Mycophenolate
Mycophenolate mofetil
CAS: 115007-34-6;128794-94-5
Molecular Formula: C23H31NO7
Mycophenolate - Names and Identifiers
Mycophenolate - Physico-chemical Properties
| Molecular Formula | C23H31NO7 |
| Molar Mass | 433.49 |
| Density | 1.222g/cm3 |
| Melting Point | 95-96°C |
| Boling Point | 637.6°C at 760 mmHg |
| Flash Point | 339.4°C |
| Solubility | DMSO: ≥15mg/mL |
| Vapor Presure | 7.51E-17mmHg at 25°C |
| Appearance | White to off-white crystalline powder |
| Storage Condition | 2-8℃ |
| Refractive Index | 1.557 |
| MDL | MFCD00867568 |
| Physical and Chemical Properties | Appearance: White or almost white crystalline powder |
Mycophenolate - Standard
Authoritative Data Verified Data
This product is (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1, 3-dihydroisobenzofuran-5-yl)-4-methyl-4-hexenoic acid 2-(morpholin-4-yl) ethyl ester. The content of Mycophenolate Mofetil (C23H33N07) shall be between 98.0% and 102.0% based on the dry product.
Last Update：2024-01-02 23:10:35
Mycophenolate - Trait
Authoritative Data Verified Data
- This product is white or off-white crystalline powder; Odorless.
- This product is very soluble in dichloromethane, dissolved in acetonitrile, ethyl acetate and 0.lmol/L hydrochloric acid solution, slightly soluble in methanol, slightly soluble in ethanol, insoluble in water.
melting point
The melting point of this product (General rule 0612) is 93~99°C, and the melting distance should be within 3°C.
Last Update：2022-01-01 11:53:00
Mycophenolate - Differential diagnosis
Authoritative Data Verified Data
- take an appropriate amount of this product, add 0.1 mol/L hydrochloric acid solution was dissolved and diluted to make a solution containing about 25ug per 1 ml, and the maximum absorption was measured by UV-visible spectrophotometry (General 0401) at 250nm and 304nm wavelengths.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 1241).
Last Update：2022-01-01 11:53:00
Mycophenolate - Exam
Authoritative Data Verified Data
clarity and color of solution
take this product O.lg, add 96% ethanol 10ml to dissolve, the solution should be clear and colorless (General rule 0902 first method and general rule 0901 first method).
Related substances
freshly made or stored at 4~8°C. Take an appropriate amount of this product, precision weigh, add acetonitrile to dissolve and quantitatively dilute to make a solution containing about 2mg per lml, as a test solution; Take an appropriate amount of precision, A solution containing 2u per 1 ml was prepared as a control solution by quantitative dilution with acetonitrile; An appropriate amount was accurately taken and a solution containing 0.5ug per 1 ml was prepared as a sensitivity solution by quantitative dilution with acetonitrile. In addition, the appropriate amount of impurity F reference substance is accurately weighed, and acetonitrile is added to dissolve and quantitatively dilute to prepare a solution containing about 10ug per 1 ml, which is used as the impurity F reference solution; an appropriate amount of each of the impurity A control substance and the impurity H control substance is taken, and acetonitrile is added to dissolve and dilute to prepare A mixed solution containing about 10ug each in 1 ml as A system applicable solution. According to the high performance liquid chromatography (General 0512) test, using octanosilane bonded silica gel as filler (4.6mm X 25Omm ,5um or equivalent column), phosphate buffer (triethylamine 2ml, water ML, mixed with dilute phosphoric acid to adjust p H value to 5.3)-acetonitrile (65:35) as mobile phase; Column temperature was 45°C; the detection wavelength was 250mn. Take the sensitivity of the solution 10u1 injection of human liquid chromatography, the signal to noise ratio of the peak height of the main component should be greater than 10. Take the applicable solution 10u1 of the system and inject it into the liquid chromatograph, record the chromatogram, and the separation degree between the impurity A peak and the impurity H peak should be greater than 4.0. The sample solution, impurity F reference solution and control solution are respectively 10 u1 and injected into human liquid chromatograph. The retention time of mycophenolate mofetil peak is about 22 minutes, the chromatogram was recorded to 5 times of the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, the peak area shall be calculated according to the external standard method, and the impurity F shall not exceed 0.5%; The peak area of other individual impurities shall not be greater than the main peak area of the control solution (0.1% ) , the sum of the peak areas of other impurities shall not be greater than 4 times (0.4%) of the main peak area of the control solution. The peaks in the chromatogram of the test solution which are smaller than the main peak area of the sensitivity solution are ignored.
