Preformulation studies on solid self-emulsifying systems in powder form containing magnesium aluminometasilicate as porous carrier

The influence of alkaline and the neutral grade of magnesium aluminometasilicate as a porous solid carrier for the liquid self-emulsifying formulation with ibuprofen is investigated. Ibuprofen is dissolved in Labrasol, then this solution is adsorbed on the silicates. The drug to the silicate ratio is 1:2, 1:4, and 1:6, respectively. The properties of formulations obtained are analyzed, using morphological, porosity, crystallinity, and dissolution studies. Three solid self-emulsifying (S-SE) formulations containing Neusilin SG2 and six consisting of Neusilin US2 are in the form of powder without agglomerates. The nitrogen adsorption method shows that the solid carriers are mesoporous but they differ in a specific surface area, pore area, and the volume of pores. The adsorption of liquid SE formulation on solid silicate particles results in a decrease in their porosity. If the neutral grade of magnesium aluminometasilicate is used, the smallest pores, below 10 nm, are completely filled with liquid formulation, but there is still a certain number of pores of 40–100 nm. Dissolution studies of liquid SEDDS carried out in pH = 1.2 show that Labrasol improves the dissolution of ibuprofen as compared to the pure drug. Ibuprofen dissolution from liquid SE formulations examined in pH of 7.2 is immediate. The adsorption of the liquid onto the particles of the silicate causes a decrease in the amount of the drug released. Finally, more ibuprofen is dissolved from S-SE that consist of the neutral grade of magnesium aluminometasilicate than from the formulations containing the alkaline silicate

Charged N-terminus of Influenza Fusion Peptide Facilitates Membrane Fusion

Cleavage of hemagglutinin precursor (HA0) by cellular proteases results in the formation of two subunits, HA1 and HA2. The N-terminal fragment of HA2, named a fusion peptide (HAfp), possess a charged, amine N-terminus. It has been shown that the N-terminus of HAfp stabilizes the structure of a helical hairpin observed for a 23-amino acid long peptide (HAfp1-23), whose larger activity than HAfp1-20 has been demonstrated recently. In this paper, we analyze the effect of N-terminal charge on peptide-mediated fusion efficiency and conformation changes at the membrane interface by comparison with the corresponding N-acetylated peptides of 20- and 23-amino acid lengths. We found that higher fusogenic activities of peptides with unmodified amino termini correlates with their ability to form helical hairpin structures oriented perpendicularly to the membrane plane. Molecular dynamics simulations showed that acetylated peptides adopt open and surface-bound conformation more often, which induced less disorder of the phospholipid chains, as compared to species with unmodified amino termini

Study on a three-step rapid assembly of zolpidem and its fluorinated analogues employing microwave-assisted chemistry

We developed an efficient microwave-assisted three-step synthesis of zolpidem and its fluorinated analogues 1–3. The procedure relays on the utilization of easily accessible and inexpensive starting materials. Our protocol shows superior performance in terms of yield and purity of products, compared to conventional heating systems. Notably, the total time needed for reaction accomplishment is significantly lower comparing to oil bath heating systems. Finally, we have performed a detailed study on the preparation of zolpidem tartrate salt I, and we assessed its particle-sizes using a polarizing microscope. Our goal was to select the appropriate method that generates the acceptable particle-size, since the solid-size directly influences solubility in biological fluids and further bioavailability. We believe that the disclosed procedure will help to produce a lab-scale quantity of zolpidem and its fluorinated derivatives 1–3, as well as zolpidem tartrate salt I, with suitable fine-particle size for further biological experimentation

Erratum to: Adaptation of the ORTHO-15 test to Polish women and men

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High-throughput dissolution/permeation screening : a 96-well two-compartment microplate approach

Early formulation screening can alleviate development of advanced oral drug formulations, such as amorphous solid dispersions (ASDs). Traditionally, dissolution is used to predict ASD performance. Here, a high-throughput approach is described that simultaneously screens drug dissolution and permeation employing a two-compartment 96-well plate. Freeze-drying from hydro-alcoholic solutions was used to prepare amorphous formulations. The screening approach was tested on amorphous and crystalline tadalafil formulations with and without Soluplus®. The workflow consisted of: 1) dispersion of the formulations; 2) incubation within the two-compartment plate, where a dialysis membrane separated donor (dispersed formulation) and acceptor; 3) sampling (donor and acceptor), where donor samples were centrifuged to remove non-dissolved material; and 4) quantification by UHPLC-UV. To identify optimal screening conditions, the following parameters were varied: dispersion medium (buffer / biomimetic media), acceptor medium (buffer / surfactant solutions), and incubation time (1, 3, and 6 h). Surfactants (acceptor) increased tadalafil permeation. Biomimetic medium (donor) enhanced dissolution, but not permeation, except for freeze-dried tadalafil, for which the permeated amount increased. The predictiveness was evaluated by comparing dissolution-/permeation-results with in vivo bioavailability. In general, both dissolution and permeation reflected bioavailability, whereof the latter was a better predictor. High-throughput dissolution/permeation is regarded promising for formulation screening

