Lansoprazole for injection
Generic name:Lansoprazole for Injection
Active ingredient:Lansoprazole
Excipient:Mannitol, meglumine and sodium hydroxide
Chemical name: 2-[[[3- methyl-4-(2，2，2- trifluoroethoxyl)-2- pyridine] methyl] sulfinyl]-1H- benzimidazole
Chemical structure:
Molecular formula: C16H14F3N3O2S
Molecular weight: 369.36
Description
White or off-white porous mass.
Indications
Treatment for duodenal ulcer associated with hemorrhage while not suitable for oral administration.
Strength
30mg
Dosage and administration
Intravenous infusionis applied, normally 30mg for adults once and 2 times a day for no more than 7 days.Once the patient can take the drug orally, lansoprazole oral preparation should be used for a change. Prior to use, add 5ml of sterile water for injection into the vial to dissolve the content completely, next be added into a 100ml of 0.9% sodium chloride injection for dilution, and then followed by intravenous infusion. The recommended administration time should be not less than 30 minutes.
Precaution
(1)When using this product in intravenous infusion, a filter with a pore size of 1.2μm should be provided in order to remove precipitates that may be generated during infusion. These precipitates may cause microvascular embolism with serious consequences.
(2)In any dangerous cases where there is an eruptive or gushing bleeding or vascular exposure, endoscopic hemostasis should be used.
(3)This product is only used for intravenous infusion. After dissolution, it should be used immediately and storage is prohibited. Mixing for intravenous infusion with liquids other than 0.9% sodium chloride injection and other drugs is not allowed.
(4)If the hemostatic effect is achieved within the first 3 days after treatment with this product, oral administration should be used instead of intravenous administration. Unlimited intravenous administration is not allowed.
Adverse reaction
In domestic clinical studies, this product was used twice a day, each time 30mg for intravenous infusion and 7 days of treatment course. In 109 subjects, two adverse events occurred with symptoms of dizziness, abdominal discomfort, and diarrhea. After the introduction of lansoprazole for injection in foreign countries, more than 1,000 patients are well tolerated after use. In the United States, after using lansoprazole for injection in 161 patients in four clinical trials, adverse reactions of more than 1% includingnausea (1.3%), headache (1%) and pain at the injection site (1%) occurred; while less than 1% including abdominal pain, diarrhea, dyspepsia, vomiting, dizziness, paresthesia, abnormal taste, skin rashand vasodilation occurred. No adverse effects different from oral administration occurred. Japanese clinical research data reported that after 221 subjects used lansoprazole for injection, 31 cases (14.0%) had abnormal clinical laboratory tests, mainly alanine aminotransferase (ALT) elevation (6.2%), aspartate aminotransferase (AST) elevation (5.7%), lactate dehydrogenase (LDH) elevation (2.0%), γ-glutamyl transferase (γ-GGT) elevation (1.5%) ) and so on.The following adverse reactions arecommon with oral lansoprazole, whileit may also occur during intravenous injection.
1.The medication course should be closely observed. If any of the following serious adverse reactions occur, the medication should be stopped in time and treat it appropriately.
(1)Allergic reactions (systemic rash, facial edema, dyspnea, etc.) (<0.1%) and even shock (<0.1%)
(2)Pancytopenia and agranulocytosis, hemolysis (<0.1%), neutropenia, thrombocytopenia, anemia (0.1% to <5%);
(3)Severe hepatic impairment with jaundice, elevated AST and ALT (<0.1%);
(4)Toxic epidermal necrolysis (Lyell syndrome), mucocutaneous ophthalmopathy syndrome (Stevens-Johnson syndrome) (<0.1%);
(5)Interstitial pneumonia (<0.1%), fever, cough, dyspnea, abnormal breath sounds in the lungs (acute pronunciation) and so on; discontinue the medication quickly, thenchest X-ray examination is performed and adrenocortical hormone as well as other appropriate treatments should be given.
2．Other adverse reactions.
When the following adverse reactions occur, discontinue the medication and appropriate treatment is performed if necessary.
Contraindication
1. Do not use this product in patients who are allergic to lansoprazole and any ingredient of it.
2. Patients using atazanavir sulfate are prohibited from using this product.
Precaution
1. The following patients were careful medication:(1)Patients with past history of drug allergy;(2)Patients with liver damage.
2. This product will cover up the symptoms of digestive tract tumors, and it should be used after excluding malignant tumor.
