Water-soluble Base Research Articles

Efficient Synthesis of Quinazolinones by Transition-Metal-Free Direct Aerobic Oxidative Cascade Annulation of Alcohols with o-Aminoarylnitriles.

A mild and atom-economic method was developed for direct and efficient synthesis of quinazolinones through a transition-metal-free aerobic oxidative cascade annulation reaction of widely available o-aminoarylnitriles and alcohols. Air could be employed as an effective oxidant under mild conditions, generating water as the only byproduct. Possibly owing to the "cesium effect", the water-soluble base CsOH was found to be crucial in all key steps of the reaction mechanism. Because a wide range of substrates can be used to prepare substituted quinazolinones without contamination by transition-metal residues, this method may be of interest for application in pharmaceutical synthesis. Possible reaction paths were also proposed according to control reactions.

Pengaruh konsentrasi air dalam formula salep minyak cengkeh (syzigium aromaticum)

Abstract
 
 The clove flower essential oil (Syzygium aromaticum) with the active compound eugenol has been widely investigated and is known to be efficacious as an anti-inflammatory agent, and further research on its formulation continues. The formula developed in this study was a topical ointment dosage form using a water soluble base (oleic acid enhancer and propylene glycol). This study aims to determine the physical and irritant properties of the clove flower essential oil ointment (MABC) if a hydrocarbon base is used. The ointment is made by the smelting method with a concentration of 5% (F1), 10% (FII) and 15% (FIII). The ointments of the three formulas were then evaluated for their physical properties, including dispersion, adhesion and pH. The results of statistical tests with the LSD test showed that there were significant differences between formulas. The higher the concentration of MABC, the greater the spread (p0.05). The results of the Simplex Lattice Design irritation test also show that water-soluble base ointment with a concentration of 5%, 10% and 15% MABC does not cause an irritating effect.
 
 Keywords: Syzygium aromaticum, base of water soluble ointment, anti-inflammatory.

Optimasi sediaan salep minyak cengkeh (syzigium aromaticum) dalam basis larut air

Abstract
 
 The clove flower essential oil (Syzygium aromaticum) with the active compound eugenol has been widely investigated and is known to be efficacious as an anti-inflammatory agent, and further research on its formulation continues. The formula developed in this study was a topical ointment dosage form using a water soluble base (oleic acid enhancer and propylene glycol). This study aims to determine the physical and irritant properties of the clove flower essential oil ointment (MABC) if a hydrocarbon base is used. The ointment is made by the smelting method with a concentration of 5% (F1), 10% (FII) and 15% (FIII). The ointments of the three formulas were then evaluated for their physical properties, including dispersion, adhesion and pH. The results of statistical tests with the LSD test showed that there were significant differences between formulas. The higher the concentration of MABC, the greater the spread (p0.05). The results of the Simplex Lattice Design irritation test also show that water-soluble base ointment with a concentration of 5%, 10% and 15% MABC does not cause an irritating effect.
 
 Keywords: Syzygium aromaticum, base of water soluble ointment, anti-inflammatory.

EVALUASI SIFAT FISIK SEDIAAN SALEP MINYAK CENGKEH (SYZIGIUM AROMATICUM) DALAM BASIS LARUT AIR


 The clove flower essential oil (Syzygium aromaticum) with the active compound eugenol has been widely investigated and is known to be efficacious as an anti-inflammatory agent, and further research on its formulation continues. The formula developed in this study was a topical ointment dosage form using a water soluble base (oleic acid enhancer and propylene glycol). This study aims to determine the physical and irritant properties of the clove flower essential oil ointment (MABC) if a hydrocarbon base is used. The ointment is made by the smelting method with a concentration of 5% (F1), 10% (FII) and 15% (FIII). The ointments of the three formulas were then evaluated for their physical properties, including dispersion, adhesion and pH. The results of statistical tests with the LSD test showed that there were significant differences between formulas. The higher the concentration of MABC, the greater the spread (p0.05). The results of the Simplex Lattice Design irritation test also show that water-soluble base ointment with a concentration of 5%, 10% and 15% MABC does not cause an irritating effect.
 
 Keywords: Syzygium aromaticum, base of water soluble ointment, anti-inflammatory.

