CN100339082C - Terazosin hydrochloride dripping pills, and its prepn. method - Google Patents
Terazosin hydrochloride dripping pills, and its prepn. method Download PDFInfo
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- CN100339082C CN100339082C CNB2004100199312A CN200410019931A CN100339082C CN 100339082 C CN100339082 C CN 100339082C CN B2004100199312 A CNB2004100199312 A CN B2004100199312A CN 200410019931 A CN200410019931 A CN 200410019931A CN 100339082 C CN100339082 C CN 100339082C
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- terazosin hydrochloride
- polyethylene glycol
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- drop pill
- terazosin
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Abstract
The present invention relates to a terazosin hydrochloride drop pill and a preparation method thereof. The drop pill is formed by combining terazosin hydrochloride and basal materials by weight proportion of 0.5-10 to 39.5-30, wherein the basal materials are one kind or two kinds of polyethylene glycol 6000, polyethylene glycol 4000, polyethylene glycol 2000, polyethylene glycol 1500, polyethylene glycol 1000, poloxamer and span 40. The terazosin hydrochloride drop pill of the present invention is formed by solid dispersion technology. Compared with tablets, the dosage of auxiliary materials of the present invention is relatively reduced. Therefore, the present invention can be dissolved and absorbed in body fluid rapidly and can take effect quickly. The biological availability of the present invention is high and the stability is good. Moreover, because the volume of the pill is small, the pill not only can be swallowed, but also can be kept in mouth. The present invention can be carried conveniently. Therefore, the present invention is particularly suitable for old people, sickbed patients and dysphagia patients to take. The technology of the method of the present invention and the production equipment are simple. The present invention has low production cost and is suitable for large-scale production and preparation.
Description
Technical field
The present invention relates to medicine, particularly relate to a kind of terazosin hydrochloride drop pill for the treatment of prostatic hyperplasia.
Background technology
Prostatic hyperplasia is a kind of common male's infirmities of age.It is because the mechanical obstruction that the body of prostate that increases causes is that functional the urinating that is caused occurring by the prostate smooth muscle contraction blocked on the other hand on the one hand that urinating of being caused by prostatic hyperplasia blocked.Prostate and bladder neck smooth muscle have abundant α
1-adrenoceptor, α
1-adrenoceptor blocker can act on the α of neck of bladder, prostate film and intraprostatic smooth muscle cell
1-adrenoceptor, the release that the retardance adrenal gland can mediator and relaxing smooth muscle, thereby be acknowledged as the active drug that can alleviate the prostatic obstruction symptom.Terazosin hydrochloride is 1-(4-amino-6,7-dimethoxy-2-quinazolyl)-4-[(tetrahydrochysene-2-furan) formoxyl] piperazine hydrochloride two hydrates are a kind of novel α
1-adrenoceptor blocker, it optionally acts on α
1-adrenoceptor distends the blood vessels, and bring high blood pressure down with the resistance that reduces peripheral vessels, so it can significantly reduce the blood pressure with hypertensive hyperplasia of prostate patient.Commercially available terazosin hydrochloride is a tablet at present, because the disintegration time of this medicine is longer, dissolution and dissolution rate are lower, and absorption difference and bioavailability are low, thereby for the patient of old people, bed patient and dysphagia, not only take inconvenience, and compliance difference and stable bad.
Summary of the invention
In order to address the above problem, the object of the present invention is to provide a kind of disintegrate molten loose fast, dissolution and dissolution rate height, not only can swallow but also can buccal, easy to carry, onset is rapid, bioavailability is high, compliance is good and production cost is lower terazosin hydrochloride drop pill.
In order to achieve the above object, terazosin hydrochloride drop pill provided by the invention by as the terazosin hydrochloride of active component and substrate with 1: 3 and 1: the weight ratio of 39-79 combines, and described substrate is selected from one or both among polyethylene glycol 6000, Macrogol 4000, Macrogol 2000, polyethylene glycol 1500, cetomacrogol 1000, poloxamer and the Si Ban 40.
