scholarly journals Fast-acting insulin aspart: a review of its pharmacokinetic and pharmacodynamic properties and the clinical consequences

2020 ◽  
Vol 23 (2) ◽  
pp. 140-160
Author(s):  
Hanne Haahr ◽  
Tim Heise
Keyword(s):  
Clinical Pharmacology ◽  
Insulin Aspart ◽  
Postprandial Glucose ◽  
Phase Iii ◽  
Initial Exposure ◽  
Glucose Lowering ◽  
Lowering Effect ◽  
Acting Insulin ◽  
Glucose Lowering Effect ◽  
Fast Acting

Fast-acting insulin aspart (faster aspart) is insulin aspart (IAsp) with two added excipients, L-arginine and niacinamide, to ensure formulation stability with accelerated initial absorption after subcutaneous administration compared with previously developed rapid-acting insulins. The pharmacokinetic/pharmacodynamic properties of faster aspart have been characterised in clinical pharmacology trials with comparable overall methodology. In subjects with type 1 (T1D) or type 2 (T2D) diabetes, the serum IAsp concentration-time and glucose-lowering effect profiles are left-shifted for faster aspart compared with IAsp. In addition, faster aspart provides earlier onset, doubling of initial exposure, and an up to 2.5-fold increase in initial glucose-lowering effect within 30 min of subcutaneous injection, as well as earlier offset of exposure and effect. Similar results have been shown using continuous subcutaneous insulin infusion (CSII). The improved pharmacological properties of faster aspart versus IAsp are consistent across populations, i.e. in the elderly, children, adolescents and the Japanese. Thus, the faster aspart pharmacological characteristics more closely resemble the mealtime insulin secretion in healthy individuals, giving faster aspart the potential to further improve postprandial glucose control in subjects with diabetes. Indeed, change from baseline in 1-h postprandial glucose increment is in favour of faster aspart versus IAsp when used as basal-bolus or CSII treatment in phase III trials in subjects with T1D or T2D. This review summarises the currently published results from clinical pharmacology trials with faster aspart and discusses the potential clinical benefits of faster aspart compared with previous rapid-acting insulin products.

scholarly journals Fast‐acting insulin aspart in people with type 2 diabetes: Earlier onset and greater initial exposure and glucose‐lowering effect compared with insulin aspart

2019 ◽  
Vol 21 (9) ◽  
pp. 2068-2075 ◽  
Author(s):  
Thomas R. Pieber ◽  
Eva Svehlikova ◽  
Martina Brunner ◽  
Inge B. Halberg ◽  
Karen Margrete Due Thomsen ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Insulin Aspart ◽  
Initial Exposure ◽  
Glucose Lowering ◽  
Lowering Effect ◽  
Acting Insulin ◽  
Glucose Lowering Effect ◽  
Fast Acting

Postprandial glucose-lowering effect of cagaita (Eugenia dysenterica DC) fruit juice in dysglycemic subjects with metabolic syndrome: An exploratory study

2021 ◽  
Vol 142 ◽  
pp. 110209
Author(s):  
Renata Luise de Araujo ◽  
Francisco A. Tomás-Barberán ◽  
Rosa Ferreira dos Santos ◽  
J. Alberto Martinez-Blazquez ◽  
Maria Inés Genovese
Keyword(s):  
Metabolic Syndrome ◽  
Exploratory Study ◽  
Fruit Juice ◽  
Postprandial Glucose ◽  
Glucose Lowering ◽  
Lowering Effect ◽  
Glucose Lowering Effect ◽  
Eugenia Dysenterica

scholarly journals Pharmacokinetics and Pharmacodynamics of Three Different Formulations of Insulin Aspart: A Randomized, Double-blind, Crossover Study in Men With Type 1 Diabetes

