Levothyroxin (LT4) je léčbou volby pro pacienty s hypotyreózou. Je spousta známých faktorů, které ovlivňují absorpci LT4 a nastavení správné dávky. Pokud pacienti dosáhnou optimálních hladin hormonů štítné žlázy, stačí kontroly provádět jednou ročně. Nicméně často je dávka LT4 nedostatečná nebo nadměrná z mnohých důvodů. V poslední době máme dostupné gelové kapsle levothyroxinu oproti tradičním tabletám, které dle dostupných studií dosahují stabilnějších hladin TSH a to nejen u pacientů s poruchou vstřebávání.
Levothyroxine (LT4) is the treatment of choice for patients with hypothyroidism. There are many known factors that influence the absorption of LT4 and the setting of the correct dose. As long as patients achieve optimal thyroid hormone levels, it is sufficient to check once a year. However, often the LT4 dose is insufficient or excessive for many reasons. Recently, we have levothyroxine gel capsules available versus traditional tablets, which studies show achieve more stable TSH levels, and not only in patients with absorption disorders.
- Klíčová slova
- gelové kapsle,
- MeSH
- autoimunitní tyreoiditida * farmakoterapie MeSH
- lidé středního věku MeSH
- lidé MeSH
- thyreotropin analýza účinky léků MeSH
- thyroxin aplikace a dávkování farmakologie terapeutické užití MeSH
- tobolky terapeutické užití MeSH
- Check Tag
- lidé středního věku MeSH
- lidé MeSH
- ženské pohlaví MeSH
- Publikační typ
- kazuistiky MeSH
- Klíčová slova
- gelové kapsle,
- MeSH
- absorpce v žaludku účinky léků MeSH
- autoimunitní tyreoiditida * diagnóza farmakoterapie imunologie MeSH
- hypotyreóza komplikace MeSH
- lidé středního věku MeSH
- lidé MeSH
- rozhodování účinky léků MeSH
- thyreotropin * analýza krev MeSH
- thyroxin * aplikace a dávkování farmakologie terapeutické užití MeSH
- tobolky aplikace a dávkování MeSH
- Check Tag
- lidé středního věku MeSH
- lidé MeSH
- ženské pohlaví MeSH
- Publikační typ
- kazuistiky MeSH
OBJECTIVE: This research aims to design and evaluate an enteric-coated hard capsule dosage form for targeted delivery of biological materials, such as FMT (fecal microbiota transplant) or live microbes, to the distal parts of the GIT. The capsules are designed to be internally protected against destruction by hydrophilic filling during passage through the digestive tract. METHODS: Hard gelatin capsules and DRcapsTMcapsules based on HPMC and gellan were used to encapsulate a hydrophilic body temperature-liquefying gelatin hydrogel with caffeine or insoluble iron oxide mixture. Different combinations of polymers were tested for the internal (ethylcellulose, Eudragit® E, and polyvinyl acetate) and external (Eudragit® S, Acryl-EZE®, and cellacefate) coating. The external protects against the acidic gastric environment, while the internal protects against the liquid hydrophilic filling during passage. Coated capsules were evaluated using standard disintegration and modified dissolution methods for delayed-release dosage forms. RESULTS: Combining suitable internal (ethylcellulose 1.0 %) and external (Eudragit® S 20.0 %) coating of DRcapsTM capsules with the wiping and immersion method achieved colonic release times. While most coated capsules met the pharmaceutical requirements for delayed release, one combination stood out. Colonic times were indicated by the dissolution of soluble caffeine (during 120-720 min) measured by the dissolution method, and capsule rupture was indicated by the release of insoluble iron oxide (after 480 min) measured by the disintegration method. This promising result demonstrates the composition's suitability and potential to protect the content until it's released, inspiring hope for the future of colon-targeted delivery systems and its potential for the pharmaceutical and biomedical fields. CONCLUSION: Innovative and easy capsule coatings offer significant potential for targeted drugs, especially FMT water suspension, to the GIT, preferably the colon. The administration method is robust and not considerably affected by the quantity of internal or external coatings. It can be performed in regular laboratories without specialized individual and personalized treatment equipment, making it a practical and feasible method for drug delivery.
