Preparation, characterization, and in vitro cytogenotoxic evaluation of a novel dimenhydrinate-β-cyclodextrin inclusion complex.

Dimenhydrinate (DMH), used to alleviate motion sickness symptoms such as nausea, vomiting, dizziness, and vertigo, encounters limitations in oral pharmaceutical formulations due to its poor water solubility and bitter taste. Our research hypothesized that inclusion complexation with β-cyclodextrin (β-CD) might address these drawbacks while ensuring that the newly formed complexes exhibit no cytotoxic or genotoxic effects on peripheral blood mononuclear cells (PBMCs). Inclusion complexes were prepared using the kneading method and the solvent evaporation method.

Sweeteners in Orodispersible Films: How Much is too Much?

Four natural sweeteners (sucrose, xylitol, fructose, and isomalt) were selected to examine the influence of their qualities and amounts on the characteristics of orodispersible films. Sodium carboxymethylcellulose (2% w/w) was utilized as the film-forming polymer and 1% w/w glycerol as a plasticizer. Films were produced through the solvent casting method, rendering them suitable for convenient application in community or hospital pharmacy settings.

Development and Characterization of Cationic Nanostructured Lipid Carriers as Drug Delivery Systems for miRNA-27a.

Although miRNA-27a has been identified as a promising candidate for miRNA mimic therapy of obesity, its application is limited due to enzymatic degradation and low membrane permeation. To overcome these problems, we developed cationic nanostructured lipid carriers (cNLCs) using high-pressure homogenization and used them as non-viral carriers for the anti-adipogenic miRNA-27a. Cargo-free octadecylamine-containing NLCs and miRNA/cNLC complexes were characterized regarding particle size, size distributions, zeta potential, pH values, particle topography and morphology, and entrapment efficacy.

Quality by Design-Based Development of Solid Self-Emulsifying Drug Delivery System (SEDDS) as a Potential Carrier for Oral Delivery of Lysozyme.

For many years, researchers have been making efforts to find a manufacturing technique, as well as a drug delivery system, that will allow for oral delivery of biopharmaceuticals to their target site of action without impairing their biological activity. Due to the positive in vivo outcomes of this formulation strategy, self-emulsifying drug delivery systems (SEDDSs) have been intensively studied in the last few years as a way of overcoming the different challenges associated with the oral delivery of macromolecules. The purpose of the present study was to examine the possibility of developing solid SEDDSs as potential carriers for the oral delivery of lysozyme (LYS) using the Quality by Design (QbD) concept.

A Critical Assessment of Extemporaneous Formulations for Proton Pump Inhibitors: The Importance of Proper Vehicle Selection.

Objective: To examine the influence of vehicles on the stability of extemporaneous suspensions of proton pump inhibitors (PPIs), to single out the formulation most suitable for children, providing appropriate evidence and arguments.

Methods: A review was performed of data identified from Medline, Embase, Science Direct, as well as public digital archive PubMed, including reference texts, related to the field of stability testing of extemporaneous PPI suspensions.

Results: Fourteen selected formulations of extemporaneous suspensions are presented and discussed.

3D Printing-A "Touch-Button" Approach to Manufacture Microneedles for Transdermal Drug Delivery.

Microneedles (MNs) represent the concept of attractive, minimally invasive puncture devices of micron-sized dimensions that penetrate the skin painlessly and thus facilitate the transdermal administration of a wide range of active substances. MNs have been manufactured by a variety of production technologies, from a range of materials, but most of these manufacturing methods are time-consuming and expensive for screening new designs and making any modifications. Additive manufacturing (AM) has become one of the most revolutionary tools in the pharmaceutical field, with its unique ability to manufacture personalized dosage forms and patient-specific medical devices such as MNs.

Novel Drug Delivery Systems Fighting Glaucoma: Formulation Obstacles and Solutions.

