Phospholipid-containing films for improved drug release

2021 ◽  
pp. 30-33
Author(s):  
Jiahao Huang ◽  
◽  
Shawn Wettig
Keyword(s):  
Water Solubility ◽  
Aqueous Media ◽  
Active Pharmaceutical Ingredients ◽  
Natural Sources ◽  
Pharmaceutical Ingredients ◽  
Alternative Approach ◽  
Poor Water Solubility ◽  
Dissolution Efficiency ◽  
Oral Films ◽  
Liquid Liquid Phase Separation

Phospholipids from natural sources can delay liquid-liquid phase separation and improve supersaturation for active pharmaceutical ingredients with poor water-solubility in aqueous media. Researchers have developed oral films containing phospholipids to enhance the dissolution efficiency of hydrophobic pharmaceutical ingredients. Phospholipid-based oral films provide an alternative approach for compounding pharmacies to formulate drugs with poor water solubility.

scholarly journals Highly water soluble room temperature superionic liquids of APIs

2017 ◽  
Vol 41 (15) ◽  
pp. 6986-6990 ◽  
Author(s):  
Gonçalo V. S. M. Carrera ◽  
Miguel M. Santos ◽  
Alexandra Costa ◽  
Luis Paulo N. Rebelo ◽  
Isabel M. Marrucho ◽  
...  
Keyword(s):  
Room Temperature ◽  
Water Solubility ◽  
Water Soluble ◽  
Active Pharmaceutical Ingredients ◽  
Pharmaceutical Ingredients ◽  
Straightforward Approach

Herein a straightforward approach for the enhancement of the water solubility of common antibiotic and NSAID active pharmaceutical ingredients (APIs) is presented.

scholarly journals The Crystallization of Active Pharmaceutical Ingredients with Low Melting Points in the Presence of Liquid–Liquid Phase Separation

Crystals ◽  
2021 ◽  
Vol 11 (11) ◽  
pp. 1326
Author(s):  
Wei Han Lin ◽  
Zai-Qun Yu ◽  
Pui Shan Chow ◽  
Reginald Beng Hee Tan
Keyword(s):  
Phase Separation ◽  
Liquid Phase ◽  
Hydroxypropyl Methylcellulose ◽  
Tween 80 ◽  
Liquid Phase Separation ◽  
Water Mixture ◽  
Active Pharmaceutical Ingredients ◽  
Melting Points ◽  
Pharmaceutical Ingredients ◽  
Liquid Liquid Phase Separation

Liquid–liquid phase separation (LLPS) during the crystallization of active pharmaceutical ingredients (APIs) often causes agglomeration and other quality issues in crystal products; thus, it should be avoided if possible. However, LLPS in the crystallization of APIs with low melting points cannot be circumvented in some cases due to yield considerations. The crystallization of ibuprofen in an ethanol/water mixture was studied to explore methods to reduce agglomeration in the presence of LLPS. It was found that unseeded crystallization produced agglomerates when LLPS took place. The two liquid phases resulting from LLPS underwent LLPS again when they were cooled separately, indicating the dynamic nature of LLPS. Seeding and seed ageing at a low supersaturation were very effective in mitigating agglomeration. The effects of two widely used surfactants, i.e., Tween 80 and hydroxypropyl methylcellulose (HPMC), on LLPS and crystallization were confirmed preliminarily. More work needs to be conducted to explore their usefulness in LLPS handling. The findings and techniques presented in this study may be applicable to the crystallization of other APIs with low melting points.

scholarly journals A Pediatrics Utilization Study in The Netherlands to Identify Active Pharmaceutical Ingredients Suitable for Inkjet Printing on Orodispersible Films

Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 164 ◽  
Author(s):  
J. Carolina Visser ◽  
Lisa Wibier ◽  
Olga Kiefer ◽  
Mine Orlu ◽  
Jörg Breitkreutz ◽  
...  
Keyword(s):  
The Netherlands ◽  
Inkjet Printing ◽  
Water Solubility ◽  
Anatomical Therapeutic Chemical ◽  
High Water ◽  
Water Soluble ◽  
Active Pharmaceutical Ingredients ◽  
Formulation Development ◽  
Orodispersible Films ◽  
Pharmaceutical Ingredients

Background: The use of medication in pediatrics, children aged 0–5 years, was explored so as to identify active pharmaceutical ingredients (APIs) suitable for inkjet printing on a plain orodispersible film (ODF) formulation in a pharmacy. Methods: The database IADB.nl, containing pharmacy dispensing data from community pharmacies in the Netherlands, was used to explore medication use in the age group of 0–5 years old, based on the Anatomical Therapeutic Chemical classification code (ATC code). Subsequently, a stepwise approach with four exclusion steps was used to identify the drug candidates for ODF formulation development. Results: there were 612 Active Pharmaceutical Ingredients (APIs) that were dispensed to the target group, mostly antibiotics. Of the APIs, 221 were not registered for pediatrics, but were used off-label. After the exclusion steps, 34 APIs were examined regarding their suitability for inkjet printing. Almost all of the APIs were sparingly water soluble to practically insoluble. Conclusion: Pharmaceutical inkjet printing is a suitable new technique for ODF manufacturing for pediatric application, however the maximal printed dose as found in the literature remained low. From the selected candidates, only montelukast shows a sufficiently high water-solubility to prepare a water-based solution. To achieve higher drug loads per ODF is ambitious, but is theoretically possible by printing multiple layers, using highly water-soluble APIs or highly loaded suspensions.

