2, 3, 4 (trisübstitüe benzaldehit)-N-(6, 7 sübstitüe-1,3-benzotiyazol-2-il) semikarbazon [2.026a-o] dan hareketle yeni bir seri azetidinon (AZ1-6) türevi hazırlanmıştır. Sentezlenen bileşiklerin yapıları elemental analiz, IR ve 1H NMR verileriyle kanıtlanmış ve antibakteriyel aktiviteleri denenmiştir. Bileşiklerden AZ2, AZ3, AZ5 ve AZ6 Bacillus subtilis ve Pseudomona’a karşı referans bileşikler Prokain penisilin ve Streptomisin ile kıyaslandıklarında kayda değer aktiviteye sahip bulunmuştur.

A novel series of azetidinone AZ1-6 been prepared from the building blocks 2, 3, 4 (trisubstituted benzaldehyde)-N-(6,7 substituted-1,3-benzothiazol-2-yl) semicarbazone [2.026a-o]. All of the synthesized compounds have been confirmed by elemental analyses, IR and 1H NMR spectral data. These newly synthesized compounds were screened for their antibacterial activity. Variable and modest activity was observed against the investigated strains of bacteria, however compounds AZ2, AZ3, AZ5 and AZ6 revealed significant antibacterial activity against Bacillus subtilis and Pseudomonas compared to the reference drug Procaine penicillin and Streptomycin.

Ballota türleri Türkiye’de halk arasında yara ve yanıkların tedavisinde, öksürüğe karşı ve üst solunum yolu enfeksiyonlarında kullanılmaktadır. Daha önce yapılan fitokimyasal çalışmalarda Ballota türlerinden terpenoit, flavonoit, fenil propanoit, uçucu yağ, tanen ve saponozit yapısında bileşikler izole edilmiştir. Bu çalışmanın amacı, Ballota türlerinin içerdiği toplam orto-dihidroksisinnamik asit türevlerini (TSİ) ve toplam flavonoit (TFİ) içeriklerini Avrupa Farmakopesine göre spektrofotometrik olarak değerlendirmektir. Bu çalışmanın sonuçları Ballota türlerinin değişik miktarlarda fenolik içeriğe sahip olduğunu göstermiştir. Ballota nigra subsp. anatolica orto-dihidroksisinnamik asit türevi bileşikleri en yüksek oranda taşırken, Ballota glandulosissima flavonoitleri en yüksek oranda taşımaktadır. Diğer taraftan, Ballota nigra subsp. foetida orto-dihidroksisinnamik asit türevleri en düşük oranda taşırken, Ballota rotundifolia flavonoitleri en düşük oranda taşımaktadır.

Ballota species have been used in Turkish folk medicine for treatment of wounds and burns, suppression cough and upper respiratory inflammation. According to the previous phytochemical investigations terpenoids, flavonoids, phenylpropanoids, essential oils, tannins, and saponins were isolated from Ballota species. The aim of the present research is to evaluate total ortho-dihydroxycinnamic acid derivatives (TCC) and total flavonoid content (TFC) of Ballota species by spectrophotometrically according to European Pharmacopoeia. The results of this study show that; Ballota species have distinct phenolic contents. Ballota nigra subsp. anatolica extract contained the highest amount of ortho-dihydroxycinnamic acid derivatives, while highest proportion of flavonoids was found in Ballota glandulosissima. On the other hand, Ballota nigra subsp. foetida extract contained the lowest amount of ortho-dihydroxycinnamic acid derivatives, while lowest proportion of flavonoids was found in Ballota rotundifolia.

The aim of this present study is to develop micro-beads for controlled release of Metoprolol succinate (MS). Different combinations of alginate and poloxamer 407 (PL) were taken to prepare beads by employing ionotropic gelation method, where CaCl2 used as gelling agent. FTIR technique was used to study the drug and polymers interaction. The prepared beads were evaluated for drug loading, entrapment efficiency, particle size and morphology, in vitro drug release and drug release kinetics. There were no shift in the major peaks of the pure drug was observed from the FTIR spectra, which indicates the absence of interaction between drug and polymers. The highest drug loading and entrapment efficiency were found to be 3.11 % and 35.67 %, respectively for the formulation FB1. The particle size was measured by sieving method and it was found that the particles were in the micron range for all the formulations. The morphology of the formulation FB4 was studied by SEM and the image showed irregular surface. The in vitro drug release study was carried out in pH 6.8 phosphate buffer for 12 hr at 37ºC and the results demonstrate cumulative percentage of drug release was decreased with the increase in PL ratio in the composition that indicates controlled drug release. To know the mechanism of drug release the in vitro drug release data were fitted to zero order, first order, Higuchi and Korsmeyer-Peppas equation. The formulation FB4 showed highest correlation coefficient (r2) of 0.97 for Higuchi equation due to which it was selected as best formulation. The release exponent (n) of all the formulation were below 0.45 except FB4 (0.48) demonstrating Fickian diffusion is the drug release mechanism, whereas the formulation FB4 indicated non-Fickian diffusion i.e. diffusion and erosion were the mechanism.