Glaucoma is considered to be one of the biggest health problems in the world. It is the main cause of preventable blindness due to its asymptomatic nature in the early stages on the one hand and patients' non-adherence on the other. There are several approaches in glaucoma treatment, whereby this has to be individually designed for each patient.

In vitro pH dependent passive transport of ketoprofen and metformin.

The kinetics of passive transport of ketoprofen and metformin, as model substances for high and low permeability, respectively, across the artificial membrane under the influence of the pH of donor solution was investigated. There was an upward trend in the apparent permeation coefficient ( ) of ketoprofen with the decrease in pH to a value close to pa. At the pH value below pa the permeation coefficient had lower value, due to the higher retention of ketoprofen in the artificial membrane.

Microneedles: Characteristics, Materials, Production Methods and Commercial Development.

Although transdermal drug delivery systems (DDS) offer numerous benefits for patients, including the avoidance of both gastric irritation and first-pass metabolism effect, as well as improved patient compliance, only a limited number of active pharmaceutical ingredients (APIs) can be delivered accordingly. Microneedles (MNs) represent one of the most promising concepts for effective transdermal drug delivery that penetrate the protective skin barrier in a minimally invasive and painless manner. The first MNs were produced in the 90s, and since then, this field has been continually evolving.

Development of ternary solid dispersions with hydrophilic polymer and surface adsorbent for improving dissolution rate of carbamazepine.

In this study solid dispersions of carbamazepine in the hydrophilic Kollidon® VA64 polymer, adsorbed onto Neusilin® UFL2 adsorption carrier have been employed to improve carbamazepine dissolution rate. In order to evaluate effects of changing in the proportions of all solid dispersion components on carbamazepine dissolution rate, D-optimal mixture experimental design was used in the formulation development. From all prepared solid dispersion formulations, significantly faster carbamazepine dissolution was observed compared to pure drug.

Propylene carbonate quantification by its derivative 3,5-diacetyl-1,4-dihydro-2,6-lutidine.

Propylene carbonate (PC) is a non-toxic solvent currently used in various pharmaceutical formulations. Consequently, a simple, cost-effective and most accurate analytical method for the quantification of this optical inert solvent is of major interest. Based on a consecutive three-step reaction 3,5-diacetyl-1,4-dihydro-2,6-lutidine was obtained from PC and used for quantification by either UV and fluorescent detection.

Stability of suspensions: theoretical and practical considerations before compounding.

Suspension stability can be theoretically estimated prior to the beginning of the formulating process based on the solid phase particle size, liquid phase density, and viscosity. Stokes equation can be used to predict suspension stability in order to save time and resources. The examples of these calculations for the assessment of suspension physical characteristics are given in this article.

Impairment of the in vitro release of carbamazepine from tablets.

Carbamazepine belongs to the class II biopharmaceutical classification system (BCS) which is characterized by a high per-oral dose, a low aqueous solubility and a high membrane permeability. The bioavailability of such a drug is limited by the dissolution rate. The present study deals with the formulations of immediate release tablets of poorly soluble carbamazepine.

Dissolution studies of physical mixtures of indomethacin with alpha- and gamma-cyclodextrins.

Oral administration of indomethacin has been limited by its poor water solubility. Cyclodextrins have been recognized as potential candidates to overcome the poor solubility of indomethacin through the formation of inclusion complexes. The aim of our study was to compare the dissolution profiles of pure indomethacin and its mixtures with α- and γ-cyclodextrins The inclusion complexes of indomethacin with α- and γ-cyclodextrins were prepared by direct mixing in dissolution vessel.

Influence of splitting on dissolution properties of metoprolol tablets.

The objective of this work was to compare several profiles of dissolution data for metoprolol controlled release tablet formulations in order to identify possible changes in dissolution profiles of whole and scored tablets. Adequate design of score lines (on one or both sides) as well as the technology of preparation of tablet mixtures ensure forming a score line of adequate thickness, shape, size, curvature. According to the obtained results, this type of extended release formulation is eligible for splitting and use in therapy either as a whole or scored tablets.

