CN105687213A - Glipizide/voglibose hypoglycemic oral preparation composition and preparation method thereof - Google Patents
Glipizide/voglibose hypoglycemic oral preparation composition and preparation method thereof Download PDFInfo
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- CN105687213A CN105687213A CN201410690757.8A CN201410690757A CN105687213A CN 105687213 A CN105687213 A CN 105687213A CN 201410690757 A CN201410690757 A CN 201410690757A CN 105687213 A CN105687213 A CN 105687213A
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Abstract
The present invention discloses a glipizide/voglibose hypoglycemic oral preparation composition and a preparation method thereof, and the glipizide/voglibose hypoglycemic oral preparation composition comprises the following raw materials: 2-6% by weight of main components, 50-90% by weight of a filler, 5-15% by weight of a disintegrant, 0.1-3% by weight of a binder, 0.01-5% by weight of a lubricant. The main components comprise 2.5mg-5mg of glipizide and 0.1mg-0.3mg of voglibose, and auxiliary materials comprises the filler, the disintegrant, the binder and the lubricant. The glipizide/voglibose hypoglycemic oral preparation composition has the advantages of complementary main material action mechanism, multi targets, good patient compliance, and the like, and is more applicable to type 2 diabetes patients of which blood-glucose rises after meals and fasting blood-glucose rises insignificantly.
Description
Technical field
The invention belongs to pharmaceutical technology field, be specifically related to a kind of glipizide/voigelibo sugar-lowering oral preparation and preparation method thereof。
Background technology
Type 2 diabetes mellitus original name Adult Onset's patients with type Ⅰ DM, how the sequela of 35～40 years old, accounts for diabetics more than 90%。Type 2 diabetes mellitus produces the ability of insulin in the patient and not completely loses, the insulin in the patient having even produces too much, but the action effect of insulin is poor, therefore insulin in the patient is a kind of shortage relatively, it is possible to stimulated the secretion of internal insulin by some oral drugs。
The performance that the symptom of type ii diabetes is relevant with metabolism disorder, especially " three-many-one-little ", in type ii diabetes, often not fairly obvious or only have part performance；Additionally characteristicness is the performance of various acute, chronic complicating diseases。
1. polyuria
Being owing to blood glucose is too high, exceed renal glucose threshold (8.89～10.0mmol/L), the glucose leached through glomerule completely by reabsorption, can not form osmotic diuresis。Blood glucose is more high, and glucose in urine excretion is more many, and urine volume is more many, and 24h urine volume is up to 5000～10000ml。But old people and the person that has kidney disease, renal glucose threshold increases, glucose in urine acatharsia, and when the light moderate of blood glucose increases, polyuria can be inconspicuous。
2. polydipsia
Making plasma osmotic pressure substantially increase mainly due to hyperglycemia, in addition polyuria, loss of moist is too much, dehydration in cell occurs, increases the weight of hyperglycemia, make plasma osmotic pressure significantly raised further, stimulates thirst center, causes thirsty and polydipsia。Polydipsia increases the weight of polyuria further。
3. polyphagia
The mechanism of polyphagia is not fully aware of。Most scholar's tendencies are caused by glucose utilization rate (before and after turnover histiocyte, in arteriovenous blood, concentration of glucose is poor) reduces。In normal person's arteriovenous blood on an empty stomach, concentration of glucose difference reduces, and stimulates feeding center, produces hunger sensation；After ingesting, blood glucose raises, and arteriovenous blood level difference strengthens (more than 0.829mmoL/L), and feeding center is suppressed, and satiety center is excited, and requirement of ingesting disappears。But diabetes patient due to the absolute of insulin or relatively lack or organizes insulin insensitivity, tissue picked-up utilizes glucose ability to decline, although blood glucose is in high level, but the concentration difference of glucose is only small in arteriovenous blood, histiocyte is practically at " starvation ", thus stimulating feeding center, cause hunger, polyphagia；It addition, body can not make full use of glucose, a large amount of glucoses are excretion from urine, and therefore body is practically at semistarvation state, and energy deficiency also causes bulimia。
