Rifaximin

Rifaximin - Names and Identifiers

Name	Rifaximin
Synonyms	normix XIFAXAN rifaxidin Rifaximin RIFAXIMIN rifamycinl105 rifamycinl105sv ole-1,15(2h)-dione,25-(acetyloxy)-5,6,21,23-tetrahydroxy-27-methoxy-2,4,11,16 2s-acetyloxy-5,6,21,23-tetrahydroxy-27-methoxy-2,4,11, 16,20,22,24,26-octamethyl-2,7-(epoxypentoeleca(1,11,13)trienimino)benzofuro[4,5-e]pyride[1,2-a]benzimidazole-1,15(2h)-dione 2S-Acetyloxy-5,6,21,23-tetrahydroxy-27-methoxy-2,4,11, 16,20,22,24,26-octamethyl-2,7-(epoxypentoeleca(1,11,13)trienimino)benzofuro[4,5-e]pyride[1,2-a]benzimidazole-1,15(2H)-dione
CAS	80621-81-4
EINECS	617-130-4
InChI	InChI=1/C43H51N3O11/c1-19-14-16-46-28(18-19)44-32-29-30-37(50)25(7)40-31(29)41(52)43(9,57-40)55-17-15-27(54-10)22(4)39(56-26(8)47)24(6)36(49)23(5)35(48)20(2)12-11-13-21(3)42(53)45-33(34(32)46)38(30)51/h11-18,20,22-24,27,35-36,39,48-51H,1-10H3,(H,45,53)/b12-11+,17-15+,21-13-/t20-,22+,23+,24+,27-,35-,36?,39+,43-/m0/s1
InChIKey	NZCRJKRKKOLAOJ-XRCRFVBUSA-N

Rifaximin - Physico-chemical Properties

Molecular Formula	C43H51N3O11
Molar Mass	785.89
Density	1.36±0.1 g/cm3(Predicted)
Melting Point	200-2050C (dec)
Solubility	ethanol: soluble1mg/mL
Appearance	powder
Color	dark orange
Merck	14,8220
pKa	2.83±0.70(Predicted)
Storage Condition	Sealed in dry,Store in freezer, under -20°C
Stability	Hygroscopic
Refractive Index	1.633
Physical and Chemical Properties	Orange powder, soluble in ethanol, acetic acid, ethyl ester, chloroform and toluene, insoluble in water.
Use	Applicable to gram-positive and negative bacteria, aerobic and anaerobic bacteria caused by acute and chronic intestinal infections, Diarrhea syndrome, intestinal flora changes caused by Diarrhea

Rifaximin - Risk and Safety

WGK Germany	2
RTECS	KD1576000
Toxicity	LD50 orally in rats: >2000 mg/kg (Borelli, Bertoli)

Rifaximin - Reference

Reference

1. [IF=4.411] Xin Meng et al."Drug Repurposing for Influenza Virus Polymerase Acidic (PA) Endonuclease Inhibitor."Molecules. 2021 Jan;26(23):7326

Rifaximin - Standard

Authoritative Data Verified Data

This product is -5,6,21,23, 25-pentahydroxy-27-methoxy-2, 4,11,16,20,22,24,26-octamethyl-2, 7-(epoxydecapentyl-[1,11,13] trienimino) benzofurano [4,5-e] pyrido [1,2-a]-benzimidazole-1, 15(2H)-Dione, 25-acetate. Rifaximin (C43H51N3O11) shall not be less than 95.0% calculated on a dry basis.

Last Update：2024-01-02 23:10:35

Rifaximin - Trait

Authoritative Data Verified Data

This product is orange-red to dark-red crystalline powder; Odorless.
This product is soluble in methanol and acetonitrile, soluble in ethanol, and almost insoluble in O.lmol/L hydrochloric acid solution or water.

Last Update：2022-01-01 11:58:09

Rifaximin - Differential diagnosis

Authoritative Data Verified Data

in the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the rifaximin control solution.
The infrared absorption spectrum of this product should be consistent with that of the reference substance (General rule 0402).

