CN116196286A - Sodium mycophenolate gastric floating tablet - Google Patents

Abstract

The invention provides a sodium mycophenolate gastric-floating tablet, which is prepared from the following raw materials in parts by weight: every 1000 pieces of sodium mycophenolate gastric-floating tablets are prepared, and the raw materials comprise 180g of sodium mycophenolate, 130-160 g of hydroxypropyl methylcellulose K4M, 934-40 g of carbomer, 50-65 g of lactose, 4000 25-40 g of PEG and 2.7g of magnesium stearate; and preparing the sodium mycophenolate gastric-floating tablet according to the raw material dosage of the sodium mycophenolate gastric-floating tablet. The sodium mycophenolate oral preparation disclosed by the invention has the advantages of simple production process, capability of solving the risk of hydrate formation caused by sodium mycophenolate and water in the production process, universal production equipment, low cost and convenience in carrying and swallowing for patients. Has the same curative effect as the existing dosage forms.

Description

A kind of mycophenolate sodium gastric floating tablet

technical field

The invention belongs to the technical field of medicine, and more specifically relates to a mycophenolate sodium gastric floating tablet.

Background technique

Mycophenolate Sodium is a highly efficient, selective, non-competitive and reversible inhibitor of hypoxanthine mononucleotide dehydrogenase (IMPDH), which can inhibit the classical synthesis pathway of guanine nucleotides. Mycophenolic acid (MPA) has a highly selective effect on lymphocytes. The concentration of MPA required to inhibit the proliferation of lymphocytes has no inhibitory effect on most lymphocytes. MPA can also inhibit the formation of antibodies by directly inhibiting the proliferation of B cells. Therapeutic doses of mycophenolate sodium did not inhibit the polysaccharide-activated human peripheral blood lymphocytes to produce interleukin-I, nor inhibited the synthesis of interleukin-II and its receptor expression by mitogen-activated peripheral lymphocytes, which is also different from cyclosporine Su, FK-506. Furthermore, MPA-mediated depletion of guanosine triphosphate in lymphocytes in vitro inhibited the conversion of mannose and fucose into glycoproteins. Through this mechanism, MPA reduces the accumulation of lymphocytes and monocytes at sites of chronic inflammation.

On April 25, 2009, Beijing Novartis Pharmaceuticals Co., Ltd. grandly held a launch meeting for the innovative drug Mycophenolate Sodium Enteric-Coated Tablets (Miff) for suppressing rejection in organ transplantation in Beijing. Mifu is the only mycophenolate sodium enteric solution approved by the US Food and Drug Administration (FDA), and it was approved by my country's State Food and Drug Administration (SFDA) on December 18, 2008. It is compatible with cyclosporine A and corticosteroids Combination steroids for prophylaxis of acute postoperative rejection in adult patients undergoing renal allograft transplantation. Mycophenolate Sodium Enteric-coated Tablets can improve the compliance of kidney transplant patients receiving immunosuppressant therapy and reduce the loss of graft function caused by drug side effects due to its good rejection suppression effect and drug tolerance. Previously, Mifu had been approved for marketing in 91 countries including Switzerland and the United States.

However, the enteric-coated material coating technology used in commercially available enteric-coated tablets and the organic solvent used in the preparation process have a greater impact on the environment, and the equipment cost is higher; in view of this, the present invention is proposed.

Contents of the invention

The purpose of the present invention is to disclose an oral mycophenolate sodium gastric floating tablet. The oral preparation has a simple production process, requires less equipment, is convenient to take, and has little individual difference.

To achieve the above object, the present invention adopts the following technical solutions:

The invention discloses a mycophenolate sodium gastric-floating tablet. The dosage of the raw materials of the mycophenolate sodium gastric-floating tablet is as follows: for every 1000 mycophenolate sodium gastric-floating tablets, the raw materials used include 180g of mycophenolate sodium, Hydroxypropyl methylcellulose K4M 130~160g, Carbomer 934 20~40g, lactose 50~65g, PEG4000 25~40g, magnesium stearate 2.7g;

Mycophenolate Sodium Gastric Floating Tablets are prepared according to the raw material dosage of the Mycophenolate Sodium Gastric Floating Tablets.

In some embodiments, during the preparation of the mycophenolate sodium gastric floating tablet, no liquid material is added during fluidized bed granulation, and the granules are obtained after cooling in a fluidized bed state.

In some embodiments, the hardness of mycophenolate sodium gastric floating tablet is 5-7KN.