Influence of type and neutralisation capacity of antacids on dissolution rate of ciprofloxacin and moxifloxacin from tablets.

Dissolution rate of two fluoroquinolone antibiotics (ciprofloxacin and moxifloxacin) was analysed in presence/absence of three antacid formulations. Disintegration time and neutralisation capacity of antacid tablets were also checked. Variation in disintegration time indicated the importance of this parameter, and allowed evaluation of the influence of postponed antacid-fluoroquinolone contact.

Comparison of some physical parameters of whole and scored lisinopril and lisinopril/hydrochlorthiazide tablets.

Tablets are one of the most popular and preferred solid dosage forms because they can be accurately dosed, easily manufactured and packaged on a large scale, have good physical and chemical stability, and can contribute to good patient compliance given their ease of administration. The ability to match doses to patients depends on the availability of multiple dose sizes and adequate dose-response information. These are not always provided, so splitting of the tablets is sometimes necessary.

Stability of anthocyanins from commercial black currant juice under simulated gastrointestinal digestion.

Anthocyanins are effective antioxidants but they have also been proposed to have other biological activities independent of their antioxidant capacities that produce health benefits. Examples range from inhibition of cancer cell growth in vitro, induction of insulin production in isolated pancreatic cells, reduction of starch digestion through inhibition of a-glucosidase activity, suppression of inflammatory responses as well as protection against age-related declines in cognitive behavior and neuronal dysfunction in the central nervous system. However, to achieve any biological effect in a specific tissue or organ, anthocyanins must be bioavailable; i.

Study of the applicabilty of content uniformity and dissolution variation test on ropinirole hydrochloride tablets.

When considering single-dose preparations, it is fundamental that the patient receives in his individual dose an amount of drug close to that claimed on the label. Since drug content and content uniformity of single-dose preparations depend on a number of processes associated with their manufacture, it is obviously unrealistic to expect every unit of product to possess exactly the same amount of the active ingredient. For that reason, pharmacopeial standards and specifications have been established to provide limits for permissible variations in the amount of active ingredient of individual single-dose units.

Stability of cefuroxime axetil oral suspension at different temperature storage conditions.

Stability testing of an active substance or finished product provides information of the variation of drug substance or final product with time influenced by a variety of environmental factors such as temperature, humidity and light. Knowledge gained from stability studies enables understanding of the effects of the environment on the drugs. The aim of our study was to determine the stability of cefuroxime axetil oral suspension at different temperature storage conditions (stored at room /20 degrees C/ and refrigerated /5 degrees C/ conditions).

Influence of tablet splitting on content uniformity of lisinopril/hydrochlorthiazide tablets.

Dose-related adverse effects of medications are a major problem in modern medical practice. The "correct" dose, based on drug company guidelines in package inserts, may not be correct for many patients. Tablet splitting or dividing has been an accepted practice for many years as a means of obtaining the prescribed dose of medication.

Effect of magnesium stearate concentration on dissolution properties of ranitidine hydrochloride coated tablets.

Most pharmaceutical formulations also include a certain amount of lubricant to improve their flowability and prevent their adhesion to the surfaces of processing equipment. Magnesium stearate is an additive that is most frequently used as a lubricant. Magnesium stearate is capable of forming films on other tablet excipients during prolonged mixing, leading to a prolonged drug liberation time, a decrease in hardness, and an increase in disintegration time.

Physico-chemical characterisation of different clindamycin phosphate samples.

For the majority of the pharmaceutical dosage forms, the substances that are used maintain solid state under the standard storage conditions, i.e. powders.

Iontophoresis: fundamentals, developments and application.

The skin is an excellent barrier to the transport of charged compounds and large molecules. Many substances of present and potential therapeutic utility carry charge at physiological pH, have high molecular weights and/or are hydrophilic and, consequently, do not transport well across the skin. Pathways for the transport of small ions do appear to exist through the skin and flow along these pathways can be substantially enhanced by iontophoresis.