Current Issue : October - December Volume : 2016 Issue Number : 4 Articles : 6 Articles
Chitin, the excellent biocompatible and biodegradable polymer, does not find much practical applications in the\npharmaceutical and biomedical fields owing to its insolubility in common solvents. This aspect has been discoursed by the\nsynthesis of mixed ester derivatives (acetyl and propionyl) of chitin. In the present investigation, the sustained release potential\nof the synthesized chitin co-(acetate/propionate) copolymers has been evaluated by formulating the matrix tablets of metformin\nhydrochloride (MFH) and comparing them with the marketed sustained release tablets (Glycomet�®-500 SR). IR investigations\nconfirmed the absence of drug polymer interactions in the developed formulations. Although, all the batches of formulated\ntablets showed somewhat sustained release of the drug, but the drug release profile of formulation F7 (containing AA70/PA30\nCAPC copolymer) was almost similar to that of the marketed formulation and both of them showed drug release up to 12 hours.\nThe drug release from the formulations F8 and F9 (containing AA80/PA20 and AA90/PA10 CAPC copolymers, respectively) was\nstill slower indicating their use at a lower concentration. Therefore, the outcomes of the present study indicates AA70/PA30,\nAA80/PA20 and AA90/PA10 CAPC copolymers as attractive matrix forming agents for sustained release tablets of MFH....
The choice of proper excipients is one of the key factors for successful formulation of pharmaceutical dosage forms. Increasing number of new therapeutic compounds suffers from poor solubility and/or bioavailability, creating a challenge from the drug formulation point of view. Problems have also been encountered in attempts to formulate biological drugs such as peptides and proteins, considering their sensitivity towards certain production processes and routes of administration. In both cases the choice of the right excipient(s) is essential to provide particular process ability and development of systems with desirable drug delivery kinetics. The aim of this work was to evaluate pharmaceutical applications of nanofibrillar cellulose (NFC), a renewable, biodegradable and widely available plant based material, as a potential excipient in the production of pharmaceutical dosage forms. Initially, tablets with immediate drug release were manufactured by methods of direct compression using spray dried NFC as a filler material. Addition of NFC improved the flow properties of commercially available and widely used microcrystalline cellulose. The main focus of the research was to evaluate NFC material for immediate drug release purposes. This goal was successfully achieved by setting up a spray drying method for the production of drug loaded NFC solid dispersion. System was able to fast the drug release over short periods of time. The purpose of this study was to further clarify and fully understand the mechanisms behind the successful performance of NFC as immediate drug release material. Binding of drugs to NFC due to the electrostatic interactions was observed. This kind of knowledge is beneficial when choosing the proper drug/excipient combination for the formulation process. In conclusion, NFC was shown to be a versatile excipient for the production of pharmaceutical dosage forms, while the comprehensive evaluation of the full potential of NFC in pharmaceutical applications warrants further experiments in the future....
The availability of licensed paediatric drugs is lagging behind those for adults,\nand there is a lack of safe formulations in suitable doses that children are able and willing to\ntake. As a consequence, children are commonly treated with off-label or unlicensed drugs. As\noff-label and unlicensed drug use are associated with a greater risk for harm than on-label\ndrug use, a range of global initiatives have been developed to realize Bbetter^ medicines for\nchildren. This review describes the challenges and achievements of the European Union to\nrealize this goal, with a focus on paediatric drug development and formulation design. In\n2007, a European Paediatric Regulation was installed enforcing companies to consider\nchildren in the early development of drugs with a new drug substance, for a new indication or\nwith a new route of administration. The Regulation, e.g. requires companies to develop a\npaediatric investigation plan discussing the proposed clinical trials in children of different\nages and the formulations for future marketing. Since 2013, the pharmaceutical design of any\nnewly marketed paediatric drug should comply with the BGuideline on the Pharmaceutical\nDevelopment of Medicines for Paediatric Use.^ Companies should, e.g. justify the route of\nadministration, dosage form, formulation characteristics, safety of excipients, dosing\nfrequency, container closure system, administration device, patient acceptability and user\ninformation. In this review, the guideline�s key aspects are discussed with a focus on novel\nformulations such as mini-tablets and orodispersible films, excipients with a potential risk for\nharm such as azo dyes and adequate user instructions....
