Method for preparing compound controlled release capsule for treating benign prostatic hyperplasia and the compound controlled release capsule

A technology for prostatic hyperplasia and compound prescription, applied in the field of medicine, can solve the problems of lack of controlled release accuracy, inability to effectively control and coordinate the speed and degree of drug release, and unsuitable preparation procedures.

Inactive Publication Date: 2009-07-22
NAT INST OF PHARMA R & D CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage of this method is that the precision of the controlled release of the process is still lacking, and the drug pellets made by this process cannot effectively control and coordinate the release speed and degree of the drug.
In addition, the goal of this patent is to prepare single-drug capsules. In the selection and design of excipients, only the matching with the single drug should be considered. The selection of auxiliary materials and the preparation procedure of sustained-release pellets are not suitable for compound controlled-release drugs.

Method used

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  • Method for preparing compound controlled release capsule for treating benign prostatic hyperplasia and the compound controlled release capsule
  • Method for preparing compound controlled release capsule for treating benign prostatic hyperplasia and the compound controlled release capsule
  • Method for preparing compound controlled release capsule for treating benign prostatic hyperplasia and the compound controlled release capsule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1: Preparation of finasteride immediate-release pellets

[0040] Finasteride micropellet coating preparation process: mix the drug, binder, co-solvent and organic solvent in the formula to make a coating solution; use the above coating solution to coat the blank sugar pill core in a fluidized bed Coating, during coating, the control 100mg pellets contain 5mg of finasteride.

[0041] Here, the drug is finasteride; the binder can be selected from starch slurry, methylcellulose, hydroxypropylcellulose, hypromellose, ethylcellulose, povidone, gelatin, polyethylene glycol, etc. One or more of them are mixed; the organic solvent can be methanol, ethanol, isopropanol, acetone or any one or more of them mixed or any one or more of them in aqueous solution; when the drug solubility is not enough, A co-solvent can be added, and the co-solvent is selected from sodium lauryl sulfate, Tween, Span, phospholipid, polyoxyethylene polyoxypropylene copolymer, glyceryl stearat...

Embodiment 2

[0065] Embodiment 2: Preparation of doxazosin sustained-release pellets

[0066] 1. The coating preparation process of doxazosin sustained-release pellets: first, mix the drug with fillers and binders, then perform wet granulation, and then extrude and spheronize to prepare drug pellets. After the drug pellets are dried, use a fluidized The bed is coated with a coating liquid, and the weight gain of the coating is 5-17%.

[0067] Here, the drug in the drug pellets is doxazosin or its pharmaceutically acceptable salt, and the pharmaceutically acceptable salt can be hydrochloride, sulfate, mesylate, maleate, preferably doxazosin mesylate; The agent is selected from one or more of starch slurry, methyl cellulose, hydroxypropyl cellulose, hypromellose, ethyl cellulose, povidone, gelatin, polyethylene glycol, etc.; the filler is A mixture of one or more selected from lactose, mannitol, xylitol, sorbitol, powdered sugar, dextrin, starch, pregelatinized starch, microcrystalline cell...

Embodiment 3

[0076] Embodiment 3, the preparation of doxazosin sustained-release pellets

[0077] According to the preferred process of Example 2, the following doxazosin sustained-release pellets were prepared.

[0078] Recipe 1:

[0079] drug pellets

[0080] Doxazosin 4.00g

[0081] Powdered sugar 62.00g

[0082] Starch 24.04g

[0083] Hypromellose 10.0g

[0084] Coating solution

[0085] Ethyl cellulose 10.0g

[0086] Hydroxypropyl methylcellulose 10.0g

[0087] Ethanol 380.0g

[0088] Recipe 2:

[0089] drug pellets

[0090] Doxazosin Mesylate 5.0g

[0091] Powdered sugar 55.0g

[0092] Microcrystalline Cellulose 25.0g

[0093] Hypromellose 15.0g

[0094] Coating solution

[0095] Ethyl cellulose 10.0g

[0096] Hydroxypropyl methylcellulose 10.0g

[0097] Ethanol 380.0g

[0098] Recipe 3:

[0099] drug pellets

[0100] Doxazosin 4.0g

[0101] Lactose 70.0g

[0102] Microcrystalline Cellulose 20.0g

[0103] Povidone 6.0g

[0104] Coating solution

[0105] Ethyl...

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Abstract

The invention discloses a method for preparing a compound controlled-release capsule for treating benign hyperplasia of prostate and the compound controlled-release capsule for treating the benign hyperplasia of prostate, and belongs to the technical field of medicines. The method comprises that: common micro pills containing the finasteride medicine and slow release micro pills containing the doxazosin pills are prepared respectively, and the two kinds of micro pills are mixed and encapsulated to prepare the controlled-release capsule, wherein the mass ratio of the finasteride medicine to the doxazosin medicine in the capsule is 1:0.625-2.5. In the method, ethylcellulose and hydroxypropyl emthylcellulose are used as auxiliary materials of the slow release preparation, and by combining the preparation process by which the auxiliary materials is mutually cooperated with compound medicines, the finasteride-doxazosin compound controlled-release capsule is prepared. Active ingredients in the two medicines in the preparation not only can be mutually cooperated to achieve better curative effects, but also can stably release the medicines, avoid the difference between blood concentration at wave crest and wave hollow, and reduce toxic and side effects of the medicines on human body; moreover, the controlled-release capsule can also shorten the medicine taking time of patients and improve compliance of taking medicines. The finasteride-doxazosin controlled-release capsule can be used as the medicine to treat hypertension and benign hyperplasia of prostate.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, relates to a drug preparation for treating high blood pressure and benign prostatic hyperplasia, in particular to a preparation method of a preparation with controlled-release ability prepared by compounding two or more drugs. Background technique: [0002] Benign prostatic hyperplasia is a common senile disease in men. The main reason is the increase in age and the existence of functional testicles. The urinary obstruction caused by two main reasons: one is the testosterone produced by the testis, and the function of α1 reductase Under the action, it is transformed into dihydrotestosterone, which acts on the prostate to make the prostate hyperplasia. The protruding gland protrudes into the bladder, compressing the urethra and causing mechanical obstruction of the bladder outlet. On the other hand, the bladder neck, posterior urethra, prostatic body, and capsule are rich in α-receptors. Due to...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/58A61K31/517A61P13/08
Inventor 孙从新郑少辉郑礼孙宇章王爱玲黄圆圆赵志惠邢东东郭旻彤
Owner NAT INST OF PHARMA R & D CO LTD
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