Entries by Bastian Arlt

Weakly Basic Drugs That Benefit from Acidic Environments in Modern Pharmaceutical Formulation

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Introduction: Weakly Basic Drugs and the Role of Acidic Microenvironments Weakly basic drugs benefit from acidic environments. These drugs represent a critical class of pharmaceutical compounds characterized by strong pH-dependent solubility. For these molecules, dissolution is efficient under acidic gastric conditions. Anyhow, it decreases sharply as pH increases toward intestinal values, often leading to precipitation […]

Review on Starter Pellets: Inert and Functional Cores

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Introduction to Starter Pellet Technologies Review on starter pellets: inert and functional cores examines the core particles used in multiparticulate drug delivery systems. Starter pellets provide a foundation for drug layering and controlled release. Unlike single-unit dosage forms, multiparticulates offer advantages such as more uniform gastrointestinal transit, reduced risk of dose dumping, and improved patient-centric […]

Micro environmental pH-Modulated Dissolution in Functional Pellet Cores

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Introduction to Micro environmental pH-Modulated Dissolution Micro environmental pH-modulated dissolution describes an approach in controlled oral drug delivery where the internal pH of a multiparticulate system is actively altered to enhance the release of a weakly basic drug at higher gastrointestinal pH. Weakly basic active pharmaceutical ingredients (APIs) often dissolve well at low pH but […]

tartaric acid starter core for extended release formulations

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Overview of Functional Core Use in Drug Delivery A tartaric acid starter core for extended release formulations serves as a functional nucleus around which drug layering and controlled-release coatings are built. In extended release design, dissolution and absorption of weakly basic drugs often vary with pH, which makes a stable microenvironmental pH within the dosage […]

Water-Insoluble Weakly Basic Actives on Tartaric Acid Beads – a DoE Case Study

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Introduction to Weakly Basic Actives in Oral Formulation Yes, the headline is long, the overall topic not easy. Additonally, the combination of water-insoluble weakly basic actives with a DoE (Design of Experiments) method based on functional starter beads requests more than basic knowledge. With the help of a CDMO – such as Glatt Pharmaceutical Services, […]

Analytics of Dipyridamole Modified Release Capsules

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Abstract on dipyridamole formulations A robust headspace gas chromatographic method was developed for the quantitative determination of two chemicals – acetone and isopropyl alcohol – which occur in dipyridamole modified release capsules. Due to the weakly basic properties of dipyridamole, tartaric acid pellets (TAP) are used as starter cores for this formulations. The API layered […]

Dabigatran Formulation for Oral Administration – an Evaluation

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Abstract Dabigatran etexilate mesylate is a pro-drug of Dabigatran – a BSC Class II drug used as anti-coagulant in deep vein thrombosis as a direct thrombin inhibitor. Due to increasing solubility in the acidic regime, tartaric acid pellets (TAP) are used as starter beads. A processed formulation is compared with the existing formulation from the […]

BSC Class IV APIs in oral formulations

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APIs of BSC Class IV in oral formulations represent one of four groups following the Biopharmaceutical Classification System (BCS). The BCS predicts potential effects of oral formulations on the human drug oral bioavailability. Thereby, it is a scientific tool differentiating the drug substances on the basis of solubility and intestinal permeability under prescribed condition. While […]

Influence of tartaric acid pellets on the release behavior of a basic drug

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Abstract The objective of this study is to investigate the influence of tartaric acid pellets on the release behavior of a basic drug. By applying an acid micro-environment, the release profiles of Papaverine HCI was dramatically improved. Formulations with weakly basic drugs Papaverine HCl is an opium alkaloid antispasmodic drug, used in the treatment of […]