Specific Pharmaceutical Applications Research Articles

Unravelling the polymorphic characteristics of carbamazepine through additive-assisted sonocrystallisation

ABSTRACT This paper investigates the influence of additives on the antisolvent crystallisation process of carbamazepine (CBZ) using methanol as the solvent and water as the antisolvent, with ultrasonic irradiation at a specific solvent-to-antisolvent (S/A) ratio of 1:2 and a 30-watt power ultrasonic horn. Various additives, such as Hydroxypropyl Methyl Cellulose (HPMC), Bovine Serum Albumin (BSA), Tween 80, and Sodium Dodecyl Sulphate (SDS), were employed to examine their effects on the morphology, stability (including suspension and thermal stability), crystallinity, and polymorphism of CBZ crystals. Raw CBZ exhibited irregular shapes during crystallisation, while SDS addition resulted in both plate-like and needle-like crystals. Conversely, BSA, HPMC, and Tween 80 induced the formation of needle, plate, and block-like crystal structures, respectively. Suspension stability ranked as SDS > BSA > HPMC > Tween 80. Regarding polymorphism, HPMC favoured Form 1, BSA and SDS favoured Form IV, and Tween 80 favoured Form I. Additionally, Tween 80 depicted similar preference for Form I polymorph as HPMC. Notably, Form II and Form III polymorphs were present to varying degrees in all samples, except for Tween 80. This study provides crucial insights into the controlled crystallisation of CBZ and the impact of additives on crystal properties, offering valuable information for tailoring CBZ crystal production for specific pharmaceutical applications.

Composition and Biological Activities of different Date Seed varieties (<em>Phoenix dactylifera</em>) of Oman: Cultivation Zone Influence

<p>Date (<em>Phoenix dactylifera</em> L.) seeds (pits) account for ca. 10% of the date fruit and it is the date pits that present a major problem to the date palm industry in the USA as a waste product. Currently date pits are employed as a food source for animals and poultry, as a soil fertilizer and also as a road base gravel In order to understand the varietal effects of Omani date seeds on the nutritional properties of dates and to explore the use of this waste product from the food industry, twenty two native date seeds (<em>Phoenix dactylifera</em> L.) including the varieties; Qushbu Narenjahn, Fardh, Naghal, Manhi, Qush Balquan, Helali Oman, Khasab, Seedi, Qush Jabrin, Khalas, Qush Basrah, Qushbu Maan, Handal, Khunaizi, Qush Mamoor, Barshi, Barni, Azad, Zabad, Qush Tabak, Qush LuLu, and Halali Alhasa were collected from six regions of the Sultanate of Oman and were examined for their nutritional value, antioxidant and urease properties. Energy values, dry matter, and carbohydrate level were the predominant components examined in the date seeds , followed by fiber, moisture, along with small amounts of ash, protein, and fat. The results of the 22 varieties of date seeds showed a significant energy value of between 283.0 to 407.9 kcal/100g, dry matter of between 93.3%-96.3%, carbohydrate content of between 43.8%-80.6%, moisture in the range of 4.3%-6.6%), fat in the range of 5.0%-10.9%, ash content of between 0.73%-1.08%, protein content of 0.2%-6.9% and fiber content of between 5.0%-32.5%. Furthermore the antioxidant potential ranged between 7.4 - 88.3% depending upon the type of date seeds and location of samples. In this regard the Handal date seeds collected from Al-Hamra showed the highest antioxidant potential with 88.3% inhibition. Similarly urease inhibition ranged from 0.94-70.3% and Qush Tabak date seeds collected from Al-Hamra demonstrated the highest urease potential with 70.3% inhibition. It is noteworthy that Qush Basrah, Seedi, Qush Balquan, and Handal date seeds have significantly higher nutritional attributes compared to the rest in the study group. Moreover Fardh, Khasab, Khalas, and Handal date seeds collected from more than one region of Oman showed variation in some nutritional values. The nutritional analysis further demonstrated the correlation of proximate parameters in different regions of Oman. Results of the current investigation indicate a promising and significant potential for date seeds to be used as a supplementary source of a healthy diet as well as in specific pharmaceutical applications.</p>

Formulation and characterization of a biocompatible microemulsion composed of mixed surfactants: lecithin and Triton X-100

We report on the formation and characterization of a biocompatible microemulsion (ME) system composed of lecithin (L), Triton X-100 (T) as the surfactant(s), butyl lactate (BL) as the cosurfactant, and isopropyl myristate (IPM) as the oil phase and water. Detailed phase construction reveals that mixing of surfactants (L and T) produces larger single-phase ME region compared to L. In the mixed surfactant systems, a three-phase body appears which is otherwise not obtained in the single surfactant counterparts signifying the synergistic solubilization behaviour upon mixing. The maximum solubilization capacity decreases as the content of T increases in the mixture. Viscosity, conductance and adiabatic compressibility measurements of the single-phase ME systems at a constant amphiphile concentration (80 % w/w) show a linear trend with increasing water content revealing a droplet-type structure of all the studied formulations. FTIR studies in the water-in-oil (w/o) region identify the presence of three distinct types of water molecules in these systems and their relative content changes with the interfacial composition as well as the total water content in the system. Our study offers a biocompatible mixed ME system in which the physical properties do not differ much from those of the lecithin-based systems with the additional advantage of having higher solubilization capacity, low pH dependency and low viscosity, which renders its potential to be used for specific pharmaceutical applications.