Terazosin hydrochloride drop pill provided by the invention is to utilize solid dispersion technology and make, and the consumption of comparing adjuvant with tablet is relative to be reduced, thereby its dissolving, absorption and effect in body fluid is fast, bioavailability height and good stability.In addition, because the volume of pill is little, it not only can have been swallowed but also can buccal and easy to carry, thereby the patient who is particularly suitable for old people, bed patient and dysphagia takes.
The specific embodiment
Embodiment 1
Prescription:
Terazosin hydrochloride 0.5g
Polyethylene glycol 6000 39.5g
Make 1000
Method for making: with 1000 terazosin hydrochloride drop pill is benchmark, take by weighing terazosin hydrochloride and the 39.5g polyethylene glycol 6000 of 0.5g respectively through the screening of 100 mesh sieves, polyethylene glycol 6000 is heated to fusing in water-bath, under stirring and heat-retaining condition, join in the fused polyethylene glycol 6000 terazosin hydrochloride and abundant mix homogeneously then, at last said mixture is splashed into and be condensed into ball in the dimethicone, remove dimethicone then and promptly can be made into 1000 (every 40mg) terazosin hydrochloride drop pill provided by the invention.
Embodiment 2
Prescription:
Terazosin hydrochloride 1g
Macrogol 4000 19.5g
Polyethylene glycol 6000 19.5g
Make 1000
Method for making: with 1000 terazosin hydrochloride drop pill is benchmark, take by weighing terazosin hydrochloride and 19.5g Macrogol 4000 and the 19.5g polyethylene glycol 6000 of 1g respectively through the screening of 100 mesh sieves, Macrogol 4000 and polyethylene glycol 6000 are heated to fusing in water-bath, under stirring and heat-retaining condition, join in fused Macrogol 4000 and the polyethylene glycol 6000 terazosin hydrochloride and abundant mix homogeneously then, at last said mixture is splashed into and be condensed into ball in the liquid paraffin, remove liquid paraffin then and promptly can be made into 1000 (every 40mg) terazosin hydrochloride drop pill provided by the invention.
Embodiment 3
Prescription:
Terazosin hydrochloride 5g
Polyethylene glycol 6000 31.8g
40 3.2g of class of department
Make 1000
Method for making: with 1000 terazosin hydrochloride drop pill is benchmark, take by weighing terazosin hydrochloride and 31.8g polyethylene glycol 6000 and the 3.2g department class 40 of 5g respectively through the screening of 100 mesh sieves, polyethylene glycol 6000 and Si Ban 40 are heated to fusing in water-bath, under stirring and heat-retaining condition, join among fused polyethylene glycol 6000 and the Si Ban 40 terazosin hydrochloride and abundant mix homogeneously then, at last said mixture is splashed into and be condensed into ball in the dimethicone, remove dimethicone then and promptly can be made into 1000 (every 40mg) terazosin hydrochloride drop pill provided by the invention.
Embodiment 4
Prescription:
Terazosin hydrochloride 10g
Macrogol 4000 29.5g
Stearic acid 0.5g
Make 1000
Method for making: with 1000 terazosin hydrochloride drop pill is benchmark, take by weighing terazosin hydrochloride and 29.5g Macrogol 4000 and the 0.5g stearic acid of 10g respectively through the screening of 100 mesh sieves, Macrogol 4000 and stearic acid are heated to fusing in water-bath, under stirring and heat-retaining condition, join in fused Macrogol 4000 and the stearic acid terazosin hydrochloride and abundant mix homogeneously then, at last said mixture is splashed into and be condensed into ball in the liquid paraffin, remove liquid paraffin then and promptly can be made into 1000 (every 40mg) terazosin hydrochloride drop pill provided by the invention.