4. weight loss
Although diabetics appetite and appetite are normal, even increase, but weight loss, definitely or relatively lacking or insulin resistant mainly due to insulin, body can not make full use of glucose and produce energy, causes fat and breaks down proteins is strengthened, consume too much, in negative nitrogen balance, body weight is gradually reduced, or even occurs becoming thin。Once diabetes are through reasonably treatment, it is thus achieved that after good control, weight loss can control, and even gos up to some extent。As diabetics continued weight over the course for the treatment of declines or substantially becomes thin, the possible Metabolism control of prompting is not good or merges other Chronic consumptionss。
Glipizide is applicable to through diet control and 2～3 months unsatisfied light, moderate type 2 diabetes mellitus patients of curative effect of physical training；Voglibose is a kind of new oral antidiabetic drug。α-glucosidase is inhibited, thus suppressing the hydrolysis of disaccharidase and postponing the absorption to sugar。Improve the post-prandial hyperglycemia of diabetics。
Summary of the invention
It is an object of the invention to provide glipizide/voigelibo sugar-lowering oral preparation and preparation method thereof。
The purpose of the present invention is achieved through the following technical solutions: glipizide/voigelibo sugar-lowering oral preparation, major ingredient is made up of glipizide 2.5mg-5mg, voglibose 0.1mg-0.3mg, adjuvant includes filler, disintegrating agent, binding agent, lubricant composition, wherein the percentage by weight of various raw materials is, major ingredient 2～6%, filler 50～90%, disintegrating agent 5～15%, binding agent 0.1～30%, lubricant 0.01～5%。
Described filler is the mixing of one or more in microcrystalline Cellulose, calcium sulfate, calcium phosphate, xylitol。
Described disintegrating agent is the mixing of one or more in low-substituted hydroxypropyl cellulose, carboxymethylstach sodium, cross-linking sodium carboxymethyl cellulose。
Described binding agent is starch slurry or polyvidone k30 or hypromellose。
Described lubricant is one or both the mixing in magnesium stearate, sodium lauryl sulphate。
Described glipizide/voigelibo sugar-lowering oral preparation and preparation method thereof, concretely comprising the following steps of its preparation method:
Step 1, by weight percentage, chooses glipizide, voglibose, filler, disintegrating agent, binding agent, lubricant, crosses 80 mesh sieves respectively, standby；
Step 2, the glipizide by sieving, voglibose, filler, disintegrating agent mix homogeneously; mixed supplementary material is put in wet granulator; binding agent is put in feed tank; open machine, adjust parameter, open simultaneously and shear fly cutter; 2-5 minute; discharging, uses oscillating granulator, crosses 14-18 order nylon screen and granulates；
Step 3, being placed in fluidized-bed coating machine by wet granular, inlet temperature less than 50 DEG C dries, and moisture is below 4%；
Step 4, by dry granule 16-20 order steel sieve granulate；
Step 5, addition lubricant, be placed in three-dimensional motion mixer and mix 30 minutes；
Step 6, tabletting: use rotary tablet machine tabletting, tabletting speed controlling 15-20r/min, prepare finished product。
Described glipizide/voigelibo sugar-lowering oral preparation and preparation method thereof, by the formula that following weight is determined:
Glipizide 2.5mg-5mg
Voglibose 0.1mg-0.3mg
Filler 44.15mg-79.47mg
Disintegrating agent 4.415mg-13.245mg
Binding agent 0.0883mg-26.49mg
Lubricant 0.00883mg-4.415mg。
Described glipizide/voigelibo sugar-lowering oral preparation and preparation method thereof, by the formula that optimum weight is determined:
