scholarly journals Gliclazide: Biopharmaceutics Characteristics to Discuss the Biowaiver of Immediate and Extended Release Tablets

2020 ◽  
Vol 10 (20) ◽  
pp. 7131
Author(s):  
Bruna de Carvalho Mapa ◽  
Lorena Ulhôa Araújo ◽  
Neila Márcia Silva-Barcellos ◽  
Tamires Guedes Caldeira ◽  
Jacqueline Souza
Keyword(s):  
Extended Release ◽  
Immediate Release ◽  
Pharmacokinetic Profile ◽  
Dosage Forms ◽  
New Drugs ◽  
Essential Medicines ◽  
World Health ◽  
Drug Candidate ◽  
Dissolution Profile ◽  
First Choice

The lists of essential medicines of the World Health Organization (WHO) and Brazil include gliclazide as an alternative to the oral antidiabetic drug of first choice, metformin, in the treatment of type 2 diabetes mellitus because of its pharmacokinetic profile and few side effects. Thus, it is also considered by WHO and the International Pharmaceutical Federation (FIP) as a drug candidate to biowaiver, which is the evaluation of how favorable the biopharmaceutics characteristics are in order to obtain waiver from the relative bioavailability/bioequivalence (RB/BE) studies to register new medicines. This paper presents a review about the solubility, permeability and dissolution of gliclazide. A critical analysis of the information allowed to identify gliclazide as a Biopharmaceutics Classification System (BCS) Class II drug. Therefore, new drugs in immediate release dosage forms will not be eligible for biowaiver. Regarding the extended release dosage forms, besides the limited solubility, no information on the comparative dissolution profile was found, which would be necessary to analyze a possible biowaiver for a smaller dosage. It can be concluded that the registration of new medicines containing gliclazide must undergo RB/BE studies, since there is not enough evidence to recommend the replacement and waiver of such studies for immediate and extended release formulations.

Steady-state pharmacokinetic profile of OROS hydromorphone extended release and hydromorphone immediate release

2010 ◽  
Vol 11 (4) ◽  
pp. S44
Author(s):  
K. Moore ◽  
D. St. Fleur ◽  
N. Marricco ◽  
T. Ariyawansa ◽  
V. Page ◽  
...  
Keyword(s):  
Steady State ◽  
Extended Release ◽  
Immediate Release ◽  
Pharmacokinetic Profile

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.

scholarly journals Hydromorphone in the Management of Cancer-Related Pain: An Update on Routes of Administration and Dosage Forms

2007 ◽  
Vol 10 (4) ◽  
pp. 504 ◽  
Author(s):  
Maansi G. Kumar ◽  
Senshang Lin
Keyword(s):  
Dosage Forms ◽  
World Health ◽  
Health Concern ◽  
Major Health ◽  
Routes Of Administration ◽  
First Choice ◽  
The World ◽  
Rapid Effect ◽  
Synthetic Derivative ◽  
Health Organization

Pain is experienced by a majority of cancer patients. As life expectancy has increased in developed and developing countries, cancer-related pain has become a major health concern. Despite the use of the three-step analgesic ladder proposed by the World Health Organization, pain still remains under treated. Morphine, the gold standard against which all other opioids has been compared is considered the first choice for management of cancer-related pain. However, recently focus has shifted to the use of hydromorphone, a semi-synthetic derivative of morphine, which is more potent, more soluble and has a comparable side-effect profile. This review focuses on the use of hydromorphone for the management of cancer-related pain emphasizing on the various routes of administration as well as dosage forms, and providing a direction for the preference of a particular route depending on the need for a rapid effect and the individual’s situation. Various approaches used to modify the release of hydromorphone from the drug delivery systems with the perspective of improving patient compliance are also being discussed.

scholarly journals Population pharmacokinetic models of first choice beta-lactam antibiotics for severe infections treatment: What antibiotic regimen to prescribe in children?

2020 ◽  
Vol 23 ◽  
pp. 470-485
Author(s):  
Amélie Marsot
Keyword(s):  
Pediatric Population ◽  
Individual Characteristics ◽  
Essential Medicines ◽  
World Health ◽  
Population Pharmacokinetic ◽  
Inclusion Criteria ◽  
Drug Dosing ◽  
First Choice ◽  
Dosing Regimens ◽  
Severe Infections