Z-mycophenolate mofetil
take an appropriate amount of this product, weigh it accurately, add acetonitrile to dissolve and quantitatively dilute to make a solution containing about 2.5mg per 1 ml as a test solution; Take an appropriate amount of reference substance of mycophenolate mofetil, precision weighing, adding acetonitrile to dissolve and quantitatively dilute to make a solution containing about 2.5ug per 1 ml, as a control solution; Take an appropriate amount of precision, A solution containing about 0.5ug per 1 ml was prepared as a sensitivity solution by quantitative dilution with acetonitrile. Take an appropriate amount of the reference substance of mycophenolate mofetil, place it under a 254MN UV lamp for 48 hours, add an appropriate amount of acetonitrile to ultrasonically dissolve it, and dilute it with acetonitrile to make a solution containing about 2.5mg per 1 ml, which is used as a system applicable solution. The column temperature was 60 ° C. And the detection wavelength was 215nm according to the chromatographic conditions under the related substances examination. The system applicable solution 10u1 was injected into the liquid chromatograph, and the chromatogram was recorded. The resolution between the peak of mycophenolate mofetil and the peak of Z-Mycophenolate Mofetil (relative retention time is about 1.1) should meet the requirements. Take the sensitivity of the solution 10u1 injection of human liquid chromatography, the signal to noise ratio of the peak height of the main component should be greater than 10. The sample solution and the control solution of 10 u1 were respectively injected into the liquid chromatograph, and the chromatograms were recorded. If there is a peak in the chromatogram of the test solution that is consistent with the peak retention time of Z-mycophenolate mofetil, the peak area shall not be greater than the main peak area of the control solution (0.10%).
residual solvent
take about 0.6g of this product, precision weighing, top empty bottle, precision plus internal standard solution (take the appropriate amount of methyl isobutyl ketone, diluted with dimethyl sulfoxide to make about 0 per 1 ml. lmg solution) 3ml, sealed, shake to dissolve, as a test solution; Precision weighing acetone, methanol, ethanol, dichloromethane, ethyl acetate, toluene, xylene, n-hexane, cyclohexane, the appropriate amount of butyl acetate and N, N-dimethylformamide was Diluted quantitatively with internal standard solution to prepare about 1.0mg of acetone, 0.6mg of methanol and l of ethanol per 1 ml. 0mg, dichloromethane 0.12mg, ethyl acetate l. 0mg, toluene 0.178mg, xylene 0.434mg, N-hexane 0.058mg, cyclohexane 0.776mg, Butyl Acetate 1.0mg, N, N-dimethylformamide 0.176mg mixed solution, take 3ml of precision, place in empty bottle, Seal, as a control solution. Capillary column (0861, 30m) with cyanopropyl phenyl-94% dimethyl polysiloxane (or similar polarity) as stationary liquid according to the test for determination of residual solvents (General rule 0.53 second method), 3um or performance equivalent column); The initial temperature is 35 °, for 1 minute, at a rate of 5°C per minute to 90 °, and then at a rate of 15 ° per minute to 150°C, then the temperature is raised to 230 ° at a rate of 35°C per minute for 10 minutes; The inlet temperature is 200 °; The detector temperature is 250 °; And the equilibrium temperature of the headspace bottle is 120 °, the equilibration time was 30 minutes. The reference solution was injected in Headspace according to methanol, ethanol, acetone, dichloromethane, N-hexane, ethyl acetate, cyclohexane, internal standard substance, toluene, butyl acetate, N, N-dimethylformamide, xylene is eluted sequentially, and the separation degree between peaks shall meet the requirements. The test solution and the reference solution were injected into the headspace, and the chromatogram was recorded. The peak area was calculated according to the internal standard method, acetone, methanol, ethanol, methane, ethyl acetate, toluene, xylene, residues of N-hexane, cyclohexane, butyl acetate and N, N-dimethylformamide shall be as specified.
