What Is Bisacodyl?

Bisacodyl is a white or almost white crystalline powder, which is odorless and tasteless. This product is easily soluble in chloroform, soluble in acetone, slightly soluble in ethanol or ether, and insoluble in water. Melting point is 131-135ºC. Alias must be attacked; poop stop; bisacetamidine tannate; bispyrmethamine; bisacetanilide; bisphenolate; Bisacodylum; Biscolax; Dulcoalx; Bisacodyl is an irritant laxative, mainly acting on the large intestine, and is used clinically for acute and chronic constipation. Suppository rectal medications can be used for colonoscopy, bowel X-rays, or to clean the bowel before abdominal surgery. ^[1-2]

Drug Name: Bisacodyl
Alias: Will be sprinkled; can be stopped; tannin
Foreign name: Bisacodyl
Main indications: Constipation, cleansing the bowel before and after surgery, and before giving birth
Dosage: See below for details

Adverse reactions: Diarrhea, water and electrolyte abnormalities
Main medication contraindications: People who are allergic to this medicine, acute abdomen, etc.
Dosage form: Tablets, suppositories, effervescent powders
Drug type: chemical
CAS: 603-50-9

Bisacodyl Basic Information

Chinese name

Chinese alias: procaine hydrochloride; bisacetophenidine; 4,4 '-(2-pyridinemethylene) bisphenol diacetate;

English name: Bisacodyl

English alias: LA96A; laco; neolax; zetrax; durolax; laxine; Phenol, 4,4 '-(2-pyridinylmethylene) bis-, diacetate (ester); ivilax; Bicol; deficol; Laxans;

CAS number: 603-50-9 ^[1]

Molecular formula: C22H19NO4

Molecular weight: 361.39100

Chemical Structure:

Exact mass: 361.13100

PSA: 65.49000

LogP: 4.11240 ^[1]

Bisacodyl physicochemical properties

Appearance and properties: white to off-white crystalline powder

Density: 1.2 g / cm3

Melting point: 131-135ºC

Boiling point: 492ºC

Stability: Stable. Incompatible with strong oxidizing agents.

Storage conditions: 2-8ºC ^[1]

Bisacodyl Safety Information

Customs Code: 2942000000

Danger category code: R22; R36 / 37/38

Safety instructions: S26-S36

Dangerous goods mark: Xi ^[1]

Bisacodyl Pharmacopoeia Standard

Bisacodyl

Chinese name: bisacodyl

Phonetic script (Hanyu Pinyin): Bishakeding

English name: Bisacodyl ^[2]

Bisacodyl molecular formula and molecular weight

C22H19NO4 361.40 ^[2]

Bisacodyl source (name), content (potency)

This product is 4,4 '-(2-pyridinemethylene) diphenol diacetate. Calculated based on dry products, containing C22H19NO4 shall not be less than 98.0%. ^[2-3]

Bisacodyl traits

This product is white or off-white crystalline powder; odorless and tasteless.

This product is easily soluble in chloroform, soluble in acetone, slightly soluble in ethanol or ether, and insoluble in water.

3.5.1 melting point

The melting point of this product (Appendix VIC of Part Two of the 2010 Pharmacopoeia) is 132 ~ 136 ° C. ^[2]

Bisacodyl identification

(1) Take this product, add 0.1mol / L methanol-made potassium hydroxide solution to make a solution containing 10g per 1ml, and measure it by ultraviolet-visible spectrophotometry (Appendix IVA of Pharmacopoeia Part II of the 2010 edition) at a wavelength of 248nm There is a maximum absorption at 0.62 0.68.

(2) The infrared absorption spectrum of this product should be the same as that of the control ("Infrared Spectra of Drugs" 35). ^[2-3]

Bisacodyl check

3.7.1 pH

Take 1.0g of this product, add 20ml of water, heat to boiling, cool, filter, and measure the filtrate according to law (Appendix VI H of the second edition of the Pharmacopoeia 2010), the pH value should be 5.0 ~ 7.5.

3.7.2 Related substances

Take this product, add acetone to make a solution containing 20mg per 1ml, and use it as the test solution; take a precise amount, dilute it with acetone to make a solution containing 0.20mg per 1ml, and use it as a control solution. Take another 40mg of this product, add 1ml of acetone, shake to dissolve, add 0.5ml of 30% hydrogen peroxide solution, shake well, let stand for 1 hour, add acetone to dilute to 2ml, shake well, and use it as a system suitability test solution. According to the thin layer chromatography (2010 edition Pharmacopoeia Part II Appendix VB) test, draw 10 l each of the system suitability test solution, the test solution and the control solution, and point them on the same silica gel GF254 thin-layer plate, using xylene-butanone (1: 1) As a developing agent, unfold, dry, and inspect under UV light (254nm). The impurity spots in the system suitability test solution should be clearly separated from the spots of bisacodyl, and the Rf value of bisacodyl should be about 0.7. If the test solution shows obvious impurity spots, it must not be deeper than the main spot of the control solution (1.0%).

Loss on drying

Take this product and dry it at 105 to constant weight, and the weight loss shall not exceed 0.5% (Appendix L of Part Two of the Pharmacopoeia of 2010 Edition).

