22 research outputs found
Orodispersible films (ODF) in individualized therapy
Jednym z czynnik贸w wp艂ywaj膮cych na zapewnienie bezpiecznej i skutecznej farmakoterapii jest opracowanie odpowiedniej postaci leku dostosowanej do wieku pacjenta oraz 艂atwej w aplikacji, a tak偶e urz膮dze艅 dozuj膮cych umo偶liwiaj膮cych dob贸r odpowiedniej dawki leku. Takie podej艣cie jest zgodne z ide膮 leczenia skoncentrowanego na pacjencie. Spo艣r贸d doustnych postaci leku, ze wzgl臋du na zalety takie jak bezpiecze艅stwo, 艂atwo艣膰 po艂ykania czy mo偶liwo艣膰 regulacji dawki szczeg贸ln膮 uwag臋 po艣wi臋ca si臋 postaciom takim jak minitabletki, tabletki i filmy rozpadaj膮ce si臋 w jamie ustnej. Filmy ODF s膮 wskazywane jako odpowiednia posta膰 leku dla pacjent贸w pediatrycznych i geriatrycznych ze wzgl臋du na szybki rozpad w jamie ustnej bez konieczno艣ci popijania wod膮, przywieranie do b艂ony 艣luzowej zmniejszaj膮c ryzyko wyplucia leku oraz mo偶liwo艣膰 dostosowania dawki leku dla indywidualnego pacjenta. Wed艂ug bada艅 filmy ODF s膮 dobrze tolerowane przez dzieci jak r贸wnie偶 przez opiekun贸w. Maj膮 posta膰 cienkiego polimerowego p艂atka umieszczanego na j臋zyku. Filmy ODF mog膮 by膰 wytwarzane przy u偶yciu r贸偶nych metod, tj. wylewania z odparowaniem rozpuszczalnika, ekstruzji topliwej, prz臋dzenia elektrostatycznego, druku (atramentowego, fleksograficznego oraz druku przestrzennego 3D) na skal臋 przemys艂ow膮 oraz potencjalnie np. w aptekach szpitalnych. Przygotowywanie film贸w ODF ex tempore zapewnia wi臋ksz膮 mo偶liwo艣膰 regulacji dawkowania, wp艂ywaj膮c na przestrzeganie przez pacjenta zalece艅 farmakoterapii. Nowoczesne rozwi膮zania dotycz膮 tak偶e specjalnie zaprojektowanych urz膮dze艅 s艂u偶膮cych do przechowywania i dozowania ODF, a tak偶e metod znakowania i identyfikacji pojedynczych dawek leku. W pracy przedstawiono przegl膮d pi艣miennictwa z ostatnich lat, dotycz膮cy nowych rozwi膮za艅 technologicznych w zakresie sporz膮dzania film贸w ulegaj膮cych rozpadowi w jamie ustnej z uwzgl臋dnieniem metod wytwarzania, modyfikacji uwalniania substancji leczniczej oraz mo偶liwo艣ci ich zastosowania w indywidualizacji terapii.One of the mains factors affecting the effectiveness and safety of the therapy is the development of an appropriate dosage form adapted to the age of the patients and ease to administer as well as a dosing devices that provide flexible dosing. This approach is in accordance with the idea of patient-centered treatment. Given advantages such as safety, easy swallowing and flexible dose adjustment, special attention is paid to oral dosage forms such as orally disintegrating tablets, minitablets and orodispersible films (ODF). The ODF films are indicated as a suitable dosage form for pediatric, geriatric and uncooperative patients due to their fast disintegration in the mouth without need for water to facilitate swallowing, adhesion to the oral cavity to prevent spitting out the medicine and the ability to adjust the dose of the drug for an individual patient. According to many studies, orodispersible films are well accepted by infants and preschool children, their caregivers (nurses) and parents. They have the form of a postage stamp sized strip of thin polymeric film applied on the tongue. The ODF films can be manufactured using various methods, i.e. casting method, hot melt extrusion, electrospinning or printing (inkjet, flexographic and 3D printing) on an industrial scale and potentially in hospital pharmacies. Extemporaneous preparation of the ODF films create more dose flexibility affecting patient鈥檚 adherence to pharmacotherapy. Innovative solutions in this area concern also designed specifically devices for storage and dosing of ODF, as well as methods of labeling and identification of single doses, for example Quick Response (QR) codes. The paper presents a review of the literature from recent years regarding new technology in the terms of the ODF films preparation, including manufacturing methods and modification of the drug release, as well as the possibilities of their application in individualization of the therapy especially in pediatric and geriatric population
Practical aspects of using Witepsol H15 in pharmaceutical compounding
New excipients increase new possibilities of the modifications in the composition of a compounded drugs. One of the examples is a Witepsol H15 suppository base registered in 2018 as an alternative to the previously used cocoa oil. The use of Witepsol H15 requires the determination of the replacement factors for active substances and excipients to calculate the optimal amount of this suppository base to prepare a certain number of suppositories. The classical method, which has been used so far, is based on the measurements of the mass of the suppositories with and without API, and the determination of the replacement factor using a calculation formula. Taking into account the differences between replacement coefficients resulting for example from a type and concentration of the active substance or excipient, the method of mixing and its parameters, it is reasonable to introduce an alternative calculation method based on the density measurements determined pycnometrically. Density measurements of excipients, APIs and selected medicinal products were carried out using the helium pycnometry method. Based on the ratio between density of the substrate to the API/excipient, the replacement coefficients were calculated. In total, two suppository bases (Witepsol H15 and Cacao oleum), 17 active substances, 2 excipients and 8 medicinal products were tested. The results were presented in tables, compared with available literature data and percentage differences were calculated.