Glipizide 5mg
Voglibose 0.3mg
Microcrystalline Cellulose 55mg
Carboxymethylstach sodium 10mg
Hypromellose 16mg
Sodium lauryl sulphate 2mg。
Beneficial effects of the present invention: glimepiride of the present invention/acarbose hypoglycemic oral preparation, there is the complementation of major ingredient mechanism of action, Mutiple Targets, the advantages such as patient compliance is good, are more suitable for post-prandial glycemia and raise and the fasting glucose inapparent type 2 diabetes mellitus patient of rising。
The present invention is through two groups of clinical verifications, one of which is that treatment group takes the present invention, take the present invention every day once, it within 7 days, it is a course for the treatment of, another group matched group takes gliclazid in tablets, every day uses once, it within 7 days, it is a course for the treatment of, every group selection outpatient 110 example, wherein male 40 examples, female 70 example, max age 75 years old, minimal ages 35 years old, clinical manifestation is polyuria, polydipsia, weak, blood glucose value rising, visual disorder, weight loss, immunity degradation, and table one is the contrasting data after taking a course for the treatment of:
Table 1 is taken front and back and is compared (unit: people) two groups of courses for the treatment of
There were significant differences for treatment group and matched group, it will thus be seen that the application that the present invention is clinically has significant curative effect。
Detailed description of the invention
Embodiment 1
Glipizide/voigelibo sugar-lowering oral preparation, major ingredient is made up of glipizide 2.5mg-5mg, voglibose 0.1mg-0.3mg, adjuvant includes filler, disintegrating agent, binding agent, lubricant composition, wherein the percentage by weight of various raw materials is, major ingredient 2～6%, filler 50～90%, disintegrating agent 5～15%, binding agent 0.1～30%, lubricant 0.01～5%。
Described filler is the mixing of one or more in microcrystalline Cellulose, calcium sulfate, calcium phosphate, xylitol。
Described disintegrating agent is the mixing of one or more in low-substituted hydroxypropyl cellulose, carboxymethylstach sodium, cross-linking sodium carboxymethyl cellulose。
Described binding agent is starch slurry or polyvidone k30 or hypromellose。
Described lubricant is one or both the mixing in magnesium stearate, sodium lauryl sulphate。
Embodiment 2
Glipizide/voigelibo sugar-lowering oral preparation and preparation method thereof, concretely comprising the following steps of its preparation method:
Step 1, by weight percentage, chooses glipizide, voglibose, filler, disintegrating agent, binding agent, lubricant, crosses 80 mesh sieves respectively, standby；
Step 2, the glipizide by sieving, voglibose, filler, disintegrating agent mix homogeneously; mixed supplementary material is put in wet granulator; binding agent is put in feed tank; open machine, adjust parameter, open simultaneously and shear fly cutter; 2-5 minute; discharging, uses oscillating granulator, crosses 14-18 order nylon screen and granulates；
Step 3, being placed in fluidized-bed coating machine by wet granular, inlet temperature less than 50 DEG C dries, and moisture is below 4%；
Step 4, by dry granule 16-20 order steel sieve granulate；
Step 5, addition lubricant, be placed in three-dimensional motion mixer and mix 30 minutes；
Step 6, tabletting: use rotary tablet machine tabletting, tabletting speed controlling 15-20r/min, prepare finished product。
Embodiment 3
Glipizide/voigelibo sugar-lowering oral preparation and preparation method thereof, by the formula that following weight is determined:
Glipizide 2.5mg-5mg
Voglibose 0.1mg-0.3mg
Filler 44.15mg-79.47mg
Disintegrating agent 4.415mg-13.245mg
Binding agent 0.0883mg-26.49mg
Lubricant 0.00883mg-4.415mg。
Embodiment 4
Glipizide/voigelibo sugar-lowering oral preparation and preparation method thereof, by the formula that optimum weight is determined:
Glipizide 5mg
Voglibose 0.3mg
Microcrystalline Cellulose 55mg
Carboxymethylstach sodium 10mg
