CN1989972B - Finasteroid oral preparation and method for preparing same - Google Patents
Finasteroid oral preparation and method for preparing same Download PDFInfo
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- CN1989972B CN1989972B CN2005100622388A CN200510062238A CN1989972B CN 1989972 B CN1989972 B CN 1989972B CN 2005100622388 A CN2005100622388 A CN 2005100622388A CN 200510062238 A CN200510062238 A CN 200510062238A CN 1989972 B CN1989972 B CN 1989972B
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Abstract
The invention relates to a non-finasteride oral preparation and preparation method, specifically which consists of main drug non-finasteride and medicinal findings. Its contents are oily liquid or semi-solid, and it can be made of soft capsules, liquid-filled capsules and oral emulsion. The important contribution of the invention is preparing the steroidal hormone compounds into liquid or semi-solid in agent preparation early period, avoiding occupational hazard caused by dust flying, protecting workers involving in manufacture;In addition, non-finasteride is the combination of lipophilic compounds, oily liquid or semi-solid drugs and supplies, it can increase the drug dissolution rate, improve bioavailability. The application of the invention can improve labor protection, and also can provide better curative effect in clinical application.
Description
Technical field
The invention belongs to technical field of pharmaceuticals, specifically, relate to a kind of 5-alpha-reductase activity inhibitor medicine Finasteroid oral preparation and preparation method thereof.
Background technology
Benign prostate hyperplasia (BPH) is a kind of special organization pathological conditions, and its feature shows as substrate and epithelial hypertrophy, and BPH can cause the increase (BPH) of benign prostate and the displayable benign prostate of urodynamics to block (BPO).BPH is the commonly encountered diseases of elderly men, and result of study shows that male's great majority more than 50 years old have benign prostatic hyperplasia in various degree.94 years to Beijing more than 40 years old male resident's a sampling survey show have the BPH symptom to reach 37.6%.Among 20 the Urology Surgery inpatients of big city hospital in the 1990-1991 whole nation, patient BPH accounts for 13.6%.Along with China's constant development of economy, the improving constantly of people's living standard, the continuous prolongation in population life-span, these factors all will impel the sickness rate of BPH constantly to raise.
Finasteride is a kind of four aza steroids, has competitive and selectivity inhibition 5-alpha-reductase activity, changes into dihydrotestosterone (DHT) thereby suppress testosterone.Finasteride has DHT level in the prostate of reduction and the circulation, dwindles prostate volume, increases the urine flow.Be mainly used in the treatment benign prostatic hyperplasia clinically, the prostate of increase is dwindled, improve other symptom that urine stream and benign prostatic hyperplasia occur.
Finasteride was developed by U.S. Merck company, and China ratified this medicine import in 1994, and domestic priority has enterprises such as MSD Corp., Zhejiang Province XianJu Pharmacy stock Co., Ltd to get permission raw materials for production and preparation.
The main dosage form of present domestic finasteride is tablet, capsule.Because finasteride is difficult for dissolving in water, the preparation specification is little, its conventional formulation (tablet, capsule) technology difficulty mainly is dissolution and uniformity of dosage units, thereby at first affected be the control difficulty of suitability for industrialized production, secondly be consequent quality fluctuation and influence its therapeutic effect.
The labor protection of hormone medicine production is more and more to be subjected to the problem that society payes attention to, preparation production of the present invention, and material medicine does not need to pulverize again; produce after can directly being mixed with liquid state or semisolid; no dust, thereby more help sanitation and hygiene and labor protection, possess higher social benefit.
Summary of the invention
The purpose of this invention is to provide a kind of industrialization easily and can improve the Finasteroid oral preparation of labor protection.
Another object of the present invention provides the preparation method of above-mentioned oral formulations.
