scholarly journals Liposomes, Formulation and Pharmacotechnical Assessment of Anti-Acne Preparations

2019 ◽  
Vol 70 (2) ◽  
pp. 425-430 ◽  
Author(s):  
Alin Laurentiu Tatu ◽  
Alina Mihaela Elisei ◽  
Violeta Bezman ◽  
Camelia Diaconu ◽  
Olimpia Dumitriu Buzia
Keyword(s):  
Controlled Release ◽  
Side Effects ◽  
Benzoyl Peroxide ◽  
Future Study ◽  
Active Ingredients ◽  
Secondary Reactions ◽  
Active Substances

The present study aims at obtaining an efficient local formulation able to ensure both stability and increased penetration of the active ingredients in effective optimal concentrations without side-effects. The novelty of this study is the association in an encapsulated form (liposomes) of tretinoin to benzoyl peroxide as an innovative alternative capable of minimizing side-effects, but preserving at the same time their efficiency. The pharmaceutical forms using liposomes ensure the controlled release of medicine, as a result of the encapsulation of the active substances in the amphiphile structure�liposomes, with the possibility to diminish irritating secondary reactions in various forms of acne, and to provide efficiency, tollerability, conformity and cosmetic acceptability, to be proved in a future study.

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

Data ◽  
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 ◽  
Active Pharmaceutical Ingredients ◽  
Sources Of Information ◽  
Active Ingredients ◽  
Field Exposure ◽  
Essential Information ◽  
Pharmaceutical Ingredients ◽  
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.

Encapsulation of Imatinib in Targeted KIT-5 Nanoparticles for Reducing its Cardiotoxicity and Hepatotoxicity

2020 ◽  
Vol 20 (16) ◽  
pp. 1966-1980
Author(s):  
Jaleh Varshosaz ◽  
Saeedeh Fardshouraki ◽  
Mina Mirian ◽  
Leila Safaeian ◽  
Setareh Jandaghian ◽  
...  
Keyword(s):  
Controlled Release ◽  
Side Effects ◽  
Kinase Inhibitor ◽  
Lymphoblastic Leukemia ◽  
Drug Carrier ◽  
Free Drug ◽  
Jurkat Cells ◽  
Targeted Nanoparticles ◽  
Inhibitor Drug ◽  
Histopathological Results

Background: Using imatinib, a tyrosine kinase inhibitor drug used in lymphoblastic leukemia, has always had limitations due to its cardiotoxicity and hepatotoxicity side effects. The objective of this study is to develop a target-oriented drug carrier to minimize these adverse effects by the controlled release of the drug. Methods: KIT-5 nanoparticles were functionalized with 3-aminopropyltriethoxysilane and conjugated to rituximab as the targeting agent for the CD20 positive receptors of the B-cells. Then they were loaded with imatinib and their physical properties were characterized. The cell cytotoxicity of the nanoparticles was studied by MTT assay in Ramos (CD20 positive) and Jurkat cell lines (CD20 negative) and their cellular uptake was shown by fluorescence microscope. Wistar rats received an intraperitoneal injection of 50 mg/kg of the free drug or targeted nanoparticles for 21 days. Then the level of aspartate Aminotransferase (AST), alanine Aminotransferase (ALT), Alkaline Phosphatase (ALP) and Lactate Dehydrogenase (LDH) were measured in serum of animals. The cardiotoxicity and hepatotoxicity of the drug were also studied by hematoxylin and eosin staining of the tissues. Results: The targeted nanoparticles of imatinib showed to be more cytotoxic to Ramos cells rather than Jurkat cells. The results of the biochemical analysis displayed a significant reduction in AST, ALT, ALP, and LDH levels in animals treated with targeted nanoparticles, compared to the free drug group. By comparison with the free imatinib, histopathological results represented less cardiotoxicity and hepatotoxicity in the animals, which received the drug through the current designed delivery system. Conclusion: The obtained results confirmed that the rituximab targeted KIT-5 nanoparticles are promising in the controlled release of imatinib and could decrease its cardiotoxicity and hepatotoxicity side effects.

Adverse Drug Reactions to acetaminophen and ibuprofen in the paediatric population: analysis of the Italian spontaneous reporting database

2021 ◽  
Vol 17 ◽  
Author(s):  
Valentina Pelliccia ◽  
Serena Rossi ◽  
Ilaria Zollino ◽  
Francesco Quagliarella ◽  
Giuseppe Buonocore
Keyword(s):  
Side Effects ◽  
Spontaneous Reporting ◽  
Soft Tissues ◽  
Population Analysis ◽  
Kidney Injury ◽  
Paediatric Population ◽  
Drug Reactions ◽  
Spontaneous Reporting Database ◽  
Drug Agency ◽  
Active Substances

