Enhancement of Loperamide Dissolution Rate by Liquisolid Compact Technique

Venkateswarlu, K.; J, Preethi; Chandrasekhar, K. B.

doi:10.15171/apb.2016.050

Cited by 16 publications

(8 citation statements)

References 17 publications

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“…That is soft gelatin elastic capsules containing solutions of such medications demonstrate higher bioavailability when compared to conventional oral solid dosage forms. A similar principle underlies the mechanism of drug delivery from liquisolid compacts [3].…”

Section: Introductionmentioning

confidence: 82%

See 1 more Smart Citation

Neusilin based liquisolid compacts of albendazole: Design, development, characterization and in vitro anthelmintic activity

Shete¹,

Salunkhe²,

Yadav³

et al. 2019

jrp

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The present investigation deals with enhancement of dissolution rate of high dose drug albendazole (ABZ) using liquisolid compacts. Study of precompression characteristics, influence of excipients on drug release characteristics and to compare drug release profile of the formulated liquisolid compacts with the directly compressible laboratory made formulation. Liquisolid compacts were prepared by using three by twofactorial designs and evaluated for differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), in vitro nthelmintic, in vitro antifungal study and in vitro dissolution study. There was improvement in the dissolution rate and solubility was attributed to decreased melting point and crystallinity of albendazole. In vitro anthelmintic and antifungal activities of neusilin based liquisolid compacts were more than pure albendazole. The drug content of liquisolid compacts was not affected when stored at room temperature for a period of 3 months. This study also provided evidence that it is possible to load high amounts of drug into liquisolid compacts due to the neusilin allows higher liquid adsorption capacities. Neusilin based technique is useful for the preparation of liquisolid compacts of high dose drug like albendazole with enhancement in dissolution rate

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Section: Introductionmentioning

confidence: 82%

“…Intravenous injection leads 'per definition' to a 100% bioavailability, but this technology is too economic. In generic development cost of formulation will be high [3].…”

Section: Introductionmentioning

confidence: 99%

Neusilin based liquisolid compacts of albendazole: Design, development, characterization and in vitro anthelmintic activity

Shete¹,

Salunkhe²,

Yadav³

et al. 2019

jrp

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“…Another critical factor to consider is the solubility of the active ingredients in the disintegration medium. The solubility of pilocarpine HCl (the active ingredient of freeze-dried pilocarpine HCl) in water is reported to be 100 mg/mL in comparison to loperamide HCl (the active ingredient of Imodium Instant) which is classified as an active with low solubility profile of 1.02 mg/m ( 45 ).…”

Section: Discussionmentioning

confidence: 99%

Digital Image Disintegration Analysis: a Novel Quality Control Method for Fast Disintegrating Tablets

Malallah

Rashid²,

et al. 2021

AAPS PharmSciTech

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Measuring tablet disintegration is essential for quality control purposes; however, no established method adequately accounts for the timeframe or small volumes of the medium associated with the dissipation process for fast disintegrating tablets (FDTs) in the mouth. We hypothesised that digital imaging to measure disintegration in a low volume of the medium might discriminate between different types of FTD formulation. A digital image disintegration analysis (DIDA) was designed to measure tablet disintegration in 0.05–0.7 mL of medium. A temperature-controlled black vessel was 3D-printed to match the dimensions of each tablet under investigation. An overhead camera recorded the mean grey value of the tablet as a measure of the percentage of the formulation which remained intact as a function of time. Imodium Instants, Nurofen Meltlets and a developmental freeze-dried pilocarpine formulation were investigated. The imaging approach proved effective in discriminating the disintegration of different tablets (p < 0.05). For example, 10 s after 0.7 mL of a saliva simulant was applied, 2.0 ± 0.3% of the new pilocarpine tablet remained, whereas at the same time point, 22 ± 9% of the Imodium Instants had not undergone disintegration (temperature within the vessel was 37 ± 0.5°C). Nurofen Meltlets were observed to swell and showed a percentage recovery of 120.7 ± 2.4% and 135.0 ± 6.1% when 0.05 mL and 0.7 mL volumes were used, respectively. Thus, the new digital image disintegration analysis, DIDA, reported here effectively evaluated fast disintegrating tablets and has the potential as a quality control method for such formulations.

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“…A liquisolid formulation allows an insoluble drug to be solubilized, almost molecularly dispersed in a solid dosage form, which greatly enhances the dissolution rate of solubility-limiting drugs due to ameliorative wetting property and dissolution surface area, hence the oral bioavailability. There a great number of poorly water-soluble drugs have been developed into liquisolid formulations in an attempt to enhance their dissolution and/or bioavailability, including Rosuvastatin [ 195 ], Aprepitant [ 217 ], Fenofibrate [ 218 ], Curcumin [ 198 ], Indomethacin [ 219 ], Griseofulvin [ 205 ], Loperamide [ 208 ], Ketoprofen [ 220 ], Olmesartan Medoxomil [ 207 ], Loratadine [ 221 ], Nimesulide [ 222 ], Furosemide [ 223 ], Lovastatin [ 224 ], Carbamazepine [ 203 ], Telmisartan [ 200 ], Valsartan [ 225 ], and Mosapride Citrate [ 196 ].…”

Section: Liquisolid Dispersion Techniquementioning

confidence: 99%

Pharmaceutical Dispersion Techniques for Dissolution and Bioavailability Enhancement of Poorly Water-Soluble Drugs

et al. 2018

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Over the past decades, a large number of drugs as well as drug candidates with poor dissolution characteristics have been witnessed, which invokes great interest in enabling formulation of these active ingredients. Poorly water-soluble drugs, especially biopharmaceutical classification system (BCS) II ones, are preferably designed as oral dosage forms if the dissolution limit can be broken through. Minimizing a drug’s size is an effective means to increase its dissolution and hence the bioavailability, which can be achieved by specialized dispersion techniques. This article reviews the most commonly used dispersion techniques for pharmaceutical processing that can practically enhance the dissolution and bioavailability of poorly water-soluble drugs. Major interests focus on solid dispersion, lipid-based dispersion (nanoencapsulation), and liquisolid dispersion (drug solubilized in a non-volatile solvent and dispersed in suitable solid excipients for tableting or capsulizing), covering the formulation development, preparative technique and potential applications for oral drug delivery. Otherwise, some other techniques that can increase the dispersibility of a drug such as co-precipitation, concomitant crystallization and inclusion complexation are also discussed. Various dispersion techniques provide a productive platform for addressing the formulation challenge of poorly water-soluble drugs. Solid dispersion and liquisolid dispersion are most likely to be successful in developing oral dosage forms. Lipid-based dispersion represents a promising approach to surmounting the bioavailability of low-permeable drugs, though the technique needs to traverse the obstacle from liquid to solid transformation. Novel dispersion techniques are highly encouraged to develop for formulation of poorly water-soluble drugs.

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Enhancement of Loperamide Dissolution Rate by Liquisolid Compact Technique

Cited by 16 publications

References 17 publications

Neusilin based liquisolid compacts of albendazole: Design, development, characterization and in vitro anthelmintic activity

Neusilin based liquisolid compacts of albendazole: Design, development, characterization and in vitro anthelmintic activity

Digital Image Disintegration Analysis: a Novel Quality Control Method for Fast Disintegrating Tablets

Pharmaceutical Dispersion Techniques for Dissolution and Bioavailability Enhancement of Poorly Water-Soluble Drugs

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