studies the domestic market of vasodilators for cardiac diseases in Belarus by analyzing and comparing secondary marketing information. The structure of the market depending on the manufacturing country was studied. It was established that medicines containing isosorbide mononitrate/dinitrate have the greatest number of indications to use and the least number of side effects. The dynamics of changing the sales of medicines in the vasodilators group for cardiac diseases for the period 2010-2018 is presented. The market attractiveness of medicines of the vasodilators group for cardiac diseases was studied using the matrix of the Boston Consulting Group (BCG matrix).

The use of phytotherapy in diseases caused by parasitic protozoa

2014 ◽  
Vol 60 (1) ◽  
pp. 1-8 ◽  
Author(s):  
Monika Derda ◽  
Edward Hadaś
Keyword(s):  
Side Effects ◽  
Chronic Diseases ◽  
Conventional Treatment ◽  
Therapeutic Agents ◽  
Pharmaceutical Market ◽  
Parasitic Diseases ◽  
Plant Origin ◽  
Parasitic Protozoa ◽  
Herbal Preparations ◽  
Increasing Demand

AbstractThe paper presents an overview of the use of natural therapeutic agents in combating parasitic diseases. Nowadays there is increasing demand for proven plant therapies, which often are found to be more effective than synthetic pharmaceuticals in chronic diseases. In many cases herbal preparations perfectly supplement the conventional treatment and at the same time do not cause side effects. On the pharmaceutical market there are many drugs of plant origin which have been applied in the treatment of parasitic diseases. However, researchers are still looking for new plants, or specific substances isolated from them, which can be used in therapy. In this paper, drugs of plant origin used in the treatment of amoebiasis, giardiasis, malaria, leishmaniasis, trypanosomiasis and acanthamoebiasis are described.

scholarly journals Using Oral and Intranasal Dosage Forms of Ketamine for Managing Treatment-Resistant Depression: A Review of the Literature

2016 ◽  
Vol 4 (2) ◽  
pp. 64-71 ◽  
Author(s):  
Patrick Arthur Twohig ◽  
Vaughn Huckfeldt
Keyword(s):  
Health Care ◽  
Side Effects ◽  
Care Setting ◽  
Dosage Forms ◽  
Treatment Resistant Depression ◽  
Treatment Resistant ◽  
Similar Reduction ◽  
Aspartate Receptor ◽  
Pubmed Database ◽  
Resistant Depression

A lack of effective treatment for patients with treatment-resistant depression (TRD) has led to the evaluation of ketamine, an N-methyl- D-aspartate receptor antagonist. Despite the demonstrated short-term benefits of using intravenous (IV) ketamine, side effects and the difficulty in administering ketamine outside the health-care setting has raised interest in alternative dosage forms. Research articles evaluating oral or intranasal (IN) ketamine were retrieved from the PubMed database. Patients who received oral or IN ketamine experienced a similar reduction in depressive symptoms within 24 hours of treatment and fewer side effects compared to patients who received IV ketamine. Novel administration forms of ketamine provide an opportunity for patients with TRD to achieve remission with fewer adverse side effects. Future studies should continue to evaluate these administration strategies in the hope of promoting ketamine’s use outside health-care settings and for longer time periods.

scholarly journals FORMULASI DAN KARAKTERISASI FISIK MASKER GEL PEELOFF EKSTRAK LENGKUAS (Alpinia galanga, (L.) Sw)

2019 ◽  
Vol 16 (02) ◽  
pp. 14
Author(s):  
Mar’atus Sholikhah ◽  
Rahayu Apriyanti
Keyword(s):  
Statistical Tests ◽  
Ease Of Use ◽  
Gelling Agent ◽  
P Value ◽  
Topical Drug Delivery ◽  
Drying Time ◽  
Pharmaceutical Dosage Forms ◽  
Alpinia Galanga ◽  
Organoleptic Parameters

ABSTRACT Alpinia galanga (L.) Sw or galangal is widely used by Indonesian people as a spice in cooking. The content of catechins and 1-acetoxicavicol acetate in the extract is known to have antioxidant activity. The ability of these antioxidants needs to be applied to pharmaceutical dosage forms to improve aesthetics and ease of use. One of the topical drug delivery systems that is in accordance with the needs of the community today is the preparation of peel-off gel mask. The purpose of this study was to determine the effect of variations in PVA gelling agent concentration as a mask base on the physical characteristics of galangal extract peel-off gel masks. Three mask formulations were made based on variations in the concentration of PVA in the range of 5% -15%. The physical characterization of the preparations included organoleptic tests, homogeneity, pH, viscosity, adhesion, dispersion, and drying time. Homogeneity and organoleptic parameters were analyzed descriptively. The parameters of viscosity, drying time, pH, spreadability, and adhesion were analyzed statistically using Anova Single Factor with a confidence level of 95%. The results showed that the F1 and F2 formulas with PVA concentrations of 10% and 12.5% were the optimum formulas as a mask base. Based on statistical tests, variations in the concentration of PVA significantly influence the parameters of mask adhesion with a p-value of 0.0001 (

scholarly journals EFFECT OF SOLID DISPERSIONS ON THE SOLUBILITY OF METRONIDAZOLE

2021 ◽  
Vol 9 (3) ◽  
pp. 195-204
Author(s):  
I. I. Krasnyuk (Jr.) ◽  
S. R. Naryshkin ◽  
I. I. Krasnyuk ◽  
A. V. Belyatskaya ◽  
O. I. Stepanova ◽  
...  
Keyword(s):  
Optical Properties ◽  
Solid Dispersion ◽  
Active Substance ◽  
Solid Phase ◽  
Solid Dispersions ◽  
Dosage Forms ◽  
Polyethylene Glycols ◽  
Uv Spectrophotometry ◽  
Colloidal Solutions ◽  
Constant Weight

