Physicochemical properties of various alginate-based raft-forming antacid products: a comparative study

Background: Alginate-based, raft-forming antacid products with reflux suppressant activity are complex formulations expected to achieve effective raft formation and cause elimination or displacement of the acid pocket, which is typically manifested in gastroesophageal reflux disease (GERD).Methods: In the present study, six alginate-based raft-forming products commercially available in the Indian market were compared in terms of their acid neutralization properties, strength, resilience and structural and thermal properties of their rafts. Percent alginate content was also determined.Results: Rafts of products containing calcium-based antacids formed voluminous, porous and floating rafts within seconds of addition to the simulated gastric fluid (SGF) compared with the products that contained aluminium and magnesium-based antacids. Marked differences were not evident in the ANC (acid neutralization capacity) values of the various products. No correlation was observed between ANC and raft-forming capacity or duration of neutralization. Raft structures affected their neutralization profiles. Rafts of porous and absorbent nature could retain their ANC probably due to release of trapped antacids. Further, raft strengths of only two products were above the British Pharmacopoeia specification of not less than 7.5 g. Sodium alginate content was within specifications (85-115%) for three of the six products.Conclusions: Raft-forming formulations with higher alginate content and calcium-based antacids have better physicochemical properties such as ANC, neutralization profiles, raft strength and raft resilience than those with lower alginate content or those containing aluminium or magnesium-based antacids.

Determination of Vancomycin B and Vancomycin Impurities by Liquid Chromatography

The preferred test methods for control of product-related impurities in medicinal products are high-performance liquid chromatography (HPLC) with a fine sorbent, and ultra-performance liquid chromatography (UPLC), which allow for better chromatographic separation of active substances and related impurities, reduction of time costs, and saving of material resources. The aim of the study was to develop HPLC and UPLC test procedures and assess the chromatographic separation capacity and efficiency in order to improve determination of the main vancomycin component and related impurities. Materials and methods: vancomycin hydrochloride lyophilisate for oral solution and solution for injection, and vancomycin hydrochloride reference standard (USP RS) were used as test objects. Agilent 1290 Infinity liquid chromatography system, and Chromolith® Performance RP-18e, Kinetex C18, Nucleodur C18 Isis, Zorbax RRHD Eclipse Plus C18, and LiChrospher® RP-18 columns were used for the testing. Results: HPLC analysis using a Chromolith® column (100×4.6 mm) reduces the testing time by 10 minutes compared to the USP test procedure, and by 15 minutes compared to the British Pharmacopoeia procedure. The proposed test procedure requires less eluent and increases chromatographic separation efficiency. UPLC analysis using a Kinetex C18 column (50×4.6 mm, 2.6 μm) made it possible to reduce the testing time by two thirds compared to the British Pharmacopoeia procedure. The use of isocratic elution greatly simplified the testing. The testing time under the proposed chromatographic conditions was 10 minutes. Conclusions: the selected HPLC and UPLC test conditions made it possible to significantly reduce the time of testing, minimise the use of expensive reagents, and increase efficiency of chromatographic separation in the determination of vancomycin impurities and the main component Vancomycin B.

An Internal Standard High-Performance Liquid Chromatography Method for Simultaneous Quantification of Candesartan and Hydrochlorothiazide in Combined Formulations

The internal standard method is a versatile procedure that avoids misleading results caused by the instability of the chromatographic system or inexperienced workers. It is an effective way to judge the accuracy of any obtained data. As the detector responses of chlorzoxazone (CZN) resemble those of candesartan (CDZN) and hydrochlorothiazide (HCTZ), CZN was employed as an internal standard. Herein, a simple chromatographic method was established for quantification of CDZN and HCTZ. Isocratic elution was conducted using 1% premixed acetonitrile/formic acid (7:3 v/v) at a 0.8 mL/min flowrate. The separation of the three components was maintained using the universal 20 µL loop, and for further simplicity in application, the analysis was optimized at 25 °C. CDZN, HCTZ, and CZN were simultaneously monitored and quantified at 270 nm. The method developed here complies with all the validation limits according to the British Pharmacopoeia (BP), United States Pharmacopoeia (USP), and the guidelines of the International Council ForHarmonisation (ICH). The method proved to be linear in the range of 6.4 to 25.6 µg/mL and 5.0–20 µg/mL for CDZN and HCTZ, respectively, while the quantitation detection limits were less than 1.0µg/mL for both.

