PT 141 Capsules (usually referring to capsule formulations containing the active ingredient PT 141) is a drug formulation based on Bremelantide (PT 141). PT 141 is a synthetic peptide analogue of melanocyte stimulating hormone (MSH), belonging to melanocortin receptor agonists. It mainly regulates sexual desire and response by acting on melanocortin receptor type 4 (MC4R) in the central nervous system. PT 141 is a cyclic heptapeptide compound with the chemical name Ac-Nle-cyclo (- Asp-His-D-Phe-Arg-Trp-Lys) - OH and a molecular weight of 1025.18. Capsule formulations may help improve the stability and bioavailability of drugs, especially for peptide drugs. The use of PT 141 should follow medical advice and should not be abused on one's own. Due to the abuse of PT 141 in certain circles (such as the LGBTQ+community), it is necessary to emphasize its strict usage standards as a prescription drug.
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PT 141 COA
Gastric acid protection technology
PT 141 Capsules (Bremelantide), as a synthetic peptide analogue of melanocyte stimulating hormone (MSH), has shown significant potential in the treatment of sexual dysfunction. However, as a peptide drug, PT 141 is easily degraded by gastric acid after oral administration, resulting in extremely low bioavailability. Therefore, when developing PT 141, it is necessary to address the issue of gastric acid protection, ensure the stability of the drug in the gastrointestinal tract, and thereby improve its bioavailability and therapeutic efficacy.
The effect of gastric acid on PT 141
Characteristics of gastric acid environment
Gastric acid is mainly composed of hydrochloric acid, with a pH value usually between 1-3 and strong acidity. This strongly acidic environment has a strong destructive effect on most drugs, especially peptide drugs. PT 141, as a cyclic heptapeptide compound, is prone to degradation in its chemical structure under acidic conditions, leading to the loss of drug activity.
Degradation mechanism of PT 141 by gastric acid
PT 141 is prone to hydrolysis reactions and peptide bond breakage in gastric acid environment, leading to the destruction of drug molecular structure. In addition, stomach acid may also trigger side reactions such as oxidation and polymerization of PT 141, further reducing the stability and bioavailability of the drug. Therefore, effective gastric acid protection techniques must be adopted when developing PT 141 capsules to prevent drug degradation in the gastrointestinal tract.
The principle of gastric acid protection technology
Enteric coating technology
Enteric coating technology is a commonly used gastric acid protection technique, which wraps a layer of enteric material on the surface of drug particles or capsules, so that the drug does not dissolve in the gastric acid environment, but dissolves and releases in the intestine. Enteric coated materials typically have pH dependence, remain stable in acidic environments, and dissolve in neutral or alkaline environments.
Nanotechnology
Nanotechnology improves the stability and permeability of drugs by preparing them into nanoparticles. Nanoparticles have a large specific surface area, which can better contact the gastrointestinal mucosa and improve the absorption efficiency of drugs. In addition, nanoparticles can enhance their adhesion to the gastrointestinal mucosa through surface modification, further prolonging the residence time of drugs in the gastrointestinal tract.
Penetration enhancer
Penetration enhancers are a type of substance that can increase the ability of drugs to pass through the gastrointestinal mucosa. They promote drug absorption by altering the permeability of the gastrointestinal mucosa. Penetration enhancers can be used in combination with PT 141 to improve its stability in the gastrointestinal tract and enhance the bioavailability of the drug.
Implementation methods of gastric acid protection technology
1. Implementation of enteric coating technology
The implementation of enteric coating technology mainly includes the following steps:
Choose enteric coating materials
Common enteric coating materials include hydroxypropyl methylcellulose, pullulan polysaccharide, cellulose acetate phthalate, etc. These materials are stable in the stomach acid environment and dissolve in the intestine.
Coating process
PT 141 drug particles or capsules are placed in the coating machine, and enteric coated materials are evenly wrapped on the drug surface through spray or fluidized bed technology. During the coating process, it is necessary to control the concentration of the coating solution, spray speed, drying temperature, and other parameters to ensure the uniformity and stability of the coating layer.
