scholarly journals Recent solubility and dissolution enhancement techniques for repaglinide a BCS class II drug: a review

Pharmacia ◽  
2021 ◽  
Vol 68 (3) ◽  
pp. 573-583
Author(s):  
Saba Albetawi ◽  
Amer Abdalhafez ◽  
Ala Abu-Zaid ◽  
Aseel Matrouk ◽  
Noor Alhourani
Keyword(s):  
Pancreatic Beta Cells ◽  
Polymeric Micelles ◽  
Class Ii ◽  
Dissolution Enhancement ◽  
Therapeutic Effects ◽  
Glucose Lowering ◽  
The Past ◽  
Lowering Drug ◽  
Biopharmaceutical Classification System

Repaglinide is an oral blood-glucose-lowering drug used to manage type-2 diabetes mellitus by lowering post-prandial glucose by stimulating insulin secretion from pancreatic beta cells. According to the biopharmaceutical classification system, repaglinide falls under the class II category. For such drugs, limited solubility and poor dissolution rate are the major hurdles to overcome by formulation scientists, as they hinder drug absorption and lead to inadequate therapeutic effects. Therefore, this review aims to discuss in depth the various approaches investigated in the past five years to improve the solubility and dissolution of orally administered repaglinide: namely, solid dispersion, co-amorphous technology, cyclodextrin complexation, phospholipid complexes and polymeric micelles, nanocrystals, nanosuspensions and nanofibers.

Trends in First-Line Glucose-Lowering Drug Use in Adults With Type 2 Diabetes in Light of Emerging Evidence for SGLT-2i and GLP-1RA

Diabetes Care ◽  
2021 ◽  
pp. dc202926
Author(s):  
HoJin Shin ◽  
Sebastian Schneeweiss ◽  
Robert J. Glynn ◽  
Elisabetta Patorno
Keyword(s):  
Type 2 Diabetes ◽  
Drug Use ◽  
First Line ◽  
Glucose Lowering ◽  
Lowering Drug

977-P: Trends in First-Line Glucose-Lowering Drug Use in Adults with Type 2 Diabetes in Light of Emerging Evidence for SGLT2i and GLP-1RA

Diabetes ◽  
2021 ◽  
Vol 70 (Supplement 1) ◽  
pp. 977-P
Author(s):  
HOJIN SHIN ◽  
SEBASTIAN SCHNEEWEISS ◽  
ROBERT GLYNN ◽  
ELISABETTA PATORNO
Keyword(s):  
Type 2 Diabetes ◽  
Drug Use ◽  
First Line ◽  
Glucose Lowering ◽  
Lowering Drug

scholarly journals Anthocyanins as Antidiabetic Agents—In Vitro and In Silico Approaches of Preventive and Therapeutic Effects

Molecules ◽  
2020 ◽  
Vol 25 (17) ◽  
pp. 3813 ◽  
Author(s):  
Hélder Oliveira ◽  
Ana Fernandes ◽  
Natércia F. Brás ◽  
Nuno Mateus ◽  
Victor de Freitas ◽  
...  
Keyword(s):  
In Silico ◽  
Functional Foods ◽  
Therapeutic Strategies ◽  
Therapeutic Effects ◽  
Metabolizing Enzymes ◽  
The Past ◽  
The Matrix ◽  
Made In

Many efforts have been made in the past two decades into the search for novel natural and less-toxic anti-diabetic agents. Some clinical trials have assigned this ability to anthocyanins, although different factors like the food source, the amount ingested, the matrix effect and the time of consumption (before or after a meal) seem to result in contradictory conclusions. The possible mechanisms involved in these preventive or therapeutic effects will be discussed—giving emphasis to the latest in vitro and in silico approaches. Therapeutic strategies to counteract metabolic alterations related to hyperglycemia and Type 2 Diabetes Mellitus (T2DM) may include: (a) Inhibition of carbohydrate-metabolizing enzymes; (b) reduction of glucose transporters expression or activity; (c) inhibition of glycogenolysis and (d) modulation of gut microbiota by anthocyanin breakdown products. These strategies may be achieved through administration of individual anthocyanins or by functional foods containing complexes of anthocyanin:carbohydrate:protein.

