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Journal of Pharmacy & Pharmaceutical... 2010Hydroxypropyl methylcellulose (HPMC) is employed for a wide variety of pharmaceutical and food preparations. Its applications as viscolizing agent (thickening agent),... (Review)
Review
Hydroxypropyl methylcellulose (HPMC) is employed for a wide variety of pharmaceutical and food preparations. Its applications as viscolizing agent (thickening agent), coating polymer, bioadhesive, in solid dispersion to enhance solubility, binder in the process of granulation and in modified release formulations have been well documented. One other notable use is in the production of capsule shells, replacing the animal derived gelatin in conventional two-piece capsules. The aim of this review is to systemically survey published literature on the HPMC use in capsule shells and resolve questions regarding their suitability as a replacement for hard gelatin capsules. Future refinements in the production and filling of HPMC capsule shells and improvement in their in vivo/in vitro dissolution would ensure their superiority over hard gelatin capsules.
Topics: Administration, Oral; Capsules; Drug Compounding; Excipients; Gelatin; Hardness; Humans; Hypromellose Derivatives; Methylcellulose; Pharmaceutical Preparations; Polymers; Solubility; Water
PubMed: 21092714
DOI: 10.18433/j3k881 -
International Journal of Molecular... 2012The effect of dietary feeding of hydroxyethyl methylcellulose (HEMC) and hydroxypropyl methylcellulose (HPMC) on the glucose metabolism and antioxidative status in mice...
The effect of dietary feeding of hydroxyethyl methylcellulose (HEMC) and hydroxypropyl methylcellulose (HPMC) on the glucose metabolism and antioxidative status in mice under high fat diet conditions was investigated. The mice were randomly divided and given experimental diets for six weeks: normal control (NC group), high fat (HF group), and high fat supplemented with either HEMC (HF+HEMC group) or HPMC (HF+HPMC group). At the end of the experimental period, the HF group exhibited markedly higher blood glucose and insulin levels as well as a higher erythrocyte lipid peroxidation rate relative to the control group. However, diet supplementation of HEMC and HPMC was found to counteract the high fat-induced hyperglycemia and oxidative stress via regulation of antioxidant and hepatic glucose-regulating enzyme activities. These findings illustrate that HEMC and HPMC were similarly effective in improving the glucose metabolism and antioxidant defense system in high fat-fed mice and they may be beneficial as functional biomaterials in the development of therapeutic agents against high fat dietinduced hyperglycemia and oxidative stress.
Topics: Animals; Antioxidants; Blood Glucose; Diet, High-Fat; Dietary Supplements; Glucose; Glycogen; Hypoglycemic Agents; Hypromellose Derivatives; Insulin; Insulin Resistance; Lipid Metabolism; Lipid Peroxidation; Liver; Male; Methylcellulose; Mice; Mice, Inbred C57BL; Oxidative Stress; Weight Gain
PubMed: 22489179
DOI: 10.3390/ijms13033738 -
Molecules (Basel, Switzerland) Mar 2022The present study aimed to develop a local dental nanoemulgel formulation of oil (NSO) for the treatment of periodontal diseases. NSO purchased from a local market was...
The present study aimed to develop a local dental nanoemulgel formulation of oil (NSO) for the treatment of periodontal diseases. NSO purchased from a local market was characterized using a GC-MS technique. A nanoemulsion containing NSO was prepared and incorporated into a methylcellulose gel base to develop the nanoemulgel formulation. The developed formulation was optimized using a Box-Behnken statistical design (quadratic model) with 17 runs. The effects of independent factors, such as water, oil, and polymer concentrations, were studied on two dependent responses, pH and viscosity. The optimized formulation was further evaluated for droplet size, drug release, stability, and antimicrobial efficacy. The developed formulation had a pH of 7.37, viscosity of 2343 cp, and droplet size of 342 ± 36.6 nm. Sustained release of the drug from the gel for up to 8 h was observed, which followed Higuchi release kinetics with non-Fickian diffusion. The developed nanoemulgel formulation showed improved antimicrobial activity compared to the plain NSO. Given the increasing emergence of periodontal diseases and antimicrobial resistance, an effective formulation based on a natural antibacterial agent is warranted as a dental therapeutic agent.
