2 English reference buscopan
3. Clean Genie in Pharmacopoeia 3. 1 Product Name 3. 1. 1 Chinese Name Clean Genie
3. 1.2 Chinese Pinyin Ding Xiudong Lang Dangjian
3. 1.3 English name scopolamine butyl bromide
3.2 structural formula 3.3 molecular formula and molecular weight C2 1H30BrNO4? 440.38
3.4 Source (name) and content (potency) This product is 6β, 7β epoxy 3a hydroxyl 8 butyl 1αH, 5αH tropine (i) tropine bromide. The content of C2 1H30BrNO4 should be no less than 99.0% in terms of dry products.
3.5 Properties This product is white or white-like crystalline powder; Tasteless or almost tasteless.
This product is soluble in water or chloroform and slightly soluble in ethanol.
3.5. 1 Take this product with specific rotation, accurately weigh it, dissolve it in water, dilute it quantitatively, make a solution containing about 0. 1 gram per1ml, and determine it according to law (Appendix 6 E of Pharmacopoeia Part II, 20 10), with the specific rotation range of/kloc-
3.6 Identification (1) Take this product, add 0.0 1mol/L hydrochloric acid solution to dissolve and dilute it, make a solution containing 1mg per 1ml, and determine it by ultraviolet-visible spectrophotometry (Appendix 4A of Pharmacopoeia II, 20 10 edition). At 252 nm and 257 nm,
(2) The infrared absorption spectrum of this product should be consistent with the control spectrum (Figure 2 1 of the infrared spectrum of drugs).
(3) Identification reaction of tropine alkaloids in this product (Appendix III of Pharmacopoeia II, 20 10 edition).
(4) Identification reaction of bromide in aqueous solution of this product (Appendix III of Pharmacopoeia II, 20 10 edition).
3.7 Check the acidity of 3.7. 1 Take this product, add water to make a solution containing 0. 1g per 1ml, and measure it according to law (Appendix VI H of Pharmacopoeia II, 20 10), and the pH value should be 5.5 ~ 6.5.
3.7.2 Solution clarity Take 0.5g of this product, add 15ml water to dissolve, and the solution should be clarified.
3.7.3 Take the related substances of this product, weigh them accurately, add mobile phase to dissolve them, and make a solution containing 2.5mg per 1ml as the test solution; Take scopolamine hydrobromide reference substance, accurately weigh it, make a solution containing 0.0 1mg per 1ml with mobile phase as the reference substance solution, take 1ml as the test solution, put it in a 10ml volumetric flask, dilute it to scale with the reference substance solution, and shake it evenly as the system suitability test solution. According to high performance liquid chromatography (Appendix V D of Pharmacopoeia Part II, 20 10), octadecylsilane bonded silica gel was used as filler, and 0.008mol/L sodium dodecyl sulfate solution prepared from 0.004% phosphoric acid solution and acetonitrile (50: 50) was used as mobile phase, and the detection wavelength was 2 10nm. Inject the system adaptability test solution of 10μl into the liquid chromatograph, and adjust the detection sensitivity so that the peak height of scopolamine hydrobromide chromatographic peak is about 20% of the full scale. According to the calculation of spasmolysis peak, the number of theoretical plates is not less than 3,000, and the resolution of spasmolysis peak and scopolamine hydrobromide peak should meet the requirements. Accurately measure 10μl of test solution and reference solution, inject them into liquid chromatograph respectively, and record the chromatogram until the retention time of the principal component peak is twice. If there is a chromatographic peak with the same retention time as the scopolamine hydrobromide peak in the chromatogram of the test sample, its peak area shall not be larger than the main peak area of the reference solution (0.4%); The total area of each impurity peak (excluding the bromine ion peak near the solvent peak) shall not exceed 2 times (0.8%) of the main peak area of the reference solution.
3.7.4 loss on drying takes this product and dries it to constant weight at 105℃, and the weight loss shall not exceed 2.5% (Appendix VIII L of Pharmacopoeia II, 20 10).
3.7.5 residue on ignition shall not exceed 0. 1% (Appendix VIII N of Pharmacopoeia II, 20 10).
3.8 Content determination: Take about 0.25g of this product, weigh it accurately, add 50ml of water to dissolve it, potentiometric titration (Appendix ⅶ A of Pharmacopoeia II, 20 10), titrate with silver electrode and silver nitrate titrant (0. 1mol/L). Every 1ml silver nitrate titration solution (0. 1mol/L) is equivalent to 44.04mg C2 LH 30 Brno 4.
Class 3.9 anticholinergic drugs.
3. 10 storage and shading, sealed preservation.