Background: Acetaminophen and ibuprofen are the only antipyretics drugs approved in children, and are considered safe and well tolerated. However, data regarding the adverse drug reaction (ADR) profile of these drugs in children are scattered. Aim: The aim of our study is to evaluate the ADRs of acetaminophen and ibuprofen through an observational study over a period of 15 years (January 2005-April 2020). Reports of suspected ADRs to the active substances ‘acetaminophen’ and ‘ibuprofen’ are listed and accessible through the Italian spontaneous reporting database (RAM system) by AIFA (Pharmacovigilance of the Italian Drug Agency). Methods: Acetaminophen ADRs in paediatric populations were 15% of cases, with more frequent involvement of skin and soft tissue (54.36%) and gastrointestinal apparatus (44.09%); liver dysfunction accounts for 5.67%. Results: Ibuprofen paediatric ADRs were 26%: skin and soft tissues in 63.16% of cases, gastrointestinal tract in 47.75%, hematemesis and melena in 6.38%; kidney injury in 2.25% of cases. Conclusion: Children aged 2 to 11 are more frequently affected by ADRs than infants and adolescents. The risk of gastrointestinal and renal side effects is significantly higher with ibuprofen. Hepatobiliary side effects are more frequently linked to acetaminophen. Potentially fatal ADRs have been reported sporadically for both drugs.

scholarly journals Risk Assessment of Malakite with the Active Substances Dithianon and Pyrimenthanil

2019 ◽  
pp. 312-314
Author(s):  
Torsten Källqvist ◽  
Merete Grung ◽  
Katrine Borgå ◽  
Hubert Dirven ◽  
Ole Martin Eklo ◽  
...  
Keyword(s):  
Risk Assessment ◽  
Surface Waters ◽  
Plant Protection ◽  
Aquatic Organisms ◽  
Toxicity Tests ◽  
Concentration Addition ◽  
Active Ingredients ◽  
Active Substances ◽  
Assessment Factor

The plant protection product Malakite (BAS 669 01 F), containing the active substances dithianon and pyrimethanil, is a fungicide against scab in pome fruits. Products containing these active plant protection substances are approved in Norway, but not with both substances in the same product. The Swedish Chemicals Agency (KemI) has as zonal Rapporteur Member State (zRMS) of the Northern Zone evaluated the product Malakite and decided on non-approval due to the observation of unacceptable effects in exposed birds, aquatic organisms, non-target arthropods and earthworms. On request from The Norwegian Food Safety Authority, the VKM Panel on Plant Protection Products has discussed the available data and the report prepared by KemI, and has concluded as follows on the questions raised: On the refinement of DT50 in long term risk assessment for birds: It is the view of the VKM panel that the refinement is not acceptable because the analysis using first order kinetics seems not in line with a realistic and sufficiently conservative approach for the data provided. Furthermore, field studies from more sites are required. On the long term cumulative effects of the active substances on birds: VKM shares the view of KemI, that the combined sub-lethal and reproduction effects should be assessed because the mode of action of the two ingredients has only been shown in fungi, and since the mechanisms in birds could be different. On the reduction of assessment factor for fish: VKM opposes to the reduction of assessment factor for dithianon in fish because the data from acute toxicity tests cannot be extrapolated to chronic toxicity, and because the factor should reflect not only the variation in interspecies sensitivity, but also the uncertainty involved in extrapolation from laboratory tests to the field situation. On the choice of end point in risk assessment for fish: The VKM panel considers the NOEC of dithianon for fish determined from the study at pH 7.9 not to be adequate for the more acidic Norwegian surface waters, and recommends using the data from the test performed at pH 6.5. On the formulation studies for aquatic organisms: It is the opinion of the VKM panel that the formulation studies may be used together with corresponding studies with the active ingredients as long as the studies compared are performed and evaluated according to the same principles. However, VKM notes that the formulation tests as well as the tests of the active ingredients have been performed at high pH values, which are not representative to most Norwegian surface waters. Thus, the toxic effect of dithianon shown in these tests are likely to be lower than expected under typical conditions in Norway. On the assessment factors for concentration addition in fish: It is the opinion of the VKM panel that a reduction in assessment factor for one component in a mixture cannot be used for a formulation containing components for which a similar reduction has not been accepted. On effect studies of active substances and formulations on non-target arthropods: The VKM panel shares the view of KemI that the risk assessment should be based on all available information, including the studies presented for the active substances. On the endpoint in earthworm risk assessment: VKM supports the view of KemI that the observed effects of pyrimethanil on reproduction of earthworms should be considered in the risk assessment of Malakite.

scholarly journals Investigation on the Enzymatic Profile of Mulberry Alkaloids by Enzymatic Study and Molecular Docking

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1776 ◽  
Author(s):  
Zhihua Liu ◽  
Ying Yang ◽  
Wujun Dong ◽  
Quan Liu ◽  
Renyun Wang ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Molecular Docking ◽  
Side Effects ◽  
Inhibitory Effect ◽  
Active Ingredients ◽  
Wide Range ◽  
Consensus Score

