scholarly journals APPLICATION OF INDOMETHACIN IN MEDICINE AND PHARMACY

2018 ◽  
Vol 73 (2) ◽  
pp. 130-134
Author(s):  
I. I. Krasnuk ◽  
T. M. Kosheleva ◽  
A. V. Belyatskaya ◽  
I. I. Krasnuk ◽  
O. I. Stepanova ◽  
...  
Keyword(s):  
Water Solubility ◽  
Solid Phase ◽  
Dosage Forms ◽  
Multicomponent Systems ◽  
Inhibit Protein Synthesis ◽  
Highly Dispersed ◽  
Partial Formation ◽  
Anti Inflammatory ◽  
The 1960S ◽  
Proliferation And Invasion

Indomethacin, a non-steroid anti-inflammatory drug (NSAID), has been used in different spheres of medicine since the 1960s. It is successfully administered as an anti-inflammatory and pain-relieving medication in rheumatoid and other diseases. According to recent research, indomethacin may become a promising drug enhancing endogenous remyelination in patients with multiple sclerosis. Also, indomethacin affects cell proliferation and invasion, thus it is used to manage pancreatic cancer in patients with hyperglycemia. In addition, indomethacin can inhibit protein synthesis in colorectal carcinoma and other types of cancer cells. The article reviews modern indomethacin medications and the different dosage forms on the Russian pharmaceutical market. Indomethacin poor water solubility is one of the reasons for decreasing its biopharmaceutical characteristics. According to the conducted research, a prospective way to improve indomethacin solubility and bioavailability is the Solid Dispersion (SD) method. SDs are bi- or multicomponent systems consisting of the drug and the carrier. They are a highly dispersed solid phase of the drug or molecular-dispersed solid solutions with a partial formation of a variable composition complex and a carrier. The article provides a brief overview on different aspects of obtaining, investigating, and applying indomethacin SDs with various polymers.

Primordial science and pioneering approaches of guggul for chronic ailments – A modernized review

2020 ◽  
Vol 7 (2) ◽  
pp. 14-20
Author(s):  
Jamal Basha D ◽  
Kumar P R ◽  
Ranganayakulu D
Keyword(s):  
Water Solubility ◽  
Therapeutic Potential ◽  
Chemical Constituents ◽  
Signs And Symptoms ◽  
Dosage Forms ◽  
The Novel ◽  
Lipids Metabolism ◽  
Clinical Conditions ◽  
Novel Drug ◽  
Conventional Dosage

An oleo gum resin guggulu is a product which obtained as a result of gummosis from the bark of Commiphora wightii (Arnott) Bhandari [syn. Commiphoramukul (Hook. Ex Stocks) Family, Burseraceae]. It has been known for its immense applicability in the Ayurveda since time immemorial for the treatment of variety of disorders such as inflammation, gout, rheumatism, impotence, leprosy, obesity, and disorders of lipids metabolism. It is a mixture of phytoconstituents like terpenoids, steroids, flavonoids, guggultetrols, lignans, sugars, and amino acids. This review is an effort to compile all the information available on all of its chemical constituents which are responsible for its therapeutic potential, limitation of guggul extracts and the necessity of novel principles for gum guggul. Nowadays, Guggul is available as the marketed formulation for curing numerous clinical conditions and is accessible in combination with various other ingredients. Though conventional dosage form shows the dominance as patient compliance and easy availability, yet it has found to pose the problems like dose fluctuation, peak-valley effect, non-adjustment of the administered drug, invasiveness etc. Guggul lacks its desired effect due to its low bioavailability and water solubility. This makes it a partial or a deficient therapy for remedy of many signs and symptoms. Novel drug delivery system (NDDS), a new approach and has excluded many of drawbacks exhibited by conventional dosage forms. Some of the novel dosage forms of guggul has been formed like nanoparticles, nanovesicles, gugglusomes and proniosomal gel. But still, the novel formulations for guggul has its less outspread in the market. Guggul can be executed as a profitable drug using NDDS. There is a need to highlight the unidentified and unexplained facts about guggul so as to make it more efficacious and effective in terms of bioavailability and aqueous insolubility.

scholarly journals Farnesol-Loaded Liposomes Protect the Epidermis and Dermis from PM2.5-Induced Cutaneous Injury

