REVIEW: AN EFFORTS TO INCREASE THE SOLUBILITY AND DISSOLUTION OF ACTIVE PHARMACEUTICAL INGREDIENTS

The most significant aspect of a drug's physicochemical nature is its solubility. If the medicine is in a dissolved form, it can dissolve and enter the membrane, resulting in a therapeutic effect. The pharmacokinetic phase of the drug in the body, which includes absorption, distribution, metabolism, and excretion, will be correlated with solubility. Some medications, however, have a low solubility. To obtain a therapeutic impact, an effort must be made to increase the drug's solubility. Based on the literature research, the goal of this paper is to explain approaches that can be utilized to improve solubility. In general, physical, chemical, and micelle formation efforts can all be used it to enhance solubility. Particle size reduction, crystal shape modification, and the utilization of matrices in the disperse phase are examples of physical alterations. pH adjustment, buffering, salt formation, complexation, and derivatization all are examples of chemical alterations. The employment of supercritical processes in solutions and also excipients such as surfactants, cosolvents, stabilizing solutions, and others are examples of how micelle formation can be modified.

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Application Of Power Ultrasound For Nano-Particle Size Reduction Of Active Pharmaceutical Ingredients

International Journal on Applied Bio-Engineering ◽

10.18000/ijabeg.10027 ◽

2008 ◽

Vol 2 (1) ◽

pp. 66-76

Author(s):

Annam Renita A ◽

Shyam Saxena ◽

Prabhu K. Shukla

Keyword(s):

Particle Size ◽

Size Reduction ◽

Nano Particle ◽

Active Pharmaceutical Ingredients ◽

Particle Size Reduction ◽

Power Ultrasound ◽

Pharmaceutical Ingredients

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Degradation of lipid based drug delivery formulations during nebulization

10.1101/2021.03.16.21253714 ◽

2021 ◽

Author(s):

David M. Klein ◽

Albert Poortinga ◽

Frank M. Verhoeven ◽

Daniel Bonn ◽

Sylvestre Bonnet ◽

...

Keyword(s):

Drug Delivery ◽

High Frequency ◽

The Body ◽

Target Area ◽

Active Pharmaceutical Ingredients ◽

Drug Formulations ◽

Pharmaceutical Ingredients ◽

Inhalation Devices ◽

Lipid Nanoparticle ◽

Jet Nebulizers

AbstractEncapsulating pharmaceuticals in protective lipid based nanoparticles, and nebulizing them towards the target area in the body offers a range of clinical advantages. However, the process of nebulization might possibly damage sensitive nanoparticle structures, such as liposomes, resulting in loss of active pharmaceutical ingredients. We compare this loss for two types of lung inhalation devices: high-frequency piezo-actuated vibrating mesh nebulizers and non-actuated continuous jet nebulizers. We find that vibrating mesh nebulizers cause model liposomes to release more than ten times as much encapsulated material as the continuous jet nebulizers because the energies involved in nebulization are much larger. This result highlights the importance of applying a mild nebulization technology when administering shear-sensitive drug formulations such as lipid nanoparticle based drugs to the lungs.

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A review on emerging micropollutants: sources, environmental concentration and toxicity

Bionatura ◽

10.21931/rb/2021.06.04.29 ◽

2021 ◽

Vol 6 (4) ◽

pp. 2305-2325

Author(s):

Vadiraj K.T ◽

Raghu Ram Achar ◽

Sindhuja Siriger

Keyword(s):

Endocrine Disruptors ◽

Crop Protection ◽

Endocrine System ◽

Emerging Pollutants ◽

Active Pharmaceutical Ingredients ◽

Environmental Concentration ◽

Pharmaceutical Ingredients ◽

Physical Chemical ◽

Living Things ◽

Pollutant Sources

Every minute, the environment is filled with pollutants of various types, including physical, chemical, and biological. A new threat has emerged in recent years due to human activity, which is of significant concern. These pollutants are not like conventional pollutants but can alter the physiology of living things, and hence these are named emerging pollutants. The pollutant sources include crop protection chemicals, personal care products, antimicrobial mixtures, active pharmaceutical ingredients (API). These compounds are biologically crucial because their minute quantity can also disrupt an individual's endocrine system, and hence they are also called endocrine disruptors. This current work reviews many aspects, including source, problems, and legislative solutions that have been farmed to cope with the current situation of emerging micropollutants.

