CN103127030B - Propylene glycol alginate sodium sulfate enteric capsule and preparation method thereof - Google Patents

Propylene glycol alginate sodium sulfate enteric capsule and preparation method thereof Download PDF

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CN103127030B
CN103127030B CN201310093377.1A CN201310093377A CN103127030B CN 103127030 B CN103127030 B CN 103127030B CN 201310093377 A CN201310093377 A CN 201310093377A CN 103127030 B CN103127030 B CN 103127030B
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propylene glycol
sodium sulfate
enteric
glycol alginate
alginate sodium
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CN103127030A (en
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王明刚
任莉
陈阳生
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Qingdao Guoxin Pharmaceutical Co ltd
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Qingdao Chia Tai Haier Pharmaceutical Co Ltd
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Abstract

The invention discloses a propylene glycol alginate sodium sulfate enteric capsule and a preparation method thereof. The propylene glycol alginate sodium sulfate enteric capsule is prepared by loading a propylene glycol alginate sodium sulfate enteric pellet into a capsule shell, wherein the propylene glycol alginate sodium sulfate enteric pellet comprises a propylene glycol alginate sodium sulfate pellet and an enteric coating layer wrapped outside the propylene glycol alginate sodium sulfate pellet, the propylene glycol alginate sodium sulfate pellet comprises propylene glycol alginate sodium sulfate and a filler, the enteric coating layer comprises an enteric material, a plasticizer and an anti-sticking agent, and the propylene glycol alginate sodium sulfate enteric capsule is prepared by wrapping the enteric coating layer outside the propylene glycol alginate sodium sulfate pellet. The propylene glycol alginate sodium sulfate enteric capsule is convenient to take, has an ideal enteric effect, can improve the bioavailability, has a simple preparation technology, can produce products with stable quality and is applicable to mass production.