loss on drying
taking this product, using phosphorus pentoxide as desiccant, drying under reduced pressure at 60°C for 3 hours, the weight loss shall not exceed 0.5% (General rule 0831).
ignition residue
take l.Og of this product and check it according to law (General rule 0841). The residue left 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 11:53:02
Mycophenolate - Content determination
Authoritative Data Verified Data
take this product about 0.4g, precision weighing, add 50ml of glacial acetic acid to dissolve, according to the potentiometric titration method (General 0701), with perchloric acid titration solution (0.1 mol/L) titration, and the results of the titration were corrected with a blank test. Each 1 ml of perchloric acid titration solution (0.1 mol/ L) corresponds to 43.35mg of C23H31NO7.
Last Update：2022-01-01 11:53:02
Mycophenolate - Category
Authoritative Data Verified Data
immunosuppressant.
Last Update：2022-01-01 11:53:03
Mycophenolate - Storage
Authoritative Data Verified Data
storage at 30°C or below in the dark.
Last Update：2022-01-01 11:53:03
Mycophenolate - Mycophenolate mofetil tablets
Authoritative Data Verified Data
This product contains Mycophenolate Mofetil (C23H33N07) should be 90.0% to 110.0% of the label amount.
trait
This product is a film-coated tablet, white or off-white after removal of the coating.
identification
- 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.
- take an appropriate amount of fine powder of this product and add O. 1 mol / L hydrochloric acid solution mycophenolate mofetil was dissolved and diluted to prepare a solution containing about 25FXG of mycophenolate mofetil per 1 ml, which was determined by UV-Vis spectrophotometry (General 0401), there is maximum absorption at wavelengths of 250Nm and 304nm.
examination
- Related substances are newly prepared or stored at 4-8°C. Take the fine powder of this product (about equivalent to 0.2g of mycophenolate mofetil), weigh it accurately, put it in a 100ml measuring flask, add appropriate amount of acetonitrile and ultrasound to dissolve the mycophenolate mofetil, dilute it with acetonitrile to scale, shake it well, filter, take the filtrate as the test solution; According to the method of mycophenolate mofetil, if there are impurity peaks in the chromatogram of the test solution, the impurity F is calculated by the peak area according to the external standard method, 1.0% of the marked amount shall not be exceeded; The peak area of other individual impurities shall not be greater than the main peak area of the control solution (0.1% ) , and the sum of the peak areas of other impurities shall not be greater than 8 times (0.8%) of the main peak area of the control solution.
- Z-mycophenolate mofetil take an appropriate amount of fine powder of this product (about 0.25g of mycophenolate mofetil), weigh it accurately, put it in a 100ml measuring flask, add 10ml of water, and sonicate it for 15 minutes, an appropriate amount of acetonitrile was added and sonicated to dissolve mycophenolate mofetil, which was diluted to a scale with acetonitrile, shaken, filtered, and the filtrate was taken as a test solution. According to the method of mycophenolate mofetil, if there are chromatographic peaks in the chromatogram of the test solution with the same retention time as the peak of 2-mycophenolate mofetil, the peak area shall not be greater than the main peak area of the control solution (0.10%).
- dissolution of this product, according to the dissolution and release determination method (General 0931 second method), with 0.lmol/L hydrochloric acid solution 900ml as the dissolution medium, the rotation speed is 50 revolutions per minute, according to the operation, after 15 minutes, take the appropriate amount of solution, filtration, precision take the appropriate amount of filtrate, with 0.1 mol/L hydrochloric acid solution was Diluted quantitatively to prepare a solution containing about 25ug of mycophenolate mofetil per 1 ml, and the absorbance was measured at the wavelength of 304nm according to ultraviolet-visible spectrophotometry (General rule 0401); take an appropriate amount of the reference substance of mycophenolate mofetil and weigh it precisely, add 0.1 mol/L hydrochloric acid solution was dissolved and quantitatively diluted to prepare a solution containing about 25ug per 1 ml, which was measured by the same method, and the dissolution amount of each tablet was calculated. The limit is 80% of the labeled amount and shall be in accordance with the provisions.
- others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).