Preparation of the present invention is made up of finasteride and oily diluent.The oily diluent is specially: one or more mixture of glycerol, propylene glycol, Macrogol 200～1000, medium chain triglyceride, vegetable oil, soybean phospholipid, lecithin, Tween-80, Tween-60, Tween-40, Tween-20, stearic acid polyethyleneglycol glyceride, lauric acid polyethyleneglycol glyceride, sad capric acid polyethyleneglycol glyceride, lauric acid polyethyleneglycol glyceride, polyoxyethylene hydrogenated Oleum Ricini, polyoxyethylene monoglyceride, polyethylene glycol list isostearate, polyoxyethylene castor oil wherein are preferably vegetable oil.Vegetable oil can be: refined oil, soybean oil, olive oil, Oleum Arachidis hypogaeae semen, linolenic acid oil, perilla oil, Radix Oenotherae erythrosepalae oil, Oleum Vitis viniferae, Oleum Helianthi, safflower oil, Oleum Hippophae, Semen Maydis oil, Oleum Sesami, Oleum Ricini, Oleum Gossypii semen.
The ratio of above-mentioned preparation herb liquid content is: the weight ratio of finasteride and diluent is 1: 2～1: 2000, and weight ratio is preferably: 1: 20～1: 500.
Above-mentioned preparation can be made into soft capsule, liquid type hard capsule and Orally taken emulsion.The specification of soft capsule and liquid type hard capsule is every and contains finasteride 0.25～10mg that the concentration of Orally taken emulsion Chinese medicine is 0.05～10mg/ml.
The preparation method of Finasteroid oral preparation of the present invention, preparation process is as follows: finasteride adds diluent stirring/heating for dissolving and becomes oily liquids or semisolid, and packing becomes oral formulations then, can be soft capsule, liquid type hard capsule and Orally taken emulsion.
The concrete preparation method of finasteride soft capsule is: take by weighing finasteride, take by weighing diluent in proportion and stir, grinding repeatedly mixed dissolution with colloid mill is settled solution, emits, and measures medicament contg, stand for standby use; Take by weighing gelatin, glycerol, purified water joins in the glue pot, fully swelling, heating and melting in glue pot, insulation adds antiseptic, stirs, and evacuation is emitted glue, is incubated standby.The medicinal liquid for preparing is put into the soft capsule unit, make soft capsule by the method for system of dripping or compacting, send in the soft gelatin capsule calibrator, typing is dry.Wipe the lubricating oil of capsule surface, packing gets product after the assay was approved.
The concrete preparation method of finasteride liquid type hard capsule is: take by weighing finasteride, add the diluent take by weighing in proportion and stir, heating for dissolving or grind repeatedly to being dissolved as settled solution with colloid mill, emit, measure medicament contg, regulate loading amount, be filled in the hard capsule case.Packing gets product after the assay was approved.
The concrete preparation method of Finasteroid oral Emulsion is: take by weighing finasteride, take by weighing diluent in proportion and stir, grind repeatedly with colloid mill and mix, add correctives, essence, mix homogeneously makes.
The present invention disperses dilution with finasteride with the suitable dilution agent, adds various adjuvants, forms stable oily liquids or semisolid, makes dosage forms such as soft capsule, liquid type hard capsule and Orally taken emulsion.The existing dosage form in novel formulation and market compares, and have following advantage: soft capsule and the disintegrate of liquid type hard capsule preparation are fast, reach higher medicine stripping quantity in the short period, and absorption of human body is faster, and onset is faster, improves human bioavailability; Orally taken emulsion has easily to be taken, and absorbs fast characteristics, is fit to various crowds and takes; Content is the solution form that contains medicine, and uniform content easily is an industrial production control.
The specific embodiment
Embodiment 1
Finasteride 5g labrafac cc (medium chain triglyceride) 145g
Gelatin 80g glycerol 40g purified water 90g methyl hydroxybenzoate 0.1g
Method for making: get labrafac cc, add finasteride, stir, ground 15 minutes, emit, measure medicament contg, stand for standby use with colloid mill; Gelatin, glycerol are added in the pure water, contribute in the glue pot, fully swelling is heated to 60 ℃ in glue pot, be incubated 40 minutes, add methyl hydroxybenzoate, stir evacuation 10 minutes, emit glue, 50 ℃ of insulations are standby, and the medicinal liquid for preparing is put into the glue bucket, inject the soft capsule unit, drip system or make soft capsule, deliver in the soft gelatin capsule calibrator,, emit soft gelatin capsule in dry 3 hours of 10 ℃ of typings, 20 ℃ of dryings 24 hours, wipe capsule surface lubricating oil, packing gets product after the assay was approved.
