scholarly journals Dosing Patterns during Conversion to IPX066, Extended-Release Carbidopa-Levodopa (ER CD-LD), in Parkinson’s Disease with Motor Fluctuations

2018 ◽  
Vol 2018 ◽  
pp. 1-8 ◽  
Author(s):  
John C. Morgan ◽  
Rohit Dhall ◽  
Robert Rubens ◽  
Sarita Khanna ◽  
Suneel Gupta
Keyword(s):  
Extended Release ◽  
Immediate Release ◽  
Oral Formulation ◽  
Study Entry ◽  
Dose Ratio ◽  
Dose Frequency ◽  
Open Label ◽  
Two Phase ◽  
Treatment Regimens ◽  
Link Type

Background. IPX066 is an extended-release (ER) oral formulation of carbidopa-levodopa (CD-LD). Following an initial peak at about one hour, plasma LD concentrations are maintained for about 4-5 hours. Objective. To present dosing factors that may affect the successful conversion to ER CD-LD from other LD formulations. Methods. Two-phase 3 studies of ER CD-LD vs. immediate-release (IR) CD-LD (ADVANCE-PD) and vs. CD-LD + entacapone (CLE; ASCEND-PD) in subjects with advanced PD included a 6-week, open-label conversion to ER CD-LD prior to treatment randomization. The “converted” daily LD dose ratio and dose frequency for ER CD-LD were compared to the prior LD treatment regimens at study entry. Results. The average daily LD dose ratio at the end of dose conversion to ER CD-LD was approximately 2.1 for IR CD-LD and 2.8 for CLE. The final dose ratios tended to be slightly higher for participants taking lower LD doses at study entry but independent of dose frequency. ER CD-LD dose frequency increased with increasing LD dose and dose frequency at study entry. Participants on higher baseline LD doses ≥800 mg and dose frequencies ≥6 tended to have higher rates of discontinuation during conversion to ER CD-LD. Conclusions. Converting participants from other LD formulations to ER CD-LD is based on their current LD regimen. For the most common daily doses (≤1250 mg) and dose frequencies (<7) of LD, final mean dose ratios were within tight ranges of 2.1 to 2.4 for IR CD-LD (ADVANCE-PD) and 2.4 to 2.8 for CLE (ASCEND-PD) and were generally independent of the LD dosing frequency at study entry. These trials are registered with NCT00974974, NCT01130493.

Development of Capsule containing Immediate Release Tablet and Extended Release Floating Tablet for Monitoring Release of Atenolol

2021 ◽  
pp. 2216-2220
Author(s):  
Mahesh Hari Kolhe ◽  
Ritu Mehra Gilhotra ◽  
Govind Sarangdhar Asane
Keyword(s):  
Dosage Form ◽  
Extended Release ◽  
Heart Diseases ◽  
Immediate Release ◽  
High Plasma ◽  
Release Behavior ◽  
Dose Frequency ◽  
Floating Tablet ◽  
Formulation Parameters ◽  
Single Dosage

Atenolol is beta blocker absorbed through GIT use for heart diseases. Single tablets, floating tablets and sustained released formulations studied are insufficient to produce effective dose to enhance bioavailability and effectiveness. Our study is focused on development of capsule dosage form containing immediate release (IR) and floating extended release (ER) tablets for monitoring release of atenolol in single dosage form. Two different tablets for IR and ER were prepared in three different combinations (Batch). Pre-formulation and post formulation parameters found to be within acceptable limits of formulation. Release behavior of individual tablets and capsule containing two tablets were studied. Among the batches, capsules containing smaller amount of atenolol in IR and large amount of Atenolol in ER (batch II) showed impressive drug release pattern. This formulation was stable even after a month and achieved optimum release behavior of immediate release and sustained release. This study could be used for effective treatment for different heart complications and reduce toxicity due to high plasma concentration in increased dose frequency.

scholarly journals Safety and efficacy of extended release ketamine tablets in patients with treatment-resistant depression and anxiety: open label pilot study

2020 ◽  
Vol 10 ◽  
pp. 204512532092247 ◽  
Author(s):  
Paul Glue ◽  
Natalie J. Medlicott ◽  
Shona Neehoff ◽  
Peter Surman ◽  
Fred Lam ◽  
...  
Keyword(s):  
Extended Release ◽  
Vital Signs ◽  
Oral Formulation ◽  
Depression And Anxiety ◽  
Treatment Resistant Depression ◽  
Treatment Resistant ◽  
Open Label ◽  
Oral Ketamine ◽  
Tolerability Data ◽  
Resistant Depression

