The Experts below are selected from a list of 75 Experts worldwide ranked by ideXlab platform
Michael Rosario Defelippis - One of the best experts on this subject based on the ideXlab platform.
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research articlespreparation of a Microcrystalline Suspension formulation of lysb28prob29 human insulin with ultralente properties
Journal of Pharmaceutical Sciences, 1999Co-Authors: Jane P Richards, Mary P Stickelmeyer, Bruce H Frank, Michelle Barbeau, Jerry Radziuk, David G Smith, Michael Rosario DefelippisAbstract:The monomeric analogue, LysB28ProB29‐human insulin (LysPro), has been crystallized using similar conditions employed to prepare extended‐acting insulin ultralente formulations. In the presence of zinc ions, sodium acetate and sodium chloride, but without phenolic preservative, LysPro surprisingly forms small rhombohedral crystals with similar morphology to human insulin ultralente crystals with a mean particle size of 20 ± 1 µm. X‐ray powder diffraction studies on the LysPro crystals prior to dilution in ultralente vehicle ([NaCl] = 1.2 M) revealed the presence of T3R3f hexamers. Consistent with human insulin ultralente preparations, LysPro crystals formulated as an ultralente Suspension ([NaCl] = 0.12 M) contain T6 hexamers indicating that a conformational change occurs in the hexamer units of the crystals upon dilution of the salt concentration. The pharmacological properties of subcutaneously administered ultralente LysPro (ULP) were compared to ultralente human insulin (UHI) using a conscious dog model (n = 5) with glucose levels clamped at basal. There were no statistically significant differences between the kinetic and dynamic responses of ULP compared to UHI [Cmax (ng/mL): 3.58 ± 0.76, ULP and 3.61 ± 0.66, UHI; Tmax (min): 226 ± 30, ULP and 185 ± 42, UHI; Rmax (mg/kg min): 11.2 ± 1.9, ULP and 13.3 ± 2.0, UHI; and TRmax (min): 336 ± 11, ULP and 285 ± 57, UHI]. Although the Pro to Lys sequence inversion destabilizes insulin self‐assembly and greatly alters the time action of soluble LysPro preparations, this modification has now been found neither to prevent the formation of ultralente crystals in the absence of phenolics nor to compromise the protracted activity of the insulin analogue Suspension.
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preparation of a Microcrystalline Suspension formulation of lysb28prob29 human insulin with ultralente properties
Journal of Pharmaceutical Sciences, 1999Co-Authors: Jane P Richards, Mary P Stickelmeyer, Bruce H Frank, Michelle Barbeau, Jerry Radziuk, David G Smith, Michael Rosario DefelippisAbstract:Abstract The monomeric analogue, Lys B28 Pro B29 ‐human insulin (LysPro), has been crystallized using similar conditions employed to prepare extended‐acting insulin ultralente formulations. In the presence of zinc ions, sodium acetate and sodium chloride, but without phenolic preservative, LysPro surprisingly forms small rhombohedral crystals with similar morphology to human insulin ultralente crystals with a mean particle size of 20 ± 1 µm. X‐ray powder diffraction studies on the LysPro crystals prior to dilution in ultralente vehicle ([NaCl] = 1.2 M) revealed the presence of T 3 R 3 f hexamers. Consistent with human insulin ultralente preparations, LysPro crystals formulated as an ultralente Suspension ([NaCl] = 0.12 M) contain T 6 hexamers indicating that a conformational change occurs in the hexamer units of the crystals upon dilution of the salt concentration. The pharmacological properties of subcutaneously administered ultralente LysPro (ULP) were compared to ultralente human insulin (UHI) using a conscious dog model ( n = 5) with glucose levels clamped at basal. There were no statistically significant differences between the kinetic and dynamic responses of ULP compared to UHI [ C max (ng/mL): 3.58 ± 0.76, ULP and 3.61 ± 0.66, UHI; T max (min): 226 ± 30, ULP and 185 ± 42, UHI; R max (mg/kg min): 11.2 ± 1.9, ULP and 13.3 ± 2.0, UHI; and T Rmax (min): 336 ± 11, ULP and 285 ± 57, UHI]. Although the Pro to Lys sequence inversion destabilizes insulin self‐assembly and greatly alters the time action of soluble LysPro preparations, this modification has now been found neither to prevent the formation of ultralente crystals in the absence of phenolics nor to compromise the protracted activity of the insulin analogue Suspension.
