Challenges of Dissolution Methods Development for Soft Gelatin Capsules

Damian, F.; Harati, Mohammad; Schwartzenhauer, Jeff; Cauwenberghe, Owen Van; Wettig, Shawn

doi:10.3390/pharmaceutics13020214

Cited by 22 publications

(12 citation statements)

References 148 publications

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“…This is due to the influence of the addition of glycerol as a plasticizer. The volume of glycerol being too high causes the distribution of the constituent components to be uneven [ 28 ]. This indicates more NCC content has the ability to increase the hydrogen bonds formed between the same polymers, thereby requiring more energy to break the bonds but having the ability to break them at low strains [ 27 ].…”

Section: Resultsmentioning

confidence: 99%

Sugarcane Bagasse as the Source of Nanocrystalline Cellulose for Gelatin-Free Capsule Shell

Sabara

Mutmainnah

Kalsum

et al. 2022

International Journal of Biomaterials

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Gelatin-free capsules are possibly produced through an innovation which involves utilizing environmentally friendly materials derived from plants such as bagasse which are produced into nanocrystalline cellulose (NCC). This research was conducted to report the extraction and characterization of NCC from the abundant industrial plantation waste of sugarcane and its application as the base material for gelatin-free capsule shell material. The process involved using different concentrations of NCC at 1%, 2%, 4%, and 7% (in wt. %) with the addition of 1% hydroxypropyl methylcellulose (HPMC) (in wt. %) and 1% carbopol (in wt. %). Moreover, the NCC capsules obtained from sugarcane bagasse were tested for moisture content, tensile strength, elongation, solubility, and pH. The results showed that sugarcane bagasse contains 40–50% cellulose, 6.15%–9.5% moisture content which indicates they are potentially better in terms of storage, 7.25–7.85 pH, and 0.05–0.136 MPa gel strength, and the elongation value ranges from 7.19 to 87.51%. These values were discovered to have satisfied the standard requirements as indicated by the optimal concentration of 4% NCC +1% HPMC, which is in line with the Japanese Industrial Standard (JIS), thereby leading to the consideration of the material safe to be used as raw material in making capsule shells.

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Section: Resultsmentioning

confidence: 99%

Sugarcane Bagasse as the Source of Nanocrystalline Cellulose for Gelatin-Free Capsule Shell

Sabara

Mutmainnah

Kalsum

et al. 2022

International Journal of Biomaterials

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“…Also, soft gels have been reported to improve the extent of absorption as well as to significantly reduce plasma variability. Preparations of liquid-filled soft gel have further proven beneficial to oxidative or hydrolytic degradable drugs [14,15].…”

Section: Methodsmentioning

confidence: 99%

“…The washout period between the treatments was one week. In contrast to hard capsules consisting of "two-pieces", a soft gel capsule represents a one-piece/unitary package containing a liquid, a suspension, or a semisolid-imbedded between gelatin outer layers [14,15]. Such soft gel delivery systems have many advantages over other traditional dosage forms e.g., tablets and/or hard capsules, as aforementioned.…”

Section: Subjects and Study Designmentioning

confidence: 99%

Quercetin LipoMicel—A Novel Delivery System to Enhance Bioavailability of Quercetin

