Consistency of coating thickness of delayed-release mesalamine formulations: drug release characteristics across the pH range found in the GI tract of patients with ulcerative colitis

The Pharmaceutical industry has become more interested in developing fixed-dose combinations (FDCs) in recent years. FDCs have been used successfully in a variety of clinical areas, including diabetes, HIV/AIDS,and cardiovascular diseases etc. FDCs are intended to extend the product life cycle and enhance patient compliance by decreasing cost. Active Pharmaceutical ingredients are chosen for FDC development based on variety of purposes such as Pharmacokinetic profile, drug-drug interactions, mechanism of action, and manufacturability for successful development. Tablet in tablet technology has gained popularity in recent years for creating modified release products. The compression coating or solvent-free-coating technology is also known as Tablet in Tablet technology. Tablet in Tablet technology is presently the finest alternative technology for the formulation of bilayer tablets for physical separation of active medicines and used to avoid chemical incompatibilities and to produce different drug release patterns such as rapid release, sustained release, controlled release, delayed release, and pulsatile release. This review mainly focuses on combining the techniques of both FDC and Tablet in Tablet formulations which offer a wide variety of benefits such as increased patient compliance, convenience, separation of incompatible ingredients, avoiding close interaction of two drugs, achieving various drug release patterns and maximizing the potency of both drugs over conventional oral dosage forms Keywords: Fixed dose combinations, Tablet in tablet technology, Compression coated tablet, Bilayer tablet, delayed release

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Clinical assessment of inflammatory bowel disease activity: a critical overview

Journal of Medical Science ◽

10.20883/medical.e26 ◽

2015 ◽

Vol 84 (2) ◽

pp. 113-125

Author(s):

Adam Fabisiak ◽

Natalia Murawska ◽

Anna Mokrowiecka ◽

Ewa Małecka-Panas ◽

Jakub Fichna

Keyword(s):

Ulcerative Colitis ◽

Inflammatory Bowel Disease ◽

Clinical Aspects ◽

Gi Tract ◽

Inflammatory Conditions ◽

Symptom Recognition ◽

Bowel Diseases ◽

Inflammatory Bowel ◽

Critical Overview ◽

Future Concepts

Crohn’s disease (CD) and ulcerative colitis (UC), which belong to the group of inflammatory bowel diseases (IBD), are chronic inflammatory conditions of the gastrointestinal (GI) tract. Over the last eighty years the overview of IBD has evolved, along with disease symptom recognition, hypotheses on etiology and recommendations for clinical treatment. This review focuses on the clinical aspects of IBD throughout the years and discusses the most recent and future concepts in IBD diagnosis.

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Enrichment of aqueous solubility and dissolution profile of mesalamine: In vitro evaluation of solid dispersion

Journal of Pharmaceutical and Biological Sciences ◽

10.18231/j.jpbs.2021.018 ◽

2021 ◽

Vol 9 (2) ◽

pp. 127-135

Author(s):

Anil Raosaheb Pawar ◽

Pralhad Vitthalrao Mundhe ◽

Vinayak Kashinath Deshmukh ◽

Ramdas Bhanudas Pandhare ◽

Tanaji Dilip Nandgude

Keyword(s):

Ulcerative Colitis ◽

Drug Release ◽

Dissolution Rate ◽

Solid Dispersion ◽

Solid Dispersions ◽

Aqueous Solubility ◽

In Vitro Dissolution ◽

Dissolution Profile ◽

Peg 4000

The aim of the present study was to formulate solid dispersion (SD) of Mesalamine to enrich the aqueous solubility and dissolution rate. Mesalamine is used in the management of acute ulcerative colitis and for the prevention of relapse of active ulcerative colitis. In the present study, Solid dispersion of Mesalamine was prepared by Fusion and Solvent evaporation method with different polymers. SD’s were characterized by % practical yield, drug content, Solubility, FT-IR, PXRD (Powder X- ray diffractometry), SEM (Scanning electron microscopy), in vitro dissolution studies and Stability studies. The percent drug release of prepared solid dispersion of Mesalamine by fusion and solid dispersion method (FM47, FM67, SE47 and SE67) in 1:7 ratio was found 81.36±0.41, 86.29±0.64, 82.45±0.57and 87.25±1.14 respectively. The aqueous solubility and percent drug release of solid dispersion of Mesalamine by both methods was significantly increased. The PXRD demonstrated that there was a significant decrease in crystallinity of pure drug present in the solid dispersions, which resulted in an increased aqueous solubility and dissolution rate of Mesalamine.The significant increase in aqueous solubility and dissolution rate of Mesalamine was observed in solid dispersion as the crystallinity of the drug decreased, absence of aggregation and agglomeration, increased wetability and good dispersibility after addition of PEG 4000 and PEG 6000.

