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Calcium dobesilate medical composition with high drug loading capacity

A technology of calcium dobesilate and high drug loading, which is applied in drug combination, drug delivery, anhydride/acid/halide active ingredients, etc. It can solve the problems of large tablets, reduced drug compliance, and slow onset of action

Inactive Publication Date: 2013-06-26
SHANGHAI FOSUN PHARMA DEV CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since the dose of calcium dobesilate itself is relatively large, and a certain amount of skeleton material must be used, it may cause the unit dose of the tablet to be too large, and the patient's compliance with medication will be reduced.
Membrane-controlled sustained-release technology also has the same problem. For calcium dobesilate with good water solubility, a relatively large amount of sustained-release membranes needs to be packaged to achieve the desired sustained-release effect. The problem of reduced compliance
At the same time, calcium dobesilate immediate-release tablets can only reach the maximum blood concentration 6 hours after administration, and the onset of effect is relatively slow, while membrane-controlled sustained-release preparations often basically do not release drugs within 1-2 hours of the early release period. Relatively slower release is unable to meet clinical needs

Method used

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  • Calcium dobesilate medical composition with high drug loading capacity
  • Calcium dobesilate medical composition with high drug loading capacity
  • Calcium dobesilate medical composition with high drug loading capacity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] formula:

[0070]

[0071]

[0072] Preparation: According to the prescription of the sustained release part, 25 grams of hypromellose was made into a 10% aqueous solution, 450 grams of calcium dobesilate and 25 grams of microcrystalline cellulose were mixed evenly, and the aqueous solution of hypromellose E3 was added to the The wet material is prepared in a high-speed stirring granulator, and the wet material is extruded and spheronized by an extrusion spheronizer to obtain drug-containing pellets (extrusion port screen 1.0mm), and the drug-containing pellets are dried at 50°C for 2-4 After drying, collect the pellets between 0.4mm-1.4mm as quick-release pellets; in addition, 167 grams of polyacrylic resin NE30D (30% solid content) and 50 gram talcum powder are made into the coating of 20% solid content water dispersion, coating the collected drug-containing pellets to obtain sustained-release coated pellets.

[0073] According to the prescription of the immedi...

Embodiment 2

[0076] formula:

[0077]

[0078] Preparation: 15 grams of hypromellose E6 in the slow-release part was made into a 10% aqueous solution, and 300 grams of calcium dobesilate were granulated in a high-speed stirring granulator with the aqueous solution of hypromellose E6, at 50 Dry at ℃ for 2-4 hours, pass through a 1.4mm sieve after drying, mix the sieved dry granules, 100 grams of hypromellose K15M, 4 grams of silicon dioxide and 1 gram of magnesium stearate, and set aside.

[0079] Mix 10 grams of hypromellose E6 and 200 grams of calcium dobesilate in the immediate release part evenly, add 80 grams of purified water, wet granulate in a high-speed stirring granulator, and dry at 50°C for 2-4 hours. Pass through a 1.4mm sieve after drying, mix the sieved dry granules, 2 grams of silicon dioxide and 0.5 gram of magnesium stearate, and set aside.

[0080] The two-part granules are compressed into a double-layer tablet by using a double-layer tablet press machine, with the su...

Embodiment 3

[0082] formula:

[0083]

[0084] Preparation: 25 grams of hypromellose E3 in the slow-release part was made into a 10% aqueous solution, 450 grams of calcium dobesilate and 45 grams of microcrystalline cellulose were mixed evenly, and the aqueous solution of hypromellose E3 was used at high speed The wet material was prepared in a stirring granulator, dried at 50°C for 2-4 hours, passed through a 1.4mm sieve after drying, mixed the sieved granules, 4 grams of silicon dioxide and 1 gram of magnesium stearate, and pressed piece. 167 grams of polyacrylic resin NE30D (30% solid content) and 50 grams of talcum powder of the slow-release part are made into the coating aqueous dispersion of 20% solid content, and the above-mentioned tablet core is coated to obtain a slow-release coating piece.

[0085] Disperse and dissolve 15 grams of polyacrylic acid resin E100 and 50 grams of calcium dobesilate in 800 grams of isopropanol for the immediate-release part, and coat the above-me...

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Abstract

The invention provides a calcium dobesilate medical composition with high drug loading capacity. The composition comprises a quick release part and a slow release part and is combined by the two parts in a single unit or multiple units. The calcium dobesilate in the quick release part accounts for 10-40% of total weight of calcium dobesilate, while the calcium dobesilate in the slow release part accounts for 60-90% of total weight of calcium dobesilate. The single dose of the composition comprises 500-100mg of calcium dobesilate. According to Chinese pharmacopoeia, in pH6.8 buffer liquid, the quick release part of the calcium dobesilate medical composition is quickly released within 30 minutes by a dissolution rate detection slurry method, and the total release amount of calcium dobesilate reaches over 80% of the total weight in 12-16 hours. According to the invention, not only is medicine in initial period relatively more released to solve the problem of over-slow effect of the medicine, but also good slow release effect can be obtained just by relatively less amount of slow release auxiliary materials because calcium dobesilate in the slow release part is reduced, thereby avoiding the problem that the preparation in unit dosage is overlarge and hard to swallow. The composition has greater clinical application value. The composition provided by the invention is simple and accessible and is suitable for industrialized production.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to a pharmaceutical composition of calcium dobesilate with high drug load. Background technique [0002] "Diabetes" is a disease in which glucose in the blood tends to accumulate excessively. Its alias is "silent killer" (Silent Killer), especially "adult-onset diabetes", and the prevalence rate of middle-aged people over the age of 40 is particularly high. Once suffering from "diabetes", life expectancy will be reduced by as much as ten years, and possible complications can spread throughout the body. Among these complications, retinopathy, nephropathy and neurological disorder are the most frequent, which are called "three major complications" of "diabetes". While controlling and treating diabetes, it is necessary to treat these complications. Calcium dobesilate has its unique curative effect in the treatment of retinopathy, and calcium dobesilate is by inhibiting the high-throug...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K9/24A61K9/32A61K9/36A61K9/52A61K31/185A61P9/10
Inventor 何平钱晓明
Owner SHANGHAI FOSUN PHARMA DEV CO LTD
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