In order to complete the practical information regarding use of Witepsol H15, the numerous test on the functional properties of the base were carried out, including: volume contraction, sensitivity to process factors, thermal changes during heating and cooling. The ability to reduce the volume of the base during solidification has been confirmed, which allows an easy withdrawal of the suppository from the mold before application. The average contraction for Witepsol H15 is 3.23%, which is about 3 times higher compared to cocoa oil (1.13%). An analysis of the behavior during cooling of Witepsol H15 heated to different temperatures, was carried out and it was found that the overheated base shows stepped thermal changes profile while solidifying. The profile of temperature changes of properly liquefied base is predictable and does not show dynamic changes. Based on the DSC data, the liquid fraction content of Witepsol H15 was calculated. The base heated previously to 45 掳C contains more liquid components than the unheated base. A practical implication is the recommendation to not overheat the base in order to obtain proper liquefaction of the suppository mass, easy filling of molds and limitation in the sedimentation of ingredients in suppositories.
The results of performed studies confirm the usefulness of helium pycnometry to measure the density of substances and suppository bases, and to determine on their basis the displacement coefficients of active substances/excipients not included in the compendia so far. The helium pycnometry method enables the calculation of the displacement coefficient in the objective manner, independent of many factors, such as: base variability, preparation method, mixing parameters, content of API and excipients, size and load of the mixing container, conditions of solidification of the suppository mass. The replacement factors obtained in this way may be helpful in compounding practice. With the correct selection of mixing parameters, they lead to the obtainment of optimal amount of liquefied suppository mass necessary to fill the molds
Compression-Induced Phase Transitions of Bicalutamide
The formation of solid dispersions with the amorphous drug dispersed in the polymeric
matrix improves the dissolution characteristics of poorly soluble drugs. Although they provide an
improved absorption after oral administration, the recrystallization, which can occur upon absorption
of moisture or during solidification and other formulation stages, serves as a major challenge.
This work aims at understanding the amorphization-recrystallization changes of bicalutamide.
Amorphous solid dispersions with poly(vinylpyrrolidone-co-vinyl acetate) (PVP/VA) were obtained
by either ball milling or spray drying. The applied processes led to drug amorphization as confirmed
using X-ray diffraction and differential scanning calorimetry. Due to a high propensity towards
mechanical activation, the changes of the crystal structure of physical blends of active pharmaceutical
ingredient (API) and polymer upon pressure were also examined. The compression led to drug
amorphization or transition from form I to form II polymorph, depending on the composition
and applied force. The formation of hydrogen bonds confirmed using infrared spectroscopy and
high miscibility of drug and polymer determined using non-isothermal dielectric measurements
contributed to the high stability of amorphous solid dispersions. They exhibited improved wettability
and dissolution enhanced by 2.5- to 11-fold in comparison with the crystalline drug. The drug
remained amorphous upon compression when the content of PVP/VA in solid dispersions exceeded
20% or 33%, in the case of spray-dried and milled systems, respectively.Polish National Science Centre
2015/16/W/NZ7/0040
A Bulb of Narcissus on the Egyptian Mummy from University of Wroc艂aw Collection
The object of the present study is the ancient bulb of the narcissus found on the mummy, probably of the Ptolemaic period, brought to Wroc艂aw from Italy in the sixteenth century AD. For about four hundred years the mummy was kept by the successive owners of one of pharmacies in Wroc艂aw, and after the World War II became the possession of Wroc艂aw University. Computed tomography made in 2002 revealed an atypical object lying under the left hand of the mummy. Extracted in 2004 it appeared to be the bulb of a flower, and botanical analysis has revealed that it represents the Narcissus tazetta L. species. Although the narcissus was known in Egypt, its identification in the ancient sources has never been attempted. Thanks to the analysis of the bio-medical