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Tacrolimus slow-release mini-pill and preparation method thereof

A technology of tacrolimus and sustained-release pellets, which is applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, block delivery, etc. It can solve the problems of poor drug stability, difficult to determine adverse reactions, and adverse reactions of patients. Many problems, to achieve the effect of improving bioavailability, convenient storage, and small adverse reactions

Inactive Publication Date: 2016-06-22
HEILONGJIANG ZHICHENG MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] At present, there are tacrolimus capsules in the market for the prevention of graft rejection after liver or kidney transplantation, and for the treatment of graft rejection uncontrollable by other immunosuppressive drugs after liver or kidney transplantation, but the drug of this capsule is stable Sex is not very good, and adverse reactions are difficult to determine, most patients have more adverse reactions in a few weeks after surgery

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] A tacrolimus sustained-release pellet, comprising drug-containing pellets and a coating layer, the coating layer wraps the drug-containing pellets, and the drug-containing pellets include: 5 mg tacrolimus, 70 mg blank pills Core, 120-220mg filler, 25-125mg lubricant, 5-50mg binder, the coating layer includes: 35-175mg Eudragit NE30D, 5-52mg talcum powder.

[0034] The optimal mass ratio of raw materials in the drug-containing pellets is: 5 mg tacrolimus, 70 mg blank pellet core, 200 mg filler, 55 mg lubricant, and 10 mg binder.

[0035] The optimal mass ratio of raw materials in the coating layer is: 95mg Eudragit NE30D, 21mg talcum powder.

[0036] The filler is microcrystalline cellulose.

[0037] Described lubricant is talcum powder.

[0038] The binder is hypromellose.

[0039] The coating layer also includes traces of sodium lauryl sulfate or polyethylene glycol.

Embodiment 2

[0041] A preparation method of tacrolimus sustained-release pellets, comprising the following steps:

[0042] Step 1: Preparation of raw materials: according to the above mass ratio, crush tacrolimus with a pulverizer, and pass through a 100-mesh sieve;

[0043] Step 2: Mixing: Weigh tacrolimus and microcrystalline cellulose according to the above mass ratio, put them into a three-dimensional mixer and mix for 30 minutes to make a fine drug powder, take it out for later use;

[0044] Step 3: Preparation of adhesive: Weigh an appropriate amount of hypromellose according to the above mass ratio, add an appropriate amount of hot water to prepare an adhesive with a concentration of 2%, and set aside;

[0045] Step 4: Pill making: put the mixed drug fine powder into the feeding tank of the centrifugal pellet machine, put the adhesive into the liquid supply tank, put the blank pellet core into the pot, turn on the machine, adjust the parameters, and start spraying When th...

Embodiment 3

[0051] Tacrolimus is metabolized by hepatic CYP3A4 enzymes. There is also evidence for gastrointestinal metabolism by CYP3A4 enzymes in the intestinal wall. Coadministration with other drugs or herbs known to inhibit or induce CYP3A4 enzymes may affect tacrolimus metabolism, thereby increasing or decreasing tacrolimus blood levels. Therefore, if it is used in combination with drugs that can potentially alter the metabolism of CYP3A4 enzymes, it is recommended to monitor the plasma concentration of tacrolimus and adjust the dose of tacrolimus to maintain similar tacrolimus exposure.

[0052] The following drugs have been clinically shown to increase tacrolimus plasma concentrations:

[0053] Strong interaction with antifungal drugs such as ketoconazole, fluconazole, itraconazole and voriconazole, macrolide erythromycin or HIV protease inhibitors (such as ritonavir). When coadministered with these drugs, almost all patients will require a dose reduction of tacrolimus.

...

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PUM

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Abstract

A tacrolimus slow-release mini-pill and a preparation method thereof are disclosed, the tacrolimus slow-release mini-pill includes a drug-containing mini-pill and a coating layer, the drug-containing mini-pill is coated with the coating layer, the drug-containing mini-pill comprises 5mg of tacrolimus, 70mg of a blank pill core, 120-220mg of a filler, 25-125mg of a lubricant and 5-50mg of a binder, the coating layer comprises 35-175mg of Eudragit NE30D and 5-52mg of talc powder, preparation steps of the preparation method are as follows: 1, preparing materials; 2, mixing; 3, preparing the binder; 4, pelleting; 5, preparing a coating agent; 6, coating; 7, filling; and 8, aluminum molding and finishing. The tacrolimus slow-release mini-pill is used for preventing of graft rejection reaction after liver or kidney transplantation and treatment of graft rejection reaction which cannot be controlled by other immunosuppressive drugs after liver or kidney transplantation, and the tacrolimus slow-release mini-pill is more secure, better in stability, and smaller in adverse reactions.

Description

technical field [0001] The invention belongs to the technical field of chemical medicine sustained-release preparations, in particular to a tacrolimus sustained-release pellet and a preparation method thereof. Background technique [0002] During allogeneic tissue and organ transplantation, the immune system of the recipient often produces a rejection reaction to the graft (transplant rejection), which is a very complex immunological phenomenon involving various immune injury mechanisms mediated by cells and antibodies. Both are responses to human major histocompatibility antigen HLA (humanleucocyteantigen) in the graft, and the degree of difference between donor and recipient HLA determines the severity or severity of rejection. Transplant rejection can be divided into hyperacute rejection, acute rejection and chronic rejection according to different pathogenesis and pathological changes. The rapid and severe rejection of the graft by the recipient within a few minutes to 2...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K9/16A61K31/436A61K47/32A61P37/06
Inventor 张昕
Owner HEILONGJIANG ZHICHENG MEDICAL TECH
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