Last Update：2022-01-01 11:58:09

Rifaximin - Exam

Authoritative Data Verified Data

crystallinity

take a small amount of this product, according to the law inspection (General Principles 0981-law), should comply with the provisions.

pH

take this product, add water to make a suspension containing about 10 mg per lml, and determine it according to law (General 0631). The pH value should be 4.5~7.5.

Related substances

new system for clinical use. Take an appropriate amount of this product, precision weigh, add mobile phase to dissolve and quantitatively dilute to make a solution containing about 0.4mg per lml, as a test solution; Precision weigh an appropriate amount of rifaximin reference substance, the mobile phase was added to dissolve and quantitatively dilute to prepare a solution containing about 4ug per 1 ml as a control solution. The appropriate amount of the control solution was accurately taken, and the solution containing about 0.2ug per 1 ml was prepared by quantitative dilution with the mobile phase as the sensitivity solution. According to the chromatographic conditions under the content determination item, the sensitivity solution 20u1 is injected into the human liquid chromatograph, and the signal-to-noise ratio of the peak height of the principal component chromatography should be greater than 10. 20 u1 of the test solution and the control solution were respectively injected into the human liquid chromatograph, and the chromatogram was recorded until the impurity B Peak (relative retention time is about 4) was completely eluted. If there are impurities in the chromatogram of the test solution
Peak, calculated according to the external standard method for the peak area of rifaximin, the single impurity should not exceed 1.0%, the total amount of impurities should not exceed 3.0%. The peaks in the chromatogram of the test solution which are smaller than the main peak area of the sensitivity solution are ignored.

residual solvent

precision weigh about 0.1g of this product, put it in 10ml headspace bottle, Precision Add internal standard solution (precision weigh the right amount of methyl ethyl ketone, use N ,N-dimethylformamide diluted into a solution containing about 0.2mg per lml, shake well) lml, shake to dissolve, seal, as a test solution; Another precision weighing ethanol, dichloromethane, the appropriate amount of n-hexane, n-butanol, toluene and butyl acetate were quantitatively diluted with internal standard solution to prepare ethanol, dichloromethane, n-hexane, n-butanol, toluene and butyl acetate in each lml, which were about 0.5mg, respectively, 0.06mg, 0.029mg, 0.5mg, 0.089mg and 0861 mg of mixed solution, take the precision of 1ml in 10ml headspace bottle, sealed, as a reference solution according to the residual solvent determination method (General Principles of the second method) assay. A capillary column with 100% dimethylpolysiloxane (or similar polarity) as a stationary liquid is a chromatographic column, the initial temperature is 40°C, and the temperature is maintained for 4 minutes, and the temperature is raised to 100°C at a rate of 10°C per minute for 2 minutes. The inlet temperature was 200°C and the detector temperature was 250°C; The headspace bottle equilibrium temperature was 80°C and the equilibrium time was 20 minutes. The reference solution was injected in Headspace, and the chromatogram was recorded. The peak sequence was ethanol, dichloromethane, butanone (internal standard), N-hexane, N-butanol, toluene, N,N-dimethylformamide (solvent). And butyl acetate, the separation between the peaks should meet the requirements. The test solution and the reference solution were injected into the headspace, the chromatogram was recorded, and the peak area ratio was calculated according to the internal standard method. Ethanol, dichloromethane, n-hexane, n-butanol, residual amounts of toluene and butyl acetate shall be as specified.

loss on drying

take this product, dry to constant weight at 105°C, weight loss shall not exceed 4.5% (General rule 0831).

ignition residue

lg of this product shall be taken for inspection according to law (General rule 0841), and the remaining residue shall not exceed 0.1%.

Heavy metals

The residue left under the item of taking the ignition residue shall not contain more than 20 parts per million of heavy metal when examined by law (General rule 0821, Law II).

