S u m m a r yIntroduction: The general Hildebrand-Scatchard theory of solubility supplemented by Fedors' solubility parameter -δ 1 2 = Σ Σ E V i i / was used to estimate the real solubility by -log x 2 (log of the mole fraction) of phytochemicals contained in Ext. Taraxaci e radix cum herba aqu. siccum. Surface activity of aqueous solution of extracts was determined and quantified -solubilizing capabilities of solutions of c exp. ≥cmc in relation to cholesterol particle size of Ø=1.00 mm, as well as of ketoprofen were defined. Objective: The calculated value -log x 2 collated with the polarity of extraction medium ε M allows to estimate the optimal solubility of phytochemicals that determine the viscosity of the aqueous extract of dandelion and above all its surface activity and the ability to solubilize lipophilic therapeutic agents (ketoprofen). Methods: Viscosity of water model solutions of dandelion extracts and exhibition solutions after the effective micellar solubilization of cholesterol and ketoprofen was measured using Ubbelohde viscometer in accordance with the Polish Standard. The surface tension of aqueous solutions of extract and exhibition solutions after solubilization of cholesterol and ketoprofen was measured according to the Polish Standard with stalagmometric method. Results: The calculated factual solubility, and mainly the determined and calculated hydrodynamic size mean, that despite the complex structure of the micelle, it solubilizes cholesterol (granulometric grain of diameter Ø=1.00 mm) and ketoprofen (state of technological fragmentation) in equilibrium conditions. Equilibrium solubilization of ketoprofen also occurs in an environment of model gastric juice (0.1 mol HCl). Conclusions: The obtained results indicate that after the administration (and/or dietary supplementation) with Ext. Taraxaci e radix cum herba aqu. siccum, the physiological parameters of gastric juice would not be measured and its presence (phytosurfactant) in the body of the duodenum (bile A) increases abilities of solubilizing lipophilic therapeutic agents and cholesterol accounting for its use in the treatment of liver diseases and cholesterol gall bladder stones.
Summary Introduction: Using the general Hildebrand-Scatchard-Fedors theory of solubility, the mole fraction (x2) of solubility of phytochemicals contained in the dry green tea leaves was calculated which determines the profile of pharmacological activity. Objective: The applicative purpose of the study was to estimate the actual solubility of phytochemicals – S|real.| [mol/dm3] in water and in water-ethanol solutions of diversified polarity (εM) for their selective extraction and optimal formulation of oral solid dosage form. Methods: The basic physico-chemical and structural quantities of phytochemicals and corresponding mathematical equations of general Hildebrand-Scatchard-Fedors theory of solubility were used to calculate the actual solubility – S|real.| and the level of hydrophilic-lipophilic balance (HLB). Results: The calculated actual solubility values – S|real.| [mol/dm3] collated with correlation equations enabled the assessment of phytochemical capability for the process of mass exchange on phase boundary. Correlation equations for the dependence log P = f (– log S|real.|) point to the structural preferences of phytochemicals in the kinetics of the mass exchange (diffusion) through the natural phase boundary. Conclusions: Calculations and correlations between the values characterizing the actual solubility – S|real.|, media polarity (water, ethanol and their solutions) and the partition coefficient (log P) including the level of hydrophilic-lipophilic balance (HLB) show that basing on thermodynamic components of the general Hildebrand-Scatchard-Fedors theory of solubility, the diffusion profile of phytochemicals contained in the green tea extract (Ext. Camellia sinensis L. aqu. siccum) through the biological phase boundary as well as optimal choice of the extraction medium for selective extraction of the class of phytochemicals can be estimated.
