Evaluation of Community Pharmacists Knowledge, Attitude and Practice towards Modified Release Dosage Forms

Purpose:To evaluate knowledge, practice and attitude of community pharmacists in Basra regarding modified release dosage forms which are widely used for many therapeutic purposes in pharmacy practice. Methods:The current study was conducted among certified pharmacists in Basra governorate- south of Iraq. Data collection was carried out by a questionnaire. Results:A total number of 175 community pharmacists responded to the questionnaire. The majority worked in OTC based dispensing pharmacies located in the center of the city. Most respondents missed K1 and were unable to state the difference between different types of modified products. There was a major positive agreement towards medical representatives' rule in promoting the prescribing of modified release products by physicians. Avoiding crushing and breaking of solid oral modified release drugs were identified by the majority of participants. Correlation analysis showed a 22.8 correlation coefficient between knowledge and attitude which was statistically significant. Males showed statistically significant higher knowledge and practice scores than females. Conclusions:The conduction of a brief educational program would be very beneficial in bringing basic theoretical knowledge with practicing points of interest and promote a more positive attitude toward this unique class of novel drug delivery system.

Analytical quality by design approach to RP-HPLC method development and validation for simultaneous estimation of esomeprazole and naproxen in modified-release dosage form

Background The present work describes the development and validation of a new, specific, accurate, and precise stability-indicating RP-HPLC method for the simultaneous estimation of Esomeprazole (ESP) and Naproxen (NAP) in modified-release bi-layer tablet dosage form. Analytical Quality by Design concept was implemented through the method development exercise to establish the robustness of the method. Results Method development was performed on C18, 250 × 4.6 mm ID, and 5 µm particle size column with 10 µl injection volume using a photodiode array (PDA) detector to monitor the detection at 280 nm. The mobile phase consisted of the buffer: methanol at a ratio of 50: 50 (v/v), and the flow rate was maintained at 1.5 ml/min, and the column oven temperature was maintained at 30 °C. The retention times for NAP and ESP were found 5.9 ± 0.1 and 8.9 ± 0.1 min, respectively. The method was validated in terms of system suitability, specificity, accuracy, linearity, precision, and solution stability. Linearity was observed over the range of concentration 8–12 µg/ml for ESP and 200–300 µg/ml for NAP, and the correlation coefficient (R2) was found excellent > 0.999. The method was specific to ESP and NAP, and the peak purity was found 99.97% for ESP and 100.00% for NAP. The method was precise and had %RSD less than 2. Recovery study for accuracy with placebo was found in the range of 99.63–100.36% for ESP and 99.91–100.43% for NAP. Conclusion This proposed fast, reliable, cost-effective method can be used as a quality control tool for the simultaneous determination of Esomeprazole and Naproxen in routine laboratory analysis. Graphical Abstract

AN EXPERIMENTAL DESIGN IN THE OPTIMIZATION OF VARIOUS TABLET EXCIPIENT FORMULATIONS = A CONCISE REVIEW

The use of an experimental design technique in the development of various pharmaceutical preparations, including tablet preparations, has become the latest trend. Because of their ease of use, tablet formulations are popular among both producers and patients. To increase the usage of tablets in diverse circles and settings, researchers are working to develop a variety of tablet excipients for various functions. Fast dissolving tablets (FDT), effervescent tablets, modified-release tablets, oral mucoadhesive tablets, gastroretentive tablets, and colon targeted tablets are some of the tablet formats that have been developed in addition to traditional tablets. This review will look at how formulation optimization in tablet preparations has been done during the previous ten years using specific literacies. The articles for this review were found using the keywords tablet, excipient, matrices, formulation, and QBD in specialized databases such as Elsevier, Pubmed, and Cambridge. Other options include Springer publications, material from the Internet, and articles published online by The Lancet Respiratory Medicine, Medscape, and Statpearls. The formulation design strategy is based on the experimental design approach carried out on the kind of tablet preparation, which has distinct important quality parameters.

Development of a Once-Daily Modified-Release Formulation for the Short Half-Life RIPK1 Inhibitor GSK2982772 using DiffCORE Technology

Purpose GSK2982772 is a selective inhibitor of receptor-interacting protein kinase-1 (RIPK1) with a short 2- to 3-h half-life. In a previous modified-release (MR) study, a matrix monolithic formulation (80% GSK2982772 released over 12 h) provided a once-daily (QD) pharmacokinetic (PK) profile in the fasted state; however, it was susceptible to food effects. The current study evaluated the safety and PK of MR formulations using GSK proprietary DiffCORE™ technology. Methods Part A evaluated PK following single-dose (240 mg) fasted and fed (high-fat meal) administration of three DiffCORE MR formulations within pre-defined in vitro extremes of 80% GSK2982772 released over 12 h (MR-12 h) to 80% GSK2982772 released over 18 h (MR-18 h) versus an immediate-release formulation. Part B evaluated MR-16 h (120–960 mg) in different prandial states. Results Pharmacokinetic profiles for all MR formulations and doses tested in the fasted and fed states were consistent with QD dosing. Conclusions The DiffCORE technology overcame the food effect vulnerability observed with the matrix monolithic formulation. The MR-16 h formulation was selected for further clinical development as a QD dosing regimen (NCT03649412 September 26, 2018).