Last Update：2022-01-01 11:58:10

Rifaximin - Content determination

Authoritative Data Verified Data

The new system is in use. Determined by high performance liquid chromatography (General 0512).
chromatographic conditions and system suitability test using octylsilane bonded silica as filler; Using methanol, acetonitrile-buffer [0.O75mol/L potassium dihydrogen phosphate solution -0.5mol/L citric acid solution (55:10)](513:95:392) as mobile phase, the detection wavelength was 240nm. Rifaximin control, impurity A control and impurity B control were dissolved and diluted with mobile phase to make rifaximin about 40ug/lml, for the mixed solution of impurity A about 40ug and impurity B about lOOug, take 20ul injection liquid chromatograph, record the chromatogram, and peak according to the order of impurity A, rifaximin and impurity B, the resolution between the rifaximin peak and the impurity A peak should be greater than 5.0.
the appropriate amount of this product is measured, accurately weighed, dissolved and quantitatively diluted with mobile phase to prepare a solution containing about 40ug per lml, which is used as a sample solution and injected into the liquid chromatograph with precise amount, the chromatogram was recorded until the impurity B peak was completely eluted. An appropriate amount of rifaximin reference substance was taken and determined by the same method. According to the external standard method to calculate the peak area, that is.

Last Update：2022-01-01 11:58:11

Rifaximin - Category

Authoritative Data Verified Data

antibiotics.

Last Update：2022-01-01 11:58:11

Rifaximin - Storage

Authoritative Data Verified Data

sealed and stored in a dry, cool place.

Last Update：2022-01-01 11:58:12

Rifaximin - Rifaximin For Suspension

Authoritative Data Verified Data

This product contains rifaximin (C43H51N3O11) should be 90.0% to 110.0% of the label.

trait

This product is orange-red or dark-red granules and powder.

identification

take an appropriate amount of fine powder of this product, add methanol to dissolve and dilute to prepare a solution containing about 10 mg of rifaximin per 1 ml, shake well, filter, and use as a test solution; an appropriate amount of rifaximin control was taken, dissolved in methanol and diluted to prepare a solution containing about 10 mg per 1 ml as a control solution. According to the thin layer chromatography (General rule 0502) test, absorb 10 u1 of each of the above two solutions, respectively point on the same silica gel GF254 thin layer plate, with dichloromethane-methanol (95:5) as the developing solvent, it was unfolded, taken out, dried, dried at 105 ° C. For 30 minutes, and examined under a UV lamp (254nm). The position and color of the main spot displayed by the test solution should be consistent with the position and color of the main spot of the reference solution.
in the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
two items (1) and (2) above can be selected as one item.

examination

new system of related substances in clinical use. Weigh the appropriate amount of fine powder (equivalent to rifaximin 40mg) under the content determination item, put it in a 100ml measuring flask, add the appropriate amount of mobile phase, and fully shake to dissolve rifaximin, dilute with the mobile phase to the scale, shake, filter, take the filtrate as the test solution; Take 1ml with precision, put it in a 100ml measuring flask, dilute with the mobile phase to the scale, shake, as a control solution. The appropriate amount of control solution was taken accurately, and a solution containing about 0.2ug of rifaximin per 1ml was prepared by quantitative dilution with mobile phase as a sensitivity solution. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than the area of the main peak of the control solution (1.0% ) , the sum of each impurity peak area shall not be greater than 3 times (3.0%) of the main peak area of the control solution.
dissolution: according to the dissolution and release determination method (General rule 0931 second method), 0.5% sodium dodecyl sulfate solution is used as the dissolution medium, and the rotation speed is 75 rpm, after 45 minutes, take the appropriate amount of solution, filter, take the appropriate amount of filtrate, and dilute quantitatively with the above dissolution medium to make a solution containing about 20ug of rifaximin per lml, according to UV-visible spectrophotometry (General rule 0401), measure absorbance at the wavelength of 448nm, and take appropriate amount of rifaximin reference substance, the above dissolution medium was added to dissolve and quantitatively dilute to prepare a solution containing about 20ug per 1 ml, which was measured by the same method, and the dissolution amount of each bag was calculated. The limit is 75% of the labeled amount and shall be in accordance with the provisions.
weight loss on drying this product shall be dried under reduced pressure at 60°C for 3 hours with phosphorus pentoxide as desiccant, and the weight loss shall not exceed 2.0% (General rule 0831).
other than sedimentation volume ratio (single dose packaging), should comply with the relevant provisions under the item of oral suspension (General Principle 0123).

