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青蒿琥酯皮肤擦剂在小鼠和兔体内的药代动力学研究   总被引:1,自引:0,他引:1  
赵凯存  宣文漪  赵一  宋振玉 《药学学报》1989,24(11):813-816
将青蒿琥酯溶于苯二甲酸二甲酯,加适量氨酮制成皮肤擦剂。给兔脱毛后,皮肤涂抹此擦剂25mg/kg后,血药浓度达峰时间平均为2 h,峰浓度平均为1.80μg/ml。药物在兔体内平均驻留时间为3.54 h,清除半衰期约为2.46 h。给小鼠脱毛皮肤涂抹擦剂6.7,31.3和71.4 mg/kg,血药浓度在给药后0.5~4 h达高峰,峰浓度分别为0.82,2.05和7.11μg/ml,体内药物平均驻留时间为3.39,2.79及3.54 h,清除半衰期为2.35,1.93及2.45 h。可见,给兔及小鼠皮肤擦剂后,青蒿琥酯吸收良好,血药浓度维持时间较长。  相似文献   
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1. It was the aim of this study to determine the extent to which a mammalian motoneuron can sprout in a partially denervated muscle, which motor unit types are involved in sprouting, and whether polyneuronal innervation exists between sprouted units. 2. The fast-twitch flexor digitorum longus (FDL) and slow-twitch soleus were partially denervated by unilateral section of the L7 ventral root in 12-wk-old kittens. After approximately 100 days single motor units were isolated, and their isometric contractile characteristics were determined. FDL units were also tested for their resistance to fatigue and categorized as fast-twitch, fatiguing fibers (FF), fast-twitch, fatigue-resistant fibers (FR), and slow-twitch, fatigue-resistant fibers (S). The presence of polyneuronal innervation was investigated between pairs of like and unlike units. 3. The extent of the original denervation was variable and was estimated from the distribution of motor axons innervating the muscle via the L7 and S1 (soleus) or L6 and L7 (FDL) ventral roots on the contralateral side. In soleus, denervations ranged from 75 to 98%; in FDL, 60 to 97% (denervations less than 60% were not investigated). In general, motor-unit force increased in proportion to the extent of the denervation. 4. Within soleus, unit force increased to over 2 N, which was about 16 times greater than the average for a normal muscle (133 mN). However, most units increased in force to between five and 12 times normal. 5. Within FDL, the force development of type S units was unaffected by partial denervation. Type FF units increased by up to 11 times (4.3 N) compared with normal FF units (395 mN) with most increasing between two and four times. FR units exhibited the greatest relative increase in force [up to 19 times (4.3 N) compared with normal (225 mN)]. Most units were two to seven times the normal. 6. A few FDL units were glycogen depleted, the muscles frozen, and cross sections prepared for histochemical analysis. This indicated that the largest units contained approximately 5,000 fibers, and there was little fiber hypertrophy. In the extensively denervated soleus muscle, large numbers of small, presumably denervated fibers were observed. The innervation ratio of several large units was determined indirectly using mean fiber area. This gave estimates of 3,000-4,000 fibers for the largest units. Again, fiber hypertrophy contributed little to the increase in unit force. It was concluded that the increased force of units in both muscles was largely attributable to terminal and axonal sprouting of the intact motor axons. 7. No evidence for polyneuronal innervation was found in either FDL or soleus muscle.(ABSTRACT TRUNCATED AT 400 WORDS)  相似文献   
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Advances in the detection of carcinoma of the prostate during the last 15 years have accounted for a sharp increase and then an abrupt decrease in the incidence of the disease. A more recent decline in its mortality rates has been variously interpreted as either the success of early detection and improved treatment or lead-time bias. The recently reported Prostate Cancer Prevention Trial had an overall detection rate that approached the 30%-40% prevalence rates reported in autopsy series in which men died of other causes. However, the prognostic information that can be obtained from prostate cancer found on biopsy is limited. Three-dimensional computer modeling is one technique that allows multiple studies on "immortal" prostates to test methods of biopsy sampling accuracy and to assist in the determination of the disease's severity. Computer modeling can assess detection rates and assesses tumor multifocality and heterogeneity. It can provide a more accurate representation of tumor volume, aiding in therapeutic decision making, and can assess sampling errors of various biopsy methods. It has been shown to be superior to wire-frame technique by immortalizing the original shape and dimensions of the surgically excised prostate gland. Moreover, our 3-dimensional computer modeling system improves upon other systems: It is more than a simple extension of the planimetric technique, and it is able to demarcate clearly the boundaries of Gleason grades just 1 grade apart.  相似文献   
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1. It was the aim of this study to determine the effect that regenerating motor axons would have on enlarged or sprouted motor units that had been established for a relatively long time. 2. The fast-twitch flexor digitorum longus (FDL) and slow-twitch soleus were partially denervated by unilateral section of the L7 ventral root in 12-wk-old kittens. After 200+ days single motor units were isolated, and their isometric contractile properties were determined. FDL units were also tested for their resistance to fatigue and categorized as fast-twitch-fatigable (FF), fast-twitch-fatigue-resistant (FR), and slow-twitch-fatigue-resistant (S). 3. It had been established previously that regenerating motor axons via L7 returned to the experimental muscles by approximately 100 days. Therefore from 100 to 200 days it was assumed that the sprouted units would be in competition with the regenerating axons. The extent of the original denervations was variable and was estimated from the contralateral side. In soleus most denervations ranged from 83 to 99%; in FDL, from 37 to 81%. 4. In both soleus and FDL there was no evidence that the motor units had sprouted to any less extent than found previously. Within some soleus muscles the largest motor units were developing substantially more force than was expected. However, determination of mean fiber cross-sectional area from muscles frozen, sectioned, and prepared for histochemical analysis showed that this was attributable to increased mean cross-sectional area of the type I fibers.(ABSTRACT TRUNCATED AT 250 WORDS)  相似文献   
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