2021 ◽  
Vol 22 (11) ◽  
pp. 6076
Author(s):  
Yu-Chiuan Wu ◽  
Wei-Yun Chen ◽  
Chun-Yin Chen ◽  
Sheng I. Lee ◽  
Yu-Wen Wang ◽  
...  
Keyword(s):  
Chronic Inflammation ◽  
Water Solubility ◽  
Antibacterial Properties ◽  
Hair Follicles ◽  
Protective Effects ◽  
Cutaneous Injury ◽  
Anti Inflammatory ◽  
High Concentrations ◽  
Acute And Chronic Inflammation

Particulate matter with aerodynamic diameter ≤2.5 μm (PM2.5) increases oxidative stress through free radical generation and incomplete volatilization. In addition to affecting the respiratory system, PM2.5 causes aging- and inflammation-related damage to skin. Farnesol (Farn), a natural benzyl semiterpene, possesses anti-inflammatory, antioxidative, and antibacterial properties. However, because of its poor water solubility and cytotoxicity at high concentrations, the biomedical applications of Farn have been limited. This study examined the deleterious effects of PM2.5 on the epidermis and dermis. In addition, Farn-encapsulated liposomes (Lipo-Farn) and gelatin/HA/xanthan gel containing Lipo-Farn were prepared and applied in vivo to repair and alleviate PM2.5-induced damage and inflammation in skin. The prepared Lipo-Farn was 342 ± 90 nm in diameter with an encapsulation rate of 69%; the encapsulation significantly reduced the cytotoxicity of Farn. Lipo-Farn exhibited a slow-release rate of 35% after 192 h of incubation. The half-maximal inhibitory concentration of PM2.5 was approximately 850 μg/mL, and ≥400 μg/mL PM2.5 significantly increased IL-6 production in skin fibroblasts. Severe impairment in the epidermis and hair follicles and moderate impairment in the dermis were found in the groups treated with post-PM2.5 and continuous subcutaneous injection of PM2.5. Acute and chronic inflammation was observed in the skin in both experimental categories in vivo. Treatment with 4 mM Lipo-Farn largely repaired PM2.5-induced injury in the epidermis and dermis, restored injured hair follicles, and alleviated acute and chronic inflammation induced by PM2.5 in rat skin. In addition, treatment with 4 mM pure Farn and 2 mM Lipo-Farn exerted moderate reparative and anti-inflammatory effects on impaired skin. The findings of the current study indicate the therapeutic and protective effects of Lipo-Farn against various injuries caused by PM2.5 in the pilosebaceous units, epidermis, and dermis of skin.

scholarly journals Syntheses of two deacetyl-thymosin β4analogs and their anti-inflammatory effect on carrageenin-induced edema in the mouse paw

2001 ◽  
Vol 10 (2) ◽  
pp. 89-92 ◽  
Author(s):  
T. Abiko ◽  
R. Ogawa
Keyword(s):  
Marked Reduction ◽  
Solid Phase ◽  
The Other ◽  
Para Position ◽  
Phase Method ◽  
Antiinflammatory Effect ◽  
Solid Phase Method ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Two {Met(0)6}deacetyl-thymosin β4analogs containing Phe(4F) or Tyr(Me) at position 12 were synthesized by the manual solid-phase method, and their anti-inflammatory effect on carrageenin-induced edema in the mouse paw was studied. Fluorination of the para-position of Phe12resulted in a marked antiinflammatory effect on carrageenin-induced edema in the mouse paw compared with that of our synthetic {Met(0)6}deacetyl-thymosin β4, but the other analog, {Met(0)6, Tyr(Me)12}deacetyl-thymosin β4, showed a marked reduction of the anti-inflammatory effect.

scholarly journals Competitive Biological Activities of Chitosan and Its Derivatives: Antimicrobial, Antioxidant, Anticancer, and Anti-Inflammatory Activities

2018 ◽  
Vol 2018 ◽  
pp. 1-13 ◽  
Author(s):  
Suyeon Kim
Keyword(s):  
Water Solubility ◽  
Biological Activities ◽  
Biological Properties ◽  
Biomedical Science ◽  
Amino Groups ◽  
Chitosan Oligosaccharides ◽  
Primary Amino ◽  
Anti Inflammatory ◽  
Key Functional Groups ◽  
Application Fields

Chitosan is obtained from alkaline deacetylation of chitin, and acetamide groups are transformed into primary amino groups during the deacetylation. The diverse biological activities of chitosan and its derivatives are extensively studied that allows to widening the application fields in various sectors especially in biomedical science. The biological properties of chitosan are strongly depending on the solubility in water and other solvents. Deacetylation degree (DDA) and molecular weight (MW) are the most decisive parameters on the bioactivities since the primary amino groups are the key functional groups of chitosan where permits to interact with other molecules. Higher DDA and lower MW of chitosan and chitosan derivatives demonstrated higher antimicrobial, antioxidant, and anticancer capacities. Therefore, the chitosan oligosaccharides (COS) with a low polymerization degree are receiving a great attention in medical and pharmaceutical applications as they have higher water solubility and lower viscosity than chitosan. In this review articles, the antimicrobial, antioxidant, anticancer, anti-inflammatory activities of chitosan and its derivatives are highlighted. The influences of physicochemical parameters of chitosan like DDA and MW on bioactivities are also described.