Topics: Emulsions; Methylcellulose; Oral Health; Plant Oils
PubMed: 35335159
DOI: 10.3390/molecules27061796 -
International Journal of Nanomedicine 2023We designed a 0.05% mometasone furoate (MF) nanocrystal dispersion and investigated whether the application of MF nanocrystals in nasal formulations enhanced local...
PURPOSE
We designed a 0.05% mometasone furoate (MF) nanocrystal dispersion and investigated whether the application of MF nanocrystals in nasal formulations enhanced local absorption compared to traditional nasal MF formulations (CA-MF).
METHODS
MF nanocrystal dispersions (MF-NPs) were prepared by bead milling MF microcrystal dispersions (MF-MPs) consisting of MF, 2-hydroxypropyl-β-cyclodextrin, methylcellulose, and purified water. Pluronic F-127 combined with methylcellulose, Pluronic F-68, or carbopol was used as a base for in situ gelation (thickener). MF concentrations were measured using high-performance liquid chromatography, and nasal absorption of MF was evaluated in 6 week-old male Institute of Cancer Research (ICR) mice.
RESULTS
The particle size range of MF prepared with the bead mill treatment was 80-200 nm, and the nanoparticles increased the local absorption of MF, which was higher than that of CA-MF and MF-MPs. In addition, unlike the results obtained in the small intestine and corneal tissue, the high absorption of nanocrystalline MF in the nasal mucosa was related to a pathway that was not derived from energy-dependent endocytosis. Moreover, the application of the in situ gelling system attenuated the local absorption of MF-NPs, owing to a decrease in drug diffusion in the dispersions.
CONCLUSION
We found that nanoparticulation of MF enhances local intranasal absorption, and nasal bioavailability is higher than that of CA-MF. In addition, we demonstrate that viscosity regulation is an important factor in the design of nasal formulations based on MF nanocrystals. These findings provide insights for the design of novel nanomedicines with enhanced nasal bioavailability.
Topics: Male; Animals; Mice; Mometasone Furoate; Nasal Absorption; Nasal Mucosa; Methylcellulose
PubMed: 37841023
DOI: 10.2147/IJN.S430952 -
The British Journal of Ophthalmology Apr 1983Methylcellulose has been used since 1976 to prevent damage to the corneal endothelium during operations for implantation of intraocular lenses. Originally one drop of a...
Methylcellulose has been used since 1976 to prevent damage to the corneal endothelium during operations for implantation of intraocular lenses. Originally one drop of a 1% solution was placed on the artificial lens just before its insertion. Later the anterior chamber was completely filled with a 2% solution of methylcellulose before implantation. In this way it is possible to maintain a space between the cornea and iris even if vitreous pressure is present and to operate without risk to the corneal endothelium. This paper demonstrates the safety of the intraocular use of methylcellulose on the basis of over 400 operations. The substance is cheap, universally available, and can be easily prepared for intraocular use.
Topics: Corneal Diseases; Endothelium; Humans; Intraocular Pressure; Intraoperative Complications; Lenses, Intraocular; Methylcellulose
PubMed: 6830744
DOI: 10.1136/bjo.67.4.259 -
Carbohydrate Polymers Dec 2017The objective of this study was to develop a new approach for fabrication of zero order release of active pharmaceutical ingredients (APIs) using hot-melt extrusion...
