scholarly journals Structure of the active pharmaceutical ingredient bismuth subsalicylate

2021 ◽  
Author(s):  
Erik Svensson Grape ◽  
Victoria Rooth ◽  
Mathias Nero ◽  
Tom Willhammar ◽  
A. Ken Inge
Keyword(s):  
Active Pharmaceutical Ingredient ◽  
Bismuth Subsalicylate

scholarly journals Structure of the active pharmaceutical ingredient bismuth subsalicylate

2021 ◽  
Author(s):  
Erik Svensson Grape ◽  
Victoria Rooth ◽  
Mathias Nero ◽  
Tom Willhammar ◽  
A. Ken Inge
Keyword(s):  
Structure Determination ◽  
Three Dimensional ◽  
Active Pharmaceutical Ingredient ◽  
Bismuth Subsalicylate ◽  
Pharmaceutical Ingredients ◽  
Transmission Electron ◽  
Small Crystals ◽  
Scanning Transmission ◽  
H Pylori

Structure determination of pharmaceutical compounds is invaluable for drug development but is challenging for those that form as small crystals with defects. Bismuth subsalicylate (BSS), among the most commercially significant bismuth compounds, is an active ingredient in over-the-counter medications such as Pepto-Bismol, used to treat dyspepsia and H. pylori infections. Despite its century-long history, the structure has remained unknown. Three-dimensional electron diffraction and hierarchical clustering analysis were applied on select data from ordered crystals, revealing a layered structure. In other less ordered crystals, high-resolution scanning transmission electron microscopy revealed variations in the stacking of layers. Together, these modern electron crystallography techniques provide a new toolbox for structure determination of active pharmaceutical ingredients and drug discovery, demonstrated by this study of BSS.

Topical Analgesic Formulations: Following the Transdermal Treatment Paradigm Only?

2019 ◽  
Author(s):  
Jan M Keppel Hesselink
Keyword(s):  
Ad Hoc ◽  
Active Pharmaceutical Ingredient ◽  
Mechanisms Of Action ◽  
Onset Of Action ◽  
Good Tolerability ◽  
Short Commentary ◽  
Topical Analgesics ◽  
The Usa ◽  
Treatment Paradigm ◽  
Topical Analgesic

Topical analgesics are regarded as new inroads to treat peripheral neuropathic pain, with a number of advantages over oral treatments. Topical treatment reduces systemic induced side-effects and have good tolerability, without problems of misuse or abuse, or dependency. Furthermore, the onset of action is fast, mostly within 30 minutes. The mechanism of action of topical analgesics is either via transdermal delivery of the analgesic, or via intradermal mechanisms of action. In the latter case, plasma levels of analgesics in the blood are absent or very low. This perspective is missing in the approach of the ad hoc committee of the National Academies of Sciences, Engineering, and Medicine in the USA, installed by the FDA. In this short commentary, we plead for a more comprehensive approach of topical analgesics, including those formulations which explicitly are not based on transdermal penetration of the active pharmaceutical ingredient, but on intradermal mechanisms of action.

Comparative analysis of business models of top pharmaceutical manufacturing companies: fifi nancial analysis

2020 ◽  
pp. 43-52
Author(s):  
L.E. Yasinskaya ◽  
Keyword(s):  
Comparative Analysis ◽  
Business Models ◽  
Financial Analysis ◽  
Active Pharmaceutical Ingredient ◽  
Pharmaceutical Companies ◽  
Manufacturing Companies ◽  
Revenue Growth ◽  
Commercial Activities ◽  
Pharmaceutical Manufacturers ◽  
Research Procedure

Introduction. Earlier, the comparative analysis of the commercial and investment activities of the companies that play the key roles in the investment processes in the Russian pharmaceutical industry and operate within the four main business models (biotechnological, generic, specialized pharmaceutical companies, active pharmaceutical ingredient (API) manufacturers) has been conducted. No full assessment of the companies’ activitiesis conceivable without a financial analysis of their activities to identify the risks of investment activities. Objective of the study. A detailed comparative analysis of the financial standing of domestic pharmaceutical manufacturers operating within the selected business models for further identification of potential financial risks for investors. Research procedure and article structure. Analysis of RAS statements (forms 1 and 2) of 72 over 500 million revenue companies grouped together as selected business models for the period from 2015 to 2019. Results. The researchers provided a detailed description of the commercial activities of domestic pharmaceutical companies within the business models under consideration. The companies within various business models showed positive revenue growth rates over the past five years. All business models demonstrate consistently high business profitability and a significant share of own capital in the asset profile. Conclusion. The results of the study show the stable financial standing of the pharmaceutical companies within various business models. The biotechnology sector companies that are the most attractive for investments have the highest quality financial standing. The specialized and generic companies show similar consistently strong performance. API manufacturers that the companies with relatively small revenues are actively developing and are attractive to restrained budget investors.

