Bioavailability of Lumefantrine Is Significantly Enhanced with a Novel Formulation Approach, an Outcome from a Randomized, Open-Label Pharmacokinetic Study in Healthy Volunteers.

The artemether-lumefantrine combination requires food intake for the optimal absorption of lumefantrine. In an attempt to enhance the bioavailability of lumefantrine, new solid dispersion formulations (SDF) were developed, and the pharmacokinetics of two SDF variants were assessed in a randomized, open-label, sequential two-part study in healthy volunteers. In part 1, the relative bioavailability of the two SDF variants was compared with that of the conventional formulation after administration of a single dose of 480 mg under fasted conditions in three parallel cohorts.

Efficacy and insecticidal properties of some essential oils against Caryedon serratus (Oliver)-a storage pest of groundnut.

During storage groundnut is attacked by number of stored grain pest and management of these insect pests particularly bruchid beetle, Caryedon serratus (Oliver) is of prime importance as they directly damage the pod and kernels. Hence, some essential oils were tested for their insecticidal and fungicidal properties. Highest total bruchid mortality was recorded with the application of neem oil and pongamia oil at 10% (v/w) concentration and lowest in eucalyptus oil at 5% (v/w).

Enantiotropically related polymorphs of gaboxadol hydrochloride.

Gaboxadol hydrochloride, also known as THIP hydrochloride (systematic name: 3-hydroxy-4,5,6,7-tetrahydro-1,2-oxazolo[5,4-c]pyridin-6-ium chloride), C6H9N2O2(+)·Cl(-), exists as two enantiotropically related polymorphs. Transformation between the polymorphs occurs in a single-crystal-to-single-crystal manner at 221 K, and the enthalpy of transformation from the high-temperature form to the low-temperature form is -0.7 kJ mol(-1).

Atomic pairwise distribution function analysis of the amorphous phase prepared by different manufacturing routes.

Amlodipine besilate, a calcium channel antagonist, exists in several solid forms. Processing of anhydrate and dihydrate forms of this drug may lead to solid state changes, and is therefore the focus of this study. Milling was performed for the anhydrate form, whereas the dihydrate form was subjected to quench cooling thereby creating an amorphous form of the drug from both starting materials.

Investigation of solid phase composition on tablet surfaces by grazing incidence X-ray diffraction.

Purpose: To investigate solid state transformations of drug substances during compaction using grazing incidence X-ray diffraction (GIXD).

Methods: The solid forms of three model drugs-theophylline (TP), nitrofurantoin (NF) and amlodipine besylate (AMB)-were compacted at different pressures (from 100 to 1000 MPa); prepared tablets were measured using GIXD. After the initial measurements of freshly compacted tablets, tablets were subjected to suitable recrystallization treatment, and analogous measurements were performed.