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Osmotic pump controlled release tablet of solid dispersion of hydroxy camptothecin and prepn. method

A technology of hydroxycamptothecin and solid dispersions, which is applied in the direction of medical preparations containing non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc. Low-level problems, to achieve sustained drug release, improve bioavailability, and constant-rate release

Inactive Publication Date: 2006-12-06
TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the extremely low solubility of hydroxycamptothecin, the osmotic pump tablet of the above form still cannot achieve constant release of the drug.

Method used

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  • Osmotic pump controlled release tablet of solid dispersion of hydroxy camptothecin and prepn. method
  • Osmotic pump controlled release tablet of solid dispersion of hydroxy camptothecin and prepn. method
  • Osmotic pump controlled release tablet of solid dispersion of hydroxy camptothecin and prepn. method

Examples

Experimental program
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preparation example Construction

[0034] Wherein, the hydroxycamptothecin solid dispersion is prepared by mixing hydroxycamptothecin with a mass ratio of 1:2-1:30 and a polymer carrier, and the preparation method includes: melting method, solvent-melting preparation coprecipitation method and spray drying, etc.

[0035] The core of the single-layer osmotic pump tablet is prepared according to the following process: the solid dispersion of hydroxycamptothecin, the excipients with controlled release effect and other excipients are pulverized and sieved respectively, mixed evenly, and the soft material is made with a binder, and the sieve is made. After granulation, it is dried at 50°C, sieved again for granulation, and pressed into tablet cores by adding lubricant.

[0036] The core of the push-pull osmotic pump tablet is prepared according to the following process: the solid dispersion of hydroxycamptothecin, the excipients with controlled release effect and other excipients are pulverized and sieved respective...

Embodiment 1

[0039] Example 1: Preparation of hydroxycamptothecin bilayer osmotic pump tablet

[0040] Using film coating technology, wet granulation and tableting, laser drilling is performed on the coating film of the drug-containing layer as drug release holes. Wherein the preparation of hydroxycamptothecin solid dispersion adopts solvent-melting method.

[0041] The composition of the hydroxycamptothecin solid dispersion is (mass percent):

[0042] Hydroxycamptothecin 17%

[0043] Macrogol 6000 83%

[0044] The content composition of each 100 osmotic pump tablets is as follows:

[0045] The composition of the drug-containing layer of the tablet core is:

[0046] Hydroxycamptothecin solid dispersion 9g

[0047] Polyoxyethylene 50 4g

[0048] Sodium Chloride 4g

[0049] Lactose 3g

[0050] Magnesium Stearate 0.05g

[0051] The push layer consists of:

[0052] Polyoxyethylene 550 4g

[0053] Hydroxypropyl methylcellulose 1g

[0054] Sodium Chloride 2g

[0055] Lactose 3g

[...

Embodiment 2

[0063] Example 2: Preparation of hydroxycamptothecin bilayer osmotic pump tablet

[0064] As in Example 1, hydroxycamptothecin was prepared into a double-layer osmotic pump tablet. In this example, the preparation of the hydroxycamptothecin solid dispersion adopts the coprecipitation method.

[0065] The composition of the hydroxycamptothecin solid dispersion is (mass percent):

[0066] Hydroxycamptothecin 14%

[0067] Polyvinylpyrrolidone (K30) 86%

[0068] The content composition of each 100 osmotic pump tablets is as follows:

[0069] The composition of the drug-containing layer of the tablet core is:

[0070] Hydroxycamptothecin solid dispersion 9g

[0071] Polyoxyethylene 50 4g

[0072] Sodium Chloride 4g

[0073] Lactose 3g

[0074] Magnesium Stearate 0.05g

[0075] The push layer consists of:

[0076] Polyoxyethylene 550 4g

[0077] Hydroxypropyl methylcellulose 1g

[0078] Sodium Chloride 2g

[0079] Lactose 3g

[0080] Magnesium Stearate 0.05g

[0081] ...

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Abstract

A tablet of the dispersed hydroxy camptothecine solid released under the control of osmotic pump is composed of a tablet core containing dispersed hydroxy camptothecine solid, release controlling auxiliaries, and carrier and a perforated coated layer. Its preparing process includes preparing tablet core, coating and perforating.

Description

technical field [0001] The invention relates to the technical field of preparations, specifically, it is a controlled-release preparation that utilizes solid dispersion solubilization technology and osmotic pump technology to realize zero-order release of hydroxycamptothecin. Background technique [0002] Hydroxycamptothecin (HCPT) is a cell cycle-specific drug. Studies have found that it can selectively inhibit DNA topoisomerase I, thereby inhibiting the replication and transcription of cancer cell DNA. It has no cross-resistance with other commonly used anticancer drugs, its anticancer effect is 30 times that of camptothecin, and its toxicity is significantly lower than that of camptothecin. Clinically, it is mostly used for digestive system cancers such as gastric cancer, esophageal cancer, liver cancer, etc. It also has good curative effect on oral cavity, neck and face cancer. Hydroxycamptothecin is a water-insoluble and lipid-insoluble drug, with rapid metabolism and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/30A61K31/475A61K47/34A61K47/38A61K47/26A61P35/00A61K47/10A61K47/32
Inventor 陈欢欢蒋国强朱德权江盛阳丁富新
Owner TSINGHUA UNIV
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