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Preparation of a Microcrystalline Suspension formulation of LysB28ProB29‐human insulin with ultralente properties
Journal of Pharmaceutical Sciences, 1999Co-Authors: Jane P Richards, Mary P Stickelmeyer, Bruce H Frank, Michelle Barbeau, Jerry Radziuk, G.david Smith, Michael Rosario DefelippisAbstract:Abstract The monomeric analogue, Lys B28 Pro B29 ‐human insulin (LysPro), has been crystallized using similar conditions employed to prepare extended‐acting insulin ultralente formulations. In the presence of zinc ions, sodium acetate and sodium chloride, but without phenolic preservative, LysPro surprisingly forms small rhombohedral crystals with similar morphology to human insulin ultralente crystals with a mean particle size of 20 ± 1 µm. X‐ray powder diffraction studies on the LysPro crystals prior to dilution in ultralente vehicle ([NaCl] = 1.2 M) revealed the presence of T 3 R 3 f hexamers. Consistent with human insulin ultralente preparations, LysPro crystals formulated as an ultralente Suspension ([NaCl] = 0.12 M) contain T 6 hexamers indicating that a conformational change occurs in the hexamer units of the crystals upon dilution of the salt concentration. The pharmacological properties of subcutaneously administered ultralente LysPro (ULP) were compared to ultralente human insulin (UHI) using a conscious dog model ( n = 5) with glucose levels clamped at basal. There were no statistically significant differences between the kinetic and dynamic responses of ULP compared to UHI [ C max (ng/mL): 3.58 ± 0.76, ULP and 3.61 ± 0.66, UHI; T max (min): 226 ± 30, ULP and 185 ± 42, UHI; R max (mg/kg min): 11.2 ± 1.9, ULP and 13.3 ± 2.0, UHI; and T Rmax (min): 336 ± 11, ULP and 285 ± 57, UHI]. Although the Pro to Lys sequence inversion destabilizes insulin self‐assembly and greatly alters the time action of soluble LysPro preparations, this modification has now been found neither to prevent the formation of ultralente crystals in the absence of phenolics nor to compromise the protracted activity of the insulin analogue Suspension.
Raimo Hiltunen - One of the best experts on this subject based on the ideXlab platform.
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Effects of Microcrystalline plant sterol Suspension and a powdered plant sterol supplement on hypercholesterolemia in genetically obese Zucker rats.
The Journal of pharmacy and pharmacology, 2003Co-Authors: J. Summanen, Teijo Yrjönen, Leena Christiansen, Eero Mervaala, Timo Vaskonen, Markus Lassila, Markku Ahotupa, Jouko Yliruusi, Heikki Karppanen, Raimo HiltunenAbstract:Because dietary fat appears to be an effective vehicle for dispensing plant sterols into the diet, a special plant-sterol-containing ingredient has recently been developed. This ingredient is a plant sterol Suspension in oil in which the sterols are in Microcrystalline form. The objective of the present study was to analyse the cholesterol-lowering effects and safety of two different plant sterol preparations, an orally administered Microcrystalline plant sterol Suspension (MPS) in rapeseed oil and a powdered plant sterol supplement, in obese Zucker rats. Dietary plant sterol supplements (0.5%, w/w) were given concurrently with a high cholesterol diet (HCD, 1% cholesterol and 18% fat, w/w). No significant changes in serum triglyceride, blood glucose, serum glutamate oxaloacetic transaminase and glutamic pyruvic transaminase values or body and liver weights were observed. The powdered plant sterol supplement lowered the serum cholesterol by 25% (P < 0.05) and the MPS diet by 35% (P < 0.001) compared with HCD by the end of the 12-week experiment. Interestingly, the plant sterol supplements also produced a marked reduction in serum ubiquinone levels, suggesting a possible effect on isoprene synthesis. Unlike the powdered plant sterol, both MPS and plain rapeseed oil decreased the serum baseline diene conjugation values, suggesting that they protect against oxidative stress-induced lipid peroxidation in rats. This lipid peroxidation diminishing effect is probably due to some antioxidative components in rapeseed oil. These findings indicate that an unesterified plant sterol, such as the Microcrystalline Suspension in oil, effectively prevents cholesterol absorption in obese Zucker rats.
