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| Pharmacokinetics and Metabolism: Glipizide is rapidly and completely absorbed following oral administration in an immediate release dosage form. The absolute bioavailability of glipizide was 100% after single oral doses in patients with type 2 diabetes. Beginning 2 to 3 hours after administration of GLUCOTROL XL Extended Release Tablets, plasma drug concentrations gradually rise reaching maximum concentrations within 6 to 12 hours after dosing. With subsequent once daily dosing of GLUCOTROL XL Extended Release Tablets, effective plasma glipizide concentrations are maintained throughout the 24 hour dosing interval with less peak to trough fluctuation than that observed with twice daily dosing of immediate release glipizide. The mean relative bioavailability of glipizide in 21 males with type 2 diabetes after administration of 20 mg GLUCOTROL XL Extended Release Tablets, compared to immediate release Glucotrol (10 mg given twice daily), was 90% at steady-state. Steady-state plasma concentrations were achieved by at least the fifth day of dosing with GLUCOTROL XL Extended Release Tablets in 21 males with type 2 diabetes and patients younger than 65 years. Approximately 1 to 2 days longer were required to reach steady-state in 24 elderly (≥65 years) males and females with type 2 diabetes. No accumulation of drug was observed in patients with type 2 diabetes during chronic dosing with GLUCOTROL XL Extended Release Tablets. Administration of GLUCOTROL XL with food has no effect on the 2 to 3 hour lag time in drug absorption. In a single dose, food effect study in 21 healthy male subjects, the administration of GLUCOTROL XL immediately before a high fat breakfast resulted in a 40% increase in the glipizide mean Cmax value, which was significant, but the effect on the AUC was not significant. There was no change in glucose response between the fed and fasting state. Markedly reduced GI retention times of the GLUCOTROL XL tablets over prolonged periods (e.g., short bowel syndrome) may influence the pharmacokinetic profile of the drug and potentially result in lower plasma concentrations. In a multiple dose study in 26 males with type 2 diabetes, the pharmacokinetics of glipizide were linear over the dose range of 5 to 60 mg of GLUCOTROL XL in that the plasma drug concentrations increased proportionately with dose. In a single dose study in 24 healthy subjects, four 5-mg, two 10-mg, and one 20-mg GLUCOTROL XL Extended Release Tablets were bioequivalent. In a separate single dose study in 36 healthy subjects, four 2.5-mg GLUCOTROL XL Extended Release Tablets were bioequivalent to one 10-mg GLUCOTROL XL Extended Release Tablet. Glipizide is eliminated primarily by hepatic biotransformation: less than 10% of a dose is excreted as unchanged drug in urine and feces; approximately 90% of a dose is excreted as biotransformation products in urine (80%) and feces (10%). The major metabolites of glipizide are products of aromatic hydroxylation and have no hypoglycemic activity. A minor metabolite which accounts for less than 2% of a dose, an acetylamino-ethyl benzene derivative, is reported to have 1/10 to 1/3 as much hypoglycemic activity as the parent compound. The mean total body clearance of glipizide was approximately 3 liters per hour after single intravenous doses in patients with type 2 diabetes. The mean apparent volume of distribution was approximately 10 liters. Glipizide is 98–99% bound to