Hypromellose 16mg
Sodium lauryl sulphate 2mg。
Claims (8)
1. glipizide/voigelibo sugar-lowering oral preparation, it is characterized in that: major ingredient is made up of glipizide 2.5mg-5mg, voglibose 0.1mg-0.3mg, adjuvant includes filler, disintegrating agent, binding agent, lubricant composition, wherein the percentage by weight of various raw materials is, major ingredient 2～6%, filler 50～90%, disintegrating agent 5～15%, binding agent 0.1～30%, lubricant 0.01～5%。
2. glipizide according to claim 1/voigelibo sugar-lowering oral preparation, it is characterised in that: described filler is the mixing of one or more in microcrystalline Cellulose, calcium sulfate, calcium phosphate, xylitol。
3. glipizide according to claim 1/voigelibo sugar-lowering oral preparation, it is characterised in that: described disintegrating agent is the mixing of one or more in low-substituted hydroxypropyl cellulose, carboxymethylstach sodium, cross-linking sodium carboxymethyl cellulose。
4. glipizide according to claim 1/voigelibo sugar-lowering oral preparation, it is characterised in that: described binding agent is starch slurry or polyvidone k30 or hypromellose。
5. glipizide according to claim 1/voigelibo sugar-lowering oral preparation, it is characterised in that: described lubricant is one or both the mixing in magnesium stearate, sodium lauryl sulphate。
6. the glipizide according to claim 1-5/voigelibo sugar-lowering oral preparation and preparation method thereof, it is characterised in that: concretely comprising the following steps of its preparation method:
Step 1, by weight percentage, chooses glipizide, voglibose, filler, disintegrating agent, binding agent, lubricant, crosses 80 mesh sieves respectively, standby；
Step 2, the glipizide by sieving, voglibose, filler, disintegrating agent mix homogeneously; mixed supplementary material is put in wet granulator; binding agent is put in feed tank; open machine, adjust parameter, open simultaneously and shear fly cutter; 2-5 minute; discharging, uses oscillating granulator, crosses 14-18 order nylon screen and granulates；
Step 3, being placed in fluid bed dryer by wet granular, inlet temperature less than 50 DEG C dries, and moisture is below 4%；
Step 4, by dry granule 16-20 order steel sieve granulate；
Step 5, addition lubricant, be placed in three-dimensional motion mixer and mix 30 minutes；
Step 6, tabletting: use rotary tablet machine tabletting, tabletting speed controlling 15-20r/min, prepare finished product。
7. glipizide according to claim 1/voigelibo sugar-lowering oral preparation and preparation method thereof, it is characterised in that: the formula determined by following weight:
Glipizide 2.5mg-5mg
Voglibose 0.1mg-0.3mg
Filler 44.15mg-79.47mg
Disintegrating agent 4.415mg-13.245mg
Binding agent 0.0883mg-26.49mg
Lubricant 0.00883mg-4.415mg。
8. glipizide according to claim 1/voigelibo sugar-lowering oral preparation and preparation method thereof, it is characterised in that: the formula determined by optimum weight:
Glipizide 5mg
Voglibose 0.3mg
Microcrystalline Cellulose 55mg
Carboxymethylstach sodium 10mg
Hypromellose 16mg
Sodium lauryl sulphate 2mg。
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201410690757.8A CN105687213A (en) | 2014-11-27 | 2014-11-27 | Glipizide/voglibose hypoglycemic oral preparation composition and preparation method thereof |
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| CN201410690757.8A CN105687213A (en) | 2014-11-27 | 2014-11-27 | Glipizide/voglibose hypoglycemic oral preparation composition and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105963280A (en) * | 2016-06-30 | 2016-09-28 | 合肥华方医药科技有限公司 | Voglibose oral instant film and preparation method thereof |
-
2014
- 2014-11-27 CN CN201410690757.8A patent/CN105687213A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105963280A (en) * | 2016-06-30 | 2016-09-28 | 合肥华方医药科技有限公司 | Voglibose oral instant film and preparation method thereof |
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Application publication date: 20160622 |
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| WD01 | Invention patent application deemed withdrawn after publication |