Content determination
- measured by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test octyl silane bonded silica gel as filler (4.6mm X 250mm , 5um or equivalent chromatographic column), with phosphate buffer solution (take 2ml of triethylamine, add ml of water, mixed with dilute phosphoric acid to adjust the pH value to 5.3)-acetonitrile (65:35) as mobile phase; Column temperature was 45°C; Detection wavelength was 250nm. Take appropriate amount of reference substance of impurity A and impurity H, add acetonitrile to dissolve and dilute to prepare A solution containing about 10ug in each lml, and use 10ul to inject human liquid chromatograph as the applicable solution of the system, the chromatogram shows that the peak retention time of mycophenolate mofetil is about 22 minutes, and the separation degree between impurity A peak and impurity H peak should be greater than 4.0.
- determination of 10 tablets of this product, precision weighing, fine grinding, precision weighing fine powder appropriate amount (equivalent to mycophenolate mofetil 0.2g ) , put 100ml measuring flask, add appropriate amount of acetonitrile and ultrasonic to dissolve mycophenolate mofetil, dilute to the scale with acetonitrile, shake well, filter, Take 5ml of continued filtrate precisely, put it in a 25ml measuring flask, dilute to the scale with acetonitrile, shake well, as a sample solution, take 10ul injection liquid chromatograph for precise measurement, record chromatogram; Take appropriate amount of reference substance of mycophenolate mofetil for precise weighing, acetonitrile was added to dissolve and quantitatively diluted to prepare a solution containing about 0.4mg per 1 ml, which was determined by the same method. According to the external standard method to calculate the peak area, that is.
category
Same as mycophenolate mofetil.
specification
(1)0.25g (2)0.5g
storage
storage at 30°C or below in the dark.
Last Update：2022-01-01 11:53:04
Mycophenolate - Mycophenolate Mofetil Capsules
Authoritative Data Verified Data
This product contains Mycophenolate Mofetil (C23H33N07) should be 90.0% to 110.0% of the label amount.
trait
The contents of this product are white or off-white powder or granules or lumps.
identification
- 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.
- take an appropriate amount of the contents of this product and add O. 1 mol/ L hydrochloric acid solution the mycophenolate mofetil was dissolved and diluted to prepare a solution containing about 25ug of mycophenolate mofetil per 1 ml, which was determined by UV-Vis spectrophotometry (General 0401), there is maximum absorption at wavelengths of 250Nm and 304nm.
examination
- Related substances are newly prepared or stored at 4-8°C. Take an appropriate amount of the content under the difference of loading (equivalent to 0.2g of mycophenolate mofetil), weigh it accurately, put it in a 100ml measuring flask, add an appropriate amount of acetonitrile and ultrasound to dissolve the mycophenolate mofetil, and dilute it to the scale with acetonitrile, shake well, filter, and take the continued filtrate as the test solution; Determine according to the method under the item of mycophenolate mofetil, and calculate the impurity F based on the peak area according to the external standard method, and shall not exceed 1.0% of the label amount; the Peak area of other individual impurities shall not be greater than the main peak area of the control solution (0.1% ) , and the sum of the peak areas of other impurities shall not be greater than 8 times (0.8%) of the main peak area of the control solution.
- the content of Z-Mycophenolate Mofetil (equivalent to 0.25g of mycophenolate mofetil) should be weighed accurately, put in a 100ml measuring flask, add 10ml of water, and sonicate for 15 minutes, add appropriate amount of acetonitrile and ultrasound to dissolve mycophenolate mofetil, dilute to the scale with acetonitrile, shake, filter, and take the filtrate as the test solution, if there is a peak in the chromatogram of the test solution that is consistent with the retention time of Z-mycophenolate mofetil, the peak area shall not be greater than the main peak area of the control solution (0.10%).
