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Pharmaceutical compositions having a selected release duration

A composition and polymer technology, applied in the direction of drug delivery, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as not suitable for patients, and achieve the effect of easy production

Pending Publication Date: 2020-08-07
FORESEE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, such dispersed phases can be used to make microspheres, but are not suitable for administration to patients by direct injection

Method used

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  • Pharmaceutical compositions having a selected release duration
  • Pharmaceutical compositions having a selected release duration
  • Pharmaceutical compositions having a selected release duration

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0116] Example 1: Stability of peptide agents and biodegradable polymers in injectable polymer compositions

[0117] Poly(DL-lactide-co-glycolide) (PLGA) having a lactide to glycolide ratio of 85 / 15 with laurate end groups was dissolved in N-methyl-2-pyrrolidone ( NMP) to obtain a 50% by weight solution. The leuprolide salt and PLGA solution were mixed in NMP at the ratios shown in Table 1 to obtain a homogeneous injectable composition. The injectable composition is filled into a 1.2 mL polypropylene syringe with a luer-lock tip. The prefilled syringe is then sealed using the Luer lock cap. Capped syringes were packaged in containers and sealed under vacuum in plastic bags, then stored at 4°C and room temperature (approximately 22°C) for up to 18 months. Injectable compositions were sampled at 24 hour, 1, 2, 3, 6, 12 and 18 month time points. The purity of leuprolide in the samples was determined by HPLC. The molecular weight of the polymers was determined by gel permeati...

Embodiment 2

[0130] Example 2: Delivery of Leuprolide Over 6 Months

[0131] 45 mg provides continuous delivery of leuprolide acetate for 6 months. The product is supplied in two separate syringes, leuprolide acetate in one syringe and polymer solution in the other. Mix the two immediately before injection. The polymer solution contained a 50% solution of 8515PLGA polymer in NMP. The molecular weight of the polymer is about 20k Daltons. Comparable formulations were made using leuprolide mesylate at a molar ratio of methanesulfonic acid to leuprolide of 1.55:1 (LAMS(1.55)) and a similar 8515PLGA polymer. The polymer also has a molecular weight of approximately 20,000 Daltons and a polydispersity index (PDI) of 1.7. Leuprolide mesylate is prepared from leuprolide acetate by ion-exchange lyophilization, which contains a small amount of acetate. The formulations are mixed and stored in a single syringe. Another formulation was prepared with LAMS using a PLA polymer with a molecular wei...

Embodiment 3

[0133] Example 3: In vivo delivery of leuprolide over 6 months

[0134] The aim of this study was to characterize the pharmacokinetics of a depot containing leuprolide mesylate after a single subcutaneous administration in male rats for 7 months and to investigate the effect of different polymers following SC administration and activity of the preparation. 45 mg was used as a reference drug. Leuprolide (LA) release was determined by analyzing the serum concentration of LA over time following SC administration.

[0135] Male rats were divided into groups (6 per group) and received the following leuprolide mesylate (LAMS 1.55) formulations. 55.2% 8515PLGA-3 / 44.8% NMP (irradiation dose 25kGy), 57.6% PLA-1 / 42.4% NMP (irradiation dose 25kGy), or reference drug 45mg. 8515PLGA-3 polymer has a molecular weight similar to 45 mg (20k) molecular weight, the PLA-1 polymer has a molecular weight of 15k. Blood samples were collected before and after dosing up to Day 196. figure 2...

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Abstract

The present invention provides for a stabilized biodegradable polymeric composition useful as a controlled release delivery system for peptide agents. The compositions of the present invention comprise a) a strong acid salt of a LHRH agonist or antagonist; b) a biodegradable polymer of poly(lactide-co-glycolide), wherein the ratio of lactide: glycolide of the copolymer is from 50:50 to about 100:0; and c) N-methyl-2-pyrrolidone (NMP), wherein the composition does not contain excess strong acid in addition to the strong acid used to form the salt of the LHRH agonist or antagonist. The composition, when injected, can provide a controlled release of leuprolide for a period of up to 6 months.

Description

[0001] field of invention [0002] The present invention relates to delivery systems for the sustained and controlled release of peptides with tailored delivery durations, and methods of preparing such compositions. Background technique [0003] Many peptide agents are unstable because they are easily hydrolyzed or degraded by enzymes in vivo, resulting in very short circulating half-lives. Therefore, most peptide drugs are administered by injection, usually multiple times a day. However, administration by injection is painful, very expensive and inconvenient. Often, patient compliance is very challenging. For many peptide agents, especially hormones, it is required that the drug be delivered continuously at a controlled rate over a long period of time, thus requiring a controlled release delivery system. Such systems can be provided by incorporating peptides into biodegradable and biocompatible polymer matrices. Biocompatible and biodegradable polymers have been used as d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/09A61K47/34A61K9/00
CPCA61K38/09A61K9/0024A61K47/34A61K47/22A61K9/00
Inventor 李雨华A·瓜里诺
Owner FORESEE PHARMA CO LTD
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