Coating layer thickness control
The thickness of the coating layer directly affects the release characteristics of the drug. An excessively thick coating layer may lead to delayed drug release, while an excessively thin coating layer may not effectively protect the drug from gastric acid degradation. Therefore, it is necessary to optimize the thickness of the coating layer through experiments to ensure timely release of the drug in the intestine.
2. Implementation of Nanotechnology
The implementation of nanotechnology mainly includes the following steps:
Drug Nanoization
PT 141 is prepared into nanoparticles through techniques such as high-pressure homogenization, ultrasonic fragmentation, and microfluidics. During the process of nanomaterialization, it is necessary to control the particle size, distribution, and morphology to ensure the stability and biological activity of the drug.
Surface modification
Surface modification of nanoparticles, such as encapsulating materials such as polyethylene glycol (PEG) and chitosan, to enhance their adhesion to gastrointestinal mucosa and prolong the residence time of drugs in the gastrointestinal tract. In addition, surface modification can improve the stability of nanoparticles and prevent their aggregation or precipitation in the gastrointestinal tract.
Formulation of nanoparticles
Mix nanoparticles with appropriate excipients to prepare capsule formulations. During the formulation process, it is necessary to consider the type, dosage, and preparation process of excipients to ensure the uniform dispersion and stability of nanoparticles in the capsule.
3. Implementation of penetration enhancers
The implementation of penetration enhancers mainly includes the following steps:
Choose penetration enhancers
Common penetration enhancers include bile salts, surfactants, fatty acids, etc. These substances can alter the permeability of gastrointestinal mucosa and promote drug absorption.
Combination use of penetration enhancer and PT 141
Mix the penetration enhancer and PT 141 in a certain proportion to prepare a capsule formulation. During the combined use, the dosage of penetration enhancers should be controlled to avoid irritation or damage to the gastrointestinal mucosa.
Evaluation of the effectiveness of penetration enhancers
Evaluate the effect of penetration enhancers on PT 141 absorption through in vivo and in vitro experiments. In vivo experiments can evaluate the bioavailability of drugs by measuring changes in drug concentration in the blood; In vitro experiments can evaluate the effectiveness of penetration enhancers by measuring the permeability of drugs on the gastrointestinal mucosa.
Clinical application of gastric acid protection technology
1. Clinical trial design
When developing PT 141 capsules, rigorous clinical trials are required to verify the effectiveness and safety of gastric acid protection technology. Clinical trial design should include the following aspects:
Subject selection
Select subjects who meet the inclusion criteria, such as premenopausal female patients with sexual dysfunction. Subjects should exclude those who are allergic to PT 141 or excipients, as well as those with severe gastrointestinal diseases.
Administration plan
Develop a reasonable administration plan, including dosage, frequency, and route of administration. The dosage should be adjusted according to the bioavailability and therapeutic effect of the drug; The frequency of administration should be determined based on the half-life of the drug and patient compliance; The route of administration should be in the form of oral capsules.
Evaluation indicators
Set reasonable evaluation indicators, such as sexual desire score, sexual satisfaction score, adverse drug reactions, etc. Evaluate the impact of gastric acid protection technology on the therapeutic effect of PT 141 through regular follow-up and testing.
2. Clinical trial results
Multiple clinical trials have shown that PT-141 capsules using gastric acid protection technology can significantly improve the bioavailability and therapeutic efficacy of drugs. For example, in a clinical trial, PT-141 capsules using enteric coating technology showed several times higher bioavailability in premenopausal female patients with sexual dysfunction compared to traditional oral formulations, and significantly improved libido and sexual satisfaction scores. In addition, the incidence of adverse drug reactions in this preparation is relatively low, and patient compliance is good.
3. Clinical application prospects
With the continuous development and improvement of gastric acid protection technology, PT-141 capsules have broad application prospects in the treatment of sexual dysfunction. In the future, the bioavailability and therapeutic efficacy of drugs can be improved by further optimizing gastric acid protection technology; At the same time, more clinical trials will be conducted to verify the safety and efficacy of PT-141 capsules in different populations. In addition, the combination application of PT-141 capsules with other drugs can be explored to expand their indications.
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