Jane P Richards - One of the best experts on this subject based on the ideXlab platform.
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research articlespreparation of a Microcrystalline Suspension formulation of lysb28prob29 human insulin with ultralente properties
Journal of Pharmaceutical Sciences, 1999Co-Authors: Jane P Richards, Mary P Stickelmeyer, Bruce H Frank, Michelle Barbeau, Jerry Radziuk, David G Smith, Michael Rosario DefelippisAbstract:The monomeric analogue, LysB28ProB29‐human insulin (LysPro), has been crystallized using similar conditions employed to prepare extended‐acting insulin ultralente formulations. In the presence of zinc ions, sodium acetate and sodium chloride, but without phenolic preservative, LysPro surprisingly forms small rhombohedral crystals with similar morphology to human insulin ultralente crystals with a mean particle size of 20 ± 1 µm. X‐ray powder diffraction studies on the LysPro crystals prior to dilution in ultralente vehicle ([NaCl] = 1.2 M) revealed the presence of T3R3f hexamers. Consistent with human insulin ultralente preparations, LysPro crystals formulated as an ultralente Suspension ([NaCl] = 0.12 M) contain T6 hexamers indicating that a conformational change occurs in the hexamer units of the crystals upon dilution of the salt concentration. The pharmacological properties of subcutaneously administered ultralente LysPro (ULP) were compared to ultralente human insulin (UHI) using a conscious dog model (n = 5) with glucose levels clamped at basal. There were no statistically significant differences between the kinetic and dynamic responses of ULP compared to UHI [Cmax (ng/mL): 3.58 ± 0.76, ULP and 3.61 ± 0.66, UHI; Tmax (min): 226 ± 30, ULP and 185 ± 42, UHI; Rmax (mg/kg min): 11.2 ± 1.9, ULP and 13.3 ± 2.0, UHI; and TRmax (min): 336 ± 11, ULP and 285 ± 57, UHI]. Although the Pro to Lys sequence inversion destabilizes insulin self‐assembly and greatly alters the time action of soluble LysPro preparations, this modification has now been found neither to prevent the formation of ultralente crystals in the absence of phenolics nor to compromise the protracted activity of the insulin analogue Suspension.