Embodiment 5
Prescription:
Terazosin hydrochloride 1g
Polyethylene glycol 6000 35g
Polyethylene glycol 1500 4g
Make 1000
Method for making: with 1000 terazosin hydrochloride drop pill is benchmark, take by weighing terazosin hydrochloride and 35.0g polyethylene glycol 6000 and the 4.0g polyethylene glycol 1500 of 1g respectively through the screening of 100 mesh sieves, polyethylene glycol 6000 and polyethylene glycol 1500 are heated to fusing in water-bath, under stirring and heat-retaining condition, join in fused polyethylene glycol 6000 and the polyethylene glycol 1500 terazosin hydrochloride and abundant mix homogeneously then, at last said mixture is splashed into and be condensed into ball in the dimethicone, remove dimethicone then and promptly can be made into 1000 (every 40mg) terazosin hydrochloride drop pill provided by the invention.
Embodiment 6
Prescription:
Terazosin hydrochloride 3g
Poloxamer 32g
Cetomacrogol 1000 5g
Make 1000
Method for making: with 1000 terazosin hydrochloride drop pill is benchmark, take by weighing terazosin hydrochloride and 32.0g poloxamer and the 5.0g cetomacrogol 1000 of 3g respectively through the screening of 100 mesh sieves, poloxamer and cetomacrogol 1000 are heated to fusing in water-bath, under stirring and heat-retaining condition, join in fused poloxamer and the cetomacrogol 1000 terazosin hydrochloride and abundant mix homogeneously then, at last said mixture is splashed into and be condensed into ball in the liquid paraffin, remove liquid paraffin then and promptly can be made into 1000 (every 40mg) terazosin hydrochloride drop pill provided by the invention.
Embodiment 7
Prescription:
Terazosin hydrochloride 5g
Macrogol 4000 17.5g
Poloxamer 17.5g
Make 1000
Method for making: with 1000 terazosin hydrochloride drop pill is benchmark, take by weighing terazosin hydrochloride and 17.5g Macrogol 4000 and the 17.5g poloxamer of 5g respectively through the screening of 100 mesh sieves, Macrogol 4000 and poloxamer are heated to fusing in water-bath, under stirring and heat-retaining condition, join in fused Macrogol 4000 and the poloxamer terazosin hydrochloride and abundant mix homogeneously then, at last said mixture is splashed into and be condensed into ball in the liquid paraffin, remove liquid paraffin then and promptly can be made into 1000 (every 40mg) terazosin hydrochloride drop pill provided by the invention.
Embodiment 8
Prescription:
Terazosin hydrochloride 1g
Polyethylene glycol 6000 26g
Macrogol 2000 13g
Make 1000
Method for making: with 1000 terazosin hydrochloride drop pill is benchmark, take by weighing terazosin hydrochloride and 26.0g polyethylene glycol 6000 and the 13.0g Macrogol 2000 of 1g respectively through the screening of 100 mesh sieves, polyethylene glycol 6000 and Macrogol 2000 are heated to fusing in water-bath, under stirring and heat-retaining condition, join in fused polyethylene glycol 6000 and the Macrogol 2000 terazosin hydrochloride and abundant mix homogeneously then, at last said mixture is splashed into and be condensed into ball in the dimethicone, remove dimethicone then and promptly can be made into 1000 (every 40mg) terazosin hydrochloride drop pill provided by the invention.
The assay of each embodiment:
| Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Embodiment 5 | Embodiment 6 | Embodiment 7 | Embodiment 8 | |
| Disintegration | 7 minutes | 6 minutes | 8 minutes | 10 minutes | 6 minutes | 8 minutes | 8 minutes | 9 minutes |
| Dissolution | 92.2％ | 91.8％ | 90.8％ | 89.5％ | 92.4％ | 91.5％ | 90.1％ | 89.8％ |
| Character | White | White | Off-white color | Off-white color | White | White | White | White |
| Related substance | Up to specification | Up to specification | Up to specification | Up to specification | Up to specification | Up to specification | Up to specification | Up to specification |
The terazosin hydrochloride drop pill packing sample that to make according to the present invention is placed 6 months to carry out accelerated test under 40 ℃, the condition of RH75%, observe character and detect related substance, dissolve scattered time limit and content in 1,2,3 and 6 sampling at the end of month and according to quality standard.Found that with 0 month and compare, the equal no change of sample character, related substance, dissolve scattered time limit and content in placement 1,2,3 and June.