3. Closely observe the condition when the product is used, and other measures should be appliedif the treatment fails.
4. There is currently no more than 7 days of medication experience for this product.
5. The same kind of proton pump inhibitor omeprazole has caused visual impairment in foreign countries, while for this product, it is not yet clear.
6. In animal experiments, on rats, benign testicular stromal cell tumors, carcinoid tumors and retinal atrophy appeared after extensive use of the product for a long time. However, similar phenomena did not appear in carcinogenicity tests in mice, toxicity tests in dogs and monkeys.
Medication for pregnant and lactating women
Oral administration of lansoprazole in rats showed that the lansoprazole drug concentration in the fetal plasma was higher than that in the maternal plasma. In addition, an increase in fetal death rate was observed in rabbits (orally, 30 mg/kg/day).For pregnant women and women who may be pregnant, it is advisable to use this product only if it is judged that the benefit of the treatment is greater than the risk. Test results of Lansoprazole oral administration in rats showed that Lansoprazole was secreted from human milk. It is recommended that breast-feeding women avoid using this product as much as possible and stop breast-feeding under the condition that they must be used.
Child medication
The safety of children using this product has not been determined and there is no experience in using it.
Elderly medication
The physiological function of the elderly is generally reduced, so medication should be used with caution.
Medicine interactions
Lansoprazole is metabolized by the liver cytochrome P450 enzyme system, particularly the CYP3A4 and CYP2C19 enzymes. Lansoprazole can significantly and long-term inhibit gastric acid secretion, so it can theoretically promote or inhibit the absorption of some drugs。
Incompatibility
Overdose
There is currently no clinical experience of drug overdose for reference, but lansoprazole cannot be removed from the circulatory system by hemodialysis.
Pharmacology and toxicology
Pharmacologic action
Lansoprazole is a proton pump inhibitor. After it is distributed in the acidic environment of the gastric mucosal wall cells, it will be transformed into active metabolites.This metabolite binds to the sulfhydryl of H+, K+-ATPase enzyme exists the acid-generating site and inhibits the secretion of gastric acid by inhibiting the activity of the H+, K+-ATPase. Lansoprazole inhibited the secretion of gastric acid in a dose-dependent manner, within 24 hours after drug administration it shows a inhibition of gastric acid secretion caused by basal and stimuli was inhibited. A healthy adult is administrated once 30mg, 2 times a day, and the sustained inhibition of gastric acid secretion can be observed. It has been reported that blood coagulation and platelet aggregation are greatly impaired under acidic conditions. The fibrin formed by blood coagulation can be dissolved by pepsin under acidic conditions. The drug improves blood coagulation and platelet aggregation by raising the pH in the stomach, inhibits the activity of pepsin and inhibits bleeding. In addition, under acidic conditions, repair of the damaged mucosa of the stomach is inhibited. The drug increases gastric pH by inhibiting acid secretion and promotes the repair of damaged mucous membranes.
Toxicological research
Genotoxicity: All results of Ames test, rat liver cell program DNA synthesis test, mouse micronucleus test and rat bone marrow cell chromosome aberration test were negative. Results of In vitro human lymphocyte chromosome aberration test are positive.
Reproductive toxicity: Rats and rabbits were given lansoprazole intravenously at a dose of 30mg/kg/day (8 times and 16 times the clinical recommended dose based on body surface area), and no adverse effects on fertility and embryos were found.
Oncogenicity:After oral administration of lansoprazole 5-150mg/kg/day for 24 months in SD rats (1 to 40 times the clinical recommended dose of 30mg/d equivalent to a 50kg patient based on body surface area), the results showed thatlansoprazole induced gastrointestinal chromophilic-like (ECL) cell proliferation and benign ECL cell tumors in a dose-dependent manner; the occurrence of intestinal epithelialization in the gastric epithelium of the test animals was increased. The incidence of testicular stromal cell adenomas in male rats increased in a dose-related manner. In rats with the dosages of 15 to 150mg/kg/day (4 to 40 times the human clinical recommended dose based on body surface area), the incidence of these adenomas exceeds the natural incidence of this strain of rats (1.4 ~10%).In a one-year toxicity study, one of the 30 rats dosed at 50 mg/kg/day (13 times the human clinical recommended dose based on body surface area) had testicular stromal cell adenomas. CD-1 mice were orally administered with lansoprazole 15 to 600mg/kg/day for 24 months (2~80 times the human clinical recommended dose based on body surface area), and the results showed that lansoprazole induced ECLhyperplasia in a dose-dependent manner, liver tumors incidence increased in mice and the incidence of tumors in the 300 and 600mg/kg/day male mice and 150 to 600mg/kg/day female mice exceeded the incidence of historical tumors in this germline mouse group. Lansoprazole was administered at 75-600mg/kg/day and testicular adenomas developed in mice.