S u m m a r y Introduction:The common bean (Phaseolus vulgaris L.) is an annual plant grown in many countries all over the world including its different varieties in Poland. Herbal raw material are elongated pods -pericarp. Phaseoli pericarpium decreases the glucose blood level. Phaseoli pericarpium extracts manifest duretic properties, can be used in the treatment of edema, kidney diseases with decreased urinary excretion, nephrolithiasis. Objectives: To investigate the usefullness of selected excipients as carriers of dry extract from Phaseolus vulgaris pericarp. Methods: The method of direct tableting was used. In the further stage, the obtained tablets were subjected to appropriate tests. The first stage of the study evaluates Prosolv SMCC 50, PROSOLV EASYtab, EMDEX, Carmellose calcium and PRUV. These were used to manufacture 4 batches of tablets. In the second stage, an oral solid dosage was manufactured on the basis of the formulation composition of batch 1 tablets (Phaseoli pericarpium extract, Prosolv SMCC 50, PRUV). Then, different surfactants (cholesterol oxyethylate n TE = 30, cholesterol oxyethylate n TE = 40, Rofam n TE = 50), were successively added to this formulation, to obtain 3 batches of tablets. All 7 batches were manufactured in the Erweka tableting machine. Then, they were subjected to morphological tests and physicochemical evaluation. The release of active substances to 3 selected acceptor fluids (water, artificial gastric juice, artificial intestinal juice) was measured in accordance with the requirements of the general and specific monographs in European Pharmacopoeia 7. Results: The manufactured tablets had a smooth uniform surface with no stains, spalls or mechanical damage and yellow color originating from the extract. The obtained tablets, with surfactants in their com- INTRODUCTIONPhaseolus is a genus of the family Fabaceae including about 200 species of annual and perennial plants, vines and subshrubs with large leaves and white, yellow or red flowers [1]. The common bean (Phaseolus vulgaris L.) belongs to this family. It is an annual plant originating from South America. It is cultivated in many countries, including Poland, for food, dry seeds and immature pods. It exhibits a wide variety of seed coat patterns and colors [2,3].The pharmacopoeic material described in the Polish Pharmacopoeia VI [4] is the dried pericarp (bean pod, Phaseoli pericarpium) derived only from white-flowered cultivars of Phaseolus vulgaris. The pericarps are curled and slightly thin, up to 20 cm long and up to 2 cm wide. One end has a short beak-like point, while a 1 cm stalk is often attached to the other. The outside surface is pale yellow or dark brown yellow, the inside is covered with a whitish, shiny membrane. In the areas where seeds are present, the pericarp is concave inside and convex outside [4].The main pharmacologically active compounds of Phaseoli pericarpium are: choline, amino acids (arginine, asparagine, leucine, lysine), pipecolic acid, trigonelline, allantoin, phenolic acids, mineral ...
Summary Introduction: Dandelion (Taraxacum officinale coll.), also called the common dandelion grows wild throughout Europe, Asia and the Americas. It is a perennial plant of the family of Asteraceae, having powerful healing properties. The entire plant – flowers, roots and leaves – is the medicinal raw material. Objective: The aim of this study was to manufacture model tablets of pharmacopoeial disintegration time by direct compression of dry titrated extract of dandelion with selected excipients. Methods: Tablets were obtained by direct compression using reciprocating tableting machine (Erweka). Morphological parameters – hardness, friability, disintegration time in pharmacopoeial acceptor fluids were investigated using Erweka equipment. Their actual surface area was also calculated. There was also tested the rate of dissolution of phytochemicals from model tablets in the presence of excipients in pharmacopoeial acceptor fluids (V=1.0 dm3) by the method of a basket in Erweka apparatus. Spectrophotometric determinations were performed. Results: It results from the morphological studies of model tablets containing Ext. Taraxaci e radix cum herba aqu. siccum that they are characterized by comparable surface and friability at varying hardness, the latter depending on the applied excipients. This is reflected in the effective disintegration time in model acceptor fluids consistent with pharmacopoeial requirements. Conclusions: The used excipients enabled to produce model tablets containing dry extract of dandelion by direct compression. The obtained results demonstrated that microcrystalline Prosolv-type cellulose, Vivapur 200 and Emdex were compatible with the structure of the extract of dandelion. They allow to manufacture a model solid oral dosage forms of the desired morphological parameters and effective disintegration time complying with the pharmacopoeial requirements.
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