The choice of method of introduction of active substances into the basis of the cream for the treatment of acne and demodecosis

Benzyl Benzoate ◽

Optimal Method ◽

Important Place ◽

Dermatological Diseases ◽

Active Substances

Among dermatological diseases demodicosis and acne occupy a very important place. The incidence of demodicosis is more than 5% and ranks seventh in frequency among dermatological diseases. It is known that demodicosis can turn into acne. Treatment of demodicosis and acne does not lose its relevance. This medical problem can be solved through the development of the composition and technology of a soft drug of complex action with the content of active substances used to treat these diseases. Since in dermatology for external use the optimal soft medicines is a cream (taking into account the medical and biological requirements for the drug for the treatment of this disease), we have developed the composition of the base, which is the rheological properties of the cream. The aim of the work is to substantiate the optimal method of introducing active pharmaceutical ingredients into the basis of a soft medicines. Materials and research methods – metronidazole, benzyl benzoate, benzoyl peroxide, emulsion base. When choosing the optimal method of introduction of active pharmaceutical ingredients to the base used pharmaco-technological research methods (homogeneity of the content of API in the base). Used a microscope with a photoresist (microscope – OLYMPUS BX-41, photoresist – OLYMPUS U-CMAD3, Japan). Active pharmaceutical ingredients was added to the base in the form of a suspension with glycerol. According to previous studies, we found that propylene glycol and polyethylene oxide were used to obtain the suspension. Studies have shown that in the process of storage for 6 months at room temperature there is a stratification of the base, in order to improve the stability of the composition of the developed cream, we introduced glycerin. Experimental studies have shown that active pharmaceutical ingredients in the form of a suspension must be introduced into the base alternately: a suspension of metronidazole, a suspension of benzoyl peroxide. After bringing the mass to homogeneity, benzyl benzoate was finally introduced. We studied 8 samples with different sequence of administration of active substances in suspension with glycerol, sample № 2 in the study showed the best results of homogeneity of the suspension, so this method we used in further studies. Experimental studies have established the procedure for the introduction of active pharmaceutical ingredients in the form of a suspension to the base: a suspension of metronidazole, a suspension of benzoyl peroxide and, last but not least, benzyl benzoate. The results of the research make it possible to develop a rational technology for the production (manufacture) of a treated soft medicines with metronidazole, benzyl benzoate and benzoyl peroxide for dermatology.

Technology administration active substance in the ointment base

Farmatsevtychnyi zhurnal ◽

10.32352/0367-3057.1.15.02 ◽

2019 ◽

pp. 38-42

Author(s):

V. V. Trochimchuk ◽

V. V. Shmatenko ◽

V. O. Tarasenko ◽

A. O. Drozdova

Keyword(s):

Antimicrobial Activity ◽

Military Medicine ◽

Experimental Studies ◽

Optimal Method ◽

Solid Agar ◽

Ointment Base ◽

Important Challenge ◽

Technological Route

The problem of expanding the range of medicines that are used for the topical treatment of wound process, remains an important challenge for practical military medicine. In this aspect, there are topical ointments combining development for use in the first phase of wound process, which has a complex influence on the pathological processes and exhibits antibacterial, anti-inflammatory and local anesthetic activity. The aim of the study was substantiation of technological route of administration of the active pharmaceutical ingredients in the ointment base, depending on the antimicrobial activity of model compositions. The study included a model sample of ointment bases, cooked on a hydrophilic carrier containing active pharmaceutical ingredients – ofloxacin, nimesulide and lidocaine. Microbiological studies were performed by difution on solid agar medium, which is based on the ability of substances to inhibit the growth antibakterial microorganisms. Comparative analysis of experimental studies showed that the samples of ointments, which are based whith the active pharmaceutical ingredients ofloxacin, nimesulide and lidocaine was injected as a solution in DMSO showed the highest antimicrobial activity. As a result of study on the antimicrobial activity of ointments model samples determined that the optimal method of administering the basis AFI – ofloxacin, nimesulide and lidocaine – a method of administering them in the form of a solution in DMSO.