properties of the narcissus, compared with some descriptions of remedies proposed by the medical papyri Ebers and Hearts, as well as with some religious magical texts an identification of the sennut plant with narcissus is proposed here.The object of the present study is the ancient bulb of the narcissus found on the mummy, probably of the Ptolemaic period, brought to Wroc艂aw from Italy in the sixteenth century AD. For about four hundred years the mummy was kept by the successive owners of one of pharmacies in Wroc艂aw, and after the World War II became the possession of Wroc艂aw University. Computed tomography made in 2002 revealed an atypical object lying under the left hand of the mummy. Extracted in 2004 it appeared to be the bulb of a fl ower, and botanical analysis has revealed that it represents the Narcissus tazetta L. species. Although the narcissus was known in Egypt, its identification in the ancient sources has never been attempted. Thanks to the analysis of the bio-medical properties of the narcissus, compared with some descriptions of remedies proposed by the medical papyri Ebers and Hearts, as well as with some religious magical texts an identification of the sennut plant with narcissus is proposed here
NEW TECHNOLOGICAL SOLUTIONS IN THE ASPECT OF TOPICAL AND ORAL ADMINISTRATION OF RESVERATROL
Resveratrol (3,5,4-trihydroxystilbene) is a natural polyphenolic compound with a wide spectrum of biological activities, which could possibly be useful in the prevention or treatment of cardiovascular, neurodegenerative diseases, cancer, as well as premature skin aging. The extraction and synthesis methods have been developed rapidly for resveratrol. It is isolated mainly from Polygonum cuspidatum due to its high concentration in this herb. However, rapid development of biotechnology led to a new way of resveratrol synthesis directly in recombinant yeast, but also in bacteria, such as Escherichia coli. Currently, resveratrol is used as a dietary supplement in form of tablets, capsules or sublingual drops. Nonetheless, resveratrol application is still being a major challenge due to its poor solubility in water as well as low and erratic bioavailability. However, the latest studies showed the possibility of extending the therapeutic range of resveratrol utility, including its potential as a wound care agent. The systems designed for application to the skin are particularly promising, although the formulations proposal for oral administration are also interesting. Despite its potential as a compound administered topically, nowadays resveratrol is available only as an anti-aging ingredient in skin care products. As a substance with the pleiotropic mode of action, it has become the object of interest of many research groups as well as the pharmaceutical industry. Most studies have tended to focus on pharmacological activity of raw resveratrol and its poor bioavailabilty, thus the number of research concerning the development of a drug delivery system for resveratrol is very limited. The present review summarizes the most recent literature which demonstrates the currently used technologies allowing to overcome poor bioavailability of resveratrol, with particular emphasis put on its topical and oral administration. The article shows the current state of knowledge on delivery systems with resveratrol such as liposomes, nanoemulsions, lipid nanoparticles and nanocrystals. It presents also an overview of recent developments in the use of resveratrol in the prevention and treatment of different skin diseases.Resweratrol (3,4',5-trihydroksystilben) jako substancja o szerokim spektrum aktywno艣ci biologicznej stanowi przedmiot wielokierunkowego zainteresowania. Obecnie stosowany jest jako suplement diety oraz sk艂adnik kosmetyk贸w o przeciwstarzeniowym dzia艂aniu, jednak najnowsze wyniki bada艅 wskazuj膮 mo偶liwo艣膰 rozszerzenia zakresu terapeutycznego resweratrolu m.in. o piel臋gnacje ran. Wielokierunkowe dzia艂anie farmakodynamiczne, przy jednocze艣nie trudnej rozpuszczalno艣ci w wodzie i niskiej biodost臋pno艣ci rozszerza problematyk臋 badawcz膮 o poszukiwanie nowych form leku zapewniaj膮cych uzyskanie optymalnego efektu terapeutycznego. Szczeg贸lnie obiecuj膮ce s膮 uk艂ady przeznaczone do aplikacji na sk贸r臋, jakkolwiek ciekawa jest te偶 propozycja formulacji do podania drog膮 doustn膮. W pracy przedstawiono aktualny stan wiedzy na temat w艂a艣ciwo艣ci i zakresu stosowania resweratrolu, ze szczeg贸lnym uwzgl臋dnieniem nowych rozwi膮za艅 technologicznych w formie liposom贸w, nanoemulsji, nanokryszta艂贸w, nanocz膮stek lipidowych czy materia艂贸w opatrunkowych pod k膮tem jego miejscowego i doustnego podania