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preparation of a Microcrystalline Suspension formulation of lysb28prob29 human insulin with ultralente properties
Journal of Pharmaceutical Sciences, 1999Co-Authors: Jane P Richards, Mary P Stickelmeyer, Bruce H Frank, Michelle Barbeau, Jerry Radziuk, David G Smith, Michael Rosario DefelippisAbstract:Abstract The monomeric analogue, Lys B28 Pro B29 ‐human insulin (LysPro), has been crystallized using similar conditions employed to prepare extended‐acting insulin ultralente formulations. In the presence of zinc ions, sodium acetate and sodium chloride, but without phenolic preservative, LysPro surprisingly forms small rhombohedral crystals with similar morphology to human insulin ultralente crystals with a mean particle size of 20 ± 1 µm. X‐ray powder diffraction studies on the LysPro crystals prior to dilution in ultralente vehicle ([NaCl] = 1.2 M) revealed the presence of T 3 R 3 f hexamers. Consistent with human insulin ultralente preparations, LysPro crystals formulated as an ultralente Suspension ([NaCl] = 0.12 M) contain T 6 hexamers indicating that a conformational change occurs in the hexamer units of the crystals upon dilution of the salt concentration. The pharmacological properties of subcutaneously administered ultralente LysPro (ULP) were compared to ultralente human insulin (UHI) using a conscious dog model ( n = 5) with glucose levels clamped at basal. There were no statistically significant differences between the kinetic and dynamic responses of ULP compared to UHI [ C max (ng/mL): 3.58 ± 0.76, ULP and 3.61 ± 0.66, UHI; T max (min): 226 ± 30, ULP and 185 ± 42, UHI; R max (mg/kg min): 11.2 ± 1.9, ULP and 13.3 ± 2.0, UHI; and T Rmax (min): 336 ± 11, ULP and 285 ± 57, UHI]. Although the Pro to Lys sequence inversion destabilizes insulin self‐assembly and greatly alters the time action of soluble LysPro preparations, this modification has now been found neither to prevent the formation of ultralente crystals in the absence of phenolics nor to compromise the protracted activity of the insulin analogue Suspension.
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Preparation of a Microcrystalline Suspension formulation of LysB28ProB29‐human insulin with ultralente properties
Journal of Pharmaceutical Sciences, 1999Co-Authors: Jane P Richards, Mary P Stickelmeyer, Bruce H Frank, Michelle Barbeau, Jerry Radziuk, G.david Smith, Michael Rosario DefelippisAbstract:Abstract The monomeric analogue, Lys B28 Pro B29 ‐human insulin (LysPro), has been crystallized using similar conditions employed to prepare extended‐acting insulin ultralente formulations. In the presence of zinc ions, sodium acetate and sodium chloride, but without phenolic preservative, LysPro surprisingly forms small rhombohedral crystals with similar morphology to human insulin ultralente crystals with a mean particle size of 20 ± 1 µm. X‐ray powder diffraction studies on the LysPro crystals prior to dilution in ultralente vehicle ([NaCl] = 1.2 M) revealed the presence of T 3 R 3 f hexamers. Consistent with human insulin ultralente preparations, LysPro crystals formulated as an ultralente Suspension ([NaCl] = 0.12 M) contain T 6 hexamers indicating that a conformational change occurs in the hexamer units of the crystals upon dilution of the salt concentration. The pharmacological properties of subcutaneously administered ultralente LysPro (ULP) were compared to ultralente human insulin (UHI) using a conscious dog model ( n = 5) with glucose levels clamped at basal. There were no statistically significant differences between the kinetic and dynamic responses of ULP compared to UHI [ C max (ng/mL): 3.58 ± 0.76, ULP and 3.61 ± 0.66, UHI; T max (min): 226 ± 30, ULP and 185 ± 42, UHI; R max (mg/kg min): 11.2 ± 1.9, ULP and 13.3 ± 2.0, UHI; and T Rmax (min): 336 ± 11, ULP and 285 ± 57, UHI]. Although the Pro to Lys sequence inversion destabilizes insulin self‐assembly and greatly alters the time action of soluble LysPro preparations, this modification has now been found neither to prevent the formation of ultralente crystals in the absence of phenolics nor to compromise the protracted activity of the insulin analogue Suspension.
J. Summanen - One of the best experts on this subject based on the ideXlab platform.
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Effects of Microcrystalline plant sterol Suspension and a powdered plant sterol supplement on hypercholesterolemia in genetically obese Zucker rats.