Description

A kind of propylene glycol alginate sodium sulfate enteric coated capsule and preparation method thereof
Technical field
The present invention relates to a kind of Western medicine preparation technical field, relate in particular to a kind of propylene glycol alginate sodium sulfate enteric coated capsule, the invention still further relates to the preparation method of this enteric coated capsule.
Background technology
Propylene glycol alginate sodium sulfate (Alginic Sodium Diester) is a kind of polysaccharide sulfate class (Polysaccharide sulfate is called for short PSS) marine drug.It is take from Thallus Laminariae (Thallus Eckloniae) and Alga Sgrgassi Enerves etc. extract alginic acid as raw material, make through hydrolysis, esterification and sulfonation.Propylene glycol alginate sodium sulfate has heparinoid sample physiologically active, can reduce the viscosity of blood, there is the effect of anticoagulant effect and antithrombotic, reducing blood viscosity and peripheral blood vessel expansion, be mainly used in ischemic cerebrovascular as the transient ischemic attacks such as cerebral thrombosis, cerebral embolism, cerebral arteriosclerosis, apoplexy, hyperlipidemia, coronary heart disease, high blood viscosity syndrome and coronary heart disease, anginal control.In recent years, along with going deep into that propylene glycol alginate sodium sulfate is familiar with, its clinical application range is expanded to some extent, and propylene glycol alginate sodium sulfate also can be used for treating disseminated inravascular coagulation, chronic glomerulonephritis, also can treat sudden deafness, acne, hepatopathy, diabetes.In China market, mainly contain at present oral tablet, the capsule of propylene glycol alginate sodium sulfate, and injection, although oral tablet and capsule taking convenience, but be subject to the impact of the factor such as disintegrate, drug release, assimilation effect is undesirable, and bioavailability is low, although and injection curative effect is fast, but carry, use all inconveniences, and propylene glycol alginate sodium sulfate is also unstable in aqueous solution.
Enteric coated preparation refers to and do not discharge under one's belt at the appointed time or discharge hardly medicine, and enters in intestinal, can be most of in a part of intestinal or all discharge the preparation of medicine, and enteric coated capsule belongs to the one of enteric coated preparation.Enteric coated preparation can avoid medicine to be subject to the destruction of gastric enzyme or gastric acid, avoids medicine to produce intense stimulus to gastric mucosa, and delayed release effect is provided, and by being mainly passed to this position with maximum concentration as far as possible by the medicine of intestinal absorption, has improved bioavailability.
Summary of the invention
In order to overcome the deficiencies in the prior art, the present invention to adjuvant screening and process optimization, provides a kind of propylene glycol alginate sodium sulfate enteric coated capsule by lot of experiments.This enteric coated capsule steady quality, medicine discharges in intestinal, and bioavailability is high, and preparation technology is simple.
For achieving the above object, the technical scheme that the present invention takes is:
A kind of propylene glycol alginate sodium sulfate enteric coated capsule, incapsulate in shell and make by alginate diester sodium enteric-coated pellet, described alginate diester sodium enteric-coated pellet is made up of propylene glycol alginate sodium sulfate micropill and the enteric coat layer being wrapped in outside propylene glycol alginate sodium sulfate micropill, described propylene glycol alginate sodium sulfate micropill comprises propylene glycol alginate sodium sulfate and filler, described enteric coat layer comprises enteric material, plasticizer and antiplastering aid, it is characterized in that: note by ratio of weight and the number of copies, the consumption of each composition is:
Figure BDA00002947909100021
Preferably, note by ratio of weight and the number of copies, the consumption of each composition is:
Figure BDA00002947909100022
Wherein, described filler is mannose; Described enteric material is selected from least one in cellulose acetate-phthalate, cellulose acetate benzenetricarboxylic acid ester and Lac; Described plasticizer is triethyl citrate; Described antiplastering aid is Pulvis Talci.
Wherein, described enteric material is preferably cellulose acetate-phthalate and Lac; Most preferably, the weight ratio of cellulose acetate-phthalate and Lac is 3:1.
Propylene glycol alginate sodium sulfate enteric coated capsule of the present invention can be prepared as follows:
(1) get propylene glycol alginate sodium sulfate and mix homogeneously with filler, take 85% ethanol as binding agent, make 20~30 object propylene glycol alginate sodium sulfate micropills, for subsequent use;
(2) with 80% dissolve with ethanol enteric material, plasticizer, antiplastering aid, make enteric coating liquid;
(3) enteric coating liquid preparing is evenly sprayed to the propylene glycol alginate sodium sulfate micropill surface that step (1) prepares, after being dried, obtains alginate diester sodium enteric-coated pellet.
(4) alginate diester sodium enteric-coated pellet is packed in capsule shells, obtains final product.
The propylene glycol alginate sodium sulfate enteric coated capsule the present invention relates to has following beneficial effect:
(1) steady quality, enteric is satisfactory for result, can improve bioavailability;
(2) selected adjuvant is common, and preparation technology is simple, and products obtained therefrom steady quality is applicable to large-scale production and application.
The specific embodiment
Below in conjunction with embodiment, the specific embodiment of the present invention is further described, advantage and disadvantage of the present invention will be more clear along with description.But these embodiment are only exemplary, scope of the present invention are not formed to any restriction.It will be understood by those skilled in the art that lower without departing from the spirit and scope of the present invention and can the details of technical solution of the present invention and form be modified or be replaced, but these modifications and replacement all fall within the scope of protection of the present invention.
A preparation method for propylene glycol alginate sodium sulfate enteric coated capsule, comprises the following steps:
(1) get propylene glycol alginate sodium sulfate and mix homogeneously with filler, take 85% ethanol as binding agent, make 20~30 object propylene glycol alginate sodium sulfate micropills, for subsequent use;