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Review of normal gastrointestinal tract, ulcerative colitis, proctitis and rectal medication adherence

British Journal of Nursing ◽

10.12968/bjon.2020.29.14.805 ◽

2020 ◽

Vol 29 (14) ◽

pp. 805-811

Author(s):

Pineshwari Naeck-Boolauky ◽

Jitka Adio ◽

Jennie Burch

Keyword(s):

Ulcerative Colitis ◽

Inflammatory Bowel Disease ◽

Gastrointestinal Tract ◽

Side Effects ◽

Rectal Mucosa ◽

Gi Tract ◽

Therapeutic Outcomes ◽

Rectal Medication ◽

Inflammatory Bowel

The gastrointestinal (GI) tract has a number of functions—ingestion, digestion, absorption and elimination. When the GI tract is working normally, it is efficient. However, this can change when disease, such as inflammatory bowel disease (IBD) occurs. IBD is a long-term relapsing and remitting autoimmune disease; it incorporates ulcerative colitis (UC). In UC, part or all the mucosa lining the rectum and colon becomes inflamed and ulcerated. UC that affects the rectum only is called proctitis. Effective treatment is essential. It is better to target the rectal mucosa directly in proctitis, using topical rectal medications in enemas or suppositories, as these have fewer side-effects and resolve symptoms more quickly than systemic drugs. However, patients may not feel clear about aspects of their IBD care and can find it difficult to initiate and comply with treatment and maintenance regimens. Nurses need to educate and support them to achieve optimal therapeutic outcomes in both the immediate and long terms.

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Delayed-Release Multi Matrix System (MMX™) Mesalazine in Ulcerative Colitis

Drugs ◽

10.2165/00003495-200767170-00011 ◽

2007 ◽

Vol 67 (17) ◽

pp. 2643-2644

Author(s):

Åke Nilsson

Keyword(s):

Ulcerative Colitis ◽

Matrix System ◽

Delayed Release

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A Phase 2a, Multicenter, Randomized, Double-Blind, Parallel-Group, Placebo-Controlled Trial of IBD98-M Delayed-Release Capsules to Induce Remission in Patients with Active and Mild to Moderate Ulcerative Colitis

Cells ◽

10.3390/cells8060523 ◽

2019 ◽

Vol 8 (6) ◽

pp. 523 ◽

Cited By ~ 3

Author(s):

Gionata Fiorino ◽

Giacomo Carlo Sturniolo ◽

Fabrizio Bossa ◽

Andrea Cassinotti ◽

Antonio Di Sabatino ◽

...

Keyword(s):

Ulcerative Colitis ◽

Clinical Response ◽

Activity Index ◽

Controlled Trial ◽

Disease Activity Index ◽

Fecal Calprotectin ◽

Summary Score ◽

Double Blind ◽

Release Formulation ◽

Delayed Release

IBD98-M is a delayed-release formulation of mesalamine (mesalazine) and SH with a potential therapeutic role in ulcerative colitis (UC). A total of 51 patients with a modified Ulcerative Colitis Disease Activity Index (UCDAI) score of ≥4 and ≤10, and a modified UCDAI endoscopy subscore ≥1 were randomized for 6 weeks of double-blind treatment with IBD98 0.8 g/day or IBD 1.2 g/day or placebo. The efficacy and safety of IBD98-M in mild to moderate active UC were primarily evaluated. At week 6, 1 (5.9%), 2 (12.5%), and 2 (11.1%) patients receiving IBD98-M 0.8 g, IBD98-M 1.2 g, and placebo, respectively, (p > 0.999) achieved clinical remission. Higher clinical response was seen in IBD98-M 1.2 g (31.3%) versus placebo (16.7%) and endoscopic improvement in IBD98-M 0.8 g (29.4%) versus placebo (22.2%) was seen. Fecal calprotectin levels were reduced in IBD98-M groups versus placebo (p > 0.05). IBD98-M patients achieved significant improvement in physical health summary score component of the SF-36 (p = 0.01 and p = 0.03 respectively) compared to placebo. IBD98-M did not meet the primary end point but had higher clinical response (1.2 g/day) and endoscopic improvement (0.8 g/day) compared to placebo. The safety result shown that IBD98-M treatment was safe and well tolerated in this patient population. No new safety signals or unexpected safety findings were observed during the study. Further trials with different stratification and longer follow-up may be needed to evaluate the efficacy.

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