3.7.4 Ignition residue

Must not exceed 0.1% (Appendix N of Part Two of the 2010 Pharmacopoeia). ^[2-3]

Determination of bisacodyl

Take about 0.3g of this product and accurately weigh it. After dissolving in 25ml of glacial acetic acid, add 2 drops of naphthol benzyl alcohol indicator solution, titrate with perchloric acid titration solution (0.1mol / L) until the solution is yellow-green, and The results are corrected with a blank test. Each 1ml of perchloric acid titration solution (0.1mol / L) is equivalent to 36.14mg of C22H19NO4. ^[2-3]

Bisacodyl Categories

laxative. ^[2-3]

Bisacodyl storage

Shaded and sealed. ^[2-3]

Bisacodyl preparation

(1) bisacodyl enteric-coated tablets (2) bisacodyl suppository ^[2-3]

Overview of Bisacodyl Drug Related Information

Bisacodyl Drug Name

Chinese name

English name: Bisacodyl

Alias: must be sprinkled; can be stopped; bisacetanilide tannate; bispyridine; bisacetanilide; bisphenolate; Bisacodylum; Biscolax; Dulcoalx; Metalax ^[2]

Bisacodyl Classification

Digestive System Drugs> Laxatives ^[2]

Bisacodyl dosage form

1. Tablet: 5mg, 10mg;

2. Suppositories: 5mg, 10mg;

3. Effervescent powder: containing 5mg of bisacodyl. ^[2]

Bisacodyl pharmacological action

Bisacodyl is an irritant laxative that acts primarily on the large intestine. After the oral administration of bisacodyl, the products of intestinal bacterial decomposition and the drug itself have a strong stimulating effect on the intestinal wall, which can stimulate the parasympathetic reflex of sensory nerve endings, causing bowel reflex peristalsis and causing bowel movement. Bisacodyl also stimulates local axonal reflexes and segmental reflexes, and produces extensive colonic peristalsis, so bisacodyl may be effective in patients with ganglion blockage or spinal cord damage (paraplegia, polio). At the same time, bisacodyl can inhibit the absorption of sodium, chlorine and water in the colon, increase the intestinal volume, and cause reflective defecation. Clinical application has confirmed that the use of bisacodyl has no damage to the heart, lungs, liver, kidneys, hematopoietic system and immune system. ^[2] ^[4]

Bisacodyl pharmacokinetics

After meals, oral bisacodyl is effective within 10-12 hours, and rectal administration is effective within 15-60 minutes. After oral administration of bisacodyl, only a small amount is absorbed. After the liver is combined with glucuronic acid, 38% is excreted by the kidney and 3% is excreted by the bile. Unabsorbed drugs are excreted in the stool. Whether bisacodyl is excreted in milk is unclear. ^[2] ^[4]

Bisacodyl indication

1. For the treatment of acute, chronic constipation and habitual constipation.

2. For abdominal X-ray examination or endoscopic examination to clean and empty the bowel.

3. For cleaning the intestine before and after surgery and before delivery. ^[2]

Bisacodyl contraindications

1. Compare those who are allergic to sacodyl.

2. Acute abdomen (appendicitis, gastroenteritis, rectal bleeding, intestinal obstruction).

3. Inflammatory bowel disease.

4. Severe water and electrolyte disorders.

5. Anal rupture or hemorrhoid ulcer.

6. Fecal blockers. ^[2]

Bisacodyl precautions

1. (1) pregnant women, nursing women, children under 6 years of age; (2) sudden and persistent changes in bowel habits.

2. Do not take antacids and milk within 2 hours after taking the medicine. ^[2]

Bisacodyl adverse reactions

Diarrhea is accompanied by severe functional bowel disease, abnormalities of water and electrolytes with hypokalemia, and can produce a dependency on sarcodine, which necessitates an increase in the dose of the drug and severe constipation during withdrawal. ^[2]

Bisacodyl Dosage

1. 5-10mg each time, once a day. Swallow the entire tablet.

2. Rectal administration: 100mg each time, once a day. ^[2]

Interaction of bisacodyl with other drugs

1. Bisacodyl combined with barium enema can assist the diagnosis of patients with colon diseases.

2. Bisacodyl should not be combined with antiarrhythmic drugs (such as amiodarone, bromobenzylamine, propidamine, quinidines, sotalol, etc.) that can produce sharp twists, or non-anti-arrhythmic that can produce sharp twists. Arrhythmic drugs (such as asmizole, benzpredil, sutopril, terfenadine, vinblastine, etc.) are combined, because hypokalemia, one of the adverse reactions of bisacodyl, can induce tip twist and should be switched to Non-irritating laxatives.

3. When bisacodyl is combined with digitalis drugs, hypokalemia, which is one of the adverse reactions of bisacodyl, can induce toxic effects of digitalis drugs, so blood potassium should be monitored during medication.

4. Do not take antacids within 2h before and after taking bisacodyl. ^[2] ^[4]

Bisacodyl Expert Reviews

Clinically used to treat constipation. Effective for both acute and chronic constipation. It is also clinically used before digestive organ examination or before and after surgery. Exclusion of intestinal contents. ^[2]