Impact of Pharmacists’ Religious and Personal Beliefs in Dispensing Contraceptives

Background: Until recently, pharmacies were not permitted to dispense any emergency contraceptives to women to prevent pregnancy. No legal statutes existed under which pharmacists with religious, moral or ethical objections could refuse to fill a prescription for contraceptives, nor were there direct guidelines describing the pharmacist’s professional obligations. Objectives: The purpose of this study is to explore the frequency of cases in which pharmacists have refused, due to their personal beliefs, to provide counsel regarding contraceptives or have refused to refer to a patient to a different pharmacist or healthcare provider. This study will compare and contrast the differences between independent pharmacies and chain pharmacies (i.e. time spent, location, most common recommended contraception). Finally, this study will compare the results evident between male pharmacists and female pharmacists. Method: Quantitative method employed uses two interview questions directed to pharmacists: (1) “I am moving in with my fiancée/boyfriend next month and I have never used contraceptives. What are my options?” (2) “If I use a condom and it breaks, do I have any choices to prevent pregnancy after the fact?” The survey was conducted in two locations, the greater Philadelphia area and Hershey, PA. The survey was conducted through face-to-face interactions with pharmacists, either employed at independent pharmacy or at a chain pharmacy. Data collected from each pharmacist included number of approximate age/gender; minutes spent in each consultation with a patient; the kind of privacy provided during the consultation; and the referrals given, if any. Results: Fifty (50) pharmacists were interviewed. No pharmacist indicated that counseling would be denied, although one (1) pharmacist refused to counsel on Plan B and four (4) pharmacists referred the interviewer to a doctor immediately, indicating that all medications require a prescription. Two (2) pharmacists spent more than 10 minutes providing the best possible counseling.   Type: Student Projec

Impact of Pharmacists’ Religious and Personal Beliefs in Dispensing Contraceptives

Background: Until recently, pharmacies were not permitted to dispense any emergency contraceptives to women to prevent pregnancy. No legal statutes existed under which pharmacists with religious, moral or ethical objections could refuse to fill a prescription for contraceptives, nor were there direct guidelines describing the pharmacist’s professional obligations. Objectives: The purpose of this study is to explore the frequency of cases in which pharmacists have refused, due to their personal beliefs, to provide counsel regarding contraceptives or have refused to refer to a patient to a different pharmacist or healthcare provider. This study will compare and contrast the differences between independent pharmacies and chain pharmacies (i.e. time spent, location, most common recommended contraception). Finally, this study will compare the results evident between male pharmacists and female pharmacists. Method: Quantitative method employed uses two interview questions directed to pharmacists: (1) “I am moving in with my fiancée/boyfriend next month and I have never used contraceptives. What are my options?” (2) “If I use a condom and it breaks, do I have any choices to prevent pregnancy after the fact?” The survey was conducted in two locations, the greater Philadelphia area and Hershey, PA. The survey was conducted through face-to-face interactions with pharmacists, either employed at independent pharmacy or at a chain pharmacy. Data collected from each pharmacist included number of approximate age/gender; minutes spent in each consultation with a patient; the kind of privacy provided during the consultation; and the referrals given, if any. Results: Fifty (50) pharmacists were interviewed. No pharmacist indicated that counseling would be denied, although one (1) pharmacist refused to counsel on Plan B and four (4) pharmacists referred the interviewer to a doctor immediately, indicating that all medications require a prescription. Two (2) pharmacists spent more than 10 minutes providing the best possible counseling.   Type: Student Projec

75-year-old man with lung cancer obscured by an implantable cardioverter-defibrillator — case report

We present a case of a 75-year-old man, who underwent a scheduled implantable cardioverter-defibrillatorreoperation and has had a lung cancer found in a chest X-ray taken after the procedure, that wascompletely obscured by the previous device