Drugs, Active Ingredients and Diseases Database in Spanish. Augmenting the Resources for Analyses on Drug–Illness Interactions

Data ◽

10.3390/data6010003 ◽

2021 ◽

Vol 6 (1) ◽

pp. 3

Author(s):

Irene López-Rodríguez ◽

César F. Reyes-Manzano ◽

Israel Reyes-Ramírez ◽

Tania J. Contreras-Uribe ◽

Lev Guzmán-Vargas

Keyword(s):

Side Effects ◽

Near Field ◽

Quantitative Information ◽

Sources Of Information ◽

Active Ingredients ◽

Field Exposure ◽

Essential Information ◽

Active Substances

Quantitative and qualitative data on active-ingredient drug composition are essential information for characterizing near-field exposure of consumers to product-related chemicals, among other things. Equally as important is the characterization of the relationship between one or many active ingredients in terms of the diseases they are prescribed for. Such evaluations, however, require quantitative information at different anatomical levels. To complement the available sources of information on active substances and diseases, we have designed a database with enough versatility to potentially be used in a variety of analyzes. By using information provided by a well-established online pharmacological dictionary, we present a database with 11 tables which are easy to access and manipulate. Specifically, we present datasets containing the details of 12,827 marketed drug products, 40,164 diseases, 6231 active pharmaceutical ingredients and 4093 side effects. We exemplify the usefulness of our database with three simple visualizations, which confirm the importance of the data for quantifying the complexity in the associations among active substances, diseases and side effects. Although there are databases with detailed information on active substances and diseases, none of them can be found in Spanish. Our work presents an option that contributes substantially to obtaining well classified information in order to evaluate the roles of active pharmaceutical ingredients, diseases and side effects. These datasets also provide information about clinical and pharmacological groupings which may be useful for clinical and academic researchers. The database will be regularly updated and extended with the newly available Virtual Medicinal Products.

The quality assurance of the medicinal composition using the “Antimicrobial activity” indicator

Upravlìnnâ ekonomìka ta zabezpečennâ âkostì v farmacìï ◽

10.24959/uekj.21.2 ◽

2021 ◽

pp. 27-34

Author(s):

A. S. Koval ◽

S. V. Birukova ◽

Y. V. Voyda

Keyword(s):

Antimicrobial Activity ◽

Benzoyl Peroxide ◽

Skin Diseases ◽

Physical And Mechanical Properties ◽

Tween 80 ◽

Rheological Parameters ◽

Rapid Improvement ◽

Common Skin

The aim of the work is to determine the spectrum and strenght of antimicrobial activity of the studied compositions, to compare them with the activity of substancesand to select the most optimal concentration for further combination with each other. Topicality. Nowadays, one of the most common skin diseases is acne and demodicosis, the manifestations of which can be mild (comedones in seborrheic areas), more noticeable (papules-pustular rash) and severe (large cyanotic infiltrative elements in the back, prone to abscessing and scarring). The prevalence of acne and demodicosis currently reaches 90%. With these skin pathologies, it is desirable to use safe and effective drugs for external therapy, which provide rapid improvement of the skin (reduction of inflammation without side effects) to obtain a rapid and high-quality therapeutic effect. In the course of our research, we selected 3 active pharmaceutical ingredients (APIs): metronidazole, benzyl benzoate and benzoyl peroxide - according to the purpose of ICD-10 and their effectiveness in these pathologies. Mild medicines have an advantage over dermatological diseases such as acne and demodicosis because the use of soft medicines is local, namely a targeted effect on the microbial microflora. At present for production of soft medicines for local application such substances as macromolecular compounds are widely used, plasticizers, surfactants,etc. When creating a drug composition, a study was conducted aimed at obtaining soft medicines with certain consumer properties, in particular physicochemical (pH, osmotic activity, homogeneity,etc.) , physical and mechanical properties (rheological parameters). Materials for the study – soft medicines based on cetyl alcohol, Emulgade Sucro Plus, Polyvinylpyrrolidone, Carboxymethylcellulose, Tween 80, Triethanolamine, Propylene glycol, vaseline oil, which as (API) contains metronidazole, benzoyl peroxide, benzylbenzene. The specific antimicrobial activity of the samples was tested in accordance with Order № 167 of the Ministry of Health of Ukraine dated 05.04.2007 by the standard macromethod of serial dilutions in liquid nutrient medium and by the method of diffusion into agar. The minimum inhibitory concentration (MIC) of API (substrates) was determined. Results. The studied compositions of soft medicines and substrates revealed to presence of antibacterial (bacteriostatic) action against the test strains of microorganisms. Conclusions. The test of the compositions of soft medicines and the substance revealed the presence of a slight antibacterial (bacteriostatic) effect against the test strains of microorganisms. Key words: antimicrobial activity; active pharmaceutical ingredients (API); excipients; soft dosage form

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 ◽

First Line ◽

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.

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 ◽

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.

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 ◽

Laser Desorption Ionization ◽

Over The Counter ◽

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.

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 ◽

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.

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

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

10.1177/1741134321994316 ◽

2021 ◽

pp. 174113432199431

Author(s):

María Fabiana Jorge

Keyword(s):

Supply Chain ◽

Trade Policy ◽

Pharmaceutical Products ◽

Drug Supply ◽

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.