Simulating the Hydrodynamic Conditions of the Human Ascending Colon: A Digital Twin of the Dynamic Colon Model

The performance of solid oral dosage forms targeting the colon is typically evaluated using standardised pharmacopeial dissolution apparatuses. However, these fail to replicate colonic hydrodynamics. This study develops a digital twin of the Dynamic Colon Model; a physiologically representative in vitro model of the human proximal colon. Magnetic resonance imaging of the Dynamic Colon Model verified that the digital twin robustly replicated flow patterns under different physiological conditions (media viscosity, volume, and peristaltic wave speed). During local contractile activity, antegrade flows of 0.06–0.78 cm s−1 and backflows of −2.16–−0.21 cm s−1 were measured. Mean wall shear rates were strongly time and viscosity dependent although peaks were measured between 3.05–10.12 s−1 and 5.11–20.34 s−1 in the Dynamic Colon Model and its digital twin respectively, comparable to previous estimates of the USPII with paddle speeds of 25 and 50 rpm. It is recommended that viscosity and shear rates are considered when designing future dissolution test methodologies for colon-targeted formulations. In the USPII, paddle speeds >50 rpm may not recreate physiologically relevant shear rates. These findings demonstrate how the combination of biorelevant in vitro and in silico models can provide new insights for dissolution testing beyond established pharmacopeial methods.

Pharmaceutical Lozenges: Recent Trends and Developments with an Update on Research and Patents

Pharmaceutical oral dosage forms are tremendously preferred by both consumers as well as pharmaceutical manufacturers owing to the plethora of benefits they offer. Lozenges (LZs) are one of the dosage forms that provide a palatable means of drug administration and have great importance with respect to their pharmaceutical applications. LZs offer additional benefits to pediatric and geriatric patients, along with people having associated problems with the gastro-intestinal tract. Dysphagia is a common problem faced by all age groups, which gives rise to the need for LZs. Moreover, the foremost merit presented by the medicated LZs includes its augmented retention time in the oral cavity that results in an enhanced bioavailability for buccal or upper gastro-intestinal disorders. Further, LZs can also be used to bypass the first-pass effect. The present review covers various aspects of LZs such as formulation, manufacturing techniques, evaluation parameters, marketed products, patents, and a compilation of research work that has been done on lozenges as a delivery system.

Preparation and Evaluation of Diclofenac Sodium Effervescent Tablet

The oral dosage forms are the most popular way of taking medicine although having some disadvantages like deliberate absorption and thus onset of action is extend. This can be overcome by administrating the drug in a liquid form i.e. effervescent tablet. The research is a formulation of diclofenac sodium as a effervescent tablet by wet granulation method. The bitter taste of the drug are masked by added sweetening agent (lactose, glucose etc.) In the present work we are prepared effervescent tablet in that we are used active drug diclofenac sodium and other active ingredient acid like tartaric acid and base sodium bicarbonate in different concentrations. The formulation of tablet was done by using wet granulation, wet granulation is found to be acceptable method of effervescent tablet formulation. The various pre-formulation studies was performed hardness, weight variation, disintegration, dissolution etc.

An Update to Dialysis-Based Drug Release Testing—Data Analysis and Validation Using the Pharma Test Dispersion Releaser

Currently, a wide variety of complex non-oral dosage forms are entering the global healthcare market. Although many assays have been described in recent research, harmonized procedures and standards for testing their in vitro performance remain widely unexplored. Among others, dialysis-based techniques such as the Pharma Test Dispersion Releaser are developed for testing the release of drugs from nanoparticles, liposomes, or extracellular vesicle preparations. Here, we provide advanced strategies and practical advice for the development and validation of dialysis-based techniques, including documentation, analysis, and interpretation of the raw data. For this purpose, key parameters of the release assay, including the hydrodynamics in the device at different stirring rates, the selectivity for particles and molecules, as well as the effect of excipients on drug permeation were investigated. At the highest stirring rate, a more than twofold increase in the membrane permeation rate (from 0.99 × 10−3 to 2.17 × 10−3 cm2/h) was observed. Additionally, we designed a novel computer model to identify important quality parameters of the dialysis experiment and to calculate error-corrected release profiles. Two hydrophilic creams of diclofenac, Voltaren® Emulgel, and Olfen® gel, were tested and provide first-hand evidence of the robustness of the assay in the presence of semisolid dosage forms.