Formulation and evaluation of Neem (Azadirachta indica A. Juss) seed oil suppositories

Background: Neem seed is very vital because of its rich lipid content and bitter constituents. Aims: This study was designed to provide a scientific rationale for the preparation and use of Neem seed oil as suppositories using dika fat (DF), and macrogol (MG), as bases. Materials and Methods: The suppositories which were prepared by fusion method using a pre-calibrated mould, were characterized using parameters like appearance, crushing strength, weight variation, melting point, pH, liquefaction time and in-vitro release according to standard procedures. Results: Results show that, the suppository strengths were in the order; bland, MG (25.00 ± 1.50N) > DF (12.90 ± 0.72 N), while those containing medicaments were NSM1 (20.00 ± 1.92) > NSD1 (12.90 ± 0.94) > NSM2 (12.70 ± 1.24 N) > NSD2 (10.00 ± 1.35 N). The pH of medicated formulations were NSM1 (6.50 ± 0.01), NSM2 (6.54 ± 0.03) > NSD1 (5.73 ± 0.04) and NSD2 (5.07 ± 0.03). Melting point values show that, macrogol base had mean values of 36.80 °C ± 0.62 and 36.40 °C ± 0.46 for NSM1 and NSM2 respectively, whereas, those with DF gave an average melting point values of 32.10 °C ± 0.87 and 30.90 °C ± 0.79 for NSD1 and NSD2 respectively. Conclusion: Results obtained showed that suppositories prepared with Macrogol (MG) base exhibited better physicochemical properties than Dika fat (DF) base suppositories, therefore water soluble bases may be bases of choice in the delivery of neem seed oil.

Uji Daya Hambat Formulasi Salep Ekstrak Etanol Umbi Hati Tanah (Angiopteris sp) terhadap Bakteri Staphylococcus aureus

Hati Tanah tuber (Angiopteris sp) is a plant part that is often used by Dayak tribes in Central Kalimantan as a medicine to heal wounds. This plant is known to contain flavonoid, saponin, tannin and catechol compounds which in previous studies have proven that ethanol extract of this plant can inhibit the growth of Staphylococcus aureus bacteria. Staphylococcus aureus is a Gram-positive bacterium that causes infection in wounds. Some of these strains of bacteria are resistant to available antibiotics. In this study two bases of ointment were used, namely, the bottom of the hydrocarbon ointment and the base of the water-soluble lotion. This study aims to determine the ointment formulation which can inhibit the growth of S. aureus bacteria. Plant extraction is done by the soxhletation method. The inhibitory test in this study uses a process of planting discs that contain active substances as the primary test material. The results showed that the base ointment formulation which could inhibit the growth of Staphylococcus aureus bacteria was an ointment formulation with a water-soluble base.

Bioinspired co-crystals of Imatinib providing enhanced kinetic solubility

Realizing the full potential of co-crystals enhanced kinetic solubility demands a comprehensive understanding of the mechanisms of dissolution, phase conversion, nucleation and crystal growth, and of the complex interplay between the active pharmaceutical ingredient (API), the coformer and co-existing forms in aqueous media. One blueprint provided by nature to keep poorly water-soluble bases in solution is the complexation with phenolic acids. Consequently, we followed a bioinspired strategy for the engineering of co-crystals of a poorly water-soluble molecule – Imatinib – with a phenolic acid, syringic acid (SYA). The dynamics of dissolution and solution-mediated phase transformations were monitored by Nuclear Magnetic Resonance (NMR) spectroscopy, providing mechanistic insights into the 60 fold-increased long lasting concentrations achieved by the syringate co-crystals as compared to Imatinib base and Imatinib mesylate. This lasting effect was linked to SYA’s ability to delay the formation and nucleation of Imatinib hydrate – the thermodynamically stable form in aqueous media – through a metastable association of SYA with Imatinib in solution. Results from permeability studies evidenced that SYA did not impact Imatinib’s permeability across membranes while suggesting improved bioavailability through higher kinetic solubility at the biological barriers. These results reflect that some degree of hydrophobicity of the coformer might be key to extend the kinetic solubility of co-crystals with hydrophobic APIs. Understanding how kinetic supersaturation can be shaped by the selection of an interactive coformer may help achieving the needed performance of new forms of poorly water-soluble, slowly dissolving APIs.

