Formulation and characterization of gastroretentive discs containing famotidine

Raval, Jignyasha A.; Patel, Madhabhai M.

doi:10.1590/s1516-89132011000200010

Cited by 8 publications

(5 citation statements)

References 29 publications

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“…As thiolated formulations will form strong disulfide bonds with mucus, accordingly maximum force is required for the detachment from the mucus. Both residence time and mucoadhesion strength were increased accordingly with the concentrations of TOG in RGM-5 and RGM-6 due to high -SH content which favors the number of disulfide bonds with the mucus gel layer [41]. Formulations with SA showed moderate mucoadhesion time and strength.…”

Section: Evaluation Of Ex-vivo Mucoadhesion Time and Mucoadhesion Strmentioning

confidence: 99%

Okra-Thioglycolic Acid Conjugate—Synthesis, Characterization, and Evaluation as a Mucoadhesive Polymer

Naveen¹,

Gopinath

Kurakula

2020

Processes

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The success of mucoadhesive drug delivery systems relies on the type of polymer used, which becomes adhesive naturally upon hydration. Intended polymers should be able to maintain prolonged contact with biological membranes, and to protect or cater the drug to a prolonged period. Most of the hydro polymers form weak non-covalent bonds, that hinder localization of dosage forms at specific sites resulting in therapeutic inefficiency. This can be overcome by the thiol functionalization of natural polymers. In the present study, natural okra gum (OG) was extracted, followed by thiolation (TOG) and evaluated for mucoadhesion property and its role in enhancing the efficacy of repaglinide as a model drug (short-acting Type II antidiabetic drug). The thiol functionalization of OG (TOG) was confirmed by a Fourier-transform infrared spectroscopy (FTIR) study that showed a polyhedral to a spherical shape that had a rougher surface. Differential scanning calorimetry (DSC) and X-Ray Diffraction (XRD) studies of TOG indicated a decline in endothermic transition temperature and high crystallinity, respectively, in comparison to OG. CSFR (Crushing Strength: Friability Ratio), weight and thickness variations of repaglinidetablets formulated using TOG were >80% and <2.5% respectively. The highest swelling index (107.89 ± 1.99%) and strong mucoadhesion due to high disulfide bonds were observed for repaglinide TOG tablets in comparison to RG OG tablets. In-vitro release studies indicated a controlled drug release from thiolated formulations proportional to the concentration of thiomers that have a good correlation with in-vivo studies. Pharmacokinetic studies indicated higher AUC (area under the curve), longer t 1/2 with thiomers. and Level A IVIV (in vitro in vivo) correlation was established from the bioavailability and dissolution data. Consequently, all the obtained results suggest that thiomers based formulations can be promising drug delivery systems, even in targeting onerous mucosal surfaces like nasal, ocular or vaginal.by suitable approaches such as thiolation, to employ in mucoadhesion drug delivery systems [9]. Nevertheless, to date, there has been no research reported in demonstrating the synthesis of thiolated okra gum (TOG) and evaluating its use in designing mucoadhesive drug delivery systems.The term bio adhesion depicts the adhesion of the polymer to the biological membrane. Specifically, when the adhesion is limited to the mucosal surface it is named mucoadhesion [10]. The conception of mucoadhesion, as well as mucoadhesion polymers, was developed in the mid 1980s as an intriguing methodology especially for targeting the delivery of drugs at a site or at the absorption window. Mucoadhesive polymers become adhesive on hydration and characterized to have prolonged contact and residence time with the mucous membrane. [11]. Despite a few notable exceptions, gastric mucoadhesive systems do not reach their full potential. The success of the majority of the first generation mucoadhesion polymers was limited owing to thei...