Resolution of Risperidone-Induced Hyperprolactinemia with Substitution of Quetiapine

2003 ◽  
Vol 37 (2) ◽  
pp. 206-208 ◽  
Author(s):  
Arun Raj Kunwar ◽  
James L Megna
Keyword(s):  
Adverse Effects ◽  
Prolactin Level ◽  
Atypical Antipsychotics ◽  
Significant Degree ◽  
Psychotic Symptoms ◽  
Therapeutic Effects ◽  
The Past ◽  
Case Summary ◽  
Level Elevation

OBJECTIVE: To report a case of risperidone-induced hyperprolactinemia that was successfully managed with quetiapine. CASE SUMMARY: A 30-year-old white woman with schizoaffective disorder, depressive type, and comorbid alcohol and cocaine abuse was treated successfully for her psychotic symptoms with risperidone until she developed adverse effects consistent with hyperprolactinemia. This was confirmed by laboratory blood tests, as her prolactin level was 186.9 ng/mL (normal for nonpregnant women 2.8–29.2). The woman had experienced similar effects in the past, which had led to noncompliance and subsequent psychotic relapse. Normalization of prolactin levels and associated adverse effects were achieved upon switching to quetiapine. No psychotic symptoms reoccurred. DISCUSSION: Dopamine type 2 (D2) receptor blockade in the mesolimbic tract is thought to mediate the therapeutic effects of antipsychotics. This action in the tuberoinfundibular system produces prolactin level elevation. Risperidone has a relatively higher affinity for the D2 receptor in comparison with other atypical antipsychotics, which may explain why it is associated with a higher incidence of hyperprolactinemia. Quetiapine, which has one of the lowest D2 receptor affinities, is not known to increase prolactin levels to any significant degree. This pharmacologic property allows quetiapine to be a reasonable treatment option for patients who develop risperidone-induced hyperprolactinemia. CONCLUSIONS: Quetiapine may be a suitable substitute when a patient taking risperidone develops hyperprolactinemia.

scholarly journals The Role of Glucagon in the Acute Therapeutic Effects of SGLT2 Inhibition

2020 ◽  
Author(s):  
Ada Admin ◽  
Sofie Hædersdal ◽  
Asger Lund ◽  
Elisabeth Nielsen-Hannerup ◽  
Henrik Maagensen ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Glucose Production ◽  
Endogenous Glucose Production ◽  
Therapeutic Effects ◽  
Acute Administration ◽  
Glucagon Receptor ◽  
Glucose Lowering ◽  
Urinary Glucose ◽  
Sglt2 Inhibition

S<a>odium-glucose cotransporter 2 (SGLT2) inhibitors (SGLT2i)</a> effectively lower plasma glucose (PG) concentration in patients with type 2 diabetes, but studies suggest that circulating glucagon concentrations and endogenous glucose production (EGP) are increased by SGLT2i, possibly compromising their glucose-lowering ability. To tease out whether and how glucagon may influence the glucose-lowering effect of SGLT2 inhibition, we subjected 12 patients with type 2 diabetes to a randomized, placebo-controlled, double-blinded, crossover, double-dummy study comprising, on four separate days, a liquid mixed meal test preceded by single-dose administration of either 1) placebo, 2) the SGLT2i empagliflozin (25 mg), 3) the glucagon receptor antagonist LY2409021 (300 mg), and 4) the combination <a>empagliflozin+LY2409021</a>. Empagliflozin and LY2409021 individually lowered fasting PG compared to placebo and the combination further decreased fasting PG. Previous findings of increased glucagon concentrations and EGP during acute administration of SGLT2i were not replicated in this study. Empagliflozin reduced postprandial PG via increased urinary glucose excretion. LY2409021 reduced EGP significantly, but gave rise to a paradoxical increase in postprandial PG excursion, which was annulled by empagliflozin during their combination (empagliflozin+LY2409021). In conclusion, our findings do not support that an SGLT2i-induced glucagonotropic effect is of importance for the glucose-lowering property of SGLT2 inhibition.

