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Molecules (Basel, Switzerland) Nov 2022The chemical stability of diphenhydramine (DIPH), azelastine (AZE) and bepotastine (BEPO) was examined in solutions and solids. The drugs were subjected to high...
Chemical Stability Study of H Antihistaminic Drugs from the First and the Second Generations, Diphenhydramine, Azelastine and Bepotastine, in Pure APIs and in the Presence of Two Excipients, Citric Acid and Polyvinyl Alcohol.
The chemical stability of diphenhydramine (DIPH), azelastine (AZE) and bepotastine (BEPO) was examined in solutions and solids. The drugs were subjected to high temperature (70 °C for 35 h) or UV/VIS light (18.902−94.510 kJ/m2) at pH 1−13, to examine their percentage degradation and kinetics of degradation. Further, the stability of solid DIPH, AZE and BEPO was examined in the presence of excipients of different reactivity, i.e., citric acid (CA) and polyvinyl alcohol (PVA) under high temperature/high humidity (70 °C/80% RH) or UV/VIS light (94.510 kJ/m2). Under high temperature, DIPH degraded visibly (>19%) at pH 1 and 4, AZE was shown stable, while the degradation of BEPO was rather high (>17%) in all pH conditions. Under UV/VIS irradiation all the drugs were shown labile with degradation in the range 5.5−96.3%. As far as the solid mixtures were concerned, all drugs interacted with excipients, especially under high temperature/high humidity or UV/VIS light. As a result, DIPH, AZE and BEPO were compared in terms of their stability, with regard to their different structures and acid/base properties. All these results may be helpful for manufacturing, storing and applying these drugs in their topical (skin, nasal and ocular), oral and injectable formulations.
Topics: Excipients; Drug Stability; Polyvinyl Alcohol; Diphenhydramine; Citric Acid; Histamine Antagonists
PubMed: 36500415
DOI: 10.3390/molecules27238322 -
Environmental Health Perspectives Nov 2012
Topics: Dietary Supplements; Environmental Exposure; Excipients; Nonprescription Drugs; Phthalic Acids; Prescription Drugs
PubMed: 23117125
DOI: 10.1289/ehp.1205763 -
Polimery W Medycynie 2014Natural polymers have been used as pharmaceutical excipients. They are easily available, cheap, less toxic andbiodegradable. Many of them have been identified and...
BACKGROUND
Natural polymers have been used as pharmaceutical excipients. They are easily available, cheap, less toxic andbiodegradable. Many of them have been identified and research is ongoing regarding their characterization.
OBJECTIVE
The present study depicts the extraction and characterization of Aegle marmelos derived polymer which can be used as a pharmaceutical excipient.
MATERIAL AND METHODS
A water based extraction method was used to extract Aegle marmelos derived polymer. Its yield was found to be 15.07%. Characterization was based on various parameters such as a test for carbohydrates, test for purity, organoleptic properties, ash value, solubility behavior, pH, swelling index, surface tension, viscosity, particle size, loss on drying, bulk density, bulkiness, powder flow behavior, etc.
RESULT
The polymer was yellowish-brown and showed poor flow (angle of repose 19.28 degrees ± 0.883) with neutral pH, i.e. 7, and bulkiness depicting the heaviness of polymer. The extracted polymer showed solubility in warm water and insolubility in organic solvents.
CONCLUSIONS
The results easily predict the fact that the yield of the polymer was quite good, so it can be used as a commercial source of mucilage. The isolated polymer can be used as a pharmaceutical excipient in different dosage forms. 2 /
Topics: Aegle; Excipients; Hydrogen-Ion Concentration; Plant Extracts; Polymers; Powders; Solubility; Solvents; Viscosity
PubMed: 25696938
DOI: No ID Found -
International Journal of Molecular... Jul 2023The excess of free radicals causes numerous imbalances in the body that lead to premature aging, the degradation of internal structures, and the appearance of numerous...
The excess of free radicals causes numerous imbalances in the body that lead to premature aging, the degradation of internal structures, and the appearance of numerous pathologies responsible for the increased risk of premature death. The present work aims to evaluate the physical, chemical, pharmacotechnical, and antioxidant activity of newly achieved capsule formulations. These two formulations were , which contains melatonin:biotin:coenzyme Q10 (weight ratio of 1:2:60), and which contains quercetin:resveratrol:biotin:coenzyme Q10 (weight ratio of 10:10:1:10). The adequate selection of the excipient types and amounts for final capsule formulations (, ) was based on preformulation studies performed on the powders containing active ingredients. The antioxidant activity assessed using three methods (ABTS, DPPH, and FRAP) compared with acid ascorbic as a positive control demonstrated that the formulation possesses the strongest antioxidant capacity. The results confirmed the suitable formulation and the accurate selection of the types and amounts of active ingredients, as well as the auxiliary excipients used in newly developed capsule formulations as supplements with an excellent antioxidant effect on the human body.