Introduction: In this study, physical and chemical characteristics of Lamivudine, Tenofovir Disoproxil\nFumarate (TDF) and potential excipients were systematically followed and documented [1].\nObjective: The objective of this scientific work was to carry out pre-formulation studies including\ncompatibility studies on Lamivudine and Tenofovir Disoproxil Fumarate with their potential excipients\nprior a direct compression process [2]. Methodology: The interaction was studied in three set\nof environments namely uncontrolled room conditions for Zone VI b (30 �± 2), oven conditions in\nwhich the oven was set at 50 and accelerated climatic conditions in which a climatic chamber was\nset at 40 �± 2/75% �± 5% Relative Humidity (RH %). Sample preparation was done by mixing the\namount of formulation excipients to active substances at a ratio of 1:10, whereas active substance to\nanother active substance at a ratio of 1:1, active substance to coating materials at 1:4, coating materials\nto the whole set of excipients 1:4. The whole set of samples was geometrically mixed and triturated\nby mortar and pestle to very fine uniform powder to ensure homogeneity of the mixture. HPLC\nanalytical method was used for simultaneous quantitative determination of lamivudine and tenofovir\ndisoproxil fumarate. Transmittance of the mixture was determined by Near Infra-Red (NIR)\ntechnique. Results: The amount of Lamivudine as on day 0 was comparable to day 90 for in all tested\nconditions (Room, Oven and Climatic Chamber), whereas for Tenofovir Disoproxil Fumarate only the\namount of the drug at Room (30 �± 2) was comparable to results on day 90. A significant drop of\namount of Tenofovir Disoproxil Fumarate (TDF) exposed to moisture (Climatic chamber at 40 �± /75% �± 5% Relative Humidity (RH %)) and temperature of 50 was observed. Colour change\nwas observed for samples subjected to moisture (Climatic chamber at 40 �± 2/75% �± 5% Relative\nHumidity (RH %)) and as well picked up in the NIR region 400 to 1500 cm1 (Finger print region) by\na significant shift in Transmittance. Conclusion: It can be concluded that microcrystalline cellulose,\ncross linked sodium carboxymethyl cellulose, magnesium stearate and sodium carbxymethyl cellulose\ncan be compressed together with Lamivudine and Tenofovir Disoproxil Fumarate (TDF) to\nproduce a pharmaceutically acceptable solid dosage form, tablet. The produced tablets should be\npacked in moisture and light protective containers as Tenofovir Disoproxil Fumarate (TDF) has\ndiester linkages which can be hydrolysed into the active drug Tenofovir in the presence of moisture....
Extraction, purification and synthesis of acetylated cassava starch was undertaken. The degree of modification for\nthe acetylated (modified) starch was calculated to be 0.03. Physicochemical indices interrogated were all significantly\n(P<0.05) affected by the acetylation. Microstructural studies revealed starches that were predominantly polygonal in\nshape. The FTIR results confirmed introduction of an acetyl group with a new band at 1728 cm-1. The results further\nshow that, the modification did not degrade the granule morphology, but x-ray pattern showed increased crystallinity\nin the acetylated derivative. Thermogravimetric analysis and differential scanning calorimetry revealed 2 phase\ndecomposition of both starches and improved gelation capacity with new peaks respectively. Rifampicin (RIF) loaded\nstarch-stabilized silver nanoparticles yielded good mean particle size (248 nm), polydispersity index (0.276) and zeta\npotential (18.68 mV). There was a significant (P<0.01) sustained release of RIF from the nano formulations up to 14.0\nh. Antimicrobial susceptibility tests show that, the nano formulation exhibited good antimicrobial activity. It is therefore\nconcluded that, acetylated cassava starch could be a good stabilizer and vehicle for drug delivery....
This work was aimed at the use of dissolution testing and similarity factor to assess the\nlevel of damage taken by active drug microspheres during compression in tablet dosage form.\nTo achieve that, combinations of suitable excipients were used to protect drug microspheres\nduring compression. The excipients were used in the form of powders, granules or placebo\npellets prepared by extrusion-spheronization technology. The excipients were evaluated alone,\nin combinations and post-compression into compacts. Preliminary experiments included\nassessing density, hardness, friability and disintegration of all the selected excipients. Based on\nsuch experiments it was found that the flowability of combination of powders was more\nacceptable than individual excipients. Two combinations of microcrystalline -starch and\nmicrocrystalline cellulose -calcium carbonate granules were selected to be compressed with\npellets of the active pharmaceutical ingredient ketoprofen. In all the combinations used there\nwas a significant amount of damage to drug pellets. The kinetics of drug release appears to\nfollow the zero-order rate, which remained unchanged even when a significant degree of\ndamage to pellets occurs. It was found that a high level of excipients is required in order to\nprepare microspheres as a rapid disintegrating tablet....
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