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PubMed1987

Plasma amino acid concentrations in normal adults administered aspartame in capsules or solution: lack of bioequivalence.

Some clinical studies require administration of test compounds in capsules to assure that the compound cannot be distinguished from a placebo. This raises the question of whether the pharmacokinetic responses produced by capsule administration are similar to values obtained when test compounds are ingested in solution. To test this, plasma phenylalanine and aspartate concentrations were compared in ten normal subjects ingesting 3 g aspartame in solution and in capsules in a balanced Latin square design. Peak plasma phenylalanine levels were significantly higher (191 +/- 65.4 v 117 +/- 39.5 mumol/L, mean +/- SD) and were reached significantly earlier (32 +/- 15 v 123 +/- 74 minutes) when aspartame was administered in solution than when it was administered in capsules. The area under the four-hour plasma phenylalanine concentration-time curve was significantly higher (15,340 +/- 4,820 v 8,465 +/- 3,356 mumol/L X min) when aspartame was ingested in solution. Administration in solution also produced a significantly higher ratio of plasma phenylalanine concentration to the sum of the plasma concentrations of the other large neutral amino acids (0.36 +/- 0.12 v 0.23 +/- 0.06). Similarly, peak plasma aspartate concentrations were significantly higher 26.2 +/- 16.3 v 10.4 +/- 5.0 mumol/L) and were reached significantly earlier (30 +/- 14 v 106 +/- 61.3 min) when aspartame was administered in solution. The data indicate different plasma phenylalanine and aspartate pharmacokinetics between solution and capsule administration of aspartame.

Adult↗

PubMed1996

Gellan in sustained release formulations: preparation of gel capsules and release studies.

The ability of gellan to form gels in the presence of calcium ions enabled us to prepare capsules by gelation of this polysaccharide around a core containing starch, calcium chloride and a model drug. Release from the dried capsules was studied in vitro by means of the rotating basket technique (USP) in different environmental conditions (distilled water, pH = 2.0, pH = 6.8) and the effects of the presence of increasing amounts of drug in the formulation were also investigated. The behaviour of the gellan capsules was compared with that of beads prepared with the same polysaccharide but containing different additives. Results obtained indicate that gellan is suitable for the formulation of sustained release capsules and that solvent uptake by the dried capsules is most likely the main factor capable of affecting the rate of delivery from the tested preparations.

Calcium Chloride↗

PubMed1994

Sensory properties of ankle joint capsule mechanoreceptors in acute monoarthritic chickens.

The physiological properties of joint capsule mechanoreceptors in the ankle joint of monoarthritic chickens were studied by recording the electrical activity from single sensory afferent nerve fibres dissected from the parafibular nerve. A monoarticular arthritis was induced by the intra-articular injection of Freund's complete adjuvant which resulted in an acute inflammatory condition and a very rapid onset of destructive cartilage damage. A detailed description of the anatomy in both the normal and arthritic joints was presented. It was considered that by day 3 after adjuvant injection there was a reproducible severe destructive arthropathy which was of value for investigating the physiological responses of the joint capsule receptors. The majority of receptor units identified were slowly adapting mechanoreceptors which were divided into groups III (CV: 2.5-20 m/sec) and IV (CV: < 2.5 m/sec) units. At least 3 significant differences were observed in the response characteristics of the joint capsule receptors from arthritic joints compared to those receptors found in normal joints. Firstly, there was an increase in receptive field size with 62% of group IV and 80% of group III units having large receptive fields. Secondly, there was a decrease in response threshold to mechanical stimulation of the joint capsule. Thirdly, a higher proportion of units responded to joint movement in the arthritic joints. These changes in sensitivity of the joint capsule receptors showed some similarities to adjuvant arthritis models in the rat and provide peripheral neural evidence for the possible painful consequences of the inflammatory arthropathies found in chicken.

Acute Disease↗

PubMed1992

Interaction of Klebsiella capsule type 7 with human polymorphonuclear leucocytes.

