Marian Mikołaj Zgoda

Solubility and solubilizing capabilities of aqueous solutions of Extractum Taraxaci e radix cum herba aqu. siccum in light of selected values of general Hildebrand-Scatchard-Fedors theory of solubility

Summary Introduction: The general Hildebrand-Scatchard theory of solubility supplemented by Fedors’ solubility parameter −δ12

Erroneous administration of vinblastine

- \delta ^{{1 \over 2}}

Actual solubility (S|real.|), level of hydrophilic-lipophilic balance (HLBRequ., HLBD, HLBG) and partition coefficient (log P) of phytochemicals contained in Ext. Camellia sinensis L. aqu. siccum in the light of general Hildebrand-Scatchard-Fedors theory of solubility

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.

Formulation and profile of pharmaceutical availability from a model oral solid form of a drug of phytochemicals contained in dry Taraxacum officinale extract

This case describes a series of errors which resulted in an avoidable death of the patient. Upon being presented with the 83-year-old patient and her complaints, the physician in charge attempted to prescribe Vasolastine® (a complex preparation used, for example, in treatment of angiopathy, which is administered intramuscularly once a day). Unfortunately he misspelled the name of the medicine as Vinplastyna—a non-existent preparation. When the patient’s daughter went to collect the prescription from the pharmacist she was dispensed Vinblastin (vinblastine—a cytostatic medicine used, for example, in treating Hodgkin’s disease, non-Hodgkin’s lymphoma, chronic lymphatic leukemia and testicular cancer). The visiting community nurses administered a dose of this medicine on seven consecutive days. Upon being given the seventh dose, the patient displayed symptoms of myelophthisis, and was admitted to an Intensive Care Ward, where despite the treatment, she died.

Maidenhair tree (Ginkgo Bilobae) leaf extraction products in the light of Biopharmaceutics Classification System (BCS) requirements and medium of diversified polarity (εM)

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.

Selected physicochemical and solubilization properties of pharmacopeal solutions of dry green tea leaf extract (Ext. Camellia sinensis L. folium aqu. siccum)

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.

The influence of the viscosity of the ointment vehicles magisterial topical preparations, on the speed transfer of biologically active substances

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. Streszczenie Wytworzono modelowe ekstrakty z liści miłorzębu japońskiego (Ginkgo bilobae), korzystając z medium o zróżnicowanej polarności (εM). Przeprowadzono analizę chromatograficzną metodą HPLC tzw. suchej pozostałości uzyskanej po odparowaniu rozpuszczalnika z nasyconych wodnych roztworów i z 0,1 mol HCl. Przeprowadzono pomiary lepkościowe i aktywności powierzchniowej na granicy faz. Wyliczono podstawowe wielkości lepkościowe ([η], Mη) i hydrodynamiczne (Ro, Robs., Ω). Korzystając z referencyjnej kwercetyny i rutyny (rutozydu) przeliczeniową metodą UV oznaczono również zawartość flawonoidów w wytworzonych ekstraktach.

Teat tablet with sodium ibuprofen: the effect of sorbitol on therapeutic agent pharmaceutical availability and on physicochemical parameters of a drug form

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.

[Microcrystalline cellulose and their flow -- morphological properties modifications as an effective excpients in tablet formulation technology containing lattice established API and also dry plant extract].

Abstract The aim of this study was to analyze the morphological parameters (viscosity, viscous elasticity and the rate of volatile component loss) of salicylic and boric acid-containing magisterial formulae (ointments). Moreover, the effects of these parameters on the diffusion rate of a therapeutic agent (salicylic acid) to an in vitro external compartment were analyzed. Finally, the applicatory properties of the ointments prepared by way of a conventional technique (in a mortar) and with the aid of an unguator, were compared. The rheological parameters of the analyzed ointments suggest that the preparations made with an aid of an unguator, irrespective of the physicochemical characteristics of their vehicles, are characterized by higher values of diffusion coefficient (D). In addition, conventionally-prepared formulae containing salicylic were shown to be characterized by better viscous elasticity. Surprisingly, irrespective of the preparation technique, the ointments based on an absorptive vehicle (containing lanolin) were characterized by similar viscous elasticity. The rate of volatile (water) component loss from ointments containing a 3% solution of boric acid suggests that such formulae lose no more than 2.3% of their mass when exposed at 37℃. Therefore, the viscosity of such ointments applied onto a patient’s skin should remain relatively stable.

Application of guar gum biopolymer in the prescription of tablets with sodium ibuprofen--quality tests and pharmaceutical availability in vitro.

Dosing pediatric drugs available on pharmaceutical markets of analgesic, antifebrile and anti-inflammatory activity to children up to 3 years of age is not precise and frequently causes problems. The aim of the study was to work out a pediatric teat form of a drug with sodium ibuprofen and to determine the effect of sorbitol content on pharmaceutical availability of the therapeutic agent. Three variants of tablets containing 50 mg of sodium ibuprofen differing in the percentage content of sorbitol (from 37% - batch I to 79% - batch III) were produced. Quality tests of the produced forms of drugs (PPVI) were performed and the tests of therapeutic agent pharmaceutical availability by spatula method and by a method with a teat. Tablets of all batches had a smooth surface and same shape. The content of the therapeutic agent was within the limit of 95-105% of the declared value. The highest value of Q coefficient in the release test by pharmacopeal method and the shortest disintegration time (12 minutes) were obtained for tablets with 79% content of sorbitol. In conclusion, teat tablets with sodium ibuprofen of the highest sorbitol content (79%) demonstrated the expected physicochemical parameters and high pharmaceutical availability.