Pharmacokinetics
Absorption When lansoprazole is administered intravenously, there are individual differences in serum concentration. In healthy individuals, lansoprazole was administered intravenously 30mg (30min), the plasma concentration showed a double exponential reduction with a terminal half-life of 1.3 (±0.5) h, the peak plasma concentration (Cmax) of 1705 (±292) ng/mL and the area under the curve (AUC) of 3192 (±1745) ng•h/mL. Once daily oral or intravenous lansoprazole of 30mg, the pharmacokinetic parameters after 7 days did not change with time.12 healthy adult men were divided into fast metabolizer group and slow metabolizer group according to the CYP2C19 genotype, intravenous infusion once 30mg, twice daily and for 5 days, the main pharmacokinetic parameters are shown in the following table.
Time/Parameters
In patients with different degrees of chronic liver disease, the average drug half-life of orally administered lansoprazole was extended from 1.5 hours to 3.2~7.2 hours. In patients with hepatic injury homeostasis, the AUC can be increased to 500% when compared with healthy subjects, so the dose of intravenous administration should be reduced in patients with severe hepatic impairment. Oral lansoprazole studies suggest that there is no difference in the pharmacokinetics of patients with gender and renal insufficiency, so intravenous administration does not require dose adjustment.
Distribution The apparent volume of lansoprazole is approximately 15.7(±1.9)L, and is mainly distributed in the extracellular fluid. The plasma protein binding rate was 97%, and plasma protein binding was constant when the plasma concentration was 0.05-5.0 μg/mL.
Metabolism The plasma elimination half-life of lansoprazole is not related to the duration of action for inhibiting gastric acid secretion. The elimination half-life of lansoprazole is less than 2 hours, and duration of action for inhibiting gastric acid secretion is at least 24 hours. Lansoprazole is metabolized by the cytochrome P450 enzyme system, particularly the CYP2C19 enzyme and the CYP3A4 enzyme. According to reports, there is a genetic polymorphism in CYP2C19, and about 10% to 20% of Mongolian species in Asia are slow metabolizers. Lansoprazole is extensively metabolized in the liver and two major metabolites (hydroxylated sulfinyl and sulfo derivatives) can be detected in plasma. These metabolites are only converted into two active components that inhibit the H+, K+-ATPenzymein the gastric parietal tubules, but they are not detectable in the systemic circulation.
EliminationThe average clearance rate of intravenous injection of lansoprazole was 11.1 (±3.8) L/h.In healthy adult men, once intravenous administration of 30mg, no prototype drug was detected in urine and all were metabolites, and the cumulative urinary excretion rate was 12% to 17% after 24 hours from the end of administration.An oral 14C-labeled lansoprazole study showed that about 1/3 of the dose (radioactivity) was excreted in the urine and about 2/3 of the radioactive material was in the faeces, suggesting that the metabolites of lansoprazole excreted through Bile and urine
Storage
Kept under a condition of sealed, free from light and not exceed 25oC.
Packaging
Unopened glass vials, 1vial/box, 6vials/box and 10vials/box.
Shelf life
24 months
Specification
YBH03402014and ChP (2015)
Approval number
GUOYAOZHUNZI H20143293
Active ingredient:Lansoprazole
Excipient:Mannitol, meglumine and sodium hydroxide
Chemical name: 2-[[[3- methyl-4-(2，2，2- trifluoroethoxyl)-2- pyridine] methyl] sulfinyl]-1H- benzimidazole
Chemical structure:
Molecular formula: C16H14F3N3O2S
Molecular weight: 369.36
Description
White or off-white porous mass.
Indications
Treatment for duodenal ulcer associated with hemorrhage while not suitable for oral administration.
Strength
30mg
Dosage and administration
Intravenous infusionis applied, normally 30mg for adults once and 2 times a day for no more than 7 days.Once the patient can take the drug orally, lansoprazole oral preparation should be used for a change. Prior to use, add 5ml of sterile water for injection into the vial to dissolve the content completely, next be added into a 100ml of 0.9% sodium chloride injection for dilution, and then followed by intravenous infusion. The recommended administration time should be not less than 30 minutes.