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Section: Evaluation Of Ex-vivo Mucoadhesion Time and Mucoadhesion Strmentioning

confidence: 99%

Okra-Thioglycolic Acid Conjugate—Synthesis, Characterization, and Evaluation as a Mucoadhesive Polymer

Naveen¹,

Gopinath

Kurakula

2020

Processes

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“…This property can further increase its residence time in the stomach. This mucoadhesive force is less than that detected in the formulation with one of the most frequently used hydrophilic polymers [13,41]. On the other hand, the PEG content of our formulation may contribute to a prolonged gastric residence time.…”

Section: Discussionmentioning

confidence: 64%

Preparation of Acyclovir-Containing Solid Foam by Ultrasonic Batch Technology

et al. 2021

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In recent years, the application of solid foams has become widespread. Solid foams are not only used in the aerospace field but also in everyday life. Although foams are promising dosage forms in the pharmaceutical industry, their usage is not prevalent due to decreased stability of the solid foam structure. These special dosage forms can result in increased bioavailability of drugs. Low-density floating formulations can also increase the gastric residence time of drugs; therefore, drug release will be sustained. Our aim was to produce a stable floating formula by foaming. Matrix components, PEG 4000 and stearic acid type 50, were selected with the criteria of low gastric irritation, a melting range below 70 °C, and well-known use in oral drug formulations. This matrix was melted at 54 °C in order to produce a dispersion of active substance and was foamed by different gases at atmospheric pressure using an ultrasonic homogenizer. The density of the molded solid foam was studied by the pycnometer method, and its structure was investigated by SEM and micro-CT. The prolonged drug release and mucoadhesive properties were proved in a pH 1.2 buffer. According to our experiments, a stable foam could be produced by rapid homogenization (less than 1 min) without any surfactant material.

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“…In vivo gastroretentive study was performed to confirm the retention of the BaSO 4 -loaded samples in the stomach, for the suitability of the technology for drug development. BaSO 4 is a contrast agent that is used in clinical imaging area with high-density and high X-ray absorbing properties which make it suitable to determine the intracorporeal location of the compositions [23,24].…”

Section: In Vivo Gastroretentive Studymentioning

confidence: 99%

“…BaSO 4 is a contrast agent that is used in clinical imaging area with high-density and high X-ray absorbing properties which make it suitable to determine the intracorporeal location of the compositions [23,24]. Figure 8 (a) shows that the formulation appeared in a well-defined way in the stomach 30 min after the administration.…”

Section: In Vivo Gastroretentive Studymentioning

confidence: 99%

Process Optimization for the Continuous Production of a Gastroretentive Dosage Form Based on Melt Foaming

et al. 2021

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Several drugs have poor oral bioavailability due to low or incomplete absorption which is affected by various effects as pH, motility of GI, and enzyme activity. The gastroretentive drug delivery systems are able to deal with these problems by prolonging the gastric residence time, while increasing the therapeutic efficacy of drugs. Previously, we developed a novel technology to foam hot and molten dispersions on atmospheric pressure by a batch-type in-house apparatus. Our aim was to upgrade this technology by a new continuous lab-scale apparatus and confirm that our formulations are gastroretentive. At first, we designed and built the apparatus and continuous production was optimized using a Box–Behnken experimental design. Then, we formulated barium sulfate-loaded samples with the optimal production parameters, which was suitable for in vivo imaging analysis. In vitro study proved the low density, namely 507 mg/cm3, and the microCT record showed high porosity with 40 μm average size of bubbles in the molten suspension. The BaSO4-loaded samples showed hard structure at room temperature and during the wetting test, the complete wetting was detected after 120 min. During the in vivo study, the X-ray taken showed the retention of the formulation in the rat stomach after 2 h. We can conclude that with our device low-density floating formulations were prepared with prolonged gastric residence time. This study provides a promising platform for marketed active ingredients with low bioavailability.

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Formulation and characterization of gastroretentive discs containing famotidine

Cited by 8 publications

References 29 publications

Okra-Thioglycolic Acid Conjugate—Synthesis, Characterization, and Evaluation as a Mucoadhesive Polymer

Okra-Thioglycolic Acid Conjugate—Synthesis, Characterization, and Evaluation as a Mucoadhesive Polymer

Preparation of Acyclovir-Containing Solid Foam by Ultrasonic Batch Technology

Process Optimization for the Continuous Production of a Gastroretentive Dosage Form Based on Melt Foaming

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