Application of clay as a means of support to biomaterial with anti-inflammatory agents

2010 ◽  
Vol 1277 ◽  
Author(s):  
M.L. Domínguez-Patiño ◽  
M Chávez-Castillo ◽  
A. Rodríguez-Martínez ◽  
R.M. Melgoza Alemán ◽  
E Jiménez-Ferrer ◽  
...  
Keyword(s):  
Human Body ◽  
Current Trend ◽  
Dosage Forms ◽  
Native Plant ◽  
Plant Origin ◽  
Solid Dosage Forms ◽  
Organic Extract ◽  
Solid Dosage ◽  
Inflammatory Agent ◽  
Anti Inflammatory

In the last fifteen years, there have been significant changes in the production of medicines, mainly in the addition of new components to the formulation of solid dosage forms. The current trend of “back to nature” to lead to a healthier life has led those who are engaged in the pharmaceutical field to develop new formulations that allow the use of natural products of plant originFor example, excipient ingredients, used as carriers for a drug's active ingredients, are now being used. These are incorporated into a drug in order to facilitate the drug's preparation, maintenance, or administration. The excipient is beneficial to the patient because it allows the drug to be easily administered and absorbed by the human body [3]There is evidence that the clays have great potential for both absorption and adsorption due to its tiny particles. In addition, it has been reported that some clays have an effective antiseptic and healing ability [5–8]In the present work, a clay called bentonite was tested as a support vehicle of an inflammatory agent derived from a Mexican native plant called Distictis buccinatoria, commonly named “Tonacaxóchitl”. Studies carried out by Rojas et al. have shown that the organic extract of this plant has important antibacterial, antifungal, cytotoxic and anti-inflammatory properties [9]

scholarly journals Clinical-pharmacological aspects of the choice of phytocomponents for the regulation of the gastrointestinal function

2021 ◽  
pp. 158-163
Author(s):  
E. V. Shikh ◽  
S. M. Rykova ◽  
N. V. Shikh
Keyword(s):  
Water Solubility ◽  
Clinical Symptoms ◽  
Primary Tumour ◽  
Gastrointestinal Diseases ◽  
Gastric Glands ◽  
Flower Extract ◽  
Anti Inflammatory ◽  
Mechanisms Of Development ◽  
Chamomile Flower ◽  
Inflammatory Effect

The presentations of dyspepsia include a range of clinical symptoms, each of which has different mechanisms of development, and, therefore, requires different approaches to the correction. In this context, the combination preparations containing components of natural origin with polymodal action on the gastrointestinal tract deserve special attention. Combination of synergistic components: highly bioavailable curcumin and prebiotic fibers; artichoke leaf extract and chamomile flower extract provide simultaneous effects on three key digestive organs: stomach, pancreas and liver. Curcumin has an anti-inflammatory effect, helps to normalize acidity and restore microflora; epithelialization of ulcers; normalization of the gallbladder function; elimination of toxins. It inhibits the processes of primary tumour formation and prevents the development of metastatic processes in gastrointestinal cancer. Pharmaceutical technologies using cyclodextrin as an excipient increase curcumin’s water solubility, dispersibility and absorption, which has been confirmed in several comparative bioavailability studies in healthy volunteers. Chamomile flower extract has anti-inflammatory, antimicrobial, antispasmodic, antiulcer, wound healing and astringent effects. Chamomile is rich in slimy substances that envelop and protect the inflamed mucous membrane, including the stomach, from irritation with hydrochloric acid, bile components, food, and drugs. Mucous substances also have an anti-inflammatory effect and improve digestion. The artichoke facilitates the outflow of bile, affects the secretion of gastric glands, pancreas, increases the enzymatic activity of gastric juice, enhances intestinal motility during its atony, and has a hepatoprotective effect. As can be seen from the above, a combination of these synergistic components can be used in patients with chronic diseases, functional disorders as part of combination therapy, as well as for the prevention of gastrointestinal diseases in healthy people.

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.

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