Precaution
(1)When using this product in intravenous infusion, a filter with a pore size of 1.2μm should be provided in order to remove precipitates that may be generated during infusion. These precipitates may cause microvascular embolism with serious consequences.
(2)In any dangerous cases where there is an eruptive or gushing bleeding or vascular exposure, endoscopic hemostasis should be used.
(3)This product is only used for intravenous infusion. After dissolution, it should be used immediately and storage is prohibited. Mixing for intravenous infusion with liquids other than 0.9% sodium chloride injection and other drugs is not allowed.
(4)If the hemostatic effect is achieved within the first 3 days after treatment with this product, oral administration should be used instead of intravenous administration. Unlimited intravenous administration is not allowed.
Adverse reaction
In domestic clinical studies, this product was used twice a day, each time 30mg for intravenous infusion and 7 days of treatment course. In 109 subjects, two adverse events occurred with symptoms of dizziness, abdominal discomfort, and diarrhea. After the introduction of lansoprazole for injection in foreign countries, more than 1,000 patients are well tolerated after use. In the United States, after using lansoprazole for injection in 161 patients in four clinical trials, adverse reactions of more than 1% includingnausea (1.3%), headache (1%) and pain at the injection site (1%) occurred; while less than 1% including abdominal pain, diarrhea, dyspepsia, vomiting, dizziness, paresthesia, abnormal taste, skin rashand vasodilation occurred. No adverse effects different from oral administration occurred. Japanese clinical research data reported that after 221 subjects used lansoprazole for injection, 31 cases (14.0%) had abnormal clinical laboratory tests, mainly alanine aminotransferase (ALT) elevation (6.2%), aspartate aminotransferase (AST) elevation (5.7%), lactate dehydrogenase (LDH) elevation (2.0%), γ-glutamyl transferase (γ-GGT) elevation (1.5%) ) and so on.The following adverse reactions arecommon with oral lansoprazole, whileit may also occur during intravenous injection.
1.The medication course should be closely observed. If any of the following serious adverse reactions occur, the medication should be stopped in time and treat it appropriately.
(1)Allergic reactions (systemic rash, facial edema, dyspnea, etc.) (<0.1%) and even shock (<0.1%)
(2)Pancytopenia and agranulocytosis, hemolysis (<0.1%), neutropenia, thrombocytopenia, anemia (0.1% to <5%);
(3)Severe hepatic impairment with jaundice, elevated AST and ALT (<0.1%);
(4)Toxic epidermal necrolysis (Lyell syndrome), mucocutaneous ophthalmopathy syndrome (Stevens-Johnson syndrome) (<0.1%);
(5)Interstitial pneumonia (<0.1%), fever, cough, dyspnea, abnormal breath sounds in the lungs (acute pronunciation) and so on; discontinue the medication quickly, thenchest X-ray examination is performed and adrenocortical hormone as well as other appropriate treatments should be given.
2．Other adverse reactions.
When the following adverse reactions occur, discontinue the medication and appropriate treatment is performed if necessary.
|
Adverse Effects Rate |
0.1~＜5% |
<0.1% |
|
1）Anaphylaxis |
Rash, itching |
-- |
|
2）Liver |
AST, ALT, Al-P,LDH and γ-GTP elevation |
-- |
|
3）Blood system |
· Eosinophilia |
Eosinophilia |
|
4）Digestive system |
Constipation, diarrhea, dry mouth and bloating |
Nausea, vomiting, loss of appetite, abdominal pain, candidiasis, stomatitis, glossitis and dysgeusia |
|
5）Mental nervous system |
Headache, lethargy |
Depression, insomnia, vertigo, tremor |
|
6）Others |
Fever, total cholesterol and uric acid elevation |
Men's female breasts, blurred vision, edema, weakness, tongue, numbness of the lips, numbness of the extremities, joint pain, muscle pain and hair loss. |
1. Do not use this product in patients who are allergic to lansoprazole and any ingredient of it.
2. Patients using atazanavir sulfate are prohibited from using this product.
Precaution
1. The following patients were careful medication:(1)Patients with past history of drug allergy;(2)Patients with liver damage.
2. This product will cover up the symptoms of digestive tract tumors, and it should be used after excluding malignant tumor.
3. Closely observe the condition when the product is used, and other measures should be appliedif the treatment fails.
4. There is currently no more than 7 days of medication experience for this product.
5. The same kind of proton pump inhibitor omeprazole has caused visual impairment in foreign countries, while for this product, it is not yet clear.
