scholarly journals Nitrofurans for External Use (Review)

2019 ◽  
Vol 8 (2) ◽  
pp. 38-47
Author(s):  
A. V. Beliatskaya ◽  
I. M. Kashlikova ◽  
А. O. Elagina ◽  
I. I. Krasnyuk (jr.) ◽  
I. I. Krasnyuk ◽  
...  

Introduction. Aspects of the use of nitrofurans for external use (nitrofural, furazolidone and furazidin) are described in the article. Review of current research that is dedicated to development of drugs containing nitrofuran derivatives has been carried out. The prospects for creating dosage forms of furaсillin and furazolidone containing their solid dispersions with polymers are considered.Text. The group of nitrofurans is widely in demand in the modern pharmaceutical market. The most common active ingredients – furacillin, furazolidone and furazidin are represented by various dosage forms for both internal and external use. All nitrofuran derivatives have a wide spectrum of antimicrobial action and a specific mechanism of action on bacterial cells. The low level of development of antimicrobial resistance allows nitrofurans to remain one of the most effective chemotherapeutic groups of antimicrobial compounds for many decades. The review shows a numerous current developments carried out by both Russian and foreign authors about use of furacillin, furadonin and furazidin to develop the composition of new drugs, including combination drugs, as well as promising treatment methods. Currently, on the basis of Sechenov University, research is actively conducted to increase the solubility and dissolution rate of nitrofurans in water using the method of solid dispersions. Also, work is underway to develop the composition and technology of solid (instant) dosage forms granules and tablets, and soft dosage forms gels containing furacillin and furazolidone as active substances.Conclusion. Despite the use of active substances from the nitrofuran group in pharmaceutical practice for more than half a century and their low solubility in water, research on the development of complex drugs for external use and mono-preparations of nitrofurans have not lost their relevance and are actively conducted to this day.

2021 ◽  
pp. 45-51
Author(s):  
А.Б. ДЖУМАГАЗИЕВА ◽  
Е.Н. САХИПОВ ◽  
С. ТУРГАНБАЙ ◽  
Н.М. АТАГЕЛЬДИЕВА ◽  
У.М. ДАТХАЕВ ◽  
...  

Лекарственная устойчивость к антибиотикам вызвала необходимость поиска новых лекарственных средств и лекарственных форм. Известно, что семиорганические аддукты иода обладают широким спектром антимикробного действия. Эти же соединения, содержащие в своем составе молекулу галогена - иода, могут выступать в качестве галогенирующего агента в отношении антибиотиков. Изучено взаимодействие антибиотиков тетрациклина, гентамицина, хлорамфеникола, относящихся к классам поликетидов, аминогликозидов и амфениколов, соответственно, с аддуктом иода методами рефрактометрии, УФ-спектроскопии и ИК-спектроскопии. Показано, что антибиотик хлорамфеникол не взаимодействует с семиорганическим аддуктом иода ди2-аминопропионовой кислоты дитрииодоводород моногидратом (субстанция D1). Antibiotic drug resistance has necessitated the search for new drugs and dosage forms. It is known that semiorganic iodine adducts have a wide spectrum of antimicrobial effects. The same compounds containing a halogen-iodine molecule may act as a antibiotics halogenating agent. The interaction of antibiotics tetracycline, gentamicin, chloramphenicol belonging to the classes of polyketides, aminoglycosides and amphenicols, respectively, with iodine adduct by refractometry, UV spectroscopy and IR spectroscopy was studied. It has been shown that the antibiotic chloramphenicol does not interact with the semiorganic adduct of di-2-aminopropionic acid ditriiodinehydride monohydrate (D1 substance).


2016 ◽  
Vol 2 (2) ◽  
pp. 91-95
Author(s):  
Neelima Rani T ◽  
Pavani A ◽  
Sobhita Rani P ◽  
Srilakshmi N

This study aims to formulate solid dispersions (SDs) of Simvastatin (SIM) to improve the aqueous solubility, dissolution rate and to facilitate faster onset of action. Simvastatin is a BCS class II drug having low solubility & therefore low oral bioavailability. In the present study, SDs of simvastatin different drug-carrier ratios were prepared by kneading method. The results showed that simvastatin solubility & dissolution rate enhanced with polymer SSG in the ratio 1:7 due to increase in wetting property or possibly may be due to change in crystallinity of the drug.


