Development of raft-forming liquid and chewable tablet formulations incorporating quercetin solid dispersions for treatment of gastric ulcers

: Glipizide (GZ) is an oral blood-glucose-lowering drug of the sulfonylurea class characterized by its poor aqueous solubility. Aiming for the production of GZ tablets with rapid onset of action followed by prolonged effect; GZ-Polyethylene glycol (PEG 4000 and 6000) solid dispersions with different ratios, (using melting and solvent evaporation method), as well as, coprecipitate containing GZ with polymethyl-methacrylate (PMMA) were prepared. Four tablet formulations were prepared containing; a) GZ alone, b) GZ: PEG6000, 1:10, c) GZ:PMMA 1:3, and, d)both GZ:PEG6000 1:10 and GZ:PMMA 1:3. The solvent evaporation method showed more enhancement of GZ solubility than the melting one, and this solubilizing effect increased with PEG increment. Generally, PEG6000 showed more enhancement of dissolution than PEG4000 especially at 1:10 drug: polymer ratio (the most enhancing formula). Also, the prepared tablet formulations showed acceptable physical properties according to USP/NF requirements. The dissolution results revealed that tablets containing PEG6000 (1:10) have the most rapid release rate, followed by the formula containing both PEG6000 and PMMA, while that including PMMA alone showed the slowest dissolution rate. Moreover, In-vivo studies for each of the above four formulations, were performed using four mice groups. The most effective formula in decreasing the blood glucose level, through the first 6 hours, was that containing GZ and PEG6000, 1:10. However, formula containing the combination of enhanced and sustained GZ was the most effective in decreasing the blood glucose level through 16 hours. Successful in-vitro in-vivo correlations could be detected between the percent released and the percent decreasing of blood glucose level after 0.5 hours.

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Valuing Best Poloxamer Carrier for Meloxicam Solid Dispersions by novel microwave fusion: Designing and Characterization

Abasyn Journal Life Sciences ◽

10.34091/ajls.2.1.1 ◽

2019 ◽

pp. 1-15

Keyword(s):

Solid Dispersions ◽

Physicochemical Characterization ◽

Poloxamer 407 ◽

Research Activity ◽

Fusion Technique ◽

Poloxamer 188 ◽

Tablet Compression ◽

Tablet Formulations

Present research activity is to establish the best Poloxamer carriers for making solid dispersions (SD) with Meloxicam. The main aim of this investigation is to find the best among the better Poloxamer carriers viz., Poloxamer-108, Poloxamer-188, Poloxamer-237, Poloxamer-338 and Poloxamer-407 for making SD by novel microwave fusion technique. Four portions of Meloxicam: Poloxamer in various ratios (1:1, 1:2, 1:4 and 1:6) are used for making SD by microwave fusion technique later compressed using 8 station tablet compression machine. The SD and tablet formulations are evaluated for physicochemical characterization. All the prepared batches found to have satisfactory specifications as per pharmacopoeia. The authors concluded that Poloxamer-188 is found to be the best carrier among the Poloxamer carriers used for making Meloxicam SD. Keywords: Meloxicam, Poloxamer, microwave, solid dispersions, tablets

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Formulation and Evaluation of Isabgol and Liquorice Based Nutraceuticals Floating Tablets for Management of Gastric Ulcer

Current Nutraceuticals ◽

10.2174/2665978601999200930143521 ◽

2020 ◽

Vol 01 ◽

Author(s):

Ritesh Kumar Tiwari ◽

Lalit Singh ◽

Shashi Verma ◽

Vijay Sharma

Keyword(s):

Drug Release ◽

Sodium Bicarbonate ◽

Magnesium Stearate ◽

Gastric Ulcers ◽

Physical Parameters ◽

Floating Tablets ◽

Zero Order Kinetics ◽

Liquorice Extract ◽

Tablet Formulations

Background: Floating tablets extend drug residence time, enhance bioavailability and promote the delivery of local drugs to the stomach. With this objective, floating tablets were prepared for the treatment of gastric ulcers containing aqueous extract of liquorice and Isabgol. Methods: Tablets containing HPMC K100M (hydrophilic polymer), liquorice extract, sodium bicarbonate (gas generating agent), talc, and magnesium stearate were prepared using direct compression method. Physical parameters of formulations such as diameter, thickness, hardness, friability, weight uniformity, drug content, buoyancy time, dissolution, and mechanism for drug release, were assessed. The formulations have been optimized based on buoyancy time and in- vitro drug release. Results: The diameter of all formulations was in the range 11.310-11.833 mm; thickness was in the range 4.02-4.071 mm. The hardness ranged from 3.1 to 3.4 kg/cm. All formulations passed the USP requirements for friability and uniformity of weight. All tablet formulations had a buoyancy period of less than 5 min and throughout the research, the tablet stayed in floating condition. All tablet formulations were accompanied in drug discharge by zero-order kinetics and model Korsemeyer-Peppas. Conclusion: It was discovered that the optimized formulation was F7, which released 98.5 percent of the drug in 8 hr. invitro, while the buoyancy time was 3.5 min. For gastroretentive drug delivery systems, formulations containing Isabgol, sodium bicarbonate and HPMC K100 M in combination may be promising.

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Bioequivalence of the 4-mg Oral Granules and Chewable Tablet Formulations of Montelukast

Archives of Drug Information ◽

10.1111/j.1753-5174.2010.00029.x ◽

2010 ◽

pp. no-no ◽

Cited By ~ 1

Author(s):

Barbara Knorr ◽

Alan Hartford ◽

Xiujiang Susie Li ◽

Amy Yifan Yang ◽

Gertrude Noonan ◽

...

Keyword(s):

Chewable Tablet ◽

Tablet Formulations

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Downstream processing of polymer-based amorphous solid dispersions to generate tablet formulations

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2015.03.053 ◽

2015 ◽

Vol 486 (1-2) ◽

pp. 268-286 ◽

Cited By ~ 76

Author(s):

B. Démuth ◽

Z.K. Nagy ◽

A. Balogh ◽

T. Vigh ◽

G. Marosi ◽

...

Keyword(s):

Solid Dispersions ◽

Amorphous Solid ◽

Downstream Processing ◽

Amorphous Solid Dispersions ◽

Tablet Formulations

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Gastric Ulcers Produced by Cisplatin

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100099337 ◽

1981 ◽

Vol 39 ◽

pp. 582-583

Author(s):

S.K. Aggarwal ◽

J. San Antonio

Keyword(s):

Electron Microscopy ◽

Single Dose ◽

Side Effects ◽

Antitumor Agent ◽

Gastric Ulcers ◽

Enzyme Cytochemistry ◽

Intestinal Toxicity ◽

Ovarian Cancers ◽

Inner Surface

Cisplatin (cis-dichlorodiammineplatinum(II)) a potent antitumor agent is now available for the treatment of testicular and ovarian cancers. It is however, not free from its serious side effects including nephrotoxicity, gastro intestinal toxicity, myelosuppression, and ototoxicity. Here we now report that the drug produces peculiar bloating of the stomach in rats and induces acute ulceration.Wistar-derived rats weighing 200-250 g were administered cisplatin(9 mg/kg) ip as a single dose in 0.15 M NaCl. After 3 days the animals were sacrificed by decapitation. The stomachs were removed, the contents analyzed for pepsin and acidity. The inner surface was examined with a dissecting microscope after a moderate stretching for ulcers. Affected areas were fixed and processed for routine electron microscopy and enzyme cytochemistry.The drug treated animals kept on food and water consistently showed bloating and lesions (Fig. 1) with a frequency of 6-70 ulcers in the rumen section of the stomachs.

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