metric ratio of 1:1, 2:1, 3:1, 4:1 and 8:1. Their pH ranged from 3.92 to 4.44 for 1:1 gels and from 2.36 to 2.84 for the 8:1 ratio. The addition of 5% polyvinylpyrrolidone K-90 increased the pH from 4.28 to 4.52 for 1:1 and from 2.58 to 3.30 for the 8:1 ratio. The addition of 5% polyvinylpyrrolidone K-90 increased the dynamic viscosity from 84 to 510 mPa.s for 1:1 gels and from 47 to 386 mPa.s for the 8:1 ratio. The gels obtained from powders possess the work of adhesion - the energy needed to separate the gel from the probe was 15.2 g/s for gels with 5% polyvinylpyrrolidone K-15, 52.76 g/s for gels with 5% polyvinylpyrrolidone K-30, and 56.6 g/s for gels containing 5% polyvinylpyrrolidone K-90. The results proved that it is possible to produce a preparation with optimal pharmaceutical and application properties.
pH of gels ranged from 3.92 to 4.44 for gels 1:1 and from 2.36 to 2.84 for 8:1 ratio. The addition of 20%, 23% or 25% poloxamer 407 increases the pH ranged from 4.00 to 4.91 for gels with 1:1 ratio and from 2.56 to 3.42 for 8:1 ratio. Rheological studies demonstrated that the investigated gels obtained from powders have the dynamic viscosity ranged from 53 mPa*s to 398 mPa*s for the 1:1 stoichiometric ratio in the complex and from 19 mPa*s to 242 mPa*s for 8:1 ratio. The addition of calcium alginate with polyoxyethylene glycol-200 reduces the pH and maintains high dynamic viscosity. The thermosensitive gels obtained from thermosensitive powders shows high adhesion and are difficult to separate from the probe.
The insufficient duration of the drug’s contact with the vaginal mucosa does not provide adequate pH, conditioning the physiological biocenosis of the organ. This effect is hampered by numerous anatomic and physiological conditions which do not facilitate prolonged contact of the drug with the application site. This study has shown the impact of the used excipients and the ratio of lactic acid to chitosan on pH, dynamic viscosity and adhesiveness of methylcellulose gels obtained from powders. The addition of sodium alginate and excipients to these complexes allows various formulations to be obtained over a wide range of pH. Rheological investigations revealed an increase in the dynamic viscosity of preparations containing lactic acid complexed with chitosan and sodium alginate in comparison to gels without sodium alginate. Studies of the work of adhesion showed the effect of glycerol, 1,2-propylene glycol and their concentrations on the value of the work of adhesion.
The troublesome symptoms of gastro-oesophageal reflux disease are a serious health, medical, and social problem for patients. The main problem is gastro-oesophageal acid reflux. In this study, I investigated hydrogels that could prevent the destruction of the oesophageal mucosa. I investigated the effect of chitosan and poloxamer 407 on the protective properties of gels. The addition of chitosan to all the tested gels increased their pH and dynamic viscosity. Preparations containing 25% poloxamer 407 showed the highest pH. Texture tests showed the effect of the poloxamer concentration on the adhesion performance of the tested gels. The findings suggest that the gels can be used to treat advanced acid reflux.
Continuing the implementation of research on the problem of treatment of vaginal pH disorders, intravaginal globules were examined as vaginal drug form which carries the lactic acid complexes with chitosan. The intravaginal application of globules that transform into gel under natural conditions is aimed at achieving the physiological pH of the vaginal environment. Formulations were prepared with varying pH and rheological properties. The test showed the work of adhesion of gels. All gels with ratios of 1:1 and 2:1 of lactic acid to chitosan showed a pH in the physiological range at 37°C. Additional hydroxypropylmethylcellulose and excipients allows various formulations with a wide range of pH to be obtained. Rheological investigation revealed an increase in the dynamic viscosity of preparations containing lactic acid complexed with chitosan and hydroxypropylmethylcellulose in comparison to the gels without hydroxypropylmethylcellulose. The study of the work of adhesion showed the effect of hydroxypropylmethylcellulose and their concentration on the value of the work of adhesion.
Thermosensitive hydrophilic powders passing in gels containing lactic acid complexed with chitosan at a stoichiometric ratio 1:1 and 8:1 reveal pH ranged from 4.00 to 4.91 and 2.56 to 3.42. Rheological studies demonstrated that the investigated thermosensitive gels obtained from powders have the dynamic viscosity in the ranged from 269 mPa*s to 579 mPa*s for the 1:1 stoichiometric ratio and in the range from 220 mPa*s to 530 mPa*s for 8:1 ratio. As a result of the research preparations with different pH values including the physiological range were obtained. The thermosensitive gels obtained from the thermosensitive powders were characterized by the specific dynamic viscosity. The results proved that it is possible to produce a preparation with optimal pharmaceutical and application properties.
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Opracowano nowy sposób otrzymywania kluczowego półproduktu do syntezy substancji oftalmicznej nepafenak. Zgodnie z procedurą 2-amino-3-benzoilo-α-(metylotio)fenyloacetamid (5A) uzyskano w wyniku przegrupowania [2,3]-sigmatropowego Gassmana, w reakcji 2-aminobenzofenonu (1A) z 2-(metylotio)acetamidem (2), wobec dotychczas nieopisanych w literaturze czynników chlorujących, takich jak N-chloroftalimid (3) i 1,3-dichloro-5,5-dimetylohydantoina (4). Nowa metoda charakteryzuje się efektywnością, dogodnymi warunkami prowadzenia reakcji oraz wysoką czystością otrzymywanego półproduktu.
EN
Known synthesis of 2-amino-3-benzoyl-α-(methylthio)phenylacetamide (nepafenac intermediate) was improved by using N-chlorophthalimide or 1,3-dichloro-5,5-dimethylhydantoin as chlorination reagents. The product showed a purity of above 98%.
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W artykule przedstawiono wydajną metodę syntezy cyklezonidu z wykorzystaniem dezonidu jako substancji wyjściowej. Proces acylowania dezonidu za pomocą bezwodnika izomasłowego, do izobutyrylodezonidu zachodzi w temperaturze pokojowej w środowisku pirydyny. Powstały produkt z procesie transketalizacji z użyciem cykloheksanokarbaldehydu tworzy mieszaninę izomerów R/S-cyklezonidu, który bez wydzielania, pod wpływem kwasu nadchlorowego ulega przemianie do cyklezonidu o czystości powyżej 99,85%.
EN
An efficient method of ciclesonide synthesis using dezonide as the starting material is presented in the paper. Acylation of desonide to isobutyryldesonide with isobutyric anhydride occurs at room temperature in pyridine. The product subjected to transketalization reaction with cyclohexanecarbaldehyde yields a mixture of R/S-ciclesonide isomers, which without separation, in the presence of perchloric acid, undergo transformation to ciclesonide of over 99,85% purity.
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