Topics: Humans; Antioxidants; Biotin; Resveratrol; Dietary Supplements; Quercetin; Excipients
PubMed: 37511185
DOI: 10.3390/ijms241411426 -
AAPS PharmSciTech Apr 2015Oral drug delivery is a non-invasive and therefore a very convenient route of administration. Orally disintegrating dosage forms, like soluble films and (mini-)tablets,... (Review)
Review
Oral drug delivery is a non-invasive and therefore a very convenient route of administration. Orally disintegrating dosage forms, like soluble films and (mini-)tablets, appear promising for use in the pediatric population. New guidance for the development of pediatric medicines has been published, which provides considerations on how pediatric products should be designed. However, most of the considerations leave a lot of room for interpretations. Bearing in mind the different aspects discussed in the latest guideline, the use of orally disintegrating films and tablets, in particular, small-sized tablets, is discussed and reflected upon by providing evidence from the scientific literature. The available dosage forms for children are various and examples of currently licensed products for use in the pediatric population were compiled. Aspects such as the appropriateness for pediatrics, the choice of excipients, the opportunities for modified drug release preparations or fixed-dose combinations, the acceptability and palatability, and also limitations were discussed with respect to the new dosage forms of orally disintegrating films and mini-tablets. This paper points out that innovation in pediatric medicines are planned and should be encouraged; however, supported by the regulatory guidance, only general considerations are provided. Nevertheless, the guideline summarizes multiple points to consider during the development of medicines for pediatric use. Considering the scientific evidence and the regulatory guidance, orally disintegrating dosage forms, like soluble films and (mini-)tablets, offer an innovative solution for pediatric drug delivery.
Topics: Administration, Oral; Animals; Drug Delivery Systems; Excipients; Humans; Pediatrics; Tablets
PubMed: 25739913
DOI: 10.1208/s12249-015-0313-1 -
Advanced Drug Delivery Reviews Nov 2022Selecting the appropriate formulation and solubility-enabling technology for poorly water soluble drugs is an essential element in the development of formulations for... (Review)
Review
Selecting the appropriate formulation and solubility-enabling technology for poorly water soluble drugs is an essential element in the development of formulations for paediatric patients. Different methodologies and structured strategies are available to select a suitable approach and guide formulation scientists for development of adult formulations. However, there is paucity of available literature for selection of technology and overcoming the challenges in paediatric formulation development. The need for flexible dosing, and the limited knowledge of the safety of many formulation excipients in paediatric subjects, impose significant constraints and in some instances require adaptation of the approaches taken to formulating these drugs for the adult population. Selection of the best drug delivery system for paediatrics requires an efficient, systematic approach that considers a drug's physical and chemical properties and the targeted patient population's requirements. This review is a step towards development of a strategy for the design of solubility enhancing paediatric formulations of highly insoluble drugs. The aim of this review is to provide an overview of different approaches and strategies to consider in order to assist development of paediatric formulation for poorly water-soluble drugs with the provision of examples of some marketed products. In addition, it provides recommendations to overcome the range of challenges posed by these strategies and adaptations of the adult approach/product presentation required to enable paediatric drug development and administration.
Topics: Administration, Oral; Adult; Child; Drug Delivery Systems; Excipients; Humans; Pharmaceutical Preparations; Solubility; Water
PubMed: 36049580
DOI: 10.1016/j.addr.2022.114507 -
Journal of Pharmaceutical Sciences May 2022Although many therapeutically active peptides and proteins have been developed there is a lack of topical pharmaceutical products on the market containing these...
