scholarly journals Systèmes à libération contrôlée pH-dépendants de principes actifs hydrophobes à partir d’oléogels

2021 ◽  
Vol 15 (2) ◽  
pp. 388-398
Author(s):  
Papa Mady Sy ◽  
Peggy Ngadou Ntchobaha ◽  
Sidy Mouhamed Dieng ◽  
Louis Augustin D. Diouf ◽  
Alphonse R. Djiboune ◽  
...  
Keyword(s):  
Controlled Release ◽  
Large Scale ◽  
Sol Gel ◽  
Active Pharmaceutical Ingredient ◽  
Sub Saharan Africa ◽  
Gelling Agent ◽  
Active Pharmaceutical Ingredients ◽  
Medium Ph ◽  
Pharmaceutical Ingredients ◽  
Ph Dependent

Les rhumatismes inflammatoires chroniques sont une cause importante d'invalidité dans le monde entier. De ce fait, les affections rhumatismales chroniques font peser une lourde charge sociale et économique sur toutes les sociétés, pas seulement sur celles où l’espérance de vie est élevée. L’objectif principal de ce travail était d’étudier le profil de libération pH-dépendante de principes actifs hydrophobes à partir d’oléogels oraux et/ou cutanés. La formulation des oléogels a été réalisée selon une méthode sol-gel, reproductible à grande échelle. La caractérisation et le suivi dans le temps ont montré une bonne stabilité des oléogels. Les valeurs de pH des oléogels étaient globalement acides (entre 4,3 et 5,8) et dépendaient de la quantité de gélifiant utilisée. Les études de libération du kétoprofène, principe actif hydrophobe, en fonction du pH des milieux de dissolution ont montré des profils de libération d’une cinétique du premier ordre d’équation 𝑷𝒕=𝑷𝟎+𝑨.𝒆𝒙𝒑𝑲𝒕 avec des coefficients de détermination proches de 1 (milieux à pH égal à 1,2 et 5,5). Une meilleure libération du kétoprofène a été obtenue dans un milieu intestinal simulé (pH égal à 6,8) pour les formulations qui présentaient déjà une saturation en milieu gastrique simulé (pH égal à 1,2). Cette étude qui a permis de formuler, d’évaluer et de modéliser le profil de libération du kétoprofène à partir d’oléogels peut constituer une étape importante dans un objectif de souveraineté thérapeutique des pays d’Afrique subsaharienne notamment le Sénégal.Mots clés : Oléogels, rhumatismes inflammatoires chroniques, kétoprofène, libération contrôlée, pH-dépendant.   English Title: pH-dependent controlled release systems of hydrophobic active pharmaceutical ingredients from oleogels Chronic inflammatory rheumatism is a major cause of disability around the world. As a result, chronic rheumatic diseases place a heavy social and economic burden on all societies, not just those with high life expectancy. The main objective of this work was to control the pH-dependent release of hydrophobic active pharmaceutical ingredients from oral and / or skin oleogels. The formulation of the oleogels was carried out using a sol-gel large-scale reproducible method. Characterization and monitoring over time have shown good stability of the oleogels. The pH values of the oleogels were overall acid (between 4.3 and 5.8) and depended on the amount of gelling agent used. The release studies of ketoprofen, a hydrophobic active pharmaceutical ingredient, as a function of the pH of the dissolution media have shown release profiles of first-order kinetics of equation 𝑷𝒕=𝑷𝟎+𝑨.𝒆𝒙𝒑𝑲𝒕 with coefficients of determination close to 1 (media at pH equal to 1.2 and 5.5). Better release of ketoprofen was obtained in simulated intestinal medium (pH equal to 6.8) for formulations which already exhibited saturation in simulated gastric medium (pH equal to 1.2). This study, which made it possible to formulate, evaluate and model the release profile of ketoprofen from oleogels, may constitute an important step in an objective of therapeutic sovereignty of the countries of sub-Saharan Africa, particularly Senegal.Keywords: oleogels - chronic inflammatory rheumatism - ketoprofen - controlled release – pH-dependent.

