A Comparison of Oral and Rectal Absorption of L-Dopa Esters in Rats and Mice

Short-chain alkyl esters of L-dopa were administered to rats and mice via oral and rectal routes. Plasma L-dopa esters and L-dopa were determined in the systemic and portal circulation by HPLC. A comparison of isopropyl, butyl, and 4-hydroxybutyl esters of L-dopa demonstrated significantly higher levels of the esters in both systemic and portal blood samples following rectal administration than following oral administration. In most cases, oral administration resulted in nondetectable (<0.01 µg/ml) levels of the esters in plasma. Correspondingly, the plasma levels of L-dopa itself were consistently higher following rectal administration. At very high oral doses (500 mg L-dopa equivalents/kg body weight), systemic plasma levels of the butyl ester could be detected (1.25 µg/ml at 10 min), which might indicate saturation of the esterase activity of the small intestine. These studies indicate that the systemic availability of L-dopa from short-chain alkyl esters of L-dopa may be best optimized by rectal administration, which avoids the relatively high esterase activity characteristic of the small intestine.     

Pharmacokinetics of orally administered norethisterone enanthate in rabbit, monkey, and women

Norethisterone enanthate (NET-En), an established intramuscular long-acting contraceptive agent, has previously been shown to be effective in inhibiting fertility in two rodent species even 4 days after oral ingestion. Pharmacokinetics of NET and NET-En were studied after oral and intramuscular doses in two animal species and a few women. The results suggest that the NET-En was absorbed within a day in all the species after oral dose. The estimates of relative bioavailability ranged from 13 to 51% in rabbits, monkeys, and women. The elimination half-life was 5–10 days. The presence of the active component, NET, in the circulation over the experimental period of 15 days suggests that NET-En could be useful as a long-acting oral pill. The suppression of progesterone levels during the luteal phase of menstrual cycle in women also supports this finding.     

Expression of c-erbB-2 protein in keratinocytes of oral mucosal lichen planus and subsequent squamous cell carcinoma

Oral mucosal lichen planus (OMLP) is a well recognized mucosal disease with unknown etiology. Considerable controversy exists as to whether OMLP is intrinsically premalignant, or if the disorder facilitates the development of oral mucosal squamous cell carcinoma (OMSCC) by external factors. The aim of the present study was to investigate the expression of c-erbB-2 protein in the keratinocytes of initial biopsies of oral mucosal disorders diagnosed as OMLP with no evidence of epithelial dysplasia. and to compare the results with the expression of c-erbB-2 protein in subsequent biopsies obtained from the same patients. These results were compared with the findings from control groups (patients with dysplasia with no evidence of OMLP, patients with OMSCC with no evidence of OMLP and normal oral mucosa). The expression of the c-erbB-2 protein was evaluated by immunohistochemical staining of the gene product with the avidin-biotin-complex method using paraffin-embedded tissue sections. Five of the initial biopsies from patients with OMLP expressed the c-erhB-2 protein and one did not. None of the OMLP cases that subsequently showed evidence of dysplasia expressed the c-erhB-2 protein, and of the three OMSCC specimens from the patients with OMLP. two were negative and one expressed c-erbB-2 protein. The specimens from the control groups all expressed the c-erhB-2 protein. The results indicated the probability of the absence of c-erbB-2 staining being an indication of a potential for neoplastic transformation in OMLP with dysplastic changes.     

Periodontal conditions among the middle-aged and the elderly in Hong Kong

Abstract The aim of this study was to describe the periodontal conditions in 372 35–44-yr-old and 537 noninstitutionalized 65–74-yr-old Hong Kong Chinese who were examined clinically for loss of attachment, recession, probing depth, calculus, and bleeding after probing. Community Periodontal Index (CPI) data and treatment need indications were compiled from index teeth or their substitutes. The prevalence of loss of attachment varied considerably in both cohorts according to the definition of the threshold (≥6, ≥9, and ≥12 mm, respectively). The mean numbers of teeth with loss of attachment at the ≥6-mm threshold and at higher thresholds were small. In both age cohorts, about one-fifth of subjects had probing depths ≥6-mm, while al the ≥9-mm threshold only 2–3% were so affected. Although recession was an important component of loss of attachment in the younger cohort, in the older cohort the prevalence and extent of recession were greater than for probing depths at thresholds ≥4 mm. All subjects had one or more teeth with calculus, bleeding, or both, most teeth being so affected. Eighty-four of the 537 65–74-yr-old subjects were excluded either because of edentulousness or because extractions indicated for the remaining teeth would have rendered the subjects edentulous. The distribution of subjects according to their highest CPI score was remarkably similar for the two cohorts. No subjects in either age group were assessed as “healthy” (CPI code 0) or had “bleeding only” (code 1) as their highest score. While most subjects scored CPI code 2 or 3 us their highest score, only 17% of the younger and 15% of the older cohort scored Community Periodontal Index of Treatment Needs (CPITN) code 4. Differences in the mean number of sextants affected by CPI codes between the two cohorts were mainly due to a greater number of excluded sextants in the older cohort. CPI findings for 35–44-yr-olds differed little from those reported in 1984.     