Hydrogels for modified-release drug delivery systems

Hydrogels for the modified-release drug delivery systems is a continuously growing area of interest for the pharmaceutical industry. According to the global market, the use of polymers in this area is projected to reach $31.4 million by 2027. This review discusses the recent advances and perspectives of hydrogel in drug delivery systems for oral, parenteral, nasal, topical, and ophthalmic. The search strategy did in January 2021, and it conducted an extensive database to identify studies published from January 2010 to December 2020.We described the main characteristic of the polymers to obtain an ideal hydrogel for a specific route of administration and the formulations that was a highlight in the literature. It concluded that the hydrogels are a set useful to decrease the number of doses, side effects, promote adhesion of patient and enhances the bioavailability of the drugs improving the safety and efficacy of the treatment.

Formulation, Characterization and Release Behaviour of Metformin Hydrochloride Modified Release Tablet by Using Hydrophilic Polymers

Amongst the many public health problems, the diabetes mellitus is considered as a chronic life-style related disease which is now growing as an epidemic in both developed as well as developing countries. The current study is about formulation of metformin hydrochloride tablet to confirm their sustained release property by using various polymers. The tablets are prepared by granulation techniques using binding solution containing polyvinyl pyrolline K30. The possible interaction between the pure metformin hydrochloride and polymers are identified by Fourier transform-infrared spectroscopy. Tablets were formulated with different polymers like Hydroxy propyl methyl cellulose K100 and sodium carboxymethyl cellulose. Matrix prepared with high concentration of HPMC K100 polymer retards the drug release up to 6 h at 59 %, but the formulation 2 (F2) showed 72.72% of drug release in 6 h. The release of drug from the F2 formulation was found to be prolonged drug release when compared to other formulations. Hence our study conclude that the HPMC K100 polymer containing formulation showed good sustained release property owing to the high gel strength and well high viscosity nature of the polymer.

Development and Characterization of Nanoemulsions for Ophthalmic Applications: Role of Cationic Surfactants

The eye is a very complex organ comprising several physiological and physical barriers that compromise drug absorption into deeper layers. Nanoemulsions are promising delivery systems to be used in ocular drug delivery due to their innumerous advantages, such as high retention time onto the site of application and the modified release profile of loaded drugs, thereby contributing to increasing the bioavailability of drugs for the treatment of eye diseases, in particular those affecting the posterior segment. In this review, we address the main factors that govern the development of a suitable nanoemulsion formulation for eye administration to increase the patient’s compliance to the treatment. Appropriate lipid composition and type of surfactants (with a special emphasis on cationic compounds) are discussed, together with manufacturing techniques and characterization methods that are instrumental for the development of appropriate ophthalmic nanoemulsions.

COMPARISON OF EFFICACY OF COMBINATION OF METFORMIN PLUS MODIFIED-RELEASE GLICLAZIDE WITH COMBINATION OF METFORMIN PLUS SITAGLIPTIN IN PATIENTS WITH TYPE-2 DIABETES MELLITUS

Introduction: Diabetes Mellitus (DM) is one of the leading causes of morbidity and mortality around the world and is responsible for 3.8 million deaths per year. Its prevalence had shown an exponential rise worldwide in the last two decades, from 30 million cases in 1985 to 177 million in 2000 Objective: To compare the efficacy of the combination of Metformin plus modified-release Gliclazide with a variety of Metformin plus Sitagliptin in patients with type-2 diabetes mellitus. Methodology: This study was conducted at the Department of Medicine, Lady Reading Hospital Peshawar. The study design was a randomized controlled trial conducted for one year from May 2017 to May 2018, in which 62 patients in each group were observed. All patients with type 2 Diabetes Mellitus with baseline HbA1c ≥ 8% and duration >1 year, either gender with age range 35 to 65 years, were included. All patients were subjected to detailed history and clinical examinations. All patients were randomly allocated in two groups by lottery method. Patients in Group A were subjected to the combination of Metformin (1gm twice daily) with modified-release Gliclazide (60mg), and patients in Group B were subjected to the variety of Metformin (1 gm twice daily) with Sitagliptin (50 mg twice daily). All patients were followed up after three months, and blood samples for HbA1c levels were obtained. The analysis was done in SPSS version 20. Results: The Study showed that the mean age in Group A was 58 years ± 12.78, and the mean age in Group B was 55 years ± 13.12. In Group A, 44% of patients were male, and 56% of patients were female, while in Group B, 45% of patients were male, and 55% of patients were female. Moreover, Group A (Metformin (1gm twice daily) + Gliclazide (60mg) was effective in 45% of patients while Group B Metformin (1 gm twice daily) + Sitagliptin (50 mg twice daily) was effective in 71% of patients. Conclusion: Our study concludes that Metformin plus Sitagliptin is more effective than Metformin plus modified-release Gliclazide.