Klebsiella serotype K7 is found among the capsule types that are most prevalent in respiratory tract isolates. To evaluate the significance of the K7 antigen in bacteria-leucocyte interactions, K7-encapsulated Klebsiella pneumoniae strains and their non-capsulate mutants were investigated. The K7 isolates were compared to K2-capsulate strains and their respective K- derivatives. K7-capsulate bacteria were less hydrophilic, and more readily phagocytosed and killed by human polymorphonuclear leucocytes (PMNL) than K2 strains. Loss of the K7 antigen resulted in increased surface hydrophobicity but did not affect phagocytosis and killing, whereas loss of the K2 capsule caused greater susceptibility to the phagocytic and killing action of PMNL. Both the K7 and K2 antigen stimulated the extracellular release of lysozyme from neutrophils but not of myeloperoxidase, indicating degranulation of only secondary granules. All K- mutants induced the release of both lysozyme and myeloperoxidase. Our results suggest that, in contrast to the K2 antigen, the K7 capsular polysaccharide does not confer antiphagocytic properties on bacteria. However, the K7 antigen is able to impede the extracellular release of primary granule enzymes.

Antigens, Bacterial↗

PubMed2005

Immunological identification of types I and III collagen in bovine lens epithelium and its anterior lens capsule.

To define the molecular structure of bovine lens epithelium and its anterior lens capsule, we investigated the composition of lens capsule basement membrane proteins. Immunofluorescence and immunogold techniques were used to demonstrate the presence of type I and type III collagen in the lens capsule and in primary explant epithelial cultures grown on protein-binding membranes. Immunofluorescence staining with specific antibodies indicated that type I and type III collagen were constituents of lens basement membrane. We observed that deposition of type III collagen was more than type I collagen. The synthesis of fibrillar collagen by lens epithelium and its deposition in the lens capsule was established by localization of fibrillar collagen by transmission immunoelectron microscopy. These results demonstrate for the first time that normal lens epithelium synthesize fibrillar collagen which is an intrinsic component of the anterior lens capsule basement membrane.

Animals↗

PubMed2004

Wireless capsule video endoscopy compared to barium follow-through and computerised tomography in patients with suspected Crohn's disease--final report.

BACKGROUND: Wireless capsule endoscopy is a superior diagnostic tool to barium small bowel follow-through and enteroscopy in diagnosing patients with occult blood loss. AIM: To compare capsule endoscopy with barium follow-through and entero-computerised tomography in patients with suspected Crohn's disease. SUBJECTS AND METHODS: Thirty-five patients with suspected Crohn's disease underwent the three examinations. The radiologist and gastroenterologist were blinded to each other's results. In cases of discrepancy, colonoscopy and ileoscopy were performed. RESULTS: Thirty-five patients (22 males), mean age 28.4 years, were included. Eighty-eight percent had abdominal pain, 83% had diarrhoea and 69% had weight loss. The diagnostic yield of capsule endoscopy was 77% versus 23% and 20% of barium and computerised tomography examinations, respectively (P < 0.05). The capsule detected all of the lesions diagnosed by barium follow-through and entero-computerised tomography. CONCLUSIONS: Capsule endoscopy is a superior and more sensitive diagnostic tool than barium follow-through and entero-computerised tomography in patients with suspected Crohn's disease.

Adult↗

PubMed2004

Search for technological reasons to develop a capsule or a tablet formulation with respect to wettability and dissolution.

Proquazone, a poorly wettable compound, was used as a model drug in the search for reasons to develop a capsule or tablet formulation. The capsules were filled with proquazone as active ingredient, with lactose monohydrate (200 mesh) as filler and with magnesium stearate as lubricant. The tablet was made out of a granulate as internal phase which consisted of proquazone as active ingredient, lactose as filler, corn starch as disintegrant and PVP as a binding agent. The external phase consisted of magnesium stearate and corn starch. The concentration of proquazone in the capsule and in the tablet formulation was varied. The capsule formulations showed a significantly slower dissolution of the drug substance than the tablet formulations especially for a high-drug load. Independently of the drug load, only the tablet formulation showed a high-dissolution rate. Thus, concerning drug load, only the tablet formulations showed to be robust. It became clear that proquazone needs to be formulated as a granulate or a tablet to achieve a fast dissolution rate. Thus, a poorly wettable drug, especially when it is found in high concentrations, can have direct impact on the decision to develop a tablet or a capsule formulation.