The aim of this present study is to develop micro-beads for controlled release of Metoprolol succinate (MS). Different combinations of alginate and poloxamer 407 (PL) were taken to prepare beads by employing ionotropic gelation method, where CaCl2 used as gelling agent. FTIR technique was used to study the drug and polymers interaction. The prepared beads were evaluated for drug loading, entrapment efficiency, particle size and morphology, in vitro drug release and drug release kinetics. There were no shift in the major peaks of the pure drug was observed from the FTIR spectra, which indicates the absence of interaction between drug and polymers. The highest drug loading and entrapment efficiency were found to be 3.11 % and 35.67 %, respectively for the formulation FB1. The particle size was measured by sieving method and it was found that the particles were in the micron range for all the formulations. The morphology of the formulation FB4 was studied by SEM and the image showed irregular surface. The in vitro drug release study was carried out in pH 6.8 phosphate buffer for 12 hr at 37ºC and the results demonstrate cumulative percentage of drug release was decreased with the increase in PL ratio in the composition that indicates controlled drug release. To know the mechanism of drug release the in vitro drug release data were fitted to zero order, first order, Higuchi and Korsmeyer-Peppas equation. The formulation FB4 showed highest correlation coefficient (r2) of 0.97 for Higuchi equation due to which it was selected as best formulation. The release exponent (n) of all the formulation were below 0.45 except FB4 (0.48) demonstrating Fickian diffusion is the drug release mechanism, whereas the formulation FB4 indicated non-Fickian diffusion i.e. diffusion and erosion were the mechanism.

Galaktomannanlar (GM), bazı baklagillerin tohumlarında doğal olarak bulunan nötral nontoksik polisakkaritlerin bir grubu olup, tekstil, farmasötik, biyomedikal, kozmetik ve gıda endüstrisinde kullanılırlar. Bugüne kadar HPTLC ile polisakkaritlerin şeker kompozisyonunu belirlemeye yönelik herhangi bir çalışma bildirilmemiştir ve bu çalışma ile bu amaçlanmıştır. Caesalpinia pulcherrima L.’nin (CP) tohumlarından galaktomannanlar alkol kullanılarak çöktürme yöntemi ile izole edilmiş ve saflaştırılmıştır. C. pulcherrima’nın galaktomannnanlarından izole edilen galaktoz, mannoz, ksiloz ve glukoz gibi monosakkaritlerin analizi için basit, duyarlı, seçici, kesin ve güçlü olan yeni bir HPTLC metodu geliştirilmiş ve valide edilmiştir. Kromatogramlar silikajel GF aluminyum TLC plak üzerinde mobil faz olarak aseton: su (9: 1 v/v) kullanılarak develope edilmiştir ve UV spektrofotometresi ile 254 nm’de miktarı belirlenmiştir. Mannoz, galaktoz, ksiloz ve glukoz için Rf değerleri sırası ile 0.45, 0.34, 0.40 ve 0.60 bulunmuştur. Yöntemin doğrusallığı yukarıda bahsedilen tüm monosakkaridler için 2.000-10.000 ng/spot konsantrasyon aralığında bulunmuştur.
Mannoz, galaktoz, ksiloz ve glukoz için tespit edildiği limit değerler sırasıyla 0.14986 ng/spot, 0.31973 ng/spot, 0.27569 ng/spot ve 0.36808 ng/spot olarak bulunmuştur. Mannoz, galaktoz, ksiloz ve glukoz için tayin limiti sırasıyla 1.498 ng/spot, 3.197 ng/spot, 2.756 ng/spot ve 3.680 ng/spot olarak bulunmuştur. Metod aynı zamanda kesinlik, spesifiklik ve geri kazanım için valide edilmiştir. Geliştirilen bu metod C. pulcherrima’nın galaktomannanlarına ait monosakkaridlerin bileşimini analiz etmek için kullanılmıştır.

Galactomannans (GM), a group of neutral nontoxic polysaccharides naturally occurring in the seeds of some legumes, are used in the textile, pharmaceutical, biomedical, cosmetics and food industries. As to date there are no documented reports on determination of the sugar composition in polysaccharides by HPTLC and the following study is an attempt in this direction. GM from seeds of Caesalpinia pulcherrima L. (CP) was isolated and purified by precipitation method using alcohol. A new, simple, sensitive, selective, precise, and robust HPTLC method for analysis of monosaccharides such as galactose, mannose, xylose and glucose in isolated CP GM has been developed and validated. Chromatograms were developed using a mobile phase of acetone: water (9: 1 v/v) on pre-coated plate of silica gel GF aluminium TLC plate and quantified by UV spectrophotometer at 254nm. The Rf values were 0.45, 0.34, 0.40 and 0.60 for mannose, galactose, xylose and glucose, respectively. The linearity of method was found to be within the concentration range of 2000-10000 ng/spot for all above monosaccharides. The limit of detection for mannose, galactose, xylose and glucose was found to be 0.14986 ng/spot, 0.31973 ng/spot, 0.27569 ng/spot, and 0.36808 ng/spot, respectively. The limit of quantification for mannose, galactose, xylose and glucose was found to be 1.498 ng/spot, 3.197 ng/spot, 2.756 ng/spot, and 3.680 ng/spot, respectively. The method was also validated for precision, specificity and recovery. This developed method was used to analyze CP GM for monosaccharides compositions.