Background: Ketamine’s defining side effects are dissociation and increased blood pressure/heart rate. An oral formulation with delayed absorption could minimize these effects. We recently reported safety and tolerability data for an extended release ketamine tablet in healthy volunteers. Methods: To assess safety, tolerability, efficacy, and pharmacokinetics of an extended release oral ketamine tablet in patients with treatment-resistant depression/anxiety. This was a multiple dose open-label flexible dose uncontrolled study in seven patients with treatment-resistant depression/anxiety, who had all previously demonstrated mood improvement to subcutaneous ketamine. Assessments included ratings of anxiety, depression and dissociation, safety and tolerability, and blood samples for ketamine pharmacokinetics and brain-derived neurotrophic factor (BDNF) concentrations. Results: Improvements in anxiety and depression ratings occurred gradually over 96 h; all patients had >50% improvements in mood ratings. Ketamine was safe and well tolerated, with no changes in vital signs, and a single brief report of dissociation. Ketamine may induce its own metabolism, as the ratio of norketamine to ketamine increased out to 96 h. Serum BDNF concentrations did not change during the study. Conclusion: Ketamine’s safety/tolerability may be improved with an extended release oral formulation. Onset of mood improvement is slightly delayed compared with parenteral dosing. These data support the further development of extended release ketamine tablets for treatment of resistant depression and anxiety disorders.

Oxymorphone and oxymorphone extended release: A pharmacotherapeutic review

2018 ◽  
Vol 4 (3) ◽  
pp. 131 ◽  
Author(s):  
Paul Alexander Sloan, MD ◽  
Robert L. Barkin, PharmD, MBA
Keyword(s):  
Chronic Pain ◽  
Extended Release ◽  
Analgesic Efficacy ◽  
Opioid Analgesics ◽  
Immediate Release ◽  
The United States ◽  
Efficacy And Safety ◽  
Open Label ◽  
Opioid Agonist ◽  
Noncancer Pain

The treatment of chronic pain remains an enormous challenge in the United States. Opioid analgesics are an important component of pharmacotherapy for chronic pain and have proven efficacy in the management of cancer and noncancer chronic pain. The newest addition to oral opioid pharmacotherapy is oral oxymorphone, a semisynthetic opioid agonist that is now available in oral immediate-release (IR) and extended-release (ER) formulations. This review discusses the pharmacology, pharmacokinetics, pharmacodynamics, pharmacotherapeutics, and clinical use of oral oxymorphone IR and ER formulations for the management of moderate to severe pain for different types of patients in a variety of settings. Two published studies evaluated the efficacy and safety of oxymorphone IR in patients with moderate to severe postoperative pain and demonstrated that it provides rapid and effective analgesia and is generally well tolerated. Six published randomized controlled trials and three published open-label studies evaluated the efficacy and safety of oxymorphone ER for chronic cancer or noncancer pain. These trials found analgesic efficacy and tolerability comparable to that provided by morphine controlled release (CR) or oxycodone CR; treatment effects with oxymorphone ER were durable for treatment periods of 12 weeks at the same dose or up to 1 year with little dose escalation. Titrated doses of oxymorphone ER were effective and generally well tolerated in both opioid-experienced and opioid-naïve patients. Aspects of oxymorphone metabolism and limited protein binding may simplify treatment in certain populations.

Microsphere oxycodone for pain management in head and neck cancer (HNC) patients receiving radiotherapy.

2019 ◽  
Vol 37 (31_suppl) ◽  
pp. 123-123
Author(s):  
Andrew Michael McDonald ◽  
Sharon Spencer ◽  
Christopher Douglas Willey ◽  
James A. Bonner ◽  
Thomas A Swain ◽  
...  
Keyword(s):  
Clinical Trial ◽  
Extended Release ◽  
Common Adverse Effect ◽  
Immediate Release ◽  
Gastrostomy Tube ◽  
World Health ◽  
Future Research ◽  
Transdermal Fentanyl ◽  
Open Label ◽  
Opioid Dose