(2) with 80% dissolve with ethanol enteric material, plasticizer, antiplastering aid, make enteric coating liquid;
(3) enteric coating liquid preparing is evenly sprayed to the propylene glycol alginate sodium sulfate micropill surface that step (1) prepares, after being dried, obtains alginate diester sodium enteric-coated pellet.
(4) alginate diester sodium enteric-coated pellet is packed in capsule shells, obtains final product.
The preparation of embodiment 1~6 propylene glycol alginate sodium sulfate enteric coated capsule
The supplementary material of according to the form below, by above-mentioned preparation method, makes the propylene glycol alginate sodium sulfate enteric coated capsule of six embodiment.Wherein, "/" representative is not used.
Figure BDA00002947909100031
The dissolution determination of test example 1 embodiment 1~6 gained propylene glycol alginate sodium sulfate enteric coated capsule
According to dissolution method (60 page of second method of Chinese Pharmacopoeia two appendix of version in 2000), precision takes appropriate alginate diester sodium enteric-coated pellet, dissolution medium is respectively: pH1.2 simulated gastric fluid and pH6.8 simulated intestinal fluid, respectively take simulated gastric fluid and simulated intestinal fluid as solvent, measure dissolution.The results are shown in Table 1 and table 2.
Table 1 embodiment 1~6 propylene glycol alginate sodium sulfate enteric coated capsule dissolution investigation table in simulated gastric fluid
? 30min 1h 2h 3h 4h
Embodiment 1 6.5% 7.5% 9.7% 10.4% 11.4%
Embodiment 2 7.6% 9.4% 10.1% 11.8% 12.9%
Embodiment 3 5.6% 6.1% 8.2% 9.8% 11.7%
Embodiment 4 7.4% 8.4% 9.8% 11.2% 12.0%
Embodiment 5 5.2% 5.7% 6.3% 7.2% 8.4%
Embodiment 6 8.5% 9.8% 10.2% 11.3% 12.3%
As can be seen from Table 1, the stripping in pH1.2 simulated gastric fluid of the prepared propylene glycol alginate sodium sulfate enteric coated capsule of embodiment 1~6 is slow, 4h stripping is the highest by only 12.9%, there is good acid resistance, wherein the propylene glycol alginate sodium sulfate enteric coated capsule 4h stripping of embodiment 5 is minimum, illustrates that the propylene glycol alginate sodium sulfate enteric coated capsule acid resistance that uses cellulose acetate-phthalate and Lac to make as the enteric material of coating is best.
Table 2 embodiment 1~6 propylene glycol alginate sodium sulfate enteric coated capsule dissolution investigation table in simulated intestinal fluid
? 5min 10min 15min 20min 30min 40min 50min 60min
Embodiment 1 15.6% 40.3% 55.4% 64.6% 73.1% 79.0% 82.2% 84.1%
Embodiment 2 14.2% 38.7% 50.9% 62.2% 71.0% 78.5% 83.7% 85.2%
Embodiment 3 16.3% 45.8% 60.0% 71.2% 76.3% 79.4% 80.2% 82.6%
Embodiment 4 13.5% 33.6% 48.3% 60.6% 71.2% 76.2% 78.4% 80.0%
Embodiment 5 17.7% 44.9% 60.2% 72.8% 83.4% 86.2% 89.0% 91.4%
Embodiment 6 16.7% 40.2% 54.8% 65.9% 74.6% 80.1% 82.5% 84.4%
As can be seen from Table 2, the prepared propylene glycol alginate sodium sulfate enteric coated capsule of embodiment 1~6 discharges rapidly in pH6.8 simulated intestinal fluid, can reach the object of rapid release, wherein propylene glycol alginate sodium sulfate enteric coated capsule dissolution in 60min of embodiment 5 is the highest, illustrates that the propylene glycol alginate sodium sulfate enteric coated capsule rapid release effect in intestinal that uses cellulose acetate-phthalate and Lac to make as the enteric material of coating is best.
The preparation of embodiment 7~13 propylene glycol alginate sodium sulfate enteric coated capsulees
The supplementary material of according to the form below, by above-mentioned preparation method, each embodiment makes respectively propylene glycol alginate sodium sulfate enteric coated capsule.The cellulose acetate-phthalate of embodiment 7 and the weight ratio of Lac are 4:1, the cellulose acetate-phthalate of embodiment 8 and the weight ratio of Lac are 3:1, the cellulose acetate-phthalate of embodiment 9 and the weight ratio of Lac are 2:1, the cellulose acetate-phthalate of embodiment 10 and the weight ratio of Lac are 1:1, the cellulose acetate-phthalate of embodiment 11 and the weight ratio of Lac are 1:2, the cellulose acetate-phthalate of embodiment 12 and the weight ratio of Lac are 1:3, the cellulose acetate-phthalate of embodiment 13 and the weight ratio of Lac are 1:4.
Figure BDA00002947909100051
The propylene glycol alginate sodium sulfate enteric coated capsule dissolution determination of test example 2 embodiment 7~13 gained
Assay method is with test example 1.Measurement result is in table 3 and table 4.
Table 3 embodiment 7~13 propylene glycol alginate sodium sulfate enteric coated capsulees dissolution investigation table in simulated gastric fluid
? 30min 1h 2h 3h 4h
Embodiment 7 5.5% 6.5% 7.2% 8.0% 9.6%
Embodiment 8 4.3% 5.1% 5.9% 6.7% 7.0%
Embodiment 9 6.1% 7.0% 7.8% 9.0% 9.6%
Embodiment 10 5.2% 5.7% 6.3% 7.2% 8.4%
Embodiment 11 6.8% 8.1% 9.2% 10.0% 10.9%
Embodiment 12 7.2% 8.4% 9.7% 10.4% 11.6%
Embodiment 13 7.0% 7.9% 8.7% 9.9% 11.0%
As known from Table 3, the stripping in pH1.2 simulated gastric fluid of the prepared propylene glycol alginate sodium sulfate enteric coated capsule of embodiment 8 is the slowest, when the weight ratio that enteric material cellulose acetate-phthalate and Lac is described is 3:1, prepared propylene glycol alginate sodium sulfate enteric coated capsule acid resistance is best.
Table 4 embodiment 7~13 propylene glycol alginate sodium sulfate enteric coated capsulees dissolution investigation table in simulated intestinal fluid
? 5min 10min 15min 20min 30min 40min 50min 60min
Embodiment 7 17.0% 41.2% 55.3% 68.9% 73.2% 80.0% 85.3% 88.9%
Embodiment 8 19.3% 56.6% 70.2% 78.3% 84.1% 88.9% 91.3% 95.2%
Embodiment 9 18.0% 48.9% 65.4% 75.8% 80.3% 84.2% 88.7% 92.5%
Embodiment 10 17.7% 44.9% 60.2% 72.8% 83.4% 86.2% 89.0% 91.4%
Embodiment 11 16.1% 46.8% 56.8% 67.3% 73.1% 79.5% 83.6% 86.7%
Embodiment 12 15.5% 40.2% 57.8% 66.8% 74.2% 78.9% 82.4% 86.8%
Embodiment 13 16.0% 43.7% 59.0% 69.3% 76.1% 79.5% 84.1% 89.6%
As known from Table 3, the prepared propylene glycol alginate sodium sulfate enteric coated capsule of embodiment 8 discharges rapidly in pH6.8 simulated intestinal fluid, in 60min, dissolution is the highest, when the weight ratio that enteric material cellulose acetate-phthalate and Lac is described is 3:1, prepared propylene glycol alginate sodium sulfate enteric coated capsule rapid release effect in intestinal is best.
In sum, known when using cellulose acetate-phthalate and Lac as enteric material, and both weight ratios are while being 3:1, prepared propylene glycol alginate sodium sulfate enteric coated capsule acid resistance in gastric juice is good, in intestinal juice stripping rapid, dissolution is high, effect is best.

