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  • Author: Marian Mikołaj Zgoda x
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Open access

Elżbieta Nowak, Michał Jakub Nachajski and Marian Mikołaj Zgoda

Summary

Model maidenhair tree (Ginkgo bilobae) leaf extracts were created basing on medium of diversified polarity (εM). Chromatographic analysis was performed with the HPLC method, with the so-called dry residue remaining after evaporating the dissolving agent from saturated aqueous solutions and from 0.1 mol HCl. Viscosity measure and surface activity estimations were conducted on phase boundary. Then, basic values of viscosity ([η], Mη) and hydrodynamic values (Ro, Robs., Ω) were calculated. Moreover, reference quercetin and rutin (rutoside) were used to mark the conversion contents of flavonoids in produced extracts with the UV method.

Open access

Zbigniew Marczyński, Maria Elżbieta Fornal, Jerzy Jambor and Marian Mikołaj Zgoda

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.

Open access

Zbigniew Marczyński, Sławomira Nowak, Jerzy Jambor and Marian Mikołaj Zgoda

Summary

Introduction: The general Hildebrand-Scatchard theory of solubility supplemented by Fedors’ solubility parameter δ12 was used to estimate the real solubility by −log x2 (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 cexp. ≥cmc in relation to cholesterol particle size of Ø=1.00 mm, as well as of ketoprofen were defined.

Objective: The calculated value −log x2 collated with the polarity of extraction medium εM 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.

Open access

Zbigniew Marczyński, Beata Skibska, Sławomira Nowak, Jerzy Jambor and Marian Mikołaj Zgoda

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.

Open access

Zbigniew Marczyński, Beata Skibska, Sławomira Nowak, Izabela Rychlińska, Jerzy Jambor and Marian Mikołaj Zgoda

Summary

Introduction: Green tea offers not only pleasant, delicate flavor, but also provides health benefits. The extract contains, among others, polyphenols responsible for antioxidant and anti-inflammatory properties. They reduce the risk of cancer and their presence exerts preventive activity against cardiovascular diseases.

Objective: Analysis of selected physicochemical and solubilizing properties of pharmacopoeial-true solutions of dry green tea extract.

Methods: The caffeine content was determined in the extract and in dry residue after solubilization by high performance liquid chromatography. The process of micellar solubilization of cholesterol granules and ketoprofen was carried out in model solutions of green tea extract.

Results: The obtained results indicate that the prepared ‘ex tempore’ leaf green tea infusion subjected to short thermal exposure will be characterized by significant solubilization abilities.

Conclusions: The outcomes of the research pointed to the possibility of developing a solid oral dosage form with titrated dry green tea extract of expected pharmacotherapeutic profile.

Open access

Adrian Głogowski, Zbigniew Marczyński, Michał Krzysztof Kołodziejczyk, Jerzy Jambor, Marta Kinga Stefan and Marian Mikołaj Zgoda

Summary

Introduction: Dietary supplements are a good way to supplement the deficiency of certain micronutrients and organic components (therapeutic agents) in human body. They are most often available in concentrated form as tablets, capsules, powder or liquid.

Objective: To investigate morphological parameters and the pharmaceutical availability of coated tablets – dietary supplements – that contain selected pharmacopeial titrated dry plant extracts.

Methods: Testing of the effective time of the tablet surface erosion was performed in model acceptor fluids using pharmacopeial methods in static (Erweka apparatus) and dynamic (unlimited diffusion method) conditions. Furthermore, morphological parameters of tablets (the original shape of an ellipse) as well as their hardness were determined.

Results: The effective erosion time was determined by conductometric method using carboxymethylcellulose sodium salt (NaCMC) contained in the tablet. The content of gum arabic and NaCMC in the tablet testifies that the granulate was produced using the “wet granulation” technique which resulted in high hardness of original, esthetic, elliptical tablets and in prolonged disintegration time (erosion).

Conclusions: The used excipients: gum arabic and NaCMC for the production of the tested tablets containing selected dry plant extracts result in their high hardness. The tested dietary supplements are characterized by esthetic design, original shape, and prolonged disintegration time which affects the pharmaceutical availability.

Open access

Elżbieta Nowak, Zbigniew Marczyński, Beata Skibska, Michał Jakub Nachajski, Jerzy Jambor and Marian Mikołaj Zgoda

Summary

Introduction: Common ivy (Hedera helix) is a plant used successfully in the treatment of various ailments. This is possible owing to the unique set of substances contained in it such as large amount of saponins, flavonoids, phenolic acids and phytosterols as well as polyacetylenes and coumarins. All these substances have been used in the production of cosmetic and medicinal preparations. Clinical trials on the efficacy and safety of dry ivy leaf extract have shown its high efficacy, comparable to synthetic medications, and better tolerance of herbal drugs.

Objective: Investigations were performed on model ivy leaf (Hedera helix) extracts which were created using a medium of diversified polarity ( εM). Measurements of viscosity and surface activity on phase boundary were performed. During preformulation studies attention was drawn to the possibility of micellar solubilization of cholesterol and selected structures of nonsteroidal anti-inflammatory drugs (NSAIDs) – ketoprofen.

Methods: Viscosity measurements of Extractum Hederae helicis e folium aqueous solutions and in 0.1 mol HCl were performed according to the Polish Standard with Ubbelohde dilution viscometer. The surface tension of aqueous solutions -Δγsol25 of Hederae helicis e folium extracts was determined according to the Polish Standard with stalagmometric method. Critical micellar concentration (cmc) was calculated. This enabled to evaluate the dependence ΔGm0=2.303 RT×log cmc of the thermodynamic potential of micelle formation (ΔGm0 ). Results: It has been confirmed in the conducted comparative studies that aqueous solutions of Extr. Hederae helicis e folium created with maltodextrin as well as with SiO2 – maltodextrin result in micellar solubilization. The increase of granulometric size of cholesterol particle to Ø 1.60 mm decreased the amount of solubilized cholesterol but solubility preferences of the extracts were maintained.

Conclusions: Model extracts produced from Hederae helicis e folium with diversified polarity of the extraction medium (water – ethanol) are characterized by appropriate solubility of the components which results not only from the presence of chlorophyll and its derivatives in the extract but also from the technique used for spray drying of the extract.