et al. 2021

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BACKGROUND: Quercetin, a flavonoid found in plant-based foods, has a range of biological activities that may be beneficial for human health. The pharmacokinetic profile of quercetin remains, however, a limiting factor for its use as a nutritional supplement. Quercetin LipoMicel ® -a novel delivery system encapsulating quercetin into a liquid micelle matrix-has been designed to address the low bioavailability issue associated with non-conjugated forms by improving the absorption of quercetin. OBJECTIVE:The purpose of this study was to evaluate the solubility and gastrointestinal absorption of quercetin in a novel Quercetin LipoMicel delivery system in healthy adult volunteers by comparing it with free quercetin and another commercial quercetin product. Several pharmacokinetic parameters were compared between these three formulations. METHODS:Twelve healthy adult male and female volunteers aged between 21 and 65, with BMIs under 30, participated in a non-blinded, crossover bioavailability study conducted with three quercetin products. Each treatment contained a total dose of 500 mg quercetin. Capillary whole blood samples from participants were collected serially at intervals from 0-24 hours. Quercetin concentrations were detected and measured by ultra-performance liquid chromatography (UHPLC) coupled to a Thermo QExactive Orbitrap Mass Spectrometer. Solubility of quercetin in water and simulated gastrointestinal media was determined by UHPLC. RESULTS:Oral absorption of quercetin was significantly enhanced with the LipoMicel delivery system compared to free quercetin. Improvements in in vitro gastric stability and intestinal solubility were observed with LipoMicel, leading to significantly higher blood concentration and enhanced duration of a stable concentration of quercetin in the body. Compared to free quercetin, 8-and 9-fold increases in AUC and Cmax were attained with the LipoMicel delivery system, and 10-fold higher quercetin plasma concentrations detected at 12 hours after administration. CONCLUSIONS:Quercetin LipoMicel represents an efficient delivery system for augmenting the bioavailability of quercetin in vivo. Significantly higher blood concentrations and a sustained release of quercetin over the study period was achieved following the administration of quercetin via the LipoMicel technology. Optimization in the in vivo bioavailability of quercetin may promote its salutary effects.

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“…There have been various effective approaches used to improve the solubility, dissolution, and bioavailability of these drugs [2][3][4][5][6][7][8]. Some of the most prevalent approaches are reduction in particle size (micronization, nanosizing) [9], cyclodextrin drug complexation [10,11], lipid based formation [12], using of surfactant [13,14], formation of a salt with alkalizing agent [15,16], and using different alkalizers in SD to change the pH of the microenvironment [17]. Among these, the incorporation of alkalizing agents in an SD has been identified as an effective method for increasing the dissolution rate of water-insoluble drugs [18].…”

Section: Introductionmentioning

confidence: 99%

A Promising Ternary Solid Dispersion of Aceclofenac Containing Tablet with Enhanced Dissolution, and Potentiated Anti-inflammatory Efficacy

Ebraheem¹,

El-Gawad

Girgis

2022

J. Pharm. Res. Int.

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The major objective of the current study is to implement a plan to enhance the dissolution rate and oral bioavailability of a poorly water-soluble aceclofenac. The drug is classified according to the biopharmaceutical classification system as class II drug. Amorphous alkalinized aceclofenac solid dispersion was formulated as a ternary mixture. This mixture was prepared by introducing polymeric carriers [polyvinylpyrrolidone, Hydroxy propyl beta cyclodextrin or Polyethylene glycol] and an alkalizer (Na2CO3) by applying the solvent evaporation method. Optimum formulations were compressed into tablets that were subjected to in-vitro studies compared to the market product Bristaflam and free drug containing one. Finally, tablets were assessed for stability studies and carrageenan-induced rat paw edema treatment to evaluate potentiated anti-inflammatory efficacy. Results showed that optimum amorphous alkalinized aceclofenac solid dispersion formulations containing polyvinylpyrrolidone K30 or Hydroxy propyl beta cyclodextrin in 1:5 ratio have significant in-vitro dissolution improvement (>90% in 10 min) compared to untreated aceclofenac. Solid-state characterization emphasized the conversion of the crystalline drug into the amorphous form with no drug−polymers interactions. Stability and dissolution studies ensured that tablets containing amorphous alkalinized solid dispersions were stable with strikingly improving dissolution behavior compared to Bristaflam or free drug containing tablets. Moreover, regarding anti-inflammatory activity against carrageenan induced paw edema, and histopathological examination, we concluded that amorphous alkalinized solid dispersions containing tablets are a promising approach to enhance the dissolution rate and oral bioavailability and hence anti-inflammatory efficacy of aceclofenac.

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Challenges of Dissolution Methods Development for Soft Gelatin Capsules

Cited by 22 publications

References 148 publications

Sugarcane Bagasse as the Source of Nanocrystalline Cellulose for Gelatin-Free Capsule Shell

Sugarcane Bagasse as the Source of Nanocrystalline Cellulose for Gelatin-Free Capsule Shell

Quercetin LipoMicel—A Novel Delivery System to Enhance Bioavailability of Quercetin

A Promising Ternary Solid Dispersion of Aceclofenac Containing Tablet with Enhanced Dissolution, and Potentiated Anti-inflammatory Efficacy

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