3. 1 1 preparation (1) jiejingling injection? (2) Jiejingling Capsule
3. 12 Edition People's Republic of China (PRC) Pharmacopoeia 20 10 Edition
4 Description of Jiejing Ling 4. 1 Drug Name Jiejing Ling
4.2 English name scopolamine butyl bromide
4.3 Jiejing Ling alias butyryl ketone; Scopolamine butylbromide; Bromobutyric acid ester; Scopolamine bromide; Scopolamine butyl bromide; Pina, Busca; Buscopan; Scopolamine ethidium bromide; scopolamine n butyl bromide
4.4 classification of digestive system drugs >; Gastrointestinal antispasmodic
4.5 dosage form10 mg; ;
2. Capsule:10 mg; ;
3. Injection: 1 0mg (1 ml), 20mg (1ml), 20mg (2ml);
4. Solution: 5mg(5ml).
4.6 drug understanding of Jiejingling Jingling is a peripheral anticholinergic drug, which not only has spasmolytic effect on smooth muscle, but also blocks ganglion and neuromuscular junction, but has weak effect on central nervous system. The antispasmodic effect of Jiejingling on intestinal smooth muscle is stronger than that of atropine and anisodamine, and it can selectively relieve spasm and inhibit the peristalsis of smooth muscle of gastrointestinal tract, biliary tract and urinary tract, but has less effect on heart, pupil and salivary gland, so atropine causes less adverse reactions such as central nervous system excitement, dilated pupils and inhibition of saliva secretion.
4.7 Pharmacokinetics of Jiejingling The oral absorption of Jiejingling is poor, and it is absorbed quickly after intramuscular injection or intravenous injection. It takes effect 2 ~ 4 minutes after intravenous injection, 8 ~ 10 minutes after subcutaneous or intramuscular injection, 20 ~ 30 minutes after oral administration, and the drug effect lasts about 2 ~ 6 hours. Intestinal and hepatic circulation, not easy to penetrate the blood cerebrospinal fluid barrier. Almost all of it is metabolized in the liver, mainly excreted by feces, and a small part is excreted by the kidney in its original form.
4.8 indications of jiejingling 1. It can be used for treating gastrointestinal spasm, biliary colic, renal colic or gastrointestinal peristalsis caused by various reasons. It can also be used for uterine spasm.
2. It is used for preoperative preparation of endoscopy of stomach, duodenum and colon to reduce intestinal peristalsis.
3. Used in endoscopic retrograde cholangiopancreatography to inhibit intestinal peristalsis before or during operation.
4. It is used for gas barium hypotonic radiography of stomach, duodenum and colon or abdominal CT scanning to reduce or inhibit intestinal peristalsis.
4.9 Contraindications of Jiejing Ling 1. Severe heart disease.
2. Organic pyloric stenosis.
3. Paralytic intestinal obstruction.
4. glaucoma.
5. Prostate hypertrophy (even urinary retention).
6. It is not suitable for symptoms such as low gastric tension, gastric dyskinesia (gastroparesis), epigastric pain and heartburn caused by gastroesophageal reflux.
4. 10 Precautions 1. (1) baby. (2) Patients with low blood pressure.
2. Jiejing Ling and alkaline potions are incompatible.
3. The speed of intravenous injection should not be too fast.
4. 1 1 Adverse reactions of Jiejing Elf Most of the adverse reactions of Jiejing Elf are related to their anticholinergic properties, such as thirst, impaired vision, drowsiness, palpitation, facial flushing, nausea, vomiting, dizziness and headache. Jiejingling can also reduce the pressure of lower esophageal sphincter (LES), so it can promote gastroesophageal reflux. People who also have allergic reactions. It is easy to have dysuria and even mental disorder when high dose is used.
4. Usage and dosage of 1 2 antispasmodic1. (1) tablets and capsules: each time 10 ~ 20 mg, 3 ~ 5 times a day, which should be swallowed whole or whole. (2) Oral liquid: each time 10mg, 3-5 times a day.
2. intramuscular injection: 20 ~ 40mg each time, or 20mg each time after 20 ~ 30 minutes. When acute colic attacks, 20 mg each time, several times a day.
3. Intravenous drip: dissolve Jiejingling in 5% glucose injection or 0.9% sodium chloride injection for intravenous drip, 20 ~ 40mg each time, or 20mg each time, with an interval of 20 ~ 30 minutes. When acute colic attacks, 20 mg each time, several times a day.
4. 13 drug interaction 1. Tricyclic antidepressants, quinidine and amantadine can enhance the anticholinergic effect of Jiejingling when administered by injection.
2. Jiejing Ling cannot be combined with domperidone, metoclopramide, cisapride and other prokinetic drugs, because they will antagonize each other.
4. 14 Expert opinion