Development and Evaluation of Lactose-Free Single-Unit and Multiple-Unit Preparations of a BCS Class II Drug, Rivaroxaban.

: The aim of the present study was to develop lactose-free formulations of rivaroxaban, a novel oral anticoagulant used for the treatment and prevention of blood clotting. As a BCS Class II drug, rivaroxaban is characterized by poor solubility in aqueous media, posing a significant formulation challenge. : To address this, phosphate-based excipients were employed to prepare both traditional single-unit dosage forms (tablets) and modern multiple-unit pellet systems (MUPS).

Immediate Effects of Wearing an Ankle Bandage on Fine Coordination, Proprioception, Balance and Gait in the Subacute Phase of Ankle Sprains.

Ankle sprains are the most frequently occurring musculoskeletal injuries among recreational athletes. Ankle support through bandages following the initial orthotic treatment might be beneficial for rehabilitation purposes. However, the literature is sparse regarding the use of an ankle support directly after the acute phase of an ankle sprain.

Does Impaired Plantar Cutaneous Vibration Perception Contribute to Axial Motor Symptoms in Parkinson's Disease? Effects of Medication and Subthalamic Nucleus Deep Brain Stimulation.

Objective: To investigate whether impaired plantar cutaneous vibration perception contributes to axial motor symptoms in Parkinson's disease (PD) and whether anti-parkinsonian medication and subthalamic nucleus deep brain stimulation (STN-DBS) show different effects.

Methods: Three groups were evaluated: PD patients in the medication "on" state (PD-MED), PD patients in the medication "on" state and additionally "on" STN-DBS (PD-MED-DBS), as well as healthy subjects (HS) as reference. Motor performance was analyzed using a pressure distribution platform.

Effect of Compaction Pressure on the Enzymatic Activity of Pancreatin in Directly Compressible Formulations.

Tableting of biomolecules is a challenging formulation phase due to their sensitivity to various process parameters, such as compression pressure, process dynamics, or the temperature generated. In the present study, pancreatin was employed as a model enzyme mixture, which was formulated in tablet form utilizing the synergistic effects of brittle and plastic excipients (dibasic calcium phosphate and microcrystalline cellulose, respectively). The effect of varying compaction pressure and lubricant concentration on the generated temperature and enzymatic activity was evaluated.

The Use of Calcium Phosphate-Based Starter Pellets for the Preparation of Sprinkle IR MUPS Formulation of Rosuvastatin Calcium.

Sprinkle formulations represent an interesting concept of medicinal products aimed at the steadily growing population of patients suffering from swallowing difficulties (dysphagia). In the present work, immediate-release sprinkle MUPS (multiple-unit pellet system) containing rosuvastatin calcium as a model drug substance was successfully developed. The formulation was prepared by drug layering technique using novel calcium phosphate-based starting pellets (PharSQ Spheres CM) of three different particle sizes.

Towards the Continuous Manufacturing of Liquisolid Tablets Containing Simethicone and Loperamide Hydrochloride with the Use of a Twin-Screw Granulator.

Continuous manufacturing is becoming the new technological standard in the pharmaceutical industry. In this work, a twin-screw processor was employed for the continuous production of liquisolid tablets containing either simethicone or a combination of simethicone with loperamide hydrochloride. Both active ingredients present major technological challenges, as simethicone is a liquid, oily substance, and loperamide hydrochloride was used in a very small amount (0.

Anticipatory Postural Adjustments and Compensatory Postural Responses to Multidirectional Perturbations-Effects of Medication and Subthalamic Nucleus Deep Brain Stimulation in Parkinson's Disease.

Background: Postural instability is one of the most restricting motor symptoms for patients with Parkinson's disease (PD). While medication therapy only shows minor effects, it is still unclear whether medication in conjunction with deep brain stimulation (DBS) of the subthalamic nucleus (STN) improves postural stability. Hence, the aim of this study was to investigate whether PD patients treated with medication in conjunction with STN-DBS have superior postural control compared to patients treated with medication alone.

Exploiting synergistic effects of brittle and plastic excipients in directly compressible formulations of sitagliptin phosphate and sitagliptin hydrochloride.

Direct compression (DC) is the simplest and most economical way to produce pharmaceutical tablets. Ideally, it consists of only two steps: dry blending of a drug substance(s) with excipients followed by compressing the powder mixture into tablets. In this study, immediate-release film-coated tablets containing either Sitagliptin phosphate or Sitagliptin hydrochloride were developed using DC technique.

Directly compressible formulation of immediate release rosuvastatin calcium tablets stabilized with tribasic calcium phosphate.

Reliable and stable tablet formulations for rosuvastatin calcium (RSC) in four strengths: 5 mg, 10 mg, 20 mg, and 40 mg have been developed. Rosuvastatin is a cholesterol-lowering statin drug and is known to be unstable during storage. The possibility of its stabilization with inorganic salts of multivalent metals has already been reported in the literature.

Studies on the pH-Dependent Solubility of Various Grades of Calcium Phosphate-based Pharmaceutical Excipients.

Calcium phosphate-based pharmaceutical excipients, including calcium hydrogen phosphate anhydrous and dihydrate, calcium hydroxide phosphate have been well established in pharmaceutical technology for a very long time. Nowadays, they are of increasing interest to the pharmaceutical industry because, in addition to their advanced functional properties, they offer beneficial biocompatible and biodegradable properties. Yet, there is limited availability of embracing information regarding the solubility of these popular excipients, especially in variable pH conditions, reflecting those of the gastrointestinal tract (GIT).

Development of a Biphasic-Release Multiple-Unit Pellet System with Diclofenac Sodium Using Novel Calcium Phosphate-Based Starter Pellets.

Novel calcium phosphate-based starter pellets were used to develop a biphasic-release multiple-unit pellet system (MUPS) with diclofenac sodium as a model drug in the form of hard gelatin capsules. For comparative purposes, corresponding formulations based on the inert cores made of microcrystalline cellulose, sucrose and isomalt were prepared. The developed system consisted of two types of drug-layered pellets attaining different release patterns: delayed-release (enteric-coated) and extended-release.

Postural performance and plantar cutaneous vibration perception in patients with idiopathic normal pressure hydrocephalus.

Objective: To investigate whether impaired plantar cutaneous vibration perception contributes to postural disturbance in idiopathic normal pressure hydrocephalus (iNPH).

Methods: Three different groups were tested: iNPH-patients (iNPH), iNPH-patients after surgical shunt therapy (iNPH shunt), and healthy subjects (HS). Postural performance was quantified during quiescent stance on a pressure distribution platform.

Effects of plantar hypothermia on quasi-static balance: Two different hypothermic procedures.

Inducing hypothermia to examine its effects on balance is performed with various approaches. However, data interpretations of underlying postural mechanisms often do not consider the applied hypothermic protocol. In this context, the effects of diminished plantar mechanoreceptor activity on quasi-static balance performance were investigated, examining the applicability of a continuously cooling thermal platform in comparison with conventional ice pads.

closo-borane conjugated regulatory peptides retain high biological affinity: synthesis of closo-borane conjugated Tyr(3)-octreotate derivatives for BNCT.

Despite the improvements in cancer therapy during the past years, high-grade gliomas and many other types of cancer are still extremely resistant to current forms of therapy. Boron neutron capture therapy (BNCT) provides a promising way to destroy cancer cells without damaging healthy tissue. However, BNCT in practice is still limited due to the lack of boron-containing compounds that selectively deliver boron to cancer cells.