Content determination

new system for clinical use. Take the contents under the difference of loading, mix evenly, grind finely, weigh appropriately (about equivalent to rifaximin lOOmg), put them in 250ml measuring flask, add mobile phase to dissolve and dilute to the scale, shake well, filter, Take 5ml of continuous filtrate with precision, put it in 50ml measuring flask, dilute to the scale with mobile phase, shake well, as test solution, obtained by determination according to the method under the item rifaximin.

specification

(l)0.lg (2)0.2g

storage

sealed and stored in a cool and dry place.

Last Update：2022-01-01 11:58:13

Rifaximin - Rifaximin Tables

Authoritative Data Verified Data

This product contains rifaximin (C43H51N3O11) should be 90.0% to 110.0% of the label.

trait

This product is a film-coated tablet, showing orange-red to dark-red color after removing the coating.

identification

take an appropriate amount of fine powder of this product, add methanol to dissolve and dilute to prepare a solution containing about 10 mg of rifaximin per 1 ml, shake well, filter, and use as a test solution. Take an appropriate amount of rifaximin reference substance and add methanol to make a solution containing about 10 mg per 1 ml as a reference solution. According to thin layer chromatography (General 0502), draw 10ul of each of the above two solutions, each point on the same silica gel GF254 thin layer plate, with dichloromethane-methanol (95:5) as the developer, expand, take out, dry, dry at 105°C for 30 minutes, put the ultraviolet lamp (254nm) next view. The position and color of the main spot displayed by the test solution should be consistent with the position and color of the main spot of the reference solution.
in the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
two items (1) and (2) above can be selected as one item.

examination

new system of related substances in clinical use. Weigh the appropriate amount of fine powder (about equivalent to rifaximin 40mg) under the content determination item, add the mobile phase to dissolve and dilute to make a solution containing about 0.4mg rifaximin per 1ml, filter, the continuous filtrate was taken as the test solution; 1ml was accurately measured, placed in a 100ml measuring flask, diluted to the scale with the mobile phase, and shaken, as a control solution. The appropriate amount of control solution was taken accurately, and a solution containing about 0.2ug of rifaximin per 1ml was prepared by quantitative dilution with mobile phase as a sensitivity solution. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than the area of the main peak of the control solution (1.0% ), the sum of each impurity peak area shall not be greater than 3 times (3.0%) of the main peak area of the control solution.
dissolution: according to the dissolution and release determination method (General rule 0931 second method), 0.5% sodium dodecyl sulfate solution is used as the dissolution medium, and the rotation speed is 75 rpm, after 45 minutes, the appropriate amount of the solution was taken, filtered, and the appropriate amount of the filtrate was taken in a precise amount. The solution was quantitatively diluted with the above dissolution medium to make a solution containing about 20ug of rifaximin per 1 ml. Measure absorbance at the wavelength of 448mn by UV-Vis spectrophotometry (General rule 0401), and take appropriate amount of rifaximin reference substance, the solution containing about 20ug per 1 ml was prepared by dissolving and quantitatively diluting with the above dissolution medium, and the dissolution amount of each tablet was calculated by the same method. The limit is 75% of the labeled amount and shall be in accordance with the provisions.
loss on drying: take an appropriate amount of the fine powder of this product, use phosphorus pentoxide as desiccant, and dry under reduced pressure at 60°C for 3 hours. The loss of weight shall not exceed 8.0% (General rule 0831).
others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).

