Characterization of Synthesized and Commercial Forms of Magnesium Stearate Using Differential Scanning Calorimetry, Thermogravimetric Analysis, Powder X-Ray Diffraction, and Solid-State NMR Spectroscopy
Abstract:Magnesium stearate is the salt of a complex mixture of fatty acids, with the majority being stearate and palmitate. It has multiple crystalline forms and, potentially, an amorphous form. Magnesium stearate is used in the pharmaceutical manufacturing industry as a powder lubricant, and typically is added at low levels (∼1%) during the manufacturing process and blended for a relatively short time (∼5 min). Proper levels and mixing times are needed, as too short a mixing time or too small a quantity will result i… Show more
“…1c. The patterns are in accordance with previously reported diffractograms [15]. The intensity and sharpness of the peaks at the 3.3°2θ, 5.5°2 θ and 23°2θ scale revealed higher crystalline portions for Ligamed MF-2-V and Ligamed MF-3-V compared with MgSt-BDH.…”
Section: Powder X-ray Diffractionsupporting
confidence: 91%
“…MgSt is a mixture of stearic and palmitic salts [4]. Several different hydrates and corresponding solid-state forms of MgSt have been identified: anhydrous, monohydrate (needle-shape or disordered), dihydrate (plate-shape), trihydrate (needle-shape) [14,15]. MgSt samples may comprise of crystalline (single or combination of 2 or more forms) or disordered forms [15].…”
Section: Introductionmentioning
confidence: 99%
“…Several different hydrates and corresponding solid-state forms of MgSt have been identified: anhydrous, monohydrate (needle-shape or disordered), dihydrate (plate-shape), trihydrate (needle-shape) [14,15]. MgSt samples may comprise of crystalline (single or combination of 2 or more forms) or disordered forms [15]. Molecular, structural, particle properties and excipient level have been identified as potential critical material attributes of MgSt [4].…”
Excipients are major components of oral solid dosage forms, and changes in their critical material attributes (excipient variability) and/or amount (excipient variation) in pharmaceutical formulations may present a challenge for product performance. Understanding the biopharmaceutical factors affecting excipient performance is recommended for the successful implementation of excipient variability on Quality by Design (QbD) approaches. The current study investigated the impact of magnesium stearate (MgSt) variability on the apparent solubility of drugs with a wide range of physicochemical properties (drug ionization, drug lipophilicity, drug aqueous solubility). Compendial and biorelevant media were used to assess the role of gastrointestinal (GI) conditions on the excipient effects on drug apparent solubility. The lipophilic nature of MgSt decreased the apparent solubility of most compounds. The reduction in drug apparent solubility was more pronounced for highly soluble and/or highly ionized drugs and in presence of more highly crystalline or smaller particle size MgSt. The use of multivariate data analysis revealed the critical physicochemical and biopharmaceutical factors and the complex nature of excipient variability on the reduction in drug apparent solubility. The construction of a roadmap combining drug, excipient and medium characteristics allowed the identification of the cases where the presence of excipient or excipient variability may present risks for oral drug performance.