Susceptibility to ketoconazole of Candida albicans strains from sequentially followed HIV-1 patients with recurrent oral candidosis

The MIC values of the antifungal drug ketoconazole were evaluated on 66 Candida albicans strains. These strains were isolated from 26 HIV-1 infected patients with oral recurrent candidosis. Each episode of oral candidosis observed in these patients was orally treated with ketoconazole (200 mg/day) until the clinical disappearance of the lesions. The most frequent MIC values were 20 micrograms/ml and 10 micrograms/ml, observed in 37 and 19 isolates respectively. Only strains from five patients showed changes in their susceptibility to ketoconazole. This fact could indicate that a different strain causes the subsequent reappearance of the oral lesions, rather than the drug selecting resistant fungal strains. Our results stress the role of host characteristics in the occurrence of candidal infections, pointing to the progressing failure of the immunological response as the most important factor responsible for the recurrence of oral candidosis during HIV-1 infection.     

Treatment of gingival lichen with free palatal grafts

BACKGROUND: Recalcitrant gingival erythematous lichen planus/lichenoid lesions comprise a considerable therapeutic problem. The objective of this study was to evaluate the therapeutic effect of grafting keratinized oral palatal mucosa to the sites of gingival lichen. METHODS: In 12 patients 20 grafts were transplanted to buccal gingival lesions. Mean age of the patients was 59.8 +/- 7.1 years (range 46-71 years). The mean observation time was 32 +/- 32.7 months (range 5-97 months). RESULTS: On a 4-point clinical grade scale (0-3), 12 (60%) transplants showed complete healing grade 3, six (30%) grade 2 and two (10%) grade 1. CONCLUSIONS: Using oral mucosal grafts from the palatal mucosa for the treatment of recalcitrant erythematous gingival lichen planus/lichenoid lesions seems to be a promising treatment modality.     

Comparison of fibre optic transillumination with clinical and radiographic caries diagnosis

Fibre optic transillumination (FOTI) has been employed during the course of a 3-yr clinical dentifrice trial which initially involved 3003 children. At the initial examination, a subgroup of 813 13-yr-olds, and at the following annual visit, 2247 14-yr-olds, were examined using a 150 W lamp and 0.5 mm diameter probe. Routine clinical and radiographic examinations were performed separately. Compared to the clinical scores for anterior teeth, FOTI detected an additional 64% of interproximal lesions at the first visit while, for the larger number of children at the second visit, the increase in lesion detection level using FOTI was 37%. For the posterior teeth the comparable figure at the second examination was 92%. When FOTI data were compared to radiographic data for more than 52,000 posterior interproximal surfaces, FOTI could only detect 17% of radiographic Grade 2 lesions and 48% Grade 3 lesions. Thus any assumption that FOTI diagnoses may be a substitute for bitewing radiography appears premature.     

Prevalence of traumatic injuries to the permanent incisors in candidates for orthodontic treatment

Abstract  – The dental records made on presentation of 1367 consecutive patients (731 females and 636 males) for orthodontic treatment at a private orthodontic practice between 1998 and 2002 were examined for data relating to trauma to the permanent incisors. The results showed that 10.3% of these patients had suffered from dental trauma before the onset of orthodontic treatment. The highest prevalence of dental trauma was determined in the 11–15 years age group, corresponding to the dental developmental stage of the late mixed dentition. The most frequently affected teeth were the maxillary central incisors (79.6%), and the most common types of trauma were fracture of enamel–dentin without pulpal involvement (42.7%) and fracture of enamel (33.8%). Compared to patients with normal overjet and adequate lip coverage, the frequency of dental trauma was significantly higher in patients with increased overjet and adequate lip coverage ( P  = 0.028) or with increased overjet and inadequate lip coverage ( P  = 0.003). The results of the present study indicate that a significant percentage of candidates for orthodontic treatment, and especially those with increased overjet and inadequate lip coverage, suffer trauma to their permanent incisors before the onset of orthodontic treatment. It might also be concluded that preventive orthodontic treatment of such patients should be initiated and completed before the age of 11, i.e. in the early to middle mixed dentition.     

The immunohistology of CD40 in human oral epithelium in health and disease

BACKGROUND: CD40 has a role in the regulation of immune responses, cell proliferation and migration, and apoptosis. Little is known of its distribution in oral mucosal pathology. METHODS: Oral keratinocyte lines were tested for CD40 protein by Western blotting. Immunohistochemistry was used to stain paraffin sections of oral mucosa in health and in inflammatory, reactive, dysplastic and malignant disease. RESULTS: Western blotting confirmed the presence of CD40 in oral keratinocytes. CD40 was generally expressed by keratinocytes in the basal layer, with variable parabasal expression. Langerhans cells also stained positively. Expression was lost in nine of 33 (27%) epithelial dysplasias, seven of which were severe. Eighty-one percent of well, 69% of moderately and 50% of poorly differentiated oral squamous cell carcinomas (OSCC) expressed CD40. Overall, 45 of 65 (69%) OSCC were positive. The pattern of expression was unrelated to tumour differentiation. CONCLUSION: CD40 expression by basal and parabasal oral keratinocytes is physiological. Expression is lost in approximately one-third of oral epithelial dysplasias and OSCC. The significance of such loss remains unknown, but may be related to immunological or other abnormalities of keratinocyte homeostasis.