Active ingredient: Insulin Aspart
Chemical name: B28-Asp insulin (human)
Chemical structural formula:
Molecular formula: C256H381N65O79S6
Molecular weight: 5825.8
Excipient: glycerol, phenol, m-cresol, zinc chloride, disodium phosphate dihydrate, sodium chloride, protamine sulfate, hydrochloric acid/sodium hydroxide for pH adjustment and water for injections.
According to literatures, in insulin aspart, substitution of amino acid proline with aspartic acid at position B28 reduces the tendency to form hexamers as observed with soluble human insulin. The insulin aspart in the soluble phase of Raplin 30 comprises 30% of the total insulin; this is absorbed more rapidly from the subcutaneous layer than the soluble insulin component of biphasic human insulin. The remaining 70% is in crystalline from as protamine-crystallised insulin aspart; this has a prolonged absorption profile similar to human NPH insulin.
The maximum serum insulin concentration is, on average, 50% higher with Rapilin 30 than with biphasic human insulin 30. The time to maximum concentration is, on average, half of that for biphasic human insulin 30. In healthy volunteers, a mean maximum serum concentration of 140±32 pmol/L was reached about 60 minutes after a subcutaneous dose of 0.20 unit/kg body weight. The mean half life (t1/2) of Rapilin 30, reflecting the absorption rate of the protamine bound fraction, was about 8-9 hours. Serum insulin levels returned to baseline 15-18 hours after a subcutaneous dose. In type 2 diabetic patients, the maximum concentration was reached about 95 minutes after dosing, and concentrations well above zero for not less than 14 hours post-dosing were measured.
Special populations: the pharmacokinetics of Rapilin 30 have not been investigated in elderly patients or in patients with renal or hepatic impairment.
Paediatric population: the pharmacokinetics of Rapilin 30 have not been investigated in children or adolescents. However, the pharmacokinetic and pharmacodynamic properties of soluble insulin aspart have been investigated in children (6-12 years) and adolescents (13-17 years) with type 1 diabetes. Insulin aspart was rapidly absorbed in both age groups, with similar tmax as in adults. However, Cmax differed between the age groups, stressing the importance of the individual titration of insulin aspart.
The following content is intended to answer your questions only and is not intended to be used for promotional purposes or as a clinical medication guidance.
※ Product Characteristics
● What is the basic information about Rapilin®30?
The generic name of Rapilin®30 is Mixed Protamine Recombinant Human Insulin Aspart Injection (30R). It consists of two active ingredients: 30% insulin aspart and 70% insulin aspart protamine. This medicine is intended for the treatment of people with diabetes and was launched in China in 2021. Insulin Aspart 30 is a bi-phasic insulin formulation for once- to twice-daily injections, depending on the patient's blood glucose levels. This insulin product can be administered just before meals and can also be used immediately after meals if required. As a biosimilar, Rapilin®30 closely matches the approved reference medicine (originator) in terms of quality, safety, and efficacy.
● Will Rapalin®30 cause liver and kidney problems like some oral hypoglycemic drugs?
Rapilin®30 is not associated with liver or kidney problems. The liver and kidneys are involved in the elimination of the body's own insulin. The introduction of exogenous insulin does not place an additional burden on these organs. In cases of liver or kidney dysfunction, the need for insulin may be reduced due to the reduced breakdown of endogenous insulin. Therefore, people using insulin should continue to monitor their blood glucose levels and adjust their dose if necessary.
● Is injecting Rapilin®30 injection addictive? Could higher doses lead to dependence?
Rapilin®30 injection is not associated with addiction or dependence. Addiction is when an individual develops an intense craving for a substance to obtain psychological or physiological effects, leading to uncontrollable and compulsive use. Unlike addictive substances, Rapilin®30 is a form of insulin, a natural hormone that is essential for metabolic processes and the maintenance of life. The use of insulin is determined by factors such as blood glucose control and the functioning of the body's β cells. It is not addictive and its necessity is dictated by medical considerations rather than addictive tendencies.
● What are the precautions for the use of Rapilin®30 in special populations? Are there efficacy and safety data?
Pregnant and breastfeeding women: Use with caution. This product has not been studied in pregnant women (as stated in the prescribing information).
Children: If there is a preference for premixed insulin, this product may be considered for use in children and adolescents over the age of 10. There is limited clinical data in children aged 6-9 years, so it is important to follow your doctor's advice in these cases. It's important to note that studies have not been conducted on children under the age of 6 years (as stated in the prescribing information).
Older people: The elderly population can use this product; however, there is limited experience with its combination with oral hypoglycaemic agents in patients over 75 years of age.
※ Clinicial Study
● How is the hypoglycaemic efficacy and safety of Rapilin®30 compared with the original reference insulin aspart 30?
The study was a multicenter, randomized, open-label, parallel-group Phase III clinical trial, which was conducted by the China-Japan Friendship Hospital. In December 2023, at the International Diabetes Federation (IDF) Virtual Congress 2023, Gan & Lee Pharmaceuticals unveiled the Phase III clinical study data of its self-developed Insulin Aspart 30 Injection (Rapilin®30) for the first time. The results showed that Rapilin®30 is similar in efficacy and safety to the reference product, NovoRapid®30.
The study enrolled 569 patients with type 1 or type 2 diabetes (HbA1c 7.0% < HbA1c ≤ 13.0%, FBG ≥ 7.8 mmol/L) who required insulin therapy. Participants, previously on a stable dose of one or two oral hypoglycemic agents for over three months but still not meeting glycemic targets, were randomly assigned in a 3:1 ratio to receive either Rapilin®30 (N = 428) or NovoRapid®30 (N = 141) twice daily before breakfast and dinner for 24 weeks. The primary objectives of the study were to evaluate HbA1c levels, monitor changes in fasting and postprandial glucose levels, and assess several safety parameters including total insulin dose, changes in body weight, and the occurrence of hypoglycaemic events in both treatment groups. The efficacy was evaluated based on changes in glycated hemoglobin (HbA1c), the percentage of patients achieving target HbA1c levels (<7.0% and ≤6.5%), changes in fasting blood glucose (FBG), and 2-hour postprandial glucose (2hPPG) after 24 weeks of treatment. Safety was compared by analyzing hypoglycemic events and adverse events (including local injection reactions) at 24 weeks.
The results demonstrate that Gan & Lee Pharmaceuticals' Insulin Aspart 30 Injection (Rapilin®30) is equivalent in its therapeutic effect on patients with type 1 and type 2 diabetes to NovoRapid®30, with comparable safety and tolerability profiles during treatment.
Figure 1 Study design and resluts of the study
※ Clinicial Application
● Does Rapilin®️30 require a higher dosage than the original insulin aspart to achieve equivalent efficacy?
Rapilin®️30 showed no significant difference in dose compared with the original insulin aspart. In the Phase 3 clinical trial conducted in China, the average change in daily insulin dose per kilogram of body weight per day at study endpoint for the Rapilin®30 group was statistically indistinguishable (P=0.0887) from the original reference group, while achieving similar glucose control.
● Can Rapilin®30 be used with an insulin pump?
Rapilin®30 cannot be used in insulin pumps.
● What are the advantages of Rapilin®30 over premixed human insulin?
Compared with premixed human insulin, Rapilin®️30 has a higher rate of glycated haemoglobin compliance, a lower risk of hypoglycaemia and better control of postprandial blood glucose. It also has a faster onset of action at mealtime and can be injected with meals, making it flexible and convenient.
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