- MeSH
- bakteriální polysacharidy chemie MeSH
- biokompatibilní materiály chemie MeSH
- celulosa * chemie analogy a deriváty MeSH
- deriváty hypromelózy chemie MeSH
- hydrofobní a hydrofilní interakce * MeSH
- hydrogely chemie MeSH
- kofein chemie aplikace a dávkování MeSH
- kolon * metabolismus MeSH
- kyseliny polymethakrylové chemie MeSH
- lékové transportní systémy * metody MeSH
- léky s prodlouženým účinkem chemie MeSH
- polymery chemie MeSH
- polyvinyly chemie MeSH
- tobolky * MeSH
- uvolňování léčiv * MeSH
- želatina * chemie MeSH
- železité sloučeniny chemie aplikace a dávkování MeSH
- Publikační typ
- časopisecké články MeSH
Background and Objectives: The enteric form of omeprazole is one of the most commonly prescribed medications. Similarly to Europe, Kazakhstan relies on the localization of pharmaceutical drug production as one of its primary strategies to ensure that its population has access to affordable and good-quality medicines. This study comprehensively describes the technologically available development of bioequivalent delayed-release omeprazole. Materials and Methods: Various regimes and technological parameters were tested on laboratory- and production-scale equipment to establish a technical process where a functional and gastro-protective layer is essential. According to the ICH guidance on stability testing and Kazakhstan local rules, stability studies were conducted under conditions appropriate for climate zone II. The comparison of the rate and extent of absorption with subsequent assessment of the bioequivalence of the generic and reference drugs after a single dose of each drug at a dose of 40 mg was performed. Results: The quantitative and qualitative composition and technology of producing a new generic enteric form of omeprazole in capsules were developed and implemented at the manufacturing site of solid forms. Dissolution profiles in media with pH 1.2 and 6.8 were proven. During the accelerated six-month and long-term twelve-month studies, the developed formulation in both packaging materials at each control point passed the average weight and mass uniformity test, dissolution test, acid-resistance stage test, buffer stage test, impurity assay, and microbiological purity test and met all the specification criteria. A bioequivalence study in 24 healthy volunteers compared against the innovative drug showed the bioequivalency of the new generic system. The obtained values from the test and reference products were 1321 ± 249.0 ng/mL and 1274 ± 233 ng/mL for Cmax, 4521 ± 841 ng·h /mL and 4371 ± 695 ng·h /mL for AUC0-t, and 4636 ± 814 ng·h /mL and 4502 ± 640 ng·h /mL for AUC0-∞. Conclusions: Using affordable technologies, a bioequivalent generic delayed-release formulation of 20 and 40 mg omeprazole has been developed.
- MeSH
- klinické křížové studie MeSH
- lidé MeSH
- omeprazol * chemie MeSH
- terapeutická ekvivalence MeSH
- tobolky MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- Geografické názvy
- Evropa MeSH
BACKGROUND: There is no single gold standard for investigation of gastrointestinal motility function. Wireless motility monitoring involves a novel concept which provides a complex information on gastrointestinal function (gastrointestinal transit time, intra-luminal pH, pressure and temperature). Gastrointestinal motility functions of experimental pigs are very similar to those of humans. That is why porcine studies have already provided suitable experimental models for several preclinical projects. AIMS: The aim of our study was to adopt methods of non-invasive wireless monitoring of gastrointestinal functions in experimental pigs. METHODS: Five experimental adult female pigs were enrolled into the study. Wireless motility capsules were delivered into the porcine stomach endoscopically. Gastrointestinal transit and intra-luminal conditions were recorded for five days. RESULTS: Records of animals provided good (3 pigs) or very good quality files (2 pigs). 31150 variables were evaluated. Mean time of the presence of capsules in the stomach was 926 ± 295 min, transfer of a capsule from the stomach into the duodenum lasted 5-34 min. Mean small intestinal transit time was 251 ± 43 min. Food intake was associated with an increase of gastric luminal temperature and a decrease of intra-gastric pressure. The highest intra-luminal pH was present in the ileum. The highest temperature and the lowest intra-luminal pressure were found in the colon. All data displayed a substantial inter-individual variability. CONCLUSIONS: This pilot study has proven that a long-term function monitoring of the gastrointestinal tract by means of wireless motility capsules in experimental pigs is feasible. However, both ketamine-based induction of general anaesthesia as well as long-lasting general anaesthesia (> 6 hours) should be avoided to prevent retention of a capsule in the porcine stomach.