scholarly journals Monitoring Utilization Trends of Glucose-Lowering Drugs for Type 2 Diabetes in Older Adults by Frailty Status

2021 ◽  
Vol 5 (Supplement_1) ◽  
pp. 210-210
Author(s):  
Dae Kim ◽  
Alexander Kutz ◽  
Elisabetta Patorno ◽  
Chandrasekar Gopalakrishnan
Keyword(s):  
Type 2 Diabetes ◽  
Older Adults ◽  
Fee For Service ◽  
Glucose Lowering ◽  
Frailty Status ◽  
Frail Patients ◽  
Lowering Drug ◽  
Service Data ◽  
Over Time

Abstract Using Medicare fee-for-service data from 2013-17, we identified a cohort of patients with type 2 diabetes (T2D) who initiated a glucose-lowering drug (mean [SD] age, 74.8 (6.9) years). Amongst frail patients (CFI≥0.20), metformin use remained stable from 29.1% to 29.4%, whereas sulfonylureas (25.8% to 22.1%) and insulin (21.2% to 19.0%) use declined. Amongst non-frail patients (CFI &lt;0.20), metformin (35.3% to 33.1%) and sulfonylurea (26.2% to 22.2%) use decreased whereas insulin (11.7% to 10.6%) use remained stable. DPP-4i and glitazones use remained stable whereas the use of newer agents such as SGLT-2i and GLP-1 RA increased steadily over the study period in both frail and non-frail patients, though their use remains low ( &lt;8%). In conclusion, sulfonylureas and insulin accounted for about one-third of initiated glucose-lowering medications and were more frequently used by frail patients, though their use declined steadily over time with the availability of newer agents.

343-OR: Trends in A1C and Lipid Testing, Antilipid Therapy, and Target Attainment following First-Time Glucose-Lowering Drug Treatment in Type 2 Diabetes, Denmark, 2000-2017

Diabetes ◽  
2019 ◽  
Vol 68 (Supplement 1) ◽  
pp. 343-OR
Author(s):  
JAKOB S. KNUDSEN ◽  
DANIEL R. WITTE ◽  
ADAM HULMAN ◽  
PERNILLE F. RØNN ◽  
TORSTEN LAURITZEN ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Drug Treatment ◽  
Target Attainment ◽  
Glucose Lowering ◽  
Lipid Testing ◽  
Lowering Drug ◽  
First Time

scholarly journals UTILIZATION TRENDS OF NEWLY APPROVED GLUCOSE-LOWERING DRUGS FOR TYPE 2 DIABETES

2019 ◽  
Vol 3 (Supplement_1) ◽  
pp. S581-S581
Author(s):  
Chintan Dave ◽  
Dae Kim ◽  
Elisabetta Patorno
Keyword(s):  
Type 2 Diabetes ◽  
Standard Deviation ◽  
Fee For Service ◽  
Glucose Lowering ◽  
Medicare Population ◽  
Prior Use ◽  
Lowering Drug ◽  
Service Data

Abstract Using Medicare fee-for-service data from 2013-2015, we identified 3.2 million patients per year (mean [SD] age, 74.7 years [standard deviation, 7.2]) who were treated with glucose-lowering drugs for type 2 diabetes. Between 2013 and 2015, the proportion of patients treated with sulfonylureas declined from 27.4% to 25.1%; those using DPP4is (11.5% to 12.0%) and GLP1-RAs (1.8% to 2.4%) remained unchanged; those using SGLT2is increased from 0.2% to 1.9%. In the subgroup of patients initiating a glucose-lowering drug without prior use of the same class agent, the proportion of patients starting sulfonylureas (18.7% to 17.2% of initiators), DPP4is (16.0% to 15.0% of initiators), and GLP1-RAs (3.4% to 4.2% of initiators) changed little between 2013 and 2015, while those starting SGLT2is increased from 0.7% to 6.5% of initiators. In the Medicare population, we observed a persistently high use of sulfonylureas and a rapid uptake of SGLT2is among the newer classes.

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