Content determination

new system for clinical use. Take 10 tablets of this product, precisely weigh, grind, precisely weigh an appropriate amount (equivalent to rifaximin lOOmg), put it in a 100ml measuring flask, add the mobile phase to dissolve and dilute to the scale, shake well, filter, take 2ml filtrate accurately, put it in 50ml measuring flask, dilute it to the scale with mobile phase, shake it well, use it as test solution, and measure it according to the method of rifaximin, that's right.

specification

(1)0.lg (2)0.2g

storage

light shielding, sealed storage.

Last Update：2022-01-01 11:58:13

Rifaximin - Rifaximin capsules

Authoritative Data Verified Data

This product contains rifaximin (C43H51N3O11) should be 90.0% to 110.0% of the label.

trait

The contents of this product are orange-red to dark-red granules or powder.

identification

take an appropriate amount of the contents of this product, add methanol to make a solution containing about 10 mg of rifaximin per 1 ml, shake, filter, as a test solution. An appropriate amount of rifaximin control was taken and methanol was added to prepare a solution containing about 10 mg per 1 ml as a control solution. According to the thin layer chromatography (General rule 0502) test, absorb 10 u1 of each of the above two solutions, respectively point on the same silica gel GF254 thin layer plate, with dichloromethane-methanol (95:5) as the developing solvent, after expansion, taking out, drying, drying at 105 ° C. For 30 minutes, and viewing under a UV lamp (254mn). The position and color of the main spot displayed by the test solution should be consistent with the position and color of the main spot of the reference solution.
in the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
two items (1) and (2) above can be selected as one item.

examination

new system of related substances in clinical use. Take an appropriate amount of the content under the difference in loading (approximately equivalent to rifaximin 40mg), dissolve with mobile phase and dilute to make a solution containing approximately 0.4mg rifaximin per 1ml, filter, the continuous filtrate was taken as the test solution; 1ml was accurately measured, placed in a 100ml measuring flask, diluted to the scale with the mobile phase, and shaken, as a control solution. The appropriate amount of control solution was taken accurately, and a solution containing about 0.2ug of rifaximin per 1ml was prepared by quantitative dilution with mobile phase as a sensitivity solution. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than the area of the main peak of the control solution (1.0% ) , the sum of each impurity peak area shall not be greater than 3 times (3.0%) of the main peak area of the control solution.
dissolution: according to the dissolution and release determination method (General rule 0931 second method), 0.5% sodium dodecyl sulfate solution is used as the dissolution medium, and the rotation speed is 75 rpm, after 45 minutes, the appropriate amount of the solution was taken, filtered, and the appropriate amount of the filtrate was taken in a precise amount. The solution was quantitatively diluted with the above dissolution medium to make a solution containing about 20ug of rifaximin per 1 ml. According to UV-visible spectrophotometry (General rule 0401), measure absorbance at the wavelength of 448nm, and take appropriate amount of rifaximin reference substance, the solution containing about 20ug per 1 ml was prepared by dissolving and quantitatively diluting with the above dissolution medium, and the dissolution amount of each particle was calculated by the same method. The limit is 80% of the labeled amount and shall be in accordance with the provisions.
weight loss on drying this product shall be dried under reduced pressure at 60°C for 3 hours with phosphorus pentoxide as desiccant, and the weight loss shall not exceed 7.0% (General rule 0831).
others should be determined in accordance with the relevant provisions under the capsule (General rule 0103).

Content determination

new system for clinical use. Take the contents under the difference of loading amount, mix them evenly, weigh appropriately (about equivalent to rifaximin lOOmg), put them in a 100ml measuring flask, add the mobile phase to dissolve and dilute to the scale, shake well, filter, take 2ml of continuous filtrate with precision, put it in 50ml measuring flask, dilute to the scale with mobile phase, shake well, as test solution, obtained by determination according to the method under the item rifaximin.

specification

(1)0.lg (2)0.2g

storage

sealed and stored in a cool and dry place.