Claims (4)

1. a propylene glycol alginate sodium sulfate enteric coated capsule, incapsulate in shell and make by alginate diester sodium enteric-coated pellet, described alginate diester sodium enteric-coated pellet is made up of propylene glycol alginate sodium sulfate micropill and the enteric coat layer being wrapped in outside propylene glycol alginate sodium sulfate micropill, described propylene glycol alginate sodium sulfate micropill comprises propylene glycol alginate sodium sulfate and filler, described enteric coat layer comprises enteric material, plasticizer and antiplastering aid, it is characterized in that: note by ratio of weight and the number of copies, the consumption of each composition is:
Figure FDA0000469929250000011
Described enteric material is that the weight ratio of cellulose acetate-phthalate and described Lac is 3:1.
2. according to propylene glycol alginate sodium sulfate enteric coated capsule claimed in claim 1, it is characterized in that: note by ratio of weight and the number of copies, the consumption of each composition is:
Figure FDA0000469929250000012
3. according to propylene glycol alginate sodium sulfate enteric coated capsule claimed in claim 2, it is characterized in that: described filler is mannose; Described plasticizer is triethyl citrate; Described antiplastering aid is Pulvis Talci.
4. the method for the propylene glycol alginate sodium sulfate enteric coated capsule described in preparation claim 1~3 any one, comprise the following steps: (1) is got propylene glycol alginate sodium sulfate and mixed homogeneously with filler, take 85% ethanol as binding agent, make 20~30 object propylene glycol alginate sodium sulfate micropills, for subsequent use;
(2) with 80% dissolve with ethanol enteric material, plasticizer, antiplastering aid, make enteric coating liquid;
(3) enteric coating liquid preparing is evenly sprayed to the propylene glycol alginate sodium sulfate micropill surface that step (1) prepares, after being dried, obtains alginate diester sodium enteric-coated pellet;
(4) alginate diester sodium enteric-coated pellet is packed in capsule shells, obtains final product.
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Title
中药肠溶制剂研究进展;尹进朝等;《中成药》;20110228;第33卷(第2期);第315-318页 *
尹进朝等.中药肠溶制剂研究进展.《中成药》.2011,第33卷(第2期),第315-318页.
藻酸双醋钠引起胃出血一例报告分析;郭云欣等;《山东医药工业》;20001231;第19卷(第2期);第55-56页 *
郭云欣等.藻酸双醋钠引起胃出血一例报告分析.《山东医药工业》.2000,第19卷(第2期),第55-56页.

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