- Klíčová slova
- syntroxine,
- MeSH
- diferenciální diagnóza MeSH
- dospělí MeSH
- hypotyreóza * diagnóza farmakoterapie komplikace krev MeSH
- intravenózní podání MeSH
- komplikace těhotenství MeSH
- léková rezistence MeSH
- lidé MeSH
- mladý dospělý MeSH
- náklady na léky MeSH
- těhotenství MeSH
- thyroxin * aplikace a dávkování terapeutické užití MeSH
- tobolky terapeutické užití MeSH
- tyreoidektomie MeSH
- tyreotoxikóza chirurgie farmakoterapie MeSH
- Check Tag
- dospělí MeSH
- lidé MeSH
- mladý dospělý MeSH
- těhotenství MeSH
- ženské pohlaví MeSH
- Publikační typ
- kazuistiky MeSH
- Klíčová slova
- Syntroxine,
- MeSH
- diferenciální diagnóza MeSH
- hypotyreóza * diagnóza farmakoterapie komplikace krev MeSH
- intravenózní podání MeSH
- komplikace těhotenství MeSH
- léková rezistence MeSH
- lidé MeSH
- mladý dospělý MeSH
- náklady na léky MeSH
- těhotenství MeSH
- thyroxin * aplikace a dávkování terapeutické užití MeSH
- tobolky terapeutické užití MeSH
- tyreoidektomie MeSH
- tyreotoxikóza chirurgie farmakoterapie MeSH
- Check Tag
- lidé MeSH
- mladý dospělý MeSH
- těhotenství MeSH
- ženské pohlaví MeSH
- Publikační typ
- kazuistiky MeSH
The aim of this study was to fabricate novel microparticles (MPs) for efficient and long-term delivery of amikacin (AMI). The emulsification method proposed for encapsulating AMI employed low-molecular-weight poly(lactic acid) (PLA) and poly(lactic acid-co-polyethylene glycol) (PLA-PEG), both supplemented with poly(vinyl alcohol) (PVA). The diameters of the particles obtained were determined as less than 30 μm. Based on an in-vitro release study, it was proven that the MPs (both PLA/PVA- and PLA-PEG/PVA-based) demonstrated long-term AMI release (2 months), the kinetics of which adhered to the Korsmeyer-Peppas model. The loading efficiencies of AMI in the study were determined at the followings levels: 36.5 ± 1.5 μg/mg for the PLA-based MPs and 106 ± 32 μg/mg for the PLA-PEG-based MPs. These values were relatively high and draw parallels with studies published on the encapsulation of aminoglycosides. The MPs provided antimicrobial action against the Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and Klebsiella pneumoniae bacterial strains. The materials were also comprehensively characterized by the following methods: differential scanning calorimetry; gel permeation chromatography; scanning electron microscopy; Fourier transform infrared spectroscopy-attenuated total reflectance; energy-dispersive X-ray fluorescence; and Brunauer-Emmett-Teller surface area analysis. The findings of this study contribute toward discerning new means for conducting targeted therapy with polar, broad spectrum antibiotics.