Last Update：2022-01-01 11:58:14

Rifaximin - Reference Information

.
2. Intestinal obstruction is contraindicated.
3. Severe intestinal ulcerative lesions are contraindicated

Overview	Rifaximin (Rifaximin) is a rifamycin derivative developed by the Italian Alpha Company, in 1987, it was marketed in Italy as an anti-infectious diarrhea drug, and was still widely used in foreign countries. In 2004, it was approved by SFDA and has been used in clinical practice in China. It is a semi-synthetic antibacterial agent of Rifamycin, with wide antibacterial spectrum and strong antibacterial effect, which can form a high blood concentration in the intestinal tract, gram-negative aerobic bacteria in the genus Salmonella, Shigella and Escherichia coli, Yersinia enterocolitica, gram-positive anaerobic bacteria in the genus Bacteroides and so on have a high degree of antibacterial activity. Its mechanism of action is to inhibit bacterial polymerase, block the transcription process of RNA, and then inhibit the synthesis of bacterial protein, thereby reducing the production of ammonia, its antibacterial effect characteristics: 1) strong antibacterial, broad antibacterial spectrum, the majority of gram-positive bacteria and gram-negative bacteria (including aerobic bacteria and anaerobic bacteria) has a bactericidal effect, and the effect on Gram-positive bacteria is stronger than gram-negative bacteria; 2) it is not absorbed by the gastrointestinal tract, and has a very high concentration in the intestinal tract. It can quickly play an antibacterial role in the local area by killing the pathogens in the intestinal tract, and does not need to cooperate with the use of intestinal spasmolytic drugs and adsorbed drugs. as an intestinal antibiotic, rifaximin is not easily absorbed by the gastrointestinal tract after oral administration, and only reaches a high drug concentration in the intestinal tract, and its blood concentration can be almost ignored, the risk of systemic side effects is very low. Rifaximin has no significant difference in clinical efficacy compared with aminoglycoside antibiotics and other commonly used drugs for intestinal bacterial infection, but the side effects are significantly reduced. Rifaximin is clinically used for acute and chronic intestinal infection, Diarrhea, enterocolitis, etc., and as an adjuvant therapeutic drug for high blood ammonia and an intestinal preventive drug before or after surgery, and has a broad market prospect. at present, there are 16 rifaximin raw materials, 12 tablets, 5 capsules, 1 Soft Capsule and 3 suspensions produced in China. In 2004, the US Food and Drug Administration (FDA) approved an application for the marketing of rifaximin (Xifaxan) in the US, the indication is the treatment of patients over 12 years of age with non-invasive E. Coli-induced traveler Diarrhea (TD for short).
Background	rifaximin is effective in the treatment of bacterial intestinal infection, hepatic encephalopathy, inflammatory bowel disease and other gastrointestinal diseases. Acute bacterial intestinal infection is a common clinical digestive system disease, if not timely and effective treatment, mild can cause irritable bowel syndrome, severe can cause dehydration, electrolyte disorders, acidosis and even Shock and other complications, the quality of life has been seriously affected. At present, antibiotic therapy is the main clinical treatment. Rifaximin (Rifaximin) is an oral non-absorption, local role in the intestinal tract of antibiotics, a variety of gram-positive bacteria, gram-negative aerobic bacteria and anaerobic bacteria have a high degree of antibacterial activity, and levofloxacin, there was no significant difference in the efficacy of rifaximin against bacterial intestinal infections compared with ciprofloxacin and other antibiotics. The effective rates of rifaximin and ciprofloxacin in the treatment of bacterial intestinal infections were 97.14% and 97.19%, respectively. The cure rate, effective rate, bacterial clearance rate and incidence of adverse reactions in the treatment of acute bacterial intestinal infections were equivalent to those of ciprofloxacin and levofloxacin, it is a safe and effective