2020 ◽  
Author(s):  
Eva Svehlikova ◽  
Ines Mursic ◽  
Thomas Augustin ◽  
Christoph Magnes ◽  
David Gerring ◽  
...  
Keyword(s):  
Type 1 Diabetes ◽  
Crossover Study ◽  
Insulin Aspart ◽  
Pharmacokinetics And Pharmacodynamics ◽  
Onset Of Action ◽  
Double Blind ◽  
Glucose Lowering ◽  
Lowering Effect ◽  
Glucose Lowering Effect

OBJECTIVE <p>To investigate the pharmacokinetic and pharmacodynamic properties, and safety of a novel formulation of insulin aspart (AT247) versus currently marketed insulin aspart formulations (IAsp and faster IAsp).</p> <p> </p> <p>RESEARCH DESIGN AND METHODS</p> <p>This single-center, randomized, double-blind, three-period, crossover study was conducted in 19 men with type 1 diabetes, receiving single dosing of trial products (0.3 U/kg) in a random order on three visits. Pharmacokinetics and pharmacodynamics were assessed during a euglycemic clamp lasting up to 8 hours. </p> <p> </p> <p>RESULTS</p> <p>Onset of insulin appearance was earlier for AT247 compared with IAsp (−12 minutes [95% CI −14;−8] p=0.0004) and faster IAsp (−2 minutes [−5;−2] p=0.0003). Onset of action was accelerated compared with IAsp (−23 minutes [−37;−15] p=0.0004) and faster IAsp (−9 minutes [−11;−3] p=0.0006). Within the first 60 minutes, a higher exposure was observed for AT247 compared with IAsp (AUC<sub>Asp,0-60min</sub>: treatment ratio vs IAsp 2.3 [1.9;2.9]; vs faster IAsp 1.5 [1.3;1.8]), which was underpinned by a greater early glucose-lowering effect (AUC<sub>GIR,0-60min</sub>: treatment ratio vs IAsp 2.8 [2.0;5.5]; vs faster IAsp 1.7 [1.3;2.3]). Furthermore, an earlier offset of exposure was observed for AT247 compared with IAsp (−32 minutes [−58;−15] p=0.0015) and faster IAsp (−27 minutes [−85;−15] p=0.0017), while duration of glucose-lowering effect, measured by t<sub>Late50%GIRmax</sub>, did not differ significantly.</p> <p> </p> <p>CONCLUSIONS</p> <p>AT247 exhibited an earlier insulin appearance, exposure and offset, with corresponding enhanced early glucose-lowering effect compared with IAsp and faster IAsp. It therefore represents a promising candidate in the pursuit for second generation prandial insulin analogs to improve postprandial glycemic control.</p>

scholarly journals Pharmacokinetics and Pharmacodynamics of Three Different Formulations of Insulin Aspart: A Randomized, Double-blind, Crossover Study in Men With Type 1 Diabetes

2020 ◽  
Author(s):  
Eva Svehlikova ◽  
Ines Mursic ◽  
Thomas Augustin ◽  
Christoph Magnes ◽  
David Gerring ◽  
...  
Keyword(s):  
Type 1 Diabetes ◽  
Crossover Study ◽  
Insulin Aspart ◽  
Pharmacokinetics And Pharmacodynamics ◽  
Onset Of Action ◽  
Double Blind ◽  
Glucose Lowering ◽  
Lowering Effect ◽  
Glucose Lowering Effect