- MeSH
- amikacin aplikace a dávkování chemie MeSH
- antibakteriální látky aplikace a dávkování chemie MeSH
- Escherichia coli účinky léků MeSH
- Klebsiella pneumoniae účinky léků MeSH
- laktáty chemie MeSH
- mikrobiální testy citlivosti MeSH
- molekulová hmotnost MeSH
- nosiče léků chemie MeSH
- polyestery chemie MeSH
- polyethylenglykoly chemie MeSH
- polyvinylalkohol chemie MeSH
- příprava léků metody MeSH
- Pseudomonas aeruginosa účinky léků MeSH
- rozpustnost MeSH
- Staphylococcus aureus účinky léků MeSH
- tobolky MeSH
- uvolňování léčiv MeSH
- velikost částic MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
Significant improvements in the voltammetric determination of β-carotene (BCA) have been achieved, mainly by the replacement of toxic dichloromethane with acetone and using non-mercury electrode. The respective procedure is based on anodic oxidation of BCA at a gold electrode in the disc configuration, when using square-wave voltammetry in pure acetone (99.8%) with 0.1 mol L-1 LiClO4 as the supporting electrolyte. The method comprises extraction of the analyte from the sample with acetone, thus avoiding the usually used highly toxic solvents. Analytically, it can be characterized by a linear range from 6.0 × 10-6 to 5.9 × 10-4 mol L-1 with regression equation Ipa = 0.0184c -0.1631 and correlation coefficient, R2 = 0.9998, limits of detection and quantification LOD = 1.6 × 10-6 mol L-1 and LOQ = 5.4 × 10-6 mol L-1, respectively; both being obtained at a potential step of 5 mV, with the pulse amplitude of 25 mV, and a frequency of 80 Hz. After optimization, the method was evaluated in series of analyses; namely, with two samples of vegetables and two pharmaceutical preparations (capsules), when the results could be compared to those of a reference spectrophotometric method. Due to a simple instrumentation, including sample preparation, the voltammetric method for the determination of BCA can be recommended as a quick screening assay in food and pharmaceutical analysis.
- MeSH
- beta-karoten MeSH
- elektrochemie MeSH
- elektrody MeSH
- tobolky MeSH
- zelenina * MeSH
- zlato * MeSH
- Publikační typ
- časopisecké články MeSH
The effectiveness of cell transplantation can be improved by optimization of the transplantation site. For some types of cells that form highly oxygen-demanding tissue, e.g., pancreatic islets, a successful engraftment depends on immediate and sufficient blood supply. This critical point can be avoided when cells are transplanted into a bioengineered pre-vascularized cavity which can be formed using a polymer scaffold. In our study, we tested surface-modified poly(lactide-co-caprolactone) (PLCL) capsular scaffolds containing the pro-angiogenic factor VEGF. After each modification step (i.e., amination and heparinization), the surface properties and morphology of scaffolds were characterized by ATR-FTIR and XPS spectroscopy, and by SEM and AFM. All modifications preserved the gross capsule morphology and maintained the open pore structure. Optimized aminolysis conditions decreased the Mw of PLCL only up to 10% while generating a sufficient number of NH2 groups required for the covalent immobilization of heparin. The heparin layer served as a VEGF reservoir with an in vitro VEGF release for at least four weeks. In vivo studies revealed that to obtain highly vascularized PLCL capsules (a) the optimal VEGF dose for the capsule was 50 μg and (b) the implantation time was four weeks when implanted into the greater omentum of Lewis rats; dense fibrous tissue accompanied by vessels completely infiltrated the scaffold and created sparse granulation tissue within the internal cavity of the capsule. The prepared pre-vascularized pouch enabled the islet graft survival and functioning for at least 50 days after islet transplantation. The proposed construct can be used to create a reliable pre-vascularized pouch for cell transplantation.
- MeSH
- bioinženýrství * MeSH
- experimentální diabetes mellitus chemicky indukované metabolismus patologie MeSH
- fyziologická neovaskularizace * MeSH
- injekce intraperitoneální MeSH
- krevní glukóza analýza MeSH
- krysa rodu rattus MeSH
- molekulární struktura MeSH
- polyestery chemie metabolismus MeSH
- potkani inbrední LEW MeSH
- streptozocin aplikace a dávkování MeSH
- tobolky chemie metabolismus MeSH
- transplantace Langerhansových ostrůvků * MeSH
- vaskulární endoteliální růstové faktory chemie metabolismus MeSH
- velikost částic MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- mužské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
