[Glycol plant extracts in the prescription of topical skin-whitening hydrogels]. / Zastosowanie glikolowych wyciagów roslinnych w recepturze hydrozeli o dzialaniu wybielajacym podawanych na skóre.

An attempt was made to produce and test, according to the guidelines of Polish Pharmacopeia VIII, new prescriptions of hydrogels which could be applied in the treatment of skin diseases associated with hyperpigmentation. Hydrogel formulations containing a substance of skin-whitening activity (arbutin) and glycol plant extract was produced on Carbopol Ultrez 10 base. Two glycol plant extracts of confirmed beneficial effect on skin were selected: an extract of ginkgo leaves and of rosemary. For comparative purposes also preparations with arbutin were produced in which propylene glycol was introduced instead of glycol plant extracts. The assumption of the carried out study was to investigate physicochemical properties of model formulations, estimation of arbutin pharmaceutical availability from the suggested formulations and the assessment of the effect of glycol plant extract components on the process of arbutin diffusion from the produced hydrogel formulations. The formulation viscosity parameters were determined using cone-plate digital rheometer. Gravimetric method was applied to estimate the kinetics of volatile components from the preparations. Potentiometric method was used to measure pH. The rate of arbutin release through a semipermeable membrane to the acceptor fluid was tested in vitro. Spectrophotometric method was used for the determination of the quantity of the released therapeutic substance at defined time intervals. All the proposed formulations are viscoelastic systems having yield stress. There is a strict dependence between rheological properties characterizing the tested hydrogels and the quantity of the arbutin released from them. The process of arbutin release to the acceptor fluid through a semipermeable membrane was most effective from the formulation containing glycol extract of ginkgo (F1A+M).

[The application of Harpagophytum procumbens extract in anti-inflammatory preparations applied on skin produced on acrylic acid polymers base]. / Zastosowanie wyciagu z czarciego pazura w przeciwzapalnych preparatach aplikowanych na skóre, wytworzonych na bazie polimerów kwasu akrylowego.

An attempt was made to use dry standardized extract from Harpagophytum procumbens of confirmed anti-inflammatory activity in formulations applied on skin. To obtain synergy in the area of analgesic and anti-inflammatory activity formulations were produced containing plant extract and nonsteroidal anti-inflammatory drug (ketoprofen). All the preparations were prepared on the base of acrylic acid polymers (Carbopol Ultrez 10, Carbopol 980). The formulations were subjected to complementary physicochemical investigations. Viscosity parameters (structural viscosity, yield stress, thixotrophy) were determined with cone-plate digital rheometer. Potentiometric method was used to measure pH of the produced hydrogels. The test for ketoprofen pharmaceutical availability through a semipermeable membrane to acceptor fluid was performed in vitro. The rate of the process of release was tested by determining the quantity of the therapeutic agent diffusing into acceptor fluid at defined time intervals by spectrophotometric method. The effect of Harpagophytum procumbens extract components on ketoprofen diffusion was estimated. Viscosity tests revealed that all the formulations are viscoelastic systems having yield stress. All model formulations were tested 24h after production and after 6-month storage. All the formulations demonstrate rheological stability and high pharmaceutical availability of ketoprofen. The suggested formulations can be an alternative for market preparations applied on skin of anti-inflammatory and analgesic activity.

[Glicol plant extracts of anti-inflammatory activity in hydrogels produced on Carbopol base]. / Glikolowe wyciagi roslinne o dzialaniu przeciwzapalnym w hydroielach wytworzonych na bazie Carbopoli.

Medications originating from plants can be successfully applied in the treatment of rheumatic pain beside those from the nonsteroidal anti-inflammatory drugs (NSAIDs). An attempt was made to produce a new form of a drug applied on skim, which contains NSAID and glycol plant extract in its composition. The aim of the study was to obtain synergy in the area of analgesic and antiinflammatory activity. Formulations containing NSAID (ketoprofen) and formulations containing glycol plant extracts of confirmed anti-inflammatory and analgesic activity (extract from sage, extract form arnica) were produced on the basis of acrylic acid polymers (Carbopol Ultrez 10, Carbopol 980). Moreover, formulations were also produced containing ketoprofen and glycol plant extract in their composition. Viscosity parameters of the tested formulations (structural viscosity, yield stress, thixotrophy)were determined with cone-plate digital rheometer. Potentiometric method was used to measure pH of the produced hydrogels. The test for therapeutic agents pharmaceutical availability was performed with membrane method. Spectrophotometric method was used to estimate the quantity of the released therapeutic agent. The usefulness of acrylic acid polymers (Carbopol Ultrez 10, Carbopol 980) was assessed for the application in the prescription of dermatological hydrogels as well as their compatibility with ketoprofen and active substances contained in glycol plant extracts. Pharmaceutical availability was tested of ketoprofen and therapeutic agents contained in the investigated plant extracts. Furthermore, the effect of the components of extracts on the process of ketoprofen release to acceptor fluid through a semipermeable membrane was estimated.

[Dry plant extracts in the prescription of dental hydrogels with Carbopol 971P]. / Suche ekstrakty roslinne w recepturze hydrozeli stomatologicznych z Carbopolem 971P.