OBJECTIVE <p>To investigate the pharmacokinetic and pharmacodynamic properties, and safety of a novel formulation of insulin aspart (AT247) versus currently marketed insulin aspart formulations (IAsp and faster IAsp).</p> <p> </p> <p>RESEARCH DESIGN AND METHODS</p> <p>This single-center, randomized, double-blind, three-period, crossover study was conducted in 19 men with type 1 diabetes, receiving single dosing of trial products (0.3 U/kg) in a random order on three visits. Pharmacokinetics and pharmacodynamics were assessed during a euglycemic clamp lasting up to 8 hours. </p> <p> </p> <p>RESULTS</p> <p>Onset of insulin appearance was earlier for AT247 compared with IAsp (−12 minutes [95% CI −14;−8] p=0.0004) and faster IAsp (−2 minutes [−5;−2] p=0.0003). Onset of action was accelerated compared with IAsp (−23 minutes [−37;−15] p=0.0004) and faster IAsp (−9 minutes [−11;−3] p=0.0006). Within the first 60 minutes, a higher exposure was observed for AT247 compared with IAsp (AUC<sub>Asp,0-60min</sub>: treatment ratio vs IAsp 2.3 [1.9;2.9]; vs faster IAsp 1.5 [1.3;1.8]), which was underpinned by a greater early glucose-lowering effect (AUC<sub>GIR,0-60min</sub>: treatment ratio vs IAsp 2.8 [2.0;5.5]; vs faster IAsp 1.7 [1.3;2.3]). Furthermore, an earlier offset of exposure was observed for AT247 compared with IAsp (−32 minutes [−58;−15] p=0.0015) and faster IAsp (−27 minutes [−85;−15] p=0.0017), while duration of glucose-lowering effect, measured by t<sub>Late50%GIRmax</sub>, did not differ significantly.</p> <p> </p> <p>CONCLUSIONS</p> <p>AT247 exhibited an earlier insulin appearance, exposure and offset, with corresponding enhanced early glucose-lowering effect compared with IAsp and faster IAsp. It therefore represents a promising candidate in the pursuit for second generation prandial insulin analogs to improve postprandial glycemic control.</p>

Switching to Biphasic Insulin Aspart 30 in Patients Uncontrolled on Human Premix Insulin

2010 ◽  
Vol 7 (2) ◽  
pp. 124
Author(s):  
Jens Sandahl Christiansen ◽  
Keyword(s):  
Insulin Aspart ◽  
Postprandial Glucose ◽  
Nocturnal Hypoglycaemia ◽  
Glucose Lowering ◽  
Biphasic Insulin Aspart ◽  
Biphasic Insulin ◽  
Biphasic Insulin Aspart 30 ◽  
Neutral Protamine Hagedorn ◽  
Glucose Lowering Effect

Two cases relating to switching from biphasic human insulin 30 (BHI 30) to biphasic insulin aspart 30 (BIAsp 30) are described. Case 1: switching from BHI 30 to BIAsp 30 due to inadequate glycosylated haemoglobin (HbA1c) control. Case 2: switching from BHI to BIAsp 30 due to nocturnal hypoglycaemia. Case 1: HbA1cfell from 7.9 % with BHI to 6.9 % with BIAsp 30 at the six-month follow-up. Postprandial glucose (PPG) fell from 12.6 mmol/l with BHI to 9.1 mmol/l with BIAsp 30. Case 2: a man who had experienced recurrent nocturnal hypoglycaemia with neutral protamine Hagedorn (NPH) or BHI was able to maintain his glycaemic control without severe nocturnal hypoglycaemia with BIAsp 30. BIAsp 30 offers advantages over BHI 30 in terms of faster absorption, higher peak concentrations, and a more rapid and pronounced prandial glucose-lowering effect, which means that BIAsp 30 can improve PPG control and reduce the risk of nocturnal and major hypoglycaemic episodes.

scholarly journals Alleviating the Hydrolysis of Carbohydrates, Tangzhiqing (TZQ) Decreased the Postprandial Glycemia in Healthy Volunteers: An Eight-Period Crossover Study

2020 ◽  
Vol 2020 ◽  
pp. 1-12
Author(s):  
Yanfen Li ◽  
Ziqiang Li ◽  
Ruihua Wang ◽  
Bo Mi ◽  
Ting Jiang ◽  
...  
Keyword(s):  
Area Under The Curve ◽  
Postprandial Glucose ◽  
Postprandial Blood Glucose ◽  
Glucose Lowering ◽  
Postprandial Glycemia ◽  
Lowering Effect ◽  
Healthy Humans ◽  
Glucose Lowering Effect ◽  
Effect Of Glucose ◽  
Hydrolysis Of