scholarly journals Development of Novel API-ILs for the Optimization of Anti-Alzheimer Drugs

Proceedings ◽  
2018 ◽  
Vol 9 (1) ◽  
pp. 47
Author(s):  
Belén Tornero ◽  
Verónica Fernández-Stefanuto ◽  
Emilia Tojo ◽  
Pedro Besada ◽  
Carmen Terán
Keyword(s):  
Ionic Liquids ◽  
Water Solubility ◽  
Acetylcholinesterase Inhibitors ◽  
Current Treatment ◽  
New Drugs ◽  
Active Pharmaceutical Ingredients ◽  
Optimal Parameters ◽  
Drug Bioavailability ◽  
Pharmaceutical Ingredients ◽  
Cholinergic Neurotransmission

The current treatment of Alzheimer’s disease (AD) is mainly focused on enhancing the cholinergic neurotransmission by means of acetylcholinesterase inhibitors (AChEIs). Therefore, there is a growing interest in the development of novel AChEIs. New drugs should not only be able to inhibit the enzyme but also to show optimal parameters of solubility and permeability, since they affect drug bioavailability. Considering the potential advantages of transforming active pharmaceutical ingredients (APIs) into ionic liquids (ILs), five API-ILs derived from two AChEIs, tacrine and a donepezil analogue, were synthesized. The water solubility of these novel API-ILs was analyzed.

NMR Studies of the Inclusion Complexes Between Ezetimibe and Cyclodextrins

2018 ◽  
Vol 69 (7) ◽  
pp. 1838-1841
Author(s):  
Hajnal Kelemen ◽  
Angella Csillag ◽  
Bela Noszal ◽  
Gabor Orgovan
Keyword(s):  
Inclusion Complex ◽  
Inclusion Complexes ◽  
Water Solubility ◽  
Solution Nmr ◽  
Spectroscopic Techniques ◽  
Nmr Studies ◽  
The Poor ◽  
Poor Water Solubility

Ezetimibe, the antihyperlipidemic drug of poor bioavailability was complexed with native and derivatized cyclodextrins.The complexes were characterized in terms stability, stoichiometry and structure using various 1D and 2D solution NMR spectroscopic techniques. The complexes were found to be of moderate stability (logK[3). The least stable inclusion complex is formed with b-cyclodextrin, while the ezetimibe-methylated-b--cyclodextrin has a 7-fold higher stability. The results can be useful to improve the poor water-solubility and the concomitant bioavailability of ezetimibe.

Reversed-Phase High Performance Liquid Chromatographic Analysis of Three First Line Anti-Tuberculosis Drugs

2019 ◽  
Vol 69 (12) ◽  
pp. 3590-3592
Author(s):  
Nela Bibire ◽  
Romeo Iulian Olariu ◽  
Luminita Agoroaei ◽  
Madalina Vieriu ◽  
Alina Diana Panainte ◽  
...  
Keyword(s):  
High Performance ◽  
Biological Fluids ◽  
Gradient Elution ◽  
High Performance Liquid Chromatographic ◽  
Reversed Phase ◽  
Assay Method ◽  
Active Pharmaceutical Ingredients ◽  
First Line ◽  
Pharmaceutical Ingredients ◽  
Liquid Chromatographic

Active pharmaceutical ingredients such as isoniazid, pyrazinamide and rifampicin are among the most important first-line anti-tuberculosis drugs. A simple, rapid and sensitive reversed phase-high performance liquid chromatographic assay method for the simultaneous determination of isoniazid, pyrazinamide and rifampicin has been developed. Separation of the interest compounds was achieved in a 10 min chromatographic run in gradient elution mode on a Zorbax SB-C18 stainless steel column (150 � 4 mm, 5 mm) using a guard column containing the same stationary phase. The gradient elution was carried out with a mobile phase of 10% CH3CN aqueous solution for channel A and 50% CH3CN in pH = 6.8 phosphate buffer (20 mM), to which 1.5 mL triethylamine were added for channel B. Quantification of the analyzed substances was carried out spectrophotometrically at 269 nm. Detection limits of 0.48 mg/L for isoniazid, 0.52 mg/L for pyrazinamide and 0.48 mg/L for rifampicin were established for the developed assay method. The present work showed that the proposed analysis method was advantageous for simple and rapid analysis of the active pharmaceutical ingredients in pharmaceuticals and biological fluids.

scholarly journals Numaswitch: an efficient high-titer expression platform to produce peptides and small proteins