Capsules↗

PubMed2005

Improvement of absorption enhancing effects of n-dodecyl-beta-D-maltopyranoside by its colon-specific delivery using chitosan capsules.

In general, absorption enhancing effects of various absorption enhancers were greater in the large intestine than those in the small intestinal regions. Therefore, the effectiveness of absorption enhancers is expected to be remarkably observed, if these enhancers can be delivered to the large intestine with some poorly absorbable drugs after oral administration. In this study, therefore, we examined whether chitosan capsules were effective for the colon-specific delivery of a certain absorption enhancer and can improve the absorption enhancing action of the absorption enhancer after oral administration. 5(6)-Carboxyfluorescein (CF) was used as a model drug to investigate the site-dependent effectiveness of various absorption enhancers by an in situ closed loop method. Sodium glycocholate (NaGC), n-dodecyl-beta-d-maltopyranoside (LM), sodium salicylate (NaSal) and sodium caprate (NaCap) were used as models of absorption enhancers in this study. Overall, the absorption enhancing effects of these enhancers for intestinal absorption of CF were greater in the colon than those in the jejunum and the ileum. Especially, among these enhancers tested in this study, LM showed much greater absorption enhancing effect in the colon than in the jejunum and the ileum. Therefore, LM was selected as a model absorption enhancer to examine the effect of chitosan capsules on the absorption enhancing effect of LM. When CF and LM were orally administered to rats using chitosan capsules, the plasma concentration of CF was much higher than those in other dosage forms including solution and gelatin capsules. Therefore, chitosan capsules may be useful carriers for colon-specific delivery of LM, thereby increasing its absorption enhancing effect from the intestinal membranes.

Animals↗

PubMed2005

Asymmetric membrane capsules for delivery of poorly water-soluble drugs by osmotic effects.

A non-disintegrating polymeric capsule system, in which asymmetric membrane offers an improved osmotic effect, was used to deliver poorly water-soluble drugs in a control manner. The capsule wall membrane was made by a phase inversion process, in which asymmetric membrane was formed on stainless-steel mold pins by dipping the mold pins into a coating solution containing a polymeric material followed by dipping into a quench solution. This study evaluates the influence of coating formulation that was cellulose acetate (CA), ethylcellulose (EC), and plasticizer (glycerin and triethyl citrate). Results show capsule that made by CA with glycerin (formulation A), which appear in asymmetric structure and are able to release chlorpheniramine maleate (CM) in significant percentage. Two poorly water-soluble drugs of felodipine (FL) and nifedipine (NF) were selected as the model drug to demonstrate how the controlled release characteristics can be manipulated by the design of polymeric capsules with an asymmetric membrane and core formulations. Results show that sodium lauryl sulfate (SLS) is able to promote the release of FL from polymeric capsules prepared with CA with asymmetrical membrane. The addition of solubilizer, including RH40, PVP K-17, and PEG 4000 could enhance the release of FL but with an extent not being related to its solubility. Based on these results, influence of core formulation variables, including the viscosity and added amount of hydroxypropyl methylcellulose (HPMC), the added amount of SLS, and drug loading were examined on the release of NF. It was found that HPMC of 50 cps was suitable to be a thickening agent and both added amount of HPMC and SLS showed a comparable and profoundly positive effect, whereas NF loading had no influence on the drug release percent and rate. There existed a synergistic interaction between HPMC and SLS on the release percent and rate.

Capsules↗

PubMed2005

Preparation and characterization of novel fast disintegrating capsules (Fastcaps) for administration in the oral cavity.

The objective of this study was to prepare novel capsule-based fast disintegrating dosage forms for the oral cavity (Fastcaps). First, cast films were prepared from various additive-containing gelatin solutions and evaluated with respect to disintegration time and mechanical properties in order to identify suitable formulations for the capsule preparation. The disintegration time of films decreased with decreasing bloom strength and could be further decreased by the addition of sugars or PEGs. Fast disintegrating capsules were successfully prepared by a dipping process, whereby parameters such as the viscosity and temperature of the dipping solution and the dipping velocity of the steel pins were optimized. The required viscosity range of the dipping solution for Fastcap manufacturing was 500-600 cP. The addition of the hydrophilic additives (xylitol, sorbitol or PEG 1500) did not significantly affect the viscosity and gelation temperature of the dipping solution. The in vitro disintegration of Fastcaps (30-45 s) was twice as rapid as the one of regular hard gelatin capsules. In vivo, Fastcaps disintegrated rapidly (9-13 s) and their content was spread throughout the oral cavity within seconds. Lactose and/or microcrystalline cellulose were suitable fillers for Fastcaps. The mechanical properties of Fastcaps were similar to commercially available gelatin capsules, which assures good processability and handling.