The aim of the work is to study the effect of solid dispersions using polyethylene glycols of various molecular weights on the solubility of metronidazole in water. Metronidazole is an antimicrobial and antiprotozoal drug. Its low solubility in water limits the use of metronidazole, causing technological difficulties and reducing its bioavailability. The solubility and release of the active substance from dosage forms can be increased using the solid dispersion methods. Solid dispersions are bi- or multicomponent systems consisting of an active substance and a carrier (a highly dispersed solid phase of the active substance or molecular-dispersed solid solutions) with a partial formation of complexes of variable compositions with the carrier material.Materials and methods. The substance of metronidazole used in the experiment, was manufactured by Hubei Hongyuan Pharmaceutical Technology Co., Ltd. (China). To obtain solid dispersions, polyethylene glycols of various molar masses – 1500, 2000 and 3000 g/mol – were used. The solid dispersions were prepared by “the solvent removal method”: metronidazole and the polymer were dissolved in a minimum volume of 96% ethyl alcohol (puriss. p.a./analytical grade) at 65±2°C, and then the solvent was evaporated under vacuum to the constant weight. A vacuum pump and a water bath were used at the temperature of 40±2°C. The dissolution of the samples was studied using a magnetic stirrer with heating, and a thermostatting device. The concentration of metronidazole was determined on a spectrophotometer using quartz cuvettes at the wavelength of 318±2 nm. To filter the solutions, syringe nozzles were used, the pores were 0.45 μm, the filter was nylon. Microcrystalloscopy was performed using a microscope with a digital camera. The optical properties of the solutions were investigated using a quartz cuvette and a mirror camera (the image exposure – 20 sec).Results. Obtaining solid dispersions increases the completeness and rate of the metronidazole dissolution. The solubility of metronidazole from solid dispersions increases by 14–17% in comparison with the original substance. The complex of physical-chemical methods of the analysis, including UV spectrophotometry, microcrystalloscopy and the study of the optical properties of the obtained solutions, makes it possible to suggest the following. The increase in the solubility of metronidazole from solid dispersions is explained by the loss of crystallinity and the formation of a solid solution of the active substance and the solubilizing effect of the polymer with the formation of colloidal solutions of metronidazole at subsequent dissolution of the solid dispersion in water.Conclusion. The preparation of solid dispersions with polyethylene glycols improves the dissolution of metronidazole in water. The results obtained are planned to be used in the development of rapidly dissolving solid dosage forms of metronidazole with an accelerated release and an increased bioavailability.

Analgesics from the history to contemporary times

2021 ◽  
pp. 61-68
Author(s):  
Ekaterina Mikhailovna Grigorevskikh ◽  
Fam Tkhi Khong Zung ◽  
Svetlana Anatolievna Lebedeva ◽  
Susanna Sergeevna Sologova
Keyword(s):  
Quality Of Life ◽  
Dosage Forms ◽  
Pharmaceutical Market ◽  
Development Path ◽  
Almost All

Pain is an important signal of almost all pathological processes. At the same time, in the presence of painful sensations, a person tried to eliminate them to improve the quality of life. Therefore, at all times, painkillers are played a very important role in the pharmaceutical market. The search for new molecules with analgesic properties and the development of dosage forms for already acting drugs are still important tasks in the pharmaceutical environment. In this review, we tried to show development path of the search for a new painkillers.

FORMULASI GEL PATI BENGKUANG (Pachyrhizus erosus (L.) Urb.) DENGAN GELLING AGENT METILSELULOSA

2017 ◽  
Vol 1 (2) ◽  
pp. 121
Author(s):  
Husnul Warnida
Keyword(s):  
Dosage Forms ◽  
Gelling Agent ◽  
Whitening Agent ◽  
Pachyrhizus Erosus ◽  
Inhibitory Activities ◽  
Spreading Test

Bengkuang roots (Pachyrhizus erosus (L.) Urb.)  empirically have been used as cosmetics materials, primarily as sun screen and whitening agent. Bengkuang roots posses 6 compound which have tyrosinase inhibitory activities. Commercially, bengkuang roots available as whitening cream and lotion but those dosage forms are not suitable for oily skin. In this study the gel was formulated with varying methylcellulose (4% and 5%) as gelling agent. The evaluation included stability, organoleptic, pH, homogeneity, and spreading test. Formula A (4% methylcellulose) meets all physical requirements of gel. The result of acceptability (hedonic test. showed the most acceptance formula was formula A (4% methylcellulose).

scholarly journals Practical aspects of etomidate use in the management of hypercortisolaemia

2012 ◽  
Vol 167 (5) ◽  
pp. 729 ◽  
Author(s):  
Veronica A Preda ◽  
Ashley B Grossman
Keyword(s):  
Side Effects ◽  
Propylene Glycol ◽  
Cushing’S Syndrome ◽  
Dose Regimen ◽  
Cushing's Syndrome ◽  
Ease Of Use ◽  
Recommended Dose ◽  
Lipid Formulation ◽  
Starting Dose

We appreciate the letter from of Dr Soh et al. regarding our review on the use of etomidate in the treatment of Cushing's syndrome. We note that in their experience, our recommended dose regimen of 2.5 mg/h or thereabouts appears to be a safe and effective starting dose in most patients, and we note the utility and ease of use of the lipid formulation and its relative freedom from side effects compared with the more commonly used propylene glycol formulation; these are very helpful comments. Their experience in treating a further four patients is indeed further evidence of the usefulness of this agent.

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