The Journal of pharmacy and pharmacology, 2003Co-Authors: J. Summanen, Teijo Yrjönen, Leena Christiansen, Eero Mervaala, Timo Vaskonen, Markus Lassila, Markku Ahotupa, Jouko Yliruusi, Heikki Karppanen, Raimo HiltunenAbstract:Because dietary fat appears to be an effective vehicle for dispensing plant sterols into the diet, a special plant-sterol-containing ingredient has recently been developed. This ingredient is a plant sterol Suspension in oil in which the sterols are in Microcrystalline form. The objective of the present study was to analyse the cholesterol-lowering effects and safety of two different plant sterol preparations, an orally administered Microcrystalline plant sterol Suspension (MPS) in rapeseed oil and a powdered plant sterol supplement, in obese Zucker rats. Dietary plant sterol supplements (0.5%, w/w) were given concurrently with a high cholesterol diet (HCD, 1% cholesterol and 18% fat, w/w). No significant changes in serum triglyceride, blood glucose, serum glutamate oxaloacetic transaminase and glutamic pyruvic transaminase values or body and liver weights were observed. The powdered plant sterol supplement lowered the serum cholesterol by 25% (P < 0.05) and the MPS diet by 35% (P < 0.001) compared with HCD by the end of the 12-week experiment. Interestingly, the plant sterol supplements also produced a marked reduction in serum ubiquinone levels, suggesting a possible effect on isoprene synthesis. Unlike the powdered plant sterol, both MPS and plain rapeseed oil decreased the serum baseline diene conjugation values, suggesting that they protect against oxidative stress-induced lipid peroxidation in rats. This lipid peroxidation diminishing effect is probably due to some antioxidative components in rapeseed oil. These findings indicate that an unesterified plant sterol, such as the Microcrystalline Suspension in oil, effectively prevents cholesterol absorption in obese Zucker rats.
Mary P Stickelmeyer - One of the best experts on this subject based on the ideXlab platform.
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research articlespreparation of a Microcrystalline Suspension formulation of lysb28prob29 human insulin with ultralente properties
Journal of Pharmaceutical Sciences, 1999Co-Authors: Jane P Richards, Mary P Stickelmeyer, Bruce H Frank, Michelle Barbeau, Jerry Radziuk, David G Smith, Michael Rosario DefelippisAbstract:The monomeric analogue, LysB28ProB29‐human insulin (LysPro), has been crystallized using similar conditions employed to prepare extended‐acting insulin ultralente formulations. In the presence of zinc ions, sodium acetate and sodium chloride, but without phenolic preservative, LysPro surprisingly forms small rhombohedral crystals with similar morphology to human insulin ultralente crystals with a mean particle size of 20 ± 1 µm. X‐ray powder diffraction studies on the LysPro crystals prior to dilution in ultralente vehicle ([NaCl] = 1.2 M) revealed the presence of T3R3f hexamers. Consistent with human insulin ultralente preparations, LysPro crystals formulated as an ultralente Suspension ([NaCl] = 0.12 M) contain T6 hexamers indicating that a conformational change occurs in the hexamer units of the crystals upon dilution of the salt concentration. The pharmacological properties of subcutaneously administered ultralente LysPro (ULP) were compared to ultralente human insulin (UHI) using a conscious dog model (n = 5) with glucose levels clamped at basal. There were no statistically significant differences between the kinetic and dynamic responses of ULP compared to UHI [Cmax (ng/mL): 3.58 ± 0.76, ULP and 3.61 ± 0.66, UHI; Tmax (min): 226 ± 30, ULP and 185 ± 42, UHI; Rmax (mg/kg min): 11.2 ± 1.9, ULP and 13.3 ± 2.0, UHI; and TRmax (min): 336 ± 11, ULP and 285 ± 57, UHI]. Although the Pro to Lys sequence inversion destabilizes insulin self‐assembly and greatly alters the time action of soluble LysPro preparations, this modification has now been found neither to prevent the formation of ultralente crystals in the absence of phenolics nor to compromise the protracted activity of the insulin analogue Suspension.