2020 ◽  
Vol 16 ◽  
Author(s):  
Cansel Kose Ozkan ◽  
Ozgur Esim ◽  
Ayhan Savaser ◽  
Yalcin Ozkan

: The content and the application of pharmaceutical dosage forms must meet several basic requirements to ensure and maintain efficiency, safety and quality. A large number of active substances have limited ability to direct administration. Excipients are generally used to overcome the limitation of direct administration of these active substances. However, the function, behavior and composition of the excipients need to be well known in the design, development and production of pharmaceutical dosage forms. In this review, excipients used to assist in any pharmaceutical dosage form production processes of drugs, to preserve, promote or increase stability, bioavailability and patient compliance, to assist in product identification / separation, or to enhance overall safety and effectiveness of the drug delivery system during storage or use are explained. Moreover, the use of these excipients in drug delivery systems are identified. Excipient toxicity, which is an issue discussed in the light of current studies, also discussed in this review.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 451
Author(s):  
Beata Szulc-Musioł ◽  
Beata Sarecka-Hujar

In recent years, polyphenols have been extensively studied due to their antioxidant, anticancer, and anti-inflammatory properties. It has been shown that anthocyanins, flavonols, and flavan-3-ols play an important role in the prevention of bacterial infections, as well as vascular or skin diseases. Particularly, resveratrol, as a multi-potent agent, may prevent or mitigate the effects of oxidative stress. As the largest organ of the human body, skin is an extremely desirable target for the possible delivery of active substances. The transdermal route of administration of active compounds shows many advantages, including avoidance of gastrointestinal irritation and the first-pass effect. Moreover, it is non-invasive and can be self-administered. However, this delivery is limited, mainly due to the need to overpassing the stratum corneum, the possible decomposition of the substances in contact with the skin surface or in the deeper layers thereof. In addition, using resveratrol for topical and transdermal delivery faces the problems of its low solubility and poor stability. To overcome this, novel systems of delivery are being developed for the effective transport of resveratrol across the skin. Carriers in the micro and nano size were demonstrated to be more efficient for safe and faster topical and transdermal delivery of active substances. The present review aimed to discuss the role of resveratrol in the treatment of skin abnormalities with a special emphasis on technologies enhancing transdermal delivery of resveratrol.


Author(s):  
Rana Obaidat ◽  
Bashar Al-taani ◽  
Hanan Al-quraan

Objective: Meloxicam is classified as class II corresponding to its high permeability and low solubility (12μg/ml). This study aims to compare the effect of selected polymers on stabilization of amorphous form, and dissolution of meloxicam by preparation of different solid dispersions using selected polymers (chitosan oligomers, polyvinylpyrrolidone K30, and polyethylene glycols).Methods: These solid dispersions were prepared using two different methods; solvent evaporation method for the two molecular weights chitosan carriers (16 and 11KDa) and polyvinylpyrrolidone-K30 and melting method for the two different molecular weights polyethylene glycol (4000 and 6000). The physicochemical properties of solid dispersions were analyzed using differential scanning calorimetry, Fourier transform infra-red analysis, Powder X-ray diffraction, and scanning electron microscopy. Selected dispersions were then compared to two selected marketed drugs (Mobic® and Moven®).Results: Best dissolution rates were obtained for both polyvinylpyrrolidone-K30 and polyethylene glycol 6000, followed by chitosan 16 kDa, chitosan 11 kDa, and polyethylene glycol 4000. Increasing polymeric ratio increased dissolution rate except for chitosan. Precipitation of the drug as amorphous form occurred in chitosan and polyvinylpyrrolidone-K30 dispersions, while no change in crystallinity obtained for polyethylene glycol dispersions. Failure of polyvinylpyrrolidone-K30 in the maintenance of stability during storage time was observed while re-crystallization occurred in chitosan-based dispersions, which ends with preferences to polyethylene glycol dispersions. After comparing the release of selected dispersions with the two selected polymers; all dispersions got a higher release than that of the two marketed drugs release.Conclusion: The dissolution profile of meloxicam has been increased successfully in a reproducible manner.


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