- dissolution of this product, according to the dissolution and release determination method (General 0931 first method), with 0.lmol/ L hydrochloric acid solution 900ml as the dissolution medium, the rotation speed is 50 revolutions per minute, according to the operation, after 30 minutes, take the appropriate amount of solution, filtration, precision take the appropriate amount of filtrate, with 0.1 mol/ L hydrochloric acid solution is diluted quantitatively to prepare a solution containing about 25ug of mycophenolate mofetil per 1 ml, and the absorbance is measured at the wavelength of 304nm by ultraviolet-visible spectrophotometry (General rule 0401), take an appropriate amount of the reference substance of mycophenolate mofetil and weigh it precisely, add 0.1 mol/ L hydrochloric acid solution was dissolved and quantitatively diluted to prepare a solution containing about 25ug per 1 ml, which was measured by the same method, and the dissolution amount of each particle was calculated. The limit is 80% of the labeled amount and shall be in accordance with the provisions.
- others should comply with the relevant provisions under the capsule (General 0103).
Content determination
- measured by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using octyl silane bonded silica gel as filler (4.6mm X 250mm, or equivalent chromatographic column), phosphate buffer (take 2ml of triethylamine, add ml of water, mixed with dilute phosphoric acid to adjust the pH value to 5.3)-acetonitrile (65:35) as mobile phase; Column temperature was 45°C; Detection wavelength was 250nm. Take appropriate amount of reference substance of impurity A and impurity H, add acetonitrile to dissolve and dilute to prepare A solution containing about 10ug in each lml, and use 10u1 to inject human liquid chromatograph as the applicable solution of the system, the chromatogram shows that the peak retention time of mycophenolate mofetil is about 22 minutes, and the separation degree between impurity A peak and impurity H peak should be greater than 4.0.
- determine the amount of content under the item of difference in loading (about 0.2g of mycophenolate mofetil), weigh it accurately, put it in a 100ml measuring flask, and add appropriate amount of acetonitrile and ultrasound to dissolve mycophenolate mofetil, dilute with acetonitrile to the scale, shake, filter, Take 5ml of the filtrate accurately, put it in a 25ml measuring flask, dilute with acetonitrile to the scale, shake well, as a test solution, take 10u1 injection liquid chromatograph for accurate measurement, record chromatogram; Take appropriate amount of reference substance of mycophenolate mofetil, weigh it accurately, add acetonitrile to dissolve and quantitatively dilute to make a solution containing about 0.4mg per 1 ml, and determine with the same method. According to the external standard method to calculate the peak area, that is.
category
Same as mycophenolate mofetil.
specification
0.25g
storage
storage at 30°C or below in the dark.
Last Update：2022-01-01 11:53:05
Mycophenolate - Reference Information
| Overview | mycophenolate mofetil also known as mycophenolate mofetil (MMF), trade name Cellcept, developed by the United States Syntex company, it is a semisynthetic derivative of mycophenolic acid (MPA) isolated from the glycolysis of fungal Penicillin glucum. Mycophenolate mofetil is a reversible cell inhibitor. In fact, it has been clinically used for more than 10 years, mainly for the treatment of psoriasis. In the late 2080s, organ transplantation animal experiments confirmed that it could significantly prolong the survival time of rodent and canine allograft kidney, heart and islet. For the first time, solliner et al successfully applied MMF in the treatment of renal transplantation anti rejection, and the treatment effect was significant. FDA approved its official registration in 1995, the trade name of Cellcept, so that the clinical use of a new effective prevention and treatment of rejection of immunosuppressive agents. |
| pharmacological characteristics | after oral administration, mycophenolate mofetil was rapidly absorbed in upper digestive tract. The main absorption site is in the stomach and is metabolized by plasma lipase to the pharmacologically active product, mycophenolic acid (MPA), with an average bioavailability of 94%. One hour after drug administration, the blood drug concentration rapidly reached the peak and then rapidly decreased. MPA in the liver by glucuronidation metabolism for stable, no pharmacological activity of glucuronide (MPAG), excreted from the urine. MPAG excreted by bile in the intestinal tract enters the small intestine, and the glucosidase of intestinal flora converts it into MPA, which is reabsorbed by the intestinal tract to form the enterohepatic circulation, A second plasma MPA peak (6 to 12 hours after administration) was observed. About 6% of the MPAG was excreted by feces. It is activated by hydrolytic metabolism in vivo, non-competitive inhibition of hypoxanthine monophosphate dehydrogenase, blocking guanine nucleotide synthesis, thereby exerting its immunosuppressive effect on lymphocytes, T lymphocytes and B lymphocytes were significantly affected. |