Preparation and characterization of intravaginal vardenafil suppositories targeting a complementary treatment to boost in vitro fertilization process

Vaginal route has been recently considered as a potential route for systemic delivery of drugs with poor oral bioavailability. Vardenafil (VDF) is a relatively new phosphodiesterase-5 inhibitor that exhibits a limited oral bioavailability (≈15%) due to extensive first-pass metabolism. In this study, we attempted to enhance the systemic bioavailability of VDF via its formulation within vaginal suppositories. Witepsol H15 and Suppocire NA50 were adopted as lipophilic suppository bases while polyethylene glycol 4000/400 and glycerogelatin were used as hydrophilic suppository bases. The effect of different base types and/or the incorporation of bioadhesive polymer on in vitro release of VDF were evaluated. The in vivo fate and organ biodistribution of VDF following intravaginal (IVG) administration were also investigated. VDF release from water-soluble bases was higher than that from lipophilic bases. The incorporation of bioadhesive polymers, such as Na alginate, remarkably sustained drug release from suppository base. The organ biodistribution study showed a higher Cmax (32 times) and AUC0–4h (20 times) of VDF in uterus following IVG administration of conventional suppositories, compared to oral administration of VDF suspension. In addition, cyclic guanosine monophosphate (cGMP) serum levels, used as an indicator of the in vivo activity of VDF, in animals were higher following IVG administration rather than oral administration. This study suggests that IVG administration of VDF might represent a potential alternative to oral route with superior therapeutic benefits especially when targeting the uterus.

Identification of the significant factors determining extractability of Ni and Cu after sulfation roasting of a PGM-bearing chromitite ore

Selective sulfation-roast-water leach process of a complex, chromite-rich Cu-Ni-PGM ore to dissolve water-soluble base metal sulfates contained therein was investigated as an alternative process to remove base metals prior to the extraction of precious metals. Ground run-of-mine ore (P80<75μm) was mixed with concentrated H2SO4 (sulfating agent) and Na2SO4 (dual catalyst and sulfating agent) to intensify atmospheric sulfation roast reaction in an unvented electric furnace (static roast under reducing conditions). The acquired calcine was water leached to extract the Ni and Cu sulfates. The roasting conditions were optimized using a Response Surface Methodology which included a Desirability Function Approach in order to maximize Cu and Ni extraction whilst limiting reagent consumption and suppressing Fe and Cr co-dissolution.It was possible to decompose the chromatic-ferritic structure and produce water-soluble metal species by roasting the ore containing 12.80g/t Pt, 15.20g/t Pd, 0.0646% Cu, 0.31% Ni, 13.60% Fe and 10.40% Cr. Approximately 90% Ni and 77% Cu were recovered after roasting at 550°C in closed atmosphere for 2h with 462kg/t H2SO4, 76.9kg/t Na2SO4 and by leaching at 80°C with 2wt% solid density for 24h. The raw ore, roasted mass and water-leach residue were characterized by fire assay and Tescan Integrated Mineral Analysis (TIMA GM Model). Pt+Pd grade has been upgraded from 28(raw ore) to 32.38g/t (water-leach residue).

Dynamics of water-soluble base cations in a forest soil measured by an in situ combined IER method

Dynamics of water-soluble base cations in a forest soil measured by an in situ combined IER method

The Release of Diazepam from Different Conventional and Hollow Type Suppository Bases

The objective of this study was to investigate the release profile of different fat and water soluble bases using diazepam as a model drug , and then to develop a satisfactory formula with a rapid release of diazepam from suppository bases .The study was conducted using theobroma oil ,glycerol-gelatin and glycerol-PEG1540 bases using conventional mold method for preparation .while the later base was utilized to incorporate diazepam ( buffered solution ) in a hollow type suppositories. The results indicated that all types of bases can be utilized to formulate diazepam as rectal suppositories with acceptable disintegration time ( 12, 10, 6, and 6min.), respectively . While 100% of the released drug had been shown different release profiles with different storage time ( 15, 30, and 45 days ) in a refrigerator at 5°C , best results were obtained , when glycerol- PEG1540 used as a base for both conventional and hollow type mold methods .However , a decrease in the release rate of the drug was seen with glycerol-gelatin and glycerol-PEG1540 and to a lesser extent for glycerol-PEG1540 prepared&#x0D; by hollow type method .&#x0D; Key words: Diazepam , Hollow type suppository

Antibacterial Poly-Herbal Semisolid Formulations Containing Leaves Extracts of Tectona grandis, Mangifera indica and Anacardium occidentale

Herbal medicine have become an item of global importance both has medicinal and economical value. Plants used for medicinal purposes long before recorded history. Many plant species have been proved to have antibacterial activity. Thus, the main objective of the study was to formulate and evaluate a poly-herbal semisolid dosage forms using ethanolic extracts of frontal leaves of T. grandis, M. indica and A. occidentale. Formulations were evaluated for its physicochemical properties like color, consistency, pH, spreadability, extrudability and the results were found satisfactory. Antibacterial activity of formulations was studied against S. aureus, E. coli and P. aeruginosa by agar well diffusion method. (E. coli, P. aeruginosa) bacteria. The order of activity was as follows: Water Soluble bases &gt; Gel Bases &gt; Hydrocarbon Bases. The zones of inhibition of poly herbal formulations were in between 23-28 mm which can be comparable with standard formulation 24-29 mm. Activity of the formulations may be due to the presence of alkaloids, flavanoids, phenols and tannins in the extracts. The formulations were found to be very efficacious in all the parameters.