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preparation of a Microcrystalline Suspension formulation of lysb28prob29 human insulin with ultralente properties
Journal of Pharmaceutical Sciences, 1999Co-Authors: Jane P Richards, Mary P Stickelmeyer, Bruce H Frank, Michelle Barbeau, Jerry Radziuk, David G Smith, Michael Rosario DefelippisAbstract:Abstract The monomeric analogue, Lys B28 Pro B29 ‐human insulin (LysPro), has been crystallized using similar conditions employed to prepare extended‐acting insulin ultralente formulations. In the presence of zinc ions, sodium acetate and sodium chloride, but without phenolic preservative, LysPro surprisingly forms small rhombohedral crystals with similar morphology to human insulin ultralente crystals with a mean particle size of 20 ± 1 µm. X‐ray powder diffraction studies on the LysPro crystals prior to dilution in ultralente vehicle ([NaCl] = 1.2 M) revealed the presence of T 3 R 3 f hexamers. Consistent with human insulin ultralente preparations, LysPro crystals formulated as an ultralente Suspension ([NaCl] = 0.12 M) contain T 6 hexamers indicating that a conformational change occurs in the hexamer units of the crystals upon dilution of the salt concentration. The pharmacological properties of subcutaneously administered ultralente LysPro (ULP) were compared to ultralente human insulin (UHI) using a conscious dog model ( n = 5) with glucose levels clamped at basal. There were no statistically significant differences between the kinetic and dynamic responses of ULP compared to UHI [ C max (ng/mL): 3.58 ± 0.76, ULP and 3.61 ± 0.66, UHI; T max (min): 226 ± 30, ULP and 185 ± 42, UHI; R max (mg/kg min): 11.2 ± 1.9, ULP and 13.3 ± 2.0, UHI; and T Rmax (min): 336 ± 11, ULP and 285 ± 57, UHI]. Although the Pro to Lys sequence inversion destabilizes insulin self‐assembly and greatly alters the time action of soluble LysPro preparations, this modification has now been found neither to prevent the formation of ultralente crystals in the absence of phenolics nor to compromise the protracted activity of the insulin analogue Suspension.
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Preparation of a Microcrystalline Suspension formulation of LysB28ProB29‐human insulin with ultralente properties
Journal of Pharmaceutical Sciences, 1999Co-Authors: Jane P Richards, Mary P Stickelmeyer, Bruce H Frank, Michelle Barbeau, Jerry Radziuk, G.david Smith, Michael Rosario DefelippisAbstract:Abstract The monomeric analogue, Lys B28 Pro B29 ‐human insulin (LysPro), has been crystallized using similar conditions employed to prepare extended‐acting insulin ultralente formulations. In the presence of zinc ions, sodium acetate and sodium chloride, but without phenolic preservative, LysPro surprisingly forms small rhombohedral crystals with similar morphology to human insulin ultralente crystals with a mean particle size of 20 ± 1 µm. X‐ray powder diffraction studies on the LysPro crystals prior to dilution in ultralente vehicle ([NaCl] = 1.2 M) revealed the presence of T 3 R 3 f hexamers. Consistent with human insulin ultralente preparations, LysPro crystals formulated as an ultralente Suspension ([NaCl] = 0.12 M) contain T 6 hexamers indicating that a conformational change occurs in the hexamer units of the crystals upon dilution of the salt concentration. The pharmacological properties of subcutaneously administered ultralente LysPro (ULP) were compared to ultralente human insulin (UHI) using a conscious dog model ( n = 5) with glucose levels clamped at basal. There were no statistically significant differences between the kinetic and dynamic responses of ULP compared to UHI [ C max (ng/mL): 3.58 ± 0.76, ULP and 3.61 ± 0.66, UHI; T max (min): 226 ± 30, ULP and 185 ± 42, UHI; R max (mg/kg min): 11.2 ± 1.9, ULP and 13.3 ± 2.0, UHI; and T Rmax (min): 336 ± 11, ULP and 285 ± 57, UHI]. Although the Pro to Lys sequence inversion destabilizes insulin self‐assembly and greatly alters the time action of soluble LysPro preparations, this modification has now been found neither to prevent the formation of ultralente crystals in the absence of phenolics nor to compromise the protracted activity of the insulin analogue Suspension.