AMB Express ◽  
2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Bach-Ngan Nguyen ◽  
Florian Tieves ◽  
Thomas Rohr ◽  
Hilke Wobst ◽  
Felix S. Schöpf ◽  
...  
Keyword(s):  
Fermentation Broth ◽  
High Titer ◽  
New Technology ◽  
Active Pharmaceutical Ingredients ◽  
Pharmaceutical Ingredients ◽  
Expression Platform ◽  
Small Proteins ◽  
Production Platform ◽  
Β Amyloid ◽  
Cost Efficient

AbstractThe production of peptides as active pharmaceutical ingredients (APIs) by recombinant technologies is of emerging interest. A reliable production platform, however, is still missing due the inherent characteristics of peptides such as proteolytic sensitivity, aggregation and cytotoxicity. We have developed a new technology named Numaswitch solving present limitations. Numaswitch was successfully employed for the production of diverse peptides and small proteins varying in length, physicochemical and functional characteristics, including Teriparatide, Linaclotide, human β-amyloid and Serum amyloid A3. Additionally, the potential of Numaswitch for a cost-efficient commercial production is demonstrated yielding > 2 g Teriparatide per liter fermentation broth in a quality meeting API standard.

scholarly journals Diagnosis of Agglomeration and Crystallinity of Active Pharmaceutical Ingredients in Over the Counter Headache Medication by Electrospray Laser Desorption Ionization Mass Spectrometry Imaging

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 610
Author(s):  
Mariann Inga Van Meter ◽  
Salah M. Khan ◽  
Brynne V. Taulbee-Cotton ◽  
Nathan H. Dimmitt ◽  
Nathan D. Hubbard ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Mass Spectrometry Imaging ◽  
Laser Desorption ◽  
Ionization Mass Spectrometry ◽  
Ionization Mass ◽  
Active Pharmaceutical Ingredients ◽  
Laser Desorption Ionization ◽  
Over The Counter ◽  
Pharmaceutical Ingredients ◽  
Desorption Ionization

Agglomeration of active pharmaceutical ingredients (API) in tablets can lead to decreased bioavailability in some enabling formulations. In a previous study, we determined that crystalline APIs can be detected as agglomeration in tablets formulated with amorphous acetaminophen tablets. Multiple method advancements are presented to better resolve agglomeration caused by crystallinity in standard tablets. In this study, we also evaluate three “budget” over-the-counter headache medications (subsequently labeled as brands A, B, and C) for agglomeration of the three APIs in the formulation: Acetaminophen, aspirin, and caffeine. Electrospray laser desorption ionization mass spectrometry imaging (ELDI-MSI) was used to diagnose agglomeration in the tablets by creating molecular images and observing the spatial distributions of the APIs. Brand A had virtually no agglomeration or clustering of the active ingredients. Brand B had extensive clustering of aspirin and caffeine, but acetaminophen was observed in near equal abundance across the tablet. Brand C also had extensive clustering of aspirin and caffeine, and minor clustering of acetaminophen. These results show that agglomeration with active ingredients in over-the-counter tablets can be simultaneously detected using ELDI-MS imaging.

scholarly journals Sulfanyl Porphyrazines with Morpholinylethyl Periphery—Synthesis, Electrochemistry, and Photocatalytic Studies after Deposition on Titanium(IV) Oxide P25 Nanoparticles

Molecules ◽  
2021 ◽  
Vol 26 (8) ◽  
pp. 2280
Author(s):  
Tomasz Koczorowski ◽  
Wojciech Szczolko ◽  
Anna Teubert ◽  
Tomasz Goslinski
Keyword(s):  
Diclofenac Sodium ◽  
2D Nmr ◽  
Oxide Nanoparticles ◽  
Electrochemical Studies ◽  
Macrocyclic Compounds ◽  
Active Pharmaceutical Ingredients ◽  
Pharmaceutical Ingredients ◽  
Vis Spectroscopy ◽  
Singlet Oxygen Quencher ◽  
Nmr Techniques

The syntheses, spectral UV–Vis, NMR, and electrochemical as well as photocatalytic properties of novel magnesium(II) and zinc(II) symmetrical sulfanyl porphyrazines with 2-(morpholin-4-yl)ethylsulfanyl peripheral substituents are presented. Both porphyrazine derivatives were synthesized in cyclotetramerization reactions and subsequently embedded on the surface of commercially available P25 titanium(IV) oxide nanoparticles. The obtained macrocyclic compounds were broadly characterized by ESI MS spectrometry, 1D and 2D NMR techniques, UV–Vis spectroscopy, and subjected to electrochemical studies. Both hybrid materials, consisting of porphyrazine derivatives embedded on the titanium(IV) oxide nanoparticles’ surface, were characterized in terms of particle size and distribution. Next, they were subjected to photocatalytic studies with 1,3-diphenylisobenzofuran, a known singlet oxygen quencher. The applicability of the obtained hybrid material consisting of titanium(IV) oxide P25 nanoparticles and magnesium(II) porphyrazine derivative was assessed in photocatalytic studies with selected active pharmaceutical ingredients, such as diclofenac sodium salt and ibuprofen.

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