Administration, Oral↗

PubMed2006

Influence of rheological behaviour of particulate/polymer dispersions on liquid-filling characteristics for hard gelatin capsules.

Lactose/poloxamer dispersions were prepared by mixing under vacuum to achieve a de-aerated mix with good capsule filling properties and disperse phase uniformity at 70 degrees C. Satisfactory capsule filling of molten dispersions was achieved up to a limiting concentration of disperse phase, dependent on particle size distribution and continuous phase viscosity. Lactose/poloxamer dispersions exhibited thixotropic shear thinning behaviour with an abrupt increase in apparent viscosity above a limiting concentration of disperse phase. There was a good correlation between satisfactory filling of molten dispersions into capsules and apparent viscosity of the formulation, whereas, the pronounced increase in apparent viscosity resulted in unsatisfactory filling above a critical concentration of disperse phase. The rheological data was analysed in detail using empirical models and also used to identify capsule filling problems at extrudate shear rates for flow from hopper to pump (12 s(-1)) and from nozzle to capsule (340 s(-1)).

Capsules↗

PubMed2005

Upregulation of alphavbeta6 integrin, a potent TGF-beta1 activator, and posterior capsule opacification.

PURPOSE: To identify the predominant activation pathway of transforming growth factor (TGF)-beta1 in the lens capsule, studying the spatial and temporal expression pattern of alphavbeta6 and thrombospondin-1. Other PCO-related proteins were also studied. SETTING: Departments of Ophthalmology and Optometrics and Clinical Pathology, Medical School, University of Vienna, Vienna, Austria. METHODS: The lens capsules of 12 human donor eyes were cultivated in a protein-free medium for up to 28 days (cultivated lens capsules [CLCs]) after lens extraction. Ten intact lenses (ILs) served as the control group and were also cultured. During the culture period, cell dynamics were observed by phase-contrast microscopy. Proteins were detected by double immunofluorescence on frozen sections. RESULTS: In ILs, alphavbeta6 was absent but 91.6% of the CLCs showed extensive staining. Remnant lens epithelial cells (LECs) expressed alphavbeta6 immediately after lens extraction. The alphavbeta6 was detected throughout the culture period in all regions of the capsule. Thrombospondin-1 was absent in ILs and CLCs, suggesting that this protein is not significant in TGF-beta1 activation in the lens. Transforming growth factor-beta1 was abundantly expressed in all ILs and CLCs, slightly decreasing during intensive LEC proliferation and migration. The TGF-beta receptor II (RII) was expressed equally in all specimens, decreasing with culture time. Nonresident extracellular matrix proteins and alpha-smooth muscle actin were partially detected in CLCs but not in ILs. Latent TGF-beta binding protein 1 and collagen III were absent in all specimens. All cells found in the cultures expressed vimentin and alphaB-crystallin (LEC markers). CONCLUSION: Alphavbeta6 is the main activator of TGF-beta1 in the lens capsule and represents a new target for PCO prevention.

Actins↗

PubMed2005

Comparison of dyes for cataract surgery. Part 2: efficacy of capsule staining in a rabbit model.