Embodiment 2
Finasteride 1g soybean oil 100g perilla oil 49g
Gelatin 120g glycerol 80g purified water 100g ethyl hydroxybenzoate 0.1g
Method for making: with soybean oil and perilla oil mixing, add finasteride again, stir, ground 20 minutes, emit, measure medicament contg, stand for standby use with colloid mill; Gelatin, glycerol are added in the pure water, contribute in the glue pot, fully swelling is heated to 60 ℃ in glue pot, be incubated 30 minutes, add ethyl hydroxybenzoate, stir evacuation 20 minutes, emit glue, 50 ℃ of insulations are standby, and the medicinal liquid for preparing is put into the glue bucket, inject the soft capsule unit, pressing is made soft capsule, deliver in the soft gelatin capsule calibrator,, emit soft gelatin capsule in dry 63 hours of 15 ℃ of typings, 20 ℃ of dryings 36 hours, wipe capsule surface lubricating oil, packing gets product after the assay was approved.
Embodiment 3
Finasteride 0.5g olive oil 120g Tween-80 1.5g
Method for making: Tween-80 is added in the olive oil, add finasteride again, stir, ground 20 minutes, emit, measure medicament contg, stand for standby use with colloid mill; After the accurate metering of medicinal liquid for preparing, be filled in the hard capsule case, packing gets product after the assay was approved.
Embodiment 4
Finasteride 5g Oleum Arachidis hypogaeae semen 160g linolenic acid oil 120g
Method for making: with Oleum Arachidis hypogaeae semen and linolenic acid oil mixing, add finasteride again, stir, ground 40 minutes, emit, measure medicament contg, stand for standby use with colloid mill; After the accurate metering of medicinal liquid for preparing, be filled in the hard capsule case, packing gets product after the assay was approved.
Embodiment 5
Finasteride 1g glycerol 995g soybean phospholipid 2g flavoring orange essence 1g
Method for making: take by weighing finasteride, soybean phospholipid adding glycerol, stir, ground 30 minutes, add the flavoring orange essence mix homogeneously and promptly get Finasteroid oral Emulsion with colloid mill.
Embodiment 6
Finasteride 1g Macrogol 200 468g Tween-80 30g aspartame 20g
Method for making: take by weighing Macrogol 200, polyoxyethylene sorbitan monoleate, aspartame, behind the mix homogeneously, add finasteride again, stir, ground 40 minutes with colloid mill, mix homogeneously promptly gets Finasteroid oral Emulsion.
Embodiment 7
Finasteride 5g lauric acid polyethyleneglycol glyceride (gelucire 44/14) 200g
Method for making: the lauric acid polyethyleneglycol glyceride is heated to 55 ℃, adds finasteride again, be stirred to dissolving fully, measure medicament contg, the insulation medicinal liquid accurately measures, and is filled in the hard capsule case, and packing gets product after the assay was approved.
Embodiment 8
The sad capric acid polyethyleneglycol glyceride of finasteride 0.5g olive oil 145g (LABRASOL) 5g
Gelatin 80g glycerol 40g purified water 90g methyl hydroxybenzoate 0.1g
Method for making: get LABRASOL, add finasteride, stirring and dissolving adds olive oil and stirs, and measures medicament contg, stand for standby use; Gelatin, glycerol are added in the pure water, contribute in the glue pot, fully swelling is heated to 60 ℃ in glue pot, be incubated 40 minutes, add methyl hydroxybenzoate, stir evacuation 10 minutes, emit glue, 50 ℃ of insulations are standby, and the medicinal liquid for preparing is put into the glue bucket, inject the soft capsule unit, drip system or make soft capsule, deliver in the soft gelatin capsule calibrator,, emit soft gelatin capsule in dry 3 hours of 17 ℃ of typings, 20 ℃ of dryings 24 hours, wipe capsule surface lubricating oil, packing gets product after the assay was approved.