Formulation, evaluation and release studies of Indomethacin Suppositories

Indomethacin suppositories were prepared by using water soluble bases. All the prepared suppositories were evaluated for various physical parameters like weight variation, hardness, Liquefaction time. In-vitro release study was performed USP type I apparatus (Basket type) using phosphate buffer pH 7.4 as dissolution media. The suppositories prepared were within permissible range of all physical parameters.

Stability of Xuesaitong capsules in gastrointestinal lavage fluid

ObjectiveTo obtain a formulation with high bioavailability through evaluation of the stability of three types of Xuesaitong capsules in the stomachs and intestines of rats. We compared the stability of the Panax notoginsenoside R1 as well as the ginsenosides Rg1, Rb1, Re, and Rd in different formulations. MethodsArtificial stomach fluid (ASF) and artificial intestinal fluid (AIF) were prepared. Stability of three types of Xuesaitong capsules was examined for 4 h in stomachs and 24 h in intestines. Samples were analyzed at different times by high-performance liquid chromatography. Percent content of NGR1, GRg1, GRb1, GRe, and GRd at different times was calculated. ResultsHard capsules incubated in ASF disintegrated within 2–3 min, whereas soft capsules disintegrated within 7–8 min. Components in hard capsules were dissolved rapidly in water, with content of each compound reaching 90% in 5 min, and degradation of each compound reaching 30–50% after incubation for 240 min. Dissolution and degradation of each component in soft capsules with a water-soluble base tended to balance at 30–90 min. Contents in soft capsules with a lipid-soluble base showed slow dissolution after ASF incubation for 120 min. Five saponins in identical types of capsules incubated in ASF had similar stability curves. Contents of hard capsules and soft capsules with a water-soluble base degraded rapidly within 30 min and reached a plateau when Xuesaitong capsules were incubated in AIF. ConclusionsContents of capsules with a lipid-soluble base degraded slower than the other two types of capsules incubated in ASF and AIF, suggesting that they may have better bioavailability.

Kinetics of drug release from ointments: Role of transient-boundary layer

In the current work, an in vitro release testing method suitable for ointment formulations was developed using acyclovir as a model drug. Release studies were carried out using enhancer cells on acyclovir ointments prepared with oleaginous, absorption, and water-soluble bases. Kinetics and mechanism of drug release was found to be highly dependent on the type of ointment bases. In oleaginous bases, drug release followed a unique logarithmic-time dependent profile; in both absorption and water-soluble bases, drug release exhibited linearity with respect to square root of time (Higuchi model) albeit differences in the overall release profile. To help understand the underlying cause of logarithmic-time dependency of drug release, a novel transient-boundary hypothesis was proposed, verified, and compared to Higuchi theory. Furthermore, impact of drug solubility (under various pH conditions) and temperature on drug release were assessed. Additionally, conditions under which deviations from logarithmic-time drug release kinetics occur were determined using in situ UV fiber-optics. Overall, the results suggest that for oleaginous ointments containing dispersed drug particles, kinetics and mechanism of drug release is controlled by expansion of transient boundary layer, and drug release increases linearly with respect to logarithmic time.

Synthesis of novel Schiff base metal complexes with reactive groups and their catalytic property for hydrogen peroxide decomposition

A novel water soluble azo Schiff base ligand containing crosslinking reactive groups (A), 3,5-bis [(2-hydroxy-4′-sodiumsulphatoethylsulphonyl) azobenzene- methyneimino]-benzoic acid (BHSABA), and its complexes with Mn2+, Cu2+, Co2+, were synthesized and characterized by elemental analysis, Fourier transform infrared (FT-IR) and proton nuclear magnetic resonance (1HNMR) spectroscopy. The Schiff base ligand and its complexes had excellent water solubility. Two reactive groups, p-[(2′-sulphatoethyl) sulphonyl groups, were able to form covalent bonds with biomass, such as cellulose, chitosan and so on, to obtain functional material. Ultraviolet–visible (UV-vis) electronic absorbance and fluorescence spectra of the ligand having azo conjugated system and of the metal complexes were measured. The catalytic activity of the ligand and the complexes for H2O2 decomposition were also investigated. The results show that the fluorescence spectra of the complexes, Co2A and Mn2A, had increased fluorescence phenomena. They had strong catalytic activity for H2O2 decomposition. When the concentration of manganese complex, Mn2A, was 5 mg/l, H2O2 decomposition nearly finished in 40 min at 40℃. The order of catalytic activity of three complexes for H2O2 decomposition was Mn2A &gt; Co2A &gt; Cu2A. The ligand itself had no noticeable catalytic activity for H2O2 decomposition. These novel water soluble Schiff base metal complexes with reactive groups have potential application in the H2O2 decomposition of water treatment fields.