123 Background: Pain is a common adverse effect of RT in patients with HNC, and extended release analgesic options are limited due to high rates of dysphagia. Wax microsphere bound oxycodone was developed as an abuse-deterrent opioid and maintains a similar pharmacokinetic profile whether administered with or without an intact capsule. We hypothesized that microsphere oxycodone could be used for extended release analgesia in patients undergoing RT for HNC and would not need to be discontinued due to dysphagia or gastrostomy tube dependence. Methods: We performed an open-label prospective clinical trial (NCT03317730) to assess the feasibility of microsphere oxycodone for extended release analgesia during RT for HNC. Participants were > 18y, had histologically confirmed HNC, and were to receive > 50 Gy of RT. Analgesia was prescribed in accordance with the World Health Organization pain ladder. Non-opioid and immediate release opioids were used at the discretion of the treating physicians. Microsphere oxycodone was initiated when total daily opioid dose exceeded 30mg morphine sulfate equivalent and was titrated weekly during RT. The primary feasibility endpoint was frequency of microsphere oxycodone discontinuation within 3 months of RT for reasons other than pain resolution. Secondary endpoints included pain level during RT. Results: Twenty-six eligible patients were enrolled between June and November, 2018. Microsphere oxycodone was initiated in 13 (50%) patients at a median of 5 weeks after beginning RT (range: 0 – 7 weeks). The mean Brief Pain Index Severity composite score at time of microsphere oxycodone initiation was 5.4 (SD ±2.0) and was 4.8 (SD ±1.5) during the final week of RT ( p= 0.21). Six patients utilized a gastrostomy tube to administer microsphere oxycodone for all or part of RT. Microsphere oxycodone was discontinued in 1 (7.6%) patient due to perceived inefficacy, 0 patients due to toxicity, and 0 patients due to difficulty with administration. Conclusions: These results support the feasibility and safety of microsphere oxycodone for extended release analgesia in patients with HNC undergoing RT. Future research should compare microsphere oxycodone and transdermal fentanyl in this population. Clinical trial information: NCT03317730.

Immediate-release and extended-release formulations of second-generation antidepressants for the treatment of major depressive disorder in adults

2011 ◽  
Vol 26 (S2) ◽  
pp. 1289-1289
Author(s):  
M. Van Noord ◽  
G. Gartlehner ◽  
R. Hansen ◽  
L. Morgan ◽  
K. Thaler ◽  
...  
Keyword(s):  
Major Depressive Disorder ◽  
Depressive Disorder ◽  
Extended Release ◽  
Second Generation ◽  
Patient Adherence ◽  
Immediate Release ◽  
Cochrane Library ◽  
Open Label ◽  
Major Depressive ◽  
Extended Release Formulations

IntroductionExtended-release formulations of antidepressants have been marketed as a strategy to increase patient adherence. Changes in the formulation of drugs, however, could be related to changes in efficacy and tolerability. Among second-generation antidepressants, bupropion, fluoxetine, mirtazapine, paroxetine, and venlafaxine are available in immediate- and extended-release formulations.ObjectivesTo compare the efficacy, tolerability, and adherence of immediate- versus extended-release formulations of second-generation antidepressants for the treatment of major depressive disorder (MDD) in adults.AimTo provide an evidence base for clinicians when choosing immediate- or extended-release formulations of antidepressants for the treatment of MDD.MethodsWe conducted a comparative effectiveness review for the U.S. Agency for Healthcare Research and Quality searching PubMed, EMBASE, The Cochrane Library, and the International Pharmaceutical Abstracts up to May 2010. Two people independently reviewed the literature, abstracted data, and rated the risk of bias.ResultsSix RCTs and one observational study provided evidence about the comparative efficacy, tolerability, and adherence of bupropion SR (sustained release) versus bupropion XL (extended release), fluoxetine daily vs. fluoxetine weekly, paroxetine IR (immediate release) versus paroxetine CR (continuous release), and venlafaxine IR versus venlafaxine XR (extended release). Overall, no substantial differences in efficacy and safety could be detected. Open-label and observational evidence indicated better adherence for bupropion XL and fluoxetine weekly than for immediate-release medications. No differences in adherence could be detected between paroxetine IR and paroxetine CR.ConclusionsOur findings indicate similar efficacy and tolerability between immediate- and extended-release formulations. Whether extended-release formulations lead to better adherence remains unclear.

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