The Regulation of Biological and other Innovative Medicinal Products

This chapter discusses the phrase ‘biological medicinal product’, which is used to refer to products manufactured by biological or biotechnology means or to advanced therapy medicinal products. It examines biological medicinal products that are considered peptides or proteins and are made up of one or more linear sequences of amino acids. It also talks about the compliance of biological products with a minimum quality standard set by the British Pharmacopoeia or European Pharmacopoeia, which includes specific instructions for testing sterility, bacterial endotoxins, microbial limits, volume in container, uniformity of dosage units, and particulate matter. The chapter highlights biological products that are manufactured using recombinant cells and are extracted or made from unaltered tissues or blood that are purified in the same way as recombinant products. It explores the inherent heterogeneity of biological products as it comprises of a mixture of closely related molecules.

In vitro quality evaluation of brands of promethazine tablets marketed in Edo State, Nigeria

The increasing number of multisource pharmaceuticals has necessitated the need for continuous quality assessment of products available for atients’ consumption. Promethazine is an anti-histamine used in cases of nausea, vomiting, motion sickness etc. The study was to examine the in vitro quality parameters for ten brands of promethazine hydrochloride tablets sold in retail pharmacies in Edo State, Nigeria. The parameters determined were identification, weight variation, friability, hardness, disintegration, dissolution rate and assay. All samples were evaluated for conformity with British Pharmacopoeia (BP) 2017 standards. Results obtained showed tablet weight ranging from 0.08 g ± 1.77 % to 0.255 g ± 3.557 %, hardness from 4.36 ± 0.58 to 8.33 ± 3.21 kg/cm2, friability of < 1 %, disintegration time of 2.47 ± 0.90 to 69.66 ± 7.23 min and assay of 61.32 ± 2.04 to 183.19 ± 0.11%. The ten batches but one released more than 80 % of their drug content within 30 min. Analysis of similarity factor revealed other samples but PR-7 can be interchangeable with PR-1 based on dissolution profile. The results showed that not all samples examined passed all the pharmacopoeia tests for satisfactory quality. Thus, they all cannot be used interchangeably in clinical practice. Keywords: Promethazine; Quality Control; Dissolution; Pharmacopoeial specifications

Application of microcrystalline cellulose obtained from Gossypium herbaceum in direct compression of chlorpheniramine maleate tablets

The flow, tableting and in vitro release properties of directly compressed chlorpheniramine maleate (CPM) tablets containing fluid bed dried and lyophilized microcrystalline cellulose (MCC) obtained from Gossypium herbaceum (GH) were investigated. Delignification of dried GH linters was done through the soda process to obtain alpha cellulose which was hydrolyzed with 2.0 N hydrochloric acid to get MCC. The MCC was washed with water until neutral. Drying was done by either fluid bed method or lyophilization to obtain MCC-GossF and MCC-GossL respectively. Chlorpheniramine tablets containing 20, 30 and 40% of the MCCs were prepared by direct compression method. Avicel PH102 (AVH-102) served as comparing standard. Using standard methods, evaluation of the powders and the tablets was done. The evaluated parameters of the powders and tablets conformed to the British Pharmacopoeia specifications. The CPM tablets containing MCC-GossF (coded CGF) had better flow but were not mechanically as strong as those containing MCC-GossL (coded CGL). The hardness and disintegration times of the tablets were in the order of CGF < CGL and the friability was in the order of CGF > CGL. Similar parameters of DCL compared well with CPM tablets containing AVH-102 (coded DAV). The MCC obtained from GH had dilution potential up to 40% except in CGF-4 tablets. The in vitro dissolution showed > 80% CPM release from all the batches within 30 min. The release kinetics were of mixed order while the mechanism of drug release was Fickian. The MCCs served as good directly compressible binder for chlorpheniramine maleate.