Relevant pharmaceutical test:
Below by stability experiment and with the contrast experiment of commercially available dosage form dissolution the outstanding feature that novel formulation has is described:
One, finasteride preparation stability study tour
Two, finasteride soft capsule and tablet dissolved experimentation contrast
Three, the accelerated tests of Finasteroid oral Emulsion
| Time (moon) | Character | Related substance (%) | Content (%) |
| 0 | Colourless clear liquid | 0.35 | 100.1 |
| 1 | Colourless clear liquid | 0.38 | 99.6 |
| 2 | Colourless clear liquid | 0.52 | 99.1 |
| 3 | Colourless clear liquid | 0.58 | 98.6 |
| 6 | Colourless clear liquid | 0.54 | 98.8 |
Above result shows that the stability and the dissolution of finasteride soft capsule, liquid type hard capsule all are better than tablet, oral liquid Emulsion steady quality.
Claims (5)
1. Finasteroid oral Emulsion, it is characterized in that: said preparation is made up of finasteride and oily diluent, and the weight ratio of finasteride and diluent is: 1: 518～1: 2000.
2. Finasteroid oral Emulsion according to claim 1, wherein the oily diluent is: glycerol, propylene glycol, Macrogol 200～1000, medium chain triglyceride, vegetable oil, soybean phospholipid, lecithin, one or more mixture of Tween-80, Tween-60, Tween-40, Tween-20, stearic acid polyethyleneglycol glyceride, lauric acid polyethyleneglycol glyceride, sad capric acid polyethyleneglycol glyceride, polyoxyethylene hydrogenated Oleum Ricini, polyoxyethylene monoglyceride, polyethylene glycol list isostearate, polyoxyethylene castor oil.
3. Finasteroid oral Emulsion according to claim 2, vegetable oil wherein is: refined oil, soybean oil, olive oil, Oleum Arachidis hypogaeae semen, linolenic acid oil, perilla oil, Radix Oenotherae erythrosepalae oil, Oleum Vitis viniferae, Oleum Helianthi, one or more in safflower oil, Oleum Hippophae, Semen Maydis oil, Oleum Sesami, Oleum Ricini, the Oleum Gossypii semen.
4. the preparation method of Finasteroid oral Emulsion according to claim 1, preparation process is as follows: finasteride adds liquid diluent stirring/heating for dissolving and becomes oily liquids or semisolid, and packing becomes Orally taken emulsion then.
5. the preparation method of Finasteroid oral Emulsion according to claim 4 is specially: take by weighing finasteride, take by weighing diluent in proportion, grind repeatedly with colloid mill and mix, add correctives, essence, mix homogeneously makes.
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| Application Number | Priority Date | Filing Date | Title |
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| CN2005100622388A CN1989972B (en) | 2005-12-27 | 2005-12-27 | Finasteroid oral preparation and method for preparing same |
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| CN2005100622388A CN1989972B (en) | 2005-12-27 | 2005-12-27 | Finasteroid oral preparation and method for preparing same |
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| CN1989972A CN1989972A (en) | 2007-07-04 |
| CN1989972B true CN1989972B (en) | 2011-08-31 |
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Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102145003B (en) * | 2010-02-08 | 2015-04-22 | 张立英 | Medicinal composition containing insoluble medicament |
| CN102145007B (en) * | 2011-03-03 | 2013-03-20 | 王致中 | Finasteride soft capsule and amsulosin hydrochloride capsule compound preparation, used capsule and preparing method |
| CN105902553A (en) * | 2016-05-29 | 2016-08-31 | 山东仁和堂药业有限公司 | Compound finasteride tablets and preparation process thereof |
| CN114213502B (en) * | 2021-12-08 | 2024-02-13 | 湖南醇健制药科技有限公司 | Method for refining finasteride, finasteride preparation and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1660118A (en) * | 2004-12-23 | 2005-08-31 | 鲁南制药股份有限公司 | Medication combination of containing finasteride and cyclodextrin or ramification |
| CN1698621A (en) * | 2005-05-16 | 2005-11-23 | 济南百诺医药科技开发有限公司 | Finasteride High Concentration Solution and Its Application |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1660118A (en) * | 2004-12-23 | 2005-08-31 | 鲁南制药股份有限公司 | Medication combination of containing finasteride and cyclodextrin or ramification |
| CN1698621A (en) * | 2005-05-16 | 2005-11-23 | 济南百诺医药科技开发有限公司 | Finasteride High Concentration Solution and Its Application |
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