Oral preparation for slowing down absorption of alpha-glycosidase inhibitor and enhancing hypoglycemic drug effect

A technology of glycosidase inhibitors and oral preparations, which is applied in the field of application, can solve the problems of not being able to inhibit α-glucosidase, and achieve the effects of increasing the action time, improving drug efficacy, and delaying absorption

Active Publication Date: 2011-10-12
NANKAI UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to solve the problem that the existing α-glucosidase inhibitors are rapidly absorbed into the blood in the body and cannot inhibit the role of α-glucosidase in the small intestine

Method used

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  • Oral preparation for slowing down absorption of alpha-glycosidase inhibitor and enhancing hypoglycemic drug effect
  • Oral preparation for slowing down absorption of alpha-glycosidase inhibitor and enhancing hypoglycemic drug effect
  • Oral preparation for slowing down absorption of alpha-glycosidase inhibitor and enhancing hypoglycemic drug effect

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] The formulation and preparation process of embodiment 1 alpha-glucosidase inhibitor oral preparation

[0020] Table 1. Formulations of Oral Formulations of Alpha-Glucosidase Inhibitors

[0021]

[0022] Tablet preparation process in oral formulations of alpha-glucosidase inhibitors (1-12)

[0023] Take by weighing 12.5 grams of α-glucosidase inhibitor dry powder according to the ratio of Table 1 (1-12) and sieve and mix with 62.5 grams of corresponding adhesive auxiliary materials to obtain 75 grams of bulk drug powder; then press bulk drug powder: mannitol=3: 1 Weigh 25 grams of mannitol, sieve and mix with raw drug powder; add an appropriate amount of 95% ethanol as a wetting agent, make a soft material, extrude and sieve to obtain granules, dry the granules, and add 0.3% stearic acid Magnesium, granulated, mixed evenly, adjust the lower punch and upper punch of the tablet press to an appropriate pressure, and tablet. The corresponding α-glucosidase inhibitor tab...

Embodiment 2

[0046] Example 2. Effect of adjuvant on α-glucosidase inhibitory activity

[0047] Select sodium carboxymethylcellulose, hydroxyethylcellulose, methylcellulose, and β-cyclodextrin respectively as adhesive auxiliary materials, and prepare No. 1-4 acarbose sustained-release preparations in Table 1 and 5- No. 8 voglibose sustained-release preparation, to investigate the effect of adding excipients on the inhibitory activity of α-glucosidase inhibitor acarbose or voglibose. The change in inhibitory activity was measured by detecting the amount of glucose produced by the reaction of α-glucosidase with the substrate starch. Take 1 milliliter of 5% of the above-mentioned various auxiliary materials and add them to the test tube, then add 30 microliters of serial dilutions (10, 1, 10 -1 , 10 -2 , 10 -3 , 10 -4 , 10 -5 mg / ml) acarbose or voglibose solution and 25 μl rat-derived α-glucosidase crude enzyme solution, vortexed and added 1 mg / ml starch solution 100 μl as The substrate...

Embodiment 3

[0048] Example 3. Effects of different excipients on glucose production and transport

[0049] In order to further study the effect of adding adhesion excipients on glucose production and transport, using the inverted intestinal sac experimental model, select male SD rats fasted for 16 hours, kill them and take out the small intestine, cut the small intestine into small pieces of 3.5-4.0 cm, and invert the small intestine. One end of the inverted intestinal sac was ligated with cotton thread, and 200 microliters of Krebs-Henseleit buffer was poured into the intestinal sac from the other end and ligated. The intestinal pouch was filled with 4 ml of 1% starch aqueous solution, and No. 9-12 miglitol sustained-release preparations in Table 1 were added, and the same dose of miglitol solution alone was used as a control. Incubate for 60 minutes at 37°C in a shaking water bath. The reaction was terminated by adding 10 μl of 1 molar hydrochloric acid solution. Collect the liquid i...

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Abstract

The invention discloses an oral preparation for slowing down the absorption of an alpha-glycosidase inhibitor and enhancing a hypoglycemic drug effect. The preparation is an oral preparation prepared by adding the following adhesive auxiliary materials based on the certain proportion: carboxymethyl cellulose, hydroxyethyl cellulose, methyl cellulose or beta-cyclodextrin and the like, to each alpha-glycosidase inhibitor (acarbose, voglibose, miglitol, 1-deoxynojirimycin and extract of the 1-deoxynojirimycin). Compared with singly taken alpha-glycosidase inhibitors, the adhesives can be used for prolonging the action time of the alpha-glycosidase inhibitor in the intestine, slowing down the absorption of a medicament and glucose in the intestine and further reducing a plasma concentration, thus the hypoglycemic drug effect is improved. The oral preparation disclosed by the invention can be applied to the prevention and therapy of diseases, such as diabetes, obesity and the like.

Description

【Technical field】 [0001] The invention relates to oral preparations for delaying and reducing the absorption of alpha-glucosidase inhibitors, enhancing their intestinal action time, and improving the efficacy of hypoglycemic drugs, and their application in treating diabetes and the like. 【Background technique】 [0002] Diabetes mellitus is a complex etiological metabolic syndrome with persistent high blood sugar as the basic biochemical feature. It is a disease caused by the disorder of glucose metabolism, fat metabolism and protein metabolism in the body due to insufficient insulin secretion or impaired insulin action. It is manifested by an abnormally high concentration of glucose in the blood. Excessive blood sugar and urine sugar may cause typical symptoms of "three excesses and one deficiency", namely polydipsia, polyuria, polyphagia and weight loss, accompanied by fatigue and weakness. The World Health Organization divides diabetes into two types. Type 1 diabetes (ins...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/08A61K47/38A61K47/40A61K31/7036A61K31/133A61K31/445A61P3/10A61P3/04
Inventor 侯媛媛白钢王利强白芳彭佳敏朱元元王欣聂万达朱晓丹
Owner NANKAI UNIV
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