Excipients in drug delivery vehicles

A technology of excipient and vehicle, applied in the field of preparation and administration of the composition, can solve the problems of reducing the overall effectiveness of the dosage form, and the easy deterioration of beneficial components.

Inactive Publication Date: 2013-04-10
ALZA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] As a result, beneficial ingredients are susceptible to deterioration under the influence of several factors, thereby reducing the ov

Method used

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  • Excipients in drug delivery vehicles
  • Excipients in drug delivery vehicles
  • Excipients in drug delivery vehicles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0114] depot gel preparation

[0115] Gel vehicles for use in injectable depot compositions are prepared as follows. Place the glass container on a Mettler PJ3000 top loading balance. Poly(D,L-lactide-co-glycolide) (PLGA) was weighed into a glass container as 50:50 DL-PLG with an intrinsic viscosity of 0.15 (PLGA-BPI, Birmingham Polymers, Inc., Birmingham, AL), and 50:50 RG502 (PLGA RG502). The glass container containing the polymer was tared and the corresponding solvent was added. The percentages for various polymer / solvent combinations are described in Table 1 below. The polymer / solvent mixture was stirred (IKA electric stirrer, IKH-Werke GmbH and Co., Stanfen, Germany) at 250±50 rpm for about 5-10 minutes to obtain a viscous paste-like mass containing polymer particles. The vessel containing the polymer / solvent mixture was sealed and placed in a temperature-controlled incubator equilibrated to 37°C for 1 to 4 days with intermittent agitation, depending on solvent to ...

Embodiment 2

[0118] Bupivacaine base preparation

[0119] Bupivacaine hydrochloride (Sigma-Aldrich Corporation, St. Louis, MO) was dissolved in deionized (DI) water at a concentration of 40 mg / ml (saturated). To this solution was added a calculated amount of sodium hydroxide (1 N solution) to adjust the pH of the final mixture to 10 to precipitate out the BP base. The precipitated product was filtered and further washed with DI water at least three times. The precipitated product was dried under vacuum at about 40°C for 24 hours.

Embodiment 3

[0121] Bupivacaine particle preparation

[0122] Bupivacaine drug particles were prepared using bupivacaine hydrochloride (Sigma-Aldrich Corporation, St. Louis, MO) or bupivacaine base and hydrochloride prepared according to Example 2 as follows. Bupivacaine was ground and then sieved using a 3" stainless steel sieve. Typical ranges included 25 μm to 38 μm, 38 μm to 63 μm, and 63 μm to 125 μm.

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Abstract

The present invention provides injectable depot gel compositions and kits that provide rate-modifying excipients to stabilize beneficial ingredients. Methods of administering and preparing such systems are also provided. The gel composition comprises a biodegradable, bioerodible polymer and a water-immiscible solvent in an amount effective to plasticize the polymer and form a gel with the polymer. Suitable excipients include pH modifiers, reducing agents and antioxidants.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of U.S. Provisional Application No. 60 / 519,972, filed November 14, 2003, and U.S. Patent Application No. 10 / ., ..., ..., filed November 10, 2004, incorporated herein by reference Reference. field of invention [0003] The present invention generally relates to sustained release depot compositions and kits which provide sustained release of beneficial ingredients. The invention also relates to methods of making and administering said compositions. Background of the invention [0004] Biodegradable polymers have been used in medical applications for many years. Examples of devices composed of biodegradable polymers include sutures, surgical clips, medical staples, implants, and drug delivery systems. Most of these biodegradable polymers are based on glycolide, lactide, caprolactone and their copolymers. [0005] Biodegradable polymer formulations for injectable implants employ solv...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61F13/00
Inventor 陈国华D·T·普里贝
Owner ALZA CORP
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