An Overview on Polymethacrylate Polymers in Gastroretentive Dosage Forms

Gupta, Pravin; Kumar, Manish; Sachan, Narsingh

doi:10.2174/1874844901502010031

Cited by 19 publications

(7 citation statements)

References 24 publications

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“…They are applied as film coat, enteric coat, sustaining the drug release and as a tablet matrix. Similar kind of results has been demonstrated for different drugs using combination with polymethyl methacrylate which is reported in a review by Gupta et al [26]. Hydroxyethyl Cellulose (HEC) can be useful in control of time-related symptoms which need timecontrolled or site-specific delivery in the gastrointestinal tract.…”

Section: In -Vitro Dissolution Studysupporting

confidence: 73%

Hydroxyl Ethyl Cellulose HHX and Polymethyl Methacrylate Based Site Specific Floating Delivery of Prochlorperazine Maleate

Jagdale¹,

Randhave²

2016

PHARMSCI

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Background:Prochlorperazine maleate is a phenothiazine antipsychotic used principally in the treatment of nausea, vomiting and vertigo. Biological half- life of the drug is about 6 to 8 hrs and oral dose is 5 or 10 mg thrice or four times a day. The mean absolute bioavailability for drug is 12.5%. Due to the solubility of drug in acidic pH, it is mainly absorbed from stomach.Objective:Site specific oral floating delivery of prochlorperazine maleate will prolong the gastric retention time, increases the drug bioavailability, reduces frequency of administration and can result in better patient compliance.Method:The tablets were prepared by direct compression technique. Floating drug delivery was developed using gas forming agent and release retarding agenti.e.hydroxyethyl cellulose HHX (Natrosol HHX) and polymethyl methacrylate (PMMA). 32full factorial design was used for optimization. Prepared tablets were evaluated for pre and post compression parameters.Results:From the factorial batches it was observed that formulation containing 68.5% of hydroxyethyl cellulose HHX and 15% of polymethyl methacrylate had shown a drug release of 91.56 ± 2.7% with floating upto 10 hrs following Korsmeyer Peppas release kinetics.Conclusion:In- vivoplacebo X-ray study for optimized batch F6 had shown good gastroretention ability for 6 ± 0.5 hrs.In- vitroandin- vivostudy confirmed the site specific floating delivery for drug.

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Section: In -Vitro Dissolution Studysupporting

confidence: 73%

Hydroxyl Ethyl Cellulose HHX and Polymethyl Methacrylate Based Site Specific Floating Delivery of Prochlorperazine Maleate

Jagdale¹,

Randhave²

2016

PHARMSCI

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“…As illustrated in Figure 3(A) , the endothermic peak of untreated drug was obtained as 110.38 °C, which was broadened and shifted to 103.82 °C in PM. This might be because PEL in PM was miscible with polymer in the molten state (Paradkar et al., 2004 ; Gupta et al., 2015 ). In SRSD (F6) formulation, endothermic drug peak was disappeared, implying the change of drug crystallinity to amorphous state.…”

Section: Resultsmentioning

confidence: 99%

Sustained-release solid dispersion of pelubiprofen using the blended mixture of aminoclay and pH independent polymers: preparation and in vitro/in vivo characterization

et al. 2017

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The present study aimed to develop the sustained-release oral dosage form of pelubiprofen (PEL) by using the blended mixture of 3-aminopropyl functionalized-magnesium phyllosilicate (aminoclay) and pH-independent polymers. The sustained-release solid dispersion (SRSD) was prepared by the solvent evaporation method and the optimal composition of SRSD was determined as the weight ratio of drug: EudragitV R RL PO: EudragitV R RS PO of 1:1:2 in the presence of 1% of aminoclay (SRSD(F6)). The dissolution profiles of SRSD(F6) were examined at different pHs and in the simulated intestinal fluids. The drug release from SRSD(F6) was limited at pH 1.2 and gradually increased at pH 6.8, resulting in the best fit to Higuchi equation. The sustained drug release from SRSD(F6) was also maintained in simulated intestinal fluid at fasted-state (FaSSIF) and fed-state (FeSSIF). The structural characteristics of SRSD(F6) were examined by using powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR), indicating the change of drug crystallinity to an amorphous form. After oral administration in rats, SRSD(F6) exhibited the prolonged drug exposure in plasma. For both PEL and PEL-transOH (active metabolite), once a day dosing of SRSD(F6) achieved oral exposure (AUC) comparable to those from the multiple dosing (3 times a day) of untreated drug. In addition, the in vivo absorption of SRSD(F6) was well-correlated with the in vitro dissolution data, establishing a good level A in vitro/in vivo correlation. These results suggest that SRSD(F6) should be promising for the sustained-release of PEL, thereby reducing the dosing frequency.ARTICLE HISTORY

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“…The dissolution of this system depends on the thickness and solubility of polymers in water. 51 Faster or slower solubility will cause the drug to be released into the system uncontrollably and can reduce the effect of the drug.…”

Section: Solubilitymentioning

confidence: 99%

“…It can float on the surface of gastric fluid without affecting the gastric emptying rate because of its low density. 2 The GRDDS is a sustained drug delivery system that can keep the drug for a longer time. The advantages of GRDDS include increasing bioavailability, increasing solubility in high pH, control of therapy level to reduce fluctuation, and prolonging half-time to reduce the frequency of drug administration.…”

mentioning

confidence: 99%

The Use of Natural and Synthetic Polymers in the Formulation of Gastro retentive Drug Delivery System

Ainurofi¹,

Daryati²,

Murtadla³

et al. 2023

IJDDT

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The gastric emptying process drastically reduces the bioavailability of drugs that target the stomach for their action. A gastro retentive drug delivery system (GRDDS) becomes a solution to retain drugs in the stomach and release drugs from the formulation system within a certain period. The polymer used in the GRDDS formulation is the essential excipient that can retain the drugs in the stomach. Several ways for GRDDS to maintain its existence in the stomach are using some systems, such as mucoadhesive, low-density, high-density, swellable, eff ervescent, and expandable systems. A polymer is a macromolecular substance with a long repeating chain consisting of natural and synthetic polymers, each with diff erent potentials. It is considered for its ability to regulate drug release, good fl ow properties, can improve drug dissolution to improve bioavailability and stability during processing in the body. Combining natural and synthetic polymers is often carried out to obtain advantages and cover the existing polymer’s disadvantages. Polymers can release drugs using three diff erent mechanisms, i.e., diff usion, degradation, and expansion. These techniques are often chosen for the formulation of GRDDS because of their more fl exible system and fi t for almost all types of GRDDS. The polymer used in the GRDDS system is chosen from its physicochemical properties and the number of fl oating times, drug release rate, viscosity, fl oating lag times, bioavailability, and solubility.

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An Overview on Polymethacrylate Polymers in Gastroretentive Dosage Forms

Cited by 19 publications

References 24 publications

Hydroxyl Ethyl Cellulose HHX and Polymethyl Methacrylate Based Site Specific Floating Delivery of Prochlorperazine Maleate

Hydroxyl Ethyl Cellulose HHX and Polymethyl Methacrylate Based Site Specific Floating Delivery of Prochlorperazine Maleate

Sustained-release solid dispersion of pelubiprofen using the blended mixture of aminoclay and pH independent polymers: preparation and in vitro/in vivo characterization

The Use of Natural and Synthetic Polymers in the Formulation of Gastro retentive Drug Delivery System

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