PURPOSE: To investigate the efficacy of various dyes for anterior capsule staining to facilitate capsulorhexis during cataract surgery. SETTING: Department of Ophthalmology and Institute of Clinical Medicine, College of Medicine, National Cheng Kung University, Tainan, Taiwan. METHODS: Various concentrations of indocyanine green (ICG), methylene blue (MB), gentian violet (GV), trypan blue (TB), and fluorescein sodium (FS) were used to stain rabbit lenses in vitro. After 1 minute of exposure, the staining of each lens was evaluated using a semiquantitative scoring system in which 0 represented no staining/no contrast between the capsule and cortex and 4 represented excellent staining/remarkable contrast between the stained capsule and unstained cortex. The lowest concentration of dye with a score of 4 was considered the lowest effective concentration for capsulorhexis. RESULTS: Based on our scoring system, the lowest effective concentrations for capsulorhexis were ICG 0.25%, MB 0.10%, GV 0.01%, TB 0.10%, and FS 1.25%. The lowest effective concentrations of the 5 dyes provided comparable contrast. Increased concentrations of dye decreased contrast between the capsule and the cortex and were considered less effective for capsulorhexis. CONCLUSION: Any of the following concentrations of dyes can be used for optimal enhancement of anterior capsule visibility for capsulorhexis: ICG 0.25%, MB 0.10%, GV 0.01%, TB 0.10%, and FS 1.25%.

Animals↗

PubMed2005

Evaluation of posterior capsule opacification using a new posterior view method in rabbits: single-piece acrylic versus 3-piece acrylic intraocular lens.

PURPOSE: To introduce a new procedure for evaluating posterior capsule opacification (PCO) in rabbit eyes and to perform a comparative study of the single-piece and 3-piece acrylic intraocular lenses (IOLs) on PCO using the new evaluation method. SETTING: Jinshikai Medical Foundation, Nishi Eye Hospital, Osaka, Japan. METHODS: A single-piece or 3-piece acrylic IOL was implanted in 1 eye and the other in the contralateral eye of 5 rabbits. Three weeks after surgery, PCO was scored by Evaluation of Posterior Capsule Opacification (EPCO) in posterior view. Before the posterior view was photographed, the anterior capsule was removed from the whole optic area to eliminate disturbing anterior capsule opacification (ACO) for the PCO evaluation. RESULTS: Posterior capsule opacification could be well observed and viewed in the posterior view so that it could be scored by EPCO without confusion with ACO. The mean PCO score of the single-piece and 3-piece acrylic IOLs was 3.12 +/- 0.19 and 2.41 +/- 0.70, respectively (P < .05 and P = .03, respectively). CONCLUSION: The removal of ACO allowed scoring of PCO by EPCO in rabbit eyes. The single-piece acrylic IOL showed significantly more PCO than the 3-piece acrylic IOL at least 3 weeks after surgery in rabbits.

Acrylic Resins↗

PubMed2006

Effect of hydrodissection alone and hydrodissection combined with rotation on lens epithelial cells: surgical approach for the prevention of posterior capsule opacification.

PURPOSE: To evaluate the impact of corticocleaving hydrodissection alone and hydrodissection combined with rotation on lens epithelial cells (LECs) and residual cortical fibers (RCFs). SETTING: Iladevi Cataract and IOL Research Center, Ahmedabad, India. METHODS: An experimental laboratory study of 20 fresh human cadaver eyes (10 pairs) was conducted. A single eye from each pair was assigned to the control group, in which no hydrodissection and no rotation were performed (control). The other eye was randomized to corticocleaving hydrodissection alone (Group 1) or corticocleaving hydrodissection with rotation (Group 2). Cataract extraction was standardized. Capsule polishing was omitted. Area of LEC loss (%) in the preequatorial zone (PZ) and equatorial zone (EZ) was calculated as: [Area of capsule without cells/Total area of capsule] x 100. Area of presence of RCFs (%) was calculated as: [Circumference of EZ of capsule with RCF/Total circumference of EZ of the capsule] x 100. The Mann-Whitney U and the Wilcoxon signed rank tests were applied. RESULTS: In the control group, area of cell loss (%) was 3.9 +/- 3.2 in the PZ and 2.7 +/- 0.8 in the EZ; presence of RCFs (%) was 83.8 +/- 1.7. Area of LEC loss (%) in Groups 1 and 2 was 24.8 +/- 4.5 and 42.6 +/- 5.4 (P = .008) in the PZ and 22.4 +/- 2.1 and 54 +/- 2.5 (P = .008) in the EZ, respectively. Area of presence of RCFs (%) in Groups 1 and 2 was 34.2 +/- 3.7 and 23.7 +/- 3.7 (P = .008), respectively. CONCLUSION: Corticocleaving hydrodissection combined with rotation removed significant quantities of LECs and RCFs.