Background: To perform a review describing the pharmacokinetic (PK) parameters and covariates of interest of the eight first choice β-lactams (BL) antibiotics for treatment of severe infections in pediatric population. Pediatric sepsis and septic shock reportedly affect 30% of children admitted to pediatric intensive care units, with a 25% mortality rate. Eight BL are included as first choice antibiotic for severe infections in pediatric population in the World Health Organization model list of essential medicines for children. Methods: The PubMed/Medline databases was searched and included studies if they described a population PK model of piperacillin, amoxicillin, ampicillin, cefotaxime, ceftriaxone, cloxacillin, imipenem or meropenem in neonates or children. We compared the PK parameters for each drug. We analysed the used covariates to estimate PK parameters. We compared the pharmacokinetics/pharmacodynamics (PK/PD) targets and the drug dosing recommendations. Results: Thirty-four studies met inclusion criteria with seven studies for piperacillin, five for amoxicillin, three for ampicillin, three for cefotaxime, two for ceftriaxone, two for imipenem and twelve for meropenem. None met inclusion criteria for cloxacillin. Ages ranged from 0-19.1 years with 12 studies including preterm. Body weight, age and renal function were the three major covariates in neonates and children. Different PK/PD targets were observed (between 40% to 100% of the dosing regimen interval of time over which the unbound (or free) drug concentration remains above the minimal inhibitory concentration (MIC) (fT>MIC) or four times the MIC (fT>4xMIC)). Several drug-dosing regimens were fond recommended according to the age and pathogens MIC using intermittent, timed or continuous infusions. Conclusions: Consensus is lacking on the optimal dosing regimens for these eight first choice antibiotics. A more personalized approach to antibiotic drugs dosing with individual characteristics of patient and pathogen susceptibility is required. According PK/PD targets and used dosing regimens, prospective clinical studies are required to investigate clinical cure, patient survival and emergence of antimicrobial resistance.

scholarly journals Comparison of dissolution profile of extended-release oral dosage forms - two one-sided equivalence test

2013 ◽  
Vol 49 (2) ◽  
pp. 367-371 ◽  
Author(s):  
Felipe Rebello Lourenço ◽  
Daniela Dal Molim Ghisleni ◽  
Rosa Noriko Yamamoto ◽  
Terezinha de Jesus Andreoli Pinto
Keyword(s):  
Extended Release ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Dissolution Profile ◽  
Equivalence Test ◽  
Significance Level ◽  
Similarity Factor ◽  
Alternative Approach ◽  
Oral Dosage Forms ◽  
States Pharmacopeia

The aim of this work is to present the two one-sided test (TOST) as an alternative approach to compare dissolution profiles of extended-release dosage forms. The dissolution profiles of oxycodone extended-release tablets containing 10 mg, 20 mg and 40 mg (reference and generic) were evaluated according to the requirements described in United States Pharmacopeia. These dissolution profiles were compared using the conventional similarity factor (f2) and the proposed TOST as an equivalence test. TOST is a simple and alternative approach to compare dissolution profiles of extended-release dosage forms. It allows us to identify the time-point (or time-points) that did not show similarity. We concluded that the two one-sided test performed at a significance level of 5% and defined as D = 10 showed results comparable to those obtained by the conventional similarity factor (f2).

scholarly journals Methylphenidate Efficacy: Immediate versus Extended Release at Short Term in Mexican Children with ADHD Assessed by Conners Scale and EEG

2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
Alfredo Durand-Rivera ◽  
Efren Alatorre-Miguel ◽  
Elizabeth Zambrano-Sánchez ◽  
Celia Reyes-Legorreta
Keyword(s):  
Extended Release ◽  
Immediate Release ◽  
Pharmacological Therapy ◽  
Wilcoxon Test ◽  
Emotional Instability ◽  
Release Formulation ◽  
Extended Release Formulation ◽  
First Choice ◽  
Significant Difference ◽  
Dsm Iv

Attention deficit hyperactivity disorder (ADHD) affects 5-6% of school aged children worldwide. Pharmacological therapy is considered the first-line treatment and methylphenidate (MPH) is considered the first-choice medication. There are two formulations: immediate release (IR) MPH and long-acting (or extended release) formulation (MPH-ER). In this work, we measure the efficacy of treatment for both presentations in one month with Conners’ scales and electroencephalography (EEG).Results. for IR group, in parents and teachers Conners test, all items showed significant differences, towards improvement, except for teachers in perfectionism and emotional instability. For ER group in parent’s Conners test, the items in which there were no significant differences are psychosomatic and emotional instability. For teachers, there were no significant differences in: hyperactivity and perfectionism. Comparing the Conners questionnaires (parents versus teachers) we find significant differences before and after treatment in hyperactivity, perfectionism, psychosomatics, DSM-IV hyperactive-impulsive, and DSM-IV total. In the EEG the Wilcoxon test showed a significant difference(P<0.0001). As we can see, both presentations are suitable for managing the ADHD and have the same effect on the symptomatology and in the EEG.

scholarly journals Evaluation of Critical Quality Attributes of Immediate Release Ciprofloxacin Tablets of Different Pharmaceutical Companies in Bangladesh