Synthesis, characterization and in-vitro antitubercular activity of isoniazid-gelatin conjugate

A novel and simple method to synthesize antitubercular-protein conjugate by solid phase synthesis was developed employing a carboxypolystyrene resin. The aim was to covalently bind a drug with antitubercular activity, isoniazid, to a biomacromolecule, gelatin, widely used in the pharmaceutical, cosmetic and food industry. Calorimetric and (1) H NMR analyses were performed to verify the bond formation between the antitubercular drug and gelatin. After absorption isoniazid delivers toxic metabolites and so an oxidation test with tert-butyl hydroperoxide was performed to assess the amount of toxic metabolites released from the prodrug (gelatin linked to isoniazid), compared with isoniazid itself. Spectrophotometric analysis revealed that the protein derivative was an excellent isoniazid prodrug since there was a 40% reduction in release of toxic metabolites (isonicotinic acid) by the prodrug. The results clearly showed that antitubercular moieties, covalently linked to a natural polymer, allowed the introduction of peculiar features for specific pharmaceutical applications into the macromolecule. In addition, antitubercular activity of the new polymer was determined by Middlebrook 7H11 medium against Mycobacterium tuberculosis complex. The new isoniazid-gelatin conjugate showed significant antitubercular activity and for this reason should be useful as an efficacious tool in the treatment of tuberculosis.

ChemInform Abstract: Tin in Pharmacy and Nutrition

The occurrence of tin in plants, animals and humans is discussed in relation to its abundance in the lithosphere and hydrosphere and the range of different tin(II) and tin(IV) complexes formed. A reasoned consideration of the essentiality or otherwise of tin for living species is given and it is concluded that tin is beneficial even if not yet proved to be an essential element. After reference to the chemistry of tin compounds, there is a detailed discussion of their toxicity in animals and humans. Feasible routes for tin intake and uptake into humans are described. The use of tin pharmaceuticals in previous and current times is reviewed and areas for which they are currently permitted for use in man as dentifrices and mouth washes, as radiopharmaceuticals and for the treatment of jaundiced newborns are described. A detailed review of tin-coating antitumour agents as representative tin pharmaceuticals is given. Finally, a range of tin compounds having other specific pharmaceutical applications and which are currently being investigated are listed.

Application Of Power Ultrasound For Nano-Particle Size Reduction Of Active Pharmaceutical Ingredients

Properties of drug substances and dosage forms can be highly affected by the particle size, a critical process parameter in pharmaceutical production. The fundamental issue with particle size analysis is the variety of equivalent particle diameters generated by different methods, which is largely ascribable to the particle shape and particle dispersion mechanism involved. Thus, to enable selection of the most appropriate or optimal sizing technique, cross-correlation between different techniques may be required. This review offers an in-depth discussion on particle size analysis pertaining to specific pharmaceutical applications and regulatory aspects, fundamental principles and terminology, instrumentation types, data presentation and interpretation, in-line and process analytical technology. For illustration purposes, special consideration is given to the analysis of FXD.

The role of UHPLC in pharmaceutical development

Pharmaceutical separations can be divided into three categories: high throughput, high productivity, and high resolution. These categories contain specific pharmaceutical applications, each of which has distinct separation goals. Traditionally, these goals have been achieved utilizing conventional HPLC with typical column dimensions and particle sizes. The recent introduction of ultra-HPLC (UHPLC) has provided a new potential for method development and analysis. Pharmaceutical chemists must determine the impact of this emerging technology. UHPLC is achieved by using sub-2 microm particle size column packing at increased linear velocities. In order to utilize this technology, mobile phase viscosity must be minimized or the chromatography system must be redesigned to withstand an increased backpressure. Today, there are many commercially available UHPLC systems capable of exceeding conventional pressure limits of 400 bar. The advantage of UHPLC over conventional HPLC is the capability to increase the speed without sacrificing efficiency. In comparison to traditional HPLC, our research showed that UHPLC can decrease run times up to 7 x. In addition, for high resolution applications, UHPLC achieved significant efficiency advantages over traditional HPLC. This paper will evaluate the potential roles for utilizing UHPLC in the pharmaceutical industry.

Particle Size Analysis in Pharmaceutics: Principles, Methods and Applications

Physicochemical and biopharmaceutical properties of drug substances and dosage forms can be highly affected by the particle size, a critical process parameter in pharmaceutical production. The fundamental issue with particle size analysis is the variety of equivalent particle diameters generated by different methods, which is largely ascribable to the particle shape and particle dispersion mechanism involved. Thus, to enable selection of the most appropriate or optimal sizing technique, cross-correlation between different techniques may be required. This review offers an in-depth discussion on particle size analysis pertaining to specific pharmaceutical applications and regulatory aspects, fundamental principles and terminology, instrumentation types, data presentation and interpretation, in-line and process analytical technology. For illustration purposes, special consideration is given to the analysis of aerosols using time-of-flight and cascade impactor measurements, which is supported by a computational analysis conducted for this review.

Tin in pharmacy and nutrition

AbstractThe occurrence of tin in plants, animals and humans is discussed in relation to its abundance in the lithosphere and hydrosphere and the range of different tin(II) and tin(IV) complexes formed. A reasoned consideration of the essentiality or otherwise of tin for living species is given and it is concluded that tin is beneficial even if not yet proved to be an essential element.After reference to the chemistry of tin compounds, there is a detailed discussion of their toxicity in animals and humans. Feasible routes for tin intake and uptake into humans are described.The use of tin pharmaceuticals in previous and current times is reviewed and areas for which they are currently permitted for use in man as dentifrices and mouth washes, as radiopharmaceuticals and for the treatment of jaundiced newborns are described. A detailed review of tin‐coating antitumour agents as representative tin pharmaceuticals is given.Finally, a range of tin compounds having other specific pharmaceutical applications and which are currently being investigated are listed.