“…1c. The patterns are in accordance with previously reported diffractograms [15]. The intensity and sharpness of the peaks at the 3.3°2θ, 5.5°2 θ and 23°2θ scale revealed higher crystalline portions for Ligamed MF-2-V and Ligamed MF-3-V compared with MgSt-BDH.…”
Section: Powder X-ray Diffractionsupporting
confidence: 91%
“…MgSt is a mixture of stearic and palmitic salts [4]. Several different hydrates and corresponding solid-state forms of MgSt have been identified: anhydrous, monohydrate (needle-shape or disordered), dihydrate (plate-shape), trihydrate (needle-shape) [14,15]. MgSt samples may comprise of crystalline (single or combination of 2 or more forms) or disordered forms [15].…”
Section: Introductionmentioning
confidence: 99%
“…Several different hydrates and corresponding solid-state forms of MgSt have been identified: anhydrous, monohydrate (needle-shape or disordered), dihydrate (plate-shape), trihydrate (needle-shape) [14,15]. MgSt samples may comprise of crystalline (single or combination of 2 or more forms) or disordered forms [15]. Molecular, structural, particle properties and excipient level have been identified as potential critical material attributes of MgSt [4].…”
Excipients are major components of oral solid dosage forms, and changes in their critical material attributes (excipient variability) and/or amount (excipient variation) in pharmaceutical formulations may present a challenge for product performance. Understanding the biopharmaceutical factors affecting excipient performance is recommended for the successful implementation of excipient variability on Quality by Design (QbD) approaches. The current study investigated the impact of magnesium stearate (MgSt) variability on the apparent solubility of drugs with a wide range of physicochemical properties (drug ionization, drug lipophilicity, drug aqueous solubility). Compendial and biorelevant media were used to assess the role of gastrointestinal (GI) conditions on the excipient effects on drug apparent solubility. The lipophilic nature of MgSt decreased the apparent solubility of most compounds. The reduction in drug apparent solubility was more pronounced for highly soluble and/or highly ionized drugs and in presence of more highly crystalline or smaller particle size MgSt. The use of multivariate data analysis revealed the critical physicochemical and biopharmaceutical factors and the complex nature of excipient variability on the reduction in drug apparent solubility. The construction of a roadmap combining drug, excipient and medium characteristics allowed the identification of the cases where the presence of excipient or excipient variability may present risks for oral drug performance.
“…The temperature program of TG started at 30 °C, and reached 850 °C at 10 °C/min. The carrier gas is high purity nitrogen, with a flow rate of 40 mL/min (Delaney et al, 2017). Fig.…”
Cinnamomum camphora is an excellent tree species for construction of forest construction of Henan Province, China. The diverse bioactive components of nano-catalyzed pyrolyzates form cold-acclimated C. camphora branch (CCB) in North China were explored. The raw powder of CCB treated with nano-catalyst (Ag, NiO, 1/2Ag + 1/2NiO) were pyrolyzed at two temperatures (550 °C and 700 °C), respectively. The main pyrolyzates are bioactive components of bioenergy, biomedicines, food additive, spices, cosmetics and chemical, whose total relative contents at 550 °C pyrolyzates are higher than those at 700 °C pyrolyzates. There are abundant components of spices and biomedicine at 550 °C pyrolyzates, while more spices and food additive at 700 °C pyrolyzates. At 550 °C, the content of biomedicine components reaches the highest by 1/2Ag + 1/2NiO nanocatalysis, while the contents of spices and food additive components reach the highest by NiO nanocatalysis. At 700 °C, the content of bioenergy components reaches the highest by 1/2Ag + 1/2NiO nanocatalysis, and the content of cosmetics components reaches the highest by Ag nanocatalysis. The findings suggested that the branch of the cold-acclimated C. camphora have the potential to develop into valued-added products of bioenergy, biomedicine, cosmetics, spices and food additive by nanocatalysis.
“…Magnesium stearate is the salt of a complex mixture of fatty acids, with the main component as stearate and palmitate. It has multiple crystalline forms and an amorphous form [16].…”
Drug molecule contains various reactive functional groups which are susceptible to react with another reactive functional groups which might be excipients, excipient or drugs impurities formed during manufacturing or storage. The objective of the current review article is to provide a comprehensive review of excipients-drug compatibility study, their degradation product characterization with different analytical methods and further impact of methodologies in pharmaceutical industry for potential stability assessment. The incompatibility of drug excipient was very common due to the reactive functional groups in drugs and excipients. These leads to formation of drug related impurities as well as excipient impurities reaction with active Pharmaceutical Ingredients. Sometimes these impurities found to be mutagenic and genotaxic to human beings. Identification of drug degradation in presence of excipient impurities requires extensive knowledge and adequate analytical characterization data. Systematic literature review and understanding about the drug-excipient chemistry in formulation process is important criteria to select compatible excipient and formulate ideal formulation. The analytical characterization data gives idea about degradation pathway. This paper discusses drug-excipient interactions, compatibility and characterization by different analytical methods with case studies and provides an overview of different excipients compatibility in formulation.
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