2021 ◽  
Vol 17 (4) ◽  
pp. 781-788
Author(s):  
Paroma Arefin ◽  
Rezvi Ahmed ◽  
Md Shehan Habib ◽  
Sreebash Chandra Bhattacharjee ◽  
Dipankar Chakraborty ◽  
...  
Keyword(s):  
Immediate Release ◽  
Quality Attributes ◽  
Essential Medicines ◽  
World Health ◽  
Physical Parameters ◽  
Pharmaceutical Companies ◽  
Pharmaceutical Dosage Form ◽  
Critical Quality Attributes ◽  
Weight Variation ◽  
Tract Infections

Critical Quality Attributes (CQAs) is an important factor in Pharmaceutical development as it determines the strength, release of the API from SDFs, and stability of a pharmaceutical dosage form. Moreover, substandard and counterfeit drugs have been a major concern in recent days.Ciprofloxacin is a second-generation fluoroquinolone derivative that exerts its effects by inhibiting bacterial DNA gyrase (Topoisomerase II). It is used for the treatment of bacterial gastroenteritis, respiratory tract infections, controlling bronchitis and pneumonia caused by Gram negative bacteria. Ciprofloxacin has been listed in the World Health Organization (WHO) Model list of Essential Medicines. In recent decades, the pharmaceutical industry has been experiencing excellent growth in both local and international market.In our present study, we have analyzed theCritical Quality Attributes (CQAs) including length, thickness, friability, weight variation, hardness test and disintegration time of Ciprofloxacin tablet to study whether the ciprofloxacin immediate release tablets of different pharmaceutical companies available in the Bangladeshi market to assess whether they are compliant to BP or USP guidelines in respect of physical parameters. We have also performed statistical analysis and found that that all the tablets from different brands are within the BP or USP requirements. So, from the study, we reached the conclusion that the critical quality attributes for ciprofloxacin immediate release tablets of different pharmaceutical companies in Bangladesh ensure the appropriateness of their strength, purity, release of the API from SDFs, and stability.

scholarly journals Formulation development and evaluation of duloxetine extended-release tablets

2021 ◽  
pp. 62-67
Author(s):  
Saibabu Ch ◽  
Naresh M ◽  
Sirisha K ◽  
Vineetha R ◽  
Sai Kumar P ◽  
...  
Keyword(s):  
Extended Release ◽  
Immediate Release ◽  
Wet Granulation ◽  
Dissolution Profile ◽  
Formulation Development ◽  
Compression Process ◽  
In Vitro Drug Release ◽  
Profile Matching ◽  
Core Tablet

Duloxetine  is an anti-depressant drug which is used in depression. The aim of present investigation was to prepare an ER tablet of duloxetine with similar dissolution profile matching to Effexor ER. An immediate release core tablet of 100mg was prepared and it was compression coated using HPMC matrix system. HPMC of three viscosity grades i.e., K4M, K15M, K100M and different concentrations of 15% polymer, 25% polymer, 35% polymer & 45% polymer were taken. With the above polymers by using wet granulation and direct compression process 11 formulations were prepared. The data obtained from in vitro drug release was used to determine the similarity factor between marketed and optimized product. Out of all F11 formulation (K15M 35% polymer) is optimized and is matching with the marketed product.

Compaction of Pharmaceuticals

MRS Bulletin ◽  
1997 ◽  
Vol 22 (12) ◽  
pp. 34-37 ◽  
Author(s):  
Nicholas G. Lordi ◽  
Alberto M. Cuitino
Keyword(s):  
Oral Administration ◽  
High Speed ◽  
Extended Release ◽  
Oral Absorption ◽  
Dosage Forms ◽  
Over The Counter ◽  
First Choice ◽  
Market Requirements ◽  
Low Volume ◽  
Aseptic Conditions

It has been estimated that more than 80% of all medication doses are administered as tablets—that is, in unit dosage forms prepared by compacting powders in dies. For drugs with acceptable oral-absorption profiles, the compacted tablet is the first choice as a delivery system in drug development. Modern tablets range in size from 25 milligrams (veterinary implants) to several grams (veterinary “boluses”). The most common tablet shape is the double convex-faced disk. Shapes range from capsule to triangular forms, in many instances with bisects embossed or debossed with identification codes and company logos. Tablets may be either film- or sugar-coated, may be designed for immediate or extended release, or may be prepared as multilayer or laminated forms. In addition to oral administration, tablets may be predissolved or designed to be disintegrated in the mouth, or may be administered by injection or as suppositories. Production rates for over-the-counter products such as acetaminophen tablets can exceed three 1,000-kg batches per week, requiring high-speed multiple-station tablet presses for production. In contrast, implants—which have low-volume market requirements—must be made under aseptic conditions on special singlestation presses.

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