The terazosin hydrochloride drop pill packing sample that to make according to the present invention is placed 24 months to carry out long term test, in 3,6,9,12,18 and 24 samplings at the end of month and according to quality standard observation character, related substance, dissolve scattered time limit and content under 25 ℃, RH60% condition.Result and comparison in 0 month, placement 3,6,9,12,18 and the equal no change of sample character, related substance, dissolve scattered time limit and content after 24 months.
Terazosin hydrochloride drop pill provided by the invention has the obvious treatment effect for vascular hypertension, and do not influence carbohydrate metabolism, electrolyte and hepatic and renal function, side effect is slight, with terazosin hydrochloride drop pill treatment hypertension 100 examples of the present invention, wherein effective 60 examples, produce effects 30 examples, invalid 10 examples, total effective rate reaches 90%.Simultaneously, terazosin hydrochloride drop pill of the present invention also can be treated chronic prostatitis, and urine flow rate and residual urines that the patient takes medicine before and after its treatment of 3 week backs all have significant change, obvious effective rate 51.1%, and improvement rate 29.8%, total effective rate reaches 80.9%.In addition, the terazosin hydrochloride drop pill also can be treated benign prostate hyperplasia, and patient's international prostate gland symptoms scoring (IPSS scoring), Qmax and residual urine volume all are greatly improved after 4 weeks of treatment.Wherein 12.4 ± 4.8 after the treatment reduced in IPSS scoring 19.9 ± 4.3 before by treatment, and Qmax is increased to 15.6 ± 2.5ml/s by 10.3 ± 2.1ml/s, and residual urine volume then reduces to 35.7 ± 4.7ml by 58.9 ± 5.6ml, and untoward reaction is few.
Claims (1)
1, a kind of terazosin hydrochloride drop pill, it is characterized in that: described terazosin hydrochloride drop pill by as the terazosin hydrochloride of active component and substrate with 1: 3 and 1: the weight ratio of 39-79 combines, and described substrate is selected from one or both among polyethylene glycol 6000, Macrogol 4000, Macrogol 2000, polyethylene glycol 1500, cetomacrogol 1000, poloxamer and the Si Ban 40.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100199312A CN100339082C (en) | 2004-07-08 | 2004-07-08 | Terazosin hydrochloride dripping pills, and its prepn. method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100199312A CN100339082C (en) | 2004-07-08 | 2004-07-08 | Terazosin hydrochloride dripping pills, and its prepn. method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1718188A CN1718188A (en) | 2006-01-11 |
| CN100339082C true CN100339082C (en) | 2007-09-26 |
Family
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2004100199312A Expired - Fee Related CN100339082C (en) | 2004-07-08 | 2004-07-08 | Terazosin hydrochloride dripping pills, and its prepn. method |
Country Status (1)
| Country | Link |
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| CN (1) | CN100339082C (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101298502B (en) * | 2007-04-30 | 2010-08-11 | 福建省医学科学研究所 | Method for increasing chitose water-solubility |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1528311A (en) * | 2003-09-27 | 2004-09-15 | 南昌弘益科技有限公司 | Terazosin Hydrochloride drop pill and preparing method thereof |
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2004
- 2004-07-08 CN CNB2004100199312A patent/CN100339082C/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1528311A (en) * | 2003-09-27 | 2004-09-15 | 南昌弘益科技有限公司 | Terazosin Hydrochloride drop pill and preparing method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1718188A (en) | 2006-01-11 |
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