6. In animal experiments, on rats, benign testicular stromal cell tumors, carcinoid tumors and retinal atrophy appeared after extensive use of the product for a long time. However, similar phenomena did not appear in carcinogenicity tests in mice, toxicity tests in dogs and monkeys.
Medication for pregnant and lactating women
Oral administration of lansoprazole in rats showed that the lansoprazole drug concentration in the fetal plasma was higher than that in the maternal plasma. In addition, an increase in fetal death rate was observed in rabbits (orally, 30 mg/kg/day).For pregnant women and women who may be pregnant, it is advisable to use this product only if it is judged that the benefit of the treatment is greater than the risk. Test results of Lansoprazole oral administration in rats showed that Lansoprazole was secreted from human milk. It is recommended that breast-feeding women avoid using this product as much as possible and stop breast-feeding under the condition that they must be used.
Child medication
The safety of children using this product has not been determined and there is no experience in using it.
Elderly medication
The physiological function of the elderly is generally reduced, so medication should be used with caution.
Medicine interactions
Lansoprazole is metabolized by the liver cytochrome P450 enzyme system, particularly the CYP3A4 and CYP2C19 enzymes. Lansoprazole can significantly and long-term inhibit gastric acid secretion, so it can theoretically promote or inhibit the absorption of some drugs。
Incompatibility
|
Drug name |
Clinical manifestation |
Mechanism of action, risk factors |
|
Atazanavir sulfate |
It may weaken the efficacy of atazanavir sulfate. |
This product's inhibition of gastric acid secretion can reduce the solubility of atazanavir and reduce the plasma concentration. |
|
Theophylline |
The plasma concentration of theophylline decreased. |
This product induces drug metabolizing enzymes in the liver that can promote the metabolism of theophylline. |
|
Tacrolimus |
The plasma concentration of tacrolimus increases. |
This product can competitively block the metabolism of tacrolimus by hepatic drug metabolizing enzymes. |
|
Digoxin and Metildigoxin |
There is the possibility of enhancing the effect of drugs. |
Due to the inhibitory effect of this product on gastric acid secretion, digoxin hydrolysis is inhibited, which may raise the blood drug concentration. |
|
Itraconazole, Gefitinib |
There is a possibility of weakening the drug effect. |
Due to the inhibition of gastric acid secretion of this product, there is a possibility that the plasma concentration of the drug may decrease. |
|
Phenytoin and diazepam |
-- | Omeprazole has been reported to delay drug metabolism and excretion. |
There is currently no clinical experience of drug overdose for reference, but lansoprazole cannot be removed from the circulatory system by hemodialysis.
Pharmacology and toxicology
Pharmacologic action
Lansoprazole is a proton pump inhibitor. After it is distributed in the acidic environment of the gastric mucosal wall cells, it will be transformed into active metabolites.This metabolite binds to the sulfhydryl of H+, K+-ATPase enzyme exists the acid-generating site and inhibits the secretion of gastric acid by inhibiting the activity of the H+, K+-ATPase. Lansoprazole inhibited the secretion of gastric acid in a dose-dependent manner, within 24 hours after drug administration it shows a inhibition of gastric acid secretion caused by basal and stimuli was inhibited. A healthy adult is administrated once 30mg, 2 times a day, and the sustained inhibition of gastric acid secretion can be observed. It has been reported that blood coagulation and platelet aggregation are greatly impaired under acidic conditions. The fibrin formed by blood coagulation can be dissolved by pepsin under acidic conditions. The drug improves blood coagulation and platelet aggregation by raising the pH in the stomach, inhibits the activity of pepsin and inhibits bleeding. In addition, under acidic conditions, repair of the damaged mucosa of the stomach is inhibited. The drug increases gastric pH by inhibiting acid secretion and promotes the repair of damaged mucous membranes.
Toxicological research
Genotoxicity: All results of Ames test, rat liver cell program DNA synthesis test, mouse micronucleus test and rat bone marrow cell chromosome aberration test were negative. Results of In vitro human lymphocyte chromosome aberration test are positive.
Reproductive toxicity: Rats and rabbits were given lansoprazole intravenously at a dose of 30mg/kg/day (8 times and 16 times the clinical recommended dose based on body surface area), and no adverse effects on fertility and embryos were found.