EVALUASI SIFAT FISIK DAN UJI IRITASI SEDIAAN SALEP MINYAK ATSIRI BUNGA CENGKEH DALAM BASIS LARUT AIR

Essential oil of clove (Syzygium aromaticum) (MABC) with eugenol as its main active ingredient, has been studied as anti-inflammatory agent. Its important to develop formulation in an advanced research. This study has been conducted to develop a topical dosage form (an ointment using a water-soluble base). The physical properties of water-soluble ointment preparation of MABC and the irritation properties at various concentrations of MABC have been evaluated. Ointment preparation MABC water-soluble base created using the mixing of the PEG 400 and PEG 4000 by a fusion method. Ointment made with a various concentration of MABC (5%, 10% and 15%). Ointment with each concentration were evaluated based on its physical properties such as pH, dispersiveness and adhesion. Ointment also tested its irritative properties on the skin, using test animals guinea pigs by Draize test method. Data from those experiments analyzed by ANOVA with T-test level of 95%. The results showed that the physical properties of water-soluble ointment base with MABC concentration of 5%, 10% and 15% reach the requirements of the pH and adhesion parameter, but not for its dispersiveness. Statistical analysis of each trial did not show any significant in difference. The experimental results against irritation test showed that the water-soluble ointment base concentration of 5%, 10% and 15% did not cause irritation to the skin of guinea pigs. Â

Pharmacokinetics and anti-hypertensive effect of metoprolol tartrate rectal delivery system

The main aim of this work was to develop rectal suppositories for better delivery of metoprolol tartrate (MT). The various bases used were fatty, water soluble and emulsion bases. The physical properties of the prepared suppositories were characterized such as weight variation, hardness, disintegration time, melting range and the drug content uniformity. The in vitro release of MT from the prepared suppositories was carried out. The evaluation of the pharmacological effects of MT on the blood pressure and heart rate of the healthy rabbits after the rectal administration compared to the oral tablets was studied. Moreover, the formulation with the highest in vitro release and the highest pharmacological effects would be selected for a further pharmacokinetics study compared to the oral tablets. The results revealed that the emulsion bases gave the highest rate of the drug release than the other bases used. The reduction effect of the emulsion MT suppository base on the blood pressure and heart rate was found to be faster and greater than that administered orally. The selected emulsion suppository base (F11) showed a significant increase in the AUC (1.88-fold) in rabbits as compared to the oral tablets. From the above results we can conclude that rectal route can serve as an efficient alternative route to the oral one for systemic delivery of MT which may be due to the avoidance of first-pass effect in the liver.

Study of Fluconazole Release from O/W Cream and Water Soluble Ointment Bases

Study of Fluconazole Release from O/W Cream and Water Soluble Ointment Bases

Soil Depletion of Ca, Mg and K Due to Vicinal Intensive Hog Farming Operation Located in East Mediterranean

One of the main environmental impacts of concentrated animal feeding operations is soil degradation in the vicinity of the livestock breeding facilities due to substances such as ammonia emitted from the various stages of the process. In this research, the soil degradation effects of an intensive hog farming operation (IHFO) located at a Mediterranean limestone soil coastal area have been investigated. Soil samples of the upper mineral soil were taken in various distances and directions from the IHFO boundaries. Thirteen experimental cycles were carried out in the duration of 1.5 years starting in March 2009 until October 2010. The soil samples were analysed on total, exchangeable and water-soluble Ca, Mg and K as well as water-soluble ammonium concentrations. Significantly lower concentrations of the exchangeable and water-soluble base cations were observed on soil samples at increasing proximity downwind from the farm (south). Southern soil average concentrations of exchangeable base cations ranged between 78.6 and 128.52 mmol Ca2+ kg−1 soil, 8.42–21.39 mmol Mg2+ kg−1 soil and 4.25–8.1 mmol K+ kg−1 soil, respectively. Southern soil average concentrations of water-soluble base cations ranged between 0.57 and 2.17 mmol Ca2+ kg−1 soil, 0.16–0.89 mmol Mg2+ kg−1 soil and 0.48–0.95 mmol K+ kg−1 soil, respectively.