| Use | is mainly used to prevent allograft organ rejection. It is mainly used in kidney transplantation, and is also suitable for heart and liver transplantation, especially for refractory rejection after transplantation. Can be applied simultaneously with cyclosporine and corticosteroids. It can also be applied to rheumatoid arthritis, systemic lupus erythematosus, primary glomerulonephritis, psoriasis and other autoimmune diseases. Oral: kidney transplantation: the initial dose is 2~3 mg/kg a day, the maintenance dose is 1~2 mg/kg a day, divided into 2~3 times. Can be adjusted according to the condition. Rheumatoid arthritis: 300mg/day. Mycophenolate mofetil on the overview, pharmacological characteristics, uses, synthesis, etc. is a Yan editing. (2015-11-02) |
| synthesis | with mycophenolic acid (2) as the starting material, further, it is subjected to an esterification reaction with 4-(2-hydroxyethyl) morpholine (4) to form Mycophenolate Mofetil (1). 1 is mycophenolate mofetil synthesis (1) is directly prepared by azeotropic dehydration using (2) and (4) as starting materials and n-butyl ether or n-pentyl ether as solvent. 2 shows the above two processes for the synthesis of mycophenolate mofetil. In method 2, n-butyl ether or n-pentyl ether is used as the solvent, and the production cost is relatively high. Although there is a two-step reaction in the first method, the acid chloride product in the first step can be directly used for the next reaction without treatment, and the final product only needs to be recrystallized to obtain a pure product. |
| Clinical application | 1. organ transplantation organ transplantation is an operation in which a donor's healthy organ is transplanted into another person to quickly restore function. The biggest threat of organ transplantation is rejection, mainly manifested as acute rejection, although there are more mature immunosuppressive regimens, including cyclosporine A, azathioprine, tacrolimus, cyclophosphamide, drug combination therapy of prednisone and methylprednisolone, but there are still a considerable number of transplant patients rejection every year, eventually leading to chronic rejection and transplant failure. In addition, the adverse reactions of immunosuppressive drugs have also restricted its clinical application. In 1995, mycophenolate mofetil was successfully used in organ transplantation, postoperative prevention and treatment of graft rejection. In May of the same year, the FDA approved the use of mycophenolate mofetil in kidney transplantation, it was first successfully applied to renal transplant patients in 1996. Next, the researchers found that mycophenolate mofetil combined with cyclosporine and prednisone can reduce the occurrence of acute rejection after renal transplantation, and also has a good effect on refractory renal transplantation rejection. Mycophenolate mofetil alone can be used as an immunosuppressant for long-term maintenance therapy, which can improve renal function, especially for elderly donors with poor renal function. Immune nephropathy is a group of chronic Glomerular diseases with the same immunopathological features caused by multiple etiologies. Immune nephropathy including purpura nephritis, refractory nephrotic syndrome, primary nephrotic syndrome, lupus nephritis, IgA nephropathy, due to the patient's immune system dysfunction, the immune complex is deposited in the kidney, damage to the intrinsic cells of the kidney, causing inflammatory reactions, etc., destroying the normal function of the intrinsic cells of the kidney and causing the patient to have proteinuria, hematuria, edema and other symptoms. Autoimmune diseases of the digestive system (1) autoimmune liver diseases autoimmune liver diseases (ALD) are chronic progressive liver diseases mediated by autoimmune reactions. 20% of ALD patients are insensitive to hormones and azathioprine, and there is no suitable treatment for a long time. The researchers concluded that the use of mycophenolate mofetil, which significantly reduced hormone use, improved in 88% of ALD patients who did not respond to conventional therapies, the study showed. (2) autoimmune pancreatitis autoimmune pancreatitis (AIP) this is an inflammatory lesion of the pancreas as a result of an immune response generated by recognition of the pancreas to its own components as antigens by CD4 positive helper cells. Mycophenolate mofetil was administered to patients with hormone-dependent igg4-mediated autoimmune pancreatitis and igg4-mediated cholangitis who were initially treated with