Although many therapeutically active peptides and proteins have been developed there is a lack of topical pharmaceutical products on the market containing these sensitive molecules. The main reasons may be lack of stability and a limitation of larger molecules to penetrate into the skin. In this study we investigated the possibility to develop a peptide formulation which enables follicular permeation of peptides and passes the following criteria: 1) The formulation should be chemically and physically stable, 2) The formulation should have appealing cosmetical properties and 3) The formulation should be compatible with skin as well as sebum. The hypothesis was that increased stability of the peptide could be obtained by keeping the peptide in solid form and in a water-free environment, and that permeation into skin could be facilitated by reducing the particle size to < 10 µm and by formulating the peptide in sebum compatible excipients. By this method a safe and a cosmetically attractive formulation, facilitating the local distribution of the model peptide FOL-005 into the skin and at the same time securing chemical and physical stability, was successfully developed.
Topics: Administration, Cutaneous; Drug Delivery Systems; Excipients; Particle Size; Peptides; Sebum; Skin Absorption
PubMed: 35093338
DOI: 10.1016/j.xphs.2022.01.009 -
Pharmaceutical Research Sep 2017The alarming numbers of poorly soluble discovery compounds have centered the efforts towards finding strategies to improve the solubility. One of the attractive... (Review)
Review
The alarming numbers of poorly soluble discovery compounds have centered the efforts towards finding strategies to improve the solubility. One of the attractive approaches to enhance solubility is via amorphization despite the stability issue associated with it. Although the number of amorphous-based research reports has increased tremendously after year 2000, little is known on the current research practice in designing amorphous formulation and how it has changed after the concept of solid dispersion was first introduced decades ago. In this review we try to answer the following questions: What model compounds and excipients have been used in amorphous-based research? How were these two components selected and prepared? What methods have been used to assess the performance of amorphous formulation? What methodology have evolved and/or been standardized since amorphous-based formulation was first introduced and to what extent have we embraced on new methods? Is the extent of research mirrored in the number of marketed amorphous drug products? We have summarized the history and evolution of amorphous formulation and discuss the current status of amorphous formulation-related research practice. We also explore the potential uses of old experimental methods and how they can be used in tandem with computational tools in designing amorphous formulation more efficiently than the traditional trial-and-error approach.
Topics: Crystallization; Drug Compounding; Drug Stability; Drug Storage; Excipients; Molecular Dynamics Simulation; Pharmaceutical Preparations; Phase Transition; Solubility
PubMed: 28523384
DOI: 10.1007/s11095-017-2174-7 -
Advanced Drug Delivery Reviews Jun 2014The development of paediatric medicines can be challenging since this is a diverse patient population with specific needs. For example, the toxicity of excipients may... (Review)
Review
The development of paediatric medicines can be challenging since this is a diverse patient population with specific needs. For example, the toxicity of excipients may differ in children compared to adults and children have different taste preferences. Acceptable palatability of oral paediatric medicinal products is of great importance to facilitate patient adherence. This has been recognised by regulatory authorities and so is becoming a key aspect of paediatric pharmaceutical development studies. Many active pharmaceutical ingredients (APIs) have aversive taste characteristics and so it is necessary to utilise taste masking techniques to improve the palatability of paediatric oral formulations. The aim of this review is to provide an overview of different approaches to taste masking APIs in paediatric oral dosage forms, with a focus on the tolerability of excipients used. In addition, where possible, the provision of examples of some marketed products is made.
Topics: Chemistry, Pharmaceutical; Child; Excipients; Flavoring Agents; Humans; Pediatrics; Pharmaceutical Preparations; Taste
PubMed: 24614069
DOI: 10.1016/j.addr.2014.02.012 -
Drug Delivery Dec 2021In recent years, nanocrystal technology has been extensively investigated. Due to the submicron particle size and unique physicochemical properties of nanocrystals, they... (Review)
Review
In recent years, nanocrystal technology has been extensively investigated. Due to the submicron particle size and unique physicochemical properties of nanocrystals, they overcome the problems of low drug solubility and poor bioavailability. Although the structures of nanocrystals are simple, the further development of these materials is hindered by their stability. Drug nanocrystals with particle sizes of 1∼1000 nm usually require the addition of stabilizers such as polymers or surfactants to enhance their stability. The stability of nanocrystal suspensions and the redispersibility of solid nanocrystal drugs are the key factors for the large-scale production of nanocrystal preparations. In this paper, the factors that affect the stability of drug nanocrystal preparations are discussed, and related methods for solving the stability problem are put forward.
Topics: Chemistry, Pharmaceutical; Crystallization; Drug Stability; Excipients; Hydrophobic and Hydrophilic Interactions; Molecular Weight; Nanoparticles; Particle Size; Solubility; Surface Properties; Suspensions
PubMed: 33336609
DOI: 10.1080/10717544.2020.1856224