In Vivo Antimalarial Activity of Polyalthia longifolia (Annonaceae) Leaf Extract and Assessment of Its Formulated Oral Dosage Forms

Plant medicine is commonly employed to treat malaria and other infections in Ghana. However, many of these phytomedicines have not been scientifically investigated to justify their use. This study therefore sought to investigate the antimalarial property of Polyalthia longifolia leaves and to formulate suitable dosage forms for ease of administration. A four-day antiplasmodial suppressive and curative study was conducted on ethanol extract of P. longifolia leaves (PLE) using Plasmodium berghei infected albino mice. Tablet and suspension dosage forms of PLE were formulated and evaluated for quality and stability. Statistically significant ( P < 0.05 ) parasitaemia suppression (61.25%) and cure (58.78%) were achieved at a PLE dose of 100 mg/kg, and increases in hematological indices ( P < 0.001 ) were also observed in the PLE-treated mice as compared to the untreated group. The tablets passed the tests for uniformity of weight, friability (<1%), hardness, disintegration (<15 minutes), and in vitro dissolution (>70% release in 45 minutes). The sedimentation volume, rheology, viscosity, and pH of the formulated suspension were within the official specifications. The dosage forms showed consistency in PLE content (85–105%) and no changes in physicochemical properties over the six months period of stability study. The in vivo antimalarial activity of PLE has been established and oral dosage forms that conformed to Pharmacopoeial standards are formulated for use in the management of malaria.

Acceptability of different oral dosage forms in paediatric patients in hospital setting

ObjectiveThe understanding of acceptability of existing dosage forms is limited in most of the world and hinders the development of acceptable, age‐appropriate medicines. The attributes of paediatric medicine acceptability may differ from country to country based on culture, healthcare infrastructure and health policies. This study was designed to map the acceptability of oral medicines in paediatric patients treated in hospital in India.MethodsAn observational, cross-sectional study was conducted in patients aged below 18 years and taking any form of oral medication. Acceptability scores were obtained using CAST–ClinSearch Acceptability Score Test tool.Findings490 patients were recruited and 193 evaluations of different pharmaceutical products available in 20 dosage forms and 7 routes of administration were studied. Oral liquids (50%) and tablets (35%) were the most commonly prescribed and administered forms. Regardless of the therapeutic class and age, the oral liquids were ‘positively accepted’ in infants and toddlers. Acceptability of tablets improved with age and appeared to be generally good from the age of 6.ConclusionThis study indicates the limited progress towards adoption of age-appropriate dosage forms in India and thus impact on the acceptability of existing oral dosage forms. The key challenges posed by the adoption of age-appropriate formulations in India are (1) awareness of importance of appropriate administration and acceptability of medicines to children in India, (2) availability of age-appropriate dosage forms and (3) lack of child-appropriate medicine policies.

Requirements for Additional Strength Biowaivers for Modified Release Solid Oral Dosage Forms in International Pharmaceutical Regulators Programme Participating Regulators and Organisations: Differences and Commonalities

This article describes an overview of waivers of in vivo bioequivalence studies for additional strengths in the context of the registration of modified release generic products and is a follow-up to the recent publication for the immediate release solid oral dosage forms. The current paper is based on a survey among the participating members of the Bioequivalence Working Group for Generics (BEWGG) of the International Pharmaceutical Regulators Program (IPRP) regarding this topic. Most jurisdictions consider the extrapolation of bioequivalence results obtained with one (most sensitive) strength of a product series as less straightforward for modified release products than for immediate release products. There is consensus that modified release products should demonstrate bioequivalence not only in the fasted state but also in the fed state, but differences exist regarding the necessity of additional multiple dose studies. Fundamental differences between jurisdictions are revealed regarding requirements on the quantitative composition of different strengths and the differentiation of single and multiple unit dosage forms. Differences in terms of in vitro dissolution requirements are obvious, though these are mostly related to possible additional comparative investigations rather than regarding the need for product-specific methods. As with the requirements for immediate release products, harmonization of the various regulations for modified release products is highly desirable to conduct the appropriate studies from a scientific point of view, thus ensuring therapeutic equivalence.