antibacterial drug for the clinical treatment of acute bacterial intestinal infection. inflammatory bowel disease mainly includes Crohn's disease (CD) and ulcerative colitis (UC). Rifaximin is an oral non-gastrointestinal absorbed antibiotic, which can be used for the treatment of inflammatory bowel disease, the remission rate of CD and UC was 69% and 76% respectively. In addition, rifaximin was approved by the U. S. Food and Drug Administration (FDA) in 2005 for the treatment of hepatic encephalopathy. Intestinal ammonia-producing bacteria is the main source of intestinal ammonia, and the bactericidal effect of the antibiotic rifaximin can reduce ammonia production, with good efficacy, safety and tolerance, and can reduce the rate of re-hospitalization, hospitalization time and hospital costs, while improving the quality of life of patients.
trait	is orange powder, soluble in ethanol, chloroform and toluene, insoluble in water
pharmacological action	is a broad-spectrum intestinal antibiotic, which is a semi-synthetic derivative of rifamycin SV. The mechanism of action is the same as that of other rifamycins. By irreversibly binding to the bacterial DNA-dependent RNA polymerase β subunit, bacterial RNA synthesis is inhibited, and bacterial protein synthesis is finally inhibited to exert a bactericidal effect. The antibacterial spectrum is extensive, and it has high antibacterial activity against most Gram-positive and gram-negative bacteria including aerobic bacteria and anaerobic bacteria. This product is almost not absorbed by oral administration, and plays a role by killing pathogenic bacteria locally in the intestinal tract.
synthetic route	with rifamycin S and 2-amino-4-methylpyridine as raw materials, dichloromethane as solvent, rifaximin was synthesized with iodine as catalyst and sodium sulfite as reducing agent, in which the molar ratio of rifamycin S to catalyst iodine was 3:1, the molar ratio of 2-amino-4-methylpyridine to rifamycin S was 2.5: 1, the reaction temperature was 30 ° C., and the reaction time was 24 h. Under the optimized conditions, the yield of the product reached 85.2%, and the specific reaction process was as follows:
pharmacokinetics	, local and gastrointestinal administration is almost not absorbed (absorption rate is less than 1%), after oral administration in the intestine concentration is very high, mainly by fecal excretion.
indications	for intestinal infections caused by rifaximin-sensitive pathogens, including acute and chronic intestinal infections, Diarrhea syndrome, summer Diarrhea, travelers Diarrhea and enterocolitis. It is also used in the adjuvant treatment of hyperammonemia (hepatic encephalopathy).
specification	tablet: 200mg; Capsule: 200mg; Suspension: 5ml: 100mg; Dry suspension: 200mg; Cream: 5%
dosage	for the treatment of intestinal infections caused by sensitive bacteria, including acute and chronic intestinal infections, Diarrhea syndrome, summer Diarrhea, traveler Diarrhea and enterocolitis, etc., oral, adult Once 200mg,tid ~ qid(6~12 years old children, once 100~200mg,qid;12 years old and older doses with adults, the same below). Prevention of gastrointestinal perioperative infectious complications, oral, adults once 400mg,bid (children aged 6-12 years, once 200~400mg,bid). for the adjuvant treatment of hyperammonemia, oral, adults once 400mg,tid(6~12 years old children, once 200 ~ 300mg,tid).
adverse reactions	the drug had mild adverse reactions and was well tolerated by local and gastrointestinal administration. Central nervous system: there are Head Pain reports. Metabolism/endocrine system: patients with hepatic encephalopathy after taking the drug may have weight loss, serum potassium and serum sodium concentration slightly increased. Gastrointestinal System: common symptoms were Nausea, Vomit, abdominal distension and Abdominal Pain, the incidence was less than 1%. Nausea usually appears after the first dose, but may resolve rapidly. Skin: a large dose of long-term medication, a very small number of patients with urticaria-like skin reactions. Other: useful after drug may cause foot edema report.
