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A preparation for improving oral bioavailability of risedronate sodium and a preparing method thereof

A technology of risedronate sodium and availability, applied in the field of medicine, to achieve the effect of improving dispersibility

Inactive Publication Date: 2014-05-14
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, water-in-oil (micro) emulsions cannot be prepared into capsule-type preparations, which limits its clinical application prospects

Method used

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  • A preparation for improving oral bioavailability of risedronate sodium and a preparing method thereof
  • A preparation for improving oral bioavailability of risedronate sodium and a preparing method thereof
  • A preparation for improving oral bioavailability of risedronate sodium and a preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1 Weigh 0.201 g of risedronate sodium hydrate (containing 0.175 g of risedronate sodium) and add 0.02 g of sucrose monolaurate (trade name: L1695; Japan Mitsubishi Chemical Foods Co., Ltd.) into 10 mL of purified water to dissolve and set aside. Another 0.173 g of sucrose sinapinate (trade name: ER290; Japan Mitsubishi Chemical Foods Co., Ltd.) was weighed in 20 mL of cyclohexane. The above two-phase solution was placed in a 50 mL eggplant-shaped bottle, and a water-in-oil (W / O) emulsion was prepared using a high-speed shear (23000 rpm, 5 min). After being frozen with liquid nitrogen, the mixture is placed in a freeze dryer for 24 hours to freeze-dry to remove the cyclohexane and the water phase, and then the compound containing the drug and the surfactant is obtained. Add 9.65 g of medium-chain fatty acid triglycerides (MCT). After being stirred uniformly, a solid-in-oil suspension containing risedronate sodium was obtained. By weight, the drug content is 1...

Embodiment 2

[0021] Example 2 Weigh 0.201 g of risedronate sodium hydrate (containing 0.175 g of risedronate sodium) and add it into 10 mL of purified water containing 0.02 g of L1695 to dissolve it for later use, and weigh 0.505 g of ER290 in 20 mL of cyclohexane. Referring to the preparation method of Example 1, a compound containing a drug and a surfactant was obtained. Add 9.3 g MCT. By weight, the drug content is 1.75%, the surfactant accounts for 5.25% (the ratio of drug to surfactant is 1:3), and the external oil phase accounts for 93%.

Embodiment 3

[0022] Example 3 Weigh 0.201 g of risedronate sodium hydrate (containing 0.175 g of risedronate sodium) and add 0.02 g of sucrose monolaurate in 10 mL of purified water to dissolve it for later use; another weigh 0.855 g of ER290 and dissolve it in 20 mL of cyclohexane alkane. Referring to the preparation method of Example 1, the complex of the drug and the surfactant was obtained. Add 8.95 g of medium-chain fatty acid triglycerides and disperse evenly to obtain a solid-in-oil suspension containing risedronate sodium. By weight, the drug accounts for 1.75%. Surfactant accounts for 8.75% (the ratio of drug to surfactant is 1:5), and the external oil phase accounts for 89.5%.

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Abstract

The invention relates to the technical field of medicine, and particularly relates to a suspension that covers a solid medicine with oil (hereinafter referred to as solid-in-oil) and a preparing method thereof, and the suspension is used for improving oral bioavailability of risedronate sodium. The solid-in-oil suspension comprises the medicine, a surfactant and an outer oil phase. The outer oil phase is mixed decanoyl and octanoyl glycerides. The adding weight of the outer oil phase is 70-96.5% of the weight of the solid-in-oil suspension. The adding weight of the surfactant is 1.75-22.5% of the weight of the solid-in-oil suspension. The adding weight of the medicine is 0.5-7.5% of the weight of the solid-in-oil suspension. The dispersity of the water soluble medicine in the oil substrate is improved by preparing a composite of the medicine and the surfactant. A proper oil substrate can be selected according to targeting parts without influences on the dispersity of the medicine in the oil.

Description

Technical field: [0001] The invention relates to the technical field of medicine, specifically, it is a suspension of a class of solid medicine in oil (hereinafter referred to as solid in oil), and provides a corresponding preparation method for improving the oral bioavailability of risedronate sodium Spend. Background technique: [0002] Risedronate sodium is the first-line treatment for osteoporosis and is widely used in the treatment of osteoporosis. When administered orally, the oral bioavailability is not only low (about 0.63%), but also causes greater irritation to the gastrointestinal tract. The dosage forms that have been marketed at home and abroad are tablets, and the dosage regimens appear successively: 5 mg / day (2.5 mg×2 times / day), 30 mg / week (17.5 mg×2 times / week), 150 mg / month (75 mg / month). mg×2 times / month), the purpose of improving the quality of life of patients can be achieved by increasing the dose and reducing the frequency of administration. Impro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/48A61K31/675A61K47/14A61P19/10
Inventor 朴洪宇肖文花崔福德朴洪泽后藤雅宏
Owner SHENYANG PHARMA UNIVERSITY
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