Oncogenicity:After oral administration of lansoprazole 5-150mg/kg/day for 24 months in SD rats (1 to 40 times the clinical recommended dose of 30mg/d equivalent to a 50kg patient based on body surface area), the results showed thatlansoprazole induced gastrointestinal chromophilic-like (ECL) cell proliferation and benign ECL cell tumors in a dose-dependent manner; the occurrence of intestinal epithelialization in the gastric epithelium of the test animals was increased. The incidence of testicular stromal cell adenomas in male rats increased in a dose-related manner. In rats with the dosages of 15 to 150mg/kg/day (4 to 40 times the human clinical recommended dose based on body surface area), the incidence of these adenomas exceeds the natural incidence of this strain of rats (1.4 ~10%).In a one-year toxicity study, one of the 30 rats dosed at 50 mg/kg/day (13 times the human clinical recommended dose based on body surface area) had testicular stromal cell adenomas. CD-1 mice were orally administered with lansoprazole 15 to 600mg/kg/day for 24 months (2~80 times the human clinical recommended dose based on body surface area), and the results showed that lansoprazole induced ECLhyperplasia in a dose-dependent manner, liver tumors incidence increased in mice and the incidence of tumors in the 300 and 600mg/kg/day male mice and 150 to 600mg/kg/day female mice exceeded the incidence of historical tumors in this germline mouse group. Lansoprazole was administered at 75-600mg/kg/day and testicular adenomas developed in mice.
Pharmacokinetics
Absorption When lansoprazole is administered intravenously, there are individual differences in serum concentration. In healthy individuals, lansoprazole was administered intravenously 30mg (30min), the plasma concentration showed a double exponential reduction with a terminal half-life of 1.3 (±0.5) h, the peak plasma concentration (Cmax) of 1705 (±292) ng/mL and the area under the curve (AUC) of 3192 (±1745) ng•h/mL. Once daily oral or intravenous lansoprazole of 30mg, the pharmacokinetic parameters after 7 days did not change with time.12 healthy adult men were divided into fast metabolizer group and slow metabolizer group according to the CYP2C19 genotype, intravenous infusion once 30mg, twice daily and for 5 days, the main pharmacokinetic parameters are shown in the following table.
Time/Parameters
|
Time/Parameters |
CYP2C19 metabolic type |
AUC0~12 (ng·h/mL) |
Cmax (ng/mL) |
T1/2 (h) |
|
1 day |
Fast metabolizer group |
4386±1335 |
2262±354 |
1.5±0.4 |
|
1 day |
Slow metabolizer group |
10415±1159 |
2727±315 |
4.0±0.7 |
|
5 days |
Fast metabolizer group |
4939±1541 |
2414±406 |
1.6±0.5 |
|
5 days |
Slow metabolizer group |
12579±1939 |
3134±316 |
4.2±1.1 |
Distribution The apparent volume of lansoprazole is approximately 15.7(±1.9)L, and is mainly distributed in the extracellular fluid. The plasma protein binding rate was 97%, and plasma protein binding was constant when the plasma concentration was 0.05-5.0 μg/mL.
Metabolism The plasma elimination half-life of lansoprazole is not related to the duration of action for inhibiting gastric acid secretion. The elimination half-life of lansoprazole is less than 2 hours, and duration of action for inhibiting gastric acid secretion is at least 24 hours. Lansoprazole is metabolized by the cytochrome P450 enzyme system, particularly the CYP2C19 enzyme and the CYP3A4 enzyme. According to reports, there is a genetic polymorphism in CYP2C19, and about 10% to 20% of Mongolian species in Asia are slow metabolizers. Lansoprazole is extensively metabolized in the liver and two major metabolites (hydroxylated sulfinyl and sulfo derivatives) can be detected in plasma. These metabolites are only converted into two active components that inhibit the H+, K+-ATPenzymein the gastric parietal tubules, but they are not detectable in the systemic circulation.
EliminationThe average clearance rate of intravenous injection of lansoprazole was 11.1 (±3.8) L/h.In healthy adult men, once intravenous administration of 30mg, no prototype drug was detected in urine and all were metabolites, and the cumulative urinary excretion rate was 12% to 17% after 24 hours from the end of administration.An oral 14C-labeled lansoprazole study showed that about 1/3 of the dose (radioactivity) was excreted in the urine and about 2/3 of the radioactive material was in the faeces, suggesting that the metabolites of lansoprazole excreted through Bile and urine
Storage
Kept under a condition of sealed, free from light and not exceed 25oC.
Packaging
Unopened glass vials, 1vial/box, 6vials/box and 10vials/box.
Shelf life
24 months
Specification
YBH03402014and ChP (2015)
Approval number
GUOYAOZHUNZI H20143293