The objective of this study was to develop a new approach for fabrication of zero order release of active pharmaceutical ingredients (APIs) using hot-melt extrusion (HME) and 3D printing technology to generate tablets with specific 3D structures. By correlating the geometry of the 3D printed tablets with their dissolution and drug release rates, mathematical models that have been developed to describe drug release mechanisms were also studied. Acetaminophen was used as a model drug, and Benecel™ hydroxypropyl methylcellulose (HPMC) E5 and Soluplus were used to formulate nine fuse depositional 3D-printed tablets with different inner core fill densities and outside shell thicknesses. This work reports the successful fabrication of solid-dispersion filaments with an API dispersed in HPMC based matrix via HME technology, and the production of zero order controlled release tablets with different 3D structures (tablets #3, 5, 6, and 9) using a 3D printer.
Topics: Delayed-Action Preparations; Hypromellose Derivatives; Methylcellulose; Printing, Three-Dimensional; Solubility; Tablets; Technology, Pharmaceutical
PubMed: 28962795
DOI: 10.1016/j.carbpol.2017.08.058 -
Acta Obstetricia Et Gynecologica... 2009To evaluate the efficacy of methylcellulose (Citrucel) and loperamide (Imodium) in managing fecal incontinence by comparing cure rates with expectant management.
OBJECTIVE
To evaluate the efficacy of methylcellulose (Citrucel) and loperamide (Imodium) in managing fecal incontinence by comparing cure rates with expectant management.
DESIGN
Prospective controlled study.
SETTING
Urogynecology clinic in a university hospital.
POPULATION
Sixty-nine women with fecal incontinence.
METHODS
All incontinent women received one heaping tablespoon of methylcellulose twice a day, which was increased to two heaping tablespoons twice a day as needed. If the incontinence persisted after taking the maximum dose of methylcellulose for two weeks, loperamide, one capsule twice a day was added, which was increased to two capsules three times a day as needed. If both fecal urgency and incontinence resolved, the therapy was continued for a three-month treatment period. Women, who declined the proposed treatment and did not undergo any other therapy during the subsequent eight weeks, served as controls. A subject or control was considered cured if she stated that her incontinence was cured, had zero Pescatori incontinence point, resolution of fecal urgency, and her incontinence did not affect her emotional, social, occupational, and physical functions during the three-month treatment or eight-week observation period.
MAIN OUTCOME MEASURES
Difference in the cure rate between subjects and controls. Results. Fifty-nine subjects were treated with methylcellulose. Forty (68%) also required loperamide. Ten women served as controls. Women treated with methylcellulose and loperamide had a higher cure rate than those managed expectantly (46% vs. 0%, p<0.01).
CONCLUSION
Methylcellulose and loperamide are an effective treatment for fecal incontinence, at least on a short-term basis.
Topics: Administration, Oral; Analysis of Variance; Antidiarrheals; Fecal Incontinence; Female; Humans; Loperamide; Methylcellulose; Middle Aged; Prospective Studies; Treatment Outcome
PubMed: 19452328
DOI: 10.1080/00016340902993320 -
International Journal of Pharmaceutics Apr 2022The purpose of this study was to develop a deterministic permeation model (DPM) that predicts the in vitro release profile of an active ingredient (API) embedded in...
The purpose of this study was to develop a deterministic permeation model (DPM) that predicts the in vitro release profile of an active ingredient (API) embedded in hydroxypropyl-methylcellulose (HPMC) matrix tablets based on Raman spectra. So far in the literature, such mechanistic models were utilized only for formulation optimization (off-line dissolution prediction), while the real-time prediction of dissolution profiles based on Process Analytical Technology (PAT) data was performed by empirical methods such as Partial Least Squares (PLS) regression. Our work represents a novel conceptual approach that utilizes a mechanistic model to predict dissolution profiles based on data yielded by PAT tools. Tablets containing various API- and HPMC-amounts were produced using different compression pressures according to a 3 full factorial design, their Raman spectra were recorded before dissolution testing. The DPM was constructed using one-third of the measured dissolution profiles and is presented as a system of differential equations together with its analytical solution. The parameters of DPM were estimated by the training data set containing the spectroscopically determined API- and HPMC- amounts and the tableting pressures used, then the release profiles of the remaining two-thirds of the tablets were predicted. The Raman spectra-based predictions of DPM were compared with predictions of an Artificial Neural Network (ANN). It was found that the two methods yield similar results, however, the mechanistic approach has the benefit of requiring a lower amount of training samples. Although the model is based on a remarkable simplification of reality, it facilitates a deeper understanding of the behavior of the formulation. The DPM could improve our understanding of the effect of HPMC and tableting pressures on the release kinetics of the HPMC matrix tablets and participate in the development of PAT-based new surrogate dissolution methods for Real-Time Release testing (RTRt).