prednisone 40mg/d and had improved symptoms. When the hormone was reduced to 10mg/d, the patient developed jaundice, elevated transaminase and hyperbilirubinemia, and azathioprine was Added. The patient could not tolerate the adverse reactions. Then mycophenolate mofetil 750mg,2 times/d, combined with prednisone 15mg. After 3 months, the patient developed hyperglycemia and other hormone-related adverse reactions, after 4 months, the energy metabolism and blood glucose of the patients were significantly improved, and no adverse drug reactions were found. The use of mycophenolate mofetil solves the problem that patients cannot use hormones. It is suggested that mycophenolate mofetil or other immunosuppressants may be used to maintain or ameliorate autoimmune pancreatitis. Other diseases (1) refractory idiopathic thrombocytopenic purpura idiopathic thrombocytopenic purpura (ITP) Is a common autoimmune bleeding disease, its pathogenesis is complex, the treatment is difficult, the traditional treatment methods usually use glucocorticoid, although the majority of patients with glucocorticoid effective, however, there are still some patients with poor effect, which is called refractory idiopathic thrombocytopenic purpura (refractory idiopathic thrombocytopenic purpura,R-ITP). As a new immunosuppressant, mycophenolate mofetil has few adverse reactions. It is an effective method for R-ITP treatment and has broad clinical application prospects. (2) psoriasis psoriasis (psoriasis) commonly known as psoriasis, which is characterized by papules and erythema of varying sizes of the skin, the surface is covered with silvery white scales, the border is clear, good hair on the scalp, extensor limbs and back. Its etiology is not yet clear. In recent years, most scholars believe that it is related to heredity, infection, metabolic disorder, immune dysfunction, endocrine disorders and environment. Studies have shown that methotrexate and mycophenolate mofetil in the treatment of psoriasis has no significant difference in safety and efficacy, but mycophenolate mofetil has better safety, can not tolerate methotrexate adverse reactions or patients with contraindications can choose mycophenolate mofetil. (3) myasthenia gravis myasthenia gravis (MG) is a chronic autoimmune disease caused by conduction dysfunction between nerve and muscle junctions. Immunosuppressive agents play an important role in the treatment of MG, and the main mechanism is to reduce the destruction of cholinergic receptors or related receptors by inhibiting the formation of related autoantibodies, and to protect the smooth flow of nerve excitation transmission pathways, thereby improving the patient's symptoms of muscle weakness. Mycophenolate mofetil has fewer side effects than other immunosuppressants. |
| pharmacokinetics | MMF is rapidly and extensively absorbed after oral administration, and is deesterified by intestinal wall, liver and other tissues, rapid conversion to active MPA. The average oral bioavailability was 94% of that for intravenous injection (according to the area under the curve of MPA), and MMF was not detected in the circulation in normal people after oral administration. After cleavage from the original drug, MPA is metabolized by glucuronyltransferase in the liver to form inactivated mycophenolic acid glucuronide. After oral administration of 1H MPA drug concentration reached the peak, due to the effect of liver and intestine circulation, 6~12h after taking the drug will appear the second plasma MPA peak. Its biological half-life is 16~18h, and 97% MPA binds to plasma protein at clinically effective concentration. A very small amount ( < 1%) of MMF is excreted from the urine as MPA, most (87%) is excreted from the urine in the form of mycophenolic acid glucuronide, and about 6% is excreted from the feces. The absorption of MMF is closely related to liver function, and the absorption of MMF is less when the liver function is worse. |
| adverse reactions | mainly hypertension, atrial fibrillation, orthostatic hypotension, tachycardia, thrombosis, vasodilation, Head Pain, dizziness, sleep Initiation and Maintenance Disorders, Anxiety, hypercholesterolemia, blood glucose changes, potassium, calcium metabolism disorder, acidosis, alkaline phosphatase increased, creatinine increased, hyperlipidemia, parathyroid dysfunction, Nausea, Vomit, dyspepsia, liver dysfunction, etc. Myelosuppression is common and should be discontinued in case of severe neutropenia. Fungal dermatitis, rash. The incidence of amblyopia, cataract and conjunctivitis ranged from 3% to 10%. |
| precautions | . 2. Careful use of severe active digestive diseases, bone marrow suppression, with hypoxanthine-guanine transphosphoribosyl kinase genetic defects, severe heart, liver and kidney insufficiency.
Last Update：2024-04-09 15:16:42
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