Berberine nanoencapsulation attenuates hallmarks of scoplomine induced Alzheimer's-like disease in rats

2020 ◽  
Vol 15 ◽  
Author(s):  
Samar R. Saleh ◽  
Mariam M. Abady ◽  
Mohammed Nofal ◽  
Nashwa W. Yassa ◽  
Mohamed S. Abdel-latif ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Histopathological Examination ◽  
Memory Function ◽  
Amyloid Β ◽  
Active Pharmaceutical Ingredient ◽  
Isoquinoline Alkaloid ◽  
Drug Uptake ◽  
Male Rats ◽  
Morris Water Maze Test ◽  
Neuroprotective Effects

Background: Berberine (BBR), an isoquinoline alkaloid, acts as a multipotent active pharmaceutical ingredient to counteract several types of dementia based on its numerous pharmacological actions including antioxidant, antiinflammatory, cholesterol-lowering effect, and inhibition of Aβ production and AChE. However, BBR suffers from poor absorption, bioavailability and brain drug uptake. The present study is directed for the formulation and characterization of Chitosan BBR-nanoparticles (BBR-NPs) as well as the estimation of its neuroprotective effects against scopolamine induced cognitive impairments. Methods: BBR-NPs were formulated using ionic gelation method and tripolyphosphate was chosen as a cross linker. Nanoparticles size, zeta potential, encapsulation efficiency and releasing profile were estimated. To investigate the neuroprotective effects, adult fifty six Wistar male rats were randomly distributed into: three control groups, received saline, polyethylene glycol or chitosan- NPs respectively; induced group, received scopolamine (2 mg/ kg, i.p.) and three treated groups were orally administrated BBR (50 mg/ kg), BBR- NP (7 mg/ kg) and donepezil (2.25 mg/ kg, as positive control) followed by scopolamine injection after 40 min, daily for 4 weeks. Morris water maze test, oxidative stress parameters, cholinergic and amyloid-β processing intermediates as well as neuroplasticity markers and histopathological examination were assessed. Results: Our results showed that BBR- NPs were better than BBR and donepezil as BBR- NPs were powerful inhibitory ligands toward AChE and Aβ42 formation and significantly down regulated Tau, iNOS and BACE gene expression in rats’ hippocampus. BBR-NPs administration, at 1/6 of BBR therapeutic recommended dose, significantly improved learning and memory function. This could be accredited to the diminution of oxidative stress and amyloid-β toxicity in addition to the improvement of the neuroplasticity markers. Conclusions: The enhancing effect of BBR- NPs could be related to the enhancing of its bioavailability, absorption and brain drug uptake which need more investigation in future work.

scholarly journals Development and Validation of 2-Azaspiro [4,5] Decan-3-One (Impurity A) in Gabapentin Determination Method Using qNMR Spectroscopy

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1656
Author(s):  
Nataliya E. Kuz’mina ◽  
Sergey V. Moiseev ◽  
Mikhail D. Khorolskiy ◽  
Anna I. Lutceva
Keyword(s):  
Test Procedure ◽  
Active Pharmaceutical Ingredient ◽  
Test Methods ◽  
Intermediate Precision ◽  
Coefficients Of Variation ◽  
Validation Parameters ◽  
Limit Of Quantitation ◽  
Student’S T ◽  
Development And Validation ◽  
Student’S T Test

The authors developed a 1H qNMR test procedure for identification and quantification of impurity A present in gabapentin active pharmaceutical ingredient (API) and gabapentin products. The validation studies helped to determine the limit of quantitation and assess linearity, accuracy, repeatability, intermediate precision, specificity, and robustness of the procedure. Spike-and-recovery assays were used to calculate standard deviations, coefficients of variation, confidence intervals, bias, Fisher’s F test, and Student’s t-test for assay results. The obtained statistical values satisfy the acceptance criteria for the validation parameters. The authors compared the results of impurity A quantification in gabapentin APIs and capsules by using the 1H qNMR and HPLC test methods.

scholarly journals Synthesis and Characterization of Nano-Sized 4-Aminosalicylic Acid–Sulfamethazine Cocrystals

Pharmaceutics ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 277 ◽  
Author(s):  
Ala’ Salem ◽  
Anna Takácsi-Nagy ◽  
Sándor Nagy ◽  
Alexandra Hagymási ◽  
Fruzsina Gősi ◽  
...  
Keyword(s):  
High Power ◽  
Active Pharmaceutical Ingredient ◽  
Polymorphic Form ◽  
Degree Of Crystallinity ◽  
Dissolution Enhancement ◽  
Aminosalicylic Acid ◽  
Nano Technology ◽  
Power Ultrasound ◽  
High Power Ultrasound ◽  
High Degree

Drug–drug cocrystals are formulated to produce combined medication, not just to modulate active pharmaceutical ingredient (API) properties. Nano-crystals adjust the pharmacokinetic properties and enhance the dissolution of APIs. Nano-cocrystals seem to enhance API properties by combining the benefits of both technologies. Despite the promising opportunities of nano-sized cocrystals, the research at the interface of nano-technology and cocrystals has, however, been described to be in its infancy. In this study, high-pressure homogenization (HPH) and high-power ultrasound were used to prepare nano-sized cocrystals of 4-aminosalysilic acid and sulfamethazine in order to establish differences between the two methods in terms of cocrystal size, morphology, polymorphic form, and dissolution rate enhancement. It was found that both methods resulted in the formation of form I cocrystals with a high degree of crystallinity. HPH yielded nano-sized cocrystals, while those prepared by high-power ultrasound were in the micro-size range. Furthermore, HPH produced smaller-size cocrystals with a narrow size distribution when a higher pressure was used. Cocrystals appeared to be needle-like when prepared by HPH compared to those prepared by high-power ultrasound, which had a different morphology. The highest dissolution enhancement was observed in cocrystals prepared by HPH; however, both micro- and nano-sized cocrystals enhanced the dissolution of sulfamethazine.

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