Polymorphism control of active pharmaceutical ingredients

2021 ◽  
pp. 37-54
Author(s):  
Roman Petrovich Terekhov ◽  
Denis Igorevich Pankov ◽  
Ekaterina Aleksandrovna Anfinogenova ◽  
Irina Anatolievna Selivanova
Keyword(s):  
Active Pharmaceutical Ingredient ◽  
Development Stage ◽  
Poor Quality ◽  
Polymorphic Modification ◽  
High Tech ◽  
Active Pharmaceutical Ingredients ◽  
Pharmaceutical Ingredients ◽  
Medicinal Substances ◽  
The Usa ◽  
Economic Union

Рolymorphism is receiving increasing attention due to its influence on the physicochemical and pharmacological properties of the active pharmaceutical ingredients (API) while maintaining the molecular structure. This review is devoted to the problem of APIs phase state control both at the development stage and during the circulation of the drug. The term «polymorphism» has different definitions depending on the branch of science. There is no unambiguous solution to this issue in the regulatory documentation of pharmaceutical industry either. Based on the analysis of literary sources, the article presents a comparison of pharmacopeia methods, recommended in Russian and foreign regulatory documents for the analysis of polymorphism of medicinal substances, including state pharmacopeias of Russia, Belarus, Kazakhstan, the USA, and Japan, as well as international pharmacopeias of the European Economic Union and the Eurasian Economic Union. The trend on using a complex of high-tech equipment is revealed. A systematic approach to analysis based on X-ray diffraction, thermal, spectral, microscopic, biological, and physical methods for determining constants makes it possible not only to identify the polymorphic modification of API, but also to characterize its structure, morphology, physicochemical properties and pharmacological activity. In the Russian Federation, the phenomenon of polymorphism is being studied especially intensively, and some control methods, such as biological methods, are validated only in Russian pharmacopeia. A promising direction for further research is the improvement and harmonization of regulatory documentation within the framework of this chemical and technological field of pharmacy. A global approach will help to reduce not only the probability of poor-quality products entering the market, but also the costs of establishing the authenticity of the active pharmaceutical ingredient produced.

scholarly journals Quality Assessment of Antibiotic Oral Drug Formulations Marketed In Katsina State, Nigeria

1970 ◽  
Vol 7 (6) ◽  
pp. 6-10
Author(s):  
Mukhtar Gambo Lawal ◽  
Muhammad Dauda Mukhtar ◽  
Abdulkadir Magaji Magashi
Keyword(s):  
Active Ingredient ◽  
Active Pharmaceutical Ingredient ◽  
Oral Drug ◽  
Active Pharmaceutical Ingredients ◽  
Hplc Assay ◽  
Drug Formulations ◽  
Percentage Content ◽  
Pharmaceutical Ingredients ◽  
Three Samples ◽  
High Incidence

There are increasing reports on the high incidence of substandard drugs, especially in developing countries.Pharmaceutical products have been reported to contain either no, low, or excessive amounts of the active pharmaceutical ingredient (API). Inview of the above, 112 samples of six different antibiotic oral drug formulations were evaluated for chemical quality by assessing the presence and the percentage content of the stated active pharmaceutical ingredients using validated HPLC assay as described in the official monograph of the British and United Stated pharmacopoeia. The result indicates that 43 (38.4%) had active ingredients outside the set pharmacopoeial limit and therefore were non-compliant to the BP and the USP specifications for percentage content.  Ampiclox and Cotrimoxazole had the highest proportion of samples with active ingredient outside the pharmacopoeial limit, and in three samples (one Augmentin and two Ampiclox), no active ingredient was detected. The presence of API lower than the claimed content declared on the packaging was the primary cause of non-compliance. The potential implications of the use of substandard drugs are treatment failure and the development of drug-resistance.  

scholarly journals (1R,3S)-3-(1H-Benzo[d]imidazol-2-yl)-1,2,2-trimethylcyclopentane-1-carboxylic acid as a new anti-diabetic active pharmaceutical ingredient

2020 ◽  
Vol 76 (9) ◽  
pp. 1407-1411
Author(s):  
Sergiy M. Kovalenko ◽  
Irina S. Konovalova ◽  
Sergiy I. Merzlikin ◽  
Vladimir P. Chuev ◽  
Dmitry V. Kravchenko
Keyword(s):  
Active Pharmaceutical Ingredient ◽  
Ethanol Solution ◽  
Membered Ring ◽  
Active Pharmaceutical Ingredients ◽  
Pharmaceutical Ingredients ◽  
Compound C ◽  
Intermolecular Contacts ◽  
The Mean ◽  
Camphoric Acid

The chiral title compound, C16H20N2O2, which can be used for producing active pharmaceutical ingredients for treatment of type 2 pancreatic diabetes and other pathologies dependent on insulin resistance, was prepared from (1R,3S)-camphoric acid and o-phenylenediamine. It crystallized from an ethanol solution in the chiral monoclinic P21 space group. The five-membered ring adopts a twisted conformation with the methyl-substituted C atoms displaced by −0.273 (5) and 0.407 (5) Å from the mean plane through the other three atoms. In the crystal, molecules are linked by O—H...N hydrogen bonds, forming chains along the a-axis direction. Hirshfeld surface analysis and two-dimensional fingerprint plots were used to analyze the intermolecular contacts present in the crystal.