α-glucosidase inhibitors (AGIs) have been an important category of oral antidiabetic drugs being widely exploited for the effective management of type 2 diabetes mellitus. However, the marketed AGIs not only inhibited the disaccharidases, but also exhibited an excessive inhibitory effect on α-amylase, resulting in undesirable gastrointestinal side effects. Compared to these agents, Ramulus Mori alkaloids (SZ-A), was a group of effective alkaloids from natural Morus alba L., and showed excellent hypoglycemic effect and fewer side effects in the Phase II/III clinical trials. Thus, this paper aims to investigate the selective inhibitory effect and mechanism of SZ-A and its major active ingredients (1-DNJ, FA and DAB) on different α-glucosidases (α-amylase and disaccharidases) by using a combination of kinetic analysis and molecular docking approaches. From the results, SZ-A displayed a strong inhibitory effect on maltase and sucrase with an IC50 of 0.06 μg/mL and 0.03 μg/mL, respectively, which was similar to the positive control of acarbose with an IC50 of 0.07 μg/mL and 0.68 μg/mL. With regard to α-amylase, SZ-A exhibited no inhibitory activity at 100 μg/mL, while acarbose showed an obvious inhibitory effect with an IC50 of 1.74 μg/mL. The above analysis demonstrated that SZ-A could selectively inhibit disaccharidase to reduce hyperglycemia with a reversible competitive inhibition, which was primarily attributed to the three major active ingredients of SZ-A, especially 1-DNJ molecule. In the light of these findings, molecular docking study was utilized to analyze their inhibition mechanisms at molecular level. It pointed out that acarbose with a four-ring structure could perform desirable interactions with various α-glucosidases, while the three active ingredients of SZ-A, belonging to monocyclic compounds, had a high affinity to the active site of disaccharidases through forming a wide range of hydrogen bonds, whose affinity and consensus score with α-amylase was significantly lower than that of acarbose. Our study illustrates the selective inhibition mechanism of SZ-A on α-glucosidase for the first time, which is of great importance for the treatment of type 2 diabetes mellitus.

scholarly journals Oral controlled-release morphine sulfate. Analgesic efficacy and side effects of a 100-mg tablet in cancer pain patients

Cancer ◽  
1989 ◽  
Vol 63 (11) ◽  
pp. 2284-2288 ◽  
Author(s):  
Russell K. Portenoy ◽  
Mathelyn Maldonado ◽  
Ronald Fitzmartin ◽  
Robert F. Kaiko ◽  
Ronald Kanner
Keyword(s):  
Controlled Release ◽  
Side Effects ◽  
Cancer Pain ◽  
Analgesic Efficacy ◽  
Morphine Sulfate ◽  
Pain Patients

scholarly journals A Comparison of the Efficacy and Tolerability of Controlled-Release Carbamazepine with Conventional Carbamazepine

1991 ◽  
Vol 18 (1) ◽  
pp. 66-68 ◽  
Author(s):  
Z. Dhalla ◽  
J. Bruni ◽  
J. Sutton
Keyword(s):  
Controlled Release ◽  
Side Effects ◽  
Adverse Effects ◽  
Seizure Frequency ◽  
Detrimental Effect ◽  
Blurred Vision ◽  
Dosing Schedule ◽  
Men And Women ◽  
Epileptic Patients ◽  
Cns Side Effects

ABSTRACT:We compared the efficacy and tolerability of controlled-release carbamazepine (CBZ-CR) with conventional carbamazepine (CBZ) in 131 epileptic patients (both men and women, ages 6-65 years) in an open, multicentre, cross-over trial. Patients entered into the trial were previously on CBZ monotherapy or polytherapy. During the first 4 weeks, patients were treated with equivalent daily doses of CBZ and then switched to CBZ-CR for the subsequent 4 weeks. The majority of patients were switched to the more convenient b.i.d. dosing schedule of the controlled-release (CR) preparation without a detrimental effect on seizure frequency or adverse effects. In 44/131 (34%) of patients, the switch to CBZ-CR was accompanied by an improvement in tolerability, primarily due to a reduction in peak-dependent CNS side-effects such as tiredness, double or blurred vision, dizziness and ataxia. At the end of the study, investigators preferred CBZ-CR for 76% of their patients and 70% of the patients preferred CBZ-CR.

Film materials with controlled release of biologically active substances

1998 ◽  
Vol 30 (5) ◽  
pp. 332-336
Author(s):  
I. F. Skokova ◽  
T. N. Yudanova ◽  
I. V. Bogdanova ◽  
N. E. Petrova ◽  
L. S. Gal’braikh
Keyword(s):  
Controlled Release ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Active Substances
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