Tangzhiqing (TZQ), a Chinese herbal medicine, has been widely used to treat diabetes mellitus in China. TZQ works as a potential α-glucosidase inhibitor to reduce the absorption of glucose from dietary carbohydrates. The main aim of this study was to investigate the postprandial glucose-lowering effect of TZQ on the common carbohydrates in healthy humans. Meanwhile, the possible types of the inhibited α-glucosidase enzymes were predicted in this study. Glucose, sucrose, maltose, maltodextrin, and starch were chosen as investigated carbohydrates. The baseline incremental area under the curve (IAUC) and glycemic index (GI) values of the investigated carbohydrates were evaluated. Then, thirty-six subjects were randomly assigned to three groups to assess postprandial hypoglycemic effects of 3-, 6-, and 9-tablet TZQ. The subjects in each group were randomized to eight subgroups. An eight-period, eight-sequence, crossover design was performed to investigate the postprandial glucose-lowering effect of TZQ after drinking each carbohydrate. A significant decrease was observed on the postprandial glucose IAUCs (279.41 ± 111.31 vs. 203.86 ± 61.08) and GIs (124.91 ± 48.54 vs. 91.69 ± 27.47) of maltose after oral administration of 6-tablet TZQ, as well as IAUCs (145.05 ± 55.01 vs. 110.23 ± 57.03) and GIs (84.87 ± 33.40 vs. 65.50 ± 33.89) of sucrose after administration of 3-tablet TZQ. The glucose IAUCs (109.15 ± 55.92 vs. 57.68 ± 46.09) and GIs (49.09 ± 25.15 vs. 25.94 ± 20.73) of starch statistically reduced following the administration of 6-tablet TZQ. The lowering postprandial blood glucose effect of TZQ did not increase proportionally with increasing doses in humans. There were no significant changes in the glucose-lowering effect of glucose and maltodextrin after the administration of 3-, 6-, or 9-tablet TZQ, respectively. TZQ is a potential treatment for postprandial hyperglycemia, which can probably make α-glucosidases inhibit maltase, sucrase, and α-amylase in the digestive organs.

scholarly journals The value of fast-acting insulin aspart compared with insulin aspart for patients with diabetes mellitus treated with bolus insulin from a UK health care system perspective

2018 ◽  
Vol 9 (7) ◽  
pp. 187-197 ◽  
Author(s):  
Lalantha Leelarathna ◽  
Donna Ashley ◽  
Carrie Fidler ◽  
Witesh Parekh
Keyword(s):  
Insulin Aspart ◽  
Impact Analysis ◽  
Postprandial Glucose ◽  
Additional Cost ◽  
Onset Of Action ◽  
System Perspective ◽  
Acting Insulin ◽  
Cost Impact ◽  
The Uk ◽  
Fast Acting

Background: Fast-acting insulin aspart is a new formulation of the rapid-acting insulin analogue insulin aspart and represents an advancement over current rapid-acting insulin analogues in terms of onset of action and postprandial glucose control. The objective of the current analysis was to demonstrate the cost impact of prescribing fast-acting insulin aspart instead of insulin aspart, to highlight the value of fast-acting insulin aspart for the treatment of people with diabetes requiring mealtime insulin. Methods: A cost-impact analysis was conducted from the perspective of the UK National Health Service (NHS). The analysis excluded patients’ out-of-pocket expenses, carers’ costs and lost productivity. The time horizon of the analysis was 1 year, and no discounting was therefore applied. Results: The displacement of insulin aspart with fast-acting insulin aspart is cost neutral for the UK NHS. Fast-acting insulin aspart is at price parity to insulin aspart in terms of the vial and Penfill® cartridge and is available in the FlexTouch® pen at the same price as the insulin aspart FlexPen® (and thus cheaper than the insulin aspart FlexTouch® pen). Patients using the insulin aspart FlexPen® will be upgraded to the FlexTouch® pen device, which is preferred by patients and healthcare professionals, on switching to fast-acting insulin aspart, at no additional cost. Conclusions: Fast-acting insulin aspart offers additional clinical benefit but at no additional cost when compared with insulin aspart, and thus provides value to the UK NHS.

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