Drug interactions	less than 1% of the oral dose of rifaximin is absorbed via the gastrointestinal tract, therefore Rifaximin does not cause systemic problems due to drug interactions.
precautions	This product has mild adverse reactions and is well tolerated by local and gastrointestinal administration. The common symptoms were Nausea, Vomit, abdominal distension and Abdominal Pain, and the incidence was less than 1%. Head Pain, with edema of foot. Patients with hepatic encephalopathy after taking this product may have weight loss, serum potassium and serum sodium concentration slightly increased. Long-term use of large doses, a very small number of patients can occur urticaria-like skin reactions. This product and other rifamycin drugs may exist cross allergy. The goods or other rifamycin drug allergy, intestinal obstruction, severe intestinal ulcer lesions disabled. Use with caution in pregnant and lactating women.
contraindication
pregnant and lactating women	1. The effect of drugs on pregnancy: Animal experiments have not seen the drug teratogenicity, but the safety and effectiveness of pregnant women is not clear. Therefore, pregnant women need to weigh the pros and cons of medication. 2. Effect of drug on lactation: only a very small amount is absorbed after gastrointestinal administration, and the concentration in milk is also very low. Lactating women may take the drug with appropriate medical monitoring.
Use in Children	1. Continuous use in children should not exceed 7 days. 2. Children under 6 years of age are advised not to take this tablet or capsule.
overdose	The trial demonstrated that taking 1.6g/d, neither local nor systemic adverse events occurred; in case of overdose, gastric lavage and other appropriate treatment
toxicological studies	Repeated Dose Toxicity: 25mg/kg, 50mg/kg and 100mg/kg orally every day in rats, for 180 consecutive days, it was well tolerated, with no other abnormal changes except for the dose-related increase in serum cholesterol in female rats, which may be the result of an effect on intestinal flora. genetic toxicity: no mutagenic effect of this product in vivo or in vitro. reproductive toxicity: rats and rabbits given this product 50mg/kg and 100mg/kg No teratogenic effects and other reproductive toxicity.
Main reference materials	[1] Wu Shumei, etc. Application progress of rifaximin in digestive tract diseases. Drug and clinical. 2012,33(12):752-755. [2] Wu Shumei et al. Research progress of rifaximin in the treatment of inflammatory bowel disease. Journal of Gastroenterology and Hepatology. 2013,22(5):492-494. [3] Liu Hongyan et al. Study of rifaximin. Heilongjiang Medical University. 2013,26(3):480-481. [4] Xia Liping, editor-in-chief. Handbook of commonly used anti-infective drugs. Tianjin: Tianjin Science and Technology Publishing House. [5] Ren Juanqing, editor-in-chief. Practical Drug Handbook. Jinan: Shandong Science and Technology Publishing House. 2012. [6] Shuai Haitao et al. Study on the synthesis process of rifaximin. Applied Chemical Engineering. 2013,42(10):1801-1803. [7] Zhao Guangjuan, editor-in-chief. Rational use and application principle of commonly used antibiotics. Tianjin: Tianjin Science and Technology Publishing House. [8] Xu Jingfeng, Edited by Yang Benming. Handbook of clinical prescription drugs. Nanjing: Jiangsu Science and Technology Publishing House. 2009. [9] Chen Jisheng. New clinical pharmacology. Beijing: Chinese Medicine Press. 2013. [10] Rifaximin Tables instructions. [11] Instructions for rituximab injection. Roche Pharma(Schweiz)Ltd.
Use	An intestinal antibiotic that is a rifamycin derivative, suitable for Gram-positive and gram-negative bacteria, acute and chronic intestinal infection caused by aerobic and anaerobic bacteria, Diarrhea syndrome, Diarrhea caused by change of intestinal flora, preoperative and postoperative intestinal preventive medication, hyperammonemia, portal vein shunt encephalitis, hepatic coma. Is a high efficiency and low toxicity of intestinal antibiotics. antibiotics antibiotics, bulk drug (gastrointestinal)

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Rifaximin

Rifaximin Request for Quotation

Rifaximin

CAS: 80621-81-4

Molecular Formula: C43H51N3O11

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