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

Revista de Chimie ◽

10.37358/rc.18.12.6799 ◽

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.

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Trapping liquid drugs inside crystals

Acta Crystallographica Section A Foundations and Advances ◽

10.1107/s2053273314090159 ◽

2014 ◽

Vol 70 (a1) ◽

pp. C984-C984

Author(s):

Alessia Bacchi ◽

Davide Capucci ◽

Paolo Pelagatti

Keyword(s):

Human Health ◽

Crystal Engineering ◽

Room Temperature ◽

The Body ◽

New Materials ◽

Active Molecule ◽

Crystalline Materials ◽

Pharmaceutical Ingredients ◽

Solid Dosage ◽

Intellectual Properties

The objective of this work is to embed liquid or volatile pharmaceuticals inside crystalline materials, in order to tune their delivery properties in medicine or agrochemistry, and to explore new regulatory and intellectual properties issues. Liquid or volatile formulations of active pharmaceutical ingredients (APIs) are intrinsically less stable and durable than solid forms; in fact most drugs are formulated as solid dosage because they tend to be stable, reproducible, and amenable to purification. Most drugs and agrochemicals are manufactured and distributed as crystalline materials, and their action involves the delivery of the active molecule by a solubilization process either in the body or on the environment. However some important compounds for the human health or for the environment occur as liquids at room temperature. The formation of co-crystals has been demonstrated as a means of tuning solubility properties of solid phases, and therefore it is widely investigated by companies and by solid state scientists especially in the fields of pharmaceuticals, agrochemicals, pigments, dyestuffs, foods, and explosives. In spite of this extremely high interest towards co-crystallization as a tool to alter solubility, practically no emphasis has been paid to using it as a means to stabilize volatile or labile or low-melting products. In this work we trap and stabilize volatile and liquid APIs and agrochemicals in crystalline matrices by engineering suitable co-crystals. These new materials alter the physic state of the active ingredients allowing to expand the phase space accessible to manufacturing and delivery. We have defined a benchmark of molecules relevant to human health and environment that have been combined with suitable partners according to the well known methods of crystal engineering in order to obtain cocrystals. The first successful results will be discussed; the Figure shows a cocrystal of propofol, a worldwide use anesthetic.

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

AMB Express ◽

10.1186/s13568-021-01204-w ◽

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.

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

Molecules ◽

10.3390/molecules26030610 ◽

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.

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

Molecules ◽

10.3390/molecules26082280 ◽

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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US trade policy is putting at risk the sustainability of the generic/biosimilar industry and the drug supply chain

Journal of Generic Medicines The Business Journal for the Generic Medicines Sector ◽

10.1177/1741134321994316 ◽

2021 ◽

pp. 174113432199431

Author(s):

María Fabiana Jorge

Keyword(s):

Supply Chain ◽

Trade Policy ◽

Pharmaceutical Products ◽

Drug Supply ◽

Active Pharmaceutical Ingredients ◽

Pharmaceutical Ingredients ◽

Us Trade Policy ◽

Drug Supply Chain ◽

Security Concern ◽

The U.S

With the outbreak of the Coronavirus there is a new realization of the vulnerabilities of the U.S. drug supply chain. However, while such concerns may have been amplified by the pandemic, they preceded Covid-19 and were well documented before 2020. Indeed, in past years the U.S. Congress held several hearings addressing potential vulnerabilities in the U.S. drug supply chain, in part due to the increasing dependency on China as a dominant supplier of active pharmaceutical ingredients (APIs) and some finished pharmaceutical products. These vulnerabilities go well beyond health policy and constitute a national security concern. The article addresses how U.S. trade policy plays a significant role in shaping the pharmaceutical industry at home and abroad and is in part responsible for some of the current vulnerabilities of the U.S. drug supply chain.

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