Production and Evaluation of Disintegrant Properties of Microcrystalline Cellulose Derived from SaccharumofficinarumL (Poaceae) in Metronidazole Based Formulation

The aim of the study was to produce microcrystalline cellulose from Saccharumofficinarum and to evaluate its use as a disintegrant in metronidazole tablet formulation. Cellulose was produced and characterized. This was followed by a comparative characterization of the tablets formulated by using Saccharumofficinarummicrocrystalline cellulose (SO-MCC), maize starch and crosscarmellose sodium (Ac-di-sol®) as disintegrants. The granules were evaluated for flow properties and the tablet evaluated for hardness, friability, disintegration and dissolution properties. For disintegration studies, the disintegrants disintegrated within 10 minutes in this order: Ac-di-sol® >SO-MCC>Maize starch. All the tablets exhibited high release profile which conformed to British Pharmacopoeia standards. Hence, SO-MCC can be used as an alternative disintegrant in terms of cost and availability.

Quantifying the Effects of Vibration on Medicines in Transit Caused by Fixed-Wing and Multi-Copter Drones

The concept of transporting medical products by drone is gaining a lot of interest amongst the medical and logistics communities. Such innovation has generated several questions, a key one being the potential effects of flight on the stability of medical products. The aims of this study were to quantify the vibration present within drone flight, study its effect on the quality of the medical insulin through live flight trials, and compare the effects of vibration from drone flight with traditional road transport. Three trials took place in which insulin ampoules and mock blood stocks were transported to site and flown using industry standard packaging by a fixed-wing or a multi-copter drone. Triaxial vibration measurements were acquired, both in-flight and during road transit, from which overall levels and frequency spectra were derived. British Pharmacopeia quality tests were undertaken in which the UV spectra of the flown insulin samples were compared to controls of known turbidity. In-flight vibration levels in both the drone types exceeded road induced levels by up to a factor of three, and predominant vibration occurred at significantly higher frequencies. Flown samples gave clear insulin solutions that met the British Pharmacopoeia specification, and no aggregation of insulin was detected.

Scutellaria baicalensis – a small plant with large pro-health biological activities

Scutellaria baicalensis, known also as Huang-Qin is a traditional Chinese plant used in medicine for at least 2000 years. The plant is widely distributed in Japan, Korea, Mongolia and Russia, and is listed in Chinese Pharmacopoeia, European Pharmacopoeia and British Pharmacopoeia. The interest in Huang-Qin results from various biological activities which are primarily related to secondary plants metabolites consisting of flavonoids, phenolic compounds and terpenes. It is known that the compounds are active against numerous diseases and protect the organism against harmful pathogenic agents. Particular attention is paid to baicalein, wogonin and oroxylin A – which are characteristic secondary metabolites of the plant. In this paper, we focused on phytochemical analysis and selected biological activities used in periodontal and cardiovascular problems. The presented studies confirm the ability of Huang-Qin to scavenge free radicals, moreover, that it presents anti-bacterial, anti-inflammatory and enzyme inhibitory activities.

Comparative Quality of Different Brands of Metformin Tablet Marketed in Zaria, Nigeria.

Background: Metformin tablets are oral anti hyperglycaemic agents that are used as the first line agent in the management of type 2 diabetes mellitus. The proliferation of many brands of metformin tablets in the market has led to availability of different types; some of which may be substandard or counterfeit. Thus, the need to determine the quality of the various brands marketed in Zaria. Objective: To compare the quality of different brands of metformin tablets that are available in Zaria using British pharmacopoeia standards. Method: Seven brands of metformin tablet (500 mg) were randomly sampled from various community pharmacies within Zaria and analysed with respect to identification, weight variation, friability, disintegration time, dissolution and drug content assay using Pharmacopoeial standards. Results: Except for the dissolution and assay tests, the results of all the other parameters for the various brands were within the Pharmacopoeial limits. The percentage content of metformin in brand 2 was 89.90 % which is outside the official range (95 – 105 %). Furthermore, only 70.61, 75.34 and 70.58 % of metformin dissolved from brands 2, 4 and 7 respectively, after 30 minutes of the dissolution test. Conclusion: It can be concluded that of the seven brands evaluated, only four brands are interchangeable with each other and can be substitutes of each other.