serum proteins, primarily to albumin. The mean terminal elimination half-life of glipizide ranged from 2 to 5 hours after single or multiple doses in patients with type 2 diabetes. There were no significant differences in the pharmacokinetics of glipizide after single dose administration to older diabetic subjects compared to younger healthy subjects. There is only limited information regarding the effects of renal impairment on the disposition of glipizide, and no information regarding the effects of hepatic disease. However, since glipizide is highly protein bound and hepatic biotransformation is the predominant route of elimination, the pharmacokinetics and/or pharmacodynamics of glipizide may be altered in patients with renal or hepatic impairment. In mice no glipizide or metabolites were detectable autoradiographically in the brain or spinal cord of males or females, nor in the fetuses of pregnant females. In another study, however, very small amounts of radioactivity were detected in the fetuses of rats given labelled drug |
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zdf1021
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【答案】應(yīng)助回帖
| 藥物動(dòng)力學(xué)和新陳代謝：Glipizide 快速地而且完全地被吸收的立即版本的下列的口服行政劑量形式。glipizide 的絕對生物藥效在單一口服劑量之后在患有 2 型糖尿病的患者是 100%了。開始 2-3 小時(shí)在 GLUCOTROL XL 的行政之后延長了版本錠劑，血漿藥物濃度在 6-12 小時(shí)之內(nèi)在配之后逐漸地上升達(dá)成最大濃度。與后來的一經(jīng)每日 GLUCOTROL XL 的配延長了版本錠劑，有效的血漿 glipizide 濃度到處被維護(hù)配間隔的 24 小時(shí)與比較不最高對木缽變動(dòng)超過哪一觀察與兩次每日立即版本 glipizide 的配。在患有 2 型糖尿病的 21個(gè)男性中的 glipizide 的平均相對生物藥效在 20 毫克 GLUCOTROL XL 的行政之后延長了與立即的版本 Glucotrol（每日被給予兩次的 10 毫克）相較的版本錠劑是 90% 在不變的。不變的血漿濃度在至少第五天─在患有 2 型糖尿病的 21個(gè)男性中有 GLUCOTROL XL 廣大的版本錠劑配之前被達(dá)成了和患者比 65 年年輕。大約長 1-2 天為到達(dá)所需不變的在 24個(gè)年老的 （≥ 65 年）男性和患有 2 型糖尿病的女性中。藥物的沒有蓄積在慢性的配期間以被延長版本錠劑的 GLUCOTROL XL 在患有 2 型糖尿病的患者中被觀察。GLUCOTROL XL 的行政用食物在藥物吸收中對 2-3 小時(shí)延遲時(shí)間產(chǎn)生沒有影響。在一個(gè)劑量中，食物效果在 21個(gè)健康男性主題中學(xué)習(xí)， GLUCOTROL XL 的行政立刻在一之前高的脂肪早餐造成 glipizide 的40%增加平均數(shù) Cmax 數(shù)值，這是重要的，但是對 AUC 的影響不重要。沒有葡萄糖方面的改變響應(yīng)在這之間喂和禁食狀態(tài)。顯著地減少在延長的期數(shù) （舉例來說，短腸征候群）上的 GI 滯留 GLUCOTROL XL 錠劑的時(shí)代可能影響藥物的藥物動(dòng)力描繪而且可能地造成較低的血漿濃度。在患有 2 型糖尿病的 26個(gè)男性中的一項(xiàng)多項(xiàng)劑量研究中， glipizide 的藥物動(dòng)力學(xué)在血漿藥物濃度相稱地，以劑量增加的 5-60 毫克 GLUCOTROL XL 的劑量范圍之上是線性的。在劑量 24個(gè)健康主題中的研究中，四 5 毫克，二 10 毫克，和 20 毫克 GLUCOTROL XL 廣大的版本錠劑是 bioequivalent。在 36個(gè)健康主題的一項(xiàng)分開的單一劑量研究中，四 2.5 毫克 GLUCOTROL XL 廣大的版本錠劑是 bioequivalent 至 10 毫克 GLUCOTROL XL 延長版本錠劑。Glipizide 主要地被肝的生物轉(zhuǎn)化所除去：少于 10% 的一個(gè)劑量在尿液和糞便中當(dāng)做不變的藥物被排泄；大約 90% 的一個(gè)劑量在尿液 （80%) 和糞便 （10%) 中當(dāng)做生物轉(zhuǎn)化產(chǎn)品被排泄。glipizide 的主要新陳代謝產(chǎn)物是芬芳羥化的產(chǎn)品而且沒有血糖過低的活動(dòng)。一個(gè)占有小于 2% 的一個(gè)劑量，一個(gè) acetylamino－乙基苯的衍生物，的較小的新陳代謝產(chǎn)物被指出有 1|10-1|3 像母化合物一樣的多血糖過低的活動(dòng)。glipizide 的平均完全身體凈空大約是患有 2 型糖尿病的患者中的單一靜脈注射的劑量后的每小時(shí) 3個(gè)升。分配的平均表觀重量大約是 10個(gè)升。Glipizide 是對血清蛋白質(zhì)約束的 98-99%，主要地對蛋白素。glipizide 的平均終末排除半生期在單一或多重劑量之后在患有 2 型糖尿病的患者從 2 排列到 5 小時(shí)了。與比較年輕的健康主題相較對舊的糖尿病的主題沒有在單一劑量行政后的 glipizide 的藥物動(dòng)力學(xué)中的重要不同。關(guān)于腎損害對 glipizide 的素質(zhì)的效果、和沒有關(guān)于肝疾病的效果的信息只有有限制的信息。然而，因?yàn)?glipizide 是高度蛋白質(zhì)的界線，而且肝的生物轉(zhuǎn)化是排除的優(yōu)越路徑， glipizide 的藥物動(dòng)力學(xué)和│或者藥效學(xué)可能在患者中被腎或肝的損害所改變。在老鼠沒有 glipizide 或新陳代謝產(chǎn)物中是腦或男性或女性的脊髓中的可發(fā)覺的 autoradiographically，也不在懷孕女性的胎兒中。在另外的一項(xiàng)研究中，然而，非常小量放射性在給定的鼠的胎兒中被發(fā)現(xiàn)貼上標(biāo)簽藥物 |
5樓2011-03-17 14:13:52
yoyo198579
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6樓2011-03-18 09:41:33
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