The study assumption was to work out a prescription for dental anti-inflammatory hydrogel on Carbopol 971P base. Dry plant extracts (sage, horsetail) and nonsteroidal anti-inflammatory drug (sodium ibuprofen) were introduced into the prescription of a model hydrogel. The aim of the study was to estimate pharmaceutical availability of the applied therapeutic agents and to test their effect on physicochemical properties of the produced form of a drug. The physicochemical parameters of the produced preparation were tested. Viscosity tests were performed using cone-plate digital rheometer. Extensometric method was used to test extensibility. pH measurements were performed by direct immersing the electrode connected with pH-meter into the hydrogel samples of uniform mass. Pharmaceutical availability of therapeutic agents contained in hydrogel (active components of plant extracts, sodium ibuprofen) was estimated. The rate of the process of mass exchange was tested by spectrophotometric method determining the quantity of therapeutic agents diffusing into acceptor fluid at the same time intervals. Sodium ibuprofen is better released from the hydrogel containing horsetail extract (815.5 c.u.) than from the hydrogel of parallel prescription containing sage extract (640.8 c.u.). Hydrogels containing dry extract from horsetail have greater extensibility and lower structural viscosity as well as the value of yield stress than equivalent hydrogels containing sage extract. Introduction of sodium ibuprofen into the prescription of hydrogels with plant extracts modifies rheological parameters (greater extensibility, lower viscosity of the preparation). The tests of the kinetics of therapeutic agents release demonstrated that the presence of sodium ibuprofen in the prescription of hydrogels exerts an influence on the decrease of the effectiveness of the release of active substances contained in these extracts.

[Application of thyme extract in the prescription of dental gels produced on Carbopol base]. / Zastosowanie ekstraktu z tymianku w recepturze hydrozeli stomatologicznych wytworzonych na bazie Carbopoli.

Active components of glycol extract from thyme manifest anti-inflammatory and astringent properties which may be also used in dentistry. The assumption of this study was to work out a prescription of dental anti-inflammatory hydrogel containing nonsteroidal anti-inflammatory drug and glycol extract from thyme. The aim of this study was to assess pharmaceutical availability and physico-chemical parameters of hydrogels produced on the base of various Carbopols (974P, 971P and AA1). Pharmaceutical availability of therapeutic agents contained in the hydrogel was tested. The rate of the process of mass exchange was tested with spectrophotometric method by determining the quantity of therapeutic agents diffusing into acceptor fluid at identical time intervals. Physicochemical parameters (including viscosity) of the produced preparation were estimated dependently on the vehicle variant components (acrylic acid polymers). Viscosity tests were performed with cone-plate digital rheometer. The kinetics of volatile components from the preparation was estimated by gravimetric method. pH measurements were performed by direct immersion of the electrode connected with the pH-meter in the samples of hydrogels of the same mass. The highest pharmaceutical availability of therapeutic agents was obtained in the tests of a hydrogel with Carbopol 971P. The area under sodium ibuprofen release curve from this hydrogel was estimated as 626.06 of conventional units. The content of active components of thyme extract in the last sample collected during the test of their release was 5.2729 mg/1 cm2 of the release area. Advantageous rheological parameters as regards application such as: low value of structural viscosity (11762 mPa x s at shear rate 2.4 1/s), low value of hysteresis loop (0.51 c.u.) and yield stress (6.51 N/m2) as well as natural pH for oral cavity (6.7) were also obtained for a hydrogel with Carbopol 971P.

[The evaluation of ketoprofen pharmaceutical availability in the presence of a dry extract from goldenrod (Solidago virgaurea L.) of synthetic polymer vehicles]. / Ocena dostepnosci farmaceutycznej ketoprofenu w obecnosci suchego wyciagu z nawloci (Solidago virgaurea L.) z syntetycznych podlozy polimerowych.

The aim of this study was to produce hydrogels for topical use and having strengthened anti-inflammatory, analgesic and antirheumatic activity. To obtain the above effect dry standardized plant extract was added to enrich a formulation containing therapeutic agent (ketoprofen) from the group of nonsteroidal anti-inflammatory drugs. Dry standardized extract from Solidago virgaurea L. of confirmed anti-inflammatory activity was selected for this purpose. The derivatives of acrylic acid polymers (Carbopol Ultrez and Carbopol 980) were used as the formulation vehicles. These vehicles were selected owing to their high applicative properties--transparency, resistance to changes of temperature, perfect tactile and esthetic qualities, no sensitizing agents, no toxicity and lack of influence on therapeutic properties of the therapeutic agent and compatibility in the pharmaceutical phase. The produced formulations were exposed to basic physicochemical tests--pH, viscosity parameters (structural viscosity, yield stress and thixotropy), pharmaceutical availability and durability after six months of storage. The effect of component plant extracts on the process of ketoprofen diffusion to acceptor fluid through a semipermeable membrane was also compared. The obtained results indicate that dry standardized extract from Solidago virgaurea L. does not affect significantly the process of ketoprofen release from the tested preparations. After six months of storage the preparations with ketoprofen demonstrate rheological stability and high pharmaceutical availability.

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

The increasing interest of the technology of drug form in natural biopolymers has become the reason for undertaking investigations on the possibility of guar gum application in the prescription of oral solid form of a drug. Alternative compositions and technology of the production of tablets of regulated in time sodium ibuprofen release were worked out for children. Two series of tablets were prepared with guar gum (5 and 10% content) and a series without the biopolymer. The tablet mass in each case contained keryostatic sorbitol and bioadhesive polyvinylpyrrolidone. All tablets were tested as regards the quality of production, compliance with the requirements of Polish Pharmacopoeia VI and potential therapeutic usefulness, manifestation of which is pharmaceutical availability of the therapeutic agent (sodium ibuprofen). The tests demonstrated that the produced tablets with sodium ibuprofen have proper physicochemical properties, in compliance with Polish Pharmacopoeia VI requirements. Application of biopolymer of guar gum type as adjuvant substance contributes to the improvement of the tablet hardness parameters and prevents technological problems (lining mixture of powders to tableting machine punch). The designed tablets demonstrate proper pharmaceutical availability of over 80%. Introduction of guar gum into their prescription prolonged their disintegration time and the rate of sodium ibuprofen release, which predisposes the produced form of a drug to have the function of a tablet with slowed-down release.