Topics: Delayed-Action Preparations; Hypromellose Derivatives; Methylcellulose; Solubility; Tablets
PubMed: 35231548
DOI: 10.1016/j.ijpharm.2022.121624 -
Chemical & Pharmaceutical Bulletin 2019A system for releasing a fragrance, citral (CR) over an extended period of time using three types of enteric capsules is reported. The L- and M-type capsules released CR...
A system for releasing a fragrance, citral (CR) over an extended period of time using three types of enteric capsules is reported. The L- and M-type capsules released CR into media with a pH above 6, while the H-type capsule released CR at a pH above 7. The pH of the releasing medium was controlled by sodium borate (SB), i.e., by adding SB-methylcellulose (MC) prepared in different weight ratios (SB-MC 1 : 2, 1 : 1 and 2 : 1) to tablets and by compressing them at different pressures. The tablet containing a large amount of SB and that was pressed at higher pressures permitted the pH of the releasing medium to be changed from 5 to 9, at 4-5 h after the addition of SB to the tablets, while negligible changes were observed for tablets containing low amounts of SB and which were compressed at lower pressures. Reflecting these pH changes, CR was released after different periods of time when SB-MC tablets and capsules containing CR were simultaneously added to the releasing medium. When enteric capsules containing CR and the pH adjusting tablets were simultaneously added to a benzyl acetate (BA) solution, BA was released at a constant rate, while CR was released for different periods of time depending on the type of capsule used. The results suggest that fragrances could be released over different time frames by using enteric capsules and pH adjusting agents, for example, the release of fragrances with sedative effects at night time and with stimulating effects in the morning.
Topics: Acyclic Monoterpenes; Borates; Capsules; Delayed-Action Preparations; Drug Compounding; Drug Liberation; Hydrogen-Ion Concentration; Methylcellulose; Monoterpenes; Odorants
PubMed: 31061376
DOI: 10.1248/cpb.c18-00898 -
International Journal of Biological... Nov 2021The properties of edible films derived from corn starch (CS) and methylcellulose (MC) supplemented with fireweed extract (FE; 0.0125-0.05% w/w) were analyzed. Due to... (Comparative Study)
Comparative Study
The properties of edible films derived from corn starch (CS) and methylcellulose (MC) supplemented with fireweed extract (FE; 0.0125-0.05% w/w) were analyzed. Due to their more crystalline structure, the MC films were significantly stronger (~26 MPa) than the CS films (~4 MPa). In turn, CS produced films with lower water vapor permeability (WVP, 50.12-51.74 vs. 56.52-59.10 g mm m d kPa). The hydrothermally-disrupted starch granules contributed to high roughness and opacity of the CS films. The FE-supplemented films exhibited an intensive yellow color and improved the UV-absorbing effect. FE delayed starch retrogradation, as indicated by the reduced crystallinity and slightly improved transparency of the CS films. Incorporation of FE significantly enhanced the released radical scavenging activity (RSA) of the films, while did not affect the WVP and mechanical properties. Due to better FE-trapping capacity, the CS-based films exhibited lower antioxidant activity (RSA = 2.21-19.75%) as compared to the MC counterparts (RSA = 4.87-38.31%).
Topics: Antioxidants; Bassia scoparia; Chemical Phenomena; Edible Films; Free Radical Scavengers; Methylcellulose; Optical Phenomena; Permeability; Phenols; Plant Extracts; Starch; Steam; X-Ray Diffraction
PubMed: 34537300
DOI: 10.1016/j.ijbiomac.2021.09.079