Compared with prior art, the beneficial effect of the present invention is:

The mycophenolate sodium gastric floating tablet disclosed by the present invention utilizes reasonable raw materials, and there is no organic solvent in the prescription; it is prepared by a simple process in the prior art, and its equipment is highly popularized, suitable for large-scale production of enterprises, and extremely market development prospects. Utilize the dissolution characteristics of the drug itself to achieve the same curative effect as enteric-coated tablets.

Detailed ways

The present invention will be described in detail below in conjunction with various embodiments, but it should be noted that these embodiments are not limitations of the present invention, and those of ordinary skill in the art can make functional, method, or structural equivalent transformations or replacements based on these embodiments. , all fall within the protection scope of the present invention.

Embodiment one

Prescription: (prepare 1000 tablets)

prescription composition Dosage Mycophenolate Sodium 180g Hydroxypropyl Methyl Cellulose K4M 140g Carbomer 934 39.5g lactose 62g PEG4000 26g Magnesium stearate 2.7g

Embodiment two

Prescription: (prepare 1000 tablets)

prescription composition Dosage Mycophenolate Sodium 180g Hydroxypropyl Methyl Cellulose K4M 157.5g Carbomer 934 22g lactose 50g PEG4000 38g Magnesium stearate 2.7g

Embodiments 1 and 2 Mycophenolate Sodium Gastric Floating Tablets were prepared according to the following method:

Pass mycophenolate sodium, hydroxypropyl methylcellulose, carbomer 934, lactose, and PEG4000 through an 80-mesh sieve;

Weigh the prescription amount of mycophenolate sodium, hydroxypropyl methylcellulose, carbomer 934, lactose, PEG4000 and mix them in a mixer for 10 minutes;

Transfer the mixed material to the fluidized bed, granulate, set the material temperature to 60 degrees Celsius, set the fan frequency to 15HZ; set the outlet temperature to 40°C; after the granulation is completed, turn off the heating, set the fan frequency to 18Hz, and cool , when the temperature of the material dropped to 30°C, the material was collected.

The obtained material is mixed with the magnesium stearate and then compressed into tablets, and the hardness of the mycophenolate sodium gastric floating tablets obtained after the compression is 5-7KN.

Embodiment three, in vivo pharmacokinetic experiment:

Get 18 experimental rabbits (body weight range 1.5Kg-2.0Kg), be divided into 2 groups at random, every group of 9, respectively gavage the mycophenolate sodium gastric floating tablet that embodiment two makes and commercially available enteric-coated tablet (rice Fu), according to the dosage of 250mg/Kg, after 15min, 30min, 45min, 1h, 2h, 3h, 4h, 6h, 8h, 10h, take 1.0mL of blood from the femoral vein of rabbits, and add methanol for 20min , centrifuged, and 20 μL of the supernatant was taken, and the content was detected by HPLC. Two preparations, four cycles, and two sequences were used to repeat the crossover design, and the cleaning cycle was 7 days.

The pharmacokinetic parameters of each preparation are as follows:

The results in the above table show that compared with the commercially available preparations, the mycophenolate sodium floating tablets prepared according to Commercial Example 2 can be considered to have the same curative effect.

The oral preparation of mycophenolate sodium disclosed in the present invention has a simple production process, solves the risk of forming hydrates between mycophenolate sodium and water in the production process, has common production equipment, low cost, and is convenient for patients to carry and swallow. It has the same curative effect as the existing dosage form.

What have been described above are only some embodiments of the present invention, and it should be pointed out that for those of ordinary skill in the art, without departing from the creative concept of the present invention, other deformations and improvements can also be made, and these all belong to protection scope of the present invention.

Claims (3)

1. The mycophenolate sodium gastric-floating tablet is characterized by comprising the following raw materials in percentage by weight: every 1000 pieces of sodium mycophenolate gastric-floating tablets are prepared, and the raw materials comprise 180g of sodium mycophenolate, 130-160 g of hydroxypropyl methylcellulose K4M, 934-40 g of carbomer, 50-65 g of lactose, 4000 25-40 g of PEG and 2.7g of magnesium stearate;

and preparing the sodium mycophenolate gastric-floating tablet according to the raw material dosage of the sodium mycophenolate gastric-floating tablet.

2. The sodium mycophenolate gastric-floating tablet of claim 1, wherein no liquid material is added during the preparation of the sodium mycophenolate gastric-floating tablet, and wherein the tablet is cooled in a fluidized bed state to obtain granules.

3. The sodium mycophenolate gastric floating tablet of claim 2, wherein the sodium mycophenolate gastric floating tablet has a hardness of 5-7KN.