Aged↗

PubMed2006

Routine posterior optic buttonholing for eradication of posterior capsule opacification in adults: report of 500 consecutive cases.

PURPOSE: To study the efficacy of posterior optic buttonholing (POBH) through a primary posterior capsulorhexis (PPCCC) to preserve full capsular transparency, and its potential as a routine alternative to standard in-the-bag implantation of sharp-edged optic intraocular lenses (IOLs). SETTING: Department of Ophthalmology, Medical University of Vienna, Vienna, Austria. METHODS: After standard cataract removal, a PPCCC 4.0 to 5.0 mm in diameter was performed and the optic of a 3-piece IOL buttonholed posteriorly. One third of the eyes additionally had extensive anterior capsule polishing. All surgeries were performed under topical anesthesia. RESULTS: The first 500 consecutive surgeries were evaluated. In 11 eyes, POBH was not performed as planned. In 4 cases, anterior capsulorhexis fixation of the optic was used as an alternative. In the early series, vitreous entanglement was seen in 5 eyes, of which 1 case prompted translimbal anterior vitrectomy. No case of cystoid macula edema was observed. One case of peripheral retinal detachment in a highly-myopic eye 4 months postoperatively appeared to be unrelated to the surgery. All lenses were well-centered without tilt, and both capsule leaves remained clear especially after additional polishing. CONCLUSION: Posterior optic buttonholing precludes lens epithelial cells from accessing the retrolental space. The sandwiched posterior capsule blocks optic contact and thus fibrosis of the anterior capsule. Posterior optic buttonholing avoids after-cataract independent of optic edge design. Anterior capsule polishing adds to its efficacy by excluding any residual fibrosis. Surgery under topical anesthesia was well-controlled and safe. Posterior optic buttonholing may become a routine alternative to standard in-the-bag IOL implantation when supported by a longer follow-up.

Capsulorhexis↗

PubMed2007

The posterior segment of the temporomandibular joint capsule and its anatomic relationship.

PURPOSE: The aim of this work was to clarify the arrangement of the posterior segment of the temporomandibular joint capsule and its pertinent relationships. MATERIALS AND METHODS: The temporomandibular region was dissected bilaterally in 20 adult cadavers. Natural stained latex was injected into 16 cadavers through the external carotid artery to facilitate the dissection of the arterial vessels. RESULTS: The posterior segment of the joint capsule is made up of the so-called "bilaminar zone" of the articular disc. The upper internal portion of the posterior segment of the capsule was reinforced by the discomalleolar ligament. The retroarticular space was filled with loose connective tissue and the anterior branches of the anterior tympanic artery were distributed throughout the posterior segment of the joint capsule. CONCLUSION: The posterior segment of the temporomandibular joint capsule corresponds to the bilaminar zone of the articular disc. The structures of the retroarticular space are extracapsular.

Aged↗

PubMed2005

Thermal stability of UV-irradiated collagen in bovine lens capsules and in bovine cornea.

The thermal stability of UVB irradiated collagen in bovine lens capsules and in bovine cornea has been investigated by differential scanning calorimetry (DSC). During UVB irradiation the lens capsules and cornea were immersed in water to keep the collagen in a fully hydrated condition at all times. UV irradiation induced changes in collagen which caused both stabilization and destabilization of the collagen structure. The helix-coil transition for non-irradiated collagen in cornea occurred near 66 degrees C, instead for the irradiated one for 3h it occurred at 69 degrees C. After irradiating for longer times (20-96h) the helix-coil transition peak occurred at much lower temperatures. The peak was very broad and suggested that collagen was reduced by UV to different polypeptides of different molecular weight and different lower thermal stabilities. The irradiation of lens capsules with UVB light in vitro resulted in changes in the thermal properties of type-IV collagen consistent with increased cross-linking. DSC of lens capsules showed two major peaks at melting temperatures at 54 degrees C Tm1 and 78 degrees C Tm2, which can be attributed to the denaturation of the triple helix and 7S domains, respectively. UVB irradiation of lens capsules in vitro for 6 h caused an increase in Tm1 from 54 to 57 degrees C. The higher temperature required to denature the type-IV collagen after irradiation in vitro suggested an increase of intermolecular cross-linking.

Animals↗