15.1 Flow Chemistry in the Pharmaceutical Industry: Part 1

2018 ◽  
Author(s):  
A. G. O’Brien
Keyword(s):  
Pharmaceutical Industry ◽  
Large Scale ◽  
Flow Chemistry ◽  
Active Pharmaceutical Ingredients ◽  
Flow Process ◽  
Pharmaceutical Ingredients ◽  
Multistep Synthesis

Abstract The use of flow chemistry in the single- and multistep synthesis of active pharmaceutical ingredients has been well demonstrated. The pharmaceutical industry is now taking the next steps towards integration of flow chemistry into large-scale commercialized processes, which can effectively supply patient populations. This chapter details advances in this area, and outlines the data and knowledge required to select, develop, scale, and commercialize an efficient flow process.

scholarly journals Electrospun API-loaded mixed matrix membranes for controlled release

RSC Advances ◽  
2017 ◽  
Vol 7 (68) ◽  
pp. 43300-43309 ◽  
Author(s):  
B. Castro-Dominguez ◽  
K. Moroney ◽  
B. Schaller ◽  
S. O'Connor ◽  
A. Cloonan ◽  
...  
Keyword(s):  
Controlled Release ◽  
Fixed Time ◽  
Mixed Matrix Membranes ◽  
Active Pharmaceutical Ingredients ◽  
Mixed Matrix ◽  
Membrane Materials ◽  
Pharmaceutical Ingredients ◽  
Time Period ◽  
Matrix Membranes

The development of biocompatible membrane materials capable of delivering active pharmaceutical ingredients (APIs) over a fixed time period offers significant advantages to the pharmaceutical and biomedical industries alike.

Self-assembled polysaccharide nanostructures for controlled-release applications

2014 ◽  
Vol 3 (4) ◽  
Author(s):  
James M. Myrick ◽  
Venkat Kalyan Vendra ◽  
Sitaraman Krishnan
Keyword(s):  
Controlled Release ◽  
Intermolecular Interactions ◽  
Functional Properties ◽  
Bioactive Compounds ◽  
Controlled Delivery ◽  
Active Pharmaceutical Ingredients ◽  
Chemical Functionalization ◽  
Pharmaceutical Ingredients ◽  
Self Assembling ◽  
Wide Range

AbstractSelf-assembling polysaccharide nanostructures have moved to the forefront of many fields due to their wide range of functional properties and unique advantages, including biocompatability and stimulus responsiveness. In particular, the field of controlled release, which involves influencing the location, concentration, and efficacy of active pharmaceutical ingredients (APIs), diagnostics, nutrients, or other bioactive compounds, has benefited from polysaccharide biomaterials. Nanostructure formation, stimulus responsiveness, and controlled-release performance can be engineered through facile chemical functionalization and noncovalent intermolecular interactions. This review discusses polysaccharide nanoparticles, designed for targeted and time-controlled delivery of emerging APIs, with improved

scholarly journals Stability of Pharmaceutical Co-Crystals at Humid Conditions Can Be Predicted

Pharmaceutics ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 433
Author(s):  
Heiner Veith ◽  
Maximilian Zaeh ◽  
Christian Luebbert ◽  
Naír Rodríguez-Hornedo ◽  
Gabriele Sadowski
Keyword(s):  
Pharmaceutical Formulations ◽  
Active Pharmaceutical Ingredient ◽  
Storage Conditions ◽  
Pharmaceutical Products ◽  
Active Pharmaceutical Ingredients ◽  
Statistical Associating Fluid Theory ◽  
Pharmaceutical Ingredients ◽  
Soluble Solid ◽  
Fluid Theory ◽  
The Stability

Knowledge of the stability of pharmaceutical formulations against relative humidity (RH) is essential if they are to become pharmaceutical products. The increasing interest in formulating active pharmaceutical ingredients as stable co-crystals (CCs) triggers the need for fast and reliable in-silico predictions of CC stability as a function of RH. CC storage at elevated RH can lead to deliquescence, which leads to CC dissolution and possible transformation to less soluble solid-state forms. In this work, the deliquescence RHs of the CCs succinic acid/nicotinamide, carbamazepine/nicotinamide, theophylline/citric acid, and urea/glutaric acid were predicted using the Perturbed-Chain Statistical Associating Fluid Theory (PC-SAFT). These deliquescence RH values together with predicted phase diagrams of CCs in water were used to determine critical storage conditions, that could lead to CC instability, that is, CC dissolution and precipitation of its components. The importance of CC phase purity on RH conditions for CC stability is demonstrated, where trace levels of a separate phase of active pharmaceutical ingredient or of coformer can significantly decrease the deliquescence RH. The use of additional excipients such as fructose or xylitol was predicted to decrease the deliquescence RH even further. All predictions were successfully validated by stability measurements at 58%, 76%, 86%, 93%, and 98% RH and 25 °C.

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